Hoffmann-la Roche Inc.

Other

Schering Aktiengesellschaft

Leo Alig

Marcel Muller

Thomas Weller

Andor Furst

Rudolf Wiechert

Ulrich Kerb

Albrecht Edenhofer

Kurt Hilpert

Beat Steiner

Paul Hadvary

Arnold Trzeciak

Ulrike Obst

Holger Kuehne

Hans Peter Wessel

Alexander Chucholowski

Klaus Kieslich

Peter Keller

Jean Ackermann

Lutz Weber

Marianne Hurzeler

Katrin Groebke

Katrin Groebke Zbinden

Robert C Nickolson

Marianne Hurzeler Muller

Karl Petzoldt

Marcel M Uller

Marianne H Urzeler

The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R, E, Xto Xand Gand Gare as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

N-(4-carbamimidoyl-phenyl)-glycine derivatives

Benzazepinone-derivatives

Thiazole derivatives

The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:

Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in claim 1, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasing, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, kidney failure as well as infections caused by viruses, bacteria or fungi.

Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell--cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitrites.

Acetic acid derivatives

N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'' and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.

Amino acid derivatives

Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.

Growing community of inventors

Kaiseraugst, Switzerland

Leo Alig