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Claims for Patent: 4,529,596

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Claims for Patent: 4,529,596

Title: Thieno [3,2-c] pyridine derivatives and their therapeutic application
Abstract:This invention relates to new thieno [3,2-c] pyridine derivatives having the formula: ##STR1## in which: Y represents the OH group or an OR group in which R is a straight or branched lower alkyl radical, or Y represents a group ##STR2## in which R.sub.1 and R.sub.2 are each independently of each other, hydrogen or a straight or branched lower alkyl group; or R.sub.1 and R.sub.2 form together and with the nitrogen atom to which they are attached a heterocycle which may include a second heteroatom such as oxygen or nitrogen, wherein the latter may be substituted by a lower alkyl or benzyl radical which may be substituted; and X represents hydrogen, a halogen or a lower alkyl radical; and their addition salts with pharmaceutically acceptable mineral or organic acids if Y represents the group OR or ##STR3## or with mineral bases if Y represents OH, as well as the two enantiomers or their mixture. The invention also relates to the preparation process of new thieno [3,2-c] pyridine derivatives and to their therapeutic application as blood-platelet aggregation inhibiting agents and antithrombotics.
Inventor(s): Aubert; Daniel (Plaisance Du Touch, FR), Ferrand; Claude (Ramonville Saint-Agne, FR), Maffrand; Jean-Pierre (Garonne, FR)
Assignee: Sanofi, S.A. (Toulouse, FR)
Application Number:06/510,582
Patent Claims: 1. A compound of the formula: ##STR23## in which Y represents hydroxyl, an OR group wherein R is a straight or branched lower alkyl radical, or ##STR24## in which R.sub.1 and R.sub.2 are each independent of each other and represent hydrogen or a straight or branched lower alkyl group; or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a heterocycle selected from the group consisting of pyrrolidino, piperidino, morpholino, piperazino, N-lower alkyl piperazino and N-benzyl piperazino; and X represents hydrogen, a halogen or a lower alkyl radical; and their addition salts with pharmaceutically acceptable mineral or organic acids if Y represents OR groups or ##STR25## or with mineral bases if Y represents OH, including both enantiomeric forms or their mixture.

2. Methyl .alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlorophenyl-acetat e.

3. Methyl .alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)phenylacetate.

4. Methyl .alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.fluoro-phenylacetat e.

5. Isopropyl .alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetat e.

6. Ethyl .alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetat e.

7. N,N-dimethyl-[.alpha.-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlor ophenylacetamide.

8. A therapeutic composition having blood-platelet aggregation inhibiting activities and anti-thrombotic activities containing an effective amount of a compound of claim 1, or an addition salt thereof with a pharmaceutically acceptable mineral or organic acid or with mineral bases, or one of the two enantiomers or their mixture and a pharmaceutically acceptable carrier.

9. The composition as claimed in claim 8, in unit dosage form.

10. The composition as claimed in claim 8 or 9 in unit dosage form, each unit containing from 0.10 g to 1.00 g active ingredient.

11. A method of inhibiting platelet aggregation in mammals which comprises administering an effective amount of a composition comprising a compound of claim 1 and a suitable pharmaceutically acceptable carrier.

12. A method of treating or inhibiting thrombosis in mammals which comprises administering to a mammal in need of treatment an effective amount of a composition comprising a compound of claim 1 and a suitable pharmaceutically acceptable carrier.
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