C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 260/278
C07D 491/113 (2006.01) A61K 31/445 (2006.01) C07D 498/10 (2006.01)
Patent
CA 2023019
NOVEL 1-OXA-2-OXO-8-AZASPIROL[4,5]DECANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME Abstract The invention relates to novel l-oxa-2-oxo-8- -azaspiro[4,5]decane derivatives of the formula (I), (I) Image wherein X means oxygen or an ?NR group, wherein R stands for hydrogen, a C1-12alkyl, C3-6cyclo- alkyl, carbocyclic C6-10aryl or carbocyclic C6-10aryl-C1-4alkyl group, the two latter are optionally substituted on their aromatic part by one or more, same or different halogen(s), one or more C1-4alkyl or C1-4alkoxy group(s); R1 and R2 together represent a methylene group or, when X stands for an ?NR group, wherein R is as defined above, one of R1 and R2 may represent a hydroxyl group whereas the other is a methyl group; R3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C1-4alkyl or C1-4alkoxy or hydroxyl group(s); R4 means hydrogen, one or more halogen(s), C1-4alkyl, C1-4alkoxy, hydroxyl or trihalomethyl group(s); and n is 1, 2 or 3 as well as their acid addition and quaternary anmonium salts. The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of formula (I) possess calcium uptake- -inhibiting, antihypoxic and antianoxic properties and a low toxicity. Thus, they are useful for the treatment of brain damages of various origin.
Bodo Mihaly
Csomor Katalin
Gere Aniko
Groo Dora
Karpati Egon
Fetherstonhaugh & Co.
Richter Gedeon Vegyeszeti Gyar Rt.
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