ME03801B - Supstituisan imidazo-hinolini kao nlrp3 modulatori - Google Patents

Supstituisan imidazo-hinolini kao nlrp3 modulatori

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Publication number
ME03801B
ME03801B MEP-2020-149A MEP2020149A ME03801B ME 03801 B ME03801 B ME 03801B ME P2020149 A MEP2020149 A ME P2020149A ME 03801 B ME03801 B ME 03801B
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Montenegro
Prior art keywords
cancer
optionally substituted
compound
independently selected
pharmaceutically acceptable
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MEP-2020-149A
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German (de)
English (en)
French (fr)
Inventor
Gary Glick
Shomir Ghosh
William R Roush
Edward James Olhava
Daniel O'malley
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Innate Tumor Immunity Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=61283434&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME03801(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Innate Tumor Immunity Inc filed Critical Innate Tumor Immunity Inc
Publication of ME03801B publication Critical patent/ME03801B/me

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Optical Communication System (AREA)
  • Adhesives Or Adhesive Processes (AREA)
  • Transducers For Ultrasonic Waves (AREA)

Claims (22)

1.Jedinjenje koje ima formulu (II): ili njegova farmaceutski prihvatljiva so, pri čemu:R1 je nezavisno nesupstituisan C1-6 alkil, ili C(=O)Ra;R2 je nezavisno Hili nesupstituisan C1-6 alkil;R3 je: (i) H; (ii) nesupstituisan C1-2 alkil; (iii) X-R8, pri čemu X je nerazgranat C1-6 alkilen, a R8 je -OH, C1-4 alkoksi, -C1-4 haloalkoksi, CO2Ra, ili -CONRcRd; (iv) (C1-3 alkilen)-(C6-C10 aril), pri čemu aril je po izboru supstituisan sa od 1-3 supstituenta nezavisno odabrana od C1-6 alkila, C1-4 haloalkila, C1-4 alkoksi, i C1-4 haloalkoksi; ili (v) (C1-3 alkilen)heteroaril koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S, i pri čemu heteroaril je po izboru supstituisan sa od 1 do 3 supstituenta nezavisno odabrana od C1-6 alkila, C1-4 haloalkila, C1-4 alkoksi, i C1-4 haloalkoksi;R4 i R5 su svaki nezavisno odabrani od: (i) H; (ii) halo; (iii) -(C0-3 alkilen)-C3-10 cikloalkila, pri čemu cikloalkil je po izboru supstituisan sa od 1 do 4 nezavisno odabrana Rf; (iv) -(C0-3 alkilen)-heterociklila koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N(Re), O, i S, pri čemu heterociklil je po izboru supstituisan sa od 1 do 4 Rf; (v) -(C0-3 alkilen)-(C6-C10 arila) po izboru supstituisanog sa od 1 do 4 Rg; (vi) -(C0-3 alkilen)-heteroarila koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri čemu heteroaril je po izboru supstituisan sa od 1 do 3 Rg; (vii) C1-6 alkila po izboru supstituisanog sa od 1-2 nezavisno odabrana Rh; i (viii) -(C0-3 alkilen)-C4-10 cikloalkenila, pri čemu cikloalkenil je po izboru supstituisan sa od 1 do 2 Rf;Ra je: (i) C1-6 alkil po izboru supstituisan sa od 1 do 2 Rh; ili (ii) -(C0-3 alkilen)-C3-10 cikloalkil, pri čemu cikloalkil je po izboru supstituisan sa od 1 do 2 Rf; (iii) -(C1-3 alkilen)-heterociklil koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od N(Re), O, i S, pri čemu heterociklil je po izboru supstituisan sa od 1 do 4 nezavisno odabrana Rf; (iv) -(C0-3 alkilen)-fenil po izboru supstituisan sa od 1 do 4 nezavisno odabrana Rg; ili (v) -(C0-3 alkilen)-heteroaril koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S, pri čemu heteroaril je po izboru supstituisan sa od 1 do 3 nezavisno odabrana Rg;pri svakom pojavljivanju Rc i Rd je nezavisno H ili C1-4 alkil;pri svakom pojavljivanju Re je nezavisno H ili C1-4 alkil;pri svakom pojavljivanju Rf je nezavisno C1-6 alkil, C1-4 haloalkil, -OH, F, Cl, C1-4 alkoksi, C1-4 haloalkoksi, cijano, ili fenil po izboru supstituisan sa od 1 do 4 Rg;pri svakom pojavljivanju Rg je nezavisno halo, cijano, C1-6 alkil, C1-4 haloalkil, C1-4 alkoksi, ili C1-4 haloalkoksi; ipri svakom pojavljivanju Rh je nezavisno -OH, F, C1-4 alkoksi, C1-4 haloalkoksi, ili cijano.
