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BENZOPYRAZINE DERIVATIVES AS PROLYL HYDROXYLASE INHIBITORS
专利权人:
GLAXOSMITHKLINE LLC
发明人:
COLON, MARIELA,FITCH, DUKE M
申请号:
NZ58570108
公开号:
NZ585701A
申请日:
2008.11.26
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 6-hydroxy benzopyrazine / quinoxaline derivatives as represented by the general formula (I), wherein R' is NR6R7 or OR8; R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, nitro, cyano, halogen, -C(O)R11, C(O)OR11, OR11, SR11, S(O)R11, S(O)2R11, NR9R10, CONR9R10, N(R9)C(O)R11, N(R9)C(O)OR11, OC(O)NR9R10, N(R9)C(O)N9R10, P(O)(OR11)2, SO2NR9R10, N(R9)SO2R11, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, and heteroaryl; and wherein the remaining substituents are as defined herein. Representative compounds include N-[(6-hydroxy-3-phenyl-5-quinoxalinyl)carbonyl] glycine; N-{ [7-(3,5-difluorophenyl)-6-hydroxy-5-quinoxalinyl]carbonyl} glycine; N-[(3-(3,4-difluorophenyl)-6-hydroxy-7- { 3-[(1-methylethyl)oxy]phenyl} -5-quinoxalinyl)carbonyl]glycine; N-{ [2-(3-fluorophenyl)-6-hydroxy-5-quinoxalinyl]carbonyl} glycine; N-{ [8-(2-furanyl)-6-hydroxy-5-quinoxalinyl]carbonyl} glycine; N-{ [6-hydroxy-8-(1,3-thiazol-5-yl)-5-quinoxalinyl]carbonyl} glycine and N-{ [6-hydroxy-2-(3-pyridinyl)-5-quinoxalinyl]carbonyl} glycine. Further disclosed is a pharmaceutical composition which comprises a compound of formula (I) or a salt, solvate, as defined above and one or more of pharmaceutically acceptable carriers, diluents and excipients for treating anaemia.
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