首页> 外国专利> Oxazolidinone Derivatives, Pharmaceutical Composition and use in Medicine, bacterial infections

Oxazolidinone Derivatives, Pharmaceutical Composition and use in Medicine, bacterial infections

机译:恶唑烷酮衍生物,药物组合物和在医学上的用途,细菌感染

摘要

Claim 1: A compound of formula 1 in which R1 is hydrogen, halogen, hydroxyl, alkoxy or cyano; Y1 and Y2 each represents CH and one or two of U, V, W and X represents (n) N and the remaining each represents CH or, in the case of X, can also represent CRa, and, in the case of W, can also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, given that R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent (n) CRc and the remaining each represents CH; Ra represents halogen; Rb represents alkoxy, alkoxycarbonyl or alkoxyalkoxy; Rc, every time it appears,Independent representative of hydroxyl or oxy group; esch2ch (OH),CH2CH (NH2)CH (OH) chn2 or CH (NH2) CH2, B is CH2CH2, ch2nh or CONH, D is CH2, or a is CH2 (OH) CH2, or B is CH2CH2, ch2nh, n (R2) Co, CONH or n (R2) CH2 and D are CH2 or B is n (R2A) CH2 and D is CH2,Or a is ch (OH) ch (OH),B is ch2nh or CONH, or esch2, or a is CH2CH2, or B is CH2CH2, nr4ach2, ch2nr3, nhco, conr4, CH2O, CH (OH) CH2, CH2CH (OH),CH2 (nhr3a) CH2, CH2 or ch2ch2nh and D are CH2 or B is ch2nh, D is co, or a is CH2CH2, B is nr4bch2 or CH2CH2, and D is CH2 (OH),or A is CH = CH, B is CH2NR5, CONR6 or CH2O and D is CH2, or A is C ::: C, B is CH2NH and D is CO, or A is CH2CO, B is NHCH2 and D is CH2, or A is COCH2, B is CH2CH2 or CONH and D is CH2, or A is CH2N (R7) and either B is CH2CH2, COCH2 or CH2CH (OH) and D is CH2 or B is CH2CH2, or CH2CH (OH) and Des CH (OH) or CH (NH2),or A is CONH or CH2O, B is CH2CH2 and D is CH2, or A is NHCH2 and either B is CH2CH2 or CH2NH and D is CH2, or B is CH2NH and D is CO, or A is NHCO, B is CH ( R8) NH or CH2CH2 and D is CH2, or A is OCH2, B is CH2, CH2CH2, CH = CH or CONH and D is CH2; R2 is hydrogen or alkyl; R2a is hydrogen or alkyl; R3 is hydrogen, phenylalkyl, CO- (CH2) p-COOR3 ',(CH2) p-COOR3Acid or carbamate, or the same R3, is a substance that can be replaced once or twice with a hydroxyl group, P is the complete 1-4 and R3 'as hydrogen or tar; R3a is hydrogen, acid or alkyl; R4 is hydrogen or tar; R4A is hydrogen or (CH2) q-cour4a',Or R4A is also a kind of tar that can be replaced once or twice with hydroxyl group. Q4a is an integer from 1 to 