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Beta amino acid derivatives as integrin antagonists
专利权人:
Saint Louis University
发明人:
RUMINSKI, Peter,GRIGGS, David
申请号:
ES13742135
公开号:
ES2647585T3
申请日:
2013.07.17
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula ** Formula ** in which: W is ** Formula ** in which: RA is -H or -F; and RB is -H, -OH or -F, where if RA is -F, RB is -H or -F; A is C-R- or N, where: R- is -H or -OH; R 'is -H; X is: halo, t-butyl, CF3, CF2H or cyano; ** Formula ** in which R4 and R5 are each independently alkyl (C-8), or substituted (C-8) alkyl, where one or more Hydrogen atoms have been independently substituted with OH, -F, -Cl, -Br, -I, -NH2, -NO2, -CO2H, -CO2CH3, -CN, -SH, -OCH3, -OCH2CH3, -C (O ) CH3, -N (CH3) 2, -C (O) NH2, -OC (O) CH3 or -S (O) 2NH2; R6 is -OH, -CN, -NH2, -CF3, -CF2H, -CH2F, -CO2H, -CO2-alkyl (C-8), -C (>; = O) NH2, -CH2OH or alkoxy (C-8 ), with the proviso that when R4 and R5 are each -CF3, then R6 is -OH; ** Formula ** in which n is 1 or 2 and X1 is -H; or ** Formula ** in which: A- is a covalent bond, and thus forms a cyclopropane, alkanediyl (C-6) or alkoxyidiyl (C-8) ring; and R7 is -OH, -CN, -NH2, -CO2H, -CO2-alkyl (C-8), -C (>; = O) NH2, -CF3, -CF2H or alkoxy (C-8); Y is: t-butyl; ** Formula ** in which R8 and R9 are each independently alkyl (C-8), or substituted (C-8) alkyl, where one or more hydrogen atoms have been independently substituted with -OH, -F, -Cl, -Br, -I, -NH2, -NO2, -CO2H, -CO2CH3, -CN, -SH, -OCH3, -OCH2CH3, -C (O) CH3, -N (CH3 ) 2, -C (O) NH2, -OC (O) CH3, or -S (O) 2NH2; R10 is -OH, -CN, -NH2, -CF3, -CF2H, -CO2H, -CO2-alkyl (C-8), -C (>; = O) NH2, -CH2OH or alkoxy (C-8), with the condition that when R8 and R9 are each -CF3, then R10 is -OH; ** Formula ** in which n '' is 1 or 2 and Y1 is -H; or ** Formula ** in which: A- 'is a covalent bond, and thus forms a cyclopropane, alkanediyl (C-6) or alkoxyidiyl (C-8) ring; and R11 is -OH, -CN, -NH2, -CO2H, -CO2-alkyl (C-8), -C (>; = O) NH2, -CF3, -CF2H or alkoxy (C-8); L is hydrogen; and Z is hydrogen or hydroxy and is attached to carbon atom 2 or 6; with the proviso that if W is ** Formula ** or then X and Y are not both t-butyl; and with the additional condition that if W i
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