2.Jedinjenje prema patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so, pri čemu: R3 je H, nesupstituisan C1-2 alkil, ili X-R8, pri čemu X je nerazgranat C2-6alkilen, i R8 je CO2Ra ili -CONRcRd; R4 je nezavisno H ili halo; R5 je nezavisno odabran od: (i) H; (ii) halo; (iii) -(C0-3 alkilen)-C3-10 cikloalkila, pri čemu cikloalkil je po izboru supstituisan sa od 1 do 4 nezavisno odabrana Rf; (iv) -(C0-3 alkilen)-heterociklila koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N(Re), O, i S, pri čemu heterociklil je po izboru supstituisan sa od 1 do 4 Rf; (v) -(C0-3 alkilen)-(C6-C10 arila) po izboru supstituisanog sa od 1 do 4 Rg; (vi) -(C0-3 alkilen)-heteroarila koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri Čemu heteroaril je po izboru supstituisan sa od 1 do 3 Rg; (vii) C1-6alkila po izboru supstituisanog sa od 1-2 nezavisno odabrana Rh; i (viii) -(C0-3 alkilen)-C4-10 cikloalkenila, pri čemu cikloalkenil je po izboru supstituisan sa od 1 do 2 Rf.
3.Jedinjenje prema bilo kom od patentnih zahteva 1-2, ili njegova farmaceutski prihvatljiva so, pri čemu: R2 je nezavisno H ili nesupstituisan C1-3alkil; R3 je H, nesupstituisan C1-2 alkil, ili X-R8, pri čemu X je nerazgranat C2-4 alkilen, aR8 je CO2R8 ili -CONRcRd; R5 je nezavisno odabran od: (i) C3-6 cikloalkila po izboru supstituisanog sa od 1 do 2 nezavisno odabrana Rf; (ii) fenila po izboru supstituisanog sa od 1 do 3 Rg; (iii) heteroarila koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri čemu heteroaril je po izboru supstituisan sa od 1 do 3 Rg; (iv) C1-6 a1kila po izboru supstituisanog sa od 1 do 2 nezavisno odabrana Rh; i (v) C5-6 cik1oalkenila po izboru supstituisanog sa od 1 do 2 Rf; iRa je H, C1-4 alkil po izboru supstituisan sa OH, C3-6 cikloalkil, fenil, ili heteroaril koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S.
4. Jedinjenje prema bilo kom od patentnih zahteva 1-3, pri čemu: R2 je nezavisno H, CH3 ili CH2CH3; R3 je H, CH3, iLi -(CH2)3C(=O)OCH3; R5 je nezavisno CH3, ciklopentil, ciklopentenil, fenil, pirazol-1-il, iii pirazol-3-il; i Ra je H, CH3, CH2CH3, CH(CH3)2, C(CH3)3, ciklopropil, ili tiazolil.
5. Jedinjenje prema bilo kom od patentnih zahteva 1-4, ili njegova farmaceutski prihvatljiva so, pri čemu: R2 je nezavisno H, CH3 ili CH2CH3; R3 je H ili CH3; R5 je nezavisno CH3, ciklopentil, ciklopentenil, fenil, pirazol-1-il, ili pirazol-3-il; i Ra je CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili ciklopropil.
