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156 条记录 (耗时 0.077 秒)

    INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC N-SUBSTITUTED PIPERAZINE DERIVATIVES
    91.
    发明申请
    INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC N-SUBSTITUTED PIPERAZINE DERIVATIVES 有权
    吲哚，氮杂和相关杂环N-取代的哌嗪衍生物

    公开(公告)号：US20080132516A1

    公开(公告)日：2008-06-05

    申请号：US12028189

    申请日：2008-02-08

    申请人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J.J Kim Wright

    发明人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J.J Kim Wright

    IPC分类号： A61K31/496 ,  C07D401/14 ,  A61P31/18

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04

    摘要： This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is

    摘要翻译： 本发明提供具有药物和生物影响性质的式I化合物，包括其药学上可接受的盐，其药物组合物和使用方法。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 式I的化合物具有下式：其中：Z为Q选自m为2; A选自噌啉基，萘啶基，喹喔啉基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹唑啉基，氮杂苯并呋喃基和酞嗪基，其各自可以任选被一个或两个独立地选自甲基，甲氧基，羟基，氨基 和卤素; 和-W-是

    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
    92.
    发明授权
    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives 有权
    取代的氮杂脱氧乙酸哌嗪衍生物的组成和抗病毒活性

    公开(公告)号：US07354924B2

    公开(公告)日：2008-04-08

    申请号：US10969675

    申请日：2004-10-20

    申请人： Tao Wang ,  Zhongxing Zhang ,  Nicholas A. Meanwell ,  John F. Kadow ,  Zhiwei Yin ,  Qiufen May Xue ,  Alicia Regueiro-Ren ,  John D. Matiskella ,  Yasutsugu Ueda

    发明人： Tao Wang ,  Zhongxing Zhang ,  Nicholas A. Meanwell ,  John F. Kadow ,  Zhiwei Yin ,  Qiufen May Xue ,  Alicia Regueiro-Ren ,  John D. Matiskella ,  Yasutsugu Ueda

    IPC分类号： A61K31/496 ,  C07D487/02 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506

    CPC分类号： C07D471/04 ,  A61K31/496 ,  A61K45/06 ,  C07D491/048

    摘要： This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. Compound I is wherein: Q is selected from the group consisting of: m is 1 or 2; —W— is A is selected from the group consisting of C1-6alkoxy, aryl and heteroaryl; in which said aryl is phenyl or napthyl; said heteroaryl is selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, furanyl, thienyl, pyrrolyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothienyl, benzoimidazolyl and benzothiazolyl; and said aryl or heteroaryl is optionally substituted with one or two of the same or different members selected from the group consisting of amino, nitro, cyano, hydroxy, C1-6alkoxy, —C(O)NH2; and C1-6alkyl, —NHC(O)CH3, halogen and trifluoromethyl.

    摘要翻译： 本发明提供具有药物和生物影响性质的化合物I，其药物组合物和使用方法。 特别地，本发明涉及氮杂吲哚乙酰基哌嗪衍生物。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 化合物I是其中：Q选自：m是1或2; -W-是A选自C 1-6烷氧基，芳基和杂芳基; 其中所述芳基是苯基或萘基; 吡啶基，吡嗪基，咪唑基，噻唑基，异噻唑基，恶唑基，异恶唑基，喹啉基，异喹啉基，苯并呋喃基，苯并噻吩基，苯并咪唑基和苯并噻唑基; 并且所述芳基或杂芳基任选被一个或两个相同或不同的选自氨基，硝基，氰基，羟基，C 1-6烷氧基，-C（O） NH 2; 和C 1-6烷基，-NHC（O）CH 3，卤素和三氟甲基。

    4-aryl-3-hydroxyquinolin-2-one derivatives as ion channel modulators
    96.
    发明授权
    4-aryl-3-hydroxyquinolin-2-one derivatives as ion channel modulators 失效
    4-芳基-3-羟基喹啉-2-酮衍生物作为离子通道调节剂

    公开(公告)号：US5922735A

    公开(公告)日：1999-07-13

    申请号：US166273

    申请日：1998-10-05

    申请人： Sing-Yuen Sit ,  Nicholas A. Meanwell

    发明人： Sing-Yuen Sit ,  Nicholas A. Meanwell

    IPC分类号： C07D215/22 ,  A61K31/47 ,  A61P1/04 ,  A61P9/10 ,  A61P11/06 ,  A61P21/02 ,  A61P25/00 ,  A61P25/06 ,  A61P43/00 ,  C07D215/227 ,  A61K31/55

    CPC分类号： C07D215/227 ,  Y10S514/826

    摘要： There is provided novel substituted 4-aryl-3-hydroxyquinolin-2-one derivatives of the formula ##STR1## wherein R is hydrogen or methyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, bromo, chloro or trifluoromethyl, and when R.sup.1, R.sup.3 and R.sup.4 are hydrogen, R.sup.2 is nitro;R.sup.5 is hydrogen or methyl; andR.sup.6 is bromo or chloro;or a nontoxic pharmaceutically acceptable salt thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

    摘要翻译： 提供下式的新的取代的4-芳基-3-羟基喹啉-2-酮衍生物其中R是氢或甲基; R 1，R 2，R 3和R 4各自独立地为氢，溴，氯或三氟甲基，当R 1，R 3和R 4为氢时，R 2为硝基; R5是氢或甲基; 并且R 6是溴或氯; 或其无毒的药学上可接受的盐，其是大电导钙激活的钾通道的开放剂，并且可用于治疗对钾通道开放有反应的病症。

    Imidazo[4,5-b]quinolinyl oxy alkyl tetrazolyl piperidine derivatives
    97.
    发明授权
    Imidazo[4,5-b]quinolinyl oxy alkyl tetrazolyl piperidine derivatives 失效
    咪唑并[4,5-b]喹啉基氧基烷基四唑基哌啶衍生物

    公开(公告)号：US5348960A

    公开(公告)日：1994-09-20

    申请号：US114262

    申请日：1993-08-30

    申请人： Piyasena Hewawasam ,  Nicholas A. Meanwell

    发明人： Piyasena Hewawasam ,  Nicholas A. Meanwell

    IPC分类号： C07D471/04 ,  A61K31/445

    CPC分类号： C07D471/04

    摘要： A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or (CH.sub.2).sub.m R.sup.3 ;R.sup.3 is tetrahydro-2H-pyranyl, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy, or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.

