2-mercaptomethylene-tetrahydronaphthalene and...

C - Chemistry – Metallurgy – 07 – C

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C07C 323/60 (2006.01) A61K 31/165 (2006.01) A61K 31/19 (2006.01) A61K 31/21 (2006.01) A61K 31/36 (2006.01) C07C 327/32 (2006.01) C07C 327/34 (2006.01)

Patent

CA 2067408

This invention relates to novel 2-mercaptomethylene- tetrahydronaphthalene derivatives of the formula (see formula I) wherein n is an integer 2, Z is the radical -C(O)OR, or a phenyl group unsubsti- tuted or substituted with from 1 to 3 substituents selected from the group consisting of OH, C1-C4 alkoxy, and methylenedioxy, R is H, C1-C4 alkyl, or benzyl, R1 is H or -C(O)-A, wherein A is C1-C4 alkyl, or phenyl, and B is a radical of the formula <see formula II or III> wherein m is an integer 0 to 5, and R2 is H, C1-C4 alkyl, -CH2-OH, -CH(OH)-CH3, -CH2CH2SCH3, phenylmethyl, 4-hydroxy-phenylmethyl or OH, with the proviso that R2 cannot be OH when m is 0, which are useful as enkephalinase inhibitors.

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