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Vasopressin V1A antagonists
专利权人:
Vantia Limited
发明人:
ANDRZEJ, Roman,BAXTER, Andrew,HEENEY, Celine,STOCKLEY, Martin,ROE, Michael Bryan,HUDSON, Peter,HANDY, Rachel
申请号:
ES05773384
公开号:
ES2638114T3
申请日:
2005.08.24
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound according to general formula 1a or a compound that is a tautomer or a pharmaceutically acceptable salt thereof, ** Formula ** in which G is a group selected from general formula 2a, 3a, 4a, 5a and 6a, ** Formula ** in which: A1 is selected from CH2, CH (OH), NH, N-alkyl; O and S; A2 is selected from CH2, CH (OH), C (>; = O) and NH; A3 and A12 are independently selected from S, NH, N-alkyl, -C (R8)>; = CH-, -C (R8)>; = N-, -N>; = C (R8) - and - CH>; = C (R8) -; A4 and A13 are independently selected from C (R9) and N; A5 and A14 are independently selected from C (R10) and N; A6 is selected from CH2, NH, N-alkyl and O; A7 and A11 independently select between C and N; A8 and A9 are independently selected from CH, N, NH, N (CH2) bR11 and S; A10 is selected from -CH>; = CH-, CH, N, NH, N- (CH2) b-R11 and S; wherein the ring consisting of A7, A8, A9, A10 and A11 is aromatic; R1, R2 and R3 are independently selected from H, alkyl, O-alkyl, NO2, F, Cl and Br; R4 selects from H, alkyl, aryl, heteroaryl, - (CH2) c-R12 and ** Formula ** R7 selects from H, alkyl, aryl, heteroaryl and - (CH2) g-R14; R8, R9 and R10 are independently selected from H, alkyl, alkoxy, F, Cl, Br, CN, NH2, NO2, NH (alkyl), N (alkyl) 2; with the co-editions that when G is 3a, and R4 is H, alkyl, aryl, heteroaryl or - (CH2) c-R12, the ring containing A3, A4 and A5 is substituted in at least one position by alkyl, alkoxy, F, Cl, Br, CN, NH2, NO2, NH (alkyl) or N (alkyl) 2; and when G is 4a, R4 is H, alkyl, aryl, heteroaryl or - (CH2) c-R12, and A8 is NH, NCH3 or S, the ring containing A3, A4 and A5 is substituted in at least one position by alkyl, alkoxy, F, Cl, Br, CN, NH2, NO2, NH (alkyl) or N (alkyl) 2; R11 and R12 are independently selected from H, alkyl, aryl, heteroaryl, F, OH, O-alkyl, S-alkyl, O-acyl, NH2, NH-alkyl, N (alkyl) 2, NH-acyl, N ( alkyl) -acrylic, CO2H, CO2-alkyl, CONH2, CONH-alkyl, CON (alkyl) 2, CN and CF3; R13 selects from H, alkyl, aryl, heteroaryl, - (CH2) h-R
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