JP2019512533A5 - - Google Patents
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- Publication number
- JP2019512533A5 JP2019512533A5 JP2018551327A JP2018551327A JP2019512533A5 JP 2019512533 A5 JP2019512533 A5 JP 2019512533A5 JP 2018551327 A JP2018551327 A JP 2018551327A JP 2018551327 A JP2018551327 A JP 2018551327A JP 2019512533 A5 JP2019512533 A5 JP 2019512533A5
- Authority
- JP
- Japan
- Prior art keywords
- disorder
- formula
- alkyl
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 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 7
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 5
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 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
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens 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
- 230000002265 prevention Effects 0.000 claims 3
- 238000011282 treatment Methods 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- LTXNPDHRJIYEDL-SJLPKXTDSA-N 2-[5-[(1R,11R)-13-amino-18-(difluoromethoxy)-6-fluoro-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,12,14(19),15,17-octaen-5-yl]pyrimidin-2-yl]propan-2-ol Chemical compound FC(OC1=CC=CC=2C(N[C@H]3C=4N([C@@H](C=21)C3)C1=C(N=4)C=C(C(=C1)C=1C=NC(=NC=1)C(C)(C)O)F)=N)F LTXNPDHRJIYEDL-SJLPKXTDSA-N 0.000 claims 1
- GISOGHBONPSTDY-IEBWSBKVSA-N 2-[5-[(1R,11R)-18-(difluoromethoxy)-13-methylimino-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-5-yl]pyrimidin-2-yl]propan-2-ol Chemical compound FC(OC1=CC=CC=2/C(/N[C@H]3C=4N([C@@H](C=21)C3)C1=C(N=4)C=CC(=C1)C=1C=NC(=NC=1)C(C)(C)O)=N/C)F GISOGHBONPSTDY-IEBWSBKVSA-N 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000006978 adaptation Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16163579 | 2016-04-01 | ||
| EP16163579.2 | 2016-04-01 | ||
| PCT/EP2017/057767 WO2017167994A1 (en) | 2016-04-01 | 2017-03-31 | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512533A JP2019512533A (ja) | 2019-05-16 |
| JP2019512533A5 true JP2019512533A5 (https=) | 2020-04-23 |
| JP6968090B2 JP6968090B2 (ja) | 2021-11-17 |
Family
ID=55650327
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018551327A Active JP6968090B2 (ja) | 2016-04-01 | 2017-03-31 | 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 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10654861B2 (https=) |
| EP (1) | EP3436460B1 (https=) |
| JP (1) | JP6968090B2 (https=) |
| CN (1) | CN109195968B (https=) |
| BR (1) | BR112018069941A2 (https=) |
| CA (1) | CA3019245A1 (https=) |
| EA (1) | EA201892142A1 (https=) |
| WO (1) | WO2017167994A1 (https=) |
Families Citing this family (9)
| 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 |
| WO2025212627A1 (en) | 2024-04-03 | 2025-10-09 | Forward Therapeutics, Inc. | Modulators of tnf-alpha activity |
| WO2026055519A1 (en) | 2024-09-06 | 2026-03-12 | Rapt Therapeutics, Inc. | Fused ring imidazole compounds |
Family Cites Families (12)
| 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 |
| GB201321728D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| 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 |
| MX380578B (es) | 2014-10-03 | 2025-03-12 | Ucb Biopharma Sprl | Derivados de imidazol pentaciclicos fusionados. |
-
2017
- 2017-03-31 JP JP2018551327A patent/JP6968090B2/ja active Active
- 2017-03-31 EP EP17714785.7A patent/EP3436460B1/en active Active
- 2017-03-31 CA CA3019245A patent/CA3019245A1/en not_active Abandoned
- 2017-03-31 WO PCT/EP2017/057767 patent/WO2017167994A1/en not_active Ceased
- 2017-03-31 BR BR112018069941A patent/BR112018069941A2/pt not_active Application Discontinuation
- 2017-03-31 CN CN201780033198.5A patent/CN109195968B/zh not_active Expired - Fee Related
- 2017-03-31 EA EA201892142A patent/EA201892142A1/ru unknown
- 2017-03-31 US US16/086,408 patent/US10654861B2/en active Active