ME01838B - Pirimidinoni kao inhibitori pi3k - Google Patents

Pirimidinoni kao inhibitori pi3k

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Publication number
ME01838B
ME01838B MEP-2014-93A MEP9314A ME01838B ME 01838 B ME01838 B ME 01838B ME P9314 A MEP9314 A ME P9314A ME 01838 B ME01838 B ME 01838B
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Montenegro
Prior art keywords
nrcrd
alkyl
nrc5rd5
nrcc
nre
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MEP-2014-93A
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Brian W Metcalf
Yun-Long Li
Andrew P Combs
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Lncyte Holdings Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42575792&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME01838(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lncyte Holdings Corp filed Critical Lncyte Holdings Corp
Publication of ME01838B publication Critical patent/ME01838B/me

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Claims (35)

1.Spoj formula IId: ili njegova farmaceutski prihvatljiva sol, naznačen time da: A je aril, heteroaril, cikloalkil, ili heterocikloalkil, svaki po želji supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; gdje je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa , SRa , C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd , NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd ; R1 je NRARB; R2a je H, halo, OH, CN, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil, gdje je spomenuti C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji supstituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa2 SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe)NRc2Rd2, NRc2C(=NRe)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2 , NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, i S(O)2NRc2Rd2; R3 i R4 su nezavisno izabrani iz H, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Ra3, C(O)ORa3, NRc3Rd3, NRc3C(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)2NRc3Rd3, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, gdje je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz C1-6 alkila, C1-6 haloalkila, halo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Ra3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3(O)ORa3, C(=NRe)NRc3Rd3, NRc3C(=NRe)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, i S(O)2NRc3Rd3; RA je heteroaril, heterocikloalkil, heteroarilalkil, ili heterocikloalkilalkil, svaki nezavisno supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od -(C1-4 alkil)r-Cy1, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1 , NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1 ; RB je nezavisno izabran od H, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; Cy1 je aril, heteroaril, cikloalkil, ili heterocikloalkil, svaki po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; Ra, Rb, Rc, i Rd su nezavisno izabrani od H, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; ili Rc i Rd zajedno sa atomom N za koji su prikačeni formiraju 3-, 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu ili heteroaril grupu, svaki po želji supstituirano sa 1, 2, ili 3 substituenta nezavisno izabranih iz C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; Ra1, Rb1, Rc1, i Rd1 su nezavisno izabrani od H, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril , cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil opciono substituisan sa 1, 2, 3, 4, ili 5 substituenta nezavisno izabranih od C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRc5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; ili Rc1 i Rd1 zajedno sa atomom N za koji su prikačeni formiraju 3-, 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu ili heteroaril grupu, svaki po želji substituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od C1-6 alkila, C1-6 haloalkila, halo, CN, OR a5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; Ra2, Rb2, RC2, i Rd2 su nezavisno izabrani iz H, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocicloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilakil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji substituisan sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; ili RC2 i Rd2 zajedno sa atomom N za koji su prikačeni formiraju 3-, 4-, 5-, 6-, ili 7-članu heterocicloalkil grupu ili heteroaril grupu, svaki po želji substituiran sa 1, 2, ili 3 substituenta nezavisno izabranih iz C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; Ra3, Rb3, Rc3, i Rd3 su nezavisno izabrani iz H, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil po želji supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz C1-6 alkil, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; ili Rc3 i Rd3 zajedno sa atomom N za koji su prikačeni formiraju 3-, 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu ili heteroaril grupu, svaki po želji substituiran sa 1, 2, ili 3 substituenta nazavisno izabranih od C1-6 alkila, halo, C1-6 haloalkila, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; Re i Rf su nezavisno izabrani iz H, CN, NO2, ORa5, SRb5, S(O)2Rb5, C(O)Rb5, S(O)2NRC5Rd5, i C(O)NRC5Rd5; Ra5, Rb5, RC5, i Rd5 su nezavisno izabrani iz H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, i heterocikloalkilalkila, pri čemu je spomenuti C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil opciono substituisan sa 1, 2, ili 3 substituenta nezavisno izabranih iz OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksi, C1-6 alkiltia, C1-6 alkilamino, di( C1-6 alkil)amino, C1-6 haloalkil, i C1-6 haloalkoksi; ili RC5 i Rd5 skupa sa atomom N za koji su prikačeni formiraju 3-, 4-, 5-, 6-, ili 7-članu heterocicloalkil grupu ili heteroaril grupu, svaki po želji substituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksi, C1-6 alkiltio, C1-6 alkilamino, di(C1-6 alkil)amino, C1-6 haloalkila, i C1-6 haloalkoksi; i r je 0 ili 1.
2. Spoj iz zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je A (a)cikloalkil ili heterocicloalkil, svaki po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocicloalkila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd,NRcRd , NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril , cikloalkil, heteroaril, ili heterocikloalkil opciono supstituiran sa 1, 2, 3, 4, or 5 substituenata nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, , NRcRd NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS (O)2Rb, NRcS(O)2NRcRd, S(O)Rb, ,S(O) NRcRd S(O)2Rb, i S(O)2NRcRd ; (b)aril ili heteroaril, svaki po želji substituiran sa 1, 2, 3, 4, ili 5 substituenta nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC (O)Rb, (NRcC O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd , S(O)Rb, S(O)NRcRd, S(O)2Rb, and S(O)2NRcRd ; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil opciono substituisan sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC (=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd , S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd ; (c)aril je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa , SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC (O)NRcRd, C(=NReRb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS (O)2Rb, NRcS(O)2NRcRd , S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd ; gdje je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil opciono substituisan sa 1, 2, 3, 4, ili 5 substitenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd , NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC (O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; (d)fenil je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC (O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)RORa , NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, and S(O)2NRcRd; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa , SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd ; (e)fenil je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, ili C1-6 haloalkila; (f)fenil; (g)heteroaril je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa, SRa C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRb )Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS (O)2Rb , NRcS(O)2NRcRd, S(O)Rb, S(O),NRcRd S(O)2Rb, and S(O)2NRcRd; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkila po želji substituiranim sa 1, 2, 3, 4, ili 5 substituienata nezavisno odabranih iz halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS (O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb , i S(O)2NRcRd; (h)6-očlani heteroaril je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkil , CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O), NRcC(O)RbORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanil, CN, NO2, ORa ,SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRb)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb , NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; (i) piridil je po želji supstituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od halo, C1-6 alkila, ili C1-6haloalkila; (k) 5-očlani heteroaril je po želji supstituiran sa 1, 2, ili 3 substituenta koji su nezavisno izabrani od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, arila, cikloalkila, heteroarila, heterocikloalkila, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd , C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb , i S(O)2NRcRd; pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, ili heterocikloalkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa , SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC (=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb , i S(O)2NRcRd; ili je (l)pirazolil po želji substituiran sa 1 ili 2 substituenta koji su nezavisno izabrani od halo, C1-6 alkila, ili C1-6 haloalkila.
