CN116096717B - 咪唑并[1,2-a]吡啶和[1,2,4]三唑并[1,5-a]吡啶衍生物作为TLR9抑制剂用于纤维化的治疗 - Google Patents

咪唑并[1,2-a]吡啶和[1,2,4]三唑并[1,5-a]吡啶衍生物作为TLR9抑制剂用于纤维化的治疗

Info

Publication number
CN116096717B
CN116096717B CN202180055737.1A CN202180055737A CN116096717B CN 116096717 B CN116096717 B CN 116096717B CN 202180055737 A CN202180055737 A CN 202180055737A CN 116096717 B CN116096717 B CN 116096717B
Authority
CN
China
Prior art keywords
phenyl
pyridine
imidazo
methanesulfonyl
mmol
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
CN202180055737.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN116096717A (zh
Inventor
D·S·尹
A·雷古尔罗-伦
A·P·德格南
G·吴
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 CN116096717A publication Critical patent/CN116096717A/zh
Application granted granted Critical
Publication of CN116096717B publication Critical patent/CN116096717B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202180055737.1A 2020-08-19 2021-08-18 咪唑并[1,2-a]吡啶和[1,2,4]三唑并[1,5-a]吡啶衍生物作为TLR9抑制剂用于纤维化的治疗 Active CN116096717B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063067452P 2020-08-19 2020-08-19
US63/067,452 2020-08-19
PCT/US2021/046420 WO2022040259A1 (en) 2020-08-19 2021-08-18 Imidazo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine derivatives as tlr9 inhibitors for the treatment of fibrosis

Publications (2)

Publication Number Publication Date
CN116096717A CN116096717A (zh) 2023-05-09
CN116096717B true CN116096717B (zh) 2026-04-10

Family

ID=77693624

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180055737.1A Active CN116096717B (zh) 2020-08-19 2021-08-18 咪唑并[1,2-a]吡啶和[1,2,4]三唑并[1,5-a]吡啶衍生物作为TLR9抑制剂用于纤维化的治疗

Country Status (14)

Country Link
US (1) US12486267B2 (cg-RX-API-DMAC10.html)
EP (1) EP4200297B1 (cg-RX-API-DMAC10.html)
JP (1) JP7813775B2 (cg-RX-API-DMAC10.html)
KR (1) KR20230053644A (cg-RX-API-DMAC10.html)
CN (1) CN116096717B (cg-RX-API-DMAC10.html)
AR (1) AR123281A1 (cg-RX-API-DMAC10.html)
AU (1) AU2021328575A1 (cg-RX-API-DMAC10.html)
BR (1) BR112023002737A2 (cg-RX-API-DMAC10.html)
CA (1) CA3190065A1 (cg-RX-API-DMAC10.html)
ES (1) ES3071068T3 (cg-RX-API-DMAC10.html)
IL (1) IL300727A (cg-RX-API-DMAC10.html)
MX (1) MX2023001885A (cg-RX-API-DMAC10.html)
TW (1) TW202227432A (cg-RX-API-DMAC10.html)
WO (1) WO2022040259A1 (cg-RX-API-DMAC10.html)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
KR20240148413A (ko) * 2022-02-18 2024-10-11 브리스톨-마이어스 스큅 컴퍼니 Tlr9의 억제제로서 유용한 치환된 비시클릭 헤테로아릴 화합물
CN120230100B (zh) * 2025-05-30 2025-09-05 中国药科大学 一种咪唑并[1,2-a]吡嗪或咪唑并[1,2-a]吡啶类化合物及其医药用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017058503A1 (en) * 2015-09-29 2017-04-06 Oncotherapy Science, Inc. Bicyclic compound and use thereof for inhibiting suv39h2
WO2018089695A1 (en) * 2016-11-11 2018-05-17 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060235037A1 (en) 2005-04-15 2006-10-19 Purandare Ashok V Heterocyclic inhibitors of protein arginine methyl transferases
GB0602178D0 (en) 2006-02-03 2006-03-15 Merck Sharp & Dohme Therapeutic treatment
JP2009532501A (ja) 2006-04-04 2009-09-10 ミリアド ジェネティクス， インコーポレイテッド 疾患および障害のための化合物
AU2007272009A1 (en) 2006-07-12 2008-01-17 Syngenta Limited Triazolopyridine derivatives as herbicides
EP2205085A1 (en) 2007-09-25 2010-07-14 Merck Sharp & Dohme Corp. 2-aryl or heteroaryl indole derivatives
EP2340243B1 (en) 2008-10-17 2014-10-08 Boehringer Ingelheim International GmbH Heteroaryl substituted indole compounds useful as mmp-13 inhibitors
BR112012006630A2 (pt) 2009-09-24 2016-05-03 Hoffmann La Roche derivados em indol como moduladores dos canais de cálcio ativados para liberação de cálcio (crac)
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
EP2757883B1 (en) 2011-09-22 2021-01-13 Merck Sharp & Dohme Corp. Triazolopyridyl compounds as aldosterone synthase inhibitors
US20130158049A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 7-azaindole inhibitors of crac
US20130158066A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 4-azaindole inhibitors of crac
WO2013156431A1 (en) 2012-04-17 2013-10-24 Syngenta Participations Ag Pesticidally active pyridyl- and pyrimidyl- substituted thiazole and thiadiazole derivatives
WO2013191113A1 (ja) 2012-06-18 2013-12-27 住友化学株式会社 縮合複素環化合物
US9643967B2 (en) 2013-12-13 2017-05-09 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as TLR inhibitors
EP3194394B1 (en) * 2014-09-16 2019-01-09 Syngenta Participations AG Pesticidally active tetracyclic derivatives with sulphur containing substituents
US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
CN109715617B (zh) 2016-07-30 2022-04-19 百时美施贵宝公司 作为tlr7、tlr8或tlr9抑制剂的二甲氧基苯基取代的吲哚化合物
ES2902504T3 (es) 2016-09-09 2022-03-28 Bristol Myers Squibb Co Compuestos de indol sustituidos con piridilo
WO2018165112A1 (en) 2017-03-09 2018-09-13 Oncotherapy Science, Inc. Bicyclic compound and use thereof for inhibiting histone methyltransferase
EP3661926B1 (en) 2017-08-04 2022-02-23 Bristol-Myers Squibb Company Substituted indole compounds useful as inhibitors of tlr7/8/9
CN110997670B (zh) 2017-08-04 2022-11-01 百时美施贵宝公司 [1,2,4]三唑并[4,3-a]吡啶基取代的吲哚化合物
CN111448190B (zh) 2017-11-14 2023-09-26 百时美施贵宝公司 取代的吲哚化合物
US12030878B2 (en) 2017-12-15 2024-07-09 Bristol-Myers Squibb Company Substituted indole ether compounds
MX2020006168A (es) 2017-12-18 2020-08-13 Bristol Myers Squibb Co Compuestos de 4-azaindol.
EP3728253B1 (en) 2017-12-19 2024-03-27 Bristol-Myers Squibb Company 6-azaindole compounds
EA202091474A1 (ru) 2017-12-19 2020-11-18 Бристол-Маерс Сквибб Компани Замещенные индольные соединения, применимые в качестве ингибиторов tlr
WO2019126081A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Amide substituted indole compounds useful as tlr inhibitors
KR102730859B1 (ko) 2017-12-20 2024-11-15 브리스톨-마이어스 스큅 컴퍼니 아릴 및 헤테로아릴 치환된 인돌 화합물
JP7287967B2 (ja) 2017-12-20 2023-06-06 ブリストル－マイヤーズ スクイブ カンパニー Ｔｌｒ阻害剤として有効なアミノインドール化合物
EA202091530A1 (ru) 2017-12-20 2020-09-14 Бристол-Маерс Сквибб Компани Диазаиндольные соединения
EP4089096A4 (en) 2020-01-09 2024-01-03 Sumitomo Chemical Company, Limited HETEROCYCLIC COMPOUND AND MEANS THEREOF FOR CONTROLLING HARMFUL ARTHROPODS

