Abstract:
The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Abstract:
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.
Abstract:
Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.
Abstract:
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.
Abstract:
The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Abstract:
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.
Abstract:
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.
Abstract:
Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.
Abstract:
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.
Abstract translation:提供具有式I结构的化合物。 在式I中,R 1是H,OH,取代或未取代的C 1至C 3烷基,C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H,取代或未取代的C 1至C 4烷基,芳基,取代或未取代的C 1〜 至C 4烷氧基,取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H,取代或未取代的C 1至C 6烷基,C 1至C 6烷基, C 6至C 6全氟烷基,取代或未取代的C 2至C 6链烯基,取代或未取代的C 2, 取代或未取代的C 3至C 6环烷基,取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7,OR 7,NHSO 2 R 7,或 OSO 2 i> R 7; Q是O,S,NR 8或CR 9 R 10; 或其药学上可接受的盐,酯或前药。 这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症。
Abstract:
This invention relates to cyclic combination therapies and regimens utilizing indoline compounds which are antagonists of the progesterone receptor and having the general structure: A is O, S, or NR4; B is a bond or CR5R6; R4, to R6 are H, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, aryl, or heterocyclic, or R4 and R5 are fused to form a ring; R1 is H, OH, NH2, C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, or CORA; RA is as defined; R2 is H, halogen, CN, NO2, C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl; R3 is a substituted benzene ring, or heteroaromatic ring, in combination with a progestational agent and/or an estrogen to treat or prevent secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas, and contraception, among others.