公开(公告)号：EP1047678B1

公开(公告)日：2004-09-08

申请号：EP98957745.7

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： BRYANS, Justin Stephen ,  CAPIRIS, Thomas ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen

IPC: C07D257/04 ,  A61K31/41 ,  C07D271/06 ,  C07F9/38 ,  A61K31/66 ,  C07D291/04 ,  C07C311/10 ,  A61K31/18 ,  C07C311/07 ,  C07C239/14 ,  A61K31/16 ,  C07C309/25 ,  A61K31/255

CPC classification number: C07D257/04 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas 1, 1C, 1F, 1G and 1H or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

Abstract translation: 式（1），（1C），（1F），（1G）和（1个H）或其药学上可接受的盐，其中n是从0至2的整数的新颖胺; m是从0至3的整数; R是磺酰胺，酰胺，膦酸基，杂环，磺酸，或异羟肟酸; A“是由式（1），（2），（3），（4），（5）是worin连接点中选择的桥连的环; Z1到Z4是选自氢和甲基中选择的每个unabhängig; o是1至4的整数; 且p是上述R为0〜2。在式（1）的整数不能磺酸当m为2和n为1的盘游离缺失和是有用的，如癫痫，昏厥发作，运动机能减退，颅异常的治疗剂 ，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理症状，特别是肠易激综合征。

公开(公告)号：EP0937032B1

公开(公告)日：2007-05-09

申请号：EP97945516.9

申请日：1997-10-07

Applicant: Warner-Lambert Company LLC

Inventor： BRYANS, Justin Stephen ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen ,  THORPE, Andrew, John

IPC: C07C229/22 ,  A61K31/195 ,  C07C323/58

CPC classification number: C07C323/58 ,  C07C229/22 ,  C07C2601/14

Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

公开(公告)号：EP1045839B1

公开(公告)日：2004-03-03

申请号：EP98962805.2

申请日：1998-11-10

Applicant: Warner-Lambert Company LLC

Inventor： BELLIOTTI, Thomas, Richard ,  BRYANS, Justin Stephen ,  CAPIRIS, Thomas ,  HORWELL, David Christopher ,  KNEEN, Clare Octavia ,  WUSTROW, David, Juergen

IPC: C07D257/04

CPC classification number: C07C311/32 ,  C07C233/36 ,  C07C239/14 ,  C07C259/06 ,  C07C309/25 ,  C07C311/05 ,  C07C311/09 ,  C07C311/33 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07C2603/74 ,  C07D211/26 ,  C07D257/04 ,  C07D271/07 ,  C07D285/18 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  C07F9/3808 ,  C07F9/383 ,  C07F9/592 ,  C07F9/6552 ,  C07F9/655363

Abstract: Novel amines of formulas (1A) and (1B) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed. R is sulfonamide, amide, sulfonic acid, or phosphonic acid.

Abstract translation: 公式1A和1B的新cardamines是盘游离缺失，并可用作癫痫，昏厥发作，运动机能减退，颅异常，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理疾病，炎性疾病和胃肠功能紊乱，爱的药剂特别​​是 肠易激综合征。 因此用于制备和中间体在制备有用的方法是游离缺失盘。