Patent ID: 6699861
Filing Date: 2004-03-02
Classification: A61P,C07D

Abstract:
A dihydroquinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein:either R1 and R1â€² together form an oxo group and R2 is hydrogen, C1-C4 alkyl, â€”(C1-C4 alkyl)â€”B, â€”(C1-C4 alkyl)â€”COB, â€”(C1-C4 alkyl)â€”COâ€”(C1-C4 alkyl)â€”B, â€”(C1-C4 alkyl)â€”CO2â€”(C1-C4 alkyl)â€”B, â€”(C1-C4 alkyl)â€”CO2â€”(C2-C4 alkenyl)â€”B or â€”(C1-C4 alkyl)â€”CONHâ€”(C1-C4 alkyl)â€”B wherein B is â€”CO2H, hydroxy, C1-C4 alkoxy, amino, (C1-C4 alkyl)amino, di-(C1-C4 alkyl)amino or a 5- or 6-membered heterocyclic group, or R1â€² and R2 together form a bond and R1 is â€”Sâ€”(C1-C4 alkyl), â€”NHRâ€² or â€”NHCORâ€² wherein Râ€² is aryl or C1-C4 alkyl; R3 is â€”(CH2)pâ€”A wherein p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is â€”NAâ€²Aâ€³ wherein Aâ€² and Aâ€³ are the same or different and are each a C1-C4 alkyl group; either R4 is hydrogen, oxo or C1-C4 alkyl and R5 is hydrogen, C1-C4 alkyl or halogen, or R4 and R5, together with the carbon atoms to which they are attached, form a 5- or 6-membered carbocyclic ring, the symbol . . . indicating a double bond to R4 when R4 is oxo and a single bond to R4 when R4 is hydrogen or C1-C4 alkyl or forms a carbocyclic ring with R5; X1 is â€”Oâ€”, â€”Sâ€” or â€”NRâ€³â€” wherein Râ€³ is hydrogen, C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl; Y is a divalent aryl or heteroaryl group; R6 is hydrogen, oxo or C1-C4 alkyl, the symbol . . . indicating a double bond to R6 when R6 is oxo and a single bond to R6 when R6 is hydrogen or C1-C4 alkyl; X2 is â€”Oâ€”, â€”Sâ€” or â€”NRâ€³â€” wherein Râ€³ is as defined above; m is from 1 to 4; and R7 is pyridyl, pyrimidyl, imidazolyl, triazolyl, â€”(C1-C4 alkyl)-imidazolyl, or â€”(C1-C4 alkyl)-triazolyl, the aryl moieties in the R1 to R7 substituents being unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from halogen, hydroxyl, C1-C4 alkyl, C1-C4 alkoxy, amino, (C1-C4 alkyl)amino and di-(C1-C4 alkyl)amino substituents; said 5- or 6-membered carbocyclic ring being unsubstituted or substituted by 1 or 2 substituents selected from halogen, hydroxyl, C1-C4 alkyl, C1-C4 alkoxy, amino, (C1-C4 alkyl)amino and di-(C1-C4 alkyl)amino substituents; the said divalent heteroaryl group being unsubstituted or substituted by up to 3 substituents selected from halogen, hydroxyl, CF3, CCl3, C1-C4 alkyl, C1-C4 alkoxy, amino, (C1-C4 alkyl)amino and di-(C1-C4 alkyl)amino substituents; said 5- or 6-membered heterocyclic group being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, hydroxyl, CF3, CCl3, CO2H, amino, (C1-C4 alkyl)amino and di-(C1-C4 alkyl)amino substituents; said 5- or 6-membered N-containing heterocyclic ring being unsubstituted or substituted by up to 3 substituents selected from halogen, hydroxyl, CF3, CCl3, C1-C4 alkyl, C1-C4 alkoxy, phenyl, -phenyl-CO2H, -phenyl-CO2â€”(C1-C4 alkyl), amino, (C1-C4 alkyl)amino, di-(C1-C4 alkyl)amino, â€”CO2H, â€”CO2â€”(C1-C4 alkyl) and a 5- or 6-membered heterocyclic group; and the alkyl, alkenyl and alkynyl moieties in the R1 to R7 substituents being unsubstituted or substituted with up to 3 substituents selected from hydroxy, halogen, amino, (C1-C4 alkyl)amino and di-(C1-C4 alkyl)amino substituents.