Patent classifications
C07J13/005
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.7, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
METHODS FOR PREPARING BILE ACIDS
The present disclosure provides methods of preparing cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, and novel and useful synthetic intermediates, for example, as described for methods 1, 1A, 1B, 2, 3, 3A, and 4. The method can start with a plant derived steroid as a starting material, such as dehydroepiandrosterone (DHEA) or Acetyl-dehydroepiandrosterone (Ac-DHEA). Also provided are pharmaceutical or cosmetic compositions and uses thereof, which comprise one or more of cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, which is of high purity, for example, free of animal derived impurities.
Process for the preparation of estetrol
The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is Si(R.sup.2).sub.3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is Si(R.sup.2).sub.3.
Oxysterols and methods of use thereof
Compounds are provided according to Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.7, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
STEROLS AS NOVEL IMMUNOMODULATORY AGENTS AND THEIR USE AS VACCINE ADJUVANTS
Disclosed herein are methods of using immunomodulatory sterols as vaccine adjuvants. Accordingly, certain embodiments relates to pharmaceutical compositions containing at least one antigen and at least one immunomodulatory sterol; and, methods of inducing an immunomodulatory response in a patient by administering an immunomodulatory-effective amount of at least one immunomodulatory sterol.
Process for preparation of corticosteroids
The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen; ##STR00001##
Neuroactive steroids and methods of use thereof
3beta, 17beta disubstituted steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
##STR00001##
Methods for preparation of bile acids and derivatives thereof
The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R.sub.1 is H, -OH, -OH, or an oxo group. ##STR00001##
NOVEL PROCESS FOR PREPARATION OF CORTICOSTEROIDS
The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen;
##STR00001##