公开(公告)号：US06596772B1

公开(公告)日：2003-07-22

申请号：US09645879

申请日：2000-08-25

申请人： Ping Huang ,  Chung Chen Wei ,  Peng Cho Tang ,  Chris Liang ,  John Ramphal ,  Bahija Jallal ,  John Biltz ,  Sharon Li ,  Matt Mattson ,  Gerald McMahon ,  Marcel Koenig

发明人： Ping Huang ,  Chung Chen Wei ,  Peng Cho Tang ,  Chris Liang ,  John Ramphal ,  Bahija Jallal ,  John Biltz ,  Sharon Li ,  Matt Mattson ,  Gerald McMahon ,  Marcel Koenig

IPC分类号： A61K3105

CPC分类号： C07C311/09 ,  C07C317/14 ,  C07C317/22 ,  C07C317/32 ,  C07C317/40 ,  C07C317/44 ,  C07C317/50 ,  C07C323/65 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D231/24 ,  C07D235/16 ,  C07D235/18 ,  C07D295/096

摘要： The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.

摘要翻译： 本发明涉及三氟甲磺酰基和三氟甲磺酰氨基化合物及其生理上可接受的盐及其前药。 预期这些化合物可调节与细胞信号转导相关的蛋白质酪氨酸酶的活性，特别是蛋白酪氨酸磷酸酶，因此预期可用于预防和治疗与异常蛋白酪氨酸酶相关的细胞信号相关的病症 转导，如癌症，糖尿病，免疫调节，神经退行性疾病，骨质疏松症和感染性疾病。 本发明还涉及含有氟甲基磺酰基的化合物作为磷酸酯模拟物的用途。 这些模拟物可用于抑制，调节或调节细胞中磷酸结合蛋白的活性。