JP2016512558A5 - - Google Patents

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Publication number: JP2016512558A5
Authority: JP; Japan
Prior art keywords: butoxy; tert; acetic acid; alkyl; pyridin
Prior art date: 2014-03-13
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Pending

Application number

JP2016501870A

Other languages

English (en)

Japanese (ja)

Other versions

JP2016512558A (ja

Filing date

2014-03-13

Publication date

2017-03-09

2014-03-13 Application filed filed Critical

2014-03-13 Priority claimed from PCT/US2014/025525 external-priority patent/WO2014159959A1/en

2016-04-28 Publication of JP2016512558A publication Critical patent/JP2016512558A/ja

2017-03-09 Publication of JP2016512558A5 publication Critical patent/JP2016512558A5/ja

Status Pending legal-status Critical Current

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QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 54
125000000217 alkyl group Chemical group 0.000 claims 35
-1 homopiperidinyl Chemical group 0.000 claims 30
125000001475 halogen functional group Chemical group 0.000 claims 20
125000001188 haloalkyl group Chemical group 0.000 claims 18
125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 18
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
125000001424 substituent group Chemical group 0.000 claims 16
125000003545 alkoxy group Chemical group 0.000 claims 13
150000001875 compounds Chemical class 0.000 claims 12
125000004438 haloalkoxy group Chemical group 0.000 claims 12
125000003342 alkenyl group Chemical group 0.000 claims 10
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
125000003302 alkenyloxy group Chemical group 0.000 claims 9
125000000753 cycloalkyl group Chemical group 0.000 claims 9
229910052739 hydrogen Inorganic materials 0.000 claims 9
239000001257 hydrogen Substances 0.000 claims 9
239000003112 inhibitor Substances 0.000 claims 7
125000003386 piperidinyl group Chemical group 0.000 claims 7
125000004183 alkoxy alkyl group Chemical group 0.000 claims 6
125000004093 cyano group Chemical group *C#N 0.000 claims 6
125000002541 furyl group Chemical group 0.000 claims 6
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
125000002883 imidazolyl group Chemical group 0.000 claims 6
125000001786 isothiazolyl group Chemical group 0.000 claims 6
125000000842 isoxazolyl group Chemical group 0.000 claims 6
125000001715 oxadiazolyl group Chemical group 0.000 claims 6
125000002971 oxazolyl group Chemical group 0.000 claims 6
125000003226 pyrazolyl group Chemical group 0.000 claims 6
125000000168 pyrrolyl group Chemical group 0.000 claims 6
125000001113 thiadiazolyl group Chemical group 0.000 claims 6
125000000335 thiazolyl group Chemical group 0.000 claims 6
125000001544 thienyl group Chemical group 0.000 claims 6
125000001425 triazolyl group Chemical group 0.000 claims 6
125000002393 azetidinyl group Chemical group 0.000 claims 5
125000002757 morpholinyl group Chemical group 0.000 claims 5
125000004193 piperazinyl group Chemical group 0.000 claims 5
125000000719 pyrrolidinyl group Chemical group 0.000 claims 5
150000003839 salts Chemical class 0.000 claims 5
