1-[2-(arylsulphonylamino)-1-oxoethyl]piperidine derivatives, their
preparation and their therapeutic application
    1.
    发明授权
    1-[2-(arylsulphonylamino)-1-oxoethyl]piperidine derivatives, their preparation and their therapeutic application 失效
    1- [2-(芳基磺酰基氨基)-1-氧代乙基]哌啶衍生物,其制备及其治疗应用

    公开(公告)号:US5453430A

    公开(公告)日:1995-09-26

    申请号:US37972

    申请日:1993-03-29

    摘要: Compounds of formula (I) ##STR1## wherein R represents a ##STR2## group in which R.sub.2 is a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxylic group, a sodium carboxylate group, a --CH.sub.2 OR.sub.4 group R.sub.4 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group or a (C.sub.1 -C.sub.4)acyl group, an amide group of the formula --CONR.sub.5 R.sub.6, or a --CN.sub.4 R.sub.5 group, R.sub.5 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 being a hydrogen atom, a (C.sub.1 -C.sub.4)alkyl group, a hydroxy group or a (C.sub.1 -C.sub.4)alkoxy group, and R.sub.3 is a (C.sub.1 -C.sub.4)alkyl group,R.sub.1 represents either a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group,X represents either a sulphur atom, an oxygen atom or a methylene group, n=1 or 2 andAr represents either a naphthalen-1-yl group substituted by a di(C.sub.1 -C.sub.4)alkylamino group, or a 6,7-di(C.sub.1 -C.sub.4)alkoxynaphthalen-1-yl group, or a quinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl group, or a 1,2,3,4-tetrahydroquinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl, or a 1H-indazol-7-yl group and pharmaceutically acceptable organic or inorganic salts thereof.Application in therapy.

    摘要翻译: 式(I)化合物其中R表示其中R 2为氢原子,(C 1 -C 4)烷氧基羰基,羧基,羧酸钠基团,-CH 2 OR 4基团 R4是氢原子或(C1-C4)烷基或(C1-C4)酰基,式-CONR5R6的酰胺基或-CN4R5基,R5是氢原子或(C1-C4) )烷基,R6为氢原子,(C1-C4)烷基,羟基或(C1-C4)烷氧基,R3为(C1-C4)烷基,R1为氢原子 或(C1-C4)烷基,X表示硫原子,氧原子或亚甲基,n = 1或2,Ar表示被二(C1-C4)烷基取代的萘-1-基, 烷基氨基或6,7-二(C1-C4)烷氧基萘-1-基或在3个被(C1-C4)烷基取代的喹啉-8-基)或1,2,3 (C 1 -C 4)烷基取代的4-四氢喹啉-8-基,或1H-吲唑-7-基和药学上可接受的组 其酸性或无机盐。 应用于治疗。

    1-[2-amino-5-[1-(triphenylmethyl)-1H-imidazol-4-YL]-1-oxopentyl]
piperidine derivatives, their preparation and their use as synthetic
intermediates
    3.
    发明授权
    1-[2-amino-5-[1-(triphenylmethyl)-1H-imidazol-4-YL]-1-oxopentyl] piperidine derivatives, their preparation and their use as synthetic intermediates 失效
    1- [2-氨基-5- [1-(三苯甲基)-1H-咪唑-4-基] -1-氧代戊基]哌啶衍生物,其制备及其作为合成中间体的用途

    公开(公告)号:US5476942A

    公开(公告)日:1995-12-19

    申请号:US305663

    申请日:1994-09-14

    摘要: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxyl group, a sodium carboxylate group, a group --CH.sub.2 OR.sub.4, where R.sub.4 is a hydrogen atom or R.sub.4 is a (C.sub.1 -C.sub.4) alkyl or (C.sub.1 -C.sub.4) acyl group, a group --CONR.sub.5 R.sub.6, or a group --CN.sub.4 R.sub.5, where R.sub.5 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, hydroxyl or (C.sub.1 -C.sub.4) alkoxy or (C.sub.1 -C.sub.3) alkoxyphenyl group and R.sub.3 represents a (C.sub.1 -C.sub.4)alkyl group, and their acid addition salts are useful as synthetic intermediates.

