Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
    11.
    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

    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
    16.
    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

    IPC分类号: A61K31496

    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:

    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    18.
    发明申请
    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
    GLUCOCORTICOID受体的调节剂,AP-1和/或NF-kB活性及其用途

    公开(公告)号:US20100063051A1

    公开(公告)日:2010-03-11

    申请号:US12513187

    申请日:2007-10-31

    摘要: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.

    摘要翻译: 提供了新的非甾体化合物,其可用于治疗与调节糖皮质激素受体,AP-1和/或NF-κB活性相关的疾病,包括具有式(I)结构的炎性和免疫疾病,肥胖症和糖尿病 ),对映体,非对映体,互变异构体,溶剂合物(例如水合物)或其药学上可接受的盐,其中:M选自烷基,取代的烷基,环烷基,芳基,杂环和杂芳基,条件是如果M是烷基 那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自(i)氢,C 1 -C 4烷基和取代的C 1 -C 4烷基; 或(ii)Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或(iii)Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环,其独立地选自O,S,SO 2 和N,该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基,杂环基,芳基或杂芳基; 并且Ma,Za,R 1,R 2,R 3,R 4,R 6,R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。