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HRP20211965T1 - Novi selektivni inhibitori jak1 i njihova upotreba - Google Patents

Novi selektivni inhibitori jak1 i njihova upotreba Download PDF

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Publication number
HRP20211965T1
HRP20211965T1 HRP20211965TT HRP20211965T HRP20211965T1 HR P20211965 T1 HRP20211965 T1 HR P20211965T1 HR P20211965T T HRP20211965T T HR P20211965TT HR P20211965 T HRP20211965 T HR P20211965T HR P20211965 T1 HRP20211965 T1 HR P20211965T1
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Croatia
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compound
imidazo
nrr
pyridin
pharmaceutically acceptable
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HRP20211965TT
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Congxin Liang
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Highlightll Pharmaceutical (Hainan) Co., Ltd.
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Publication of HRP20211965T1 publication Critical patent/HRP20211965T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)

Claims (23)

1. Spoj s formulom I: [image] ili njegova farmaceutski prihvatljiva sol; ili njegov hidrat, solvat ili polimorf; naznačen time što: R1 je H, halo, ili C1-3 alkil po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine halo, OH, CN, OR, NHR, NRR', N(R)C(=O)R', N(R)C(=O)(O)R', OC(=O)NRR', C(=O)R, C(=O)NRR', N(R)S(O)2R', S(O)2R, i S(O)2NRR'; R2 je H, halo, ili C1-3 alkil; Cy je C3-7 cikloalkil, 3-7 člani heterociklil, fenil, ili 5-6 člani heteroaril, svaki po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine R3, okso, halo, OH, CN, OR, NHR, NRR', N(R)C(=O)R', N(R)C(=O)(O)R', OC(=O)NRR', C(=O)R, C(=O)NRR', N(R)S(O)2R', S(O)2R, i S(O)2NRR', pri čemu R3 je C1-3 alkil po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine halo, OH, CN, OR, NHR, NRR', N(R)C(=O)R', N(R)C(=O)(O)R', OC(=O)NRR', C(=O)R, C(=O)NRR', N(R)S(O)2R', S(O)2R, i S(O)2NRR'; R, R' svaki je neovisno H, ili C1-3 alkil po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine halo, OH, i CN.
2. Spoj s formulom I iz zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što Cy je C5-7 cikloalkil, ili 5-7 člani heterociklil, svaki po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine R3, okso, halo, OH, CN, OR, NHR, NRR', N(R)C(=O)R', N(R)C(=O)(O)R', OC(=O)NRR', C(=O)R, C(=O)NRR', N(R)S(O)2R', S(O)2R, i S(O)2NRR', pri čemu R3 je C1-3 alkil po izboru supstituiran s 1, 2, ili 3 supstituenta neovisno odabrana iz skupine koju čine halo, OH, CN, OR, NHR, NRR', N(R)C(=O)R', N(R)C(=O)(O)R', OC(=O)NRR', C(=O)R, C(=O)NRR', N(R)S(O)2R', S(O)2R, i S(O)2NRR'.
3. Spoj s formulom I iz zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što R2 je vodik.
4. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj odabran iz skupine koju čine: trans-4-[2-[(R)-1-Hidroksietil]-1H-furo[3,2-b]imidazo[4,5-d]piridin-1-il] cikloheksankarbonitril (1), trans-4-[2-(Hidroksimetil)furo[3,2-b]imidazo[4,5-d]piridin-1-il] cikloheksankarbonitril (2), 2-[trans-4-[2-[(R)-1-Hidroksietil]furo[3,2-b]imidazo[4,5-d]piridin-1-il]cikloheksil] acetonitril (3), 2-[(2R,5S)-5-[2-[(R)-1-Hidroksietil]furo[3,2-b]imidazo[4,5-d]piridin-1-il] tetrahidropiran-2-il] acetonitril (4), 3-[2-[(R)-1-Hidroksietil]-1H-furo[3,2-b]imidazo[4,5-d]piridin-1-il]-N-(2,2,2-trifluoroetil)pirolidin-1-karboksamid (5), (R)-4-[2-(1-Hidroksietil)-1H-furo[3,2-b]imidazo[4,5-d]piridin-1-il]-N-(2,2,2-trifluoroetil)piperidin-1-karboksamid (6), 2-[(2R,5S)-5-[2-(Hidroksimetil)furo[3,2-b]imidazo[4,5-d]piridin-1-il]tetrahidropiran-2-il] acetonitril (7), 2-[(2S,5S)-5-[2-(Hidroksimetil)furo[3,2-b]imidazo[4,5-d]piridin-1-il]tetrahidropiran-2-il] acetonitril (8), 2-[(2R,5S)-5-[2-Etilfuro[3,2-b]imidazo[4,5-d]piridin-1-il] tetrahidropiran-2-il]acetonitril (9), 2-[(2R,5S)-5-[2-Furo[3,2-b]imidazo[4,5-d] piridin-1-il] tetrahidropiran-2-il] acetonitril (10), i 2-[(2R,5S)-5-[2-Metilfuro[3,2-b]imidazo[4,5-d] piridin-1-il] tetrahidropiran-2-il]acetonitril (11); ili njihova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj 2-[(2R,5S)-5-[2-[(R)-1-Hidroksietil]furo[3,2-b]imidazo[4,5-d]piridin-1-il] tetrahidropiran-2-il]acetonitril (4), ili njegov hidrat, solvat ili polimorf.
6. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj farmaceutski prihvatljiva sol 2-[(2R,5S)-5-[2-[(R)-1-Hidroksietil]furo[3,2-b]imidazo[4,5-d]piridin-1-il] tetrahidropiran-2-il]acetonitril (4), ili njegov hidrat, solvat ili polimorf.
7. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj 2-[(2R,5S)-5-[2-(Hidroksimetil)furo[3,2-b]imidazo[4,5-d]piridin-1-il]tetrahidropiran-2-il] acetonitril (7), ili njegov hidrat, solvat ili polimorf.
8. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj farmaceutski prihvatljiva sol 2-[(2R,5S)-5-[2-(Hidroksimetil)furo[3,2-b]imidazo[4,5-d]piridin-l-il]tetrahidropiran-2-il] acetonitril (7), ili njegov hidrat, solvat ili polimorf.
9. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj 2-[(2R,5S)-5-[2-Metilfuro[3,2-b]imidazo[4,5-d] piridin-1-il] tetrahidropiran-2-il]acetonitril (11), ili njegov hidrat, solvat ili polimorf.
10. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj farmaceutski prihvatljiva sol 2-[(2R,5S)-5-[2-Metilfuro[3,2-b]imidazo[4,5-d] piridin-1-il] tetrahidropiran-2-il]acetonitril (11), ili njegov hidrat, solvat ili polimorf.
11. Spoj, ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-10, naznačen time što je za uporabu u liječenju bolesti.
12. Pripravak koji sadrži spoj ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od patentnih zahtjeva 1-10, naznačen time što je za uporabu u liječenju bolesti.
13. Spoj, ili njegova farmaceutski prihvatljiva sol, za uporabu prema patentnom zahtjevu 11, naznačen time što je bolest autoimuna bolest ili poremećaj, upalna bolest ili poremećaj, rak ili neoplastična bolest ili poremećaj.
14. Pripravak za uporabu prema patentnom zahtjevu 12, naznačen time što je bolest autoimuna bolest ili poremećaj, upalna bolest ili poremećaj, rak ili neoplastična bolest ili poremećaj.
15. Spoj, ili njegova farmaceutski prihvatljiva sol, ili pripravak za uporabu prema zahtjevu 13 ili zahtjevu 14, naznačen time što je bolest reumatoidni artritis.
16. Spoj s formulom Al-14, ili njegove farmaceutski prihvatljive soli: [image]
17. Postupak za pripravu spoja prema patentnom zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačen time što obuhvaća dovođenje u kontakt spoja s formulom V: [image] i spoja s formulom VI: [image] u prisutnosti (C1-6 alkil)3 oksonij tetrafluoroborata na dovoljnoj temperaturi i tijekom dovoljno vremena za proizvodnju spoja s formulom I: [image] pri čemu R2 je H, i R1 i Cy su kao što je definirano u zahtjevu 1.
18. Postupak prema patentnom zahtjevu 17, naznačen time što je reagens (C1-6 alkil)3 oksonij tetrafluoroborat, trietiloksonij tetrafluoroborat.
19. Postupak prema patentnom zahtjevu 17, naznačen time što se spoj s formulom V pripravlja postupkom koji uključuje redukciju spoja s formulom VII: [image] u prisutnosti katalizatora za hidrogeniranje i plinovitog vodika na dovoljnoj temperaturi, dovoljnom tlaku i dovoljno vremena za proizvodnju spoja s formulom V pri čemu je Cy kao što je definirano u zahtjevu 1.
20. Postupak prema patentnom zahtjevu 19, naznačen time što je katalizator za hidrogeniranje paladij na ugljiku.
21. Postupak prema patentnom zahtjevu 19, naznačen time što se spoj s formulom VII pripravlja postupkom koji obuhvaća dovođenje u kontakt spoja s formulom Al-14: [image] i spoja s formulom VIII: Cy—NH2 VIII u prisutnosti baze na dovoljnoj temperaturi, i tijekom dovoljno vremena za proizvodnju spoja formule VII pri čemu Cy je kao što je definirano u zahtjevu 1; poželjno pri čemu je baza N,N-diizopropiletilamin.
22. Postupak prema bilo kojem od patentnih zahtjeva 17-21, naznačen time što je Cy kao što je definirano u zahtjevu 2.
23. Postupak prema bilo kojem od patentnih zahtjeva 17-21, naznačen time što je spoj s formulom I, ili njegova farmaceutski prihvatljiva sol, kao što je definirano u bilo kojem od zahtjeva 4-10.
HRP20211965TT 2016-10-03 2017-09-30 Novi selektivni inhibitori jak1 i njihova upotreba HRP20211965T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662403660P 2016-10-03 2016-10-03
PCT/US2017/054668 WO2018067422A1 (en) 2016-10-03 2017-09-30 Novel jak1 selective inhibitors and uses thereof
EP17858944.6A EP3509591B1 (en) 2016-10-03 2017-09-30 Novel jak1 selective inhibitors and uses thereof

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HRP20211965T1 true HRP20211965T1 (hr) 2022-03-18

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US (2) US10738060B2 (hr)
EP (1) EP3509591B1 (hr)
JP (1) JP7089141B2 (hr)
KR (1) KR102399848B1 (hr)
CN (2) CN113214278B (hr)
AU (3) AU2017339417C1 (hr)
BR (1) BR112019005969A2 (hr)
CA (1) CA3039178A1 (hr)
DK (1) DK3509591T3 (hr)
EA (1) EA201990523A1 (hr)
ES (1) ES2901216T3 (hr)
HK (1) HK1253040A1 (hr)
HR (1) HRP20211965T1 (hr)
HU (1) HUE058120T2 (hr)
IL (3) IL265358B (hr)
MX (1) MX2019003649A (hr)
NZ (1) NZ751284A (hr)
PL (1) PL3509591T3 (hr)
PT (1) PT3509591T (hr)
RS (1) RS62695B1 (hr)
WO (1) WO2018067422A1 (hr)

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