MX344142B - (8-aza-biciclico[3.2.1]oct-8-il)-[5-(1h-pirazol-4-il)-tiofen-3-il ]-metanonas 3, 3-disubstituidas como inhibidores de 1(beta)-hsd1. - Google Patents
(8-aza-biciclico[3.2.1]oct-8-il)-[5-(1h-pirazol-4-il)-tiofen-3-il ]-metanonas 3, 3-disubstituidas como inhibidores de 1(beta)-hsd1.Info
- Publication number
- MX344142B MX344142B MX2012012413A MX2012012413A MX344142B MX 344142 B MX344142 B MX 344142B MX 2012012413 A MX2012012413 A MX 2012012413A MX 2012012413 A MX2012012413 A MX 2012012413A MX 344142 B MX344142 B MX 344142B
- Authority
- MX
- Mexico
- Prior art keywords
- disorders
- thiophen
- pyrazol
- disubstituted
- aza
- Prior art date
Links
- -1 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) Chemical group 0.000 title 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical class O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 abstract 3
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 230000001668 ameliorated effect Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 208000019622 heart disease Diseases 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000000302 ischemic effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32945310P | 2010-04-29 | 2010-04-29 | |
| PCT/GB2011/000345 WO2011135276A1 (en) | 2010-04-29 | 2011-03-10 | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2012012413A MX2012012413A (es) | 2013-02-26 |
| MX344142B true MX344142B (es) | 2016-12-07 |
Family
ID=43880967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012012413A MX344142B (es) | 2010-04-29 | 2011-03-10 | (8-aza-biciclico[3.2.1]oct-8-il)-[5-(1h-pirazol-4-il)-tiofen-3-il ]-metanonas 3, 3-disubstituidas como inhibidores de 1(beta)-hsd1. |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9365564B2 (enExample) |
| EP (1) | EP2563780B1 (enExample) |
| JP (1) | JP5899202B2 (enExample) |
| KR (1) | KR101714820B1 (enExample) |
| CN (1) | CN102947295B (enExample) |
| AU (1) | AU2011247116B2 (enExample) |
| BR (1) | BR112012027640B1 (enExample) |
| CA (1) | CA2796297C (enExample) |
| DK (1) | DK2563780T3 (enExample) |
| ES (1) | ES2543692T3 (enExample) |
| IL (1) | IL222417A (enExample) |
| MX (1) | MX344142B (enExample) |
| RU (1) | RU2593753C2 (enExample) |
| WO (1) | WO2011135276A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0724251D0 (en) | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| GB0804685D0 (en) | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| US8642621B2 (en) | 2009-09-16 | 2014-02-04 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and their use |
| CN102947295B (zh) | 2010-04-29 | 2016-01-20 | 爱丁堡大学 | 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4基)-噻吩-3-基]-甲酮 |
| FR2993563B1 (fr) * | 2012-07-20 | 2015-12-18 | Metabrain Res | Derives de thiophenes utiles dans le traitement du diabete |
| US10100047B2 (en) * | 2014-03-06 | 2018-10-16 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Piperidine derivatives as orexin receptor antagonist |
| FR3035326B1 (fr) * | 2015-04-21 | 2017-05-12 | Pf Medicament | Utilisation de la (4-hydroxy-2-methyl-1,1-dioxido-2h-benzo[e][1,2]thiazin-3-yl)(naphtalen-2-yl)methanone dans la prevention et/ou le traitement de la steatohepatite non-alcoolique |
| CN104961698A (zh) * | 2015-07-13 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 末端硝基取代的三氮唑亚砜类化合物、其制备方法及其用途 |
| CN104961677A (zh) * | 2015-07-19 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 一类腈基二吡啶叔醇结构的11β-HSD1抑制剂及其用途 |
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| DK2563780T3 (en) | 2015-07-27 |
| BR112012027640A2 (pt) | 2017-08-08 |
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