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99 条记录 (耗时 0.034 秒)

    Substituted alkyl piperazine derivatives
    23.
    发明申请
    Substituted alkyl piperazine derivatives 审中-公开
    取代的烷基哌嗪衍生物

    公开(公告)号：US20030064994A1

    公开(公告)日：2003-04-03

    申请号：US10243307

    申请日：2002-09-13

    申请人： CV Therapeutics, Inc.

    发明人： Vaibhav Varkhedkar ,  Venkata P. Palle ,  Jeff Zablocki ,  Elfatih Elzein ,  Brent K. Blackburn

    IPC分类号： A61K031/496 ,  A61K031/495 ,  C07D43/02 ,  C07D241/04

    CPC分类号： C07D295/15 ,  C07D241/04 ,  C07D241/08 ,  C07D241/42 ,  C07D317/54 ,  C07D317/58

    摘要： Novel compounds of the general formula: 1 and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.

    摘要翻译： 新的通式化合物及其药学上可接受的酸加成盐，其中所述化合物可用于治疗以保护骨骼肌免受创伤损伤或保护肌肉或全身性疾病如间歇性跛行后的骨骼肌，以治疗休克 条件，以维持移植物中使用的供体组织和器官，治疗包括心房和室性心律失常的心血管疾病，Prinzmetal（变体）心绞痛，稳定性心绞痛和运动诱发的心绞痛，充血性心脏病和心肌梗塞。

    C-pyrazole A2A receptor agonists
    24.
    发明申请
    C-pyrazole A2A receptor agonists 有权
    C-吡唑A2A受体激动剂

    公开(公告)号：US20010018428A1

    公开(公告)日：2001-08-30

    申请号：US09812176

    申请日：2001-03-19

    申请人： CV Therapeutics, Inc.

    发明人： Jeff A. Zablocki ,  Venkata P. Palle ,  Elfatih O. Elzein

    IPC分类号： A61K031/7076

    CPC分类号： C07H19/16

    摘要： 2-adenosine C-pyrazole compositions having the following formula: 1 and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.

    摘要翻译： 具有下式的2-腺苷C-吡唑组合物以及用于将该组合物用作A2A受体激动剂以刺激哺乳动物冠状血管扩张用于治疗目的和用于成像心脏的方法

    .alpha.-ketoamide inhibitors of 20S proteasome
    25.
    发明授权
    .alpha.-ketoamide inhibitors of 20S proteasome 失效
    20S蛋白酶体的α-酮酰胺抑制剂

    公开(公告)号：US6075150A

    公开(公告)日：2000-06-13

    申请号：US13365

    申请日：1998-01-26

    申请人： Lisa Wang ,  Robert T. Lum ,  Steven R. Schow ,  Alison Joly ,  Suresh Kerwar ,  Michael M Wick

    发明人： Lisa Wang ,  Robert T. Lum ,  Steven R. Schow ,  Alison Joly ,  Suresh Kerwar ,  Michael M Wick

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61P37/00 ,  C07K5/02 ,  C07K5/023 ,  C07K5/027 ,  C07K5/03 ,  C07K5/06 ,  C07K5/062 ,  C07K5/083 ,  C07D209/12 ,  A01N43/38

    CPC分类号： C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/06043 ,  C07K5/0808 ,  A61K38/00

    摘要： .alpha.-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X.sub.2 is Ar or Ar--X.sub.3 wherein X.sub.3 is --C.dbd.O, or --CH.sub.2 CO--, and wherein Ar is phenyl, substituted phenyl, indole, substituted indoles, and any other heteroaryls; R.sub.1, and R.sub.2 are each individually selected from the side chains of the known natural .alpha.-amino acids and unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear, branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle substituted heterocycle, heteroaryl and substituted heteroaryl; X.sub.1 is selected from hydroxide, monoalkylamino, dialkylamino, alkoxide, arylkoxide and ##STR1## wherein X.sub.4 is hydroxide, arylamino, monoalkylamino, dialkylamino, alkoxide, or arylalkoxide; and R.sub.3 is selected from the known natural .alpha.-amino acids, unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear and branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle, substituted heterocycle, heteroaryl and substituted heteroaryl.

