Patent IL-132690-A (IL)
Title: Prostaglandin pharmaceutical compositions
IPC: A61P1/04
Filed: 1998-06-17
Abstract: Compounds, or their compositions, of the formula A-X1-NO2 for use as medicaments, in particular as drugs for the treatment of impotence, wherein: A=R(CRaRbO)q(COX)t wherein: t and u are integers and are equal to 0 or 1; X=O, NH, NR1c wherein R1c is a linear or branched alkyl having from 1 to 10 carbon atoms; Ra and Rb, equal or different from each other, are H, C1-C3 alkyl; R is a radical having the following formula: 1047 י" ב בסיון התשס" ד - June 1, 2004 where mo is an integer and can have a value of 0 or 1; where the meaning of the various substituents of formula III is as follows: when t=1, u=0 and mo=1; R1=H; an alkyl having from 1 to 6 carbon atoms, preferably from 1 to 3, or a free valence; R2-OH, O-such as to form with R1, when R1 is free valence, and with the carbon atom at position 15, a group C=O; R3, R4 equal or different one from the other, are equal to R1; or one of them is a bond O-, and the other is a free valence so that with the carbon atom C6 they form a group C=O; R5, R6, equal or different one from the other, are equal to R1; when both R5 and R3 are each a free valence, R5 and R3 form a double bond between C5 and C6; R7, R8, R9, R10, equal or different one from the other, have the same meaning of R1; when R7 or R9, and at the same time R8 or R10 are each a free valence, there is a double bond between C13 and C14; R11=R1; R12=R11 or OH; R13, R14, R15, R16, equal or different one from the other, are equal to R1; when R13 or R15, and at the same time R14 or R16, are each a free valence, there is a double bond between C3 and C2; R19, R20, equal or different one from the other, are equal to R1; when R6 or R5 is a free valence, and R19 or R20 is a free valence, there is a double bond between C4 and C5; R21, R22, R23, R24, equal or different one from the other, are equal to R1; R25, R26, equal or different one from the other, are equal to R1, but both R25 and R26 cannot be a free valence; R27 is a linear or branched alkyl having from one to six carbon atoms; B is equal to the group O=(a keto group with the carbon atom at position 9 of the prostaglandin molecule) or is OH, or -O-; when no aliphatic chain C7-C2 is at position 8, in its place there is the alkylaromatic residue: which is bound to formula (III) (B= -O-) in the following way: 1048 י" ב בסיון התשס" ד - June 1, 2004 wherein m1 is an integer from 1 to 6, preferably from 1 to 3; Ra and Rb, equal or different from each other, are as above defined; when t=o, u=1 and mo=1 the meanings of the various substituents are as above defined; when t=1, u=0 and mo=0 the meanings of the various substituents are as above defined and C16 is bound, optionally by a bridging group -O-, to an aromatic radical or an alkyl-aryl radical, where the aryl can be substituted, preferably with halogens, preferably with Cl, F; said aryl radical can also contain heteroatoms, such as O, N; the alkyl of the alkyl-aryl radical is an aliphatic chain from 1 to 3 carbon atoms, preferably -CH2-; X1 of formula A-X1-NO2 is a bivalent connecting bridge, chosen from the following: -Y Y is a linear or whenever possible branched C1-C20 alkylene oxygen terminated, preferably having from 2 to 5 carbon atoms or is a C5-C7 cycloalkylene oxygen terminated optionally substituted; where n3 is an integer from 0 to 3;