CN111936486B - 用作IL-12、IL-23和/或IFNα响应的调节剂的包含吡啶的杂环化合物 - Google Patents

用作IL-12、IL-23和/或IFNα响应的调节剂的包含吡啶的杂环化合物 Download PDF

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CN111936486B
CN111936486B CN201980020946.5A CN201980020946A CN111936486B CN 111936486 B CN111936486 B CN 111936486B CN 201980020946 A CN201980020946 A CN 201980020946A CN 111936486 B CN111936486 B CN 111936486B
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amino
methyl
carboxamide
pyridin
methoxy
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CN111936486A (zh
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肖自立
杨光
刘春健
T·C·舍伍德
J·L·吉尔摩
D·S·韦恩斯坦
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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
    • C07D401/14—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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
CN201980020946.5A 2018-03-22 2019-03-20 用作IL-12、IL-23和/或IFNα响应的调节剂的包含吡啶的杂环化合物 Active CN111936486B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862646432P 2018-03-22 2018-03-22
US62/646,432 2018-03-22
PCT/US2019/023111 WO2019183186A1 (en) 2018-03-22 2019-03-20 Heterocyclic compounds comprising pyridine useful as modulators of il-12, il-23 and/or ifn alpha responses

Publications (2)

Publication Number Publication Date
CN111936486A CN111936486A (zh) 2020-11-13
CN111936486B true CN111936486B (zh) 2023-09-22

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Country Status (7)

Country Link
US (1) US11597721B2 (enExample)
EP (1) EP3768667B1 (enExample)
JP (1) JP7485609B2 (enExample)
KR (1) KR102741437B1 (enExample)
CN (1) CN111936486B (enExample)
ES (1) ES2944733T3 (enExample)
WO (1) WO2019183186A1 (enExample)

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KR102858043B1 (ko) * 2018-10-30 2025-09-10 브리스톨-마이어스 스큅 컴퍼니 Il-12, il-23 및/또는 ifn-알파의 조정과 관련된 상태의 치료를 위한 아미드-치환된 헤테로시클릭 화합물
BR112021013924A2 (pt) 2019-01-18 2021-09-21 Astrazeneca Ab Inibidores de pcsk9 e métodos de uso do mesmo
WO2020150473A2 (en) 2019-01-18 2020-07-23 Dogma Therapeutics, Inc. Pcsk9 inhibitors and methods of use thereof
ES2981764T3 (es) * 2020-03-11 2024-10-10 Beijing Innocare Pharma Tech Co Ltd Compuestos heterocíclicos para inhibir las actividades de TYK2
US20230295119A1 (en) 2020-04-14 2023-09-21 Gossamer Bio Services, Inc. Substituted pyridines for the treatment of inflammatory diseases
CN122520625A (zh) 2020-12-22 2026-08-07 益方生物科技(上海)股份有限公司 杂芳基化合物及其制备方法和用途
EP4308556A4 (en) 2021-03-16 2025-02-19 Anrui Biomedical Technology (Guangzhou) Co., Ltd. Amino heteroaryl compounds and compositions
CN115141149A (zh) * 2021-03-30 2022-10-04 浙江文达医药科技有限公司 作为tyk2假激酶结构域抑制剂的杂环化合物及合成方法和用途
CN116888125B (zh) * 2021-04-07 2024-04-12 上海齐鲁制药研究中心有限公司 Tyk2抑制剂及其用途
JP7740849B2 (ja) * 2021-05-04 2025-09-17 シャンハイ ゼイ バイオテクノロジー カンパニー リミテッド 含窒素複素環ピリジン化合物
US20240317718A1 (en) * 2021-05-14 2024-09-26 Bristol-Myers Squibb Company Substituted heterocyclic compounds
CA3223641A1 (en) * 2021-06-22 2022-12-29 Wenyuan Qian Sulfoximine compound and use thereof
CN117794911A (zh) * 2021-07-15 2024-03-29 南京明德新药研发有限公司 含硫/磷的芳基类化合物及其应用
WO2023027948A1 (en) * 2021-08-21 2023-03-02 Relay Therapeutics, Inc. Jak2 inhibitors and methods of use thereof
WO2023064223A1 (en) 2021-10-11 2023-04-20 Gossamer Bio Services, Inc. Tri-substituted pyridines
KR20240111312A (ko) 2021-10-25 2024-07-16 카이메라 쎄라퓨틱스 인코포레이티드 Tyk2 분해제 및 이의 용도
TW202339749A (zh) * 2021-12-16 2023-10-16 大陸商凌科藥業有限公司 Ｔｙｋ２抑制劑及其組合物和方法
EP4206196A1 (en) 2021-12-29 2023-07-05 Almirall S.A. Pyrimidine substituted derivatives as tyk2 inhibitors
CN117263913A (zh) 2022-06-20 2023-12-22 益方生物科技(上海)股份有限公司 杂芳基化合物、固体形式、制备方法及其用途
WO2024020221A1 (en) * 2022-07-21 2024-01-25 Arvinas Operations, Inc. Modulators of tyk2 proteolysis and associated methods of use
AU2023412260A1 (en) * 2022-12-22 2025-05-29 Usynova Pharmaceuticals Ltd. Salt form and crystal form of pyridine multi-substituted compound and preparation method therefor
CN120607493B (zh) * 2025-06-04 2026-04-24 江西科技师范大学 一种含嘧啶结构的酰胺类化合物及其在制备tyk2 jh2激酶抑制剂中的应用

Citations (3)

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WO2013052393A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CN104159891A (zh) * 2012-01-10 2014-11-19 霍夫曼-拉罗奇有限公司 哒嗪酰胺化合物和它们作为syk 抑制剂的用途
CN104884454A (zh) * 2012-11-08 2015-09-02 百时美施贵宝公司 用作IL-12、IL-23和/或IFNα应答调节剂的酰胺取代的杂环化合物

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EP2922841B8 (en) 2012-11-08 2017-08-02 Bristol-Myers Squibb Company Alkyl-amide-substituted pyridyl compounds useful as modulators of il-12, il-23 and/or ifn alpha responses
MA48602A (fr) 2016-12-13 2020-03-18 Bristol Myers Squibb Co Composés hétéroaryle substitués par un amide alkyle d'oxyde de phosphine en tant que modulateurs des réponses il-12, il-23 et/ou ifn alpha

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO2013052393A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CN104159891A (zh) * 2012-01-10 2014-11-19 霍夫曼-拉罗奇有限公司 哒嗪酰胺化合物和它们作为syk 抑制剂的用途
CN104884454A (zh) * 2012-11-08 2015-09-02 百时美施贵宝公司 用作IL-12、IL-23和/或IFNα应答调节剂的酰胺取代的杂环化合物

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ES2944733T3 (es) 2023-06-23
JP2021518389A (ja) 2021-08-02
US20210032220A1 (en) 2021-02-04
JP7485609B2 (ja) 2024-05-16
WO2019183186A1 (en) 2019-09-26
EP3768667A1 (en) 2021-01-27
KR102741437B1 (ko) 2024-12-10
KR20200135425A (ko) 2020-12-02
US11597721B2 (en) 2023-03-07
CN111936486A (zh) 2020-11-13
EP3768667B1 (en) 2023-04-12

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