C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/235.01
C07D 311/94 (2006.01) C07C 43/225 (2006.01) C07C 43/23 (2006.01) C07D 405/10 (2006.01) C07D 413/10 (2006.01)
Patent
CA 1212669
ABSTRACT Novel pharmacological compounds of general formula: Image (I) wherein: R is -O- or -CH2-; Z is -CH2-, -CH2CH2-, -CF2- or -CF2CH2-; or Z-R, when taken together, is trans-CH=CH- or trans-CH=CHCH2-; Y is -CH2CH2-, cis-CH=CH-, trans-CH=CH- or -C?C-; Q is -CH2OH, -CN, -C(O)CH3, or an ester, -CH2- amine, amide, cycloamine, carbonylamino or sulfonylamino group; R1 is =O, 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 or .alpha.-R14:.beta.-OR12, wherein R14 is H or -CH3; L1 is .alpha.-R15:.beta.-R16, .alpha.-R14:.beta.-R15 or a mixture there- of, wherein R15 and R16, independently, are H, F and -CH3, with the proviso that one of R15 and R16 is F only when the other is not -CH3; and R17 is (i) cis-CH=CHCH2CH3, -(CH2)2CH(OH)CH3, -(CH2)3CH=C(CH3)2, phenyl, benzyl, phenylethyl, phenylpropyl, phenoxy, Image , Image , (ii) -CmH2mCH3, wherein m is an integer of from one to 5, or (iii) mono-, di- and tri-F, -Cl, -CF3, -C1-3alkyl and -C1-3alkoxy-(phenyl)- substituted-phenyl, -benzyl, -phenylethyl, -phenylpropyl or -phenoxy, with the proviso that not more than two sub- stituents 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 (iv) Image , 3-thienyloxymethyl, C4-7cycloalkyl, or mono-, di- or tri-C1-5alkyl-substituted-C4-7cycloalkyl, (v) -C?CCqH2qCH3, wherein q is an integer of from 2 to 6, or (vi) -CpH2pCH=CH2, wherein p is an integer of from 3 to 7.
420222
Macrae & Co.
Upjohn Company (the)
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