CN111362975B - 作为jak激酶抑制剂的萘啶化合物 - Google Patents

作为jak激酶抑制剂的萘啶化合物 Download PDF

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CN111362975B
CN111362975B CN202010325911.7A CN202010325911A CN111362975B CN 111362975 B CN111362975 B CN 111362975B CN 202010325911 A CN202010325911 A CN 202010325911A CN 111362975 B CN111362975 B CN 111362975B
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amino
methyl
azabicyclo
compounds
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CN111362975A (zh
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瑞安·赫德森
J·科扎克
保罗·R·法特里
D·D·波德什托
G·E·L·勃兰特
梅丽莎·弗勒里
安妮-玛丽·博索莱伊
黄小军
文卡特·R·萨兰迪
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Theravance Biopharma R&D IP LLC
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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
    • C07D471/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202010325911.7A 2015-05-28 2016-05-26 作为jak激酶抑制剂的萘啶化合物 Active CN111362975B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201562167694P 2015-05-28 2015-05-28
US62/167,694 2015-05-28
US201662312273P 2016-03-23 2016-03-23
US62/312,273 2016-03-23
CN201680029912.9A CN107667108B (zh) 2015-05-28 2016-05-26 作为jak激酶抑制剂的萘啶化合物
PCT/US2016/034243 WO2016191524A1 (en) 2015-05-28 2016-05-26 Naphthyridine compounds as jak kinase inhibitors

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EP3712152B1 (en) 2015-11-03 2021-01-13 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
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AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
PL3959213T3 (pl) 2019-04-24 2024-11-04 Theravance Biopharma R&D Ip, Llc Pirymidynowe inhibitory JAK w leczeniu chorób skóry
JP7470713B2 (ja) 2019-04-24 2024-04-18 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋキナーゼ阻害剤としてのエステルおよびカルボナートピリミジン化合物
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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TW202144366A (zh) * 2020-05-25 2021-12-01 大陸商上海翰森生物醫藥科技有限公司 雜芳類衍生物的鹽、晶型及其製備方法
CN113717202B (zh) * 2020-05-25 2025-10-17 上海翰森生物医药科技有限公司 杂芳类衍生物的自由碱晶型及其制备方法
WO2022076717A1 (en) 2020-10-09 2022-04-14 Janssen Biotech, Inc. Solvate forms of a pan-jak inhibitor
WO2022076714A1 (en) 2020-10-09 2022-04-14 Janssen Biotech, Inc. Solid forms of a pan-jak inhibitor
JP2023545333A (ja) 2020-10-09 2023-10-27 セラバンス・バイオファーマ・アールアンドディー・アイピー・エルエルシー 汎ｊａｋ阻害物質及び関連する中間化合物を調製するプロセス
TW202228689A (zh) * 2020-10-09 2022-08-01 美商賽若凡斯生物製藥研發智財有限責任公司 泛ｊａｋ抑制劑的調配物
US20240158392A1 (en) * 2021-02-01 2024-05-16 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
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WO2022241188A1 (en) 2021-05-14 2022-11-17 Theravance Biopharma R&D Ip, Llc Enantioselective synthesis of aminotropane compound
WO2023011359A1 (zh) * 2021-08-05 2023-02-09 南京明德新药研发有限公司 桥环类化合物及其应用
WO2023102800A1 (en) 2021-12-09 2023-06-15 Theravance Biopharma R&D Ip, Llc Synthesis of 5, 7-dichloro-1, 6-naphthyridine
WO2023202706A1 (zh) * 2022-04-21 2023-10-26 南京明德新药研发有限公司 硒杂环类化合物的盐型和晶型及其应用
JP2025524846A (ja) 2022-07-27 2025-08-01 江蘇恒瑞医薬股▲ふん▼有限公司 縮合環系化合物、その調製方法及びその医薬的使用
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CN107667108B (zh) 2020-05-12
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US9725470B2 (en) 2017-08-08
US20180354974A1 (en) 2018-12-13
DK3303348T3 (da) 2019-11-11
JP2020111593A (ja) 2020-07-27
US10947254B2 (en) 2021-03-16
JP6850922B2 (ja) 2021-03-31
PL3303348T3 (pl) 2020-02-28
IL276677B (en) 2021-05-31
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CA2983453A1 (en) 2016-12-01
MX2017015211A (es) 2018-04-13
US10494382B2 (en) 2019-12-03
IL272057B (en) 2020-09-30
TW201716416A (zh) 2017-05-16
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EA032953B1 (ru) 2019-08-30
AU2020202181B2 (en) 2021-07-01
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US20240132520A1 (en) 2024-04-25
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US11780852B2 (en) 2023-10-10
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MX2020011774A (es) 2021-06-01
JP2021001196A (ja) 2021-01-07
US20200040010A1 (en) 2020-02-06
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IL272057A (en) 2020-02-27
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EP3303348B1 (en) 2019-08-07
RS59522B1 (sr) 2019-12-31

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