208000031886 HIV Infections Diseases 0.000 claims 4
108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 4
208000037357 HIV infectious disease Diseases 0.000 claims 4
125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 4
125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 4
208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 4
125000001041 indolyl group Chemical group 0.000 claims 4
239000002777 nucleoside Substances 0.000 claims 4
150000003833 nucleoside derivatives Chemical class 0.000 claims 4
239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 4
125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
239000003795 chemical substances by application Substances 0.000 claims 3
125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 3
125000000392 cycloalkenyl group Chemical group 0.000 claims 3
125000004076 pyridyl group Chemical group 0.000 claims 3
208000030507 AIDS Diseases 0.000 claims 2
102100035875 C-C chemokine receptor type 5 Human genes 0.000 claims 2
101710149870 C-C chemokine receptor type 5 Proteins 0.000 claims 2
102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims 2
229940099797 HIV integrase inhibitor Drugs 0.000 claims 2
229940122440 HIV protease inhibitor Drugs 0.000 claims 2
101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims 2
125000004450 alkenylene group Chemical group 0.000 claims 2
125000002947 alkylene group Chemical group 0.000 claims 2
230000034303 cell budding Effects 0.000 claims 2
239000003937 drug carrier Substances 0.000 claims 2
239000002835 hiv fusion inhibitor Substances 0.000 claims 2
239000003084 hiv integrase inhibitor Substances 0.000 claims 2
239000004030 hiv protease inhibitor Substances 0.000 claims 2
230000035800 maturation Effects 0.000 claims 2
239000000203 mixture Substances 0.000 claims 2
239000008194 pharmaceutical composition Substances 0.000 claims 2
IXEPTGRMARFENT-HKBQPEDESA-N (2S)-2-[2-[(4-fluoro-3-methylphenyl)methylcarbamoyl]-6-methyl-4-(2-oxa-8-azatricyclo[7.3.1.05,13]trideca-1(13),5,7,9,11-pentaen-10-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C(F)C(C)=CC(CNC(=O)C2=NN3C=C(C)C([C@H](OC(C)(C)C)C(O)=O)=C(C=4C=5N=CC=C6CCOC(C=56)=CC=4)C3=C2)=C1 IXEPTGRMARFENT-HKBQPEDESA-N 0.000 claims 1
GXHHOTNIDWJTAS-XIFFEERXSA-N (2S)-2-[2-[4-[(4-fluorophenyl)methyl]pyrazol-1-yl]-6-methyl-4-(2-oxa-8-azatricyclo[7.3.1.05,13]trideca-1(13),5,7,9,11-pentaen-10-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C=4N=CC=C5CCOC(C=45)=CC=3)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1N(N=C1)C=C1CC1=CC=C(F)C=C1 GXHHOTNIDWJTAS-XIFFEERXSA-N 0.000 claims 1
WAOBEXMKRVBRQA-YTTGMZPUSA-N (2S)-2-[2-[5-[(4-fluorophenyl)methyl]-1,3-oxazol-2-yl]-6-methyl-4-(2-oxa-8-azatricyclo[7.3.1.05,13]trideca-1(13),5,7,9,11-pentaen-10-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C=4N=CC=C5CCOC(C=45)=CC=3)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(O1)=NC=C1CC1=CC=C(F)C=C1 WAOBEXMKRVBRQA-YTTGMZPUSA-N 0.000 claims 1
