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    Thiadiazoles and their uses as antipicornaviral agents
    31.
    发明授权
    Thiadiazoles and their uses as antipicornaviral agents 失效
    噻二唑及其作为止痛药物的用途

    公开(公告)号：US5821257A

    公开(公告)日：1998-10-13

    申请号：US52178

    申请日：1998-03-31

    申请人： David J. Aldous ,  Thomas R. Bailey ,  Guy Dominic Diana ,  Theodore J. Nitz

    发明人： David J. Aldous ,  Thomas R. Bailey ,  Guy Dominic Diana ,  Theodore J. Nitz

    IPC分类号： C07D285/12 ,  A61K31/41 ,  A61K31/42 ,  A61K31/425 ,  A61K31/433 ,  A61K31/44 ,  A61K31/495 ,  A61K31/505 ,  A61P31/12 ,  A61P31/14 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/13 ,  C07D417/12

    CPC分类号： C07D417/12

    摘要： Compounds of the formula; ##STR1## wherein: Thi is thiadiazolyl or substituted thiadiazolyl alkoxy, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, halo, alkyl, cycloalkyl, hydroxyalkyl, or Y is alkylene bridge of 3-9 carbon atoms; R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl, or cyano; R.sub.3 is a heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, oxazolyl, thiazolyl, oxadiazolyl, isoxazolyl, isothiazolyl, or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl; or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.

    摘要翻译： 式的化合物; 式I其中：Thi是噻二唑基或取代的噻二唑基烷氧基，氟甲基，二氟甲基，三氟甲基，1,1-二氟乙基，卤素，烷基，环烷基，羟烷基或Y是3-9个碳原子的亚烷基桥; R 1和R 2各自独立地选自氢，卤素，烷基，烯基，氨基，烷硫基，羟基，羟基烷基，烷氧基烷基，烷硫基烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，烷氧基，硝基，羧基，烷氧基羰基，二烷基氨基烷基，烷基氨基烷基，氨基烷基，二氟甲基， ，或氰基; R3是选自苯并恶唑基，苯并噻唑基，噻二唑基，恶唑基，噻唑基，恶二唑基，异恶唑基，异噻唑基或取代的杂环基的杂环基，其中取代为烷基，烷氧基烷基，环烷基，卤代烷基，羟烷基，烷氧基，羟基，呋喃基，噻吩基或氟代烷基 ; 或其药学上可接受的盐是有效的抗虫病毒药剂。

    Thiadiazoles and their use as antipicornaviral agents
    33.
    发明授权
    Thiadiazoles and their use as antipicornaviral agents 失效
    噻二唑及其作为止痛药物的用途

    公开(公告)号：US5650419A

    公开(公告)日：1997-07-22

    申请号：US706108

    申请日：1996-08-30

    申请人： David J. Aldous ,  Thomas R. Bailey ,  Guy Dominic Diana ,  Theodore J. Nitz

    发明人： David J. Aldous ,  Thomas R. Bailey ,  Guy Dominic Diana ,  Theodore J. Nitz

    IPC分类号： C07D285/12 ,  A61K31/41 ,  A61K31/42 ,  A61K31/425 ,  A61K31/433 ,  A61K31/44 ,  A61K31/495 ,  A61K31/505 ,  A61P31/12 ,  A61P31/14 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/13 ,  C07D417/12

    CPC分类号： C07D417/12

    摘要： Described herein are compounds of the formula; ##STR1## wherein: Thi is a unsubstituted or substituted thiadiazolyl;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxylcarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, substituted or unsubstituted phenyl, alkyltetrazolyl or a substituted or unsubstituted imidazolyl, dihydroimidazolyl, pyrazolyl, furyl, thiazolyl or thienyl or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.

