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

Info

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
Authority
CN
China
Prior art keywords
substituted
alkyl
independently
group
occurrence
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980053221.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN112566916A (zh
Inventor
D·S·加德纳
J·V·德乔亚
J·B·桑特拉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN112566916A publication Critical patent/CN112566916A/zh
Application granted granted Critical
Publication of CN112566916B publication Critical patent/CN112566916B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (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

Family

ID=67766300

Family Applications (1)

Application Number Title Priority Date Filing Date
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

Country Status (7)

Country Link
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
MX2021001565A (es) 2018-08-08 2021-04-19 Bristol Myers Squibb Co Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル－マイヤーズ スクイブ カンパニー Ｐａｄ４阻害剤としての置換チエノピロール
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
WO2021158840A1 (en) 2020-02-06 2021-08-12 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
WO2021222353A1 (en) 2020-04-30 2021-11-04 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
EP4178963A1 (en) * 2020-07-02 2023-05-17 Remix Therapeutics Inc. 5-[5-(piperidin-4-yl)thieno[3,2-c]pyrazol-2-yl]indazole derivatives and related compounds as modulators for splicing nucleic acids and for the treatment of proliferative diseases
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
TW202233174A (zh) 2020-12-22 2022-09-01 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
WO2022140390A1 (en) 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
US20250109140A1 (en) * 2022-01-05 2025-04-03 Remix Theraputics Inc. 5-[5-(piperidin-4-yl)thieno[3,2-c]pyrazol-2-yl]indazole derivatives and related compounds as modulators for splicing nucleic acids and for the treatment of proliferative diseases
AU2023387505B2 (en) * 2022-11-24 2026-03-05 Helios Huaming Biopharma Co., Ltd. Selenium containing heterocycle compounds and use thereof
KR20260041867A (ko) 2023-07-21 2026-03-27 브리스톨-마이어스 스큅 컴퍼니 Pad4 조정제의 시트룰린화 및 활성을 평가하는 방법
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101916443B1 (ko) 2012-07-26 2018-11-08 글락소 그룹 리미티드 Pad4 억제제로서의 2-(아자인돌-2-일) 벤즈이미다졸
KR20180005250A (ko) 2015-05-21 2018-01-15 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Pad4 억제제로서의 벤조이미다졸 유도체
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
US10654814B2 (en) 2015-12-22 2020-05-19 Kancera Ab Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity
WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
US11026937B2 (en) 2016-09-12 2021-06-08 Padlock Therapeutics, Inc. Heteroaryl inhibitors of PAD4
JP7311228B2 (ja) 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
AU2018352142B2 (en) 2017-10-18 2022-08-25 Jubilant Epipad LLC Imidazo-pyridine compounds as PAD inhibitors
MX2021001565A (es) 2018-08-08 2021-04-19 Bristol Myers Squibb Co Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル－マイヤーズ スクイブ カンパニー Ｐａｄ４阻害剤としての置換チエノピロール
US20220348562A1 (en) 2018-08-08 2022-11-03 Bristol-Myers Squibb Company Benzimidazole inhibitors of pad enzymes

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 *

Also Published As

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

Similar Documents

Publication Publication Date Title
CN112566916B (zh) 作为pad4抑制剂的经取代的噻吩并吡咯
CN112805067B (zh) Pad酶的吲哚及氮杂吲哚抑制剂
JP7483678B2 (ja) Ｐａｄ４阻害剤としての置換ベンズイミダゾール
CN112789087B (zh) Pad酶的苯并咪唑抑制剂
IL275058B2 (en) Sulfonylurea derivatives as modulators of the NLRP3 inflammasome
CN115298175B (zh) 可用作免疫抑制剂的大环pad4抑制剂
CA3120037A1 (en) Heteroaromatic compounds as vanin inhibitors
WO2026075941A1 (en) Pyridazinone derivatives as pad4 inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant