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    Extended triterpene derivatives
    2.
    发明授权
    Extended triterpene derivatives 有权
    扩展三萜衍生物

    公开(公告)号：US09505800B2

    公开(公告)日：2016-11-29

    申请号：US12513454

    申请日：2007-11-02

    申请人： Theodore J. Nitz ,  Christian Montalbetti ,  Richard Mears ,  Xinjie Gai ,  Edward Glenn

    发明人： Theodore J. Nitz ,  Christian Montalbetti ,  Richard Mears ,  Xinjie Gai ,  Edward Glenn

    IPC分类号： A61K31/56 ,  C07J53/00

    CPC分类号： C07J63/008 ,  A61K31/57 ,  A61K31/58 ,  A61K45/06 ,  C07J53/00

    摘要： The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. 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学活性三萜衍生物，含有它们的药物组合物，它们作为药物的用途，以及该化合物在制备特定药物中的用途。 本发明还涉及涉及给药化合物的治疗方法。 具体地，化合物是在本文进一步描述的C-3，C 2-8和C-19位置的一个或多个处具有取代的桦木酸的衍生物。 新型化合物可用作抗逆转录病毒药物。 特别地，新化合物可用于治疗人类免疫缺陷病毒（HIV）。

    Substituted quinoline derivatives useful as antipiconaviral agents
    5.
    发明授权
    Substituted quinoline derivatives useful as antipiconaviral agents 失效
    可用作抗病毒药物的取代喹啉衍生物

    公开(公告)号：US5514692A

    公开(公告)日：1996-05-07

    申请号：US449463

    申请日：1995-05-24

    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 ,  A61K31/47 ,  C07D401/04

    CPC分类号： C07D413/06 ,  C07D413/14

    摘要： The invention discloses compounds of the formula ##STR1## wherein, Het.sub.1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolylY is an alkylene bridge of 3 to 9 carbon atoms.Het.sub.2 is quinolyl quinolyl substituted by R.sub.1 and R.sub.2 ;R.sub.1 and R.sub.2 are each individually 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 alkyltetrazolyl, or substituted or unsubstituted heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof are effective antipicornaviral agents.

    摘要翻译： 本发明公开了下式化合物：其中Het1选自取代或未取代的呋喃基，恶唑基，异恶唑基，恶二唑基，四唑基，噻二唑基，Y为3至9个碳原子的亚烷基桥。 Het2是被R1和R2取代的喹啉基喹啉基; 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是烷基四唑基，或者是取代或未取代的选自苯并恶唑基，苯并噻唑基，噻二唑基，咪唑基，二氢咪唑基，恶唑基，噻唑基，恶二唑基，吡唑基，噻唑基，恶唑基，呋喃基，三唑基，四唑基，噻吩基，其N-氧化物或其药学上可接受的酸 其加成盐是有效的抗虫病毒药剂。

    Therapeutic phenoxyalklpyridazines and intermediates therefor
    6.
    发明授权
    Therapeutic phenoxyalklpyridazines and intermediates therefor 失效
    治疗性苯氧亚胺idaz嗪及其中间体

    公开(公告)号：US5514679A

    公开(公告)日：1996-05-07

    申请号：US242528

    申请日：1994-05-13

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

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

    IPC分类号： C07D237/08 ,  C07D307/42 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D413/12 ,  C07D413/14 ,  A61K31/50 ,  C07D237/12

    CPC分类号： C07D307/42 ,  C07D237/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D413/12 ,  C07D413/14

    摘要： Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.

    摘要翻译： 其中：R1和R2独立地是氢，卤素，烷基，烯基，烷氧基，羟基，羟基烷基，羟基卤代烷基，烷氧基烷基，烷基硫代炔基，羟基烷氧基，烷基硫代烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，氨基，氨基烷基，烷基氨基烷基 ，二烷基氨基烷基，烷氧基羰基，羧基或氰基甲基，硝基，二氟甲基，三氟甲基或氰基; Y为3至9个碳原子的亚烷基; R3和R4独立地是氢，烷基，烷氧基，羟基，环烷基，羟基烷基，羟基卤代烷基，烷氧基烷基，羟基烷氧基，烷硫基烷基，烷酰基，烷酰氧基，烷基亚磺酰基烷基，烷基磺酰基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基羰基，羧基，氰基甲基，氟代烷基， ，炔基，烯烃或卤素; R5是烷氧基羰基，烷基四唑基，苯基或杂环; 或其药学上可接受的酸加成盐; 其N-氧化物可用作抗血管病毒药物。

