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228 条记录 (耗时 0.029 秒)

    Compositions and methods for inhibiting norovirus infection
    1.
    发明授权
    Compositions and methods for inhibiting norovirus infection 有权
    抑制诺如病毒感染的组合物和方法

    公开(公告)号：US09561239B2

    公开(公告)日：2017-02-07

    申请号：US15067337

    申请日：2016-03-11

    申请人： Children's Hospital Medical Center

    发明人： Xi Jiang ,  Ming Tan ,  Xufu Zhang

    IPC分类号： A61K31/56 ,  A61K31/57 ,  C07J41/00 ,  C07J7/00 ,  C07J9/00 ,  C07J3/00 ,  A61K31/568 ,  A61K31/575

    CPC分类号： A61K31/57 ,  A61K31/56 ,  A61K31/568 ,  A61K31/575 ,  C07J3/00 ,  C07J7/0005 ,  C07J7/002 ,  C07J9/00 ,  C07J9/005 ,  C07J41/0005 ,  C07J41/0016

    摘要： A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia is disclosed. The composition may contain a therapeutically effective amount of a binding-inhibiting compound and a carrier and/or excipient. The compounds may competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions may be administered to a human prior to or after infection by a Norovirus, to prevent, ameliorate, or reduce the effects of an infection.

    摘要翻译： 公开了用于抑制诺如病毒与上皮表面上的组织 - 血型抗原结合的组合物。 组合物可以含有治疗有效量的结合抑制化合物和载体和/或赋形剂。 这些化合物可能竞争性地结合具有与分泌型血型（包括A，B，AB和O血型）的组织 - 血型抗原结合能力的诺如病毒。 组合物可以在诺如病毒感染之前或之后施用于人，以预防，改善或减少感染的影响。

    Process for the preparation of fluticasone propionate
    6.
    发明授权
    Process for the preparation of fluticasone propionate 有权
    丙酸氟替卡松的制备方法

    公开(公告)号：US08344168B2

    公开(公告)日：2013-01-01

    申请号：US12329790

    申请日：2008-12-08

    申请人： Vinayak G. Gore ,  Mahesh Gadakar ,  K. Pokharkar ,  V. Wakchure

    发明人： Vinayak G. Gore ,  Mahesh Gadakar ,  K. Pokharkar ,  V. Wakchure

    IPC分类号： C07J3/00

    CPC分类号： C07J3/00 ,  C07J31/006

    摘要： The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.

    摘要翻译： 本发明涉及一种制备甾体17-羧酸硫代酯的方法。 更具体地说，本发明涉及使用可溶性混合氟化物通过置换化合物II中合适的离去基团X引入氟来引起选择性和受控氟化的方法和有效地合成类固醇17-羧酸硫酸酯，例如丙酸氟替卡松。 本发明还涉及中间体II及其制备方法。

    Method for the preparation of 6-α fluoro corticosteroids
    7.
    发明授权
    Method for the preparation of 6-α fluoro corticosteroids 有权
    6-α氟皮质激素的制备方法

    公开(公告)号：US07718793B2

    公开(公告)日：2010-05-18

    申请号：US11457280

    申请日：2006-07-13

    申请人： Shimon Chernyak ,  Martin Zarbov ,  Daniella Gutman

    发明人： Shimon Chernyak ,  Martin Zarbov ,  Daniella Gutman

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J71/00

    CPC分类号： C07J71/00 ,  C07J3/00

    摘要： A method for producing a 6α-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6α-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R1 may be, for example, acetate or propionate, The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®.

