Abstract: Described herein are imidazolyl compounds which either act as pure antiprogestins and methods of using such pure antagonists for gynecological indications and breast cancer.

Abstract: Described herein are compounds which exhibit progesterone antagonistic effects and methods of treating cancer using such compounds.

Abstract: The present invention relates to (11?,17?)-11-(4-(2-11C-acetyl)phenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one, an 11C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer.

Abstract: Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.

Abstract: The invention relates to 17-(1?-propenyl)-17-3?-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.

Abstract: The present invention relates to steroid-derived cyclopamine analogs and methods for using the same for inhibiting sonic hedgehog signaling and preventing or treating cancer. A method for synthesizing the analogs of the present invention from a steroid is also provided.

Abstract: The present invention is directed to novel 11-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.

Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein: —A—A—, —B—B—, R1, R3, R8 and R9 are as defined in the specification.

Abstract: New aromatic diamine derivatives and the preparations thereof are disclosed. The inventive diamine derivatives can be added to conventional polymerization reactions of tetracarboxylic acids and diamines to form new polyamic acids. After high-temperature baking, the polyamic acids are cyclized to form polyimides. These polyimides can be used as alignment film materials for liquid crystal display cell and have good alignment property and stability, and are effective in promoting pre-tilt angle.

Abstract: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

Abstract: Compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical preparations containing these compounds as well as their use for treatment of diseases. The compounds have antigestagenic, antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.

Abstract: A steroid with a 17-spiromethylene lactone group having formula I ##STR1## wherein R.sub.1 is O, (H,H), (H,OR), or NOR, R being selected from H, (1-6C) alkyl and (1-6C) acyl; R.sub.2 is H, (1-6C) alkyl optionally substituted by a halogen, (2-6C) alkenyl optionally substituted by a halogen, (2-6C) alkynyl optionally substituted by a halogen, or halogen; R.sub.2 ' is H; or R.sub.2 ' together with R.sub.2 is a (1-6C) alkylidene group or a (2-6C) alkenylidene group; or R.sub.2 ' together with R.sub.3 is a bond; R.sub.3 is H if not together with R.sub.2 ' a bond; R.sub.4 is (1-6C) alkyl; one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen or (1-6C) alkyl; X is (CH.sub.2).sub.n or (C.sub.n H.sub.

Abstract: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

Abstract: Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.

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: The invention relates to an antiprogestin 17- spirofuran-3'-ylidene steroid having the formula ##STR1## p0 R.sub.1 is NR.sub.2 R.sub.3, lower acyl, OH, SH, O-lower alkyl or S(O).sub.n -lower alkyl wherein n is 0-2;R.sub.2 and R.sub.3 are independently selected from hydrogen and lower alkyl;R.sub.4 is hydrogen or lower alkyl;R.sub.5 is O, (H,H), (H,OH), (H,O-lower acyl), or NOH;R.sub.6 and R.sub.7 are both hydrogen, or one is hydrogen and the other lower alkyl; andthe twitched line represents an .alpha. or .beta. bond.

Abstract: The present invention relates to 4-azido-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.

Abstract: The present invention relates to 4-amino-.DELTA..sup.4,6 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence of a strong acid such as sulfuric acid at about 100.degree. C.

Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.

Abstract: The present invention relates to 4-amino-.DELTA..sup.4,6 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence of a strong acid such as sulfuric acid at about 100.degree. C.

Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.The present application is a continuation-in-part of application Ser. No. 561,041, filed Aug. 1, 1990 and application Ser. No. 671,555, filed Mar. 19, 1991.

Abstract: Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.

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

Abstract: 17-Substituted estradienes and estratrienes of Formula I ##STR1## wherein ##STR2## R is alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR3## R is hydrogen, alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR4## is a CC-single or CC-double bond, exhibit, an aldosterone-antagonistic activity and a strong gestagen potency.