SRRAXFGSMNTMDJ-YTTGMZPUSA-N (2S)-2-[2-[5-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-6-methyl-4-(2-oxa-8-azatricyclo[7.3.1.05,13]trideca-1(13),5,7,9,11-pentaen-10-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C=4N=CC=C5CCOC(C=45)=CC=3)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(S1)=NC=C1CC1=CC=C(F)C=C1 SRRAXFGSMNTMDJ-YTTGMZPUSA-N 0.000 claims 1
WLFXWNMWPYJDJD-PMERELPUSA-N (2S)-2-[4-(8-fluoro-5-methyl-3,4-dihydro-2H-chromen-6-yl)-2-[(4-fluoro-3-methylphenyl)methylcarbamoyl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound Cc1cc(CNC(=O)c2cc3c(-c4cc(F)c5OCCCc5c4C)c([C@H](OC(C)(C)C)C(O)=O)c(C)cn3n2)ccc1F WLFXWNMWPYJDJD-PMERELPUSA-N 0.000 claims 1
JAORABFFBCNCEO-SANMLTNESA-N (2s)-2-[10-(8-fluoro-5-methyl-3,4-dihydro-2h-chromen-6-yl)-8-methylpyrido[1,2-b]indazol-9-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound O1CCCC2=C(C)C(C=3C4=C5C=CC=CC5=NN4C=C(C=3[C@H](OC(C)(C)C)C(O)=O)C)=CC(F)=C21 JAORABFFBCNCEO-SANMLTNESA-N 0.000 claims 1
ULHWBJXCIRQVCU-SANMLTNESA-N (2s)-2-[2-(3-bromophenyl)-6-methyl-4-(4-methyl-4-prop-2-enoxypiperidin-1-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC(C)(C)O[C@H](C(O)=O)C=1C(C)=CN2N=C(C=3C=C(Br)C=CC=3)C=C2C=1N1CCC(C)(OCC=C)CC1 ULHWBJXCIRQVCU-SANMLTNESA-N 0.000 claims 1
WRFUXBIIMNVOGZ-SNFDCCKOSA-N (2s)-2-[2-[3-[2-fluoro-3-methyl-6-[(2s)-pentan-2-yl]oxyphenyl]phenyl]-6-methyl-4-(4-methyl-4-propoxypiperidin-1-yl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1CC(OCCC)(C)CCN1C1=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2C1=CC(C=1C=C(C=CC=1)C=1C(=CC=C(C)C=1F)O[C@@H](C)CCC)=N2 WRFUXBIIMNVOGZ-SNFDCCKOSA-N 0.000 claims 1
SLZYXZFOBJKSSS-SANMLTNESA-N (2s)-2-[4-(4,4-dimethylpiperidin-1-yl)-2-[(4-fluoro-3-methylphenyl)methylcarbamoyl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C(F)C(C)=CC(CNC(=O)C2=NN3C=C(C)C([C@H](OC(C)(C)C)C(O)=O)=C(N4CCC(C)(C)CC4)C3=C2)=C1 SLZYXZFOBJKSSS-SANMLTNESA-N 0.000 claims 1
CBDSJKSTELMHIB-NDEPHWFRSA-N (2s)-2-[4-(4,4-dimethylpiperidin-1-yl)-2-[4-[(4-fluorophenyl)methyl]pyrazol-1-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC(C)(C)O[C@H](C(O)=O)C=1C(C)=CN2N=C(N3N=CC(CC=4C=CC(F)=CC=4)=C3)C=C2C=1N1CCC(C)(C)CC1 CBDSJKSTELMHIB-NDEPHWFRSA-N 0.000 claims 1
NVXPQGHMBBOOKZ-MHZLTWQESA-N (2s)-2-[4-(4,4-dimethylpiperidin-1-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-oxazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC(C)(C)O[C@H](C(O)=O)C=1C(C)=CN2N=C(C=3OC(CC=4C=CC(F)=CC=4)=CN=3)C=C2C=1N1CCC(C)(C)CC1 NVXPQGHMBBOOKZ-MHZLTWQESA-N 0.000 claims 1
KPPZTAGBWZZHPW-MHZLTWQESA-N (2s)-2-[4-(4,4-dimethylpiperidin-1-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC(C)(C)O[C@H](C(O)=O)C=1C(C)=CN2N=C(C=3SC(CC=4C=CC(F)=CC=4)=CN=3)C=C2C=1N1CCC(C)(C)CC1 KPPZTAGBWZZHPW-MHZLTWQESA-N 0.000 claims 1
IMMDGLXLSLMURK-LJAQVGFWSA-N (2s)-2-[4-(4,4-dimethylpiperidin-1-yl)-6-methyl-2-(3-pyridin-3-ylphenyl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC(C)(C)O[C@H](C(O)=O)C=1C(C)=CN2N=C(C=3C=C(C=CC=3)C=3C=NC=CC=3)C=C2C=1N1CCC(C)(C)CC1 IMMDGLXLSLMURK-LJAQVGFWSA-N 0.000 claims 1
SVDHERPQDVBDEQ-NDEPHWFRSA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-2-[(4-fluoro-3-methylphenyl)methylcarbamoyl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C(F)C(C)=CC(CNC(=O)C2=NN3C=C(C)C([C@H](OC(C)(C)C)C(O)=O)=C(C=4C(=C5NCCOC5=CC=4)Cl)C3=C2)=C1 SVDHERPQDVBDEQ-NDEPHWFRSA-N 0.000 claims 1