    摘要翻译： 通过使式II的17-羟基-12-酯环氧化物与立体选择性氟化剂反应制备6α-氟化皮质类固醇或其衍生物的方法立体选择性地形成式VII的21-酯-17-羟基6α-氟化化合物R1 可以是OC（O）-Rd; R4可以是C（O）-Rd; R3可以是H或Rd。 每个Rd可以相同或不同，并且独立地选自（C 1-4）烷基，芳基和杂芳基。 虚线可以是单键或双键。 R4可以是例如乙酰基; R3可以是例如α或β甲基; R1可以是例如乙酸酯或丙酸酯。反应中使用的立体选择性氟化剂可以是例如氟吡啶鎓或氟喹喔啉化合物，例如Selectfluor。

    Glucocorticosteroid compound having anti-inflammatory activity
    8.
    发明授权
    Glucocorticosteroid compound having anti-inflammatory activity 有权
    具有消炎活性的糖皮质激素化合物

    公开(公告)号：US07638508B2

    公开(公告)日：2009-12-29

    申请号：US11863390

    申请日：2007-09-28

    申请人： Keith Biggadike ,  Deborah Needham

    发明人： Keith Biggadike ,  Deborah Needham

    IPC分类号： A61K31/56 ,  C07J3/00

    CPC分类号： C07D233/54 ,  C07D215/26 ,  C07D451/02 ,  C07J1/0011 ,  C07J3/00

    摘要： A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the α or β configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and  represents a single or a double bond; or a physiologically acceptable salt or solvate thereof, and pharmaceutical formulations and methods of use thereof.

    摘要翻译： 式（I）的化合物：其中X表示O或S; R 1表示C 1-6烷基，C 3-8环烷基，C 3-8环烷基甲基或C 3-8环烯基，其任选可以被一个或多个甲基或卤素原子取代，或者R 1表示芳基，取代的芳基，杂芳基或取代的杂芳基; R 2表示氢，甲基，其可以是α或β构型，或亚甲基; R3和R4相同或不同，各自独立地表示氢，卤素或甲基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”4.57mm“file =”US07638508-20091229-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示单键或双键; 或其生理上可接受的盐或溶剂化物，以及药物制剂及其使用方法。

    NOVEL PROCESS AND INTERMEDIATES
    9.
    发明申请
    NOVEL PROCESS AND INTERMEDIATES 有权
    新进程和中间件

    公开(公告)号：US20090177001A1

    公开(公告)日：2009-07-09

    申请号：US12329790

    申请日：2008-12-08

    申请人： Vinayak G. Gore ,  Mahesh Gadakar ,  K. Pokharkar ,  V. Wakchure

    发明人： Vinayak G. Gore ,  Mahesh Gadakar ,  K. Pokharkar ,  V. Wakchure

    IPC分类号： C07J31/00

    CPC分类号： C07J3/00 ,  C07J31/006

    摘要： The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.

    摘要翻译： 本发明涉及一种制备甾体17β-羧酸硫酸酯的方法。 更具体地说，本发明涉及使用可溶性混合氟化物将甾族17β-羧酸硫酸酯如氟替卡松丙酸酯I的合成方法和有效的合成，通过置换化合物II中合适的离去基团X导致氟，从而导致选择性和受控的氟化。 本发明还涉及中间体II及其制备方法。

    Novel compounds
    10.
    发明申请
    Novel compounds 审中-公开
    新型化合物

    公开(公告)号：US20080021231A1

    公开(公告)日：2008-01-24

    申请号：US11863419

    申请日：2007-09-28

    申请人： KEITH BIGGADIKE ,  Deborah NEEDHAM

    发明人： KEITH BIGGADIKE ,  Deborah NEEDHAM

    IPC分类号： C07J3/00

    CPC分类号： C07D233/54 ,  C07D215/26 ,  C07D451/02 ,  C07J1/0011 ,  C07J3/00

    摘要： A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the α or β configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof.

    摘要翻译： 式（I）的化合物：其中X表示O或S; R 1表示C 1-6烷基，C 3-8环烷基，C 3-8环烷基甲基或C 其中任何一个可任选地被一个或多个甲基或卤素原子取代，或者R 1代表芳基，取代的芳基，杂芳基或取代的杂芳基; R 2表示氢，甲基，其可以是α或β构型，或亚甲基; R 3和R 4相同或不同，并且各自独立地表示氢，卤素或甲基; ＆lt; img id =“custom-character-00001”he =“2.79mm”wi =“4.91mm”file =“US20080021231A1-20080124-P00001.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键; 或其生理上可接受的盐或溶剂合物。