CN109219609B - 作为tnf活性调节剂的稠合六环咪唑衍生物 - Google Patents

作为tnf活性调节剂的稠合六环咪唑衍生物 Download PDF

Info

Publication number
CN109219609B
CN109219609B CN201780033406.1A CN201780033406A CN109219609B CN 109219609 B CN109219609 B CN 109219609B CN 201780033406 A CN201780033406 A CN 201780033406A CN 109219609 B CN109219609 B CN 109219609B
Authority
CN
China
Prior art keywords
group
difluoromethoxy
alkyl
formula
compound
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.)
Expired - Fee Related
Application number
CN201780033406.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN109219609A (zh
Inventor
T·得哈罗加西亚
M·L·R·戴里格尼
J·P·希尔
H·T·豪斯勒
S·加多特
J·凯耶尔特斯
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.)
UCB Biopharma SRL
Original Assignee
UCB Biopharma SRL
Sanofi SA
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 UCB Biopharma SRL, Sanofi SA filed Critical UCB Biopharma SRL
Publication of CN109219609A publication Critical patent/CN109219609A/zh
Application granted granted Critical
Publication of CN109219609B publication Critical patent/CN109219609B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201780033406.1A 2016-04-01 2017-03-31 作为tnf活性调节剂的稠合六环咪唑衍生物 Expired - Fee Related CN109219609B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16163577 2016-04-01
EP16163577.6 2016-04-01
PCT/EP2017/057768 WO2017167995A1 (en) 2016-04-01 2017-03-31 Fused hexacyclic imidazole derivatives as modulators of tnf activity

Publications (2)

Publication Number Publication Date
CN109219609A CN109219609A (zh) 2019-01-15
CN109219609B true CN109219609B (zh) 2022-02-01

Family

ID=55650325

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780033406.1A Expired - Fee Related CN109219609B (zh) 2016-04-01 2017-03-31 作为tnf活性调节剂的稠合六环咪唑衍生物

Country Status (8)

Country Link
US (1) US10766906B2 (enExample)
EP (1) EP3436456B1 (enExample)
JP (1) JP6968089B2 (enExample)
CN (1) CN109219609B (enExample)
BR (1) BR112018069937A2 (enExample)
CA (1) CA3018992A1 (enExample)
EA (1) EA201892144A1 (enExample)
WO (1) WO2017167995A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201510758D0 (en) 2015-06-18 2015-08-05 Ucb Biopharma Sprl Novel TNFa structure for use in therapy
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
GB201621907D0 (en) 2016-12-21 2017-02-01 Ucb Biopharma Sprl And Sanofi Antibody epitope
CA3117344A1 (en) * 2018-10-24 2020-04-30 UCB Biopharma SRL Fused pentacyclic imidazole derivatives as modulators of tnf activity
JP2025540024A (ja) 2022-11-23 2025-12-11 フォワード セラピューティクス, インコーポレイテッド TNF-α活性の調節因子
TW202513567A (zh) * 2023-06-09 2025-04-01 大陸商上海翰森生物醫藥科技有限公司 五環類衍生物抑制劑、其製備方法與應用
WO2025038927A1 (en) 2023-08-16 2025-02-20 Raythera, Inc. Modulators of tnf alpha activity and uses thereof
CN121925420A (zh) * 2023-09-29 2026-04-24 赛诺菲 作为tnf活性的调节剂的桥联五环咪唑衍生物的制备、中间体及其制备
WO2025162456A1 (en) * 2024-01-31 2025-08-07 Intelligen Therapeutics Macrocyclic compound, pharmaceutical composition and use thereof
WO2025201449A1 (zh) * 2024-03-27 2025-10-02 海思科医药集团股份有限公司 一种杂环衍生物及其在医药上的应用
WO2025212627A1 (en) 2024-04-03 2025-10-09 Forward Therapeutics, Inc. Modulators of tnf-alpha activity
WO2025244936A1 (en) * 2024-05-20 2025-11-27 Forward Therapeutics, Inc. Modulators of tnf-alpha activity
WO2026012303A1 (en) * 2024-07-09 2026-01-15 Hangzhou Highlightll Pharmaceutical Co., Ltd NOVEL BENZO [4, 5] IMIDAZO COMPOUNDS AS TNFα MODULATORS
WO2026022134A1 (en) * 2024-07-23 2026-01-29 Sanofi Novel aminocarbonylation processes
WO2026044218A1 (en) * 2024-08-23 2026-02-26 Synnovation Therapeutics, Inc. Heterocyclic compounds as modulators of tnfa activity
WO2026055519A1 (en) 2024-09-06 2026-03-12 Rapt Therapeutics, Inc. Fused ring imidazole compounds
WO2026064303A1 (en) * 2024-09-17 2026-03-26 Synnovation Therapeutics, Inc. HETEROCYCLIC COMPOUNDS AS MODULATORS OF TNFα ACTIVITY
WO2026068677A1 (en) 2024-09-27 2026-04-02 Sanofi Processes for the preparation of fused pentacyclic imidazoles and intermediates
WO2026086865A1 (zh) * 2024-10-24 2026-04-30 宜昌人福药业有限责任公司 小分子TNF-α抑制剂及其用途
WO2026112363A1 (en) 2024-11-21 2026-05-28 Rapt Therapeutics, Inc. Fused heterocyclic aromatic compounds and uses thereof
WO2026145577A1 (zh) * 2024-12-31 2026-07-09 无锡奕拓医药科技有限责任公司 桥环类化合物、其药物组合物及其应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101076525A (zh) * 2004-11-10 2007-11-21 尼古拉斯皮拉马尔印度有限公司 用作肿瘤坏死因子-α抑制剂的稠合三环化合物
WO2013186229A1 (en) * 2012-06-11 2013-12-19 Ucb Pharma S.A. Tnf -alpha modulating benzimidazoles
WO2014009295A1 (en) * 2012-07-13 2014-01-16 Ucb Pharma S.A. Imidazopyridine derivatives as modulators of tnf activity
WO2015086525A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic benzimidazoles derivatives as modulators of tnf activity
WO2015086526A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic imidazole derivatives as modulators of tnf activity
WO2015086527A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic imidazole derivatives as modulators of tnf activity