6. Jedinjenje prema bilo kom od patentnih zahteva 1-5, ili njegova farmaceutski prihvatljiva so, pri čemu: R1je nezavisno CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili C(=O)Ra; R2 je nezavisno H, CH3 ili CH2CH3; R3je H; R5 je nezavisno ciklopentil, ciklopentenil, fenil, pirazol-1-il, ili pirazol-3-il; i Ra je CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili ciklopropil.
7. Jedinjenje prema patentnom zahtevu 1, pri cemu jedinjenje jeiii njegova farmaceutski prihvatljiva so.
8. Jedinjenje prema patentnom zahtevu 1, pri čemu jedinjenje je
9. Jedinjenje prema patentnom zahtevu 1, pri čemu jedinjenje je ili njegova farmaceutski prihvatljiva so.
10. Jedinjenje prema patentnom zahtevu 1, pri čemu jedinjenje je
11. Farmaceutska kompozicija koja sadrži jedinjenje ili njegovu farmaceutski prihvatljivu so prema bilo kom od patentnih zahteva 1 do 10 i jedan ili više farmaceutski prihvatljivih ekscipijenasa.
12. Jedinjenje ili njegova farmaceutski prihvatljiva so u skladu sa bilo kojim od patentnih zahteva 1 do 10, ili farmaceutska kompozicija u skladu sa patentnim zahtevom 11, za primenu kao lek.
13. Jedinjenje ili njegova farmaceutski prihvatljiva so u skladu sa bilo kojim od patentnih zahteva 1 do 10, ili farmaceutska kompozicija u skladu sa patentnim zahtevom 11, za primenu u lečenju kancera kod subjekta.
14. Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema patentnom zahtevu 13, pri čemu kancer je odabran od akutne mijeloidne leukemija, adrenokortikalnog karcinoma, Kapoši sarkoma, limfoma, analnog kancera, kancera apendiksa, teratoidnoglrabdoidnog tumora, karcinoma bazalnih ćelija, kancera žučnih puteva, kancera bešike, kancera kostiju, kancera mozga, kancera dojke, tumora bronhija, karcinoidnog tumora, kardijaenog tumora, kancera grlica materice, hordoma, hronične limfocitne leukemije, hronične mijeloproliferativne neoplazme, kancera kolona, kolorektalnog kancera, kraniofaringioma, endometrijalnog kancera, ependimoma, kancera jednjaka, estezioneuroblastoma, Evingovog sindroma, kancera oka, kancera falopijevih tuba, kancera fucne kese, gastrointestinalnog karcinoidnog tumora, gastrointestinalnog stromalnog tumora, tumora germinativnih ćelija, leukemije vlastastih celija, kancera glave i vrata, kancera srca, kancera jetre, hipofaringealnog kancera, kancera pankreasa, kancera bubrega, laringealnog kancera, hronične mijeloicne leukemije, kancera usne i usne šupljine, kancera pluća, melanoma, karcinoma Merkelovih ćelije, mezotelioma, kancera usta, oralnog kancera, osteosarkoma, kancera jajnika, kancera penisa, faringealnog kancera, kancera prostate, rektalnog kancera, kancera pljuvaenih flezda, kancera kofe, kancera tankog creva, sarkoma mekog tkiva, kancera testisa, kancera grla, kancera stitne flezde, kancera uretre, kancera maternice, kancera vagine, i kancera vulve.
15. Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema patentnom zahtevu 13 ili patentnom zahtevu 14, pri čemu kancer je refraktorni kancer.
16. Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema patentnom zahtevu 13, pri čemu kancer je odabran od kancera dojke, kancera kolona, rektalnog kancera, kolorektalnog kancera, kancera pankreasa, i kancera prostate.
