摘要:
The phenylalkan(en)oic acids of the formula: ##STR1## wherein A isi) --NHCO--,ii) --O--iii) --NHSO.sub.2 --,iv) --CO--v) --CH.sub.2 -- orvi) --CH(OH)--;W isi) C1-13 alkylene,ii) phenylene oriii) ##STR2## R.sup.1 is i) hydrogen,ii) C1-4 alkyl,iii) --COOH,iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 member mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,v) ##STR3## vi) --CH.sub.2 OH; or A, taken together with W and R.sup.1, isi) ##STR4## ii) ##STR5## iii) --N--(SO.sub.2 R.sup.6).sub.2, iv) ##STR6## or v) ##STR7## two R.sup.2 are, same or different, i) hydrogen,ii) C1-4 alkyl oriii) 4-7 membered saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total, or two R.sup.2, taken together with a nitrogen to which they are attached, form saturated or unsaturated,i) 7-14 membered, bi- or tri-cyclic hetero ring containing one nitrogen as a hetero atom, orii) 4-7 mebered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total;Y is ethylene or vinylene;D isi) --Z--B orii) ##STR8## Z is C3-11 alkylene or alkenylene R is ##STR9## or Z taken together with B, is C3-22 alkyl;R.sup.3 isi) hydrogen,ii) halogen,iii) C1-8 alkyl, alkoxy or alkylthio, oriv) C2-8 alkenyl, alkenyloxy or alkenylthio;n is 1-3;R.sup.4 is C1-7 alkylene;R.sup.5 isi) C1-12 alkyl,ii) C2-12 alkenyl,iii) C5-7 cycloalkyl or pp2 iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;Two R.sup.6 are, same or different,i) C1-7 alkyl,ii) benzyl oriii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; andTwo R.sup.7 are, same or different, C1-4 alky; with the proviso thati) --A--W--R.sup.1 should bind to 3- or 4- carbon in benzene ring, andii) when W phenylene or ##STR10## A should not represent --O--, --CO--, --CH.sub.2 -- or --CH(OH)--; and non-toxic salts thereof,possess an antagonistic activity on leukotriene B.sub.4, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B.sub.4.
摘要:
A process for producing optically active 16-substituted prostaglandins and new 16-substituted prostaglandins produced thereby which are useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy.
摘要:
Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of --CH.sub.2 --CH-- or trans --CH.dbd.C--;T.sub.1 and T.sub.2 are attached to adjacent carbon atoms;T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl;Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms. Also disclosed are methods for preparing such prostaglandin analogues.
摘要:
11-Substituted prostaglandins E.sub.1, E.sub.2 and F.sub.2.alpha. useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy and a process for preparing these prostaglandins.