Abstract:
The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I,A-B-D-E-F-G(I)A, B, D, and E are alpha -amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond. In another embodiment, the invention includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.
Abstract:
The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I,A-B-D-E-F-G(I)A, B, D, and E are alpha -amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond. In another embodiment, the invention includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.
Abstract:
The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I,A-B-D-E-F-G(I)A, B, D, and E are alpha -amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond. In another embodiment, the invention includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.
Abstract:
Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA-B-D-E-F-G(I)and acid salts thereof, wherein A, D, and E are alpha -amino acid residues, B is an alpha -amino acid residue or an alpha -hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a beta -hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.
Abstract:
The invention relates to carbamate and carbamide derivatives of formula (I), wherein the substituents have the meaning cited in the description. The invention also relates to the production and use thereof as endothelin receptor antagonists.
Abstract:
The invention relates to carboxylic acid derivatives of formula (I), whereby the substituents have the meanings as explained in the description. The invention also relates to the production and use of said novel carboxylic acid derivatives as endothelin receptor antagonists.
Abstract:
Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.
Abstract:
The invention relates to the use of an endothelin blocker in combination with an alpha v beta 3 integrin receptor antagonist for the treatment or prevention of diseases, particularly to the use of a pharmaceutical composition, comprising an endothelin blocker and an alpha v beta 3 integrin receptor antagonist, for the treatment or prevention of cardiovascular disorders, particularly for the treatment or prevention of restenosis after vessel injury or revascularisation treatment and to the pharmaceutical composition itself.
Abstract:
The invention relates to a method for preparing sulfanyl-type endothelin receptor antagonists of general formula (I) wherein R represents hydroxy, alkoxy, sulfonamidyl, amino; R represents alkyl, aryl or heteroaryl, optionally substituted, and R , R , R can be the same or different and are alkyl or aryl, optionally substituted, by means of nucleophilic reaction of a carboxylic acid derivative of formula (II) with a sulfide of formula (III), X being SR or SO2R and R being alkyl or aryl, optionally substituted.