3. Spoj prema bilo kojem od zahtjeva 1 do 2, ili njihova farmaceutski prihvatljiva sol, naznačen time da je (a) RA heteroaril po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od -(C1-4 alkil)r-Cy1, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; (b)biciklični heteroaril po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od -(C1-4alkil)r-Cy1, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1 , NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; (c)purinil po želji substituiran sa 1 ili 2 substituenta nezavisno izabrana iz -(C1-4 alkil)r-Cy1, halo, C1-6alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; (d)purinil po želji substituiran sa 1 ili 2 substituenta nezavisno izabrana od C1-6 alkila, C1-6 haloalkila, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, NRC5C(=NRf)NRC5Rd5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5; ili (e)
4.Spoj iz bilo kojeg od zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time da je RB (a)izabran od H ili C1-6 alkila; ili je (b)H.
5.Spoj iz bilo kojeg od zahtjeva 1 do 4, ili njihova farmaceutski prihvatljiva sol naznačen time da je R2a (a)H, halo, OH, CN, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, ili C2-6 alkinil, pri čemu je spomenuti C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, ili je C2-6 alkinil po želji substituiran sa 1, 2, ili 3 substituenta nezavisno izabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRC2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRC2Rd2, C(=NRe)NRC2Rd2, NRC2C(=NRe)NRC2Rd2, NRC2Rd2, NRC2C(O)Rb2, NRC2C(O)ORa2, NRC2C(O)NRC2Rd2, NRC2S(O)Rb2, NRC2S(O)2Rb2, NRC2S(O)2NRC2Rd2, S(O)Rb2, S(O)NRC2Rd2, S(O)2Rb2, i S(O)2NRC2Rd2; (b)halo, OH, CN, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, ili C2-6 alkinil, i gdje je spomenuti C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, ili C2-6 alkinil, po želji supstituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRC2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRC2Rd2, C(=NRe)NRC2Rd2, NRC2C(=NRe)NRC2Rd2, NRC2Rd2 , NRC2C(O)Rb2, NRC2C(O)ORa2, NRC2C(O)NRC2Rd2, NRC2S(O)Rb2, NRC2S(O)2Rb2, NRC2S(O)2NRC2Rd2, S(O)Rb2, S(O)NRC2Rd2, S(O)2Rb2, i S(O)2NRC2Rd2; (c)H, halo, OH, CN, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, ili C2-6 alkinil; ili (d)metil ili etil.
6.Spoj iz bilo kojeg od zahtjeva 1 do 5, ili njihova farmaceutski prihvatljiva sol naznačen time da je R3, (a) halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, NRc3Rd3, NRc3C(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)2NRc3Rd3, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, i heterocikloalkilalkil, pri čemu je spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril , cikloalkil , heteroaril , heterocikloalkil , aril alkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od C1-6 alkila, C1-6 haloalkila, halo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRe)NRc3Rd3, NRc3C(=NRe)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, i S(O)2NRc3Rd3; (b)H, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, ,C(O)ORa3, NRc3Rd3, NRc3C(O)Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, ili C1-6 alkil, gdje je spomenuti C1-6 alkil, po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRe)NRc3Rd3, NRc3C(=NRe)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, i S(O)2NRc3Rd3; (c)H ili C1-6 alkil; (d)C1-6 alkil; ili (c)metil.
7. Spoj iz bilo kojeg od zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time da je R4 (a) izabran od H, halo, C1-6 alkila, ili C1-6 haloalkila; ili je (b) H.
8. Spoj iz bilo kojeg od zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol, sa formulom IIg: naznačen time da su R8 i R9 nezavisno izabrani iz H, C1-6 alkila, C1-6 haloalkila, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRC5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRC5Rd5, NRC5Rd5, NRC5C(O)Rb5, NRC5C(O)NRC5Rd5, NRC5C(O)ORa5, C(=NRf)NRC5Rd5, NRC5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRC5Rd5, S(O)2Rb5, NRC5S(O)2Rb5, NRC5S(O)2NRC5Rd5, i S(O)2NRC5Rd5.
9. Spoj iz patentnog zahtjeva 1, naznačen time da je A aril ili heteroaril, svaki po želji substituiran sa 1, 2, ili 3 substituenta nezavisno izabranih od halo, C1-6 alkila, C1-6 haloalkila, CN, i ORa; R1 je NRARB; R2a je C1-6 alkil; R3 i R4 su nezavisno izabrani iz H, halo, CN, NO2, ORa3, i C1-6 alkila; pri čemu je spomenuti C1-6 alkil po želji supstituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih iz halo; RA je heteroaril, koji je po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo, C1-6 alkila, CN, ORa1, i NRc1Rd1; RB je H; svaki Ra je nezavisno izabran od H i C1-6 alkila; svaki Ra1, Rc1, i Rd1 je nezavisno izabran od H i C1-6 alkila, pri čemu je spomenuti C1-6 alkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo; i svaki Ra3 je nezavisno izabran od H i C1-6 alkila, pri čemu je spomenuti C1-6 alkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo.
10. Spoj iz patentnog zahtjeva 9, ili njegova farmaceutski prihvatljiva sol, naznačen time da je A fenil, 5-člani heteroaril ili 6-člani heteroaril, svaki opciono substituiran sa 1, 2, ili 3 substituenta nezavisno odabranih od halo, C1-6 alkila, C1-6 haloalkila, CN, i ORa; R1 je NRARB; R2a je C1-6 alkil; R3 i R4 su nezavisno izabrani iz H, halo, CN, NO2, ORa3, i C1-6 alkila; gdje je spomenuti C1-6 alkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo; RA je izabran od: RB je H; svaki Ra je nezavisno izabran od H i C1-6 alkila; i svaki Ra3 je nezavisno izabran od H i C1-6 alkila, pri čemu je spomenuti C1-6 alkil po želji substituiran sa 1, 2, 3, 4, ili 5 substituenata nezavisno izabranih od halo.
