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US4529596A
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Thieno [3,2-c] pyridine derivatives and their therapeutic application
Assignee: SANDOFI SA A FRENCH CORP
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Filing: 1983-07-05
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Granted: 1985-07-16
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Expires: 2003-07-05
Abstract
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 1 and R 2 are each independently of each other, hydrogen or a straight or branched lower alkyl group; or R 1 and R 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.
Inventors
- 👤 Daniel Aubert
- 👤 Claude Ferrand
- 👤 Jean-Pierre Maffrand
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 18:54
CPC Classifications
C; C07; C07D; C07D495/00; C07D495/02; C07D495/04; A; A61; A61P; A61P7/00; A61P7/02
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
129 words
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 1 and R 2 are each independent of each other and represent hydrogen or a straight or branched lower alkyl group; or R 1 and R 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.
Claim 2
Dependent Claim
129 words
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 1 and R 2 are each independent of each other and represent hydrogen or a straight or branched lower alkyl group; or R 1 and R 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.
Claim 3
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlorophenyl-acetate.
Claim 4
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlorophenyl-acetate.
Claim 5
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)phenylacetate.
Claim 6
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)phenylacetate.
Claim 7
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.fluoro-phenylacetate.
Claim 8
Dependent Claim
2 words
Methyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.fluoro-phenylacetate.
Claim 9
Dependent Claim
2 words
Isopropyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetate.
Claim 10
Dependent Claim
2 words
Isopropyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetate.
Claim 11
Dependent Claim
2 words
Ethyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetate.
Claim 12
Dependent Claim
2 words
Ethyl α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chloro-phenylacetate.
Claim 13
Dependent Claim
1 words
N,N-dimethyl-[α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlorophenylacetamide.
Claim 14
Dependent Claim
1 words
N,N-dimethyl-[α-(4,5,6,7-tetrahydro-thieno(3,2-c)-5-pyridyl)-o.chlorophenylacetamide.
Claim 15
Dependent Claim
52 words
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.
Claim 16
Dependent Claim
11 words
The composition as claimed in claim 8, in unit dosage form.
Claim 17
Dependent Claim
24 words
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.
Claim 18
Dependent Claim
29 words
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.
Claim 19
Dependent Claim
37 words
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.
References Cited (Backward Citations)
US2527574A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-07-15 | 1989-01-14 | 1989-07-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-07-15 | 1993-01-14 | 1993-07-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-07-15 | 1997-01-14 | 1997-07-16 | $7700.00 | Window Closed / Lapsed |