Abstract: Novel sterol derivatives of formula (I), in which: R1 represents a hydroxyl group or protected hydroxyl group, R2 represents a hydrogen atom and a double bond is present at c, or R1 and R2 together represent an oxo group and a double bond is present at b or double bonds are present at a and b; R3 represents a methyl group having ?- or ?-configuration; R4 and R5, which may be the same or different, are selected from hydrogen atoms and aliphatic, cycloaliphatic, araliphatic and aryl groups, or together with the nitrogen atom to which they are attached form a heterocyclic group; and X represents a polymethylene group containing 2–5 carbon atoms, an oxa group-containing analogue thereof in which a methylene group other than that attached to the —CO.NR4R5 moiety is replaced by an oxygen atom, or an unsaturated analogue thereof containing up to two double bonds.
Type:
Grant
Filed:
August 1, 2000
Date of Patent:
June 26, 2007
Assignee:
Research Institute for Medicine and Chemistry, Inc.
Inventors:
Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal
Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
Type:
Grant
Filed:
August 2, 1993
Date of Patent:
January 7, 1997
Assignee:
University of Southern California
Inventors:
Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
Abstract: This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3.alpha.-hydroxy,3.beta.-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3.alpha.-hydroxy,3.beta.-substituted-20-one form, which can be further modified at the 20-keto position.Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
Type:
Grant
Filed:
March 4, 1992
Date of Patent:
June 7, 1994
Assignee:
Cocensys Inc.
Inventors:
Hasan Tahir, Michael Bolger, Richard Buswell, Richard Gabriel, Jay Stearns
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
Type:
Grant
Filed:
August 13, 1991
Date of Patent:
August 3, 1993
Assignee:
University of Southern California
Inventors:
Michael Bolger, Kelvin W. Gee, Nancy C. Lan, Delia Belelli, Seid Mirsadeghi, Robert Purdy
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.
Type:
Grant
Filed:
February 13, 1991
Date of Patent:
May 4, 1993
Assignee:
University of Southern California
Inventors:
Kelvin W. Gee, Michael B. Bolger, Roberta E. Brinton, Deborah J. Burke, Bruce S. McEwen
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
Abstract: Bisnaphthalimides of the formula I ##STR1## where X.sup.1 to X.sup.4 and R have the meanings stated in the description, and their preparation are described. The compounds are cytotoxic towards human cells in vitro.
Type:
Grant
Filed:
March 1, 1988
Date of Patent:
October 17, 1989
Assignee:
Knoll AG
Inventors:
Miguel F. Brana, Jose M. C. Berlanga, Gerhard Keilhauer, Erich Schlick
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
Type:
Grant
Filed:
November 23, 1992
Date of Patent:
May 20, 1997
Assignee:
University of Southern California
Inventors:
Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan