Derivatives of piperazine and pharmaceutical composition based on them

 

The invention relates to new derivatives of formula (I)

where a represents a 5 - or 6-membered monocyclic aromatic ring containing in the ring 1 or 2 nitrogen atom and unsubstituted or substituted by 1-3 substituents, A represents N; D represents a 2-indolyl, 2-benzimidazolyl or 2-benzo[b]furanyl and is unsubstituted or substituted by 1-3 halogen atoms, except 1-(5-chlorobenzophenone-2-ylsulphonyl)-4-[4-(4-pyridyl)benzoyl]piperazine and its pharmaceutically acceptable salts. The compounds of formula (I) possess antithrombine and anticoagulant properties and can find application in medicine. 2 S. and 11 C.p. f-crystals, 2 tab.

Description text in facsimile form (see graphic part).

Claims

1. The compound of formula (I)

where a represents a 5 - or 6-membered monocyclic aromatic ring containing in the ring 1 or 2 nitrogen atom and unsubstituted or substituted one, two or three atoms or groups selected from halogen, oxo, amino, hydroxy, C1-4-alkyl, C1-4-alkylamino or di-C1-4-and which is unsubstituted or substituted one, two or three halogen atoms, excluding 1-(5-chlorobenzophenone-2-ylsulphonyl)-4-[4-(4-pyridyl)benzoyl]piperazine,

and its pharmaceutically acceptable salts.

2. The compound of formula (I) under item 1, where a is peregrinae, pyrimidine, imidazolidinone or pyridazinyl ring.

3. The compound of formula (I) under item 2, where a represents 2-pyridyl, 3-pyridyl, 4-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 4-pyrimidinyl, 5-pyrimidinyl, 1-imidazolyl, 2-imidazolyl or 4-imidazolyl.

4. The compound of formula (I) according to any one of paragraphs.1-3, where a substituted C1-4-alkyl, amino and halogen.

5. The compound of formula (I) according to any one of paragraphs.1-3, where a is unsubstituted.

6. The compound of formula (I) according to any one of paragraphs.1-5, where D is substituted with halogen.

7. The compound of formula (I) under item 6, where the specified halogen represents bromine or chlorine.

8. The compound of formula (I) under item 1, where a is a pyridyl, pyrimidinyl, imidazolyl or pyridinyl;

D is a 2-indolyl or 2-benzo[b]furanyl, and both optionally substituted by fluorine, chlorine or bromine,

and its pharmaceutically acceptable salts.

9. The compound of formula (I) according to any one of paragraphs.1-8, where D is a 2-indolyl.

10. The compound of formula (I) under item 1, with representing the 11. The compound of formula (I) under item 1, representing 1-(5-Clorinda-2-ylsulphonyl)-4-[4-(1-imidazolyl)-benzoyl]piperazine or its pharmaceutically acceptable salt.

12. Pharmaceutical composition having inhibitory activity against factor XA containing the compound of formula (I) or its pharmaceutically acceptable salt p. 1 and a pharmaceutically acceptable diluent or carrier.

13. The compounds of formula (I) according to any one of paragraphs.1-11 or its pharmaceutically acceptable salt as an active ingredient of a medicinal product for the treatment of a disease or condition mediated by factor XA.

 

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