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Pyrazolylbenzothiazole derivatives and their use as therapeutic agents
专利权人:
QLT, INC.;DERMIRA (CANADA), INC.
发明人:
ZHANG, ZAIHUI,DAYNARD, TIMOTHY S.,WANG, SHISEN,DU, XINYAO,CHOPIUK, GREGORY B.,YAN, JUN,CHEN, JIANXIN,SVIRIDOV, SERGUEI V.
申请号:
ES03771002
公开号:
ES2385378T3
申请日:
2003.07.23
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula (1): as a single tautomer, a mixture of tautomers, a simple stereoisomer, a mixture of stereoisomer, a racemic mixture; or its pharmaceutically acceptable salt or solvate, where: R1 in each case is independently selected from amino, aminosulfinyl, aminosulfonyl, phenyl, azido, halogen, heteroaryl, heteroalkyl, hydrazinyl, C1-15 hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate , phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulphonamido, sulfonate, sulphonic acids, sulfonyl, sulfoxide, thiol, thioureido and ureido; R2 is amino; R3 is selected from C1-15 hydrocarbyl, -O- C1-15 hydrocarbyl, -S-C1-15 hydrocarbyl, R4 is hydrogen, where heteroalkyl is aminohydrocarboyl, amido, carboxylic acid, cyano, dihydrocarbilamide, dihydrocarbonylamino, di (hydrocarbyl) phosphide, formyl, hydrocarboyl, hydrocarboxyloxy, hydrocarbonylamino, hydrocarbyloxycarboxycarboxy , hydrocarbylsiloxy, hydrocarbylsilylamino, hydrocarbylsulfide, hydrocarbyl, hydrocarbylamide, isothiocyanate, N-heterocycle, perfluorohydrocarbyl, thiocyanate and hydrocarbi substituted by one or more groups selected from C1-15 alkylamino, amino, aminosulfinyl, aminosulfonyl, azido, di.C1-15 alkylamino, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydroxyl, nitro, nitrous, phosphate, phosphinate, phosphonate, phosphonium , phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfuric acids, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxide, thiol, thioureido and ureido, where the heteroalkyl hydrocarbyl moiety is C1-15 hydrocarbyl; N-heterocycle is a ring radical of 3 to 10 members consisting of carbon atoms and between 1 and 5 heteroatoms selected from nitrogen; heteroaryl is an aromatic ring radical of 3 to 10 members consisting of carbon atoms and between 1 and 5 heteroatoms selected from nitrogen, oxygen and sulfur.Un compuesto de fórmula (1):como un tautómero sencillo, una mezcla de tautómeros, un estereoisómero sencil
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