11. Spoj prema patentnom zahtjevu 1, naznačen time da je (a) izabrano od: 3-metil-6-fenil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-3-metil-6-fenil-5H-[1,3] tiazol[3,2-a]pirimidin-5-on; 6-((3-fluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3-fluorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-((3,5-difluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3,5-difluorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; i 3-metil-7-[1-(9H-purin-6-ilamino)etil]-6-piridin-2-il-5H-[1,3]tiazol[3,2-a]pirimidin-5-on, ili farmaceutski prihvatljiva sol od bilo kojeg od gore navedenih; ili (a)izabrano od: 6-(3,5-difluorofenil)-3-metil-7-[1-(7H-pirolo[2,3-d]pirimidin-4-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3,5-difluorofenil)-7-{1-[(2-fluoro-9H-purin-6-il)amino]etil}-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 3-metil-7-[1-(9H-purin-6-ilamino)etil]-6-piridin-4-il-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 3-metil-7-[1-(9H-purin-6-ilamino)etil]-6-(1,3-thiazol-2-il)-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 3-metil-7-[1-(9H-purin-6-ilamino)etil]-6-(1,3-thiazol-4-il)-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(4-fluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3,5-difluorofenil)-5 H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3,5-difluorofenil)-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3-fluorofenil)-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-fenil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3-fluorofenil)-7-[1-(9H-purin-6-ilamino)etil]-5H-[[1,3]tiazol[3,2-a]pirimidin-5-on; 6-fenil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 3-metil-6-(4-metilfenil)-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3-hlorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(2-fluorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(2,3-difluorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(3-hloro-5-fluorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3-hlorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3-hloro-5-fluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(5-fluoropiridin-3-il)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 7-{1-[(2-amino-9H-purin-6-il)amino]etil}-6-(2-hlorofenil)-3-metil-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(2-fluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(2,3-difluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(5-fluoropiridin-3-il)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(2-hlorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(2,5-difluorofenil)-3-metil-7-[1-(9H-purin-6-ilamino)etil]-5H-[1,3]tiazol[3,2-a]pirimidin-5-on; 6-(3-fluorofenil)-7-[(1S)-1-(3H-imidazo[4,5-b]piridin-7-ilamino)etil]-3-metil-5H-[1,3]tiazol[3,2-o]pirimidin-5-on; 6-(3-fluorofenil)-7-{(1S)-1-[(2-hidroksi-9H-purin-6-il)amino]etil}-3-metil-5H-[1,3]tiazol[3,2-o]pirimidin- 5-on; i 6-(3-fluorofenil)-7-[1-(9H-purin-6-ilamino)etil]-3-(trifluorometil)-5H-[1,3]tiazol[3,2-o]pirimidin-5-on; ili farmaceutski prihvatljiva sol od bilo kojeg od naprijed navedenih.
12. Spoj prema patentnom zahtjevu 1, naznačen time da je 7-(1-(9H-purin-6-ilamino)etil)-6-(3-fluorofenil)-3-metil-5H-tiazol[3,2-a]pirimidin-5-on; ili njegova farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 1, naznačen time da je (S)-7-(1-(9H-purin-6-ilamino)etil)-6-(3-fluorofenil)-3-metil-5H-tiazol[3,2- a]pirimidin-5-on; ili njegova farmaceutski prihvatljiva sol.
14. Pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 13, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedan farmaceutski prihvatljiv nosač.
15.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u inhibiciji aktivnosti PI3K kinaze.
16.Spoj za upotrebu prema zahtjevu 15 naznačen time da je PI3K izabrano od grupe koja se sastoji od PI3Ko, PI3K6, PI3Ky, i PI3K5.
17.Spoj za upotrebu iz zahtjeva 15 naznačen time da je spomenuti spoj selektivni inhibitor za PI3K5, preko jednog ili više od PI3Ko, PI3Kb, i PI3Ky.
18.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana bolesti pacijenata, gdje je bolest povezana sa abnormalnom ekspresijom ili aktivnošću PI3K kinaze.
19.Spoj za upotrebu prema zahtjevu 18 naznačen time da je bolest osteoartritis, restenozis, arteroskleroza, poremećaj kosti, dijebetski retinopatitis, psoriaza, benigno uvećanje prostate, angiogeneza, pankreatitis, bolest bubrega, upalna bolest crijeva, ili multipla-skleroza.
20.Spoj za upotrebu prema zahtjevu 18 naznačen time da je PI3K (a) izabran iz grupe koja se sastoji od PI3Ka, PI3KB, PI3Ky, i PI3K5; ili (b) PI3K5.
21.Spoj za upotrebu prema zahtjevu 18 naznačen time da je u kombinaciji sa inhibitorom kinaze koji inhibira kanazu koja nije PI3K kinaza.
22.Spoj prema bilo kom od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana (a) auto imune bolesti pacijenata; (b) raka; ili (c) bolesti pluća.
23.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana alergije ili astme.
24.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana Sjogrenovog sindroma.
25.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time de je za upotrebu u postupku tretmana miastenije gravis.
26.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana upale.
27.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana artritisa.
28.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana reumatskog artritisa.
29.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana lupusa.
30. Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana glomerulonefritisa.
31.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana raka, pri čemu je spomenuti rak, rak grudi, prostate, debelog crijeva, endometrijalni rak, rak na mozgu, rak mokraćnog mjehura, kože, uterusa, materice, pluća, pankreasa, bubrega, organa za varenje, ili je rak krvi.
32.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u metodu tretmana hematološkog raka, pri čemu je spomenuti hematološki rak akutna mijeloblastična leukemija ili kronična mijeloidna leukemija.
33.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku tretmana limfoma B stanica.
34.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u metodu tretmana difuznog limfoma velikih B stanica.
35.Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmacetski prihvatljiva sol, naznačen time da je za upotrebu u metodu tretmana plućnih bolesti, pri čemu je spomenuta plućna bolest akutna povreda pluća (ALI) ili sindrom respiratornog distresnog poremećaja (ARDS).