YDLOXOOSLPJIAD-PMERELPUSA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-2-[4-[(4-fluorophenyl)methyl]pyrazol-1-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4NCCOC4=CC=3)Cl)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1N(N=C1)C=C1CC1=CC=C(F)C=C1 YDLOXOOSLPJIAD-PMERELPUSA-N 0.000 claims 1
WWVITSNUKPEINU-LJAQVGFWSA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-oxazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4NCCOC4=CC=3)Cl)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(O1)=NC=C1CC1=CC=C(F)C=C1 WWVITSNUKPEINU-LJAQVGFWSA-N 0.000 claims 1
WCCOFXGPMUKLIR-LJAQVGFWSA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4NCCOC4=CC=3)Cl)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(S1)=NC=C1CC1=CC=C(F)C=C1 WCCOFXGPMUKLIR-LJAQVGFWSA-N 0.000 claims 1
BKIBDBSJHHXSKA-HKBQPEDESA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-6-methyl-2-(3-pyridin-3-ylphenyl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4NCCOC4=CC=3)Cl)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(C=1)=CC=CC=1C1=CC=CN=C1 BKIBDBSJHHXSKA-HKBQPEDESA-N 0.000 claims 1
NVJFHRRQLBAVPZ-XIFFEERXSA-N (2s)-2-[4-(5-chloro-3,4-dihydro-2h-1,4-benzoxazin-6-yl)-6-methyl-2-[3-(2-methylphenyl)phenyl]pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC1=CC=CC=C1C1=CC=CC(C2=NN3C=C(C)C([C@H](OC(C)(C)C)C(O)=O)=C(C=4C(=C5NCCOC5=CC=4)Cl)C3=C2)=C1 NVJFHRRQLBAVPZ-XIFFEERXSA-N 0.000 claims 1
FGHYDWDTGCEFGN-HKBQPEDESA-N (2s)-2-[4-(8-fluoro-5-methyl-3,4-dihydro-2h-chromen-6-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-oxazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4CCCOC4=C(F)C=3)C)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(O1)=NC=C1CC1=CC=C(F)C=C1 FGHYDWDTGCEFGN-HKBQPEDESA-N 0.000 claims 1
YKGGXUFXZCSKHI-HKBQPEDESA-N (2s)-2-[4-(8-fluoro-5-methyl-3,4-dihydro-2h-chromen-6-yl)-2-[5-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-6-methylpyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4CCCOC4=C(F)C=3)C)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(S1)=NC=C1CC1=CC=C(F)C=C1 YKGGXUFXZCSKHI-HKBQPEDESA-N 0.000 claims 1
DZVRFPSOOQHJFK-XIFFEERXSA-N (2s)-2-[4-(8-fluoro-5-methyl-3,4-dihydro-2h-chromen-6-yl)-6-methyl-2-(3-pyridin-3-ylphenyl)pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound C1=C2C(C=3C(=C4CCCOC4=C(F)C=3)C)=C([C@H](OC(C)(C)C)C(O)=O)C(C)=CN2N=C1C(C=1)=CC=CC=1C1=CC=CN=C1 DZVRFPSOOQHJFK-XIFFEERXSA-N 0.000 claims 1
QETAKGCWTITPHK-DHUJRADRSA-N (2s)-2-[4-(8-fluoro-5-methyl-3,4-dihydro-2h-chromen-6-yl)-6-methyl-2-[3-(2-methylphenyl)phenyl]pyrazolo[1,5-a]pyridin-5-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid Chemical compound CC1=CC=CC=C1C1=CC=CC(C2=NN3C=C(C)C([C@H](OC(C)(C)C)C(O)=O)=C(C=4C(=C5CCCOC5=C(F)C=4)C)C3=C2)=C1 QETAKGCWTITPHK-DHUJRADRSA-N 0.000 claims 1
ALLIZEAXNXSFGD-UHFFFAOYSA-N 1-methyl-2-phenylbenzene Chemical compound CC1=CC=CC=C1C1=CC=CC=C1 ALLIZEAXNXSFGD-UHFFFAOYSA-N 0.000 claims 1
230000005764 inhibitory process Effects 0.000 claims 1
230000001225 therapeutic effect Effects 0.000 claims 1
238000002560 therapeutic procedure Methods 0.000 claims 1

