Abstract: The present invention relates to novel 4-pregenen-11?-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.
Type:
Grant
Filed:
November 9, 2012
Date of Patent:
December 9, 2014
Assignee:
Allergan, Inc.
Inventors:
Jeffrey L. Edelman, Alissar Nehme, Thomas C. Malone
Abstract: The present invention relates to novel 4-pregenen-11?-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.
Abstract: The present invention relates to compositions and methods for achieving the efficient allylic oxidation of organic molecules, especially olefins and steroids, under aqueous conditions. The invention concerns the use of dirhodium (II,II) “paddlewheel complexes, and in particular, dirhodium carboximate and tert-butyl hydroperoxide as catalysts for the reaction. The use of aqueous conditions is particularly advantageous in the allylic oxidation of 7-keto steroids, which could not be effectively oxidized using anhydrous methods, and in extending allylic oxidation to enamides and enol ethers.
Type:
Grant
Filed:
October 6, 2008
Date of Patent:
April 24, 2012
Assignee:
University of Maryland College Park
Inventors:
Michael P. Doyle, Arthur J. Catino, Hojae Choi, Jason M. Nichols
Abstract: The invention relates to a method for representing compounds of the general formula (1). The invention further relates to the hitherto unknown compounds of general formulas (5, 6 and 7) in the form of intermediate products and to the use of 4,4-dimethyl-3&bgr; hydroxypregna-8,14-diene-21-carboxylic acid esters of the general formula (1) for producing 4,4-dimethyl-5&agr;-cholesta-8,14,24-triene-3&bgr;-ol (2).
Abstract: A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is .alpha. to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal .gamma.-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.
Abstract: Novel compounds of the formula ##STR1## wherein either K' is oxygen or a K, a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3, the 17-position dotted line is a bond, R.sub.a and R.sub.b are individually selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms or K' is an oxygen, the 17-position dotted line is an epoxy and R.sub.a and R.sub.b have the meaning indicated above which are useful intermediates for the preparation of hydrocortisone.
Type:
Grant
Filed:
August 12, 1993
Date of Patent:
March 28, 1995
Assignee:
Roussel-Uclaf
Inventors:
Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.
Type:
Grant
Filed:
August 24, 1989
Date of Patent:
July 16, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Brian W. Metcalf, Dennis A. Holt, Mark A. Levy