Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...
Patent
1980-01-31
1982-08-24
Coughlan, Jr., Paul M.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Parasitic organism or component thereof or substance...
26032615, 26032613C, 26032616, 424274, 546271, 546273, 548259, 548305, 548371, A61K 3141, C07D24918
Patent
active
043460933
ABSTRACT:
The present invention provides heterocyclic oxypropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl, aralkyl or lower alkanoyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl, hydroxyalkyl, alkoxycarbonyl or alkanoyloxyalkyl radicals or together represent an alkylene radical, R.sub.4 is a hydrogen atom or a lower alkanoyl radical or an aroyl radical, R.sub.5 is a hydrogen atom or a lower alkyl radical or an aralkyl radical, R.sub.6 is a hydrogen atom or a lower alkyl radical, R.sub.7 is a hydrogen atom, a hydroxyl group or a lower alkyl radical, Z is a valency bond, a methylene radical or an oxygen or sulphur atom, Ar is a carbocyclic aryl radical or a pyridyl radical, R.sub.8, R.sub.9 and R.sub.10, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, lower alkyl radicals, lower alkenyl radicals, lower alkoxy radicals, aralkoxy radicals, allyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or lower alkanoylamino radicals or R.sub.8 and R.sub.9 together represent a lower alkylenedioxy radical or R.sub.7 and R.sub.8 together represent a --CH.sub.2 --O-- radical and A is --X.sub.1 --Y.sub.1, in which X.sub.1 is a methylene or --NR.sub.11 -- radical, R.sub.11 being a hydrogen atom or a lower alkyl radical, and Y.sub.1 is a methylene radical or .dbd.C.dbd.Q, Q being an oxygen or sulphur atom; or A is --X.sub.2 .dbd.Y.sub.2 --, in which X.sub.2 and Y.sub.2, which can be the same or different and signify nitrogen atoms or .dbd.C(R.sub.12)-- groups, R.sub.12 being a hydrogen atom or a lower alkyl or an alkoxycarbonyl radical, and when --X.sub.2 .dbd.Y.sub.2 -- represents a --CH.dbd.N-- group and R.sub.1 is an alkyl or aralkyl radical, because of the ability of indazole to tautomerise, this can also be localized on the nitrogen atom represented by Y.sub.2, with the proviso that Y.sub.1 or Y.sub.2 is joined to .dbd.N--R.sub.1 in general formula (I), and, when Q is an oxygen atom or --X.sub.2 .dbd.Y.sub.2 -- represents --CR.sub.12 .dbd.CR.sub.12 -- and Z is a valency bond or when --X.sub.1 --Y.sub.1 -- represents ##STR2## and Z is an oxygen atom or a valency bond, either the two symbols R.sub.2 and R.sub.3 do not simultaneously represent hydrogen atoms or R.sub.7 and R.sub.8 together must form a --CH.sub.2 --O-- radical; and the pharmacologically acceptable salts thereof.
The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
Furthermore, the present invention is concerned with the use of these compounds for the treatment of cardiac and circulatory diseases.
REFERENCES:
patent: 3751429 (1973-08-01), Seemann et al.
patent: 4140789 (1979-02-01), Jaeggi et al.
patent: 4189494 (1980-12-01), Engel et al.
patent: 4215134 (1980-07-01), Ross et al.
patent: 4235919 (1980-11-01), Berthold
Bartsch Wolfgang
Dietmann Karl
Friebe Walter-Gunar
Michel Helmut
Ross Carl H.
Boehringer Mannheim GmbH
Coughlan, Jr. Paul M.
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