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公开(公告)号：US07790735B2
公开(公告)日：2010-09-07
申请号：US11500860
申请日：2006-08-08
IPC分类号： C07D239/54 , A61K31/513
CPC分类号： C07D473/34
摘要： The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloalkyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A2B, A3, P2Y2 receptors), cancer (through A3, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A1, A3 receptors), epilepsy (through A1, P2X receptors), and Huntington's Disease (through A2A receptors).
摘要翻译： 本发明提供了新的核苷和核苷酸衍生物，其是P1和P2受体的有用的激动剂或拮抗剂。 例如，本发明提供式A-M的化合物，其中A是修饰的腺嘌呤或尿嘧啶，M是受限制的环烷基。 腺嘌呤或尿嘧啶与受限制的环烷基键合。 本发明的化合物可用于治疗或预防各种疾病，包括气道疾病（通过A2B，A3，P2Y2受体），癌症（通过A3，P2受体），心律失常（通过A1受体），心脏缺血（通过 A1，A3受体），癫痫（通过A1，P2X受体）和亨廷顿病（通过A2A受体）。
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公开(公告)号：US07348315B2
公开(公告)日：2008-03-25
申请号：US10396200
申请日：2003-03-25
申请人： Bruce T Liang , Kenneth A Jacobson
发明人： Bruce T Liang , Kenneth A Jacobson
CPC分类号： C07F9/65586 , C07F9/6561 , C07H19/20 , C07K14/705
摘要： Disclosed herein are methods of using an adenosine analog or derivative for treating heart failure, increasing cardiac muscle contractility, increasing cardiac diastolic relaxation, and increasing vasodilation. Exemplary adenosine analogs/derivatives include compounds of the following formula wherein L is CH or O, wherein when L is CH, t is 1 and when L is O, t is 0; R1 is halogen or —R6—(R7)p—R8; R2 is hydrogen, alkyl, cycloalkyl, cycloalkenyl, alkynyl, alkylthio, aminoalkylthio, halogen, or —R6—(R7)p—R8; R3 is H, halogen or —R6—(R7)p—R8; R4 is —OH or —SH; R5 is —OH or —R6—(R7)p—R8; R6is NH or S; R7is CH2; R8 is H, NH2, halogen, CN, CCH, cycloallkyl, having 3 to about 10 carbon atoms or aryl having 3 to about 20 carbon atoms; R9 is OH or acetamido; R10 and R11 are independently hydrogen or halogen; X, Y, and Z are independently N or CH; m is 0, 1, or 2; n is 0 or 1; q is 0 or 1 if L is CH, or if L is O, R3 is halogen or —R6—(R7)p—R8; q is 1 if L is O, R3 is H, halogen, or —R6—(R7)p—R8; provided that at least one of m, n, and q is 1; and p is 0 to 10.
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