JP2016501870A 2013-03-14 2014-03-13 ヒト免疫不全ウイルス複製の阻害剤 Pending JP2016512558A (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201361781764P	2013-03-14	2013-03-14
US61/781,764		2013-03-14
PCT/US2014/025525 WO2014159959A1 (en)	2013-03-14	2014-03-13	Inhibitors of human immunodeficiency virus replication

Publications (2)

Publication Number	Publication Date
JP2016512558A JP2016512558A (ja)	2016-04-28
JP2016512558A5 true JP2016512558A5 (2)	2017-03-09

Family

ID=50842317

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2016501870A Pending JP2016512558A (ja)	2013-03-14	2014-03-13	ヒト免疫不全ウイルス複製の阻害剤

Country Status (6)

Country	Link
US (1)	US9527842B2 (2)
EP (1)	EP2970274B1 (2)
JP (1)	JP2016512558A (2)
CN (1)	CN105189503B (2)
ES (1)	ES2623904T3 (2)
WO (1)	WO2014159959A1 (2)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP3105236B1 (en)	2014-02-12	2017-10-18	ViiV Healthcare UK (No.5) Limited	Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication
PT3107913T (pt)	2014-02-19	2018-09-28	Viiv Healthcare Uk No 5 Ltd	Inibidores da replicação do vírus da imunodeficiência humana
US9193720B2 (en)	2014-02-20	2015-11-24	Bristol-Myers Squibb Company	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US9975906B2 (en)	2014-05-16	2018-05-22	Shionogi & Co., Ltd.	Tricyclic heterocycle derivatives having HIV replication inhibitory effect
TWI700284B (zh)	2015-05-29	2020-08-01	日商塩野義製藥股份有限公司	具有ｈｉｖ複製抑制作用之含氮３環性衍生物
US20180170903A1 (en)	2015-07-06	2018-06-21	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
RU2018102554A (ru)	2015-07-08	2019-08-08	ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД	Производные пиридин-3-ил уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека
RU2018103031A (ru)	2015-07-09	2019-08-09	ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД	Производные пиридин-3-ил уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека
US20180170904A1 (en)	2015-07-09	2018-06-21	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
KR20180035910A (ko)	2015-08-07	2018-04-06	비브 헬스케어 유케이 (넘버5) 리미티드	인간 면역결핍 바이러스 복제의 억제제로서 피리딘-3-일 아세트산 유도체
WO2017025913A1 (en)	2015-08-10	2017-02-16	VIIV Healthcare UK (No.5) Limited	Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
TWI657086B (zh)	2015-08-11	2019-04-21	英商Viiv醫療保健英國(No.5)有限公司	做為人類免疫缺陷病毒複製抑制劑之５－（ｎ－苯甲基四氫異喹啉－６－基）吡啶－３－基乙酸衍生物
CN108137553A (zh)	2015-08-12	2018-06-08	Viiv保健英国第五有限公司	作为人免疫缺陷病毒复制的抑制剂的5-(n-[6,5]-稠合双环芳基四氢异喹啉-6-基)吡啶-3-基乙酸衍生物
US10214516B2 (en)	2015-08-12	2019-02-26	VIIV Healthcare UK (No.5) Limited	5-(N-fused tricyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201718537A (zh)	2015-08-12	2017-06-01	Ｖｉｉｖ醫療保健英國（Ｎｏ．５）有限公司	做為人類免疫缺陷病毒複製抑制劑之吡啶－３－基乙酸衍生物
KR20180038047A (ko)	2015-08-20	2018-04-13	비브 헬스케어 유케이 (넘버5) 리미티드	인간 면역결핍 바이러스 복제의 억제제로서 피리딘-3-일 아세트산 유도체
WO2017070089A1 (en)	2015-10-19	2017-04-27	Incyte Corporation	Heterocyclic compounds as immunomodulators
SG10202004618TA (en)	2015-11-19	2020-06-29	Incyte Corp	Heterocyclic compounds as immunomodulators
MA44075A (fr)	2015-12-17	2021-05-19	Incyte Corp	Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
AU2016379372A1 (en)	2015-12-22	2018-08-02	Incyte Corporation	Heterocyclic compounds as immunomodulators
AR108396A1 (es)	2016-05-06	2018-08-15	Incyte Corp	Compuestos heterocíclicos como inmunomoduladores
JP2019515000A (ja)	2016-05-11	2019-06-06	ヴィーブヘルスケアユーケー（ナンバー５）リミテッド	ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−３−イル酢酸誘導体
US20190152957A1 (en)	2016-05-11	2019-05-23	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US10407410B2 (en)	2016-05-11	2019-09-10	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2017205464A1 (en)	2016-05-26	2017-11-30	Incyte Corporation	Heterocyclic compounds as immunomodulators
HUE060256T2 (hu)	2016-06-20	2023-02-28	Incyte Corp	Heterociklusos vegyületek mint immunmodulátorok