    1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
    7.
    发明授权
    1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents 失效
    1,2,4-恶二唑基 - 苯氧基烷基异恶唑及其作为抗病毒剂的用途

    公开(公告)号：US5464848A

    公开(公告)日：1995-11-07

    申请号：US131050

    申请日：1993-10-01

    申请人： Guy D. Diana ,  Theodore J. Nitz

    发明人： Guy D. Diana ,  Theodore J. Nitz

    IPC分类号： A61K31/42 ,  A61K31/422 ,  A61K31/4245 ,  A61P31/12 ,  C07D413/12 ,  C07D413/14 ,  A61K31/41

    CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14

    摘要： Compounds of the formula ##STR1## wherein: R.sub.1 is alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, or cyanomethyl;Y is alkylene of 3 to 9 carbon atoms,R.sub.2 and R.sub.3 independently are hydrogen, alkyl, alkoxy, halo, cyano, trifluoromethyl and nitro;R.sub.4 is alkoxy, hydroxy, halomethyl, dihalomethyl, trihalomethyl, dihaloethyl, cycloalkyl, heterocyclyl, alkoxycarbonyl, hydroxyalkyl, alkoxyalkyl, alkanecarbonyloxyalkyl, cyano, halo, thioalkyl, alkylthioalkyl, alkylthio, thio, 2,2,2-trifluoro-ethyl, (4-methylphenyl)sulfonyloxymethyl, N.dbd.Q or CON.dbd.Q, where N.dbd.Q is amino, alkylamino or dialkylamino;R.sub.5 is hydrogen or halo or alkyl.

    摘要翻译： 其中：R1是烷基，烷氧基，羟基，环烷基，羟基烷基，烷氧基烷基，羟基烷氧基，烷基硫代烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基羰基，羧基或氰基甲基。 Y是3至9个碳原子的亚烷基，R2和R3独立地是氢，烷基，烷氧基，卤素，氰基，三氟甲基和硝基; R4是烷氧基，羟基，卤代甲基，二卤代甲基，三卤代甲基，二卤代乙基，环烷基，杂环基，烷氧基羰基，羟基烷基，烷氧基烷基，烷基羰氧基烷基，氰基，卤素，硫代烷基，烷基硫代烷基，烷硫基，硫代，2,2,2-三氟乙基，（4 - 甲基苯基）磺酰氧基甲基，N = Q或CON = Q，其中N = Q是氨基，烷基氨基或二烷基氨基; R5是氢或卤素或烷基。

    OXADIAZOLYL-PHENOXYALKYLISOXAZOLES, COMPOSITIONS THEREOF AND METHODS FOR THEIR USE AS ANTI-PICORNAVIRAL AGENTS
    9.
    发明申请
    OXADIAZOLYL-PHENOXYALKYLISOXAZOLES, COMPOSITIONS THEREOF AND METHODS FOR THEIR USE AS ANTI-PICORNAVIRAL AGENTS 审中-公开
    氧杂环丙烷基 - 苯氧基甲基咪唑，其组合物及其作为抗血清药物使用的方法

    公开(公告)号：US20090291990A1

    公开(公告)日：2009-11-26

    申请号：US12535158

    申请日：2009-08-04

    申请人： Gerald Rhodes ,  Theodore J. Nitz

    发明人： Gerald Rhodes ,  Theodore J. Nitz

    IPC分类号： A61K31/4245 ,  A61P31/12

    CPC分类号： C07D413/12

    摘要： Oxadiazolyl-phenoxyalkylisoxazoles and pharmaceutically acceptable salts thereof, compositions comprising oxadiazolyl-phenoxyalkylisoxazole compounds or pharmaceutically acceptable salts thereof and methods for using oxadiazolyl-phenoxyalkylisoxzazole compounds or pharmaceutically acceptable salts thereof as anti-picornaviral agents are described herein. The methods include using pleconaril as a prodrug for conversion to anti-picornaviral compounds in vivo.

    摘要翻译： 本文描述了恶二唑基 - 苯氧基烷基异恶唑及其药学上可接受的盐，其包含恶二唑基 - 苯氧基烷基异恶唑化合物或其药学上可接受的盐和使用恶二唑基 - 苯氧基烷基异唑唑化合物或其药学上可接受的盐作为抗小核糖核酸病毒剂的方法。 所述方法包括使用pleconaril作为在体内转化成抗小刀毒蛋白病毒化合物的前药。