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Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2765817A1 (en) * 2009-06-25 2010-12-29 Amgen Inc. 4h-pyrido[1,2-a]pyrimidin-4-one derivatives as pi3k inhibitors
KR101763656B1 (ko) 2009-06-29 2017-08-01 인사이트 홀딩스 코포레이션 Ｐｉ3ｋ 저해물질로서의 피리미디논
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
AU2011337084A1 (en) 2010-12-03 2013-07-11 Allergan, Inc. Novel pyridine derivatives as sphingosine 1-phosphate (S1P) receptor modulators
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
PT3513793T (pt) 2011-09-02 2021-05-10 Incyte Holdings Corp Heterociclilaminas como inibidores de pi3k
EP2790705B1 (en) 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TW201414734A (zh) 2012-07-10 2014-04-16 Takeda Pharmaceutical 氮雜吲哚衍生物
WO2014015523A1 (en) * 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
WO2014072937A1 (en) 2012-11-08 2014-05-15 Rhizen Pharmaceuticals Sa Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor
ES2649156T3 (es) 2013-01-14 2018-01-10 Incyte Holdings Corporation Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim
PE20191245A1 (es) 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
TWI687220B (zh) 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
EA201690458A1 (ru) 2013-08-23 2016-07-29 Инсайт Корпорейшн Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы
WO2015091532A1 (en) * 2013-12-19 2015-06-25 Almirall, S.A. Pyrrolopyrimidine derivatives as pi3k inhibitors
WO2015106012A1 (en) 2014-01-09 2015-07-16 Takeda Pharmaceutical Company Limited Azaindole derivatives
WO2015106014A1 (en) 2014-01-09 2015-07-16 Takeda Pharmaceutical Company Limited Azaindole derivatives
SI3129021T1 (sl) * 2014-04-08 2021-07-30 Incyte Corporation Zdravljenje malignosti B-celic s kombinacijo zaviralcev JAK in PI3K
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2015192761A1 (zh) * 2014-06-17 2015-12-23 辰欣药业股份有限公司 作为mTOR/PI3K抑制剂的吡啶并[1,2-a]嘧啶酮类似物
HK1232227A1 (zh) * 2014-07-04 2018-01-05 Lupin Limited 作为pi3k抑制剂的喹嗪酮衍生物
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
ES2879809T3 (es) 2014-11-01 2021-11-23 Shanghai Fochon Pharmaceutical Co Ltd Ciertos inhibidores de proteínas quinasas
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
WO2016130501A1 (en) 2015-02-09 2016-08-18 Incyte Corporation Aza-heteroaryl compounds as pi3k-gamma inhibitors
SG10201907576SA (en) 2015-02-27 2019-09-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
CN106008479B (zh) * 2015-03-06 2020-01-10 南京圣和药业股份有限公司 作为磷脂酰肌醇3-激酶δ抑制剂的取代嘧啶类化合物及其应用
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US20160362424A1 (en) * 2015-05-11 2016-12-15 Incyte Corporation Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Ｐｉｍ激酶抑制劑之鹽
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
PT3371190T (pt) 2015-11-06 2022-07-08 Incyte Corp Compostos heterocíclicos como inibidores de pi3k-gamma
WO2017101829A1 (zh) * 2015-12-16 2017-06-22 辰欣药业股份有限公司 吡啶并[1,2-a]嘧啶酮类似物的晶型及其制备方法和中间体
WO2017103825A1 (en) 2015-12-18 2017-06-22 Lupin Limited Quinolizinone derivatives as pi3k inhibitors
US20170190689A1 (en) 2016-01-05 2017-07-06 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
KR102483020B1 (ko) 2016-03-28 2023-01-04 인사이트 코포레이션 Tam 저해제로서의 피롤로트리아진 화합물
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
MA50655B1 (fr) 2017-09-27 2021-11-30 Incyte Corp Sels de dérivés de pyrrolotriazine utiles en tant qu'inhibiteurs de tam
KR102717072B1 (ko) 2017-10-18 2024-10-15 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
SG11202011680YA (en) 2018-06-01 2020-12-30 Incyte Corp Dosing regimen for the treatment of pi3k related disorders
AR117600A1 (es) 2018-06-29 2021-08-18 Incyte Corp Formulaciones de un inhibidor de axl / mer
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
CN110078747B (zh) * 2019-04-11 2020-04-10 河南科技大学第一附属医院 一种用于医院消毒的新型噻唑类药物分子及其制备方法
TW202114681A (zh) 2019-07-02 2021-04-16 美商ｅＦＦＥＣＴＯＲ醫療公司 轉譯抑制劑及其用途
CN110721188B (zh) * 2019-11-18 2020-12-18 牡丹江医学院 一种治疗白血病的药物组合物
AU2020391161A1 (en) 2019-11-25 2022-06-09 Amgen Inc. Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use
CN114728167B (zh) 2019-11-25 2024-03-19 安进公司 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法
WO2021178779A1 (en) 2020-03-06 2021-09-10 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
CA3178569A1 (en) * 2020-05-16 2021-11-25 Zuwen ZHOU Compounds as protein kinase inhibitors
EP4032896A1 (en) 2021-01-20 2022-07-27 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Thiazolopyrimidones as inhibitors of ddr1/2 and therapeutic uses thereof
WO2023283345A1 (en) 2021-07-07 2023-01-12 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
GEAP202416555A (en) 2021-12-08 2024-10-28 Incyte Corp Anti-mutant calreticulin (calr) antibodies and uses thereof
WO2024086789A2 (en) * 2022-10-20 2024-04-25 Prelude Therapeutics Incorporated Mutant pi3k-alpha inhibitors and their use as pharmaceuticals
WO2025079605A1 (ja) * 2023-10-11 2025-04-17 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
WO2025096716A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Anti-mutant calreticulin (calr) antibody-drug conjugates and uses thereof

Family Cites Families (289)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3169967A (en) 1957-11-14 1965-02-16 Ciba Geigy Corp Methyl o-lower alkanoyl-reserpates
US3037980A (en) 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
