Heterocyclic derivatives and pharmaceutical composition

 

The present invention relates to heterocyclic derivatives of General formulain which a represents a monocyclic heterocyclic ring selected from the group consisting of pyridyl, pyrimidinyl and pyridazinyl, optionally substituted by one or two atoms or groups selected from halogen, cyano, oxo, amino, C1-4of alkyl; b is p-phenylene, optionally substituted by Deputy, is selected from C1-4of alkyl, C1-4alkoxycarbonyl, group (CH2)nY1, CON(L3Y1)2where n means an integer from 0 to 4, Y1- hydroxy, L3is2-4alkylene; R is hydrogen, C1-4alkoxycarbonyl or hydraxis1-4alkyl; X1means WITH; X2means SO2; Q denotes naphthyl, panels3-4albaniles or benzofuranyl, substituted with halogen; and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme factor Xandand can be used for the treatment of diseases caused by disorders that are associated with factor Xandfor example, for the treatment of diseases caused by thrombosis and disorders of the blood clotting system. In addition, objector Xandactions. 2 S. and 2 C. p. F.-ly, 1 table.

Description text in facsimile form (see graphic part).

Claims

1. Heterocyclic derivatives of General formulain which a represents a monocyclic heterocyclic ring selected from the group consisting of pyridyl, pyrimidinyl and pyridazinyl, optionally substituted by one or two atoms or groups selected from halogen, cyano, oxo, amino, C1-4of alkyl; b is p-phenylene, optionally substituted by Deputy, is selected from C1-4of alkyl, C1-4alkoxycarbonyl, group (CH2)nY1group CON(L3Y1)2where n means an integer from 0 to 4, Y1is hydroxy and L3is2-4alkylene; R is hydrogen, C1-4alkoxycarbonyl or hydraxis1-4alkyl; X1means WITH; X2means SO2;
Q means naphthyl, panels2-4albaniles or benzofuranyl, substituted with halogen;
or their pharmaceutically acceptable salts.

2. The compound according to claim,1, where a represents a 4-pyrimidinyl, or 4-pyridyl.

3. Connection on p. 1, selected from
1-(6-brannart-2-ilsp /> 1-(6-brannart-2-ylsulphonyl)-4-[4-(4-pyridinyl)benzoyl]piperazine;
or its pharmaceutically acceptable salt.

4. Pharmaceutical composition for use in the production of inhibiting factor XA steps that the compound of formula (I) according to any one of paragraphs.1-3 and a pharmaceutically acceptable diluent and a carrier.

Priority points and features:
08.11.1996 - p. 1 - for compounds of formula I, with all values a, b, R, X1X2and Q, in addition to compounds, where a is a monocyclic heterocyclic ring, substituted by oxopropoxy; p. 2, p. 3 - for the first during the presentation connection; p. 4 for compositions based on the compounds of formula I, having the specified value a, b, R, X1X2and Q, in addition to compositions based on the compounds, where a is a monocyclic heterocyclic ring, substituted by exography, and also compositions based on second and third in the course of the narrative in paragraph (3 connections.

09.07.1997 - p. 1 - for compounds of formula I, where a represents a monocyclic heterocyclic ring, substituted by oxopropoxy; p. 3 for the second and third during the presentation compounds; p. 4 for compositions based on compounds of the formula I, where a PR is done and the third during the statement in paragraph (3 connections.

 

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