公开(公告)号：US6017541A

公开(公告)日：2000-01-25

申请号：US906151

申请日：1997-08-05

申请人： Brian H. Barber ,  Neal den Hollander ,  Jiri J. Krepinsky ,  M. Younus Meah

发明人： Brian H. Barber ,  Neal den Hollander ,  Jiri J. Krepinsky ,  M. Younus Meah

IPC分类号： A61K38/00 ,  A61P25/36 ,  C07F9/6561 ,  C07K16/44 ,  G01N33/94 ,  A61K39/385 ,  C07K16/00

CPC分类号： C07K16/44 ,  A61K39/0013 ,  C07F9/6561 ,  G01N33/946 ,  A61K2039/6081 ,  A61K2039/627 ,  A61K38/00

摘要： Methods are described for the rapid synthesis in satisfactory yield of methyl ecgonine phenylphosphonates as analogues of transition states for the hydrolysis of the benzoyl ester of an ecgonine derivative, namely cocaine, and their linking to carrier proteins, for the purpose of using them as immunogens. The resulting immunogens elicit the formation in experimental animals of antibodies able to promote the hydrolysis of cocaine. Both these catalytic anti-cocaine antibodies and the immunogens themselves are potentially useful for the treatment of individuals seeking to avoid the pharmacological effects of cocaine and in diagnostic applications.

摘要翻译： 描述了为了以使用它们作为免疫原的目的，快速合成以令人满意的产率的甲基厄舌膦酸苯基膦酸酯作为类似物，用于水解伊万可因衍生物（即可卡因）的苯甲酰酯及其与载体蛋白的连接的过渡态的类似物。 所得到的免疫原引起实验动物中能够促进可卡因水解的抗体的形成。 这些催化抗可卡因抗体和免疫原本身都可能用于治疗寻求避免可卡因的药理作用和诊断应用的个体。

公开(公告)号：US5730985A

公开(公告)日：1998-03-24

申请号：US259004

申请日：1994-06-13

申请人： Brian H. Barber ,  Neal den Hollander ,  Jiri J. Krepinsky ,  M. Younus Meah

发明人： Brian H. Barber ,  Neal den Hollander ,  Jiri J. Krepinsky ,  M. Younus Meah

IPC分类号： A61K38/00 ,  A61P25/36 ,  C07F9/6561 ,  C07K16/44 ,  G01N33/94 ,  A61K39/385 ,  C07C69/76 ,  C07D451/12 ,  C07F9/02

CPC分类号： C07K16/44 ,  A61K39/0013 ,  C07F9/6561 ,  G01N33/946 ,  A61K2039/6081 ,  A61K2039/627 ,  A61K38/00

摘要： Methods are described for the rapid synthesis in satisfactory yield of methyl ecgonine phenylphosphonates as analogues of transition states for the hydrolysis of the benzoyl ester of an ecgonine derivative, namely cocaine, and their linking to carrier proteins, for the purpose of using them as immunogens. The resulting immunogens elicit the formation in experimental animals of antibodies able to promote the hydrolysis of cocaine. Both these catalytic anti-cocaine antibodies and the immunogens themselves are potentially useful for the treatment of individuals seeking to avoid the pharmacological effects of cocaine and in diagnostic applications.