    摘要翻译： 具有增强的水溶性生物利用度和代谢稳定性的一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的图像中，其中R1是H或C1-C4 低级烷基 R2是H或（CH2）mR3; R3是四氢-2H-吡喃基，C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。 该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

    7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones
    98.
    发明授权
    7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones 失效
    7-氧代丙基磺酰氨基 - 咪唑并[4,5-b]喹啉-2-酮

    公开(公告)号：US5208237A

    公开(公告)日：1993-05-04

    申请号：US862879

    申请日：1992-04-03

    申请人： Piyasena Hewawasam ,  Nicholas A. Meanwell

    发明人： Piyasena Hewawasam ,  Nicholas A. Meanwell

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ; benzoxazol-2yl, or benzothiazol2-yl;R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.

    摘要翻译： 具有增强的水溶性生物利用度和代谢稳定性的新一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的化合物中，其中R 1是H或C1- C4低级烷基; R2是H，（CH2）mR3; 苯并恶唑-2-基或苯并噻唑-2-基; R3是C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。 该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

    Arylpyrazole derivatives as anti-platelet agents
    99.
    发明授权
    Arylpyrazole derivatives as anti-platelet agents 失效
    芳吡唑衍生物作为抗血小板剂

    公开(公告)号：US5071866A

    公开(公告)日：1991-12-10

    申请号：US624822

    申请日：1990-12-10

    申请人： Nicholas A. Meanwell

    发明人： Nicholas A. Meanwell

    IPC分类号： C07D231/12 ,  C07D403/06 ,  C07D403/12

    CPC分类号： C07D231/12 ,  C07D403/06 ,  C07D403/12

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or phenyl, provided that R.sup.1 and R.sup.2 may not both be hydrogen;m is an integer from 3 to 9;n is an integer from 0 to 3 and the sum ofm+n is an integer from 5 to 12;Z is O, S, SO, SO.sub.2, --CH.dbd.CH-- or a direct bond;A is ##STR2## R.sup.3 is hydrogen or C.sub.1-6 alkyl; and R.sup.4 is hydrogen, C.sub.1-4 alkyl or methylsulfonyl;and pharmaceutically acceptable salts or hydrates thereof are novel inhibitors of adenosine diphosphate and collagen-induced aggregation of human platelet-rich plasma and are particularly useful as inhibitors of mammalian blood platelet aggregation.

    摘要翻译： 其中R 1和R 2各自独立地为氢或苯基，其中R 1和R 2不能均为氢; m为3〜9的整数; n为0〜3的整数，m + n的和为5〜12的整数。 Z是O，S，SO，SO 2，-CH = CH-或直接键; A是R 3是氢或C 1-6烷基; 且R 4为氢，C 1-4烷基或甲基磺酰基; 和其药学上可接受的盐或水合物是二磷酸腺苷和人血小板富集的胶原诱导的聚集的新型抑制剂，并且特别可用作哺乳动物血小板聚集的抑制剂。

    Triazine carboxylic acids and esters
    100.
    发明授权
    Triazine carboxylic acids and esters 失效
    三嗪羧酸和酯

    公开(公告)号：US5021415A

    公开(公告)日：1991-06-04

    申请号：US479563

    申请日：1990-02-13

    申请人： Nicholas A. Meanwell

    发明人： Nicholas A. Meanwell

    IPC分类号： C07D253/04 ,  C07D253/07

    CPC分类号： C07D253/04 ,  C07D253/07

    摘要： Heterocyclic acids and esters useful as inhibitors of mammalian blood platelet aggregation characterized by Formula I or II are disclosed. ##STR1## Formula I compounds are those wherein n is 6-9, R is hydrogen, lower alkyl or an alkali metal ion, and HET.sub.1 is the heterocyclic radical 2,3-dihydro-3-oxo-5,6-diphenyl-1,2,4-triazin-2-yl.Formula II compounds are those wherein R.sub.1 is hydrogen, lower alkyl or an alkali metal ion, and the radical --OCH.sub.2 CO.sub.2 R is attached in the 3 or 4 ring position; and HET.sub.2 is the heterocyclic radical 2,3-dihydro-3-oxo-5,6-diphenylmethyl-1,2,3-triazin-2-yl.

    摘要翻译： 公开了用作哺乳动物血小板聚集体抑制剂的杂环酸和酯，其特征在于式I或II。 （II）式I化合物是其中n为6-9，R为氢，低级烷基或碱金属离子的化合物，HET1为杂环基2,3-二氢 - 3-氧代-5,6-二苯基-1,2,4-三嗪-2-基。 式II化合物是其中R 1是氢，低级烷基或碱金属离子并且基团-OCH 2 CO 2 R连接在3或4环位置的化合物; HET2是杂环基2,3-二氢-3-氧代-5,6-二苯基甲基-1,2,3-三嗪-2-基。