Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1

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

Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.

Abstract: 17-Aryl -5.alpha.,14.beta.-androstane, androstene and androstadiene derivatives of formula (I): ##STR1## wherein the symbol --- represents a single or a double bond; when the double bond is not present in the 4 or 5 position, the hydrogen in position 5 has the .alpha. configuration;Y is oxygen or guanidinoimino, when --- in position 3 is a double bond;Y is hydroxy, OR.sup.2 or SR.sup.2, when in position 3 is a single bond and has an .alpha. or .beta. configuration;R is a substituted or unsubstituted aryl ring; andR.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.

Abstract: Compositions of sterodial glycosides are described wherein the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon, or similar stable linkage, and methods of using the compositions to treat patients by binding to and/or blocking cellular receptors for a variety of diseases including cancer, inflammation, and autoimmune diseases.

Abstract: Intermediate compounds of a formula selected from the group consisting of ##STR1## which are useful intermediates for the preparation of final products of the formula ##STR2## wherein the substituents are defined in the specification.

Abstract: Compounds of the general formula (1) ##STR1## wherein X represents the residue of the A, B and C rings of a asteroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R.sup.14 represents a hydrogen atom and R.sup.15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R.sup.14 and R.sup.15 together represent a double bond, and R.sup.16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or pharmaceutically acceptable acid addition salts, are used for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.

Abstract: Compounds of the general formula (1) ##STR1## wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R.sup.14 represents a hydrogen atom and R.sup.15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R.sup.14 and R.sup.15 together represent a double bond, and R.sup.16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or phannaceutically acceptable acid addition salts, are useful for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.

Abstract: The invention is related to substituted 2.beta.-morpholino-androstane derivatives, bonded at their 2.beta.-position to the nitrogen of a group of formula I ##STR1## wherein R represents one to four substituents, each one independently selected from (1-4C) alkyl, phenyl and benzyl, or two at the same carbon atom being together --(CH.sub.2).sub.n -- wherein n is 2-6; and Y is O or S, or a pharmaceutically acceptable salt thereof. These steroids are very potent intravenous anaesthetics. The compounds have fast onset times and ideal `sleep duration` vs. `recovery to full coordination` profiles.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: Present invention relates to a group of 17-(4-pyridazinyl)-5.beta.,14.beta.-androstane derivates active on the cardiovascular system and to pharmaceutical compositions containing same.

Abstract: The invention discloses Diels-Alder adducts of the following structure: ##STR1## The compounds are useful as intermediates in the production of (E)-20(22)-Dehydrovitamin D compounds.

Abstract: The present invention relates to new cyclopentanperhydrophenanthren-17-(hydroxy or alkoxy)-17-(aryl or heterocyclyl)-3.beta.-derivatives, active on the cardiovascular system, to a process for their preparation and to pharmaceutical compositions containing them. The invention relates to compounds of general formula (I) ##STR1## wherein X is O or S and R, R.sup.1 and R.sup.2 is selected from various groups.

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: Monoquaternary 2,16-bispiperidinylandrostane neuromuscular blocking derivatives having the formula: ##STR1## wherein R.sub.1 is ethyl;R.sub.2 is methyl or allyl; andX.sup.- is a pharmaceutically acceptable anion; or pharmaceutically acceptable salts thereof.

Abstract: The invention is related to a 21-chloro-pregnane derivative of the formula ##STR1## or pharmaceutically acceptable salts thereof. The compound has intravenous anaesthetic activity, short onset time and high potency.

Abstract: Disclosed are amino substituted steroids (XI) which contain a pyrazinylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: Disclosed are amino substituted steroids (XI) which contain 4-[1,3,5-triazin-2-yl]- or 4-[1,2,4-triazin-3-yl]- 1-piperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

Abstract: This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3.alpha.-hydroxy,3.beta.-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3.alpha.-hydroxy,3.beta.-substituted-20-one form, which can be further modified at the 20-keto position.Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.

Abstract: A method of controlling the attachment of organisms to an underwater surface is disclosed. The method comprises contacting the organisms with a compound of Formula I ##STR1## wherein R.sub.1 is hydrogen hydroxyl C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 aryl, C.sub.1 -C.sub.20 alkyl aryl, or carbohydrate; R.sub.2 is hydrogen or hydroxyl, and R.sub.3 is hydrogen, or R.sub.2 and R.sub.3 together form an epoxide; R.sub.4 is hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkoxy, or carboxylic acid; and L is selected from the group consisting of a moiety of Formula II, a moiety of Formula III, and a moiety of Formula IV ##STR2## wherein R.sub.5 is CH.sub.2, NH, O or S, R.sub.6 is CH.sub.2, NH, O or S, R.sub.7 is N or CH, and R.sub.8 is NH or O, and wherein the compound is optionally substituted from 1 to five times with halogen, hydroxyl, C.sub.1 -C.sub.3 alkyl, or C.sub.1 -C.sub.3 alkoxy groups at positions 1, 2, 4, 5, 6, 7, 8, 9, 10, 11, and 12.

Abstract: A method of controlling the attachment of organisms to an underwater surface is disclosed. The method comprises contacting the organisms with a compound of Formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxyl, C.sub.1-C.sub.20 alkyl, C.sub.1-C.sub.20 alkoxy, C.sub.1-C.sub.20 aryl, C.sub.1-C.sub.20 alkyl aryl, or carbohydrate; R.sub.2 is hydrogen or hydroxyl, and R.sub.3 is hydrogen, or R.sub.2 and R.sub.3 together form an epoxide; R.sub.4 is hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkoxy, or carboxylic acid; and L is selected from the group consisting of a moiety of Formula II, a moiety of Formula III, and a moiety of Formula IV ##STR2## wherein R.sub.5 is CH.sub.2, NH, O or S, R.sub.6 is CH.sub.2, NH, O or S, R.sub.7 is N or CH, and R.sub.8 is NH or O, and wherein the compound is optionally substituted from 1 to five times with halogen, hydroxyl, C.sub.1-C.sub.3 alkyl, or C.sub.1-C.sub.3 alkoxy groups at positions 1, 2, 4, 5, 6, 7, 8, 9, 10, 11, and 12.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.

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: Disclosed are .DELTA..sup.9(11) -steroids of the formula ##STR1## which have been found to be angiostatic and therefore are useful in the control of embryogenesis, inflammatory conditions, tumor growth as well as other abnormalities.

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: 2.beta.,16.beta.-diamino-3.alpha.,17.alpha.-oxygenated androstanes having one quaternized group, process for the preparation of these compounds and pharmaceutical compositions comprising such compounds as the active ingredient. The aforementioned compounds are favourable neuro-muscular blocking agents.

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.

Abstract: Steroids of the formula: ##STR1## which are characterized by a 17.alpha.-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17.beta.-hydroxy/esterified hydroxy substituent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progestational, or anti-progestational activity, depending on the particular structure.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.