C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/235.01
C07D 295/14 (2006.01) C07C 405/00 (2006.01) C07D 317/72 (2006.01) C07F 9/535 (2006.01) C07F 9/54 (2006.01)
Patent
CA 1219861
ABSTRACT OF THE DISCLOSURE The invention relates to 15-cycloaliphatic derivatives of 13,14-di- dehydro carboprostacyclins of formula (I) Image (I) wherein R is hydrogen or a C1-C6 alkyl group optionally substituted by a group Image wherein each of R3 and R4 is, independently, hydrogen or C1-C6 alkyl, or R3 and R4, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O and S; n is zero or an integer of 1 to 5; one of R1 and R2 is hydrogen or C1-C6 alkyl and the other is hydroxy; and B repre- sents: a) a C4-C7 monocycloaliphatic group either unsubstituted or substituted by one or more substituents chosen from C1-C6 alkyl, C2-C6 alkenyl and C1-C6 alkylidene; b) norbornyl; or c) adamantyl, and the pharmaceutically or veterin- arily acceptable salts of the compounds of formula (1). The invention also re- lates to pharmaceutically or veterinarily acceptable salts of compounds of for- mula I. The compounds of formula (I) show high platelet antiaggregating and disaggregating activity in that they strongly inhibit, prevent and reverse blood platelet aggregation. The compounds are therefore useful to inhibit platelet aggregation, to decrease adhesions, to prevent clot formation and to dissolve recently-formed clots. The platelet anti-aggregating activity is also associat- ed with a relaxation of the coronary arteries, so the compounds can be useful in preventing and treating myocardial infarctions and, in general, in treating or preventing thromboses, in treating conditions like atherosclerosis, arterio- sclerosis and, more generally, hyperlipidemia. The compounds also exhibit a vasodilatory, i.e. hypotensive, effect, so they may be useful for treating syndromes caused by arterial hypertension. They may also be used for treating obstructive pulmonary diseases such as, e.g. bronchial asthma. Further, they display antiulcerogenic and antisecretory activity.
438109
Gandolfi Carmelo
Mongelli Nicola
Farmitalia Carlo Erba S.p.a.
Fetherstonhaugh & Co.
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