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004087720A1 (en) 2003-03-10 2004-10-14 Pfizer Inc. Phosphate/sulfate ester compounds and pharmaceutical compositions for inhibiting protein interacting nima (pin1)
DE102008030206A1 (de) 2008-06-25 2009-12-31 Bayer Schering Pharma Aktiengesellschaft 3-Cyanoalky- und 3-Hydroxyalkyl-Indole und ihre Verwendung
TW201242953A (en) 2011-03-25 2012-11-01 Bristol Myers Squibb Co Imidazole prodrug LXR modulators
ES2576298T3 (es) 2011-06-20 2016-07-06 Vertex Pharmaceuticals Incorporated Ésteres de fosfato de inhibidores de girasa y topoisomerasa
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
ES2885432T3 (es) * 2014-10-03 2021-12-13 Ucb Biopharma Sprl Derivados de imidazol pentacíclicos condensados
PH12019502182B1 (en) * 2017-04-25 2024-01-31 Sanofi Sa Fused pentacyclic imidazole derivatives as modulators of tnf activity

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101076525A (zh) * 2004-11-10 2007-11-21 尼古拉斯皮拉马尔印度有限公司 用作肿瘤坏死因子-α抑制剂的稠合三环化合物
WO2013186229A1 (en) * 2012-06-11 2013-12-19 Ucb Pharma S.A. Tnf -alpha modulating benzimidazoles
CN104428293A (zh) * 2012-06-11 2015-03-18 Ucb生物制药私人有限公司 调节TNFα的苯并咪唑类
WO2014009295A1 (en) * 2012-07-13 2014-01-16 Ucb Pharma S.A. Imidazopyridine derivatives as modulators of tnf activity
CN104619709A (zh) * 2012-07-13 2015-05-13 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
WO2015086525A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic benzimidazoles derivatives as modulators of tnf activity
WO2015086526A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic imidazole derivatives as modulators of tnf activity
WO2015086527A1 (en) * 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused tricyclic imidazole derivatives as modulators of tnf activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
具有调节TNF-α作用的新生物反应调节剂-苯邻二甲酰亚胺类衍生物;王玉春等;《国外医药-合成药 生化药 制剂分册》;20001231;第21卷(第2期);第69-71页 *

Also Published As

Publication number Publication date
US10766906B2 (en) 2020-09-08
EP3436456B1 (en) 2021-11-17
CA3018992A1 (en) 2017-10-05
WO2017167995A1 (en) 2017-10-05
JP6968089B2 (ja) 2021-11-17
US20190100526A1 (en) 2019-04-04
CN109219609A (zh) 2019-01-15
JP2019512532A (ja) 2019-05-16
EA201892144A1 (ru) 2019-04-30
EP3436456A1 (en) 2019-02-06
BR112018069937A2 (pt) 2019-02-05

Similar Documents

Publication Publication Date Title
CN109195969B (zh) 作为tnf活性调节剂的稠合五环咪唑衍生物
US10766906B2 (en) Fused hexacyclic imidazole derivatives as modulators of TNF activity
CN109195968B (zh) 作为tnf活性调节剂的稠合五环咪唑衍生物
CN104470924B (zh) 作为tnf活性调节剂的咪唑并吡嗪衍生物
JP6629847B2 (ja) 縮合五員環イミダゾール誘導体
EP3080113B1 (en) Fused tricyclic imidazole derivatives as modulators of tnf activity
EP3080121B1 (en) Fused tricyclic benzimidazoles derivatives as modulators of tnf activity
CN105814055B (zh) 作为tnf活性调节剂的稠合咪唑和吡唑衍生物
JP7121033B2 (ja) Tnf活性のモジュレーターとしての縮合五環式イミダゾール誘導体
CN107690434B (zh) 作为tnf活性调节剂的稠合三环咪唑并吡嗪衍生物
CN109219608B (zh) 作为tnf活性调节剂的稠合五环咪唑衍生物
HK1240916B (en) Fused pentacyclic imidazole derivatives

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
TA01 Transfer of patent application right

Effective date of registration: 20191016

Address after: Brussels

Applicant after: UCB BIOPHARMA SPRL

Address before: Brussels

Applicant before: UCB BIOPHARMA SPRL

Applicant before: Sanofi

TA01 Transfer of patent application right
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20220201

CF01 Termination of patent right due to non-payment of annual fee