17.Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema bilo kom od patentnih zahteva 13-16, pri čemu jedinjenje ili kompozicija se administrira u kombinaciji sa jednom ili više dodatnih terapija protiv kancera.
18. Jedinjenje, njegova farmaceutski prihvatljiva so iii kompozicija za primenu prema patentnom zahtevu 17, pri čemu jedna ili više dodatnih terapija protiv kancera sadžii hirurgiju, radioterapiju hemoterapiju, terapiju toksinima, imunoterapiju, krioterapiju iii gensku terapiju, ili kombinacijuistih.
19. Jedinjenje, njegova farmaceutski prihvatljiva so iii kompozicija za primenu prema patentnom zahtevu 17, pri čemu dodatna terapija protiv kancera sadrži jedan ili više agenasa odabrana od cisplatina, karboplatina, mehloretamina, ciklofosfamida, hlorambucila, ifosfamida, oksaliplatina, azatioprina, merkaptopurina, vinkristina, vinblastina, vinorelbina, vindesina, takso1a, paklitaksela, docetaksela, irinotekana,, amsakrina, etopozida, etopozid fosfata, tenipozida, aktinomicina, antraciklina, doksorubicina, daunorubicina, valrubicina, idarubicina, epirubicina, bleomicina, plikamicina, mitomicina, leuprolidina, goserelina, triptorelina, histrelina, bikalutamida, flutamida, nilutamida, abciksimaba, adalimumaba, alemtuzumaba, atlizumaba, baziliksimaba, belimumaba, bevacizumaba, brentuksimab vedotina, kanakinumaba, cetuksimaba, certolizumab pegola, daklizumaba, denozumaba, ekulizumaba, efalizumaba, gemtuzumaba, golimumaba, ibritumomab tiuksetana, infliksimaba, ipilimumaba, muromonab-CD3, natalizumaba, ofatumumaba, omalizumaba, palivizumaba, panitumumaba, ranibizumaba, rituksimaba, tocilizumaba, tozitumomaba, trastuzumaba, interleukina-2, indolamin 2,3- dioksigenaze, IL-10, transformi uceg faktora rasta-ß, CD39, CD73 adenozin-CD39-CD73, i CXCR4-CXCL12.
20.Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema patentnom zahtevu 17, pri čemu dodatna terapija protiv kancera sadrži jedan ili više agenasa odabrana od urelumaba, PF-05082566, MEDI6469, TRX518, varlilumaba, CP-870893, pembrolizumaba, nivolumaba, atezolizumaba, MEDI4736, avelumaba, PDR001, BMS-986016, MGA271, lirilumaba, IPH2201, emaktuzumaba, INCB024360, galunisertiba, ulokuplumaba, BKT140, bavituksimaba, CC-90002, bevacizumaba, i MNRP1685A.
21.Jedinjenje, njegova farmaceutski prihvatljiva so iii kompozicija za primenu prema patentnom zahtevu 17, pri čemu dodatna terapija protiv kancera sadrfi jedan ili više agenasa odabrana od nivolumaba, ipilimumaba, pembrolizumaba, atezolizumaba, i avelumaba.
22.Jedinjenje, njegova farmaceutski prihvatljiva so ili kompozicija za primenu prema bilo kom od patentnih zahteva 12-20 pri temujedinjenje se administrira intratumoralno ili sistemski.
MEP-2020-149A 2017-02-17 2018-02-16 Supstituisan imidazo-hinolini kao nlrp3 modulatori ME03801B (me)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762460677P 2017-02-17 2017-02-17
US201762490881P 2017-04-27 2017-04-27
US201762573991P 2017-10-18 2017-10-18
PCT/US2018/018484 WO2018152396A1 (en) 2017-02-17 2018-02-16 Substituted imidazo-quinolines as nlrp3 modulators
EP18707612.0A EP3510034B1 (en) 2017-02-17 2018-02-16 Substituted imidazo-quinolines as nlrp3 modulators

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