    摘要翻译： 本文描述的是式的化合物; 式I其中：Thi是未取代或取代的噻二唑基; Y是3-9个碳原子的亚烷基桥; R 1和R 2各自独立地选自氢，卤素，烷基，烯基，氨基，烷硫基，羟基，羟基烷基，烷氧基烷基，烷硫基烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，烷氧基，硝基，羧基，烷氧基羰基，二烷基氨基烷基，烷基氨基烷基，氨基烷基，二氟甲基， 氰基; R3是烷氧基羰基，取代或未取代的苯基，烷基四唑基或取代或未取代的咪唑基，二氢咪唑基，吡唑基，呋喃基，噻唑基或噻吩基或其药学上可接受的盐是有效的抗虫病毒剂。

    Antipicornaviral agents
    35.
    发明授权
    Antipicornaviral agents 失效
    止痒病毒药

    公开(公告)号：US5523312A

    公开(公告)日：1996-06-04

    申请号：US312724

    申请日：1994-09-27

    申请人： David J. Aldous ,  Thomas R. Bailey ,  Guy D. Diana ,  Gee-Hong Kuo ,  Theodore J. Nitz ,  Michael Reuman

    发明人： David J. Aldous ,  Thomas R. Bailey ,  Guy D. Diana ,  Gee-Hong Kuo ,  Theodore J. Nitz ,  Michael Reuman

    IPC分类号： C07D413/06 ,  C07D413/14 ,  A61K31/41 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06

    CPC分类号： C07D413/06 ,  C07D413/14

    摘要： Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 本文公开了用于对抗小核糖核酸病毒和预防或治疗小RNA病毒感染的化合物和药物组合物。 化合物具有下式：其中Het1选自恶唑基，异恶唑基，恶二唑基; Y是3〜9个碳原子的亚烷基桥; Het2是苯并呋喃基或吲哚基; R 1和R 2各自独立地选自氢，卤素，乙酰基，烷基，烯基，氨基，烷硫基，羟基，羟基烷基，烷氧基烷基，烷硫基烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，烷氧基，硝基，羧基，烷氧基羰基，二烷基氨基烷基，烷基氨基烷基，氨基烷基，二氟甲基 ，三氟甲基或氰基; 并且R 3是恶唑基，恶二唑基，异恶唑基或被烷基，卤素，烷氧基烷基，环烷基，卤代烷基，羟基烷基，烷氧基，羟基，呋喃基，噻吩基或氟代烷基取代的任何一个。 其N-氧化物或其药学上可接受的酸加成盐。

    SALTS OF (3-0-(3',3'-DIMETHYLSUCCINYL) BETULINIC ACID AND SOLID STATE FORMS THEREOF
    37.
    发明申请
    SALTS OF (3-0-(3',3'-DIMETHYLSUCCINYL) BETULINIC ACID AND SOLID STATE FORMS THEREOF 审中-公开
    （3-0-（3'，3'-二甲基氨基）乙酸和其固体状态的盐

    公开(公告)号：US20110224182A1

    公开(公告)日：2011-09-15

    申请号：US12504883

    申请日：2009-07-17

    申请人： Peter Bullock ,  Theodore J. Nitz ,  Gary Sweetapple

    发明人： Peter Bullock ,  Theodore J. Nitz ,  Gary Sweetapple

    IPC分类号： A61K31/56 ,  C07J53/00 ,  A61P31/18

    CPC分类号： C07J53/00

    摘要： The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, methods of making the compounds, polymorphic forms of the compounds, the compounds for use as medicaments, and use of the compounds for the manufacture of medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are certain salts of 3-O-(3′,3′-dimethylsuccinyl)betulinic acid, also known as “DSB.” The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (“HIV”).

    摘要翻译： 本发明涉及新颖的药物活性化合物，含有它们的药物组合物，制备化合物的方法，化合物的多晶型物，用作药物的化合物以及用于制备药物的化合物的用途。 本发明还涉及涉及给药化合物的治疗方法。 具体地说，这些化合物是3-O-（3'，3'-二甲基琥珀酰基）桦木酸的某些盐，也称为“DSB”。该新化合物可用作抗逆转录病毒剂。 特别地，新化合物可用于治疗人类免疫缺陷病毒（HIV）。