EP3484866B1 (en)	2016-07-14	2022-09-07	Incyte Corporation	Heterocyclic compounds as immunomodulators
WO2018044783A1 (en)	2016-08-29	2018-03-08	Incyte Corporation	Heterocyclic compounds as immunomodulators
ES2874756T3 (es)	2016-12-22	2021-11-05	Incyte Corp	Derivados de triazolo[1,5-A]piridina como inmunomoduladores
LT3558990T (lt)	2016-12-22	2022-12-27	Incyte Corporation	Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
US20180179202A1 (en)	2016-12-22	2018-06-28	Incyte Corporation	Heterocyclic compounds as immunomodulators
JP7101678B2 (ja)	2016-12-22	2022-07-15	インサイト・コーポレイション	免疫調節剤としての複素環式化合物
WO2018119221A1 (en)	2016-12-22	2018-06-28	Incyte Corporation	Pyridine derivatives as immunomodulators
EP3565810A1 (en)	2017-01-03	2019-11-13	ViiV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201835068A (zh)	2017-01-03	2018-10-01	英商Viiv醫療保健英國(No.5)有限公司	作為人類免疫缺乏病毒複製之抑制劑之吡啶-3-基乙酸衍生物
US11779637B2 (en)	2017-04-24	2023-10-10	Nantcell, Inc.	Targeted neoepitope vectors and methods therefor
SMT202500157T1 (it)	2018-03-30	2025-05-12	Incyte Corp	Composti eterociclici come immunomodulatori
HUE061503T2 (hu)	2018-05-11	2023-07-28	Incyte Corp	Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
WO2019244066A2 (en)	2018-06-19	2019-12-26	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2020003093A1 (en)	2018-06-25	2020-01-02	VIIV Healthcare UK (No.5) Limited	Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
JP7665593B2 (ja)	2019-08-09	2025-04-21	インサイト・コーポレイション	Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
PE20221038A1 (es)	2019-09-30	2022-06-17	Incyte Corp	Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
CA3160131A1 (en)	2019-11-11	2021-05-20	Incyte Corporation	Salts and crystalline forms of a pd-1/pd-l1 inhibitor
TW202233615A (zh)	2020-11-06	2022-09-01	美商英塞特公司	Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
WO2022099018A1 (en)	2020-11-06	2022-05-12	Incyte Corporation	Process of preparing a pd-1/pd-l1 inhibitor
CR20230230A (es)	2020-11-06	2023-07-27	Incyte Corp	Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7939545B2 (en)	2006-05-16	2011-05-10	Boehringer Ingelheim International Gmbh	Inhibitors of human immunodeficiency virus replication
ES2402322T3 (es)	2007-11-15	2013-04-30	Gilead Sciences, Inc.	Inhibidores de la replicación del virus de la inmunodeficiencia humana
ATE541841T1 (de)	2007-11-15	2012-02-15	Boehringer Ingelheim Int	Inhibitoren der replikation des human immunodeficiency virus
ES2463720T3 (es)	2007-11-16	2014-05-29	Gilead Sciences, Inc.	Inhibidores de la replicación del virus de inmunodeficiencia humana
EA019259B1 (ru)	2007-11-16	2014-02-28	Джилид Сайенсиз, Инк.	Ингибиторы репликации вируса иммунодефицита человека
EP2215298B1 (en)	2007-11-23	2014-03-26	Koninklijke Philips N.V.	Compartment
US8338441B2 (en) *	2009-05-15	2012-12-25	Gilead Sciences, Inc.	Inhibitors of human immunodeficiency virus replication
GB0908394D0 (en)	2009-05-15	2009-06-24	Univ Leuven Kath	Novel viral replication inhibitors
GB0913636D0 (en)	2009-08-05	2009-09-16	Univ Leuven Kath	Novel viral replication inhibitors
SG181423A1 (en)	2009-12-23	2012-07-30	Univ Leuven Kath	Novel antiviral compounds
MX2012015097A (es)	2010-07-02	2013-05-28	Gilead Sciences Inc	Derivados de acido naft-2-ilacetico para tratar sida.
EP2588455B1 (en)	2010-07-02	2018-04-04	Gilead Sciences, Inc.	2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
US8633200B2 (en) *	2010-09-08	2014-01-21	Bristol-Myers Squibb Company	Inhibitors of human immunodeficiency virus replication
KR20140003438A (ko)	2010-11-15	2014-01-09	카톨리에케 유니버시테이트 루벤	항바이러스성 축합 헤테로사이클릭 화합물
EP2640729B1 (en)	2010-11-15	2016-12-21	VIIV Healthcare UK Limited	Inhibitors of hiv replication
US8791108B2 (en) *	2011-08-18	2014-07-29	Bristol-Myers Squibb Company	Inhibitors of human immunodeficiency virus replication

