利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

75 条记录 (耗时 0.061 秒)

    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    72.
    再颁专利
    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 有权
    用作降胆固醇药的羟基取代的氮杂环丁酮化合物

    公开(公告)号：USRE37721E1

    公开(公告)日：2002-05-28

    申请号：US09594996

    申请日：2000-06-15

    申请人： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    发明人： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    IPC分类号： C07D20508

    CPC分类号： C07D205/08 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K45/06 ,  Y02P20/55 ,  Y10S514/824 ,  A61K2300/00

    摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CONR6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.

    摘要翻译： 羟基取代的氮杂环丁酮低胆固醇血症药或其药学上可接受的盐，其中：Ar1和Ar2是芳基或R4取代的芳基; Ar3是芳基或R5-取代的芳基; X，Y和Z是-CH2-，-CH（ 低级烷基） - 或-C（二卤代烷基） - ; R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R 1和R 3为H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R 4选自低级烷基，R 5，-CF 3，-CN，-NO 2，卤素R 5选自-OR 6 ，-O（CO）R 6，-O（CO）OR 9，-O（CH 2）1-5 OR 6，-O（CO）NR 6 R 7，-NR 6 R 7，-NR 6（CO）R 7，-NR 6（CO）OR 9，-NR 6 （CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O）0-2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CONR6R7， - （ 低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基或芳基取代的IcR9是低级烷基，芳基或芳基取代的低级烷基;以及降低血清的方法 通过单独或与胆固醇生物合成抑制剂组合施用所述化合物，含有它们的药物组合物; 和一个准备它们的过程。

    Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom
    75.
    发明授权
    Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom 失效
    被含有一个氮原子的五，六或七元杂环取代的咪唑烷基

    公开(公告)号：US6100279A

    公开(公告)日：2000-08-08

    申请号：US185973

    申请日：1998-11-05

    申请人： Wayne D. Vaccaro ,  Ronald L. Wolin ,  Daniel M. Solomon ,  Robert G. Aslanian ,  John J. Piwinski ,  Stuart B. Rosenblum

    发明人： Wayne D. Vaccaro ,  Ronald L. Wolin ,  Daniel M. Solomon ,  Robert G. Aslanian ,  John J. Piwinski ,  Stuart B. Rosenblum

    IPC分类号： A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07D401/06 ,  C07D403/06

    CPC分类号： C07D401/06 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07D403/06

    摘要： Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment. Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H, receptor antagonist.

    摘要翻译： 公开了式I的化合物或其药学上可接受的盐或溶剂化物。 还公开了包含药学上可接受的载体和有效量的式I化合物的药物组合物。还公开了治疗过敏（例如哮喘），炎症，低血压，升高的眼内压（如青光眼）的方法， 降低眼内压，睡眠障碍，超低运动状态和胃肠道酸性分泌的方法，中枢神经系统的低血压和多动症（例如，激动和抑郁）和其他CNS疾病（例如阿兹海默氏症，精神分裂症 ，肥胖症和偏头痛）包括向需要这种治疗的患者施用有效量的式I化合物。 还公开了治疗上呼吸道过敏反应的方法，包括与组胺H受体拮抗剂组合或混合施用式I化合物或其盐或溶剂合物。