摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof.
摘要:
The present invention relates to compositions and methods related to inhibitors of Hsp90, including substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in heed thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. The invention further provides methods for designing and identifying inhibitors of Hsp90.
摘要:
The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA). The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: (IB) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: (HB) in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula: (IIIB).
摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要:
Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R 5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a subslituent R 18 , defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R 3 . Substituent R 3 is defined herein.
摘要:
The invention relates to compounds of structural formula (I); or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein R a , R b , and R 2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要:
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要:
This invention features pyrimidine compounds of formula (I): R1 is formula (II), aryl, or heteroaryl; each of R2 and R4, independently, is R , halogen, nitro, cyano, isothionitro, SR , or OR ; or R2 and R4, taken together, is carbonyl; R3 is R , alkenyl, alkynyl, OR , OC(O)R , S02R , S(O)R , S(02)NR R , SR , NR R , NR COR , NR C(O)OR , NR C(O)NR R , NR S02R , COR , C(O)OR , or C(O)NR R ; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(02), or NR ; Y is a covalent bond, CH2, C(O), C=N-R , C=N-OR , C=N-SRc, O, S, S(O), S(02), or NR ; Z is N or CH; one of U and V is N, and the other is CR ; and W is O, S, S(O), S(02), NR , or NC(O)R ; in which each of R and R , independently, is H, alkyl, aryl, heteroaryl; and each of R and R , independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译:本发明具有式(I)的嘧啶化合物:R 1是式(II),芳基或杂芳基; R 2和R 4各自独立地是R c,卤素,硝基,氰基,异硫代,SR c或OR c; 或R 2和R 4一起是羰基; R 3是R c,烯基,炔基,OR c,OC(O)R c,SO 2 R c,S(O)R c,S(O 2)NR c NR c C(O)OR d,NR c C(O)NR c, R d,NR c,SO 2 R d,COR c,C(O)OR c或C(O)NR c R d; R5是H或烷基; n是0,1,2,3,4,5或6; X是O,S,S(O),S(O 2)或NR c; Y是共价键,CH 2,C(O),C = NR c,C = N-OR c,C = N-SRc,O,S,S(O),S(O 2) NR ; Z是N或CH; U和V之一是N,另一个是CR ; 并且W是O,S,S(O),S(O 2),NR c或NC(O)R c; 其中R a和R b各自独立地是H,烷基,芳基,杂芳基; R c和R d各自独立地是H,烷基,芳基,杂芳基,环基,杂环基或烷基羰基。 该化合物可用于治疗IL-12过度生产相关疾病(例如类风湿性关节炎,败血症,克罗恩病,多发性硬化,牛皮癣或胰岛素依赖性糖尿病)。