ACID DERIVATIVES 3- (4-PIRIDIN-2-ILAMINO) -BUTIRIL) -2,3,4, 4A, 9, 9A-HEXAHIDRO-1H-3-AZA-FLUOREN-9-IL) ACETIC AND RELATED TRICICLIC INDANILS AS ALFAV BETA3 AND ALFAV AND BETA5 INTEGRIN INHIBITORS FOR THE TREATMENT OF CANCER AND THE UNSTABLE ANGINA.

摘要

A compound of Formula (I): where: R is selected from the group consisting of heterocyclyl and heteroaryl; R1 is one to two substituents selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkoxy, hydroxy, -NRARB, and halogen; wherein alkyl and alkoxy are optionally substituted on a terminal carbon with one to three substituents independently selected from the group consisting of halogen, hydroxy, or -NRARB; where RA and RB are substituents independently selected from hydrogen or C1-C6 alkyl; R2 is one to two substituents independently selected from the group consisting of hydrogen, C1-C4 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C4 alkoxy, -NRCRD, hydroxy, and halogen; wherein alkyl, alkenyl, alkynyl, and alkoxy are optionally substituted on a terminal carbon atom with one to three substituents independently selected from the group of halogen, hydroxy, C1-C4 alkoxy, and RC-RD; where RC and RD are substituents independently selected from hydrogen and C1-C6 alkyl; RC and RD are optionally taken together with the atoms to which they are anchored to form a five to seven member monocyclic ring; Z is selected from the group consisting of -CH2- and -CH-; A is selected from the group consisting of aryl, - CH (CH2) 1-3, and - (CH2) 1-3 provided that when A is - CH (CH2) 1-2- and Z is -CH- a double is formed link between A and Z; B is -NH- when optionally present; m and n are integers from 1 to 3; X is selected from the group consisting of O, S, and two hydrogen atoms; U is independently selected from -CH-, N, or S, provided that no more than one U represents S or N; and that U can only be S when W is not present; W is selected from the group consisting of -CH- and N when optionally present; and enantiomers, diastereoisomers, tautomers, solvates, or pharmaceutically acceptable salts and medicaments thereof.