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14 条记录 (耗时 0.027 秒)

    Prodrug azide compositions and compounds
    1.
    发明授权
    Prodrug azide compositions and compounds 失效
    前药叠氮组合物和化合物

    公开(公告)号：US06271212B1

    公开(公告)日：2001-08-07

    申请号：US09033996

    申请日：1998-03-03

    申请人： Chung K. Chu ,  Lakshimi Kotra ,  Kostantine K. Manouilov ,  Jinfa Du ,  Raymond Schinazi

    发明人： Chung K. Chu ,  Lakshimi Kotra ,  Kostantine K. Manouilov ,  Jinfa Du ,  Raymond Schinazi

    IPC分类号： A61K3170

    CPC分类号： A61K31/7076 ,  A61K47/52 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

    摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

    摘要翻译： 提供药物前药组合物，其包含能够在体内转化为药物的药物的叠氮衍生物。 具有胺，酮和羟基取代基的药物的叠氮衍生物在体内转化为相应的药物，增加药物的半衰期。 此外叠氮化物前药通常比相应的药物更好地穿透血脑屏障。 特别有用的是虫草素，2'-F-ara-ddI，AraA，阿昔洛韦，喷昔洛韦和相关药物的叠氮衍生物。 有用的叠氮化物前药是治疗脂环族胺，酮和羟基取代的化合物的叠氮化物衍生物，包括芳烷基，杂环芳烷基和环状脂族化合物，其中胺或氧部分在环上，或胺或氧部分在其上 脂肪族侧链，以及治疗性嘌呤和嘧啶，核苷类似物和磷酸化核苷类似物。

    Antiviral activity and resolution of 2-hydroxymethyl-5- (5-fluorocytosin-1-yl)-1, 3-oxathiolane
    3.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5- (5-fluorocytosin-1-yl)-1, 3-oxathiolane 审中-公开
    2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号：US20050215527A1

    公开(公告)日：2005-09-29

    申请号：US11125943

    申请日：2005-05-09

    申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    IPC分类号： C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  A61K31/675 ,  A61K31/513 ,  C07D49/04

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。

    Use of (R)-penciclovir triphosphate for the manufacture of a medicament for the treatment of viral diseases
    6.
    发明申请
    Use of (R)-penciclovir triphosphate for the manufacture of a medicament for the treatment of viral diseases 审中-公开
    （R） - 昔洛韦三磷酸在制备用于治疗病毒性疾病的药物中的用途

    公开(公告)号：US20060069108A1

    公开(公告)日：2006-03-30

    申请号：US11231115

    申请日：2005-12-13

    申请人： Richard Vere Hodge ,  Raymond Schinazi

    发明人： Richard Vere Hodge ,  Raymond Schinazi

    IPC分类号： A61K31/522

    CPC分类号： A61K31/522 ,  A61K31/661

    摘要： A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.

    摘要翻译： 一种治疗方法：i）哺乳动物，包括人类中的HIV-1感染; 或ii）哺乳动物，包括人类中的HBV感染; 该方法包括向需要这种治疗的人施用有效量的式（A）化合物的三磷酸的（R） - 对映异构体或其药学上可接受的盐; 和用于该方法的化合物。

    HIV-1 mutations selected for by beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine
    9.
    发明申请
    HIV-1 mutations selected for by beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine 失效
    由β-2'，3'-二脱氢-2'，3'-二脱氧-5-氟胞苷选择的HIV-1突变

    公开(公告)号：US20070025964A1

    公开(公告)日：2007-02-01

    申请号：US11542044

    申请日：2006-10-03

    申请人： Raymond Schinazi ,  Jennifer Hammond ,  John Mellors ,  Dennis Liotta

    发明人： Raymond Schinazi ,  Jennifer Hammond ,  John Mellors ,  Dennis Liotta

    IPC分类号： A61K38/21 ,  A61K31/7076 ,  A61K31/7072 ,  A61K31/522 ,  A61K31/538 ,  A61K31/513

    CPC分类号： A61K31/513 ,  A61K31/522 ,  A61K31/538 ,  A61K31/7072 ,  A61K31/7076 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention discloses a method for treating HIV that includes administering β-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.

    摘要翻译： 本发明公开了一种治疗艾滋病毒的方法，其包括向需要治疗的人组合或交替给予β-D-D4FC或其药学上可接受的盐或前药，所述药物在其它位置诱导HIV-1中的突变 比70（K至N），90或反转录酶区域的172个密码子。 还公开了将β-D-D4FC用作对其他抗HIV药物具有耐药性的患者的“补救疗法”的方法。 一般来说，β-D-D4FC可用于任何对在70（K至N），90或172个密码子以外诱导突变的药物具有抗性的患者的补救疗法。

    Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
    10.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane 有权
    2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号：US20060276492A1

    公开(公告)日：2006-12-07

    申请号：US11390861

    申请日：2006-03-28

    申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    IPC分类号： A61K31/513 ,  C07D409/04

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。