ES2525703T3 - Derivados de indol y de bencimidazol sustituidos con oxadiazol y oxazol como inhibidores de DGAT1 - Google Patents
Derivados de indol y de bencimidazol sustituidos con oxadiazol y oxazol como inhibidores de DGAT1 Download PDFInfo
- Publication number
- ES2525703T3 ES2525703T3 ES08804779.0T ES08804779T ES2525703T3 ES 2525703 T3 ES2525703 T3 ES 2525703T3 ES 08804779 T ES08804779 T ES 08804779T ES 2525703 T3 ES2525703 T3 ES 2525703T3
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- ES
- Spain
- Prior art keywords
- substituted
- phenyl
- unsubstituted
- oxadiazol
- benzoimidazol
- 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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- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 title claims description 7
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 title claims description 4
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 title claims description 4
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 title description 5
- 229940127193 DGAT1 inhibitor Drugs 0.000 title description 3
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title description 2
- 229940058303 antinematodal benzimidazole derivative Drugs 0.000 title description 2
- 229940054051 antipsychotic indole derivative Drugs 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 277
- -1 carboxy, carbamoyl Chemical group 0.000 claims abstract description 262
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 133
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 82
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 74
- 239000001257 hydrogen Substances 0.000 claims abstract description 74
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- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 5
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims description 4
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Classifications
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Landscapes
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| US976064P | 2007-09-28 | ||
| PCT/EP2008/062900 WO2009040410A1 (en) | 2007-09-28 | 2008-09-26 | Oxadiazole- and oxazole-substituted benzimidazole- and indole-derivatives as dgat1 inhibitors |
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| ES2525703T3 true ES2525703T3 (es) | 2014-12-29 |
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| AU2005315430B2 (en) | 2004-12-14 | 2010-05-27 | Astrazeneca Ab | Oxadiazole derivatives as DGAT inhibitors |
| AR058562A1 (es) | 2005-12-22 | 2008-02-13 | Astrazeneca Ab | Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1 |
| MX2008015228A (es) | 2006-05-30 | 2008-12-12 | Astrazeneca Ab | Acido 5-fenilamino-1,3,4-oxadiazol-2-ilcarbonilamino-4-fenoxi-cicl ohexanocarboxilico sustituido como inhibidor de diacilglicerol aciltransferasa de acetil coenzima a. |
| AR066169A1 (es) * | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| WO2009112445A1 (en) * | 2008-03-10 | 2009-09-17 | Novartis Ag | Method of increasing cellular phosphatidyl choline by dgat1 inhibition |
| AU2010226829A1 (en) * | 2009-03-18 | 2011-09-15 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| RU2012132682A (ru) | 2009-12-31 | 2014-02-10 | Пирамал Энтерпрайзис Лимитед | Ингибиторы диацилглицерин ацилтрансферазы |
| MA34097B1 (fr) * | 2010-03-30 | 2013-03-05 | Novartis Ag | Utilisations d'inhibiteurs de dgat1 |
| WO2012044567A2 (en) * | 2010-09-30 | 2012-04-05 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| WO2012064569A1 (en) * | 2010-11-08 | 2012-05-18 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| US9867811B2 (en) | 2011-07-08 | 2018-01-16 | Novartis Ag | Method of treating atherosclerosis in high triglyceride subjects |
| WO2013074387A1 (en) * | 2011-11-14 | 2013-05-23 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| WO2013169648A1 (en) | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| EP2903985A1 (en) | 2012-10-03 | 2015-08-12 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| US9796729B2 (en) | 2012-11-23 | 2017-10-24 | Glaxosmithkline Llc | Compounds as diacylglycerol acyltransferase inhibitors |
| WO2014081996A1 (en) * | 2012-11-23 | 2014-05-30 | Glaxosmithkline Llc | Novel compounds as diacylglycerol acyltransferase inhibitors |
| EP3492474B1 (en) * | 2012-11-23 | 2021-08-11 | GlaxoSmithKline LLC | Intermediates used in the production of diacylglycerol acyltransferase inhibitors |
| CN103087045B (zh) * | 2013-01-11 | 2015-08-12 | 上海交通大学 | 一种苯并咪唑类杂环化合物、药物组合物及其用途 |
| CN104672144A (zh) * | 2015-02-13 | 2015-06-03 | 佛山市赛维斯医药科技有限公司 | 一种环丙基酰肼和硝基苯类gpr119激动剂、制备方法及其用途 |
| CN104610152A (zh) * | 2015-02-13 | 2015-05-13 | 佛山市赛维斯医药科技有限公司 | 一类环丙基酰肼类gpr119激动剂、制备方法及其用途 |
| CA3093970A1 (en) | 2018-03-16 | 2019-09-19 | Anji Pharmaceuticals Inc. | Compositions and methods for treating severe constipation |
| EP3887363A1 (en) | 2018-11-27 | 2021-10-06 | Novartis AG | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| CN113166204B (zh) * | 2018-11-27 | 2025-01-28 | 诺华股份有限公司 | 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型（PCSK9）抑制剂的环状肽 |
| UY38485A (es) | 2018-11-27 | 2020-06-30 | Novartis Ag | Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación |
| TW202333563A (zh) | 2021-11-12 | 2023-09-01 | 瑞士商諾華公司 | 用於治療疾病或障礙之二胺基環戊基吡啶衍生物 |
| CN117466863A (zh) * | 2022-07-20 | 2024-01-30 | 盛睿泽华医药科技（苏州）有限公司 | 含芳香族取代基的苯并咪唑化合物及其制备方法和用途 |
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