    摘要翻译: 下式的化合物:其中R 1表示氢原子或(C 1 -C 4)烷基,R 2表示氢原子,(C 1 -C 4)烷氧基羰基,羧基,羧酸钠 基团,-CH 2 OR 4,其中R 4是氢原子或R 4是(C 1 -C 4)烷基或(C 1 -C 4)酰基,基团-CONR 5 R 6或基团-CN 4 R 5,其中R 5是氢原子或 (C1-C4)烷基,R6是氢原子或(C1-C4)烷基,羟基或(C1-C4)烷氧基或(C1-C3)烷氧基苯基,R3表示(C1-C4)烷基 ,其酸加成盐可用作合成中间体。

    Pyridone derivatives, their preparation and their use as synthesis intermediates
    4.
    发明授权
    Pyridone derivatives, their preparation and their use as synthesis intermediates 失效
    吡啶酮衍生物,其制备及其作为合成中间体的用途

    公开(公告)号:US06252082B1

    公开(公告)日:2001-06-26

    申请号:US09341574

    申请日:1999-07-14

    IPC分类号: C07D21186

    摘要: The invention concerns compounds of formula (I) in which: R is —NO2 or —NHR3, R3 being hydrogen, —COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, —COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), —CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), —SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a —CH2—, —SO2 or —NR1— group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.

    摘要翻译: 本发明涉及式(I)化合物,其中R为-NO 2或-NHR 3,R 3为氢,-COR 4(R 4选自(C 1 -C 4)烷基,芳基和芳基(C 1 -C 4)烷基,-COOR 5( (C1-C4)烷基和(C1-C4)烷基),-CONHR6或SO2R6(R6选自(C1-C5)烷基,芳基和芳基(C1-C4)烷基),-SO2NR7R8(R7和 相互独立地表示氢或(C1-C4)烷基或与氮原子形成吗啉基),芳基(C1-C4)烷基,R1是直链或支链的(C1-C4)烷基,环(C3 任选取代的芳基(C 1 -C 4)烷基,杂芳基,R 2是氢原子,(C 1 -C 4)烷基或芳基甲基,X是氧或硫原子,-CH 2 - ,-SO2或-NR1-基,Y为氢原子或(C1-C6)烷基,本发明适用于合成中间体。

    Antithrombotic method
    8.
    发明授权
    Antithrombotic method 失效
    抗血栓方法

    公开(公告)号:US4342759A

    公开(公告)日:1982-08-03

    申请号:US179460

    申请日:1980-08-19

    CPC分类号: C07D295/215 A61K31/395

    摘要: A method of treating a patient susceptible to thrombosis is provided which comprises treating the said patient with a compound of the formula ##STR1## wherein R' is H or CH.sub.3R is a ##STR2## radical in which Z is 0, S, SO, SO.sub.2 or NR.sub.1, R.sub.1 being H, C.sub.6 H.sub.5, CH.sub.3, CONR.sub.2 R.sub.3, COOR.sub.2, COR.sub.2 or SO.sub.2 R.sub.2, where R.sub.2 and R.sub.3 are, independently, H, C.sub.1-4 alkyl, C.sub.6 H.sub.5 or CF.sub.3.

    摘要翻译: 提供一种治疗易患血栓形成的患者的方法,其包括用下式化合物治疗所述患者:其中R'为H或CH 3 R为其中Z为0,S,SO, SO 2或NR 1,R 1是H,C 6 H 5,CH 3,CONR 2 R 3,COOR 2,COR 2或SO 2 R 2,其中R 2和R 3独立地是H,C 1-4烷基,C 6 H 5或CF 3。