摘要:
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要:
Pharmaceutical compositions and compounds are provided. The compounds of the invention deomonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要:
A method of inhibiting tumor growth is provided, comprising administering an effective dose of a compound of the formula wherein, independently at each occurrence, w is C or N, v and x are N with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic ring or a 5, 6 or 7-membered heterocyclic ring containing at least one atom selected from nitrogen, oxygen and sulfur.
摘要:
Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.
摘要翻译:提供式(1)的药物吡唑并苯并噻唑组合物。 组合物可以是药学上可接受的盐。 R 1,R 2,R 3和R 3各自独立地选自氨基,氨基亚磺酰基,氨基磺酰基,芳基,叠氮基,卤素,杂烷基, 杂芳基,肼基,烃基,氢,羟基,硝基,亚硝基,磷酸酯,次膦酸酯,膦酸酯,鏻,硫代磷酸酯,磷酰基,氨磺酰,硫酸根,亚磺酸,亚磺酰氨基,磺酸,磺酸,磺酰基,亚砜基,硫醇,硫脲基和脲基 R 4选自氢,杂烷基,杂芳基和烃基。
摘要:
A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.
摘要:
The present invention provides spiro derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
摘要:
Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.
摘要:
Organovanadium complexes, and more specifically hydroxyoxovanadium(V), &mgr;-oxo dimeric oxovanadium(V) and cis-dioxovanadium(V) complexes, are provided. The complexes may be formulated into a pharmaceutical composition. The complexes and/or compositions may be used in the treatment of a variety of disease states, including use as anti-proliferative and/or anti-metastatic agents and/or to treat drug resistant tumors and/or to methods of reducing the ability of tumors to metastasize and/or for the treatment of diabetes, arthritis, multiple sclerosis, diseases involving passageways of the body, and autoimmune diseases including but not limited to psoriasis and lupus.
摘要:
Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要:
Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.