Dr. Karl Thomae Gmbh

Karl Thomae Gmbh

Karl Thomas Gmbh

Michael Entzeroth

Wolfgang Wienen

Norbert Hauel

Uwe Joerg Ries

Jacques Van Meel

Berthold Narr

Klaus Rudolf

Henri Doods

Wolfgang Eberlein

Wolfhard Engel

Gerhard Mihm

Berthold Narr, Deceased

Jacobus C Van Meel

Klaus-Dieter Willim

Helmut Pieper

Horst Dollinger

Franz Esser

Gerd Schnorrenberg

Manfred Reiffen

Wolfgang Grell

Andreas Bomhard

Gerhard Hallermayer

Jurgen Krause

Harald Ziegler

Heike Andrea Wieland

Jacobus C Antonius Van Meel

Armin Heckel

Rudolf Hurnaus

Walter Kobinger

Ludwig Pichler

Willi Diederen

Robert Sauter

Joachim Mierau

Rainer Zimmermann

Gunter Schingnitz

Heike-Andrea Wieland

Annerose Mauz

Andres Bomhard

The present invention relates to modified amino acids of general formula whereinA, Z, X, n, m, R, R, R, Rand Rare defined as in claimsto, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.

Modified amino acids, pharmaceuticals containing these compounds and method for their production

Modified aminoacids, pharmaceuticals containing these compounds and method for their production

NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;

Amino acid derivatives, pharmaceutical compositions containing these

The invention relates to benzimidazoles of the formula ##STR1## in which R.sub.1 to R.sub.4 are as defined in claim 1,

Benzimidazoles, medicaments containing these compounds and processes for

Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-�(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.

The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.

Benzimidazoles, pharmaceutical compositions containing these compounds

New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them. These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.

Condensed diazepinones, processes for preparing them and agents

Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.

Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(1-(2-N-morpholinoethyl)-imidazol-4-yl)-benzimi dazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.

(1-(2,3 or

Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo [1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-2-carboxylic acid.

(Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as

Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An compound is:

Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biph

Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is:

Benzimidazoles useful as angiotensin-11 antagonists

Angiotensin-II inhibiting benzimidazoles, useful for the treatment of hypertension. Exemplary compounds are:

Benzimidazoles and pharmaceutical compositions containing them

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Michael Entzeroth