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：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.

公开(公告)号：EP1109813B1

公开(公告)日：2004-08-11

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：EP1202965A1

公开(公告)日：2002-05-08

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.

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.