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55 results about "Progesterone receptor modulators" patented technology

Progesterone receptor modulators are agents that act on the progesterone receptors. They act as agonists or antagonists. Some progesterone modulators act as agonists in some tissues and antagonists in other tissues.

Use of progesterone receptor modulators

A progesterone receptor modulator of the structure is provided. Use of compositions containing this compound for contraception, hormone replacement therapy, treating hormone-dependent disease, synchronizing estrus, treating dysmenorrhea, treating dysfunctional uterine bleeding, inducing amenorrhea, or treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder in a mammal are described.
Owner:WYETH LLC

Cyclothiocarbamate derivatives as progesterone receptor modulators and methods of treating skin disorders

The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is:and wherein R1-R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and conditioning the skin are described. Also provided are novel PR modulators of formula II.
Owner:WYETH LLC

Cyclothiocarbamate derivatives as progesterone receptor modulators

InactiveUS20060142280A1Organic active ingredientsOrganic chemistryProgestin AntagonistDisease
Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.
Owner:WYETH

Benzonitryl and nitrobenzyl derivatives that modulate androgen receptors

This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.
Owner:SMITHKLINE BECKMAN CORP

Sustained Release Compositions Containing Progesterone Receptor Modulators

Disclosed are sustained release compositions for vaginal or transdermal administration that contain a progesterone receptor modulator such as CDB-2914 (also referred to as VA-2914), and methods of using them for long term contraception or therapeutic purposes. Also disclosed are methods for making the compositions.
Owner:LAB HRA PHARMA SA

6-Amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators

Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
Owner:WYETH LLC

Purification of progesterone receptor modulators

Processes are provided for purifying a compound of the structure:wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.
Owner:WYETH LLC

Process for the synthesis of progesterone receptor modulators

InactiveUS20080319204A1Organic chemistryArylLeaving group
Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R1-R4, R6, and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R6X or XCH2(CH2)nX′, wherein R6 is C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X′ are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.
Owner:WYETH LLC

Thioamide derivatives as progesterone receptor modulators

Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
Owner:WYETH LLC

Purification of Progesterone Receptor Modulators

Processes are provided for purifying a compound of the structure (I):wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.
Owner:WYETH LLC

Non-steroid progestogen receptor regulator, preparation thereof, pharmaceutical compositions and uses

The invention relates to a modulator of nonsteroidal progesterone receptor with a structure of the general formula I or an acceptable salt on pharmacy and a preparation method thereof. The invention also relates to drug combination including compounds of the general formula I or an acceptable salt on pharmacy thereof and the antagonist activity of progesterone receptor which is provided by the compounds of the general formula I or the acceptable salt on pharmacy thereof; therefore, the invention can be used for preparing nonsteroidal drugs to prevent and (or) or treat symptoms or diseases such as secondary amenorrhea, functional bleeding disorder, uterine fibroids, endometriosis, polycystic ovary syndrome, breast cancer, contraceptive, induced labor, and termination of pregnancy, etc.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1

Thioamide derivatives as progesterone receptor modulators

Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
Owner:WYETH LLC

Solid dispersion of a selective modulator of the progesterone receptor

The subject matter of the present invention is a solid dispersion comprising an active ingredient chosen from the group consisting of selective modulators of the progesterone receptor, metabolites thereof and mixtures thereof, and a pharmaceutically acceptable polymeric excipient. The invention also relates to a pharmaceutical composition comprising said solid dispersion and to the therapeutic uses thereof.
Owner:LAB HRA PHARMA SA

17-phosphorous steroid derivatives useful as progesterone receptor modulators

The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.
Owner:JANSSEN PHARMA NV

C11 Modified Retrosteroids as Progesterone Receptor Modulator Compounds

Retrosteroidal compounds corresponding to formula I, representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. These compounds are useful in the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for hormone replacement therapy.
Owner:SOLVAY PHARMA GMBH

Pyridine imidazoles and aza-indoles as progesterone receptor modulators

The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
Owner:JANSSEN PHARMA NV

7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators

This invention provides progesterone receptor modulators having the structure:wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
Owner:WYETH LLC
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