公开(公告)号：EP0684951B1

公开(公告)日：1997-05-07

申请号：EP94908615.1

申请日：1994-01-25

申请人： MERRELL PHARMACEUTICALS INC.

发明人： COLLARD, Jean-Neol ,  HORNSPERGER, Jean-Marie

IPC分类号： C07F7/08 ,  A61K31/695

CPC分类号： C07F7/0803

摘要： Fluorinated silylated aromatic compounds possessing anticholinesterase activity and methods of treating Degenerative Dementias using these compounds.

公开(公告)号：EP0701546A1

公开(公告)日：1996-03-20

申请号：EP94917916.0

申请日：1994-05-05

申请人： MERRELL PHARMACEUTICALS INC.

发明人： COLLARD, Jean-Noel ,  HORNSPERGER, Jean-Marie ,  SCHIRLIN, Daniel

IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07C17 ,  C07C33 ,  C07C39 ,  C07C43 ,  C07C45 ,  C07C49 ,  C07C69 ,  C07C211 ,  C07C225 ,  C07C247 ,  C07C255 ,  C07C309

CPC分类号： C07C225/22 ,  C07C17/35 ,  C07C17/361 ,  C07C33/46 ,  C07C45/45 ,  C07C45/673 ,  C07C49/80 ,  C07C49/82 ,  C07C49/84 ,  C07C69/63 ,  C07C25/02 ,  C07C25/13

摘要： Compounds of general formula (I), stereoisomers and pharmaceutically acceptable salts thereof, wherein each of Z and Z' are independently H or F; Q is (a), CH(OH), (b); X is H, Br, Cl, F or CF3; Y is H, Br, Cl, F, OH, OR5, OC(O)R4, N3, CN, NO2, SO3H, CO2R4, NH2, NHR9, NR9R'9, C(R6)(R7)(V'R8) or C(O)R7, provided that when both Z and Z' are F, then Y is H or F; V and V' are each independently CH2 or O; R1 is H or CH3; R2, R9 and R'9 are each independently (C1-6)alkyl, or R2 and V-R3 taken together with the carbon atom to which they are attached form a 3-6 membered ring; R3, R6, R7 and R8 are each independently H, (C1-6)alkyl, or (C3-6)cycloalkyl; R4 is H, (C1-10)alkyl, (C0-4)alkylene aryl or (C3-8)cycloalkyl; and R5 is (C1-10)alkyl, benzyl, phenethyl or (C3-6)cycloalkyl, possess anticholinesterase activity and may be used in the treatment of Degenerativa Dementias.

公开(公告)号：EP0701546B1

公开(公告)日：1998-12-23

申请号：EP94917916.2

申请日：1994-05-05

申请人： MERRELL PHARMACEUTICALS INC.

发明人： COLLARD, Jean-Noel ,  HORNSPERGER, Jean-Marie ,  SCHIRLIN, Daniel

IPC分类号： C07C49/80 ,  C07C49/82 ,  C07C33/46 ,  C07C49/84 ,  C07C225/22 ,  A61K31/12

CPC分类号： C07C225/22 ,  C07C17/35 ,  C07C17/361 ,  C07C33/46 ,  C07C45/45 ,  C07C45/673 ,  C07C49/80 ,  C07C49/82 ,  C07C49/84 ,  C07C69/63 ,  C07C25/02 ,  C07C25/13

摘要： Compounds of general formula (I), stereoisomers and pharmaceutically acceptable salts thereof, wherein each of Z and Z' are independently H or F; Q is (a), CH(OH), (b); X is H, Br, Cl, F or CF3; Y is H, Br, Cl, F, OH, OR5, OC(O)R4, N3, CN, NO2, SO3H, CO2R4, NH2, NHR9, NR9R'9, C(R6)(R7)(V'R8) or C(O)R7, provided that when both Z and Z' are F, then Y is H or F; V and V' are each independently CH2 or O; R1 is H or CH3; R2, R9 and R'9 are each independently (C1-6)alkyl, or R2 and V-R3 taken together with the carbon atom to which they are attached form a 3-6 membered ring; R3, R6, R7 and R8 are each independently H, (C1-6)alkyl, or (C3-6)cycloalkyl; R4 is H, (C1-10)alkyl, (C0-4)alkylene aryl or (C3-8)cycloalkyl; and R5 is (C1-10)alkyl, benzyl, phenethyl or (C3-6)cycloalkyl, possess anticholinesterase activity and may be used in the treatment of Degenerativa Dementias.