- Novel, potent non-covalent thrombin inhibitors incorporating P3-lactam scaffolds
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Evolution of P1-argininal inhibitor prototypes led to a series of non-covalent P3-7-membered lactam inhibitors 1a-w, featuring novel peptidomimetic units that probe each of the S1, S2, and S3 specificity pockets of thrombin. Rigid P1-arginine surrogates possessing a wide range of basicity (calcd pKa's~neutral-14) were surveyed. The design, synthesis, and biological activity of these targets are presented.
- Ho, Jonathan Z.,Gibson, Tony S.,Semple
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p. 743 - 748
(2007/10/03)
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- Phosphonic acid-substituted benzazepinone-n-acetic acid derivatives process for their preparation and pharmaceutical compositions comprising them
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Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR 1 is hydrogen or a group forming a biolabile phosphonic acid ester,R 2 is hydrogen or a group forming a biolabile phosphonic acid ester and R. sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.
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- Pharmaceuticals which promote gastrointestinal blood circulation
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The use is described of compounds of the general formula I STR1 wherein R1 represents a phenyl-lower alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or represents a naphthyl-lower alkyl group, R2 denotes hydrogen or a biolabile ester-forming group, and R3 denotes hydrogen or a biolabile ester-forming group, and physiologically acceptable salts of the acids of formula I for preparing pharmaceutical compositions for the treatment and/or prophylaxis of gastrointestinal blood circulation disturbances.
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- BENZAZEPINE-, BENZOXAZEPINE- AND BENZOTHIAZEPINE-N-ACETIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds with neutral endopeptidase (NEP) inhibitory activity corresponding to the formula I STR1 in which R 1 is a lower alkoxy-lower-alkyl group whose lower alkoxy radical is substituted by a lower alkoxy group, or a phenyl-lower-alkyl or phenyloxy-lower-alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or a naphthyl-lower-alkyl group, A is CH 2, O or S,R 2 is hydrogen or halogen,R. sup.3 is hydrogen or halogen,R 4 is hydrogen or a group forming a biolabile ester, andR 5 is hydrogen or a group forming a biolabile ester, and the physiologically acceptable acid addition salts thereof.
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- 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
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Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotensin converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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- 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
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Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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