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    KMST isoeugenol derivatives and pharmaceutical activity
    2.
    发明申请
    KMST isoeugenol derivatives and pharmaceutical activity 失效
    KMST异丁香酚衍生物和药物活性

    公开(公告)号：US20040266785A1

    公开(公告)日：2004-12-30

    申请号：US10608073

    申请日：2003-06-30

    发明人： Ing-Jun Chen

    IPC分类号： A61K031/495 ,  C07D241/04

    CPC分类号： C07D295/088 ,  A61K31/495

    摘要： A compound having the following formula I: 1 where R1 is alkyl group or alkenyl group, X represents 2 R2 is selected from the group consisting of a halogen (o, m, p) group such as F, Cl, Br or I, nullNH2, nullNO2 and a hydrogen group, R3 is a hydrogen group or OH, and n is 0 to 2. The compound has pharmacologically null2-adrenergic/5-HT2A antagonist activity, 5-HT re-uptake activity, and anti-oxidant activity. The compound is produced by preparing 4-epoxy isoeugenol, mixing piperazine dissolved in methanol with the 4-epoxy isoeugenol to reflux at 100null C. for approximately 2 to approximately 6 hours, removing the methanol, passing the mixture through a silica gel column chromatography after the removing step, eluting the passed mixture with n-hexane and ethyl acetate, drying the eluted mixture, and crystallizing the dried mixture with methanol.

    摘要翻译： 具有下式I的化合物：其中R1是烷基或烯基，X表示R2选自卤素（o，m，p）基团，例如F，Cl，Br或I，-NH2， -NO 2和氢基，R 3为氢基或OH，n为0至2.该化合物具有药理学上的α2-肾上腺素能/ 5-HT2A拮抗剂活性，5-HT再摄取活性和抗氧化活性。 该化合物通过制备4-环氧异丁子香酚，将溶于甲醇的哌嗪与4-环氧异丁子香酚混合，在100℃下回流约2至约6小时，除去甲醇，使混合物通过硅胶柱色谱法 在去除步骤后，用正己烷和乙酸乙酯洗脱经过的混合物，干燥洗脱的混合物，并用甲醇使干燥的混合物结晶。

    N-aroyl piperazine derivatives as orexin receptor antagonists
    3.
    发明申请
    N-aroyl piperazine derivatives as orexin receptor antagonists 失效
    N-芳酰哌嗪衍生物作为食欲素受体拮抗剂

    公开(公告)号：US20040242575A1

    公开(公告)日：2004-12-02

    申请号：US10492250

    申请日：2004-07-02

    发明人： Clive Leslie Branch ,  Chirstopher Norbert Johnson ,  David John Nash ,  Geoffrey Stemp

    IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/495 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC分类号： C07D413/10 ,  C07D241/04 ,  C07D417/06

    摘要： This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, CnullO, SO2, or CHnullCHnull; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; R1 represents optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; Rnull2 represents hydrogen, optionally substituted (C1-4)alkyl, optionally substituted (C1-6)alkanoyl, optionally subtituted (C1-6)alkanoxycarbonyl or optionally substituted aryl(C1-6)alkyloxycarbonyl; and their use as orexin receptor-antagonists.

    摘要翻译： 本发明涉及式（I）的N-芳酰基哌嗪衍生物，其中：Y表示NR 2; m表示1,2或3; p表示0或1; X是O，S，C = O，SO 2或CH = CH-; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示苯基或含有1至3个选自N，O和S的杂原子的5或6元杂环基，其中苯基杂环基被R 1取代，另外任选的取代基; 或Ar 2表示含有1至4个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示任选取代的（C 1-4）烷氧基，卤素，任选取代的（C 1-6）烷基，任选取代的苯基，或任选取代的含有1至4个选自N， O和S; R 2 表示氢，任选取代的（C 1-4）烷基 ，任选取代的（C 1-6）烷酰基，任选取代的（C 1-6）烷氧基羰基或任选取代的芳基（C 1-6）烷氧基羰基; 以及它们作为食欲肽受体拮抗剂的用途。

    N-[(Piperazinyl)hetaryl]arylsulfonamide compounds
    8.
    发明申请
    N-[(Piperazinyl)hetaryl]arylsulfonamide compounds 审中-公开
    N - [（哌嗪基）杂芳基]芳基磺酰胺化合物

    公开(公告)号：US20040204422A1

    公开(公告)日：2004-10-14

    申请号：US10413233

    申请日：2003-04-14

    申请人： Abbott GmbH & Co. KG.

    发明人： Wilfried M. Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    IPC分类号： A61K031/496 ,  A61K031/495

    CPC分类号： C07D213/74 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D403/04 ,  C07D403/14 ,  C07D487/08

    摘要： The invention relates to N-null(piperazinyl)hetarylnullarylsulfonamide compounds of the general formula I 1 in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-null(piperazinyl)hetarylnullarylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropraite together with physiologically accpetable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

    摘要翻译： 本发明涉及通式I的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员并且任选地带有一个或两个取代基R的二价6元杂芳族基团 其选自卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4 - 烷基和C 1 -C 4 - 卤代烷基; Ar是苯基或6元杂芳族基团，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4， COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4烷基和C 1 -C 4卤代烷基， 对于与Ar的相邻C原子键合在一起为C 3 -C 4亚烷基的两个基团R b是可能的; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 C 1-4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如在专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与N-氧化物和生理上耐受的酸添加 这些化合物的盐和包含至少一种如权利要求1-10中任一项所述的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物和/或至少一种生理上耐受的酸性广告

    Human N-type calcium channel blockers
    9.
    发明申请
    Human N-type calcium channel blockers 审中-公开
    人类N型钙通道阻滞剂

    公开(公告)号：US20040204404A1

    公开(公告)日：2004-10-14

    申请号：US10674803

    申请日：2003-09-29

    发明人： Robert Zelle ,  Pravin Chaturvedi

    IPC分类号： A61K031/5415 ,  A61K031/498 ,  A61K031/495

    CPC分类号： A61K31/495 ,  A61K31/4468 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/5415

    摘要： This invention features a method for modulating human N-type calcium channel null1BnullSFVG subunit activity. The method includes administering to a subject in need thereof an effective amount of a compound of formula (I), (II), or (III): 1

    摘要翻译： 本发明的特征在于调节人类N型钙通道α1B+ SFVG亚基活性的方法。 该方法包括向有需要的受试者施用有效量的式（I），（II）或（III）化合物：

    Identification of compounds that inhibit replication of human immunodeficiency virus
    10.
    发明申请
    Identification of compounds that inhibit replication of human immunodeficiency virus 审中-公开
    鉴定抑制人类免疫缺陷病毒复制的化合物

    公开(公告)号：US20040180893A1

    公开(公告)日：2004-09-16

    申请号：US10783053

    申请日：2004-02-19

    发明人： Jan Maria Rene Balzarini ,  Anders Vahlne ,  Marita Hogberg ,  Weimin Tong

    IPC分类号： A61K031/5377 ,  A61K031/53 ,  A61K031/495 ,  A61K031/515 ,  A61K031/445

    CPC分类号： C07C237/06 ,  A61K31/164 ,  B01D15/34 ,  B01D15/362

    摘要： The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HIV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.

    摘要翻译： 本发明涉及发现抑制人类免疫缺陷病毒（HIV）复制的新一类化合物以及鉴定这些化合物的方法。 更具体地，已经发现酶制备的α-羟基甘氨酰胺和合成制备的α-羟基甘氨酰胺抑制人血清中HIV的复制。 实施方案包括鉴定修饰的抑制HIV的甘氨酰胺化合物的方法，分离和合成修饰的甘氨酰胺化合物的方法，以及包含这些化合物的治疗组合物。