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US 2003/0144343 A1Published application
p-thienylbenzylamides as agonists of angiotensin-(1-7) receptors, and methods of their preparation and use
AssigneeAventis Pharma Deutschland GmbH
InventorHolger Heitsch
Life of this patent
Estimating the term…
Abstract
The invention relates to p-thienylbenzylamides of formula (I) 1 in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings given in the description. The compounds of formula (I) are potent agonists of angiotensin-(1-7) receptors and are useful as pharmaceutically active compounds to treat and/or prevent hypertension; cardiac hypertrophy; cardiac insufficiency; coronary heart diseases, such as angina pectoris; and endothelial dysfunction or endothelial damage as a consequence, for example, of atherosclerotic processes or in association with diabetes mellitus.
Claims16
A compound of formula (I)
- 41
- in which the indicated radicals have the following meanings:
- R(1) is chosen from among
- 1. (C1-C5)-alkyl, unsubstituted or substituted by a radical chosen from among NH2, halogen, O—(C1-C3)-alkyl, CO—O—(C1-C3)-alkyl and CO2H;
- 2. (C3-C8)-cycloalkyl;
- 3. (C1-C3)-alkyl-(C3-C8)-cycloalkyl;
- 4. (C6-C10)-aryl, unsubstituted or substituted by a radical chosen from halogen and O—(C1-C3)-alkyl;
- 5. (C1-C3)-alkyl-(C6-C10)-aryl, where the aryl radical is unsubstituted or substituted by a radical chosen from halogen and O—(C1-C3)-alkyl;
- 6. (C1-C5)-heteroaryl;
- and
- 7. (C1-C3)-alkyl-(C1-C5)-heteroaryl;
- R(2) is chosen from among
- 1. hydrogen;
- 2. (C1-C6)-alkyl, unsubstituted or substituted by a radical chosen from halogen and O—(C1-C3)-alkyl;
- 3. (C3-C8)-cycloalkyl;
- 4. (C1-C3)-alkyl-(C3-C8)-cycloalkyl;
- 5. (C6-C10)-aryl, unsubstituted or substituted by a radical chosen from among halogen, O—(C1-C3)-alkyl and CO—O—(C1-C3)-alkyl;
- and
- 6. (C1-C3)-alkyl-(C6-C10)-aryl, unsubstituted or substituted by a radical chosen from halogen and O—(C1-C3)-alkyl;
- R(3) is chosen from among
- 1. hydrogen;
- 2. COOH;
- and
- 3. COO—(C1-C4)-alkyl;
- R(4) is chosen from among
- 1. hydrogen;
- 2. halogen;
- and
- 3. (C1-C4)-alkyl;
- R(5) is chosen from
- 1. hydrogen, and
- 2. (C1-C6)-alkyl;
- R(6) is chosen from among
- 1. hydrogen;
- 2. (C1-C6)-alkyl;
- 3. (C1-C3)-alkyl-(C3-C8)-cycloalkyl;
- and
- 4. (C2-C6)-alkenyl;
- X is chosen from
- 1. oxygen,and
- 2. NH;
- in all the stereoisomeric forms thereof, and mixtures thereof in all ratios, and the physiologically tolerated salts thereof.
39 more elements
Dependencies are inferred from the claim text.