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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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

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

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US (1) US11597721B2 (https=)
EP (1) EP3768667B1 (https=)
JP (1) JP7485609B2 (https=)
KR (1) KR102741437B1 (https=)
CN (1) CN111936486B (https=)
ES (1) ES2944733T3 (https=)
WO (1) WO2019183186A1 (https=)

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CA3118094A1 (en) * 2018-10-30 2020-05-07 Bristol-Myers Squibb Company Amide-substituted heterocyclic compounds for the treatment of conditions related to the modulation of il-12, il-23 and/or ifn-alpha
AU2020209216A1 (en) 2019-01-18 2021-08-26 Astrazeneca Ab PCSK9 inhibitors and methods of use thereof
SG11202107614PA (en) 2019-01-18 2021-08-30 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
DK4038063T3 (da) * 2020-03-11 2024-05-21 Beijing Innocare Pharma Tech Co Ltd Heterocykliske forbindelser til inhibering af tyk2-aktiviteter
US20230295119A1 (en) 2020-04-14 2023-09-21 Gossamer Bio Services, Inc. Substituted pyridines for the treatment of inflammatory diseases
WO2022135430A1 (en) 2020-12-22 2022-06-30 InventisBio Co., Ltd. Heteroaryl compounds, preparation methods and uses thereof
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
AU2022268464B2 (en) * 2021-05-04 2025-04-17 Shanghai Zheye Biotechnology Co. Ltd. Nitrogen-containing heterocyclic pyridine compound
US20240317718A1 (en) * 2021-05-14 2024-09-26 Bristol-Myers Squibb Company Substituted heterocyclic compounds
TWI825800B (zh) * 2021-06-22 2023-12-11 大陸商南京明德新藥研發有限公司 亞磺醯亞胺類化合物及其應用
WO2023284869A1 (zh) * 2021-07-15 2023-01-19 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
EP4387964A1 (en) * 2021-08-21 2024-06-26 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
JP2024539280A (ja) 2021-10-25 2024-10-28 カイメラ セラピューティクス, インコーポレイテッド Tyk2分解剤およびそれらの使用
EP4448514A4 (en) 2021-12-16 2025-10-29 Lynk Pharmaceuticals Co Ltd TYK2 INHIBITORS AND ASSOCIATED COMPOSITIONS AND PROCESSES
EP4206196A1 (en) 2021-12-29 2023-07-05 Almirall S.A. Pyrimidine substituted derivatives as tyk2 inhibitors
WO2024020221A1 (en) * 2022-07-21 2024-01-25 Arvinas Operations, Inc. Modulators of tyk2 proteolysis and associated methods of use
WO2024131882A1 (zh) * 2022-12-22 2024-06-27 南京明德新药研发有限公司 一种吡啶多取代化合物的盐型、晶型及其制备方法
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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US9315494B2 (en) 2012-11-08 2016-04-19 Bristol-Myers Squibb Company Alkyl-amide-substituted pyridyl compounds useful as modulators of IL-12, IL-23 and/or IFNα responses
CN110267964B (zh) 2016-12-13 2022-05-03 百时美施贵宝公司 作为IL-12、IL-23及/或IFNα响应调节剂的经取代的杂芳基氧化膦化合物

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

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