Benzopyran, benzothiopyran and benzofuran derivatives as...

Details Benzopyran, benzothiopyran and benzofuran derivatives as... Benzopyran, benzothiopyran and benzofuran derivatives as...

C - Chemistry, Metallurgy

07

D

C07D 405/12 (2006.01) A61K 31/435 (2006.01) C07D 409/12 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2129112

2129112 9316072 PCTABS00025 Compounds of formula (I) and pharmaceutically acceptable salts thereof, in which X1-(CH2)x-X2 and the aromatic carbon atoms to which they are attached form a 5-7 membered ring wherein: one of X1 and X2 is O, S or CH2 and the other is CH2; x is 1, 2 or 3; R1 is hydrogen, amino, halo, C1-6 alkyl, hydroxy or C1-6 alkoxy; R2 is hydrogen, halo, C1-6 alkyl, C1-6 alkoxy, nitro, amino or C1-6 alkylthio; R3 is hydrogen, halo, C1-6 alkyl, C1-6 alkoxy or amino; R4 and R5 are independently hydrogen or C1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c), wherein n1 is 1, 2, 3 or 4; n2 is 1 or 2; n3 is 2, 3, 4 or 5; q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2; Ra is hydrogen or a lipophilic group, such as C1-12 alkyl or aralkyl; or Ra is (CH2).GAMMA.R10 wherein r is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C(O)C1-6 alkyl, COC6H5, -CR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 wherein R11 and R12 are hydrogen or C1-6 alkyl; and R6, R7 and R8 are independently hydrogen or C1-6 alkyl; and R9 is hydrogen or C1-10 alkyl; or a compound of formula (I) wherein the CO-Y linkage is replaced by a heterocyclic bioisostere; and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

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