公开(公告)号：EP1325008B1

公开(公告)日：2005-10-05

申请号：EP01962869.2

申请日：2001-07-24

申请人： F. HOFFMANN-LA ROCHE AG ,  VERNALIS RESEARCH LIMITED

发明人： BENTLEY, Jonathan, Mark ,  HEBEISEN, Paul ,  MULLER, Marc ,  RICHTER, Hans ,  ROEVER, Stephan ,  MATTEI, Patrizio ,  TAYLOR, Sven

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P3/10

CPC分类号： C07D487/04

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1. They can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnoea.

公开(公告)号：EP1343775B1

公开(公告)日：2008-06-04

申请号：EP01990522.3

申请日：2001-12-06

申请人： F. Hoffmann-La Roche AG ,  VERNALIS RESEARCH LIMITED

发明人： ADAMS, David, Reginald ,  BENTLEY, Jonathan, Mark ,  DAVIDSON, James, Edward, Paul ,  DAWSON, Claire, Elizabeth ,  GEORGE, Ashley, Roger ,  MANSELL, Howard, Langham ,  MATTEI, Patrizio ,  MIZRAHI, Jacques ,  NETTEKOVEN, Matthias, Heinrich ,  PRATT, Robert, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  ROEVER, Stephan ,  SPECKLIN, Jean-Luc ,  STALDER, Henri ,  HARRISON, Kerry

IPC分类号： C07D295/20 ,  A61K31/495 ,  A61P3/04 ,  C07D261/08 ,  C07D213/30

CPC分类号： C07D207/325 ,  C07D213/30 ,  C07D213/64 ,  C07D213/643 ,  C07D261/08 ,  C07D277/24 ,  C07D285/14 ,  C07D295/205 ,  C07D295/21 ,  C07D307/12 ,  C07D307/42 ,  C07D333/16 ,  C07D413/04

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

摘要翻译： 本发明涉及式（I）的化学化合物及其药学上可用的盐，溶剂合物和酯，其中R 1至44，A 1，A 2和m具有权利要求1中给出的含义。可以使用它们 其为用于治疗或预防中枢神经系统疾病，心血管疾病，胃肠疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物制剂形式。

公开(公告)号：EP1325008A1

公开(公告)日：2003-07-09

申请号：EP01962869.2

申请日：2001-07-24

申请人： F. HOFFMANN-LA ROCHE AG ,  VERNALIS RESEARCH LIMITED

发明人： BENTLEY, Jonathan, Mark ,  HEBEISEN, Paul ,  MULLER, Marc ,  RICHTER, Hans ,  ROEVER, Stephan ,  MATTEI, Patrizio ,  TAYLOR, Sven

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P3/10

CPC分类号： C07D487/04

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1. They can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnoea.

公开(公告)号：EP1343775A2

公开(公告)日：2003-09-17

申请号：EP01990522.3

申请日：2001-12-06

申请人： F. HOFFMANN-LA ROCHE AG ,  VERNALIS RESEARCH LIMITED

发明人： ADAMS, David, Reginald ,  BENTLEY, Jonathan, Mark ,  DAVIDSON, James, Edward, Paul ,  DAWSON, Claire, Elizabeth ,  GEORGE, Ashley, Roger ,  MANSELL, Howard, Langham ,  MATTEI, Patrizio ,  MIZRAHI, Jacques ,  NETTEKOVEN, Matthias, Heinrich ,  PRATT, Robert, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  ROEVER, Stephan ,  SPECKLIN, Jean-Luc ,  STALDER, Henri ,  WILKINSON, Kerry

IPC分类号： C07D295/20 ,  A61K31/495 ,  A61P3/04 ,  C07D261/08 ,  C07D213/30

CPC分类号： C07D207/325 ,  C07D213/30 ,  C07D213/64 ,  C07D213/643 ,  C07D261/08 ,  C07D277/24 ,  C07D285/14 ,  C07D295/205 ,  C07D295/21 ,  C07D307/12 ,  C07D307/42 ,  C07D333/16 ,  C07D413/04

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

公开(公告)号：EP1844026B1

公开(公告)日：2011-04-27

申请号：EP06700277.4

申请日：2006-01-10

申请人： F.Hoffmann-La Roche AG ,  VERNALIS RESEARCH LIMITED

发明人： BENTLEY, Jonathan, Mark ,  DAWSON, Claire, Elizabeth ,  GUBA, Wolfgang ,  HEBEISEN, Paul ,  MONCK, Nathaniel ,  PRATT, Robert, Mark ,  RICHTER, Hans ,  ROEVER, Stephan ,  RUSTON, Vicki

IPC分类号： C07D265/30 ,  A61K31/5375 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D265/30

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.

公开(公告)号：EP1129078A2

公开(公告)日：2001-09-05

申请号：EP99943082.0

申请日：1999-09-01

申请人： VERNALIS RESEARCH LIMITED

发明人： ADAMS, David, Reginald ,  BENTLEY, Jonathan, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  HAMLYN, Richard, John ,  GEORGE, Ashley, Roger

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61P25/00

CPC分类号： C07D231/56

摘要： A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

公开(公告)号：EP1844026A2

公开(公告)日：2007-10-17

申请号：EP06700277.4

申请日：2006-01-10

申请人： F.HOFFMANN-LA ROCHE AG ,  VERNALIS RESEARCH LIMITED

发明人： BENTLEY, Jonathan, Mark ,  DAWSON, Claire, Elizabeth ,  GUBA, Wolfgang ,  HEBEISEN, Paul ,  MONCK, Nathaniel ,  PRATT, Robert, Mark ,  RICHTER, Hans ,  ROEVER, Stephan ,  RUSTON, Vicki

IPC分类号： C07D265/30 ,  A61K31/5375 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D265/30

摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.

公开(公告)号：EP1129078B1

公开(公告)日：2006-03-15

申请号：EP99943082.0

申请日：1999-09-01

申请人： VERNALIS RESEARCH LIMITED

发明人： ADAMS, David, Reginald ,  BENTLEY, Jonathan, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  HAMLYN, Richard, John ,  GEORGE, Ashley, Roger

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61P25/00

CPC分类号： C07D231/56

摘要： A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

公开(公告)号：EP1109813A1

公开(公告)日：2001-06-27

申请号：EP99943091.1

申请日：1999-09-01

申请人： VERNALIS RESEARCH LIMITED

发明人： ADAMS, David, Reginald ,  BENTLEY, Jonathan, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  HAMLYN, Richard, John ,  GAUR, Suneel ,  DUNCTON, Matthew, Alexander, James ,  DAVIDSON, James, Edward, Paul ,  BICKERDIKE, Michael, John ,  CLIFFE, Ian, Anthony ,  MANSELL, Howard, Langham

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D491/14 ,  A61K31/40

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/14

摘要： A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

公开(公告)号：EP1202965B1

公开(公告)日：2004-10-13

申请号：EP00951697.2

申请日：2000-08-04

申请人： VERNALIS RESEARCH LIMITED

发明人： BENTLEY, Jonathan, Mark ,  ROFFEY, Jonathan, Richard, Anthony ,  DAVIDSON, James, Edward, Paul ,  MANSELL,Howard, Langh am ,  HAMLYN, Richard, John ,  CLIFFE, Ian, Anthony ,  ADAMS, David, Reginald ,  MONCK, Nathaniel, Julius

IPC分类号： C07D209/80 ,  C07D495/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/28

CPC分类号： C07D495/04 ,  C07D209/94

摘要： A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT¿2C? receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.