Anti-glaucomatous pharmaceutical composition and the process for

Details Anti-glaucomatous pharmaceutical composition and the process for Anti-glaucomatous pharmaceutical composition and the process for

1994-05-25

1996-04-09

Robinson, Allen J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514178, 514181, A61K 3158, A61K 3156

Patent

active

055062202

DESCRIPTION:

BRIEF SUMMARY
This application has been filed under 37 CFR 371 from patent application PCT/FR92/00549 which was filed on Jun. 18, 1992.
The invention relates to the domaine of medicinal chemistry and in particular to the pharmacotechnology domain.
A specific subject of the invention is pharmaceutical compositions for ocular use, characterised in that they contain as active ingredient, at least one compound of steroidal structure selected from the group consisting of
A-19-NOR PREGNA 4,6-DIENES OF GENERAL FORMULA I ##STR1## in which
R1 represents a hydroxy, an alkoxy and an acyloxy radical
R2 represents hydrogen or a lower alkyl radical
R and R' together form a keto, hydroxyimino, alkoxyimino or acyloxyimino group
or separately, when R.dbd.H, R' is a hydroxy, an alkoxy or an acyloxy group
and R3 represents a lower alkyl radical having 1 to 3 carbon atoms
R-19-NOR 4,6-DIENES OF GENERAL FORMULA II ##STR2## in which
R2 represents a hydrogen atom or linear or branched chain an alkyl radical having 1 to 6 carbon atoms, R7 represents a lower alkyl radical, identical to or different from R2, having 1 to 6 carbon atoms, as a linear or branched chain
and R3 is defined as previously
C-COMPOUNDS OF 19-NOR PREGNENIC STRUCTURE, OF GENERAL FORMULA III ##STR3## in which
R1 represents a hydroxy, an alkoxy, an acyloxy or an alkyl radical having 1 to 4 atoms
R2 represents an hydrogen or a lower alkyl radical as a linear or branched chain having 1 to 4 carbon atoms
Z represents hydrogen, an alkyl radical or an acyl radical
and the dotted line represents an optional carbon-carbon double bond
D-19-NOR PREGNENIC DERIVATIVES OF GENERAL FORMULA IV ##STR4## in which
R1 represents a hydroxy, an alkoxy, an acyloxy or an alkyl radical having 1 to 4 carbon atoms
R2 represents a hydrogen or a lower alkyl radical, as a linear or branched chain, having 1 to 4 carbon atoms
and the dotted line symbolizes an optional carbon-carbon double bond
E-6-HALOMETHYL 19-NOR PREGNENIC DERIVATIVES OF GENERAL FORMULA V ##STR5## in which
X represents a halogen atom
R1 and R2 are defined as previously
and the dotted line symbolizes an optional carbon-carbon double bond
F-COMPOUNDS OF 19-NOR ANDROSTENIC STRUCTURE CORRESPONDING TO GENERAL FORMULA VI ##STR6## in which
R1 represents a hydrogen, a lower alkyl or an acyl radical derived from an organic carboxylic acid having 1 to 10 carbon atoms
R' represents a hydrogen or a lower alkynyl
R represents a methyl or ethyl
R5 represents two hydrogen or the group .dbd.O, .dbd.N--OH or ##STR7## in which R4 represents a hydrogen or the acyl residue of an organic carboxylic acid
and R3 represents two hydrogens or .dbd.CH2
G-PREGNADIENES OF GENERAL FORMULA VII ##STR8## in which
R.sub.9 represents a lower alkyl or lower cycloalkyl radical
R1 and R3 are defined as previously
H-PREGNENIC DERIVATIVES OF GENERAL FORMULA VIII ##STR9## in which the dotted line represents an optional double bond
and R1 is defined as previously
I-3,2,0-DIOXO DELTA 4-PREGNENIC COMPOUNDS CORRESPONDING TO GENERAL FORMULA IX ##STR10## in which
R1 represents a free, etherified or esterified hydroxyl radical or a lower alkyl radical
R3 represents hydrogen or a lower alkyl radical having 1 to 4 carbon atoms
and the dotted line symbolizes 2 hydrogens or a carbon-carbon double bond
J-11,18-EPOXYANDROSTENIC COMPOUNDS OF GENERAL FORMULA X ##STR11## in which, the wavy line symbolizes an alpha or beta orientation
and R.sub.10 represents a hydrogen or an acyl radical derived from an organic carboxylic acid having 1 to 10 carbon atoms
K-CORTICOSTEROIDS OF GENERAL FORMULA XI ##STR12## in which
R.sup.11 represents hydrogen or an acyl radical derived from an organic carboxylic acid having 1 to 10 carbon atoms
and L-ANDROSTENIC COMPOUNDS OF GENERAL FORMULA XII ##STR13## in which
R1 represents a hydrogen, a lower alkyl radical, a methoxy alkyl, an acyl residue derived from an organic carboxylic acid or an alkyl carbonic acid
R.sub.12 represents a hydrogen or an optionally substituted alkyl radical
R3 represents a hydrogen, a halogen or a lower alkyl
and the wary line symbolizes an

REFERENCES:
patent: 4383992 (1983-05-01), Lipari

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