Back to results
US 5,939,545 AGranted
Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series
AssigneeCoCensys, Inc.
InventorsRavindra B. Upasani, Haiji Xia, Derk Hogenkamp
Life of this patent
Estimating the term…
Abstract
Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
Claims17
A compound of the formula:
- ##STR2## wherein:
- R is hydrogen, halogen, lower alkoxy, dialkylamino, alkyl or substituted alkyl;
- R.sub.1 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted alkynyl, optionally substituted aralkynyl, alkoxyalkyl, aminoalkyl, cyanoalkyl, thiocyanoalkyl, azidoalkyl, arylalkyl, arylalkenyl, optionally substituted aralkylalkynyl, alkanoyloxyalkynyl, optionally substituted heteroaryloxyalkynyl, oxoalkynyl or a ketal thereof, cyanoalkynyl, optionally substituted heteroarylalkynyl, hydroxyalkynyl, alkoxyalkynyl, aminoalkynyl, acylaminoalkynyl, mercaptoalkynyl, hydroxyalkynyl dioic acid hemi-ester or a salt thereof, or alkynyloxyalkynyl;
- R.sub.2 is hydrogen, hydroxy, alkoxy, alkanoyloxy, carbalkoxyl, a keto group or amino group;
- R.sub.3 is imidazolylacetyl, pyrazolylacetyl, triazolylacetyl, tetrazolylacetyl, purinylacetyl or uracilacetyl, any of which is optionally substituted;
- R.sub.4 is hydrogen or methyl;
- R.sub.5 is hydrogen;
- R.sub.6 is hydrogen, alkanoyl, aminocarbonyl or alkoxycarbonyl;
- R.sub.7 is hydrogen, halogen, hydroxy, alkoxy, alkanoyloxy or carbalkoxyl;
- R.sub.8 is hydrogen or halogen;
- R.sub.9 is hydrogen, halogen, alkyl, alkoxy, arylalkoxy or amino;
- and
- R.sub.10 is hydrogen, halogen, alkyl, haloalkyl, hydroxy, alkoxy, alkanoyloxy, carbalkoxyl, cyano, thiocyano or mercapto;
- or a physiologically acceptable 3-ester thereof.
11 more elements
The compound 3.alpha.-hydroxy-2.beta.-ethynyl-5.alpha.-pregnan-20-one.
Dependencies are inferred from the claim text.