JP6860267B2 - アゼチジン誘導体、その調製方法、及びその使用 - Google Patents

アゼチジン誘導体、その調製方法、及びその使用 Download PDF

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JP6860267B2
JP6860267B2 JP2018518690A JP2018518690A JP6860267B2 JP 6860267 B2 JP6860267 B2 JP 6860267B2 JP 2018518690 A JP2018518690 A JP 2018518690A JP 2018518690 A JP2018518690 A JP 2018518690A JP 6860267 B2 JP6860267 B2 JP 6860267B2
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reaction
compound
azetidine
mmol
added
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JP2018536634A5 (show.php
JP2018536634A (ja
Inventor
イノン シェ，
イノン シェ，
ゼジン ユウ，
ゼジン ユウ，
ジィウェン デン，
ジィウェン デン，
ジュン ジュウ，
ジュン ジュウ，
アオ ワン，
アオ ワン，
イェン フェン，
イェン フェン，
ドン ロン，
ドン ロン，
フン ツェン，
フン ツェン，
フンメイ ソン，
フンメイ ソン，
チジュン イェ，
チジュン イェ，
ウェイ チィ，
ウェイ チィ，
ドンハイ スー，
ドンハイ スー，
リチュン ワン，
リチュン ワン，
ジンイ ワン，
ジンイ ワン，
Original Assignee
シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド
シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド
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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)
  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
JP2018518690A 2015-12-11 2016-12-08 アゼチジン誘導体、その調製方法、及びその使用 Active JP6860267B2 (ja)

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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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JP2018536634A JP2018536634A (ja) 2018-12-13
JP2018536634A5 JP2018536634A5 (show.php) 2019-12-19
JP6860267B2 true JP6860267B2 (ja) 2021-04-14

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2830446T3 (es) * 2015-12-11 2021-06-03 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Derivado de azetidina, método de preparación del mismo y uso del mismo
KR102485731B1 (ko) 2017-01-23 2023-01-05 상하이 롱우드 바이오파마슈티칼스 컴퍼니 리미티드 Jak 효소 억제제 및 이의 제조 방법과 용도
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
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
CN113149993A (zh) * 2017-12-01 2021-07-23 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
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
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020256720B2 (en) 2019-04-12 2022-09-01 PrimeGene (Beijing) Co. Ltd. Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof
WO2020223728A1 (en) 2019-05-02 2020-11-05 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
WO2020240586A1 (en) * 2019-05-28 2020-12-03 Mankind Pharma Ltd. Novel compounds for inhibition of janus kinase 1
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
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
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
WO2025264695A1 (en) * 2024-06-20 2025-12-26 Elanco Us Inc. Compositions and methods for treatment

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE540948T1 (de) 2005-05-20 2012-01-15 Vertex Pharma Pyrrolopyridine als proteinkinasehemmer
HUE029767T2 (en) * 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
ES2560611T3 (es) * 2011-06-20 2016-02-22 Incyte Holdings Corporation Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
MX392911B (es) 2014-04-08 2025-03-24 Incyte Holdings Corp Tratamiento de neoplasias malignas de linfocitos b mediante una combinacion de inhibidores de janus cinasa (jak) y fosfatidilinositol 3 cinasa (pi3k)
MX373232B (es) 2015-02-27 2020-05-08 Incyte Holdings Corp Sales del inhibidor fosfoinositida 3-cinasa (pi3k) y procesos para su preparación.
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
ES2830446T3 (es) * 2015-12-11 2021-06-03 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Derivado de azetidina, método de preparación del mismo y uso del mismo

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US20180289680A1 (en) 2018-10-11
CN108137603A (zh) 2018-06-08
US20200147062A1 (en) 2020-05-14
EP3360878A1 (en) 2018-08-15
HK1250707B (zh) 2020-07-03
WO2017097224A1 (zh) 2017-06-15
CN108137603B (zh) 2019-10-18
US11045455B2 (en) 2021-06-29
ES2830446T3 (es) 2021-06-03
US20190060291A1 (en) 2019-02-28
HK1251551A1 (en) 2019-02-01
EP3360878A4 (en) 2019-03-06
EP3360878B1 (en) 2020-09-16
US10159662B2 (en) 2018-12-25
JP2018536634A (ja) 2018-12-13
DK3360878T3 (da) 2020-11-09
EP3360878B9 (en) 2021-05-05

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