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121 条记录 (耗时 0.037 秒)

    Phenoxyethyl-thiourea-pyridine compounds and their use for treatment of HIV-infections
    51.
    发明申请
    Phenoxyethyl-thiourea-pyridine compounds and their use for treatment of HIV-infections 失效
    苯氧乙基 - 硫脲 - 吡啶化合物及其用于治疗艾滋病毒感染的用途

    公开(公告)号：US20030186991A1

    公开(公告)日：2003-10-02

    申请号：US10420032

    申请日：2003-04-15

    申请人： Parker Hughes Institute

    发明人： Fatih M. Uckun ,  Taracad K. Venkatachalam

    IPC分类号： A61K031/4709 ,  A61K031/502 ,  A61K031/497 ,  A61K031/444 ,  A61K031/4439 ,  C07D417/02 ,  C07D413/02 ,  C07D41/02

    CPC分类号： C07D213/75

    摘要： The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.

    摘要翻译： 本发明提供抑制逆转录酶（RT）并抑制逆转录病毒如人免疫缺陷病毒-1（HIV-1）复制的化合物。 本发明的化合物是苯氧基乙基 - 硫脲 - 吡啶。 本发明另外提供了用于抑制逆转录病毒例如HIV-1的逆转录酶活性的方法，包括使逆转录病毒与本发明的化合物接触。 本发明另外提供了一种抑制逆转录病毒如HIV-1复制的方法，其包括使逆转录病毒与本发明的化合物接触。

    Novel N-substituted 4-((-4'-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
    53.
    发明申请
    Novel N-substituted 4-((-4'-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties 有权
    具有胃动力学性质的新型N-取代的4 - （（ - 4'-氨基苯甲酰基） - 氧甲基） - 哌啶

    公开(公告)号：US20030153573A1

    公开(公告)日：2003-08-14

    申请号：US10299317

    申请日：2002-11-19

    发明人： Jean-Paul Rene Marie Bosmans ,  Christopher John Love ,  Marc Gustaaf Celine Verdonck ,  Joannes Adrianus Jacobus Schuurkes

    IPC分类号： A61K031/506 ,  A61K031/502 ,  A61K031/501 ,  A61K031/497 ,  A61K031/4545 ,  C07D43/14 ,  C07D41/14

    CPC分类号： C07D401/06 ,  C07D211/22 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

    摘要： This invention concerns the compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula -AlknullR4, -AlknullNR5R6, 1-R6-4-piperidinyl, Alk-XnullR7, -AlknullYnullC(nullO)nullR9, or -AlknullYnullC(nullO)nullNR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar-, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cyclo-alkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

    摘要翻译： 本发明涉及式I化合物的N-氧化物形式，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是C 1-6烷氧基，C 2-6烯基氧基或C 2-6炔基氧基; R 2是氢或C 1-6烷氧基，或者当R 1和R 2一起形成式2的二价基团时，其中在所述二价基团中，一个或两个氢原子可被C 1-6烷基取代，R 3是氢或卤素; L是C3-6环烷基，C5-6环烷酮，任选被芳基取代的C2-6烯基，或L是式-Alk-R4，-Alk-NR5R6，1-R6-4-哌啶基，Alk-X-R7， - Alk-YC（= O）-R9或-Alk-YC（= O）-NR11R12，其中每个Alk是C1-12烷二基; R4是氢，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het1; R5是氢或C1-6烷基; R6是Het2; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基，Ar或Het 2; X是O，S，SO 2或NR 8; 所述R8为氢，C1-6烷基或Ar; R 9为氢，C 1-6烷基，C 3-6环烷基，Ar，ArC 1-6烷基，二（Ar）甲基，C 1-6烷氧基或羟基; Y是NR10或直接键; 所述R 10为氢，C 1-6烷基或Ar; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基，Ar或ArC 1-6烷基，或R 11和R 12与带有R 11和R <

    Heterocyclic cytotoxic agents
    56.
    发明申请
    Heterocyclic cytotoxic agents 有权
    杂环类细胞毒剂

    公开(公告)号：US20030100560A1

    公开(公告)日：2003-05-29

    申请号：US10134983

    申请日：2002-04-29

    发明人： Edmond J. LaVoie ,  Leroy Fong Liu ,  Younong Yu

    IPC分类号： C07D487/14 ,  A61K031/502 ,  A61K031/503

    CPC分类号： C07D471/04 ,  C07D237/26 ,  C07D491/04

    摘要： The invention provides compounds of formula I: 1 wherein R1-R8 and A-G have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.

    摘要翻译： 本发明提供式I化合物：其中R 1 -R 8和A-G具有本说明书中定义的任何含义及其药学上可接受的盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体，以及使用式I化合物治疗癌症的治疗方法。

    Device and method for treating conditions of a joint
    59.
    发明申请
    Device and method for treating conditions of a joint 审中-公开
    用于治疗关节病症的装置和方法

    公开(公告)号：US20020169162A1

    公开(公告)日：2002-11-14

    申请号：US09985319

    申请日：2001-11-02

    发明人： Thomas J. Smith ,  David A. Watson ,  Richard LaPorte ,  Hong Guo ,  Jianbing Chen ,  Paul Ashton

    IPC分类号： A61K031/502 ,  A61K031/50

    CPC分类号： A61K9/0024 ,  A61B17/0642 ,  A61B17/1615 ,  A61B17/80 ,  A61B17/82 ,  A61B17/8615 ,  A61B17/8877 ,  A61B17/8886 ,  A61B2017/00004 ,  A61B2017/00429 ,  A61B2017/00955 ,  A61B2017/0647 ,  A61B2017/0648 ,  A61F2/30744 ,  A61F2002/30673 ,  A61F2002/30677 ,  A61L31/16 ,  A61L2300/222 ,  A61L2300/416 ,  A61L2300/602 ,  A61M31/002 ,  A61M2210/02

    摘要： An implantable drug delivery system is provided including a mechanical member attachable to a portion of a body, a first chamber having an opening configured to receive a sustained release device, a sustained release device, and a removably attachable retainer for retaining the sustained release device in the first chamber. A method for administering a drug to a joint is provided including the steps of positioning a mechanical member in or adjacent a bone, the mechanical member configured to hold a sustained release drug delivery device bearing at least one drug, and outputting the at least one drug from the sustained release drug delivery device at a substantially controlled rate. Also provided is a sustained release device intraarticularly implantable into a joint to deliver a therapeutically effective compound within a synovial capsule of the joint such that, in one aspect, the synovial fluid concentration of the compound is greater than the plasma concentration of the compound during the prolonged lifetime of the device, thereby eliminating unwanted systemic side effects and the need for frequent and repeated administrations.

    摘要翻译： 提供了一种可植入药物递送系统，其包括可连接到身体的一部分的机械构件，具有构造成容纳持续释放装置的开口的第一腔室，缓释装置和用于将持续释放装置保持在其中的可移除附接的保持器 第一个房间 提供了一种向接头施用药物的方法，包括将机械构件定位在骨中或邻近骨的步骤，所述机械构件构造成保持携带至少一种药物的缓释药物递送装置，并输出至少一种药物 以持续释放的药物输送装置以实质上受控的速率。 还提供了可关节内植入到关节中以在关节的滑膜内递送治疗有效化合物的持续释放装置，使得在一个方面，化合物的滑液浓度大于化合物的血浆浓度 延长设备的寿命，从而消除不必要的全身副作用以及频繁和重复给药的需要。