2014
- 2014-03-13 JP JP2016501870A patent/JP2016512558A/ja active Pending
- 2014-03-13 CN CN201480027109.2A patent/CN105189503B/zh not_active Expired - Fee Related
- 2014-03-13 ES ES14727271.0T patent/ES2623904T3/es active Active
- 2014-03-13 US US14/773,223 patent/US9527842B2/en not_active Expired - Fee Related
- 2014-03-13 EP EP14727271.0A patent/EP2970274B1/en not_active Not-in-force
- 2014-03-13 WO PCT/US2014/025525 patent/WO2014159959A1/en not_active Ceased

Publication	Publication Date	Title
JP2016512558A5 (2)	2017-03-09
JP2016512507A5 (2)	2017-04-13
JP2016512511A5 (2)	2017-04-13
RU2420284C2 (ru)	2011-06-10	Антагонист ccr5 для усиления иммуновосстановительной терапии и лечения оппортунистической инфекции у пациентов с вич
HRP20191821T1 (hr)	2019-12-27	Antiproliferativni spojevi i načini njihove uporabe
JP2016512825A5 (2)	2017-04-13
JP2016516692A5 (2)	2017-04-13
JP2017526748A5 (2)	2018-07-05
JP2019501133A5 (2)	2019-11-14
JP2016528301A5 (2)	2017-09-28
JP2016538313A5 (2)	2017-10-26
NO20075682L (no)	2008-01-07	Sammensetninger omfattende et oralt aktivt 1,2,4-oksadiazol for nonsense mutasjonsundertrykkelsesterapi
JP2007519649A5 (2)	2008-02-28
JP2017528494A (ja)	2017-09-28	ｓＧＣ刺激剤
JP2016535795A5 (2)	2017-12-21
RU2017107715A (ru)	2018-09-27	Производные имидазо[1,2-a]пиридина для применения в качестве ингибиторов репликации вируса иммунодефицита человека
RU2015120216A (ru)	2017-01-10	Ингибиторы тирозинкиназы брутона
JP2016506961A5 (2)	2017-03-02
JP2015524841A5 (2)	2016-09-15
HRP20200836T1 (hr)	2020-08-07	Liječenje bolesti povezanih s imunitetom i upalnih bolesti
JP2011513475A5 (2)	2012-03-22
NO20091826L (no)	2009-07-08	Fremgangsmater for dosering av oralt aktive 1,2,4-oksadiazol for nonsense mutasjonsuppresjonsterapi
JP2014532754A5 (2)	2015-12-03
IL257240A (en)	2018-03-29	History of 5– (n– benzyl tetrahydroisoquinoline – 6 – il) Pyridine – 3 – il Acetic acid as inhibitors of human immunodeficiency virus replication
RU2016142611A (ru)	2018-05-03	Пролекарственные средства ингибиторов обратной транскриптазы вич