BENSEN Deniel (US),БЕНСЕН Дэниел (US),FINN Dzhon (US),ФИНН Джон (US),LI Sak Yung (US),ЛИ Сак Юнг (US),CHEN Chzhiyun (US),ЧЭНЬ Чжиюн (US),LAM Tan To (US),ЛАМ Тан То (US),LI Syaomin (US),ЛИ Сяомин (US),BENSEN Deniel,БЕНСЕН Дэниел,FINN Dzhon,ФИНН Джон,LI Sak Yung,ЛИ Сак Юнг,CHEN Chzhiyun,ЧЭНЬ Чжиюн,LAM Tan To,ЛАМ Тан То,LI Syaomin,ЛИ Сяомин,TRZOSS Majkl,ТРЗОСС Майкл,DZHANG Majkl,ДЖАНГ Майкл,NGUEN Toa
申请号：
RU2013140798
公开号：
RU0002626979C2
申请日:
2012.03.14
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmacology.SUBSTANCE: invention relates to new tricyclic compounds of formula I having an activity of inhibitors of gyrase B (GyrB) and topoisomerase IV (ParE) enzyme. The compounds may find application in bacterial infections treatment. The invention also relates to a method for preparation of compounds of formula I and formula (1) intermediates for their preparation. In formula I:.L is O or S； R8 is H, Cl, F, Br, OH, NH2, C1-3alkyl, amino-C1-3alkyl, aminocyclopropyl, OCH3, OCH2CH3, cyclopropyl, CH2cyclopropyl, CH2Cl, CHCl2, CCl3, CH2CH2Cl, CH2Br, CHBr2, CH2F, CHF2, CF3, CH2CH2F, CH2CHF2, CH2CF3, NHNH2, NHOH, NHNHCH3, NHOCH3, NHCD3, SCH3 or NHCOH； X, Y and Z are independently selected from the group consisting of N, CRX, CRY and CRZ, provided that no more than two of X, Y and Z are N. At that, RX is H, CH3, Cl, Br or F. At that, RY is H, CH3, CHF2, CF3, CN, CH2CH3, Cl, Br or F. At that, RZ is H, CH3, Cl, Br or F； R2 is a 6-membered monocyclic aryl or 6-membered mono- or 9-10 membered bicyclic heteroaryl ring, wherein the heteroaryl ring contains 1 to 3 heteroatoms selected from O, S and N. The said 6-membered monocyclic aryl ring, 6- Membered monocyclic heteroaryl ring and a 9-10 membered bicyclic heteroaryl ring may be optionally substituted with 0-3 substituents selected from OH, CO2H, CO2CH3, C(O)NH2, C(O)CH3, =O, CN, NH2, Br, Cl, F, SO3H, SO2NH2, SO2CH3, SOCH3, NHOH, C(O)NHOCH3, CH(OH)CH3, C(OH)(CH3)2, SCH3, or C1-C6alkyl or C3-C6cycloalkyl having 0-2 heteroatoms selected from O, S or N, optionally substituted with C1-C4alkyl, OH, CN, =O, NH2, Br, F, Cl. The bicyclic heteroaryl ring can be spiro-fused with cyclopropyl； or R2 is or ； R4 is: H； optionally substituted with ORa, where Ra is pyridyl, pyrimidinyl, optionally substituted with CH3 and NH2； optionally substituted saturated secondary or tertiary amine selected from a 4-6 membered aliphatic amine, a 4-6 membered monocyclic amine, a 5-10 membered bicyclic amine with 1 to 3 heteroatoms selected fr