DE1770420U (de) 1958-02-27 1958-07-17 Tara Union G M B H Blumentopf aus kunststoff.
US3506643A (en) 1966-12-09 1970-04-14 Max Thiel N**6-aralkyl-adenosine derivatives
DE2139107A1 (de) 1971-08-04 1973-02-15 Merck Patent Gmbh Heterocyclisch substituierte adenosinverbindungen
US3814251A (en) 1972-08-09 1974-06-04 Sperry Rand Corp Power transmission
US3962443A (en) 1972-08-14 1976-06-08 Dainippon Pharmaceutical Co., Ltd. Antibacterial pharmaceutical compositions and processes for preparation thereof
DE2248232A1 (de) 1972-10-02 1974-04-11 Basf Ag 4-thiopyrimido eckige klammer auf 4,5-d eckige klammer zu pyrimidine
AR204003A1 (es) 1973-04-03 1975-11-12 Dainippon Pharmaceutical Co Procedimiento para preparar compuestos derivados del acido 2-(1-piperazinil)-5-oxopirido-(2,3-d)pirimidino-6-carboxilico y sus sales farmaceuticamente aceptables
US3936454A (en) 1973-08-14 1976-02-03 Warner-Lambert Company 5-Amino-4-chloro-6-(substituted amino)-pyrimidines
US3862189A (en) 1973-08-14 1975-01-21 Warner Lambert Co Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents
DK3375A (me) 1974-01-25 1975-09-15 Ciba Geigy Ag
JPS587626B2 (ja) 1974-02-13 1983-02-10 大日本製薬株式会社 ナフチリジン オヨビ キノリンユウドウタイノセイホウ
JPS50111080U (me) 1974-02-21 1975-09-10
JPS5625234Y2 (me) 1976-01-17 1981-06-15
JPS5359663U (me) 1976-10-25 1978-05-20
JPS5359663A (en) 1976-11-09 1978-05-29 Sumitomo Chem Co Ltd 2-halogeno methyl indole derivatives and process for praparation of the same
JPS52106897A (en) 1977-01-10 1977-09-07 Dainippon Pharmaceut Co Ltd Synthesis of piperazine derivatives
JPS5392767A (en) 1977-01-27 1978-08-15 Sumitomo Chem Co Ltd Preparation of 2-phthalimidomethylindole derivatives
JPS5625234A (en) 1979-08-02 1981-03-11 Hitachi Denshi Ltd Dropout display system
JPS56123981U (me) 1980-02-20 1981-09-21
JPS56123981A (en) 1981-02-23 1981-09-29 Dainippon Pharmaceut Co Ltd Preparation of 1,4-disubstituted piperazine
JPS5883698A (ja) 1981-11-13 1983-05-19 Takeda Chem Ind Ltd キノン化合物およびその製造法
JPS5883698U (ja) 1981-11-27 1983-06-06 石川島播磨重工業株式会社 熱交換器
JPS58162949A (ja) 1982-03-20 1983-09-27 Konishiroku Photo Ind Co Ltd ハロゲン化銀カラ−写真感光材料
JPS60140373U (ja) 1984-02-28 1985-09-17 東洋ハ−ネス株式会社 ワイヤハ−ネスのア−ス構造
JPS6190153A (ja) 1984-10-09 1986-05-08 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料の処理方法
JPS62103640A (ja) 1985-07-18 1987-05-14 Fuji Photo Film Co Ltd ハロゲン化銀カラ−写真感光材料
JPS62103640U (me) 1985-12-18 1987-07-02
JPH07119970B2 (ja) 1986-04-18 1995-12-20 富士写真フイルム株式会社 画像形成方法
JPS6310746A (ja) 1986-07-01 1988-01-18 Tanabe Seiyaku Co Ltd ナフタレン誘導体
CA1324609C (en) 1986-07-30 1993-11-23 Eastman Kodak Company Photographic element and process
US4861701A (en) 1987-10-05 1989-08-29 Eastman Kodak Company Photographic element and process comprising a compound which comprises two timing groups in sequence
AT388372B (de) 1987-10-08 1989-06-12 Tanabe Seiyaku Co Neue naphthalinderivate und sie enthaltende pharmazeutika
JPH01250316A (ja) 1987-12-28 1989-10-05 Tanabe Seiyaku Co Ltd 抗脂血剤
WO1989008113A1 (en) 1988-03-02 1989-09-08 Yoshitomi Pharmaceutical Industries, Ltd. 3,4-DIHYDROTHIENO[2,3-d]PYRIMIDINE COMPOUNDS AND PHARMACEUTICAL APPLICATION THEREOF
US5208250A (en) 1988-05-25 1993-05-04 Warner-Lambert Company Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents
ES2149761T3 (es) 1990-04-25 2000-11-16 Nissan Chemical Ind Ltd Derivado de piridazinona.
SU1712359A1 (ru) 1990-05-07 1992-02-15 Уфимский Нефтяной Институт Гидрохлорид 8 @ -гидроксихинолинового эфира 8-гидроксихинолин-7-карбоновой кислоты, в качестве бактерицида дл подавлени сульфатвосстанавливающих бактерий и культур РSеUDомоNаS и АRтнRовастеR
EP0464612B1 (en) 1990-06-28 1998-05-13 Fuji Photo Film Co., Ltd. Silver halide photographic materials
EP0481614A1 (en) 1990-10-01 1992-04-22 Merck & Co. Inc. Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists
JPH04190232A (ja) 1990-11-26 1992-07-08 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
IL101860A0 (en) 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
JP3108483B2 (ja) 1991-09-30 2000-11-13 日清製粉株式会社 インドール誘導体およびこれを有効成分とする抗潰瘍薬
HUT64064A (en) 1992-02-13 1993-11-29 Chinoin Gyogyszer Es Vegyeszet Process for producing puyrido/1,2-a/pyrimidine derivatives and pharmaceutical compositions comprising same as active ingredient
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
WO1993022291A1 (en) 1992-04-24 1993-11-11 E.I. Du Pont De Nemours And Company Arthropodicidal and fungicidal aminopyrimidines
TW229140B (me) 1992-06-05 1994-09-01 Shell Internat Res Schappej B V
FR2714907B1 (fr) 1994-01-07 1996-03-29 Union Pharma Scient Appl Nouveaux dérivés de l'Adénosine, leurs procédés de préparation, compositions pharmaceutiques les contenant.
US6342501B1 (en) 1994-02-25 2002-01-29 The Regents Of The University Of Michigan Pyrrolo[2,3-d] pyrimidines as antiviral agents
JPH0987282A (ja) 1995-09-21 1997-03-31 Kyowa Hakko Kogyo Co Ltd チアゾール誘導体
JPH09176162A (ja) 1995-12-22 1997-07-08 Toubishi Yakuhin Kogyo Kk チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物
JPH09176116A (ja) 1995-12-27 1997-07-08 Toray Ind Inc 複素環誘導体およびその医薬用途
JPH1025294A (ja) 1996-03-26 1998-01-27 Akira Matsuda 縮合ヘテロ環誘導体、その製造法及びそれを含有する悪性腫瘍治療剤
JP4373497B2 (ja) 1996-06-19 2009-11-25 ローン−プーラン・ロレ・リミテツド 置換されたアザビシクロ化合物、ならびにｔｎｆおよびサイクリックａｍｐホスホジエステラーゼ産生の阻害剤としてのそれらの使用
ES2232871T3 (es) 1996-07-03 2005-06-01 Sumitomo Pharmaceuticals Company, Limited Nuevos derivados de purina.
