GENDRON Roland (US),ГЕНДРОН Роланд (US),FLERI Melissa (US),ФЛЕРИ Мелисса (US),KHYUZ Adam D. (US),ХЬЮЗ Адам Д. (US),GENDRON Roland,ГЕНДРОН Роланд,FLERI Melissa,ФЛЕРИ Мелисса,KHYUZ Adam D.,ХЬЮЗ Адам Д.
申请号：
RU2013132533
公开号：
RU0002622288C2
申请日:
2011.12.14
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula , wherein R1 is selected from -OR7 and -NR8R9； R2 is H； X is -C1-9heteroaryl, selected from pyrazole, imidazole, triazole, benzotriazole, furan, tetrazole, pyrazine, thiophene, oxazole, isoxazole, thiazole, oxadiazole, pyridazine, pyridine, pyrimidine, benzoxazole, pyridylimidazole and pyridyltriazole； R3 is absent or is selected from H； Halogen； -C0-5alkylene-OH； -NH2； -C1-6alkyl； -CF3； -C3-7cycloalkyl； -C0-2alkylene-O-C1-6alkyl； -C(O)R20； -C0-1alkylene-COOR21； -C (O) NR22R23； -NHC(O)R24； =O； -NO2； -C(CH3) =N(OH)； Phenyl optionally substituted with one or two groups independently selected from halogen, -OH, -CF3, -OCH3, -NHC(O)CH3 and phenyl； Naphthalenyl； Pyridinyl； Pyrazinyl； Pyrazolyl optionally substituted with methyl； Thiophenyl, optionally substituted by methyl or halogen； Furanyl； and -CH2-morpholinyl； and R3, when present, is attached to a carbon atom； R4 is absent or is selected from H； -HE； -C1-6alkyl； -C1-2alkylene-COOR35； -OCH2 O(O)CH (R36)NH2； -OCH2O(O)CH3； -CH2CH(OH)CH2OH； and phenyl or benzyl optionally substituted with 1 to 3 groups selected from halogen, -COOR35, -OCH3, -OCF3 and -SCF3； and R4, when present, is attached to a carbon or nitrogen atom； or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-； A is 0 or 1； R5 is halogen； B is 0 or an integer of 1 to 3； Each R6 is independently selected from halogen, -OH, -CH3 and -OCH3； R7 is selected from H, -C1-8alkyl, -[(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl and the structure of formula (a)； R10 is -O-C3-7cycloalkyl； and R32 is -C1-6alkyl； R8 and R9 are H； R20, R21 and R35 are independently selected from H and -C1-6alkyl； R22 and R23 are independently selected from H, -C1-6alkyl, -CH2COOH, -(CH2)2OH, -(CH2)2OCH3, - (CH2)2SO2NH2, -(CH2)2N(CH3)2, -C0-1alkylene-C3-7-cycloalkyl and -(CH2)2-imidazolyl； or R22 and R23 are taken together to for
