利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

11 条记录 (耗时 0.02 秒)

    Substituted 3-cyano quinolines
    3.
    发明授权
    Substituted 3-cyano quinolines 失效

    公开(公告)号：US6002008A

    公开(公告)日：1999-12-14

    申请号：US49718

    申请日：1998-03-27

    申请人： Allan Wissner ,  Bernard D. Johnson ,  Marvin F. Reich ,  Middleton B. Floyd, Jr. ,  Douglas B. Kitchen ,  Hwei-Ru Tsou

    发明人： Allan Wissner ,  Bernard D. Johnson ,  Marvin F. Reich ,  Middleton B. Floyd, Jr. ,  Douglas B. Kitchen ,  Hwei-Ru Tsou

    IPC分类号： C07D215/54 ,  C07D215/56 ,  C07D401/04 ,  C07D401/12 ,  C07D409/12 ,  A01N43/42 ,  C07D215/16 ,  C07D215/38

    CPC分类号： C07D401/04 ,  C07D215/54 ,  C07D215/56 ,  C07D401/12 ,  C07D409/12

    摘要： This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.5 is alkyl which may be optionally substituted, or phenyl which may be optionally substituted;R.sub.6 is hydrogen, alkyl, or alkenyl;R.sub.7 is chloro or bromoR.sub.8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl, alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl+, chloro, fluoro, or bromo;Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino, piperazino, N-alkylpiperazino, or pyrrolidino;m=1-4,q=1-3, and p=0-3;any of the substituents R.sub.1, R.sub.2, R.sub.3, or R.sub.4 that are located on contiguous carbon atoms can together be the divalent radical --O--C(R.sub.8).sub.2 --O--;or a pharmaceutically acceptable salt thereof with the proviso that when Y is --NH--, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen, and n is 0, X is not 2-methylphenyl, which are inhibitors of protein tyrosine kinase.

    SGLT-2 INHIBITORS, METHODS OF MAKING THEM, AND USES THEREOF
    6.
    发明申请
    SGLT-2 INHIBITORS, METHODS OF MAKING THEM, AND USES THEREOF 失效
    SGLT-2抑制剂，其制备方法及其用途

    公开(公告)号：US20110237527A1

    公开(公告)日：2011-09-29

    申请号：US13052171

    申请日：2011-03-21

    申请人： Shuang LIU ,  Cheng GUO ,  Min HU ,  Douglas B. KITCHEN ,  Peter R. GUZZO ,  Russell DEORAZIO

    发明人： Shuang LIU ,  Cheng GUO ,  Min HU ,  Douglas B. KITCHEN ,  Peter R. GUZZO ,  Russell DEORAZIO

    IPC分类号： A61K31/706 ,  C07H7/06 ,  A61P3/10 ,  A61P27/12 ,  A61P3/06 ,  A61P3/04 ,  A61P17/02 ,  A61P9/10 ,  A61P9/12 ,  A61P19/06

    CPC分类号： A61K31/706

    摘要： The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.

    摘要翻译： 本发明涉及作为钠依赖性葡萄糖共转运体-2（SGLT-2）抑制剂的化合物。 这些化合物用于治疗各种疾病，包括糖尿病，葡萄糖耐量降低，胰岛素抵抗，视网膜病变，肾病，神经病，白内障，高血糖症，高胰岛素血症，高胆固醇血症，游离脂肪酸或甘油血液水平升高，高脂血症，高甘油三酯血症，肥胖 伤口愈合，组织缺血，动脉粥样硬化和高血压。 这些化合物和组合物还可用于治疗和预防肾结石，高尿酸血症，痛风和低钠血症。 制备这些化合物的方法也在本发明中描述。

    Biaryl-pyridoquinazolinone derivatives as anti-cancer agents
    9.
    发明授权
    Biaryl-pyridoquinazolinone derivatives as anti-cancer agents 失效
    二芳基吡啶并喹唑啉酮衍生物作为抗癌剂

    公开(公告)号：US5914327A

    公开(公告)日：1999-06-22

    申请号：US965552

    申请日：1997-11-06

    申请人： Michael P. Trova ,  Nan Zhang ,  Douglas B. Kitchen

    发明人： Michael P. Trova ,  Nan Zhang ,  Douglas B. Kitchen

    IPC分类号： C07D471/04 ,  A61K31/505 ,  A61K31/55

    CPC分类号： C07D471/04

    摘要： This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.4)alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from H, or (C.sub.1 -C.sub.4)alkyl, or R.sub.5 and R.sub.6 are alkyl groups which may be taken together to form a 4-7 membered ring;(E) W is selected from H, --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3)alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 R.sub.4 ; or a pharmacologically acceptable salt thereof which is useful as an antineoplastic agent.

    摘要翻译： 本发明提供具有下式的化合物：其中：（A）n = 2-4; （B）R 1和R 2相同或不同，选自H，（C 1 -C 3）烷基，-CH 2 CH 2 OH，-CH 2 CH 2 NH 2和-CH 2 CH 2 N（CH 3）2或R 1和R 2是可以被取代的烷基部分 一起形成4-至7-元环; （C）R 3选自H，-CH 3，-CH 2 CH 3，-CH 2 CH 2 NH 2; （D）X位于2-或3-位，并且选自2-萘基，1-萘基，1-菲基，2-菲基，3-菲基，4-菲基，9-菲基 ，苯基和单取代或多取代的苯基，其中取代基选自-OR4，-NR5R6，（C1-C3）烷基，-CF3，F，Cl，Br，I，-NO2，-CN， SO 3 H，-SO 2 NR 5 R 6，-CO 2 H，-CO 2 R 4和苯基; R4是H或（C1-C4）烷基; R5和R6相同或不同并且选自H或（C1-C4）烷基，或R5和R6是可以一起形成4-7元环的烷基; （E）W选自H，-OR4，-NR5R6，（C1-C3）烷基，-CF3，F，Cl，Br，I，-NO2，-CN，-SO2NR5R6，-CO2R4; 或其药理学上可接受的盐，其可用作抗肿瘤剂。