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    2-imidazoline, 2-oxazoline, 2-thiazoline, and 4-imidazole derivatives of methylphenyl, methoxphenyl, and aminophenyl alkylsulfonamides and ureas and their use
    1.
    发明授权
    2-imidazoline, 2-oxazoline, 2-thiazoline, and 4-imidazole derivatives of methylphenyl, methoxphenyl, and aminophenyl alkylsulfonamides and ureas and their use 失效
    2-咪唑啉，2-恶唑啉，2-噻唑啉和甲基苯基，甲氧基苯基和氨基苯基烷基磺酰胺和脲的4-咪唑衍生物及其用途

    公开(公告)号：US06057349A

    公开(公告)日：2000-05-02

    申请号：US264467

    申请日：1999-03-08

    申请人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

    发明人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

    IPC分类号： C07D233/20 ,  A61K31/00 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61P3/00 ,  A61P3/04 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P27/00 ,  A61P27/16 ,  A61P43/00 ,  C07D20060101 ,  C07D209/08 ,  C07D233/08 ,  C07D233/22 ,  C07D233/24 ,  C07D233/50 ,  C07D233/54 ,  C07D233/64 ,  C07D233/66 ,  C07D263/28 ,  C07D263/38 ,  C07D263/64 ,  C07D277/10 ,  C07D277/18 ,  C07D277/28 ,  C07D277/34 ,  C07D277/38 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12

    CPC分类号： C07D233/64 ,  C07D233/22 ,  C07D233/24 ,  C07D233/50 ,  C07D263/28 ,  C07D403/06 ,  C07D403/12

    摘要： The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is [2-imidazoline, 2-oxazolin] 2-thiazoline, [or 4-imidazole] R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5- or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or --CN, with the proviso that, when R.sup.7 is hydroxyl or lower alkylsulfonamido, then X is not --NH-- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R.sup.1 SO.sub.2 NR.sup.2 --), (R.sup.3 R.sup.60 NSO.sub.2 NR.sup.2 --), or (R.sup.3 R.sup.60 NCONR.sup.2 --). The invention also includes the use of the above compounds, and compositions containing them, as alpha.sub.1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.

    摘要翻译： 本发明涉及由下式表示的新化合物：其中：A为R 1q（R 3 R 60 N）m（Z）（NR 2）n; m和q各自为0或1，条件是当q为1时，m为0，当q为0时，m为1; Z是C = O或SO 2; n为1，条件是当Z为C = O时，m为1; X是-NH-，-CH 2 - 或-OCH 2 - ; Y是[2-咪唑啉，2-恶唑啉] -2-噻唑啉，[或4-咪唑] R 1是H，低级烷基或苯基，条件是当R 1是H时，m是1; R 2，R 3，R 60各自独立地为H，低级烷基或苯基; R4，R5，R6和R7各自独立地为氢，低级烷基，-CF3，低级烷氧基，卤素，苯基，低级烯基，羟基，低级烷基亚磺酰氨基或低级环烷基，其中R2和R7任选地可以一起形成亚烷基 或未取代或任选取代的5元或6元环中2至3个原子的亚烯基，其中环上任选取代基为卤素，低级烷基或-CN，前提条件是当R 7为羟基或低级烷基亚磺酰氨基 那么当Y是2-咪唑啉时，X不是-NH-。 所述化合物包括上述药学上可接受的盐。 在上述式A中可以是例如（R 1 SO 2 NR 2 - ），（R 3 R 60 NSO 2 NR 2 - ）或（R 3 R 60 NCONR 2 - ）。 本发明还包括上述化合物和含有它们的组合物作为α1A/ 1L激动剂在治疗各种疾病状态如尿失禁，鼻充血，阴茎异常勃起，抑郁，焦虑，痴呆，衰老，阿尔茨海默病，阿尔茨海默病， 注意力和认知，以及进食障碍，如肥胖，贪食症和厌食症。

    2-substituted 5-chlorimidazoles
    8.
    发明授权
    2-substituted 5-chlorimidazoles 失效
    2-取代的5-氯咪唑

    公开(公告)号：US5484939A

    公开(公告)日：1996-01-16

    申请号：US208956

    申请日：1994-03-11

    申请人： Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

    发明人： Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

    IPC分类号： C07D233/68 ,  C07D233/08

    CPC分类号： C07D233/68

    摘要： The 2-substituted 5-chlorimidazoles of general formula: ##STR1## are new intermediate products for the production of antihypertensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.1 is hydrogen, to the 2-substituted 5-chlorimidazole-4-carbaldehydes of general formula: ##STR2##

    摘要翻译： 2-取代的5-氯咪唑，其通式如下：图1是生产抗高血压药剂或除草化合物的新中间产物。 制备这些中间体产物的方法以及通式I的其它R 1为氢的2-取代的5-氯咪唑与2-取代的5-取代的5-氯咪唑-4-碳醛进一步反应的新方法 公式： II