HK1250707B - 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
HK1250707B
HK1250707B HK18109969.8A HK18109969A HK1250707B HK 1250707 B HK1250707 B HK 1250707B HK 18109969 A HK18109969 A HK 18109969A HK 1250707 B HK1250707 B HK 1250707B
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HK
Hong Kong
Prior art keywords
compound
reaction
pyrrolo
methyl
mmol
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HK18109969.8A
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English (en)
Chinese (zh)
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HK1250707A1 (en
Inventor
谢益农
謝益農
游泽金
邓智文
游澤金
朱军
王奥
鄧智文
冯岩
龙冬
朱軍
曾宏
宋宏梅
王奧
叶启军
齐伟
馮岩
苏东海
王利春
龍冬
王晶翼
葉启軍
齊偉
蘇東海
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四川科伦博泰生物医药股份有限公司
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Publication of HK1250707A1 publication Critical patent/HK1250707A1/xx
Publication of HK1250707B publication Critical patent/HK1250707B/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic 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
    • A61K31/343Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177Receptors; Cell surface antigens; Cell surface determinants
    • A61K38/1793Receptors; 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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (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)
HK18109969.8A 2015-12-11 2016-12-08 氮杂环丁烷衍生物、其制备方法及用途 HK1250707B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510924946.1 2015-12-11
CN201510924946 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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HK1250707A1 HK1250707A1 (en) 2019-01-11
HK1250707B true HK1250707B (zh) 2020-07-03

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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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CA3055233C (en) * 2017-01-23 2022-08-09 Shanghai Longwood Biopharmaceuticals Co., Ltd. Jak kinase inhibitor and preparation method and use thereof
EP3636647B1 (en) * 2017-06-07 2023-01-11 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Solid form of azetidine derivative and preparation method therefor and use thereof
WO2019090143A1 (en) 2017-11-03 2019-05-09 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrimidine-5-carboxylate analogs and methods of making the same
AU2018360059B2 (en) 2017-11-03 2023-07-13 Aclaris Therapeutics, Inc. Substituted pyrrolopyrimidine JAK inhibitors and methods of making and using the same
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
JP6557436B1 (ja) * 2018-03-12 2019-08-07 アッヴィ・インコーポレイテッド チロシンキナーゼ2媒介性シグナル伝達の阻害剤
AU2019317625B2 (en) 2018-08-10 2025-02-27 Aclaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
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
WO2020173364A1 (zh) * 2019-02-27 2020-09-03 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
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
CN113924301B (zh) 2019-04-12 2024-08-16 北京普祺医药科技股份有限公司 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途
US11420966B2 (en) 2019-05-02 2022-08-23 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as JAK inhibitors
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
MX2021014361A (es) * 2019-05-28 2022-04-06 Mankind Pharma Ltd Nuevos compuestos para la inhibición de janus quinasa 1.
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) 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
EP4495118A1 (en) 2022-03-18 2025-01-22 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Use and treatment method of azetidine derivative
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
WO2024153147A1 (zh) * 2023-01-18 2024-07-25 北京普祺医药科技股份有限公司 一种氮杂环烷烃化合物、药物组合物及其用途
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

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EP3360878A4 (en) 2019-03-06
JP6860267B2 (ja) 2021-04-14
CN108137603B (zh) 2019-10-18
EP3360878A1 (en) 2018-08-15
US11045455B2 (en) 2021-06-29
WO2017097224A1 (zh) 2017-06-15
HK1251551A1 (en) 2019-02-01
US20200147062A1 (en) 2020-05-14
JP2018536634A (ja) 2018-12-13
US20190060291A1 (en) 2019-02-28
ES2830446T3 (es) 2021-06-03
EP3360878B1 (en) 2020-09-16
US10159662B2 (en) 2018-12-25
US20180289680A1 (en) 2018-10-11
CN108137603A (zh) 2018-06-08
DK3360878T3 (da) 2020-11-09
EP3360878B9 (en) 2021-05-05

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