Abstract Novel compounds of the formulae: ##STR1## wherein R 2 and R 6 are hydrogen when Z 2 is a single bond and when Z 2 is a double bond R 2 and R 6 are absent; R 3 is a keto, ##STR2## R 7 is OH or OR 9 ; R 8 is H or OH; R 9 is acyl or alkoxyalkyl; R 10 is H or ##STR3## Z 1 is --CH 2 CH 2 -- or cis --CH=CH--; Z 2 is a single bond or a double bond; Z 3 is a single bond or a double bond when R 4 and R 5 are hydrogen; Z 4 is --CH 2 CH 2 -- or trans --CH=CH--; Z 5 is --CH 2 CH 2 -- or cis --CH=CH--; n is 2 to 5, m is 1 to 3, and x is 1 to 2. The compounds are useful for regulating blood pressure, for stimulating smooth muscles, for inhibiting gastric secretion and inhibiting platelet aggregation and they possess improved biological stability and enhanced membrane permeability to serve as an in vivo reservoir of the prostaglandin to ensure the biological availability of the prostaglandin.
A pharmaceutical aerosol formation for inhalation therapy wherein the aerosol is comprised of about 100 mg to 500 mg of a prostonate selected from the group consisting of 1,4-diaminobutane-11α,15(S)-dihydroxy-9-oxo-5-cis,13-trans-prostadienoate; 15(S)-hydroxy-9-oxo-10,13-trans-prostadienoate; 9α,11α,15(S)-trihydroxy-5-cis,13-trans-prostadienoate; and 9α,11α,15(S)-trihydroxy-5-cis,13-trans,17-cis-prostatrienoate wherein the prostonate is mixed with an inert non-toxic gaseous propellant and a pharmaceutically acceptable cosolvent for the propellant and the prostonate.
Claim 2
Dependent Claim
55 words
A pharmaceutical aerosol formation for inhalation therapy wherein the aerosol is comprised of about 100 mg to 500 mg of a prostonate selected from the group consisting of 1,4-diaminobutane-11α,15(S)-dihydroxy-9-oxo-5-cis,13-trans-prostadienoate; 15(S)-hydroxy-9-oxo-10,13-trans-prostadienoate; 9α,11α,15(S)-trihydroxy-5-cis,13-trans-prostadienoate; and 9α,11α,15(S)-trihydroxy-5-cis,13-trans,17-cis-prostatrienoate wherein the prostonate is mixed with an inert non-toxic gaseous propellant and a pharmaceutically acceptable cosolvent for the propellant and the prostonate.