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    Substituted quinoline derivatives useful as antipiconaviral agents
    2.
    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
    3.
    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
    4.
    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。

    Haloalkoxy phenyl 4,5 dihydro oxazoles
    5.
    发明授权
    Haloalkoxy phenyl 4,5 dihydro oxazoles 失效
    卤代烷氧基苯基4,5-二氢恶唑

    公开(公告)号：US4939267A

    公开(公告)日：1990-07-03

    申请号：US364913

    申请日：1989-06-12

    申请人： Guy D. Diana

    发明人： Guy D. Diana

    IPC分类号： A61L15/60 ,  C07D261/04 ,  C07D261/08 ,  C07D263/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D413/12 ,  A61L15/60 ,  C07C255/00 ,  C07D261/08 ,  C07D263/14 ,  C07D413/10 ,  C07D417/12

    摘要： Compounds of the formulas: ##STR1## wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed.

    摘要翻译： 下式的化合物：其中Het是恶唑或恶嗪部分; X为O，S或SO，n为3〜9的整数，Y为脂肪族桥; 并且各种R基团表示氢或本文所述的各种取代基，可用作抗病毒剂，特别是对小核糖核酸病毒。 用于式I化合物的N-（氯代烷基）酰胺中间体也作为抗病毒剂是有活性的。 还公开了上述式的范围之外的相关化合物。

    N,N'-Bridged-bis[N,N'substituted-2-hydroxy alkaneammonium] salts
    9.
    发明授权
    N,N'-Bridged-bis[N,N'substituted-2-hydroxy alkaneammonium] salts 失效
    N，N {40-双 - {{N，N {40-取代-2-羟烷基铵{9 {0盐

    公开(公告)号：US4119668A

    公开(公告)日：1978-10-10

    申请号：US833485

    申请日：1977-09-15

    申请人： Guy D. Diana ,  Royal A. Cutler

    发明人： Guy D. Diana ,  Royal A. Cutler

    IPC分类号： C07C291/04 ,  C07C87/30 ,  A61K31/14

    CPC分类号： C07C291/04

    摘要： N,N'-Bridged-bis[(O and/or N-substituted)-2-alkyl-2-hydroxyethylamines] of the formula ##STR1## are prepared by condensing an epoxide of the formula ##STR2## and a diamine of the formula R'NH-X-NHR'. The products and dicarbanilates, acid-addition salts, N,N'-dioxides and N,N'-diammonium quaternary salts derived therefrom have antibacterial activity in vitro and are useful as antibacterial agents.

    摘要翻译： 式“IMAGE”的N，N'-桥连双[（O和/或N-取代的）-2-烷基-2-羟乙基胺]是通过将式“IMAGE”的环氧化物与 式R'NH-X-NHR'。 由其衍生的产物和二羧酸酯，酸加成盐，N，N'-二氧化物和N，N'-二铵季盐在体外具有抗菌活性，可用作抗菌剂。

    1-Ethoxy-3,4-dihydroisoquindines
    10.
    发明授权
    1-Ethoxy-3,4-dihydroisoquindines 失效
    1-乙氧基-3,4-二氢异喹啉

    公开(公告)号：US4009170A

    公开(公告)日：1977-02-22

    申请号：US277051

    申请日：1972-08-01

    申请人： Guy D. Diana

    发明人： Guy D. Diana

    IPC分类号： C07D217/22 ,  C07D217/24

    CPC分类号： C07D217/22

    摘要： 1-(2-Substituted-hydrazino)-3,4-dihydroisoquinolines, prepared in one process by alkylating the corresponding 3,4-dihydroisocarbostyrils, hydrazinolyzing the resulting 1-alkoxy-3,4-dihydroisoquinolines and condensing the resulting 1-hydrazIno-3,4-dihydroisoquinolines with aldehydes or ketones, and 1,1'-azinobis(1,2,3,4-tetrahydroisoquinolines), prepared by condensing corresponding 1-alkoxy-3,4-dihydroisoquinolines and 1-hydrazino-3,4-dihydroisoquinolines, are useful as antihypertensive agents and/or as antiinflammatory agents.

    摘要翻译： 1-（2-取代 - 肼基）-3,4-二氢异喹啉，通过烷基化相应的3,4-二氢异卡波姆斯特尔在一个方法中制备，肼解所得1-烷氧基-3,4-二氢异喹啉并将所得的1-肼基 - 通过将相应的1-烷氧基-3,4-二氢异喹啉和1-肼基-3,4-二氢异喹啉缩合制备的具有醛或酮的3,4-二氢异喹啉和1,1'-氮杂双（1,2,3,4-四氢异喹啉） - 二氢异喹啉可用作抗高血压药和/或作为抗炎剂。