Abstract: The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones. The present invention also provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.

Abstract: The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a &bgr;-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5) alkyl or CF3; R3 is &bgr;H, &bgr;CH3 or together with R1 forms a &bgr;-epoxide or R3 is absent if there is a 5-10 double bond; R4 is H, lower alkyl; Y is [H, H], [OH, H], ═O, [OH, lower alkyl], [OH, (C2-C5)alkenyl], [OH, (C2-C5)alkynyl] or (C1-C6) alkylidene, whereby said alkyl, alkenyl, alkynyl and alkylidene is optionally halogenated; ═NOR5, whereby R5 is H, lower alkyl; dotted lines represent an optional double bond, or prodrugs thereof for the treatment of arthritic diseases and/or autoimmune diseases.

Abstract: This invention describes the new 17-difluoromethylene-estratrienes of general formula I ##STR1## in which R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group,R.sup.5 is a methyl or ethyl group, andR.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group in .alpha.- or .beta.-position,R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyloxy group in .alpha.- or .beta.-position,R.sup.4 is a hydrogen atom in .alpha.- or .beta.-position, and A, B, D, E and G each is a hydrogen atom, and optionally at least one of substituent pairsG and R.sup.2, R.sup.2 and R.sup.4, R.sup.4 and A, A and R.sup.3, B and D, D and E is a double bond.

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6.alpha. and 7.beta. oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6.alpha. and 7.beta. oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and .delta.-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: Compounds of the formula I ##STR1## a process for their preparation, their use in the treatment of autoimmune disorders as well as new intermediates for their preparation.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: A process for enantioselectively epoxidising a prochiral olefin, which process comprises reacting a prochiral olefin with a source of oxygen in the presence of a salen catalyst and a source of an electron donating ligand, characterized in that the donor ligand is isoquinoline N-oxide or a compound having donor ligand activity and having substantially the same solubility characteristics as isoquinoline N-oxide.

Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 represents a C1-10 alkyl group which may be substituted by one or more hydroxyl groups, R.sub.2 represents a hydrogen atom or a hydroxyl group, and R.sub.3 represents a hydrogen atom or a hydroxyl group; their intermediates; as well as synthesis processes of these compounds and intermediates are disclosed. The compounds of this invention, vitamin D derivatives substituted by sulfur atoms at the 22-position have a strong inhibitory effect against proliferation of keratinocytes.

Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.

Abstract: A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is .alpha. to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal .gamma.-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.

Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.