Abstract: A way to formulate prasterone to both increase its oral bioavailability, and decrease the variability of its oral bioavailability. In contrast to the approach taught by the prior art, the instant approach is amenable to scale-up to commercial scale. Further, the resulting product is amenable to analysis using standard, known quantitative analytical techniques; thus, unlike the prior art approach, the instant approach may be used to manufacture a product in conformity with applicable regulatory standards.
Abstract: Intravaginal DHEA is used for the treatment of at least one condition selected from the group consisting of female hypoactive sexual desire disorder, female sexual arousal disorder, female orgasm disorder and female sexual interest arousal disorder in a woman who either (1) is not suffering from symptoms of vulvo-vaginal atrophy and/or (2) is not suffering from moderate to severe dyspareunia.
Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
Abstract: A way to formulate prasterone to both increase its oral bioavailability, and decrease the variability of its oral bioavailability. In contrast to the approach taught by the prior art, the instant approach is amenable to scale-up to commercial scale. Further, the resulting product is amenable to analysis using standard, known quantitative analytical techniques; thus, unlike the prior art approach, the instant approach may be used to manufacture a product in conformity with applicable regulatory standards.
Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt thereof, may be made by a process including a triflating step by which a ketone of formula (II) is converted into a triflate of formula (III) in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12.
Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.
Type:
Grant
Filed:
April 12, 2001
Date of Patent:
August 26, 2003
Assignee:
Magainin Pharmaceuticals, Inc.
Inventors:
William A. Kinney, Steven Jones, Xuehai Zhang, Meena N. Rao, Michel Bulliard, Harold Meckler, Nancy Lee
Abstract: Intermediates for the preparation of a vitamin D derivative have the following formulas:
wherein R9 and R10 may be the same or different and each represents a hydrogen atom or a protecting group, and in Formula (5) the conjugated double bond may be protected by a protecting group.
Abstract: A method for promoting weight control by treating a subject with a therapeutic amount of one of the .DELTA.5-androstenes listed below to stimulate weight control without affecting appetite or inducing the synthesis of sex hormones. .DELTA.5-Androstenes providing the desired biological activities include:.DELTA.5-Androstene-3.beta.,7.alpha.-diol-17-one.DELTA.5-Androstene-3.beta.-ol-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17.beta.-triol.DELTA.5-Androstene-3.beta.,17.beta.-diol-7-one.DELTA.5-Androstene-3.beta.-acetoxy-7,16,17-trione.DELTA.5-Androstene-3.beta.,16.alpha.-dihydroxy-7,17-dione.DELTA.5-Androstene-3.alpha.-propionoxy-16.beta.-acetoxy-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17.beta.-triol-16-one.DELTA.5-Androstene-3.beta.,17.beta.-diol-7,16-dione.DELTA.5-Androstene-3.beta.,16.alpha.,17.beta.-triol-7-one.
Type:
Grant
Filed:
October 24, 1994
Date of Patent:
June 13, 1995
Assignee:
Humanetics Corporation
Inventors:
Henry A. Lardy, Ieva L. Reich, Yong Wei