Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...
Patent
1977-11-04
1979-03-20
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Recombinant or stably-transformed bacterium encoding one or...
424330, 424331, A61K 3112, A61K 3124, A61K 31135
Patent
active
041454413
ABSTRACT:
Compounds having the formula: ##STR1## wherein R represents hydrogen or a straight or branched C.sub.1 -C.sub.5 alkyl group; and R.sub.1 and R.sub.2 which may be the same or different represent an acyl member which is alkanoyl having 1-22 carbon atoms, alkenoyl having one or two double bonds and having 4-22 carbon atoms, cycloalkyl-C.sub.n H.sub.2n ##STR2## having a total of 4-10 carbon atoms of which 3-7 are ring carbon atoms in cycloalkyl and wherein n is zero, one, or two, phenoxyacetyl, naphthalenecarbonyl, pyridinecarbonyl, phenyl-C.sub.n H.sub.2n ##STR3## wherein n is zero, one or two and phenyl is unsubstituted or is substituted by 1-3 alkyl having 1-4 carbon atoms, alkoxy having 1-4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2-8 carbon atoms, or alkanoylamino having 1-6 carbon atoms groups; ##STR4## wherein R.sub.3 may be hydrogen, hydroxyl or a member defined in accordance with R.sub.1 and R.sub.2 above or ##STR5## wherein R.sub.8 and R.sub.9, which may be the same or different represent hydrogen, a C.sub.1 -C.sub.8 open chain or cycloalkyl, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.5 and R.sub.6 which may be the same or different represent hydrogen, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 acyloxyalkyl, phenyl, naphthyl, substituted phenyl or naphthyl, the substituents of which are selected from the group consisting of C.sub.1 -C.sub.5 acyloxy, halogen (Cl, Br, I) or wherein R.sub.5 and R.sub.6 together with the carbon atom to which they are attached form a cyclopentane or cyclohexane ring or a 5- or 6- membered heterocyclic ring (e.g., piperidine, N-(C.sub.1 -C.sub.5)alkylpiperidine, N-acylpiperidine, pyrrolidone, etc.; and wherein R.sub.7 represents hydrogen or a (C.sub.1 -C.sub.7) straight or branched alkyl; and the nontoxic pharmaceutically acceptable acid addition salts thereof are disclosed.
Upon rectal application to a warm-blooded animal, e.g., human, theraeutic anti-hemorrhoidal activity (reduction in hemorrhoidal swelling) is observed.
REFERENCES:
patent: 3809714 (1974-05-01), Hussain et al.
patent: 3825583 (1974-07-01), Hussain et al.
patent: 3839584 (1974-10-01), Hussain et al.
patent: 3868401 (1975-02-01), Hussain et al.
Friedman Stanley J.
Interx Research Corporation
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