CN112566916B - 作为pad4抑制剂的经取代的噻吩并吡咯 - Google Patents

作为pad4抑制剂的经取代的噻吩并吡咯 Download PDF

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Publication number
CN112566916B
CN112566916B CN201980053221.6A CN201980053221A CN112566916B CN 112566916 B CN112566916 B CN 112566916B CN 201980053221 A CN201980053221 A CN 201980053221A CN 112566916 B CN112566916 B CN 112566916B
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CN112566916A (zh
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D·S·加德纳
J·V·德乔亚
J·B·桑特拉
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Bristol Myers Squibb Co
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    • 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
    • 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
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201980053221.6A 2018-08-08 2019-08-07 作为pad4抑制剂的经取代的噻吩并吡咯 Active CN112566916B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862715834P 2018-08-08 2018-08-08
US62/715,834 2018-08-08
PCT/US2019/045426 WO2020033490A1 (en) 2018-08-08 2019-08-07 Substituted thienopyrroles as pad4 inhibitors

Publications (2)

Publication Number Publication Date
CN112566916A CN112566916A (zh) 2021-03-26
CN112566916B true CN112566916B (zh) 2023-10-20

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CN201980053221.6A Active CN112566916B (zh) 2018-08-08 2019-08-07 作为pad4抑制剂的经取代的噻吩并吡咯

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US (1) US11981680B2 (https=)
EP (1) EP3833671B1 (https=)
JP (1) JP7447080B2 (https=)
KR (1) KR102851932B1 (https=)
CN (1) CN112566916B (https=)
ES (1) ES2929200T3 (https=)
WO (1) WO2020033490A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019319835A1 (en) 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Indole and azaindole inhibitors of PAD enzymes
EP3833671B1 (en) 2018-08-08 2022-08-24 Bristol-Myers Squibb Company Substituted thienopyrroles as pad4 inhibitors
TW202115083A (zh) * 2019-09-27 2021-04-16 大陸商南京藥捷安康生物科技有限公司 肽醯精胺酸脫亞胺酶抑制劑及其用途
EP4100405A1 (en) 2020-02-06 2022-12-14 Bristol-Myers Squibb Company Macrocyclic pad4 inhibitors useful as immunosuppressant
TW202140477A (zh) 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環ｐａｄ４抑制劑
EP4143189A1 (en) 2020-04-30 2023-03-08 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
CN116940578A (zh) * 2020-07-02 2023-10-24 雷密克斯医疗公司 5-[5-(哌啶-4-基)噻吩并[3,2-c]吡唑-2-基]吲唑衍生物和相关化合物作为调节剂用于剪接核酸和治疗增殖性疾病
MX2023000167A (es) * 2020-07-02 2023-05-03 Remix Therapeutics Inc Derivados de 5-[5-(piperidin-4-il)tieno[3,2-c]pirazol-2-il]indazol y compuestos relacionados como moduladores para el corte y empalme de ácidos nucleicos y para el tratamiento de enfermedades proliferativas.
TW202241884A (zh) 2020-12-22 2022-11-01 美商基利科學股份有限公司 肽基精胺酸去亞胺酶之抑制劑
WO2022140428A2 (en) 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
WO2023133229A2 (en) * 2022-01-05 2023-07-13 Remix Therapeutics Inc. Compounds and methods for modulating splicing
WO2024109945A1 (en) * 2022-11-24 2024-05-30 Helios Huaming Biopharma Co., Ltd. Selenium containing heterocycle compounds and use thereof
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators
WO2026020127A2 (en) 2024-07-19 2026-01-22 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad2 modulators

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017100594A1 (en) * 2015-12-09 2017-06-15 Padlock Therapeutics, Inc. Bicyclic inhibitors of pad4
WO2017147102A1 (en) * 2016-02-23 2017-08-31 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
CN110194770A (zh) * 2018-02-26 2019-09-03 南京药捷安康生物科技有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
CN112805066A (zh) * 2018-08-08 2021-05-14 百时美施贵宝公司 作为pad4抑制剂的经取代的苯并咪唑

Family Cites Families (11)

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Publication number Priority date Publication date Assignee Title
RS55684B1 (sr) 2012-07-26 2017-07-31 Glaxo Group Ltd 2-(azaindol-2-il)benzimidazoli kao pad4 inhibitori
US10407407B2 (en) 2015-05-21 2019-09-10 Glaxosmithkline Intellectual Property Development Limited Benzoimidazole derivatives as PAD4 inhibitors
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
RU2747431C2 (ru) 2015-12-22 2021-05-05 Кансера Аб Бициклические гидроксамовые кислоты, полезные в качестве ингибиторов активности деацетилазы гистонов млекопитающих
KR102398941B1 (ko) 2016-07-27 2022-05-17 패들락 테라퓨틱스, 인코포레이티드 Pad4의 공유결합성 억제제
JP7118951B2 (ja) 2016-09-12 2022-08-16 パドロック・セラピューティクス・インコーポレイテッド Ｐａｄ４のヘテロアリール阻害剤
CN110582489B (zh) 2017-06-30 2023-10-27 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
AU2018352142B2 (en) 2017-10-18 2022-08-25 Jubilant Epipad LLC Imidazo-pyridine compounds as PAD inhibitors
CN112789087B (zh) 2018-08-08 2024-08-13 百时美施贵宝公司 Pad酶的苯并咪唑抑制剂
AU2019319835A1 (en) 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Indole and azaindole inhibitors of PAD enzymes
EP3833671B1 (en) 2018-08-08 2022-08-24 Bristol-Myers Squibb Company Substituted thienopyrroles as pad4 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017100594A1 (en) * 2015-12-09 2017-06-15 Padlock Therapeutics, Inc. Bicyclic inhibitors of pad4
WO2017147102A1 (en) * 2016-02-23 2017-08-31 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
CN110194770A (zh) * 2018-02-26 2019-09-03 南京药捷安康生物科技有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
CN112805066A (zh) * 2018-08-08 2021-05-14 百时美施贵宝公司 作为pad4抑制剂的经取代的苯并咪唑

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Synthesis of reversible PAD4 inhibitors via copper-catalyzed C−H arylation of benzimidazole;Zhengwei Guo et al.;《Sci China Chem》;第592-596页 *

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JP7447080B2 (ja) 2024-03-11
EP3833671B1 (en) 2022-08-24
US20220064180A1 (en) 2022-03-03
KR102851932B1 (ko) 2025-08-27
EP3833671A1 (en) 2021-06-16
CN112566916A (zh) 2021-03-26
KR20210042935A (ko) 2021-04-20
US11981680B2 (en) 2024-05-14
JP2021534106A (ja) 2021-12-09
WO2020033490A1 (en) 2020-02-13
ES2929200T3 (es) 2022-11-25

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