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
US6630496B1 (en) 1996-08-26 2003-10-07 Genetics Institute Llc Inhibitors of phospholipase enzymes
JPH10231297A (ja) 1997-02-20 1998-09-02 Japan Energy Corp 新規なアデニン−１−ｎ−オキシド誘導体およびその医薬用途
CN1130363C (zh) 1997-11-12 2003-12-10 三菱化学株式会社 嘌呤衍生物以及含有其作为有效成分的药物
TW572758B (en) 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
HUP0100156A3 (en) 1998-02-25 2002-12-28 Genetics Inst Inc Cambridge Indole derivatives as inhibitors of phospholipase a2 and use of them for producing pharmaceutical compositions
EA200000868A1 (ru) 1998-02-25 2001-04-23 Дженетикс Инститьют, Инк. Ингибиторы фосфолипаз
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6479487B1 (en) 1998-02-26 2002-11-12 Aventis Pharmaceuticals Inc. 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
HUP0102563A3 (en) 1998-05-04 2003-04-28 Zentaris Gmbh Indole derivatives and their use in the treatment of malignant and other diseases caused by pathological cell proliferation
ATE482945T1 (de) 1998-05-26 2010-10-15 Chugai Pharmaceutical Co Ltd Heterozyklische indolderivate und mono- oder diazaindol-derivate
JP3997651B2 (ja) 1998-06-24 2007-10-24 コニカミノルタホールディングス株式会社 新規色素及び画像記録材料及び感熱転写材料及びインクジェット記録液
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
EP1109805B1 (en) 1998-08-25 2003-12-17 The Uab Research Foundation Inhibitors of bacterial nad synthetase
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
HK1044334A1 (zh) 1999-02-01 2002-10-18 Cv治疗公司 依赖细胞周期蛋白的激酶2和IκB-α的嘌呤抑制剂
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
JP2000281654A (ja) 1999-03-26 2000-10-10 Tanabe Seiyaku Co Ltd イソキノリン誘導体
DE19932571A1 (de) 1999-07-13 2001-01-18 Clariant Gmbh Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse
JP2001151771A (ja) 1999-09-10 2001-06-05 Kyowa Hakko Kogyo Co Ltd 含窒素芳香族複素環誘導体
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6436965B1 (en) 2000-03-02 2002-08-20 Merck Frosst Canada & Co. PDE IV inhibiting amides, compositions and methods of treatment
EP1138328A1 (en) 2000-03-29 2001-10-04 Eli Lilly And Company Limited Naphthalene derivatives as CNS drugs
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
CN1331340A (zh) 2000-06-30 2002-01-16 上海博德基因开发有限公司 一种新的多肽——人拓扑异构酶12.1和编码这种多肽的多核苷酸
US6960591B2 (en) 2000-07-05 2005-11-01 Yamanouchi Pharmaceutical Co., Ltd. Propane-1,3-dione derivative
FR2814073B1 (fr) 2000-09-21 2005-06-24 Yang Ji Chemical Company Ltd Composition pharmaceutique antifongique et/ou antiparasitaire et nouveaux derives de l'indole a titre de principes actifs d'une telle composition
DOP2002000334A (es) 2001-02-14 2002-08-30 Warner Lambert Co Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
JP3616628B2 (ja) 2001-03-01 2005-02-02 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
UA76977C2 (en) 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
WO2002078700A1 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Pyralopyridines, process for their preparation and use as therapteutic compounds
WO2002078701A1 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Use of pyrazolopyridines as therapeutic compounds
ATE296826T1 (de) 2001-04-27 2005-06-15 Smithkline Beecham Corp Pyrazolo(1,5)pyridinderivate
CZ294535B6 (cs) 2001-08-02 2005-01-12 Ústav Experimentální Botaniky Avčr Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
GB0121033D0 (en) 2001-08-30 2001-10-24 Novartis Ag Organic compounds
US8124625B2 (en) 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
BR0212760A (pt) 2001-09-19 2004-12-07 Aventis Pharma Sa Compostos quìmicos
CN1578781A (zh) 2001-09-26 2005-02-09 拜尔药品公司 用作抗糖尿病药物的1,8－萘啶衍生物
WO2003029209A2 (en) 2001-10-02 2003-04-10 Smithkline Beecham Corporation Chemical compounds
DE60213842T2 (de) 2001-10-30 2007-09-06 Novartis Ag Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung
EP1450844A4 (en) 2001-11-09 2009-07-29 Enzon Inc POLYMER THIOL-LINKED PRODRUGS USING BENZYL ELIMINATION SYSTEMS
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US20050107404A1 (en) 2001-12-06 2005-05-19 Fraley Mark E. Mitotic kinesin inhibitors
CA2467722A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Thienopyrimidinone derivatives as mitotic kinesin inhibitors
TW200301135A (en) 2001-12-27 2003-07-01 Otsuka Maryland Res Inst Inc Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor
WO2003068750A1 (en) 2002-02-13 2003-08-21 Takeda Chemical Industries, Ltd. Jnk inhibitor
US20050049267A1 (en) 2002-03-01 2005-03-03 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
US6933294B2 (en) 2002-04-03 2005-08-23 Bristol-Myers Squibb Company Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same
US20040063658A1 (en) 2002-05-06 2004-04-01 Roberts Christopher Don Nucleoside derivatives for treating hepatitis C virus infection
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
ATE404537T1 (de) 2002-08-13 2008-08-15 Shionogi & Co Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung
JP4190232B2 (ja) 2002-08-26 2008-12-03 富士通株式会社 機械研磨を行う方法
MXPA05003193A (es) 2002-09-27 2005-06-08 Sumitomo Pharma Compuesto de adenina novedoso y uso del mismo.
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
EA013811B1 (ru) 2002-11-21 2010-08-30 Новартис Вэксинес Энд Дайэгностикс, Инк. 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака
JP4544999B2 (ja) 2002-11-25 2010-09-15 持田製薬株式会社 ４−ヒドロキシピペリジン誘導体を有効成分とする呼吸器疾患治療剤
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2512000C (en) 2002-12-26 2011-08-09 Eisai Co., Ltd. Selective estrogen receptor modulator
CZ294538B6 (cs) 2002-12-30 2005-01-12 Ústav Experimentální Botaniky Akademie Vědčeské Re Substituční deriváty N6-benzyladenosinu, způsob jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
RU2233842C1 (ru) 2003-01-13 2004-08-10 Петров Владимир Иванович Производные пурина, обладающие противовирусной активностью
PE20050068A1 (es) 2003-02-06 2005-03-11 Novartis Ag 2-cianopirrolopirimidinas como inhibidores de la catepsina s
GB0304640D0 (en) 2003-02-28 2003-04-02 Novartis Ag Organic compounds
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0300908D0 (sv) 2003-03-31 2003-03-31 Astrazeneca Ab Azaindole derivatives, preparations thereof, uses thereof and compositions containing them
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US20060247245A1 (en) 2003-05-05 2006-11-02 Yuelian Xu Substituted imidazolopyrazine and triazolopyrazine derivatives: gabaa receptor ligands
CN1809563A (zh) * 2003-06-20 2006-07-26 希龙公司 吡啶并[1,2－a]嘧啶－4－酮化合物用作抗癌药
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
JP4570015B2 (ja) 2003-07-14 2010-10-27 クミアイ化学工業株式会社 ２−イソオキサゾリン誘導体及びそれを有効成分として含有する除草剤
MXPA06001758A (es) 2003-08-15 2006-08-11 Irm Llc Anilino purinas sustituidas en la posicion 6 utiles como inhibidores de rtk.
MXPA06002997A (es) 2003-09-18 2007-02-08 Conforma Therapeutics Corp Novedosos compuestos heterociclicos como inhibidores- hsp90.
