Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: This invention provides a pharmaceutically acceptable salt of 5&agr;-pregn-16-en-3&bgr;-ol-20-one 3-sulfate ester, which is useful as a progestational agent.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception, for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, or prostate, minimization of side effects, cyclic menstrual bleeding, or stimulation of food intake.

Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: 1

Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.

Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut

Abstract: Methods for conversion of anilines to 1,2-dihydroquinolines. 1,2-dihydroquinoliiies are generated from combining an aniline, a silylating agent, and further condensing with a ketone in the presence of a catalyst. In one aspect, the silylation of the aniline may be performed in a one-step synthesis by adding the silylating, agent to the same reaction vessel as the ketone, aniline, and catalyst. In a second aspect, the 1,2-dihydroquinoline is generated in a two-step synthesis where an N-silyl aniline is formed prior to the addition of the ketone and catalyst.

Abstract: This invention provides a pharmaceutically acceptable salt of 5.alpha.-pregn-16-3.beta.-ol-20-one 3-sulfate ester, which is useful as a progestational agent.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is --(CH.sub.2).sub.n O--, --(CH.sub.2).sub.n S--, ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or --O--, --S-- or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluroloweralkyl, polyfluroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen lower alkyl, --COOR.sup.4 or ##STR9## R.sup.7 is OR.sup.4 or N(R.sup.4).sub.2 ; R.sup.8 is OR.sup.4 or N(R.sup.4).sub.2 ;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstruction airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, as antiinflammatory agents.

Abstract: There are disclosed compounds of the formula ##STR1## n is 0-5; R.sup.2 is, independently, hydrogen, loweralkyl, loweralkoxy, trifluoromethyl or halo; ##STR2## W represents a bond or ##STR3## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR4## or a pharmaceutically acceptable salt thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is hydrogen or loweralkyl;R.sup.4 hydrogen, lower alkyl, --COOR.sup.3 or ##STR3## R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR4## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.

Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 ##STR3## W represents a bond or --O--, --S-- or ##STR4## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR5## R.sup.6 is hydrogen, lower alkyl, --COOR.sup.4 or ##STR6## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is N or CR.sup.1Y is O, S, NR.sup.1, CHR.sup.1 or C(R.sup.1).sub.2 when n=O, or N or CR.sup.1 when n=1;p is 0-3;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is H, ##STR2## --SO.sub.2 R.sup.3 or --SO.sub.2 N(R.sup.3).sub.2, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl carbonyl prolinate;R.sup.3 is H, lower alkyl or perfluoro lower alkyl;R.sup.4 is lower alkyl, phenyl, pyridyl or thienyl;R.sup.5 is hydrogen, lower alkyl, phenyl or pyridyl;A is O or NR.sup.1 ;B is OR.sup.1 or N(R.sup.5).sub.2 ;m is 0-2;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.