Heterocyclyl-butanamide derivatives

A technology of phenyl compounds, applied in the preparation of these compounds, cardiovascular diseases, treatment of diseases, multiple sclerosis, treatment of diseases and discomforts induced by TANK, can solve problems such as insufficient angiogenesis

Active Publication Date: 2017-02-22
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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Method used

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  • Heterocyclyl-butanamide derivatives
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  • Heterocyclyl-butanamide derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[1374] Example A: Syring Vials

[1375] A solution of 100 g of the active ingredient of formula I and 5 g of disodium hydrogen phosphate in 3 liters of double distilled water was adjusted to pH 6.5 using 2 N hydrochloric acid, sterile filtered, transferred to syringe vials and lyophilized under sterile conditions And sealed under sterile conditions. Each vial for injection contains 5 mg of active ingredient.

Embodiment B

[1376] Example B: Suppositories

[1377] A mixture of 20 g of active ingredient of formula I was melted with 100 g of soy lecithin and 1400 g of cocoa butter, poured into molds and allowed to cool. Each suppository contains 20 mg of active ingredient.

Embodiment C

[1378] Example C: Solution

[1379] In 940 milliliters of heavy distilled water by the active ingredient of 1 gram formula I, 9.38 gram NaH 2 PO 4 ∙ 2H 2 O, 28.48 g Na 2 HPO 4 ∙ 12H 2 O and 0.1 g of benzalkonium chloride to prepare a solution. The pH was adjusted to 6.8, the solution was made up to 1 L and sterilized by irradiation. This solution is available in the form of eye drops.

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Abstract

Compounds of the formula I, in which W, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

Description

[0001] Background of the invention [0002] The object of the present invention was to find novel compounds having valuable properties, in particular those which can be used for the preparation of medicaments. [0003] The present invention relates to heterocyclyl-butanamide derivatives which inhibit the activity of tankyrase (TANK) and poly(ADP-ribose) polymerase PARP-1. The compounds of the invention are therefore useful in the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injuries and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds and methods of treating diseases using pharmaceutical compositions comprising these compounds. [0004] The ribozyme poly(ADP-ribose) polymerase-1 (PARP-1) is a member of the PARP enzyme family. This growing family of enzymes consists of PARPs, such as PARP-1, PARP-2, PARP-3...

Claims

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Application Information

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IPC IPC(8): C07D401/14C07D401/06C07D413/06C07D471/04C07D487/04C07D491/04C07D495/04A61K31/4985A61K31/519A61K31/517A61K31/454A61K31/4545A61K31/4725A61K31/513A61K31/502A61K31/53A61P35/00A61P25/00A61P37/02A61P9/00A61P29/00A61P19/02A61P17/06A61P17/00A61P37/08
CPCC07D401/06C07D401/14C07D413/06C07D471/04C07D487/04C07D491/04C07D495/04C07D413/04C07D491/052A61P17/00A61P17/06A61P19/02A61P25/00A61P25/04A61P29/00A61P35/00A61P37/00A61P37/02A61P37/08A61P9/00A61K31/397A61K31/4985A61K31/454A61K31/501A61K31/502A61K31/517A61K31/519
Inventor H-P.布赫斯塔勒D.多施
Owner MERCK PATENT GMBH
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