AU2004289186B2 (en) 2003-09-23 2010-12-16 Merck Sharp & Dohme Corp. Isoquinolinone potassium channel inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
JP2007520559A (ja) 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
WO2005091857A2 (en) 2004-03-12 2005-10-06 Bayer Pharmaceuticals Corporation 1,6-naphthyridine and 1,8-naphthyridine derivatives and their use to treat diabetes and related disorders
CN1560035A (zh) 2004-03-12 2005-01-05 沈阳药科大学 5－羟基吲哚－3－羧酸脂类衍生物
WO2005092892A1 (ja) 2004-03-26 2005-10-06 Dainippon Sumitomo Pharma Co., Ltd. ８−オキソアデニン化合物
AU2005231440B9 (en) 2004-04-02 2012-02-23 Dogwood Pharmaceuticals, Inc. Selective antagonists of A2A adenosine receptors
WO2005113556A1 (en) 2004-05-13 2005-12-01 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
WO2006008523A1 (en) * 2004-07-22 2006-01-26 Astrazeneca Ab Fused pyrimidones usefuel in the treatment and the prevention of cancer
EP1781674A1 (en) * 2004-08-18 2007-05-09 AstraZeneca AB Enantiomers of selected fused pyrimidones and uses in the treatment and prevention of cancer
DE102004044221A1 (de) 2004-09-14 2006-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
EP2275412A1 (en) 2004-10-19 2011-01-19 Novartis Vaccines and Diagnostics, Inc. Indole and benzimidazole derivatives
EP1807417A2 (en) 2004-11-04 2007-07-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
JP2008546843A (ja) 2005-06-27 2008-12-25 アムゲン インコーポレイティッド 抗炎症性アリールニトリル化合物
FR2889192A1 (fr) 2005-07-27 2007-02-02 Cytomics Systems Sa Composes antifongiques, compositions contenant ces composes et leurs utilisations
CA2619881A1 (en) 2005-08-16 2007-02-22 Genzyme Corporation Chemokine receptor binding compounds
US7642270B2 (en) 2005-09-14 2010-01-05 Janssen Pharmaceutica N.V. 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase
JPWO2007034817A1 (ja) 2005-09-22 2009-03-26 大日本住友製薬株式会社 新規アデニン化合物
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
EP1783114A1 (en) 2005-11-03 2007-05-09 Novartis AG N-(hetero)aryl indole derivatives as pesticides
DK1954274T3 (da) 2005-11-10 2011-01-31 Chemocentryx Inc Substituerede quinoloner og fremgangsmåder til anvendelse
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
JP2009524689A (ja) 2006-01-25 2009-07-02 スミスクライン ビーチャム コーポレーション 化合物
UY30118A1 (es) 2006-01-31 2007-06-29 Tanabe Seiyaku Co Compueto amina trisustituido
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007102392A1 (ja) 2006-03-03 2007-09-13 Shionogi & Co., Ltd. Ｍｍｐ－１３選択的阻害剤
US20100273776A1 (en) 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
WO2007114926A2 (en) 2006-04-04 2007-10-11 The Regents Of The University Of California Kinase antagonists
WO2008002490A2 (en) 2006-06-23 2008-01-03 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
US20080004253A1 (en) 2006-06-30 2008-01-03 Bryan James Branstetter Thiazolopyrimidine modulators of TRPV1
US20080009508A1 (en) 2006-07-10 2008-01-10 Lucie Szucova 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin
AU2007272009A1 (en) 2006-07-12 2008-01-17 Syngenta Limited Triazolopyridine derivatives as herbicides
EP2050749B1 (en) 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as pi3k inhibitor and use thereof
BRPI0716239A2 (pt) 2006-08-30 2013-08-13 Cellzome Ltd derivados de triazol como inibidores de cinase
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
EP1972631A1 (en) 2007-03-23 2008-09-24 Novartis AG Imidazopyridazines as PI3K lipid kinase inhibitors
WO2008055013A2 (en) 2006-10-31 2008-05-08 Janssen Pharmaceutica N.V. 5-oxo-5,8 - dihydro - pyrido - pyrimidines as inhibitors of c-fms kinase
KR20090087027A (ko) * 2006-11-13 2009-08-14 일라이 릴리 앤드 캄파니 염증 질환 및 암의 치료를 위한 티에노피리미디논
RS54510B1 (sr) 2006-11-22 2016-06-30 Incyte Holdings Corporation Imidazotriazini i imidazopirimidini kao inhibitori kinaze
CN101631786A (zh) 2006-12-20 2010-01-20 先灵公司 新颖的jnk抑制剂
ATE486877T1 (de) 2006-12-29 2010-11-15 Hoffmann La Roche Azaspiroderivate
AU2008213836A1 (en) 2007-02-05 2008-08-14 Xenon Pharmaceuticals Inc. Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions
MX2009008439A (es) 2007-02-12 2009-08-13 Intermune Inc Nuevos inhibidores de la replicacion del virus de hepatitis c.
AR065784A1 (es) 2007-03-20 2009-07-01 Dainippon Sumitomo Pharma Co Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas.
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
DK2137186T3 (en) 2007-03-23 2016-04-18 Amgen Inc Heterocyclic compounds and their uses
EP2132207A2 (en) * 2007-03-23 2009-12-16 Amgen Inc. Heterocyclic compounds and their uses
US8039505B2 (en) 2007-04-11 2011-10-18 University Of Utah Research Foundation Compounds for modulating T-cells
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
AU2008266856A1 (en) 2007-06-18 2008-12-24 University Of Louisville Research Foundation, Inc. Family of PFKFB3 inhibitors with anti-neoplastic activities
CA2691444C (en) 2007-06-29 2016-06-14 Gilead Sciences, Inc. Purine derivatives and their use as modulators of toll-like receptor 7
WO2009042294A2 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
TW200916447A (en) 2007-08-29 2009-04-16 Methylgene Inc Sirtuin inhibitors
JP2009076865A (ja) 2007-08-29 2009-04-09 Fujifilm Corp 有機電界発光素子
WO2009034386A1 (en) 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
JP2009080233A (ja) 2007-09-26 2009-04-16 Kyocera Mita Corp 電子写真感光体
CZ300774B6 (cs) 2007-10-05 2009-08-05 Univerzita Palackého Substituované 6-(alkylbenzylamino)purinové deriváty pro použití jako antagonisté cytokininových receptoru a prípravky obsahující tyto slouceniny
CA2705303A1 (en) 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
WO2009063235A1 (en) 2007-11-13 2009-05-22 Astrazeneca Ab Derivatives of 1,9-dihydro-6h-purin-6-one and uses thereof-018
JP2009120686A (ja) 2007-11-14 2009-06-04 Toyo Ink Mfg Co Ltd 光重合開始剤、重合性組成物、および重合物の製造方法。
AU2008343813B2 (en) 2007-12-19 2012-04-12 Amgen Inc. Inhibitors of PI3 kinase
EP2231660A1 (en) 2007-12-21 2010-09-29 Wyeth LLC Imidazo [1,2-a] pyridine compounds
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2231641B1 (en) 2007-12-21 2016-06-01 UCB Biopharma SPRL Quinoxaline and quinoline derivatives as kinase inhibitors
PL2228370T3 (pl) 2007-12-28 2012-10-31 Topharman Shanghai Co Ltd N-{1-[3-(2-etoksy-5-(4-etylopiperazynylo)benzenosulfonylo)-4,5-dihydro-5-okso-1,2,4-triazyn-6-yl]etylo}butyroamid, sposób jego wytwarzania i zastosowanie
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP2247596A2 (en) 2008-01-11 2010-11-10 Natco Pharma Limited Novel pyrazolo [3, 4 -d] pyrimidine derivatives as anti -cancer agents
US9089572B2 (en) 2008-01-17 2015-07-28 California Institute Of Technology Inhibitors of p97
US8987280B2 (en) 2008-01-30 2015-03-24 Genentech, Inc. Pyrazolopyrimidine PI3K inhibitor compounds and methods of use
EP2277881A4 (en) 2008-04-18 2011-09-07 Shionogi & Co HETEROCYCLIC COMPOUND HAVING INHIBITORY ACTIVITY ON P13K
US8119647B2 (en) * 2008-04-23 2012-02-21 Glenmark Pharmaceuticals S.A. Fused pyrimidineone compounds as TRPV3 modulators
WO2009140215A2 (en) 2008-05-11 2009-11-19 Geraghty, Erin Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds
US10301265B2 (en) 2008-05-28 2019-05-28 Virginia I. Roxas-Duncan Small molecule inhibitors of botulinum neurotoxins
CA2727174A1 (en) 2008-06-20 2010-01-21 Jiangao Song Aryl gpr119 agonists and uses thereof
US8026271B2 (en) 2008-07-11 2011-09-27 National Health Research Institutes Formulations of indol-3-yl-2-oxoacetamide compounds
WO2010018458A2 (en) 2008-08-12 2010-02-18 Crystalgenomics, Inc. Phenol derivatives and methods of use thereof
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
KR20160091440A (ko) 2008-11-13 2016-08-02 길리아드 칼리스토가 엘엘씨 혈액 종양에 대한 요법
EP2379547A1 (en) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
MX342128B (es) 2008-12-24 2016-09-14 Bial - Portela & C A S A Compuestos farmaceuticos.
