HUANG, KENNETH HE,EAVES, JERON,VEAL, JAMES,BARTA, THOMAS,GENG, LIFENG,HINKLEY, LINDSAY,HANSON, GUNNAR J
申请号：
NZ58896006
公开号：
NZ588960A
申请日:
2006.02.27
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
Disclosed are 4-(4-oxo-4,5,6,7-tetrahydroindazol-1-yl)-benzamide and 4-(4-oxo-4,5,6,7-tetrahydro-indol-1-yl)-benzamide derivatives as represented by the general formula (XXV), wherein: X1 is N or CRc； R3 and R4 are independently, H, halo, or optionally substituted alkyl, or R3 and R4 together with the atoms to which they are attached form a 5-12 membered mono-, bi-, or tricyclic ring system fused to the ring containing Q1 and Q2, where the 5-12 membered ring is partially unsaturated or aromatic and optionally contains one or two of oxygen, S(O)m , nitrogen, or NR33； and wherein the remaining substituents are as defined herein. Representative compounds include 2-(cyclopropylamino)-4-(3-methyl-4-oxo-4,5,6,7-tetrahydroindol-1-yl)benzamide, 4-(3-methyl-4-oxo-4,5,6,7-tetrahydroindol-1-yl)benzamide and 2-[(2-methoxyethyl)amino]-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-yl)benzamide. Further disclosed is a pharmaceutical composition which comprises at least one compound or salt as defined above and a pharmaceutically acceptable solvent, carrier, excipient, adjuvant or a combination thereof, for the treatment of a disease or disorder of proteins that are either client proteins for HSP-90 or indirectly affect its client proteins, wherein said disorder is selected from the group of inflammatory diseases, infections, autoimmune disorders, stroke, ischemia, cardiac disorders, neurological disorders, fibrogenetic disorders, proliferative disorders, tumors, leukaemia, neoplasms, cancer, carcinomas, metabolic diseases, malignant disease, sclerodenna, polymyositis, systemic lupus, rheumatoid arthritis, liver cirrhosis, keloid formation, interstitial nephritis, and pulmonary fibrosis.