    摘要翻译： 用于治疗由20S蛋白酶体介导的疾病的α-酮酰胺化合物，其具有下式：其中X2是Ar或Ar-X3，其中X3是-C = O或-CH2CO-，其中Ar是苯基，取代的苯基，吲哚 取代的吲哚和任何其它杂芳基; R1和R2分别选自已知天然α-氨基酸和非天然氨基酸的侧链，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代的芳基 ，1-10碳直链，支链取代的芳基，烷氧基芳基，3-8碳环烷基，杂环取代的杂环，杂芳基和取代的杂芳基; X1选自氢氧化物，单烷基氨基，二烷基氨基，醇盐，芳基醇盐，其中X4是氢氧根，芳基氨基，单烷基氨基，二烷基氨基，醇盐或芳基醇盐; R 3选自已知的天然α-氨基酸，非天然氨基酸，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代芳基，1-10碳直链和支链 取代的芳基，烷氧基芳基，3-8碳环烷基，杂环，取代的杂环，杂芳基和取代的杂芳基。

    Purine inhibitors of cyclin dependent kinase 2
    26.
    发明授权
    Purine inhibitors of cyclin dependent kinase 2 失效
    细胞周期蛋白依赖性激酶2的嘌呤抑制剂

    公开(公告)号：US5866702A

    公开(公告)日：1999-02-02

    申请号：US692012

    申请日：1996-08-02

    申请人： Richard Mackman ,  Robert T. Lum ,  Steven R. Schow ,  Michael M. Wick

    发明人： Richard Mackman ,  Robert T. Lum ,  Steven R. Schow ,  Michael M. Wick

    IPC分类号： C07D473/00 ,  A61K31/52 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/06 ,  A61P25/00 ,  A61P31/10 ,  A61P35/00 ,  C07D233/00 ,  C07D239/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/38 ,  C07D473/40

    CPC分类号： C07D473/16 ,  C07D473/40

    摘要： A 2,6,9-trisubstituted purine composition having the following formula: ##STR1## where X is a amino, oxo, thio, of sulfone moiety, R.sub.1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl, each having from 1 to 20 carbon atoms; R.sub.2 is hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl; and R.sub.3 is halogen, hydroxyl, thio, alkoxy, alkylthio, lower alkyl, --NR.sub.4 R.sub.5 or a component having the formula: ##STR2## wherein when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is methyl, R.sub.1 -X is not amino, 3-methyl-2-butenylamino, benzylamino, or m-hydroxybenzyl-amino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is isopropyl, R.sub.1 -X is not benzylamino, m-hydroxybenzylamino, or 3-methylbutylamino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is 2-hydroxyethyl, R.sub.1 -X is not benzylamino and when R.sub.3 is selected from the group consisting of 2-propanol-2-methylamino and 2-dimethylaminoethylamino and R.sub.2 is methyl, then R.sub.1 -X is not benzylamino.

    摘要翻译： 具有下式的2,6,9-三取代嘌呤组合物：其中X是砜部分的氨基，氧代，硫代，R1是低级烷基，取代的低级烷基，环烷基，取代的环烷基，环杂烷基，取代的 杂环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基，各自具有1至20个碳原子; R 2是氢，低级烷基，取代的低级烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基。 R 3为卤素，羟基，硫代，烷氧基，烷硫基，低级烷基，-NR 4 R 5或具有下式的组分：其中当R 3为2-羟基乙基氨基且R 2为甲基时，R 1 -X不为氨基， -2-丁烯基氨基，苄基氨基或间羟基苄基 - 氨基，当R 3为2-羟基乙基氨基且R 2为异丙基时，当R 3为2-羟基乙基氨基时，R 1 -X为苄基氨基，间羟基苄基氨基或3-甲基丁基氨基， 2-羟乙基，R1-X不是苄基氨基，当R3选自2-丙醇-2-甲基氨基和2-二甲基氨基乙基氨基，R2是甲基时，则R1-X不是苄基氨基。

    ABCA1 elevating compounds
    29.
    发明授权
    ABCA1 elevating compounds 失效
    ABCA1升高化合物

    公开(公告)号：US07432276B2

    公开(公告)日：2008-10-07

    申请号：US11646691

    申请日：2006-12-27

    申请人： Matthew Abelman ,  Robert Jiang ,  Jeff Zablocki ,  Dmitry Koltun ,  Melanie Boze

    发明人： Matthew Abelman ,  Robert Jiang ,  Jeff Zablocki ,  Dmitry Koltun ,  Melanie Boze

    IPC分类号： A61K31/4741 ,  C07D491/06

    CPC分类号： C07D491/052

    摘要： The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

    摘要翻译： 本发明提供了可用于增加哺乳动物中细胞ATP结合盒转运蛋白ABCA1产生的化合物，以及使用这些化合物治疗冠状动脉疾病，血脂异常和代谢综合征的方法。 本发明还涉及制备这些化合物的方法以及含有它们的药物组合物。