WO2010083444A1 (en) 2009-01-15 2010-07-22 Anvyl, Llc Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
EP2396315B1 (en) 2009-02-13 2016-08-31 UCB Biopharma SPRL Quinoline derivatives as pi3k kinase inhibitors
WO2010114900A1 (en) 2009-03-31 2010-10-07 Arqule, Inc. Substituted indolo-piperidine compounds
WO2010118367A2 (en) 2009-04-10 2010-10-14 Progenics Pharmaceuticals, Inc. Antiviral pyrimidines
AP2011005956A0 (en) 2009-04-20 2011-10-31 Gilead Calistoga Llc Methods of treatment for solid tumors.
WO2010127208A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
CA2765817A1 (en) 2009-06-25 2010-12-29 Amgen Inc. 4h-pyrido[1,2-a]pyrimidin-4-one derivatives as pi3k inhibitors
SG176986A1 (en) 2009-06-25 2012-02-28 Amgen Inc Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases
TWI598337B (zh) 2009-06-29 2017-09-11 阿吉歐斯製藥公司 治療化合物及組成物
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
KR101763656B1 (ko) 2009-06-29 2017-08-01 인사이트 홀딩스 코포레이션 Ｐｉ3ｋ 저해물질로서의 피리미디논
CA2768843A1 (en) 2009-07-21 2011-01-27 Gilead Calistoga Llc Treatment of liver disorders with pi3k inhibitors
HRP20130951T1 (hr) 2009-08-28 2013-11-22 Takeda Pharmaceutical Company Limited Spojevi heksahidrooksazinopteridina za uporabu kao inhibitori mtor
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CA2775009A1 (en) 2009-10-20 2011-04-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors
JP5694345B2 (ja) 2009-10-22 2015-04-01 ギリアード サイエンシーズ， インコーポレイテッド Ｔｏｌｌ様受容体の調節因子
NZ599830A (en) 2009-11-05 2014-08-29 Rhizen Pharmaceuticals Sa Novel kinase modulators
EP2947082A1 (en) 2009-11-10 2015-11-25 Pfizer Inc N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS
WO2011058111A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Aminopurine derivatives as kinase inhibitors
EP2499126B1 (en) 2009-11-12 2015-01-07 UCB Pharma, S.A. Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors
CN102812033B (zh) 2009-12-10 2015-11-25 中国医学科学院药物研究所 N6-取代腺苷衍生物和n6-取代腺嘌呤衍生物及其用途
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
MX2012006953A (es) 2009-12-18 2012-10-09 Amgen Inc Compuestos heterociclicos y sus usos.
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
JP2011136925A (ja) 2009-12-28 2011-07-14 Dainippon Sumitomo Pharma Co Ltd 含窒素二環性化合物
RU2547721C2 (ru) 2010-01-07 2015-04-10 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи ТИАЗОЛО [5, 4-d] ПИРИМИДИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ АГРОХИМИЧЕСКИХ СРЕДСТВ
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
CN102802632A (zh) 2010-03-22 2012-11-28 格兰马克药品股份有限公司 含有嘧啶酮衍生物的药物组合物
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
US20110306622A1 (en) 2010-06-11 2011-12-15 Calitoga Pharmaceuticals, Inc. Methods of treating hematological disorders with quinazolinone compounds in selected subjects
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
AU2011271460B2 (en) 2010-07-01 2014-02-06 Amgen Inc. Heterocyclic compounds and their use as inhibitors of P13K activity
US20130085131A1 (en) 2010-07-01 2013-04-04 Amgen Inc. Heterocyclic compounds and their uses
MX2012015134A (es) 2010-07-02 2013-05-06 Amgen Inc Compuestos heterociclicos y su uso como inhibidores de actividad de pi3k.
US20130324561A1 (en) 2010-09-24 2013-12-05 Gilead Calistroga Llc. Atropisomers of p13k-inhibiting compounds
JP2013541591A (ja) 2010-11-04 2013-11-14 アムジエン・インコーポレーテツド 複素環化合物およびそれらの使用
JP2013545749A (ja) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環化合物及びその使用
MX2013005567A (es) 2010-11-17 2013-10-30 Amgen Inc Derivados de quinolina como inhibidores de pik3.
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
WO2012080729A2 (en) 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
MX2013007261A (es) 2010-12-23 2013-11-04 Amgen Inc Compuestos heterociclicos y sus usos.
ES2637113T3 (es) 2011-01-10 2017-10-10 Infinity Pharmaceuticals, Inc. Procedimientos para preparar isoquinolinonas y formas sólidas de isoquinolinonas
AU2012212323A1 (en) 2011-02-01 2013-09-12 The Board Of Trustees Of The University Of Illinois HDAC inhibitors and therapeutic methods using the same
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
HK1198443A1 (en) 2011-07-19 2015-04-24 无限药品股份有限公司 Heterocyclic compounds and uses thereof
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
PT3513793T (pt) 2011-09-02 2021-05-10 Incyte Holdings Corp Heterociclilaminas como inibidores de pi3k
HK1201065A1 (en) 2011-10-04 2015-08-21 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
TWI687220B (zh) 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
HUE033587T2 (hu) 2013-05-17 2017-12-28 Incyte Corp Bipirazol-származékok mint JAK inhibitorok
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
SG10201907576SA (en) 2015-02-27 2019-09-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US20160362424A1 (en) 2015-05-11 2016-12-15 Incyte Corporation Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor

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