Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    71.
    发明授权
    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
    糖皮质激素受体,AP-1和/或NF-κB活性的调节剂及其用途

    公开(公告)号:US07642273B2

    公开(公告)日:2010-01-05

    申请号:US11330749

    申请日:2006-01-12

    摘要: A class of 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 obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

    摘要翻译: 提供了一类新型非甾体化合物,其可用于治疗与糖皮质激素受体,AP-1和/或NF-κB活性的调节相关的疾病,包括肥胖症,糖尿病,炎症和免疫疾病,并且具有 式(I)或(II):其中Q选自N,O和S;其包括其立体异构体,其互变异构体,其前药或其药学上可接受的盐; Y是芳基或杂芳基; Z是H,C 2-6烷基,环烷基,杂环烷基,芳基,杂芳基,卤素或烷氧基; 并且A,B,R,Ra,Rb,Rc和Rd在本文中定义。 还提供了治疗肥胖症,糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

    TURBO SPEED SENSOR DIAGNOSTIC FOR TURBOCHARGED ENGINES
    74.
    发明申请
    TURBO SPEED SENSOR DIAGNOSTIC FOR TURBOCHARGED ENGINES 有权
    涡轮速度传感器用于涡轮发动机的诊断

    公开(公告)号:US20090055072A1

    公开(公告)日:2009-02-26

    申请号:US12141329

    申请日:2008-06-18

    申请人: Chuan He Yun Xiao

    发明人: Chuan He Yun Xiao

    IPC分类号: F01N11/00

    摘要: A method of diagnosing operation of a turbo speed sensor that monitors a turbocharger in an internal combustion engine system includes determining whether the engine system is operating in one of a high speed and a low speed range and determining a threshold turbo speed value based on whether engine system is operating in one of the high speed and the low speed range. An actual turbo speed value of the turbocharger is monitored based on a signal generated by the turbo speed sensor. The actual turbo speed value is compared to the threshold turbo speed value and a diagnostic signal is generated based on the step of comparing.

    摘要翻译: 一种诊断内燃机系统中的涡轮增压器的涡轮速度传感器的操作的方法包括:确定发动机系统是否以高速和低速范围中的一个运行,并且基于发动机是否确定阈值涡轮转速值 系统运行在高速和低速范围之一。 基于由涡轮转速传感器产生的信号来监测涡轮增压器的实际涡轮转速值。 将实际的turbo速度值与阈值turbo速度值进行比较,并且基于比较步骤生成诊断信号。

    Process for preparing azacycloalkanoylaminothiazoles
    79.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号:US06414156B2

    公开(公告)日:2002-07-02

    申请号:US09746060

    申请日:2000-12-22

    IPC分类号: C07D41714

    摘要: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

    摘要翻译: 本发明涉及制备式I的5-(2-恶唑基烷硫基)-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的,有效的方法,其中:R是烷基,芳基或杂芳基; R 1,R 2,R 3, R4和R5各自独立地为氢,烷基,芳基或杂芳基; R6和R7各自独立地为氢,烷基,芳基,杂芳基,卤素,羟基或烷氧基; R8为氢,烷基,芳基,杂芳基,CONR9R10,COR11或COOR12; R9,R10,R11和R12各自独立地为氢,烷基或芳基; m等于0至5; 和等于0至5,这是细胞周期蛋白依赖性激酶(cdks)的新型有效抑制剂。 本发明还涉及新的关键中间体化合物,式III'的季铵盐和式IX的2-恶唑基烷基衍生物。