Patent EP0322914A2 successfully refreshed from Google Patents.
EP0322914A2
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Novel sulfhydryl containing tricyclic lactams and their pharmacological methods of use
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1988-12-29
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Granted: —
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Expires: 2008-12-29
Abstract
Abstract This invention relates to conformationally rigid sulfur containing tricyclic lactams, of formula <CHEM> wherein R is hydrogen, alkyl, or arylalkyl, and R' is hydrogen or -COR, to the intermediates and processes useful for their preparation, and to their pharmacological effects in inhibiting angiotensin converting enzyme, in treating reperfusion injury and in treating heart-failure.
Inventors
- 👤 Gary A. Flynn
- 👤 Douglas W. Beight
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-30 22:17
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/55; A61P; A61P43/00; A61P9/00; A61P9/04; A61P9/08; A61P9/10; A61P9/12
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
33 words
A compound of the formula wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl; and R′ is hydrogen or -COR, wherein R is as defined above, and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
33 words
A compound of the formula wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl; and R′ is hydrogen or -COR, wherein R is as defined above, and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
15 words
All enantiomeric isomers and diastereomeric isomers and mixtures thereof of a compound of Claim 1.
Claim 4
Dependent Claim
16 words
A compound of Claim 2 of the diastereomeric configuration: wherein the stereochemistry is 4(S), 7(S), 12b(R).
Claim 5
Dependent Claim
12 words
A compound of Claim 3 wherein R and R′ are both hydrogen.
Claim 6
Dependent Claim
13 words
A compound of Claim 3 wherein R is methyl and R′ is hydrogen.
Claim 7
Dependent Claim
15 words
A compound of the formula IV wherein R is C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl.
Claim 8
Dependent Claim
15 words
A compound of the formula IV wherein R is C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl.
Claim 9
Dependent Claim
16 words
A compound of the formula V wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl.
Claim 10
Dependent Claim
16 words
A compound of the formula V wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl.
Claim 11
Dependent Claim
24 words
Pharmaceutical compositions comprising a pharmaceutically active amount of a compound according to any of Claims 1 to 5 or of their pharmaceutically acceptable salts.
Claim 12
Dependent Claim
9 words
Pharmaceutical compositions according to Claim 8 for treating hypertension.
Claim 13
Dependent Claim
9 words
Pharmaceutical compositions according to Claim 8 for treating cardiotonia.
Claim 14
Dependent Claim
9 words
Pharmaceutical compositions according to Claim 8 for treating ischemia.
Claim 15
Dependent Claim
27 words
Use of the compounds according to any of Claims 1 to 5 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical drugs exhibiting antihypertensive activity.
Claim 16
Dependent Claim
31 words
Use of the compounds according to any of Claims 1 to 5 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical drugs exhibiting an enhancement of myocardial contractile force.
Claim 17
Dependent Claim
28 words
Use of the compounds according to any of Claims 1 to 5 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical drugs exhibiting an anti-ischemic effect.
Claim 18
Dependent Claim
112 words
A process for preparing a compound of the formula wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl, which comprises reacting a compound of the formula wherein R is as defined above with an alkylnitrite of the formula R˝ON=O, wherein R˝ is isoamyl or n-propyl, in the presence of acetic acid and an inert solvent under reflux conditions, to produce an intermediate compound of the formula and sequentially treating C first with strong acid and a phosphine selected from the group consisting of tributylphosphine or triphenylphosphine, at a temperature of about -70 °C to about 50°C, and then with a strong base and formaldehyde to produce the compound of Formula V.
Claim 19
Dependent Claim
112 words
A process for preparing a compound of the formula wherein R is hydrogen, C₁-C₆ lower alkyl, or (C₆-C₁₂)aryl(C₁-C₆)lower alkyl, which comprises reacting a compound of the formula wherein R is as defined above with an alkylnitrite of the formula R˝ON=O, wherein R˝ is isoamyl or n-propyl, in the presence of acetic acid and an inert solvent under reflux conditions, to produce an intermediate compound of the formula and sequentially treating C first with strong acid and a phosphine selected from the group consisting of tributylphosphine or triphenylphosphine, at a temperature of about -70 °C to about 50°C, and then with a strong base and formaldehyde to produce the compound of Formula V.
References Cited (Backward Citations)
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