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47 条记录 (耗时 0.032 秒)

    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
    1.
    发明授权
    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof 有权
    取代的氮杂环丁酮化合物，其制备方法，制剂及其用途

    公开(公告)号：US07235543B2

    公开(公告)日：2007-06-26

    申请号：US10791910

    申请日：2004-03-03

    申请人： Duane A. Burnett ,  John W. Clader ,  Wayne Vaccaro

    发明人： Duane A. Burnett ,  John W. Clader ,  Wayne Vaccaro

    IPC分类号： C07D205/08 ,  A61K31/397 ,  A61K31/7052 ,  A61P3/06 ,  C07H7/02

    CPC分类号： C07D403/12 ,  C07D205/08 ,  Y10S930/28

    摘要： The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.

    摘要翻译： 本发明提供由结构式（I）表示的化合物：或式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中每个取代基如本文所述，包括上述化合物的制剂， 用于制备相同的药物和治疗血管病症的方法，例如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低甾醇和/或甾醇的血浆水平。

    Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
    3.
    发明授权
    Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms 失效
    被含有两个氮原子的六元或七元杂环取代的咪唑化合物

    公开(公告)号：US06211182B1

    公开(公告)日：2001-04-03

    申请号：US09264615

    申请日：1999-03-08

    申请人： Wayne Vaccaro ,  John J. Piwinski ,  Wing C. Tom ,  Daniel M. Solomon ,  Robert G. Aslanian

    发明人： Wayne Vaccaro ,  John J. Piwinski ,  Wing C. Tom ,  Daniel M. Solomon ,  Robert G. Aslanian

    IPC分类号： A61K31496

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14

    摘要： This invention discloses novel imidazoles substituted with a six or seven membered heterocyclic ring which contains two nitrogen atoms as part of the heterocyclic ring structure. These compounds have excellent histamine-H3 receptor antagonist activity. Also disclosed are methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)—i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypomotility 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 Disease, schizophrenia, and migraine). An illustrative inventive imidazole is shown below:

    摘要翻译： 本发明公开了用含有两个氮原子作为杂环结构的一部分的六元或七元杂环取代的新型咪唑。 这些化合物具有优异的组胺H3受体拮抗剂活性。 还公开了制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含这种咪唑的药物组合物以及使用它们治疗过敏（例如哮喘），炎症，高血压，升高的眼内压（如青光眼）的方法，降低眼内压的方法， 睡眠障碍，超低运动性和胃肠道酸性分泌状态，中枢神经系统（例如，激动和抑郁）和其他CNS疾病（如阿尔茨海默病，精神分裂症和偏头痛）的低反应和多动症。 本发明的咪唑如下所示：

    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof
    5.
    发明授权
    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof 失效

    公开(公告)号：US5688787A

    公开(公告)日：1997-11-18

    申请号：US588785

    申请日：1996-01-19

    申请人： Duane A. Burnett ,  John W. Clader ,  Sundeep Dugar ,  Wayne Vaccaro

    发明人： Duane A. Burnett ,  John W. Clader ,  Sundeep Dugar ,  Wayne Vaccaro

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/08 ,  C07F7/18 ,  A61K31/395 ,  C07D403/10

    CPC分类号： C07D401/04 ,  C07D205/08 ,  C07D205/085 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/0812 ,  C07F7/186

    摘要： Novel compounds of the formula ##STR1## wherein A is --CH.dbd.CH--B; --C.tbd.C--B; --(CH.sub.2).sub.p --X--B, and X is a bone, --NH-- or --S(O).sub.0-2 --; optionally substituted heteroaryl or benzofused heteroaryl; --C(O)--B; or ##STR2## D is B'--(CH.sub.2).sub.m C(O)--, B'--(CH.sub.2).sub.q --, B'--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r, wherein Z is --O--, --C(O)--, phenylene, --NR.sub.8 -- or --S(O).sub.0-2 --, B'--(alkenylene)--; B'--(alkadienylene)--; B'--(CH.sub.2).sub.t --Z--(alkenylene), B'--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --, wherein V is cycloalkylene, B'--(CH.sub.2).sub.t --V--(alkenylene) or B'--(alkenylene)--V--(CH.sub.2).sub.t --, B'--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --, T--(CH.sub.2).sub.s --, wherein T is cycloalkyl; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B--(CH.sub.2).sub.n --; R.sub.4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, the method of using compounds of the formula II ##STR3## wherein R.sub.20 is optionally substituted phenyl, naphthyl, heteroaryl, or benzofused heteroaryl, R.sub.21, R.sub.22 and R.sub.23 are H or R.sub.20 ; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain; an interrupted alkylene, alkenylene or alkynylene chain; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R.sub.21 --E and R.sub.22 --F is selected from the group consisting of halogeno, OH, alkoxy, --OC(O)R.sub.5, --NR.sub.10 R.sub.11, --SH or --S(alkyl); R.sub.5 is alkyl, phenyl, R.sub.14 -phenyl, benzyl or R.sub.14 -benzyl; R.sub.10 and R.sub.11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.