CN115087651B - 作为激酶抑制剂的吲唑甲酰胺 - Google Patents

作为激酶抑制剂的吲唑甲酰胺 Download PDF

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Publication number
CN115087651B
CN115087651B CN202080069790.2A CN202080069790A CN115087651B CN 115087651 B CN115087651 B CN 115087651B CN 202080069790 A CN202080069790 A CN 202080069790A CN 115087651 B CN115087651 B CN 115087651B
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Prior art keywords
methyl
carboxamide
indazole
carbamoyl
hydroxypropyl
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Chinese (zh)
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CN115087651A (zh
Inventor
陈洁
C·D·德兹尔巴
郭峻青
A·C·哈特
W·J·皮茨
薛成源
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202080069790.2A 2019-10-03 2020-10-02 作为激酶抑制剂的吲唑甲酰胺 Active CN115087651B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962909920P 2019-10-03 2019-10-03
US62/909,920 2019-10-03
PCT/US2020/053882 WO2021067654A1 (en) 2019-10-03 2020-10-02 Indazole carboxamides as kinase inhibitors

Publications (2)

Publication Number Publication Date
CN115087651A CN115087651A (zh) 2022-09-20
CN115087651B true CN115087651B (zh) 2024-06-25

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Country Status (11)

Country Link
US (1) US12275721B2 (https=)
EP (1) EP4037772B1 (https=)
JP (1) JP7600228B2 (https=)
KR (1) KR20220079593A (https=)
CN (1) CN115087651B (https=)
AU (1) AU2020357986A1 (https=)
CA (1) CA3153083A1 (https=)
ES (1) ES2969756T3 (https=)
IL (1) IL291828A (https=)
MX (1) MX2022003769A (https=)
WO (1) WO2021067654A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3849968B1 (en) 2018-09-13 2022-12-21 Bristol-Myers Squibb Company 1h-indazole carboxamides as receptor-interacting protein kinase 1 inhibitors (ripk1)
EP3849969B1 (en) 2018-09-13 2023-04-19 Bristol-Myers Squibb Company Indazole carboxamides as kinase inhibitors
AR123793A1 (es) 2020-10-19 2023-01-11 Bristol Myers Squibb Co Compuestos de triazolopiridinilo como inhibidores de quinasas
CN114989079B (zh) * 2022-06-21 2023-06-23 中国药科大学 Ripk1激酶靶点抑制剂及其医药用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020056072A1 (en) * 2018-09-13 2020-03-19 Bristol-Myers Squibb Company 1h-indazole carboxamides as receptor-interacting protein kinase 1 inhibitors (ripk1)
WO2020056074A1 (en) * 2018-09-13 2020-03-19 Bristol-Myers Squibb Company Indazole carboxamides as kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2004000234A1 (es) * 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
US20110237633A1 (en) 2008-12-11 2011-09-29 Bijoy Panicker Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
US8987275B2 (en) 2010-03-16 2015-03-24 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
AU2012212323A1 (en) 2011-02-01 2013-09-12 The Board Of Trustees Of The University Of Illinois HDAC inhibitors and therapeutic methods using the same
KR20130077390A (ko) 2011-12-29 2013-07-09 제이더블유중외제약 주식회사 단백질 키나아제 저해활성을 가지는 6-아미노-3-카복스아미도인다졸 유도체
US9783573B2 (en) 2012-09-18 2017-10-10 Bristol-Myers Squibb Company IAP antagonists
EP3580220B1 (en) 2017-02-13 2021-11-17 Bristol-Myers Squibb Company Aminotriazolopyridines as kinase inhibitors
CN111093645A (zh) 2017-07-05 2020-05-01 Cs制药技术有限公司 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂
DK3704118T3 (da) 2017-10-30 2022-03-14 Bristol Myers Squibb Co Aminoimidazopyrazin som kinasehæmmere
SG11202007035YA (en) 2018-01-26 2020-08-28 Bristol Myers Squibb Co Aminopyrrolotriazines as kinase inhibitors
AR123793A1 (es) 2020-10-19 2023-01-11 Bristol Myers Squibb Co Compuestos de triazolopiridinilo como inhibidores de quinasas

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020056072A1 (en) * 2018-09-13 2020-03-19 Bristol-Myers Squibb Company 1h-indazole carboxamides as receptor-interacting protein kinase 1 inhibitors (ripk1)
WO2020056074A1 (en) * 2018-09-13 2020-03-19 Bristol-Myers Squibb Company Indazole carboxamides as kinase inhibitors

Also Published As

Publication number Publication date
CA3153083A1 (en) 2021-04-08
JP2022552158A (ja) 2022-12-15
EP4037772A1 (en) 2022-08-10
MX2022003769A (es) 2022-04-20
ES2969756T3 (es) 2024-05-22
WO2021067654A1 (en) 2021-04-08
JP7600228B2 (ja) 2024-12-16
US20220380355A1 (en) 2022-12-01
KR20220079593A (ko) 2022-06-13
CN115087651A (zh) 2022-09-20
AU2020357986A1 (en) 2022-05-26
IL291828A (en) 2022-06-01
EP4037772B1 (en) 2023-11-22
US12275721B2 (en) 2025-04-15

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