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Quinazolinones for use as anticancer agents
专利权人:
Resverlogix Corp.
发明人:
Hansen C. Henrik
申请号:
NZ70831410
公开号:
NZ708314A
申请日:
2010.03.16
申请国别(地区):
NZ
年份:
2017
代理人:
摘要:
Disclosed is the use of a 2-phenyl-4-oxo-3,4-dihydroquinazoline derivative of Formula III, or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof, in the preparation of a medicament for treating and/or preventing cancer characterized by altered expression of IL-6 or VCAM-1 in a subject (such as multiple myeloma, lymphoma, leukemia, solid tumors, prostate and bladder cancers, cardiac myxoma, tumor-induced cachexia, cerebral edema secondary to brain tumors, hormone-independent prostate cancer, B cell lymphoma, AIDS associated lymphoma, and metastatic renal cell carcinoma); wherein: Q is CR12; V is nitrogen; U is C=O; X is selected from oxygen, sulfur, NH, and CR6R7; Z is selected from unsubstituted alkyl and alkyl substituted with one or more groups selected from alkyl, alkoxy, cyclopropyl, hydroxyl, amino, and halogen; n is 0, 1, 2, 3, 4, or 5; G is selected from heterocycle optionally substituted by one or more groups selected from oxo, phenyl, methyl, ethyl, isopropyl, acetyl, C(O)NMe2, NHC(O)Me, N(i-Pr)C(O)Me, and NH(i-Pr), and/or optionally fused to phenyl; cycloalkyl; and aryl optionally substituted by one or more methyl; R1 is selected from hydrogen and alkyl; R6, R7, and R12 are independently selected from hydrogen, alkyl, cycloalkyl, heterocycle, alkoxy, and halogen; Rc is selected from hydrogen, alkyl, and cycloalkyl; Ra1, Ra2, and Ra3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, halogen, amino, amide, hydroxyl, and heterocycle, wherein Ra1 and Ra2 and/or Ra2 and Ra3 may be connected to form a cycloalkyl or a heterocycle; Rb2 and Rb6 are independently selected from hydrogen, halogen, alkyl, cycloalkyl, alkenyl, hydroxyl, and amino; and Rb3 and Rb5 are independently selected from hydrogen, halogen, alkyl, cycloalkyl, alkoxy, hydroxyl, and amino; wherein amide is -NRaC(O)(Rb) or -C(O)NRbRc, wherein Ra, Rb and Rc are each independently selected from alkyl, alkenyl, alkynyl, aryl, arylalkyl, cy
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