C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/235.01
C07D 307/935 (2006.01) C07C 405/00 (2006.01)
Patent
CA 1115700
Abstract of the Disclosure This invention relates to optically active or racemic prostaglandins having the following general formula (I) Image wherein A is a member selected from the group consisting of (a) -CH2OH; (b) -COORa, wherein Ra is hydrogen, a C1-C12 alkyl group or a cation of a pharmaceu-tically or veterinarily acceptable base; (c) Image , wherein Rb and Rc are independently selected from the group consisting of hydrogen, C1-C6 alkyl and phenyl; the symbol --- represents a single or a double bond, wherein, when the the symbol ---- is a double bond, R3 is a hydrogen atom and R1 and R2 together form an oxo group, while, when the symbol ---- is a single bond, R3 is hydroxy and one of R1 and R2 is hydrogen and the other is hydroxy or acyloxy or R1 and R2, taken together, form an oxo group; one of R4 and R5 is hydrogen and the other is hydroxy, C1-C6 alkoxy or aralkoxy; R6 is hydrogen or C1-C4 alkyl; B is -(CH2)m- or -(CH2)m1-E-(CH2)m2-, wherein each of n, m1 and m2 is independently zero, 1, 2 or 3 and E is oxygen or sulphur; R is a member selected from the group consisting of (a') C1-C6 alkyl; (b') C1-C6 alkoxy; (c') C1-C6 trihaloalkyl; (d') halogen; (e') amino; (f') Image , hydrogen where- in Rd and Re are independently selected from the group consisting of hydrogen, phenyl, benzoyl, C1-C6 alkyl, C1-C6 aliphatic acyl; (g') phenyl, unsubstituted or substituted by one or more substituents selected from the group consisting of C1-C6 alkoxy and halogen; and (h') phenoxy, unsubstituted or substituted by one or more substituents selected from the group consisting of C1-C6 alkoxy and halogen. It also relates to a process for the preparation of these compounds. The compounds of formula (I) may be used for the same Therapeutical indications as natural prostaglandins with respect to which,however, they offer the advantage of being no substrates for the enzyme 15- prostaglandin dehydrogenase, which as is known, quickly inactivates natural prostaglandins, and, moreover, are characterized by a more selective therapeutical action. The compounds of formula (I) furthermore inhibit the use of natural prostaglandins as substrate by the same enzyme. In particular the compounds of the invention have selective leuteolytic, abortifacient and labor-inducing activity and extremely low undesired gastro-intestinal effects.
279487
Ceserani Roberto
Faustini Franco
Gandolfi Carmelo
Moretti Walter
Usardi Maria M.
Farmitalia Carlo Erba S.p.a.
Fetherstonhaugh & Co.
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