4, R4A is a whole, which is hydrogen or tar; r4b is h or tar; R5 is hydrogen or acid; R6 is hydrogen, asphalt or phenyl; R7 is hydrogen or (CH2) r-coor7 ',Or R7 is also a kind of tar, which can be replaced once or twice by a group independently selected from hydroxyl, hydrogen halide, amino and dimethylamine. R is an integer from 1 to 4, R7 is hydrogen or tar, R8 is hydrogen or tar, and is one of the following formulas (2); Where Z is ch or N, q is o or s, or E is a phenyl group, consisting of halogenated, tar 1-3, propoxyc1-3, sulfur trifluoride and sulfur trifluoride, or a salt independently selected, and replaced once or twice in the target location and / or substitute respectively.
机译:1。式1的化合物,其中R 1为氢,卤素,羟基,烷氧基或氰基; Y1和Y2分别代表CH,U,V,W和X中的一个或两个代表(n)N,其余每个代表CH,或者在X的情况下也可以代表CRa,在W的情况下,也可以代表CRb,或者U,V,W,X,Y1和Y2各自代表CH或U,V,W,X和Y1各自代表CH且Y2代表N,或者一个或一个,如果R1是氢其中,U,V,W,X,Y1和Y2中的两个代表(n)个CRc,其余每个代表CH。 Ra表示卤素; Rb代表烷氧基,烷氧基羰基或烷氧基烷氧基; Rc,每次出现时,独立地代表羟基或氧基; esch2ch(OH),CH2CH(NH2)CH(OH)chn2或CH(NH2)CH2,B是CH2CH2,ch2nh或CONH,D是CH2或a是CH2(OH)CH2或B是CH2CH2,ch2nh,n (R2)Co,CONH或n(R2)CH2和D为CH2或B为n(R2A)CH2和D为CH2,或a为ch(OH)ch(OH),B为ch2nh或CONH或esch2,或a为CH2CH2,或B为CH2CH2,nr4ach2,ch2nr3,nhco,conr4,CH2O,CH(OH)CH2,CH2CH(OH),CH2(nhr3a)CH2,CH2或ch2ch2nh,D为CH2或B为ch2nh,D是co或a是CH2CH2,B是nr4bch2或CH2CH2,D是CH2(OH)或A是CH = CH,B是CH2NR5,CONR6或CH2O且D是CH2或A是C ::: C, B为CH2NH和D为CO或A为CH2CO,B为NHCH2和D为CH2或A为COCH2,B为CH2CH2或CONH且D为CH2或A为CH2N(R7)且B为CH2CH2,COCH2或CH2CH(OH)且D为CH2或B为CH2CH2或CH2CH(OH)和Des CH(OH)或CH(NH2),或A为CONH或CH2O,B为CH2CH2和D为CH2或A为NHCH2 B是CH2CH2或CH2NH且D是CH2或B是CH2NH且D是CO或A是NHCO,B是CH(R8)NH或CH2CH2且D是CH2或A为OCH 2,B为CH 2,CH 2 CH 2,CH = CH或CONH,D为CH 2;或R 2是氢或烷基; R 2a是氢或烷基; R3是氢,苯基烷基,CO-(CH2)p-COOR3',(CH2)p-COOR3酸或氨基甲酸酯,或相同的R3是可以被羟基取代一次或两次的物质,P是完整的1 -4和R 3'为氢或焦油; R 3a是氢,酸或烷基; R4是氢或焦油; R4A是氢或(CH2)q-cour4a',或者R4A也是一种可以被羟基取代一次或两次的焦油。 Q4a是1〜4的整数,R4A是氢或焦油的整数。 r4b是h或tar; R5是氢或酸; R6是氢,沥青或苯基; R7是氢或(CH2)r-coor7',或R7也是一种焦油,它可以被一个独立地选自羟基,卤化氢,氨基和二甲胺的基团取代一次或两次。 R为1〜4的整数,R7为氢或焦油,R8为氢或焦油,为下式(2)之一。其中Z为ch或N,q为o或s或E为苯基,由卤代,焦油1-3,丙氧基1-3,三氟化硫和三氟化硫或独立选择的盐组成,并取代一次或两次分别位于目标位置和/或替代位置。

著录项

  • 公开/公告号AR066012A1

    专利类型

  • 公开/公告日2009-07-15

    原文格式PDF

  • 申请/专利权人 ACTELION PHARMACEUTICALS LTD.;

    申请/专利号AR2008P101485

  • 发明设计人

    申请日2008-04-10

  • 分类号C07D471/04;C07D413/14;C07D417/14;A61K31/4375;A61P31/04;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:41

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号