JP6968089B2 - Tnf活性のモジュレーターとしての縮合六環式イミダゾール誘導体 - Google Patents
Tnf活性のモジュレーターとしての縮合六環式イミダゾール誘導体 Download PDFInfo
- Publication number
- JP6968089B2 JP6968089B2 JP2018551326A JP2018551326A JP6968089B2 JP 6968089 B2 JP6968089 B2 JP 6968089B2 JP 2018551326 A JP2018551326 A JP 2018551326A JP 2018551326 A JP2018551326 A JP 2018551326A JP 6968089 B2 JP6968089 B2 JP 6968089B2
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- Prior art keywords
- difluoromethoxy
- alkyl
- formula
- mmol
- disorders
- 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.)
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Links
- 0 C[n]1c(c(*)c(*)c(*)c2*)c2nc1* Chemical compound C[n]1c(c(*)c(*)c(*)c2*)c2nc1* 0.000 description 6
- OIBOCCUNBOKNOZ-UHFFFAOYSA-N CC(C)(C(CC=C1)=NC=C1c(cc1)cc(C2)c1C=C(C(C1)[n]3c(-c4ccc5)cnc3C)C2C1c4c5OC(F)F)O Chemical compound CC(C)(C(CC=C1)=NC=C1c(cc1)cc(C2)c1C=C(C(C1)[n]3c(-c4ccc5)cnc3C)C2C1c4c5OC(F)F)O OIBOCCUNBOKNOZ-UHFFFAOYSA-N 0.000 description 1
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 Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16163577.6 | 2016-04-01 | ||
| EP16163577 | 2016-04-01 | ||
| PCT/EP2017/057768 WO2017167995A1 (en) | 2016-04-01 | 2017-03-31 | Fused hexacyclic imidazole derivatives as modulators of tnf activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512532A JP2019512532A (ja) | 2019-05-16 |
| JP2019512532A5 JP2019512532A5 (https=) | 2020-04-30 |
| JP6968089B2 true JP6968089B2 (ja) | 2021-11-17 |
Family
ID=55650325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018551326A Active JP6968089B2 (ja) | 2016-04-01 | 2017-03-31 | Tnf活性のモジュレーターとしての縮合六環式イミダゾール誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10766906B2 (https=) |
| EP (1) | EP3436456B1 (https=) |
| JP (1) | JP6968089B2 (https=) |
| CN (1) | CN109219609B (https=) |
| BR (1) | BR112018069937A2 (https=) |
| CA (1) | CA3018992A1 (https=) |
| EA (1) | EA201892144A1 (https=) |
| WO (1) | WO2017167995A1 (https=) |
Families Citing this family (18)
| 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 |
| WO2018119142A1 (en) | 2016-12-21 | 2018-06-28 | 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 |
| CN120418259A (zh) | 2022-11-23 | 2025-08-01 | 弗沃德医疗公司 | TNFα活性的调节剂 |
| WO2024251282A1 (zh) * | 2023-06-09 | 2024-12-12 | 上海翰森生物医药科技有限公司 | 五环类衍生物抑制剂、其制备方法和应用 |
| TW202521544A (zh) | 2023-08-16 | 2025-06-01 | 美商雷瑟拉股份有限公司 | TNFα活性調節劑及其用途 |
| WO2025068505A1 (en) * | 2023-09-29 | 2025-04-03 | Sanofi | Preparation of bridged pentacyclic imidazole derivatives as modulators of tnf activity, intermeditates and their preparation |
| WO2025162456A1 (en) * | 2024-01-31 | 2025-08-07 | Intelligen Therapeutics | Macrocyclic compound, pharmaceutical composition and use thereof |
| TW202602881A (zh) * | 2024-03-27 | 2026-01-16 | 大陸商海思科醫藥集團股份有限公司 | 雜環衍生物及其在醫藥上的應用 |
| 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 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0408477A (pt) | 2003-03-10 | 2006-04-04 | Pfizer | compostos de éster de fosfato/sulfato e composições farmacêuticas para inibir a nima de interação com proteìna (pin 1) e uso dos mesmos |
| TW200615273A (en) * | 2004-11-10 | 2006-05-16 | Nicholas Piramal India Ltd | Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha |
| 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 |
| CN103702994B (zh) | 2011-06-20 | 2016-03-23 | 沃泰克斯药物股份有限公司 | 旋转酶和拓扑异构酶抑制剂的磷酸酯 |
| US9550737B2 (en) | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
| GB201212513D0 (en) | 2012-07-13 | 2012-08-29 | Ucb Pharma Sa | Therapeutic agents |
| CN104619709B (zh) * | 2012-07-13 | 2016-11-09 | 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 |
| GB201321729D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321730D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321728D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| MX380578B (es) | 2014-10-03 | 2025-03-12 | Ucb Biopharma Sprl | Derivados de imidazol pentaciclicos fusionados. |
| AU2018259040B2 (en) * | 2017-04-25 | 2022-04-28 | Sanofi | Fused pentacyclic imidazole derivatives as modulators of TNF activity |
-
2017
- 2017-03-31 US US16/086,414 patent/US10766906B2/en active Active
- 2017-03-31 CA CA3018992A patent/CA3018992A1/en active Pending
- 2017-03-31 JP JP2018551326A patent/JP6968089B2/ja active Active
- 2017-03-31 EP EP17713705.6A patent/EP3436456B1/en active Active
- 2017-03-31 EA EA201892144A patent/EA201892144A1/ru unknown
- 2017-03-31 BR BR112018069937A patent/BR112018069937A2/pt not_active Application Discontinuation
- 2017-03-31 CN CN201780033406.1A patent/CN109219609B/zh not_active Expired - Fee Related
- 2017-03-31 WO PCT/EP2017/057768 patent/WO2017167995A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| CA3018992A1 (en) | 2017-10-05 |
| US20190100526A1 (en) | 2019-04-04 |
| EP3436456A1 (en) | 2019-02-06 |
| JP2019512532A (ja) | 2019-05-16 |
| EP3436456B1 (en) | 2021-11-17 |
| CN109219609B (zh) | 2022-02-01 |
| CN109219609A (zh) | 2019-01-15 |
| EA201892144A1 (ru) | 2019-04-30 |
| BR112018069937A2 (pt) | 2019-02-05 |
| WO2017167995A1 (en) | 2017-10-05 |
| US10766906B2 (en) | 2020-09-08 |
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