Abstract: The présent invention relates to novel neurosteroids, especially derivatives of allopregnanolone and of epiallopregnanolone of formula (I) and the uses thereof as médicament for the treatment of neuropathologies, in particular neuropathies induced by the chemotherapy of a cancer. Thèse molécules according to the invention have both preventative and curative effects. The neurosteroids according to the invention may also be of use in the treatment of neurodegenerative disorders, in particular for preventing neuronal cell death. They may thus be used as neuroprotectants and/or as an agent that stimulâtes neuronal prolifération.

Abstract: This disclosure provides improved derivatives of artemisinin; pharamaceutical compositions containing these compounds; methods for preparing these compounds and compositions; methods of using these compounds and compositions for preventing, controlling or treating infectious diseases including but not limited to parasitic infectious diseases such as T. gondii infection, trypanosome parasite infection, plasmodia parasite infection, and cryptosporidium parasite infection; methods for preventing, controlling or treating toxoplasma infection; and methods for treating psychiatric disorders associated with toxoplasma infection including but not limited to schizophrenia using the disclosed compounds and compositions alone or in combination with one or more antipsychotic drugs.

Abstract: The present invention provides a method of producing (5?,7?)-3-spiro-2?-(1?,3?-dioxolan)-24-oxocholest-22-en-7-yl benzoate represented by the formula (I) including dissolving a crude product containing (5?,7?)-3-spiro-2?-(1?,3?-dioxolan)-24-oxocholest-22-en-7-yl benzoate, which is obtained by a reaction step, in methanol within the range of 1.5-3 in a mass ratio relative to the contained (5?,7?)-3-spiro-2?-(1?,3?-dioxolan)-24-oxocholest-22-en-7-yl benzoate to give a solution, adding the solution to water within the range of 5-30 in a mass ratio relative to the contained (5?,7?)-3-spiro-2?-(1?,3?-dioxolan)-24-oxocholest-22-en-7-yl benzoate to solidify (5?,7?)-3-spiro-2?-(1?,3?-dioxolan)-24-oxocholest-22-en-7-yl benzoate to give a suspension, separating the solid from the suspension, and drying the obtained solid. The compound obtained by the present invention is useful as a production intermediate for squalamine having potent antibacterial activity and antitumor activity.

Abstract: The invention provides sterile glucocorticosteroids and sterile formulations containing glucocorticosteroid and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or the lungs.

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: The invention relates to a 11-(substituted phenyl)-estra-4,9-diene derivative of formula I ##STR1## wherein A, X, R.sub.1 and R.sub.2 are as defined by the specification. The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.

Abstract: The present invention relates to novel imidazolium compounds and improved processes for the preparation of imidazolium cations with one or more imidazolium moieties optionally substituted with the same or different substituents, which are prepared from a reactant with at least one N--C--C--N group, by reacting with with an N-substituted or N,N-disubstituted thioformamide, formamide acetal or thioformamide acetal, in the presence of a halogenating agent. Examples of suitable halogenating agents include but are not limited to thionyl chloride, phosgene, and phosgene derivatives. Reactants containing more than one additional N--C--C--N group may also be used to prepare compounds with two or more imidazolium groups, by the procedures of the present invention. Certain compounds of the invention prepared from reactants with multiple N--C--C--N groups may have both unreacted N--C--C--N moieties and substituted imidazolium groups.

Abstract: Novel intermediate compounds of formula IV, V, VI, VII and VIII which are useful for the preparation of steroids of the formula ##STR1## wherein the substituents are defined in the specification.

Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.

Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.

Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.

Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.