CN108137603B - 氮杂环丁烷衍生物、其制备方法及用途 - Google Patents

氮杂环丁烷衍生物、其制备方法及用途 Download PDF

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Publication number
CN108137603B
CN108137603B CN201680059396.4A CN201680059396A CN108137603B CN 108137603 B CN108137603 B CN 108137603B CN 201680059396 A CN201680059396 A CN 201680059396A CN 108137603 B CN108137603 B CN 108137603B
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compound
reaction
pyrrolo
methyl
acetonitrile
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CN108137603A (zh
Inventor
谢益农
游泽金
邓智文
朱军
王奥
冯岩
龙冬
曾宏
宋宏梅
叶启军
齐伟
苏东海
王利春
王晶翼
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Sichuan Kelun Botai Biological Pharmaceutical Ltd By Share Ltd
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Sichuan Kelun Botai Biological Pharmaceutical Ltd By Share Ltd
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    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177—Receptors; Cell surface antigens; Cell surface determinants
    • A61K38/1793—Receptors; Cell surface antigens; Cell surface determinants for cytokines; for lymphokines; for interferons

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201680059396.4A 2015-12-11 2016-12-08 氮杂环丁烷衍生物、其制备方法及用途 Active CN108137603B (zh)

Applications Claiming Priority (3)

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CN201510924946 2015-12-11
CN2015109249461 2015-12-11
PCT/CN2016/109036 WO2017097224A1 (zh) 2015-12-11 2016-12-08 氮杂环丁烷衍生物、其制备方法及用途

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CN108137603B true CN108137603B (zh) 2019-10-18

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US (3) US10159662B2 (enExample)
EP (1) EP3360878B9 (enExample)
JP (1) JP6860267B2 (enExample)
CN (1) CN108137603B (enExample)
DK (1) DK3360878T3 (enExample)
ES (1) ES2830446T3 (enExample)
HK (1) HK1250707B (enExample)
WO (1) WO2017097224A1 (enExample)

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AU2018209579B2 (en) * 2017-01-23 2020-12-24 Shanghai Longwood Biopharmaceuticals Co., Ltd. JAK kinase inhibitor and preparation method and use thereof
WO2018223859A1 (zh) * 2017-06-07 2018-12-13 四川科伦博泰生物医药股份有限公司 氮杂环丁烷衍生物的固体形式及其制备方法和用途
US10800775B2 (en) 2017-11-03 2020-10-13 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same
BR112020008850A2 (pt) 2017-11-03 2020-10-20 Aclaris Therapeutics, Inc. composto, composição farmacêutica e método para tratar uma doença mediada por jak1 e jak3
CN109867675B (zh) * 2017-12-01 2021-01-19 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
AR117398A1 (es) * 2018-03-12 2021-08-04 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa 2
CN112823005B (zh) 2018-08-10 2024-08-20 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
CN111518096B (zh) * 2019-02-02 2022-02-11 江苏威凯尔医药科技有限公司 两面神激酶jak家族抑制剂及其制备和应用
CN113508114B (zh) * 2019-02-27 2024-03-26 四川科伦博泰生物医药股份有限公司 以氮杂环丁烷衍生物为活性成分的口服药物组合物、其制备方法及用途
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
BR112021020339A2 (pt) 2019-04-12 2021-12-07 Primegene Beijing Co Ltd Compostos derivados de pirazolopirazina, composição farmacêutica, e uso dos mesmos
KR20220004726A (ko) 2019-05-02 2022-01-11 어클라리스 쎄라퓨틱스, 인코포레이티드 Jak 억제제로서의 치환된 피롤로피리딘
CN110028432A (zh) * 2019-05-22 2019-07-19 南京合巨药业有限公司 一种（3-氨基-氮杂环丁烷-1-基）-环丙基-甲酮的制备方法
JP7592029B2 (ja) * 2019-05-28 2024-11-29 マンカインド ファーマ リミテッド ヤヌスキナーゼ１の阻害のための新規化合物
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202345824A (zh) 2022-03-18 2023-12-01 大陸商四川科倫博泰生物醫藥股份有限公司 氮雜環丁烷衍生物的用途及治療方法
WO2023226822A1 (zh) * 2022-05-26 2023-11-30 四川科伦博泰生物医药股份有限公司 氮杂环丁烷衍生物治疗病毒感染的方法及用途
CN115974864B (zh) * 2022-12-29 2025-09-16 苏州汉德创宏生化科技有限公司 一种2-(3-氮杂环丁基)噻唑盐的合成方法
WO2024148184A1 (en) * 2023-01-04 2024-07-11 Aerie Pharmaceuticals, Inc. Compounds and processes for the preparation of jak inhibitors
EP4653439A1 (en) * 2023-01-18 2025-11-26 Prime Gene Therapeutics Co., Ltd. Azacycloalkane compound and pharmaceutical composition, and use thereof
CN116444529B (zh) * 2023-06-16 2023-12-05 药康众拓(江苏)医药科技有限公司 一种氘代氮杂环丁烷类jak抑制剂及其用途
WO2025264695A1 (en) * 2024-06-20 2025-12-26 Elanco Us Inc. Compositions and methods for treatment

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CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
CN102985417A (zh) * 2010-03-10 2013-03-20 因塞特公司 作为jak1抑制剂的哌啶-4-基氮杂环丁烷衍生物
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CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
WO2010039939A1 (en) * 2008-10-02 2010-04-08 Incyte Corporation Janus kinase inhibitors for treatment of dry eye and other eye related diseases
CN102985417A (zh) * 2010-03-10 2013-03-20 因塞特公司 作为jak1抑制剂的哌啶-4-基氮杂环丁烷衍生物
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HK1250707B (zh) 2020-07-03
US20190060291A1 (en) 2019-02-28
JP6860267B2 (ja) 2021-04-14
US20180289680A1 (en) 2018-10-11
EP3360878A4 (en) 2019-03-06
CN108137603A (zh) 2018-06-08
US20200147062A1 (en) 2020-05-14
US11045455B2 (en) 2021-06-29
DK3360878T3 (da) 2020-11-09
WO2017097224A1 (zh) 2017-06-15
HK1251551A1 (en) 2019-02-01
EP3360878B1 (en) 2020-09-16
EP3360878A1 (en) 2018-08-15
ES2830446T3 (es) 2021-06-03
JP2018536634A (ja) 2018-12-13
US10159662B2 (en) 2018-12-25
EP3360878B9 (en) 2021-05-05

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