9-substituted carbacyclin analogs

Details 9-substituted carbacyclin analogs 9-substituted carbacyclin analogs

C - Chemistry, Metallurgy

07

D

167/179, 260/235

C07D 295/18 (2006.01) A61K 31/557 (2006.01) C07C 405/00 (2006.01)

Patent

CA 1237127

ABSTRACT Novel pharmacological compounds of general formula: Image (IV) wherein s is one or 2; D is cis-?=C(R3)-, trans-?=C(R3)- or -?HCH2-, wherein R3 is H or F; X is Cl, I, -CF3 or -COOH; Y is cis-CH=CH-, trans-CH=CH-, -CH2CH2- or -C?C-; Z is (i) trans-CH2-CH=CH-, (ii) -CH2-(CH2)f-C(R4)2-, wherein f is zero, one, 2 or 3 and each R4 is the same and is H or F, or (iii) when R3 is H, -(Ph)-(CH2)?, wherein g is one, 2 or 3 and Ph is 1,2-, 1,3- or 1,4-phenylene, Q is -CH2OH, -CN, -C(O)CH3, or an ester, -CH2-amine, amide, cycloamine, carbonyl- amino or sulfonylamino group; with the proviso that when X is -COOH, Q is -COOR55, wherein R55 is C1-4alkyl; L is H:H, .alpha.-OR12:.beta.-H, .alpha.-H:.beta.-OR12, .alpha.-CH2OR12:.beta.-H or .alpha.-H:.beta.-CH2OR12, wherein R12 is H or an -OH-protecting group; M is .alpha.-OR12:.beta.-R14 and .alpha.-R14:.beta.-OR12, wherein R14 is H or -CH3; L1 is .alpha.-R15:.beta.-R16, .alpha.-R16:.beta.-R15 or a mixture thereof, wherein R15 and R16, independently, are H, F or -CH3, with the proviso that one of R15 and R16 is F only when the other is not -CH3; and R17 is (iv) cis-CH=CHCH2CH3, -(CH2)2CH(OH)CH3, -(CH2)3CH=C(CH3)2, phenyl, benzyl, phenylethyl, phenylpropyl, phenoxy, Image or Image (v) -CmH2mCH3, wherein m is an integer of from one to 5, or (vi) mono-, di- or tri-F, -Cl, -CF3, -C1-3alkyl or -C1-3alkoxy-( ring )-substituted-phenyl, -benzyl, -phenylethyl, -phenylpropyl or -phenoxy, with the proviso that not more than two substitutents are other than C1-3alkyl, with the proviso that when R17 is phenoxy or substituted-phenoxy, as defined above, R15 and R16 are not F; or Image , when taken together, is: (vii) Image 3-thienyloxymethyl, C4-7cycloalkyl, or mono-, di- or tri-C1-5alkyl-substituted- C4-7cycloalkyl, (viii) -C?CCqH2qCH3, wherein q is an integer of from 2 to 6, or (ix) -CpH2pCH=CH2, wherein p is an integer of from 3 to 7.

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