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    • 2. 发明申请
    • TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS
    • 三氧化二氮唑酮类抗生素化合物
    • US20110195961A1
    • 2011-08-11
    • US13123218
    • 2009-10-06
    • Christian HubschwerlenDaniel RitzGeorg RueediJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • Christian HubschwerlenDaniel RitzGeorg RueediJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • A61K31/5415C07D413/14A61K31/538C07D417/14C07D471/06A61K31/437A61K31/5383A61P31/04
    • C07D471/06C07D471/16C07D487/06C07D519/00
    • The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
    • 本发明涉及式I的抗菌化合物,其中是一个键或不存在,V是CH,CR 6或N; R 0是H,或者如果是键,也可以是烷氧基; R1特别是H或卤素; U是CH或N,当是键时,或如果不存在,U是CH 2,NH或NR 9; R2是H,烷基羰基或-CH2-R3; R3是H,烷基或羟烷基; R4是H或如果n不为0且R5是H,也可以是OH; R5是H,烷基,羟基烷基,氨基烷基,烷氧基烷基,羧基或烷氧基羰基; R6是羟基烷基,羧基,烷氧基羰基或 - (CH2)q-NR7R8,q是1,2或3,R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - (CH 2)p - , - CH 2 CH 2 CH(OH) - 或-COCH 2 CH(OH) - ; G为取代苯基或G1或G2,其中Q为O或S,X为CH或N; Y1,Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH(OH) - 或-COCH 2 CH(OH) - 时,n为0,当A为 - (CH 2)p - ,p为1,2,3或4时,n为0,1或2, 条件是n和p之和为2,3或4; 和这些化合物的盐。
    • 9. 发明授权
    • Quinazoline-2,4-dione derivatives
    • 喹唑啉-2,4-二酮衍生物
    • US08916573B2
    • 2014-12-23
    • US14238415
    • 2012-08-10
    • Christian HubschwerlenGeorg RueediJean-Philippe SurivetCornelia Zumbrunn Acklin
    • Christian HubschwerlenGeorg RueediJean-Philippe SurivetCornelia Zumbrunn Acklin
    • A01N43/54A61K31/517C07D239/72C07D401/00
    • C07D471/04C07D413/14C07D417/14C07D498/04C07D513/04
    • The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
    • 本发明涉及式(I)的抗菌化合物,其中R1是H,卤素,(C1-C3)烷基或(C1-C3)烷氧基; R2是H,卤素,(C1-C3)烷基,(C1-C3)烷氧基或吡咯烷-1-基; R 3是H,卤素,(C 1 -C 3)烷基,(C 1 -C 3)烷氧基,乙烯基或2-甲氧基羰基乙烯基,或者R 2和R 3与它们的两个碳原子一起形成苯环; R4是H,卤素,(C1-C3)烷基或(C1-C3)烷氧基; 并且R 5是H,(C 1 -C 3)烷基或环丙基,或R 4和R 5一起形成-CH 2 CH 2 CH 2 - 基; A是二价基团-CH 2 - , - CH 2 CH 2 - , - CH 2 OH,-CH 2 - , - CH 2 OH(R ​​6) - *和-CH 2 NHCH 2 - ,其中#表示与任选取代的(喹唑啉 - 2,4-二酮-3-基)甲基残基,*表示与取代的(恶唑烷酮-4-基)甲基残基的连接点; R6是H或乙酰基; Y是CH或N; Q为O或S; 和这些化合物的盐。