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156 条记录 (耗时 0.067 秒)

    7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones
    81.
    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
    82.
    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
    83.
    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。

    Imidazole carboxylic acids and esters and inhibition of blood platelet aggregation therewith
    84.
    发明授权
    Imidazole carboxylic acids and esters and inhibition of blood platelet aggregation therewith 失效
    咪唑羧酸和酯类，抑制血小板聚集

    公开(公告)号：US5011851A

    公开(公告)日：1991-04-30

    申请号：US540988

    申请日：1990-06-20

    申请人： Nicholas A. Meanwell

    发明人： Nicholas A. Meanwell

    IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/84

    CPC分类号： C07D233/64 ,  C07D233/84

    摘要： Heterocyclic acids and esters useful as inhibitors of mammalian blood platelet aggregation characterized by Formula I or II are disclosed.HET.sub.1 --(CH.sub.2).sub.n CO.sub.2 R (I) ##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 4,5-diphenyl-1H-imidazol-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 4,5-diphenyl-1H-imidazol-2-yl.Formula VIII 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.

    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。 （VIII）式Ⅰ化合物是其中n为6-9的化合物，R为氢，低级烷基或碱金属离子，HET1为杂环基 自由基4,5-二苯基-1H-咪唑-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4,5-二苯基-1H-咪唑-2-基。 式VIII化合物是其中R 1是氢，低级烷基或碱金属离子，基团-OCH 2 CO 2 R连接在3或4个环位的那些。

    Imidazolidine carboxylic acids and esters as blood platelet aggregation inhibitors
    85.
    发明授权
    Imidazolidine carboxylic acids and esters as blood platelet aggregation inhibitors 失效
    咪唑烷羧酸和酯类作为血小板聚集抑制剂

    公开(公告)号：US4970225A

    公开(公告)日：1990-11-13

    申请号：US479564

    申请日：1990-02-13

    申请人： Nicholas A. Meanwell

    发明人： Nicholas A. Meanwell

    IPC分类号： C07D233/72 ,  C07D233/86

    CPC分类号： C07D233/86

    摘要： Heterocyclic acids and esters useful as inhibitors of mammalian blood platelet aggregation characterized by Formula I are disclosed.HET.sub.1 -(CH.sub.2).sub.n CO.sub.2 R (I)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 2,5-dioxo-3,4-diphenylimidazolidin-1-yl.

    摘要翻译： 公开了用作哺乳动物血小板聚集抑制剂的杂环酸和酯，其以式I为特征。 HET1-（CH2）nCO2R（I）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2,5-二氧代-3,4-二苯基咪唑烷 -1-基。

    Imidazoquinolinylether derivatives useful as phosphodiesterase and blood aggregation inhibitors
    86.
    发明授权
    Imidazoquinolinylether derivatives useful as phosphodiesterase and blood aggregation inhibitors 失效
    用作磷酸二酯酶和血液聚集抑制剂的咪唑喹啉醚衍生物

    公开(公告)号：US4775674A

    公开(公告)日：1988-10-04

    申请号：US866813

    申请日：1986-05-23

    申请人： Nicholas A. Meanwell ,  John J. Wright

    发明人： Nicholas A. Meanwell ,  John J. Wright

    IPC分类号： A61K31/47 ,  A61P7/02 ,  A61P9/04 ,  A61P43/00 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14

    CPC分类号： C07D471/04

    摘要： Novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyl ether derivatives of formula ##STR1## wherein R.sub.1 is hydrogen, lower alkly, benzyl; R.sub.2 is hydrogen, halogen, lower alkyl, lower alkoxy; Alk is alkylene; Y is hydroxy and alkanoic or aralkanoic esters thereof, oxo ketone, dialkylamino, carboxylic acid and esters, carboxamides, alkoxy, ethanolamines and cyclic carbamates thereof, tetrazolyl, and optionally substituted phenylsulfonyl. The compounds are cyclic AMP phosphodiesterase inhibitors and are particularly useful as inhibitors of blood platelet aggregation and/or as cardiotonic agents.

    摘要翻译： 新的一系列式（IMAGE）的2,3-二氢-2-氧代-1H-咪唑并[4,5-b]喹啉基醚衍生物，其中R1是氢，低级烷基，苄基; R2是氢，卤素，低级烷基，低级烷氧基; Alk是亚烷基; Y是羟基和其链烷酸或其芳烷酸酯，氧代酮，二烷基氨基，羧酸和酯，甲酰胺，烷氧基，乙醇胺和环状氨基甲酸酯，四唑基和任选取代的苯基磺酰基。 化合物是环AMP磷酸二酯酶抑制剂，并且特别可用作血小板聚集抑制剂和/或作为强心剂。