Orexin receptor antagonists which are [ortho bi-(hetero-)aryl]-[2-(meta bi-(hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives
US-9493446-B2 · Nov 15, 2016 · US
Crystalline salt form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonist
US9790208B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9790208-B2 |
| Application number | US-201415101832-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 2, 2014 |
| Priority date | Dec 3, 2013 |
| Publication date | Oct 17, 2017 |
| Grant date | Oct 17, 2017 |
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Abstract
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The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
First claim
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The invention claimed is: 1. A crystalline form of the compound (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone; wherein said compound is present in form of the hydrochloric acid salt; wherein said crystalline salt form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2θ: 11.0°, 24.1° and 24.5°, wherein said X-ray powder diffraction diagram is obtained by using combined Cu Kα1 and Kα2 radiation, without Kα2 stripping; and the accuracy of the 2θ values is in the range of 2θ+/−0.2°. 2. A crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride according to claim 1 , comprising peaks in the X-ray powder diffraction diagram at the following angles of refraction 2θ: 9.2°, 11.0°, 13.8°, 15.1°, 16.3°, 16.8°, 19.8°, 24.1°, 24.5°, and 27.3°, wherein said X-ray powder diffraction diagram is obtained by using combined Cu Kα1 and Kα2 radiation, without Kα2 stripping; and the accuracy of the 2θ values is in the range of 2θ+/−0.2°. 3. A crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride according to claim 1 , which essentially shows the X-ray powder diffraction pattern as depicted in FIG. 2 . 4. A pharmaceutical composition comprising the crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride according to claim 1 , and a pharmaceutically acceptable carrier. 5. A pharmaceutical composition comprising the crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride according to claim 2 , and a pharmaceutically acceptable carrier. 6. A pharmaceutical composition comprising the crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazole-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride according to claim 3 , and a pharmaceutically acceptable carrier.
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Anxiolytics · CPC title
Hypnotics; Sedatives · CPC title
Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title
Drugs for disorders of the alimentary tract or the digestive system · CPC title
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Frequently asked questions
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- What does patent US9790208B2 cover?
- The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
- Who is the assignee on this patent?
- Idorsia Pharmaceuticals Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07D403/14. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Oct 17 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 2 related publications on this page (citations in our corpus or others sharing the same primary CPC).