Abstract: Novel angiostatic .DELTA..sup.4,9(11) -steroids (I), ##STR1## C.sub.21 -oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are useful in treating diseases of neovascularization such as cancer, diabetes and arthritis.
Type:
Grant
Filed:
December 21, 1995
Date of Patent:
October 26, 1999
Assignee:
Alcon Laboratories, Inc.
Inventors:
John W. Wilks, Thomas F. DeKoning, Paul A. Aristoff
Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.
Type:
Grant
Filed:
October 13, 1995
Date of Patent:
January 20, 1998
Assignee:
The Population Council, Center for Biomedical Research
Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
Abstract: Known pregnane derivatives are prepared by esterification of know androstane derivatives to give new esters of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen or formyl, andR.sub.3 is chlorine, hydroxy or an alkanoyloxy group of up to 6 carbon atoms,and reaction of the latter with Ag(I) and formic acid.
Type:
Grant
Filed:
March 20, 1989
Date of Patent:
September 11, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Helmut Hofmeister, Klaus Annen, Henry Laurent, Rudolf Wiechert
Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.
Type:
Grant
Filed:
February 16, 1989
Date of Patent:
August 14, 1990
Assignee:
The Upjohn Company
Inventors:
John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.
Type:
Grant
Filed:
February 24, 1988
Date of Patent:
April 3, 1990
Inventors:
Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung