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    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole
    5.
    发明申请
    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole 审中-公开
    包含唑类的β淀粉样蛋白的杂环磺酰胺抑制剂

    公开(公告)号：US20100144812A1

    公开(公告)日：2010-06-10

    申请号：US12708557

    申请日：2010-02-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A61K31/4155 ,  A61K31/415 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4025 ,  A61P25/28 ,  A61P25/00 ,  C07D409/02 ,  C07D231/10

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
    6.
    发明授权
    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
    含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂

    公开(公告)号：US07674813B2

    公开(公告)日：2010-03-09

    申请号：US12142306

    申请日：2008-06-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A01N43/50 ,  A01N43/56 ,  C07D231/00

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    PRODUCTION OF CHIRALLY PURE AMINO ALCOHOL INTERMEDIATES, DERIVATIVES THEREOF, AND USES THEREOF
    8.
    发明申请
    PRODUCTION OF CHIRALLY PURE AMINO ALCOHOL INTERMEDIATES, DERIVATIVES THEREOF, AND USES THEREOF 失效
    生产纯氨基醇的中间体，其衍生物及其用途

    公开(公告)号：US20100016639A1

    公开(公告)日：2010-01-21

    申请号：US12546121

    申请日：2009-08-24

    申请人： John Sellstedt ,  Gloria Cheal ,  Razzak Noureldin ,  Anita Wai-Yin Chan ,  Panolil Raveendranath ,  Thomas Joseph Caggiano

    发明人： John Sellstedt ,  Gloria Cheal ,  Razzak Noureldin ,  Anita Wai-Yin Chan ,  Panolil Raveendranath ,  Thomas Joseph Caggiano

    IPC分类号： C07C209/00

    CPC分类号： C07C213/02 ,  C07B2200/07 ,  C07C215/08 ,  C07D333/34

    摘要： A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated with alkyl, substituted aryl or substituted heteroaryl is described. The method involves reacting a di-tert-butyl diazene-1,2-dicarboxylate with a (4S)-4-benzyl-3-[(S)-trifluoromethyl-alkyl substituted alkanoyl]-1,3-oxazolidin-2-one to afford a di-tert-butyl 1-(1S,2S)-([(4S)-4-benzyl-2-oxo-1,3-oxazolidine-3-yl]-carbonyl}-trifluoromethyl-alkyl substituted alkyl)hydrazine-1,2-dicarboxylate. This dicarboxylate is then reduced to yield di-tert-butyl 1-(1S,2S)-[trifluoromethyl-alkyl substituted alkyl]hydrazine-1-(hydroxymethyl)-1,2-dicarboxylate. The resulting product is deblocked with an acid to yield the acid addition salt of (2S,3S)-trifluoro-hydrazino-methyl alkan-1-ol. The acid addition salt of (2S,3S)-trifluoro-2-hydrazino-methyl alkan-1-ol is hydrogenated in the presence of a suitable metal catalyst to yield the amino alcohol (2S,3S)-2-amino-trifluoro-methyl alkan-1-ol HCl.

    摘要翻译： 描述了选择性制备可用于制备用烷基，取代的芳基或取代的杂芳基磺化或酰化的酰胺的手性2S-氨基醇的方法。 该方法包括使二噻唑-1,2-二羧酸二叔丁酯与（4S）-4-苄基-3 - [（S） - 三氟甲基 - 烷基取代的烷酰基] -1,3-恶唑烷-2-酮 得到1-（1S，2S） - （[（4S）-4-苄基-2-氧代-1,3-恶唑烷-3-基] - 羰基} - 三氟甲基 - 烷基取代的烷基的二 - 叔丁基） 肼-1,2-二羧酸。 然后将该二羧酸酯还原，得到1-（1S，2S） - [三氟甲基 - 烷基取代的烷基]肼-1-（羟甲基）-1,2-二羧酸二叔丁酯。 所得产物用酸解封，得到（2S，3S） - 三氟 - 肼基 - 甲基烷-1-醇的酸加成盐。 （2S，3S） - 三氟-2-肼基 - 甲基烷-1-醇的酸加成盐在合适的金属催化剂存在下氢化，得到氨基醇（2S，3S）-2-氨基 - 三氟 - 甲基链烷-1-醇HCl。

    Tricyclic diazepines tocolytic oxytocin receptor antagonists
    9.
    发明授权
    Tricyclic diazepines tocolytic oxytocin receptor antagonists 失效
    三环二氮嗪类溶瘤性催产素受体拮抗剂

    公开(公告)号：US07109193B2

    公开(公告)日：2006-09-19

    申请号：US10119971

    申请日：2002-04-10

    申请人： Amedeo Arturo Failli ,  Jay Scott Shumsky ,  Thomas Joseph Caggiano ,  Joseph Peter Sabatucci ,  Kevin Anthony Memoli ,  Eugene John Trybulski

    发明人： Amedeo Arturo Failli ,  Jay Scott Shumsky ,  Thomas Joseph Caggiano ,  Joseph Peter Sabatucci ,  Kevin Anthony Memoli ,  Eugene John Trybulski

    IPC分类号： A61P15/00 ,  A61K31/55 ,  C07D487/12

    CPC分类号： C07D487/04 ,  C07D487/14

    摘要： This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

    摘要翻译： 本发明提供新的三环二氮杂类化合物以及利用这些化合物治疗和/或预防和/或抑制可由催产素拮抗剂活性治疗或减轻的疾病的方法和药物组合物，包括治疗早产，痛经，子宫内膜炎 ，并在剖宫产分娩前抑制劳动。 这些化合物也可用于提高生育率，提高农场动物的生存率和发情同步; 并且可用于预防和治疗包括强迫症（OCD）和神经精神障碍在内的催产素系统在中枢神经系统中的功能障碍。