Patent TW-200738671-A (TW)
Title: Compounds for the inhibition of integrins and use thereof
Inventor: ZISCHINSKY GUNTHER
IPC: A61K31/395
Filed: 2007-01-31
Abstract: The present invention is related to a compound of formula (I) G-Z-A-Ar-Y-Ψ (I) wherein A is a radical selected from the group comprising nonaromatic heterocyclic and homocyclic ring systems; Ar is a radical which is either absent or present, whereby if Ar is present, Ar is selected from the group comprising 3- to 9-membered rings, or if Ar is present, Ar is a polycyclic ring system selected from the group comprising 4,4-membered rings, 4,5-membered rings, 4,6-membered rings, 5,5-membered rings, 5,6-membered rings, 6,6-membered rings, 6,7-membered rings, 7,7-membered rings, 6,5,6-membered rings, 6,6,6-membered rings, 6,7,6-membered rings; Z and Y are radicals individually and independently selected from the group comprising (CH2)n-E-(CH2)m-L-(CH2)k and (CH2)m-L-(CH2)k, wherein E is a radical which is either absent or present, whereby if E is present, E is selected from the group comprising O, S, NH, NRa, CO, SO, SO2, substituted ethylene and acetylene; L is a radical which is either absent or present, whereby if L is present, L is individually and independently selected from the group comprising O, S, NH, NRb, CO, SO, SO2, substituted ethylene and acetylene; and k, m and n are individually and independently 0, 1, 2 or 3; Ψ is a radical of formula (II), wherein Q is a radical selected from the group comprising a direct bond, C=O, C=S, O, S, CRaRb, NRa-NRb, N=N, CRa=N, N=CRa, (C=O)-O, O-(C=O), SO2, NRa, (C=O)-NRa, NRa-(C=O)-NRb, NRc-(C=O), O-(C=O)-NRc, NRc-(C=O)-O, NRc-(C=S), (C=S)-NRc, NRc-(C=S)-NRd, NRc-SO2 and SO2-NRc. R1, Ra, Rb, Rc and Rd are radicals which are individually and independently selected from the group comprising H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloyl, substituted heterocycloyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, cycloalkylalkyl, substituted cycloalkylalkyl, heterocyclylalkyl, substituted heterocyclylalkyl, alkyloxy, alkyloxyalkyl, substituted alkyloxyalkyl, alkyloxycycloalkyl, substituted alkyloxycycloalkyl, alkyloxyheterocyclyl, substituted alkyloxyheterocyclyl, alkyloxyaryl, substituted alkyloxyaryl, alkyloxyheteroaryl, substituted alkyloxyheteroaryl, alkylthioalkyl, substituted alkylthioalkyl, alkylthiocycloalkyl and substituted alkylthiocycloalkyl, hydroxy, substituted hydroxy, oxo, thio, substituted thio, aminocarbonyl, substituted aminocarbonyl, formyl, substituted formyl, thioformyl, substituted thioformyl, amino, substituted amino, hydroxyl, substituted hydroxyl, mercapto, substituted mercapto, hydrazino, substituted hydrazino, diazene, substituted diazene, imine, substituted imine, amidino, substituted amidino, iminomethylamino, substituted iminomethylamino, ureido, substituted ureido, formylamino, substituted formylamino, aminocarbonyloxy, substituted aminocarbonyloxy, hydroxycarbonylamino, substituted hydroxycarbonylamino, hydroxycarbonyl, substituted hydroxycarbonyl, formyloxy, substituted formyloxy, thioformylamino, substituted thioformylamino, ,aminothiocarbonyl, substituted aminothiocarbonyl, thioureido, substituted thioureido, sufonyl, substituted sulfonyl, sulfonamino, substituted sulfonamino, aminosulfonyl, substituted aminosulfonyl, cyano, halogen; R2 is a hydrophobic moiety; R3 is a radical selected from the group comprising OH, C1-C8alkyloxy and aryl C0-C6alkyloxy; R4 is a radical selected from the group comprising hydrogen, halogen and C1-C4alkyl; and G is a radical containing one ore more moieties, whereby such moiety is selected from the group comprising NH, OH and a basic moiety.