EA202191188A1 - Бензамиды производных пиразолил-амино-пиримидинила, композиции на их основе и способы применения - Google Patents

Бензамиды производных пиразолил-амино-пиримидинила, композиции на их основе и способы применения

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Publication number
EA202191188A1
EA202191188A1 EA202191188A EA202191188A EA202191188A1 EA 202191188 A1 EA202191188 A1 EA 202191188A1 EA 202191188 A EA202191188 A EA 202191188A EA 202191188 A EA202191188 A EA 202191188A EA 202191188 A1 EA202191188 A1 EA 202191188A1
Authority
EA
Eurasian Patent Office
Prior art keywords
methods
benzamides
pyrazolyl
amino
compositions
Prior art date
Application number
EA202191188A
Other languages
English (en)
Inventor
Чжаокуй Вань
Майкл Лоуренс Васкес
Сяодун ЛИ
Original Assignee
Линк Фармасьютикалс Ко. Лтд.
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Application filed by Линк Фармасьютикалс Ко. Лтд. filed Critical Линк Фармасьютикалс Ко. Лтд.
Publication of EA202191188A1 publication Critical patent/EA202191188A1/ru

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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
    • A61K31/495—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • C07D401/02—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 two hetero rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Изобретение обеспечивает новый класс перорально и/или местно доступных, селективных и мощных ингибиторов JAK в качестве безопасных и эффективных терапевтических средств против различных заболеваний и расстройств. Изобретение также относится к фармацевтической композиции на основе этих соединений и способам их получения и применения.
EA202191188A 2018-12-14 2019-12-16 Бензамиды производных пиразолил-амино-пиримидинила, композиции на их основе и способы применения EA202191188A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/CN2018/121165 WO2020118683A1 (en) 2018-12-14 2018-12-14 Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof
PCT/CN2019/125552 WO2020119819A1 (en) 2018-12-14 2019-12-16 Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof

Publications (1)

Publication Number Publication Date
EA202191188A1 true EA202191188A1 (ru) 2021-11-29

Family

ID=71076270

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202191188A EA202191188A1 (ru) 2018-12-14 2019-12-16 Бензамиды производных пиразолил-амино-пиримидинила, композиции на их основе и способы применения

Country Status (14)

Country Link
US (5) US20220298144A1 (ru)
EP (1) EP3877381A4 (ru)
JP (1) JP7459094B2 (ru)
KR (1) KR20210125983A (ru)
CN (1) CN113227074A (ru)
AU (3) AU2019399939A1 (ru)
BR (1) BR112021011147A2 (ru)
CA (3) CA3230060A1 (ru)
EA (1) EA202191188A1 (ru)
IL (1) IL283968A (ru)
MX (1) MX2021006866A (ru)
SG (1) SG11202105730TA (ru)
TW (1) TW202039474A (ru)
WO (2) WO2020118683A1 (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110627775A (zh) * 2019-10-24 2019-12-31 嘉兴特科罗生物科技有限公司 一种小分子化合物
TW202204333A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
CN112661655B (zh) * 2020-12-29 2022-02-18 江苏云朴医药新材料科技有限公司 一种1-氨甲基-1-环丙醇类化合物及其合成方法
WO2024041397A1 (en) * 2022-08-22 2024-02-29 Hangzhou Highlightll Pharmaceutical Co., Ltd Jak1/jak2/tyk2 inhibitors for topical treatment of dermatological diseases
CN115572269B (zh) * 2022-10-08 2024-05-17 广州大学 一种n-三氟异丙基唑类和吲哚化合物及其制备方法
WO2023151724A1 (zh) * 2023-05-19 2023-08-17 凌科药业(杭州)有限公司 一种吡唑基-氨基-嘧啶基衍生物的晶型、制备方法及应用
CN116983312A (zh) * 2023-05-24 2023-11-03 凌科药业(杭州)有限公司 一种药物组合物、外用制剂及其制备方法、应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
NZ585139A (en) * 2007-11-16 2012-05-25 Incyte Corp 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as jak inhibitors
EP2638018A1 (en) * 2010-11-09 2013-09-18 Cellzome Limited Pyridine compounds and aza analogues thereof as tyk2 inhibitors
WO2012143320A1 (en) * 2011-04-18 2012-10-26 Cellzome Limited (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors
AU2012288892B2 (en) * 2011-07-28 2016-04-21 Cellzome Limited Heterocyclyl pyrimidine analogues as JAK inhibitors
DE102011112978A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
KR101361149B1 (ko) * 2012-07-17 2014-02-24 전남대학교산학협력단 가뭄 스트레스 저항성 관련 유전자 및 형질전환 식물체
TWI675833B (zh) * 2013-12-11 2019-11-01 美商百健Ｍａ公司 布魯頓氏（ｂｒｕｔｏｎ’ｓ）酪胺酸激酶之聯芳基抑制劑
CN106349224A (zh) * 2016-08-03 2017-01-25 山东大学 一种含有4‑氨基‑(1h)‑吡唑结构的jak激酶抑制剂及其制备方法和应用
CN108864057B (zh) * 2017-05-16 2020-03-31 山东大学 含有4-氨基吡唑结构的jak与hdac双靶点抑制剂及其制备方法和应用
WO2020206588A1 (en) * 2019-04-08 2020-10-15 Lynk Pharmaceuticals Co., Ltd. Benzethers and anilines of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof
CN110330484B (zh) * 2019-07-18 2022-08-26 中国药科大学 取代类苯基嘧啶衍生物作为jak激酶抑制剂或其可药用的盐、制备方法及用途
CN110627775A (zh) * 2019-10-24 2019-12-31 嘉兴特科罗生物科技有限公司 一种小分子化合物

Also Published As

Publication number Publication date
JP2022510925A (ja) 2022-01-28
AU2019399939A1 (en) 2021-06-24
US20240025882A1 (en) 2024-01-25
AU2024201128A1 (en) 2024-03-14
JP7459094B2 (ja) 2024-04-01
CN113227074A (zh) 2021-08-06
MX2021006866A (es) 2021-11-17
SG11202105730TA (en) 2021-06-29
EP3877381A4 (en) 2022-08-24
US20240083881A1 (en) 2024-03-14
CA3230071A1 (en) 2020-06-18
EP3877381A1 (en) 2021-09-15
CA3122872A1 (en) 2020-06-18
US20230002362A1 (en) 2023-01-05
TW202039474A (zh) 2020-11-01
US20230416235A1 (en) 2023-12-28
WO2020118683A1 (en) 2020-06-18
AU2024201125A1 (en) 2024-03-14
US11981663B2 (en) 2024-05-14
IL283968A (en) 2021-07-29
WO2020119819A1 (en) 2020-06-18
CA3230060A1 (en) 2020-06-18
BR112021011147A2 (pt) 2021-08-31
US20220298144A1 (en) 2022-09-22
KR20210125983A (ko) 2021-10-19

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