17 - phenyl - 18,19,20 - trinor - pge amp; darr; 2 amp; darr; and pgf amp; darr; 2 amp; darr; amp; alpha; and medicines containing the same

摘要

1324737 Medicines comprising prostaglandins UPJOHN CO 8 Oct 1971 [2 Nov 1970 29 July 1971] 47017/71 Heading ASB [Also in Divisions C2 and C3] Pharmaceutical compositions, suitable for oral, rectal, parenteral or topical administration contain prostaglandin derivatives of the formulae or mirror images thereof or racemic compounds thereof, wherein E is CH 2 CHR 4 or trans-CH=CR 4 ; R 1 is H, C 1-8 alkyl, C 3-10 cycloalkyl, C 7-12 aralkyl, phenyl optionally substituted with 1 to 3 chlorine atoms or C 1-4 alkyl radicals, or ethyl substituted in the beta position with 3 chlorine atoms, 2 or 3 bromine atoms or 1, 2 or 3 iodine atoms; wherein R 2 , R 3 and R 4 are H or C 1-4 alkyl; CtH 2 t is a valence bond or C 1-10 alkylene optionally substituted with 1 or 2 fluorine atoms, with 1 to 7 carbon atoms between CR 3 OH and the benzene ring; T is C 1-4 alkyl, F, Cl, CF 3 or OR 9 , wherein R 9 is H, C 1-4 alkyl or 2-tetra-hydropyranyl; s is 0 to 3, with the proviso that not more than 2 T's are other than alkyl and when 2 or 3 T's are present as substituents they are the same or different; V is C 3-12 alkylene optionally substituted with 1 to 4 fluorine atoms, with 3 to 7 carbon atoms between CHR 2 and COOR 1 with the proviso that when 3 or 4 fluorine atoms are present, they are all substituents of the carbon atoms alpha and beta to COOR 1 , cis or trans -CH=CHA or C#CA, wherein A is C 1-10 alklene optionally substituted with 1 to 4 fluorine atoms with 1 to 5 carbon atoms between =CH- or #C- and COOR 1 , with the proviso that when 3 or 4 fluorine atoms are present, they are all substituents of the carbon atoms alpha and beta to COOR 1 , with the further proviso that when E is CH 2 CHR 2 , U is C 3-12 alkylene as defined above; and - indicates the attachment of the group to the ring is alpha or beta, or the pharmacologically acceptable salts thereof when R 1 is H, or C 1-8 alkanoates thereof, together with pharmaceutically acceptable carriers. The compound possess similar activities to natural prostaglandins. The compositions, especially those for topical administration, may contain other active ingredients such as antibiotics, for example, gentamycin, neomycin, polymyxin #, bacitracin, spectinomycin, and oxytetracycline, other antibacterials, for example, mafenide hydrochloride, sulphadiazine, furazolium chloride and nitrofurazone, and/or corticoid steroids, for example, hydrocortisone, prenisolone, methyl prednisolone and fluprednisolone.