JP2019512532A5 - - Google Patents
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- Publication number
- JP2019512532A5 JP2019512532A5 JP2018551326A JP2018551326A JP2019512532A5 JP 2019512532 A5 JP2019512532 A5 JP 2019512532A5 JP 2018551326 A JP2018551326 A JP 2018551326A JP 2018551326 A JP2018551326 A JP 2018551326A JP 2019512532 A5 JP2019512532 A5 JP 2019512532A5
- Authority
- JP
- Japan
- Prior art keywords
- difluoromethoxy
- methanobenzimidazo
- benzodiazocin
- triazolo
- 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.)
- Granted
Links
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- -1 [1,2,3] triazolyl Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 5
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 3
- 208000022873 Ocular disease Diseases 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000002757 inflammatory effect Effects 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- 230000003040 nociceptive effect Effects 0.000 claims 3
- 230000000771 oncological effect Effects 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 208000025966 Neurological disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- MHZUYMLTJORKQU-UHFFFAOYSA-N (3Z)-2H-2,5-benzodiazocin-1-one Chemical compound C=1(N=CC=NC=C2C=1C=CC=C2)O MHZUYMLTJORKQU-UHFFFAOYSA-N 0.000 claims 1
- KZNXKMJGYSECTN-UHFFFAOYSA-N 1,2-benzodiazocine Chemical compound N1=NC=CC=CC2=CC=CC=C21 KZNXKMJGYSECTN-UHFFFAOYSA-N 0.000 claims 1
- JXRWWYZKHITTFG-UHFFFAOYSA-N 4,5,6,9-tetrazatricyclo[9.4.0.02,6]pentadeca-1(15),2,4,7,9,11,13-heptaene Chemical compound N1=NC=C2N1C=CN=CC1=C2C=CC=C1 JXRWWYZKHITTFG-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000006978 adaptation Effects 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000005215 cycloalkylheteroaryl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000007069 methylation reaction Methods 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
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 true JP2019512532A5 (https=) | 2020-04-30 |
| JP6968089B2 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
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