C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
260/235.03
C07C 405/00 (2006.01) C08B 37/16 (2006.01)
Patent
CA 1275407
ABSTRACT OF THE DISCLOSURE The invention provides 9-halo-15-cycloalkyl prostaglandin derivatives of formula I Image (I) where R1 is hydrogen or methyl, R2 is fluorine or chlorine, n is 0 or 1 and, wherein R1 is hydrogen, their salts with physiologically tolerable bases or their cyclodextrin cla- thrates; processes for their manufacture and pharmaceutical compositions containing them. The 15-cycloalkyl prostag- landins of formula I in accordance with the invention are outstanding because of their properties typical of PGD2, i.e. they bind well to the PGD2 receptor, but poorly to the PGE2 and PGI2 receptor. Investigations of cattle coronary arteries and the pulmonary artery or rabbits likewise indicate an effective PGD2 profile of formula I compounds. The compounds lower blood pressure in rats after intravenous infusion. The compounds of the invention inhibit the secretion of gastric acid, display a cytoprotective and ulcer-healing effect and thus counteract the undesirable consequences of nonsteroidal antiphlogistics (prostaglandin synthesis inhibitors). They have the effect of regulating cardiac-rhythm disorders and inhibiting the aggregation of platelets.
504733
Loge Olaf
Raduchel Bernd
Schillinger Ekkehard
Skuballa Werner
Vorbruggen Helmut
Marks & Clerk
Schering Aktiengesellschaft
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