COMPOUNDS THAT INHIBIT THE UNION OF INTEGRINS TO THEIR RECEPTORS.

摘要

A compound of the structure ** (See formula) ** in which A is selected from the group consisting of O, S; and NR5; E is selected from the group consisting of CH2, O, S and NR6; Q is selected from the group consisting of C (O) and (CH2) k, where k is an integer of 0 or 1; J is selected from the group consisting of O, S and NR8; G is selected from the group consisting of O, NH, S and (CH2) p, where p is an integer of 0 or 1; T is selected from the group consisting of C (O) and (CH2) b, where b is an integer from 0 to 3; L is selected from the group consisting of O, NR7, S and (CH2) n, where n is an integer of 0 or 1; M is selected from the group consisting of C (R9) (R10) and (CH2) u, where u is an integer from 0 to 3; X is selected from the group consisting of CO2B, PO3H2, SO3H, OPO3H2, C (O) NHC (O) R11, C (O) NHSO2R12, tetrazolyl and hydrogen; B, R1, R2, R3, R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from the group consisting of the groups hydrogen, alkyl, cycloalkyl, aryl, hydroxyalkyl, alkoxy, alkoxyalkoxy, cycloalkylalkyl, alkylamino , haloalkyl, alkylaryl, arylalkyl, heterocyclyl, alkylheterocyclyl and heterocyclylalkyl; R4 is 1,3-benzodioxole-5-yl; wherein R2 and R3 taken together can form a ring; R4 and R7 taken together can form a ring; or R9 and R10 taken together can form a ring; and salts thereof; wherein the term "alkyl" refers to a carbon chain, linear or branched, saturated or unsaturated, having up to 10 carbon atoms; the term "lower alkyl" refers to C1-C6 alkyl; the term "cycloalkyl" refers to an aliphatic ring system having 3 to 10 carbon atoms and 1 to 3 rings, wherein the cycloalkyl groups may be unsubstituted or substituted with one, two or three substituents independently selected from lower alkyl, haloalkyl, alkoxy, thioalkoxy, amino, alkylamino, dialkylamino, hydroxy, halo, mercapto, nitro, carboxaldehyde, carboxy, alkoxycarbonyl and carboxamide; the term "cycloalkylalkyl" refers to a cycloalkyl group attached to a lower alkyl group; the term "haloalkyl" refers to a lower alkyl group, to which at least one halogen substituent is attached; the term "alkoxy" refers to RaO-, wherein Ra is a lower alkyl group; the term "alkoxyalkoxy" refers to RbO-RcO-, where Rb is lower alkyl and Rc is alkylene, where alkylene is - (CH2) n'-, where n 'is an integer from 1 to 6; the term "alkylamino" refers to RdNH-, where Rd is a lower alkyl group; the term "aryl" refers to a carbocyclic aromatic group; the term "heterocyclyl" refers to an aromatic or non-aromatic cyclic group having one or more oxygen, nitrogen or sulfur atoms in the ring; the term "heterocyclylalkyl" refers to a heterocyclyl group attached to a lower alkyl group; the term "alkylheterocyclyl" refers to an alkyl group attached to a heterocyclyl group; the aryl, alkyl, cycloalkyl or heterocyclyl groups may be substituted by alcohols, amines, heteroatoms, or any combination of aryl, alkoxy, alkoxyalkoxy, alkyl, cycloalkyl or heterocyclyl groups, either directly attached or by means of linkers, wherein the linkers they are short chains of 1-3 atoms that contain any combination of C, C = O, CO2, O, N, S, S = O or SO2.