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74 条记录 (耗时 0.032 秒)

    Substituted quinoline derivatives useful as antipiconaviral agents
    51.
    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。

    1-cyclopropyl-4-pyridyl-quinolinones
    52.
    发明授权
    1-cyclopropyl-4-pyridyl-quinolinones 失效
    1-环丙基-4-吡啶基 - 喹啉酮

    公开(公告)号：US5330992A

    公开(公告)日：1994-07-19

    申请号：US967473

    申请日：1992-10-23

    申请人： Michael A. Eissenstat ,  John D. Weaver, III ,  Gee-Hong Kuo ,  Mark P. Wentland

    发明人： Michael A. Eissenstat ,  John D. Weaver, III ,  Gee-Hong Kuo ,  Mark P. Wentland

    IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/47 ,  C07D215/233

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; andAr is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.

    摘要翻译： 其中R 1是氢，低级烷基或三氟甲基的式IMAMA的化合物; R2是低级烷基，三氟甲基或CH2Z，其中Z是羟基，氯，低级烷基氨基或二元 - 烷基氨基; R3和R4各自为氢或氟; 并且Ar是苯基，芳族的5或6元杂环，或者它们在一个或多个位置被低级烷基，氟，氯，羟基，氨基，低级烷基氨基，二元 - 二烷基氨基，羧基，亚磺酰氨基，低级 烷基亚磺酰氨基，亚甲二氧基，三氟乙酰胺基，低级烷酰氨基或氨基甲酰基; 其药学上可接受的酸加成盐可用作抗癌剂。

    Imidazopyridines, compositions and use
    56.
    发明授权
    Imidazopyridines, compositions and use 失效
    咪唑并吡啶，组合物和用途

    公开(公告)号：US5010086A

    公开(公告)日：1991-04-23

    申请号：US564011

    申请日：1990-08-07

    申请人： George Y. Lesher, deceased ,  Edward R. Bacon ,  Baldev Singh ,  Gee-Hong Kuo

    发明人： George Y. Lesher, deceased ,  Edward R. Bacon ,  Baldev Singh ,  Gee-Hong Kuo

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4-or 3-pyridinyl, or N-oxides thereof, or phenyl or substituted phenyl.

    摘要翻译： 在6位具有芳基或杂芳基的1,3-二氢-2H-咪唑并[4,5-b]吡啶-2-酮可用作磷酸二酯酶抑制剂，通过2-氨基-5-（ 芳基或杂芳基）吡啶-3-羧酸与二苯基磷酰基叠氮化物。 该化合物具有式“IMAGE”，其中R 1和R 3是氢或低级烷基，R 5是低级烷基或氟代低级烷基，Ar是4-或3-吡啶基或其N-氧化物，或苯基或 取代的苯基。

    Phthalimido arylpiperazines useful in the treatment of benign prostatic hyperplasia
    58.
    发明授权
    Phthalimido arylpiperazines useful in the treatment of benign prostatic hyperplasia 有权
    邻苯二甲酰亚氨基芳基哌嗪可用于治疗良性前列腺增生

    公开(公告)号：US06780994B2

    公开(公告)日：2004-08-24

    申请号：US10207473

    申请日：2002-07-29

    申请人： Gee-Hong Kuo ,  William V. Murray ,  Catherine P. Prouty

    发明人： Gee-Hong Kuo ,  William V. Murray ,  Catherine P. Prouty

    IPC分类号： C07D29513

    CPC分类号： C07D209/48 ,  C07D401/04

    摘要： This invention relates to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

    摘要翻译： 本发明涉及一系列含有它们的式Iph药物组合物的杂环取代的哌嗪以及用于其制备的中间体。 本发明的化合物选择性地抑制与α-1a肾上腺素能受体的结合，α受体是与良性前列腺增生有关的受体。 因此，这些化合物潜在地用于治疗这种疾病。

    Therapeutic phenoxyalkylheterocycles
    59.
    发明授权
    Therapeutic phenoxyalkylheterocycles 失效
    治疗苯氧基烷基杂环

    公开(公告)号：US5763461A

    公开(公告)日：1998-06-09

    申请号：US822995

    申请日：1997-03-21

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

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

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  A61K31/44 ,  A61K31/415 ,  A61K31/47 ,  A61K31/505 ,  C07D213/16 ,  C07D239/26 ,  C07D401/10 ,  C07D403/10

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

    摘要： Compounds of the formula ##STR1## wherein Pyr is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substitutents chosen from alkyl, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkanoyl, fluoroalkyl or the N-oxide of any of these; 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, alkylsulfinylaikyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano; R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazlnyl, pyridazinyl or a substituted phenyl or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, halo alkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, or thienyl or fluoroalkyl, the N-oxide thereof, or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agents.

    摘要翻译： 下式的化合物其中Pyr选自吡啶基，吡唑基，嘧啶基，喹啉基，吲哚基和7-氮杂吲哚基，或者被一个或两个选自烷基，烷氧基，羟基，卤代的取代基取代的那些 氰基，硝基，羟基烷基，烷氧基烷基，烷酰基，氟代烷基或其中任何一种的N-氧化物; 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，三氟甲基或 氰基; R3是烷氧基羰基，烷基四唑基，苯基或选自苯并恶唑基，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，异唑基，异噻唑基，呋喃基，三唑基，噻吩基，吡啶基，嘧啶基，吡嗪基，哒嗪基或取代苯基 或取代的杂环基，其中取代为烷基，烷氧基烷基，环烷基，卤代烷基，羟基烷基，烷氧基，羟基，呋喃基或噻吩基或氟代烷基，其N-氧化物或其药学上可接受的酸加成盐是有效的抗虫病毒药剂。

    Therapeutic phenoxyalkylheterocycles
    60.
    发明授权
    Therapeutic phenoxyalkylheterocycles 失效
    治疗苯氧基烷基杂环

    公开(公告)号：US5618821A

    公开(公告)日：1997-04-08

    申请号：US451692

    申请日：1995-05-26

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

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

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  A61K31/44 ,  A61K31/505 ,  C07D213/16 ,  C07D239/26

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

    摘要： Compounds of the formula ##STR1## wherein Q is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substituents;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, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, substituted or unsubstituted phenyl or heterocyclyl, the N-oxide thereof, or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agent.

    摘要翻译： 式I的化合物，其中Q选自吡啶基，吡唑基，嘧啶基，喹啉基，吲哚基和7-氮杂吲哚基，或者被一个或两个取代基取代的那些; 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，三氟甲基或 氰基; R3是烷氧基羰基，烷基四唑基，取代或未取代的苯基或杂环基，其N-氧化物或其药学上可接受的酸加成盐是有效的抗虫病毒剂。