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    Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
    25.
    发明授权
    Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
    取代的烟酰胺和类似物作为胱天蛋白酶的激活剂和凋亡诱导剂及其用途

    公开(公告)号：US06794397B2

    公开(公告)日：2004-09-21

    申请号：US09769420

    申请日：2001-01-26

    申请人： Sui Xiong Cai ,  John A. Drewe

    发明人： Sui Xiong Cai ,  John A. Drewe

    IPC分类号： C07D21382

    CPC分类号： C07D213/75 ,  A61K31/341 ,  A61K31/44 ,  A61K31/4965 ,  C07D207/34 ,  C07D213/82 ,  C07D239/28 ,  C07D241/24 ,  C07D307/68 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, the compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

    摘要翻译： 本发明涉及由式V代表的取代烟酰胺及其类似物：或其药学上可接受的盐或前药，其中：Ar'和Ar独立地为任选取代的芳基或任选取代的杂芳基，条件是所述任选的 取代的杂芳基包含不多于两个氮原子; 和R 11是氢; 或烷基，环烷基，芳基或杂芳基，其各自任选被取代。本发明还涉及发现具有式V的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。 因此，本发明的化合物可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

    Substituted 2-aminoacetamides and the use thereof
    29.
    发明授权
    Substituted 2-aminoacetamides and the use thereof 有权
    取代的2-氨基乙酰胺及其用途

    公开(公告)号：US06479484B1

    公开(公告)日：2002-11-12

    申请号：US09554739

    申请日：2000-08-08

    申请人： Nancy C. Lan ,  Yan Wang ,  Sui Xiong Cai

    发明人： Nancy C. Lan ,  Yan Wang ,  Sui Xiong Cai

    IPC分类号： A61K314965

    CPC分类号： C07C233/05 ,  A61K31/165 ,  C07C237/06 ,  C07C237/08 ,  C07C2601/14 ,  C07D211/46 ,  C07D213/65 ,  C07D213/68 ,  C07D215/20 ,  C07D239/34 ,  C07D241/08 ,  C07D309/12 ,  C07D317/64

    摘要： The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

    摘要翻译： 本发明涉及由式（II）表示的取代的2-氨基乙酰胺及其药学上可接受的盐和前药，其中取代基在本文中定义。 本发明还涉及取代的2-氨基乙酰胺在治疗全球和局灶性缺血后的神经元损伤的方法中的用途，以及用作治疗，预防或改善疼痛的抗惊厥药作为抗痉挛剂，作为局部麻醉剂，如 抗心律失常药物和治疗或预防糖尿病性神经病变。