Abstract: The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.
Type:
Grant
Filed:
June 7, 1994
Date of Patent:
February 28, 1995
Assignee:
Hoffmann-La Roche inc.
Inventors:
Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
Abstract: Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.
Type:
Grant
Filed:
May 1, 1992
Date of Patent:
June 1, 1993
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean-Marie Cassal, Nigel Gains, Eva-Maria Gutknecht, Georges Hirth, Hans Lengsfeld
Abstract: An optical probe enables the study of enzyme activity by absorbance spectroscopy or by sensitive fluorescence methods. In particular, the probe provides the ability to monitor the activity of cytochrome P-450.sub.scc enzyme, the rate limiting enzyme for steroid biosynthesis. Located on the inner mitochondrial membrane, P-450.sub.scc catalyzes the conversion of cholesterol to pregnenolone and isocapraldehyde by sequential oxidations of the cholesterol side chain. The fluorogenic probe includes a cholesterol-like steroid linked to a chromophore through a linking group. The chromophore is selected to have little optical response when linked to the steroid substrate and an enhanced optical response when cleaved from the substrate and linking group. Thus, a fluorescent anion that can be optically detected is generated by the side-chain cleavage reaction during steroidogenesis.
Type:
Grant
Filed:
December 20, 1991
Date of Patent:
May 4, 1993
Assignee:
The United States of America as represented by the United States Department of Energy
Inventors:
Babetta L. Marrone, Daniel J. Simpson, Clifford J. Unkefer, Thomas W. Whaley