Crystalline form of a quinolinone-carboxamide compound

A technology of crystallization and amides, which is applied in the fields of active ingredients of heterocyclic compounds, organic chemistry, digestive system, etc., and can solve the problems of reporting the crystalline salt form of the compound of formula I, etc.

Active Publication Date: 2011-07-06
THERAVANCE BIOPHARMA R&D IP LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The crystalline salt form of the compound of formula I has not been previously reported

Method used

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  • Crystalline form of a quinolinone-carboxamide compound
  • Crystalline form of a quinolinone-carboxamide compound
  • Crystalline form of a quinolinone-carboxamide compound

Examples

Experimental program
Comparison scheme
Effect test

example A

[0076] Hard gelatin capsules for oral administration are prepared as follows:

[0077] Element

[0078] representative program : The ingredients are blended well and then filled into hard gelatin capsules (260 mg composition per capsule).

example B

[0080] Hard gelatin capsules for oral administration are prepared as follows:

[0081] Element

[0082] representative program : The ingredients are blended well and then passed through a No. 45 mesh U.S. sieve and loaded into hard gelatin capsules (200 mg of composition per capsule).

example C

[0084] Capsules for oral administration are prepared as follows:

[0085] Element

[0086] representative program : The ingredients are blended well and then filled in gelatin capsules (310 mg composition per capsule).

[0087] Formulation Example D

[0088] Tablets for oral administration are prepared as follows:

[0089] Element

[0090] representative program : The active ingredient, starch and cellulose are passed through a No. 45 mesh US Standard sieve and mixed thoroughly. The polyvinylpyrrolidone solution was mixed with the resulting powder, and the mixture was then passed through a No. 14 mesh US Standard sieve. The granules thus obtained are dried at 50-60°C and passed through a No. 18 mesh US Standard sieve. The sodium carboxymethyl starch, magnesium stearate and talc (previously passed through a No. 60 mesh US Standard sieve) are then added to the granules. After mixing, the mixture is compressed on a tablet machine to obtain tablets we...

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Abstract

The present invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5HT4 receptor activity, and processes useful for preparing such crystalline salt forms.

Description

technical field [0001] The present invention relates to can be used as 5-HT 4 A crystalline salt form of the quinolinonecarboxamide compound of a receptor agonist. The invention also relates to pharmaceutical compositions comprising said crystalline compound, the use of said compound for the treatment of 4 Methods of receptor activity mediated medical conditions and methods useful in the preparation of the compounds. Background technique [0002] Novel quinolinone carboxamide compounds are disclosed in commonly assigned U.S. Provisional Application No. 60 / 560,076, filed April 7, 2004, and U.S. Patent Application No. 11 / 100,113, filed April 6, 2005, The compounds are expected to be useful in the treatment of conditions in which the motility of the gastrointestinal tract is impaired. Specifically, the compound 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R) -2-Hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide has ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D451/04A61K31/40A61P1/00
CPCC07D451/04A61K31/46A61P1/00A61P1/04A61P1/10A61P1/14A61P43/00A61P3/10A61K31/40
Inventor 保罗·R·法瑟雷S·德里克·特纳亚当·戈德布卢姆罗伯特·晁丹尼尔·格诺夫
Owner THERAVANCE BIOPHARMA R&D IP LLC
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