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017058503A1 (en) * 2015-09-29 2017-04-06 Oncotherapy Science, Inc. Bicyclic compound and use thereof for inhibiting suv39h2
WO2018089695A1 (en) * 2016-11-11 2018-05-17 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use

Also Published As

Publication number Publication date
EP4200297B1 (en) 2026-05-13
JP7813775B2 (ja) 2026-02-13
ES3071068T3 (en) 2026-06-19
TW202227432A (zh) 2022-07-16
AR123281A1 (es) 2022-11-16
WO2022040259A1 (en) 2022-02-24
AU2021328575A1 (en) 2023-03-16
IL300727A (en) 2023-04-01
US20240067638A1 (en) 2024-02-29
EP4200297A1 (en) 2023-06-28
KR20230053644A (ko) 2023-04-21
MX2023001885A (es) 2023-03-10
BR112023002737A2 (pt) 2023-03-14
EP4200297C0 (en) 2026-05-13
CA3190065A1 (en) 2022-02-24
US12486267B2 (en) 2025-12-02
CN116096717A (zh) 2023-05-09
JP2023538393A (ja) 2023-09-07

Similar Documents

Publication Publication Date Title
USRE49931E1 (en) [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
CN116075510A (zh) 1H-苯并[d]咪唑衍生物作为TLR9抑制剂用于治疗纤维化
CN111819176A (zh) 4-氮杂吲哚化合物
JP2021506941A (ja) ジアザインドール化合物
US12590091B2 (en) 1H-pyrrolo[3,2-C]pyridine and 1H-pyrrolo[2,3-C]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis
TW202227431A (zh) 可做為tlr9抑制劑之經取代雜芳基化合物
US12486267B2 (en) Imidazo[1,2-A]pyridine and [1,2,4]triazolo[1,5-A]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis
WO2023217201A2 (zh) 作为Wee1抑制剂的新型嘧啶并杂环类新化合物及其应用
WO2024125532A1 (zh) 作为CDKs抑制剂的新型并杂环类新化合物及其应用
EA050655B1 (ru) Замещенные бициклические соединения, пригодные для применения в качестве ингибиторов tlr9
US20250177363A1 (en) Substituted imidazopyridinyl compounds useful as inhibitors of tlr9
US20250163054A1 (en) Substituted bicyclic heteroaryl compounds useful as inhibitors of tlr9
CN120282961A (zh) 用作tlr9的抑制剂的取代的苯并咪唑化合物
CN118786130A (zh) 可用作tlr9抑制剂的经取代的咪唑并吡啶基化合物
HK40005511B (en) [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
HK40005511A (en) [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds

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