公开(公告)号：JP2002201187A

公开(公告)日：2002-07-16

申请号：JP2001356849

申请日：2001-11-22

Applicant: UCB SA

Inventor： COSSEMENT ERICK ,  BODSON GUY ,  GOBERT JEAN

IPC: C07D295/06 ,  A61K31/495 ,  A61P11/06 ,  A61P25/20 ,  A61P25/22 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07B53/00 ,  C07D295/04 ,  C07D295/073 ,  C07D295/08 ,  C07D295/088 ,  C07D295/22 ,  C07D295/26

Abstract: PROBLEM TO BE SOLVED: To provide a 1,4-disubstituted piperazine derivative of high optical purity having valuable pharmacological activity, particularly antihistaminic activity, and to provide an intermediate for producing the above derivative. SOLUTION: This 1,4-disubstituted piperazine derivative is obtained by reaction under heating of an enantiomer of 1-[(4-chlorophenyl)]piperazine with a halide of the formula: RX [R is methyl, (3-methylphenyl)methyl or the like; and X is a halogen atom]. The other objective method for producing the above derivative is provided as described above.

公开(公告)号：JP2006342190A

公开(公告)日：2006-12-21

申请号：JP2006266195

申请日：2006-09-29

Applicant: UCB SA

Inventor： COSSEMENT ERICK ,  BODSON GUY ,  GOBERT JEAN

IPC: C07D295/06 ,  A61K31/495 ,  A61P11/06 ,  A61P17/00 ,  A61P25/20 ,  A61P25/22 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07B53/00 ,  C07D295/04 ,  C07D295/073 ,  C07D295/08 ,  C07D295/088 ,  C07D295/22 ,  C07D295/26

Abstract: PROBLEM TO BE SOLVED: To provide a 1,4-disubstituted piperazine derivative of high optical purity having valuable pharmacological activity and especially antihistamine activity and to provide its production intermediate. SOLUTION: There is provided compounds with the optical purity of higher than 98% selected from the group consisting of a levorotatory dihydrochloride of 1-[(4-chlorophenyl)phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine, a dextrorotatory dihydrochloride of 1-[(4-chlorophenyl)phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine or the like. COPYRIGHT: (C)2007,JPO&INPIT

公开(公告)号：NO922922A

公开(公告)日：1993-01-26

申请号：NO922922

申请日：1992-07-23

Applicant: UCB SA

Inventor： KEULEN BEREND JAN VAN ,  GOLDSTEIN SOLO ,  COSSEMENT ERICK ,  GOBERT JEAN ,  WUELFERT ERNST

IPC: A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61P11/00 ,  A61P11/06 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  C07D251/12 ,  C07D251/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D401/04 ,  C07D403/04 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04 ,  C07D498/08 ,  C07D487/06 ,  C07D498/16 ,  C07D498/18

CPC classification number: C07D401/04 ,  C07D251/18 ,  C07D411/04 ,  C07D417/04 ,  Y10S514/826 ,  Y10S514/886

公开(公告)号：NO922922L

公开(公告)日：1993-01-26

申请号：NO922922

申请日：1992-07-23

Applicant: UCB SA

Inventor： KEULEN BEREND JAN VAN ,  GOLDSTEIN SOLO ,  COSSEMENT ERICK ,  GOBERT JEAN ,  WUELFERT ERNST

IPC: A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61P11/00 ,  A61P11/06 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  C07D251/12 ,  C07D251/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D401/04 ,  C07D403/04 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04 ,  C07D498/08 ,  C07D498/16 ,  C07D498/18 ,  C07D487/06

Abstract: New cyclopropylamino-1,3,5-triazines and their salts, processes for their preparation and therapeutic compositions. These compounds correspond to the formula in which R1 = alkyl, cycloalkyl or alkylcycloalkyl, R2 = bis(2-hydroxyethyl)amino, 3-hydroxy-1-azetidinyl, 3-methoxy-1-azetidinyl, 3-oxo-1-azetidinyl, morpholino, 4-hydroxypiperidino, thiomorpholino, thiomorpholino S-oxide, thiomorpholino S,S-dioxide, 3-thiazolidinyl, 3-thiazolidinyl S-oxide, 3-thiazolidinyl S,S-dioxide or 8-oxa-3-azabicyclo[3.2.1]oct-3-yl. These compounds are useful in the treatment of disorders associated with Alzheimer's disease, Alzheimer-type senile dementias and all evolutive cognitive pathologies and in the treatment of depression, anxiety, mood disorders, inflammatory phenomena and asthma.

公开(公告)号：NO300683B1

公开(公告)日：1997-07-07

申请号：NO922922

申请日：1992-07-23

Applicant: UCB SA

Inventor： KEULEN BEREND JAN VAN ,  GOLDSTEIN SOLO ,  COSSEMENT ERICK ,  GOBERT JEAN ,  WUELFERT ERNST

IPC: A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61P11/00 ,  A61P11/06 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  C07D251/12 ,  C07D251/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D401/04 ,  C07D403/04 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04 ,  C07D498/08 ,  C07D498/16 ,  C07D498/18 ,  C07D487/06

Abstract: New cyclopropylamino-1,3,5-triazines and their salts, processes for their preparation and therapeutic compositions. These compounds correspond to the formula in which R1 = alkyl, cycloalkyl or alkylcycloalkyl, R2 = bis(2-hydroxyethyl)amino, 3-hydroxy-1-azetidinyl, 3-methoxy-1-azetidinyl, 3-oxo-1-azetidinyl, morpholino, 4-hydroxypiperidino, thiomorpholino, thiomorpholino S-oxide, thiomorpholino S,S-dioxide, 3-thiazolidinyl, 3-thiazolidinyl S-oxide, 3-thiazolidinyl S,S-dioxide or 8-oxa-3-azabicyclo[3.2.1]oct-3-yl. These compounds are useful in the treatment of disorders associated with Alzheimer's disease, Alzheimer-type senile dementias and all evolutive cognitive pathologies and in the treatment of depression, anxiety, mood disorders, inflammatory phenomena and asthma.

公开(公告)号：NO303824B1

公开(公告)日：1998-09-07

申请号：NO941932

申请日：1994-05-25

Applicant: UCB SA

Inventor： MICHEL PHILIPPE ,  COSSEMENT ERICK ,  GOBERT JEAN ,  WUELFERT ERNST

IPC: A61K31/4164 ,  A61K31/4174 ,  A61K31/415 ,  A61K31/4178 ,  A61P27/02 ,  A61P27/06 ,  C07D233/54 ,  C07D233/56 ,  C07D233/64 ,  C07D403/10

Abstract: 2-Hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]benzenecarboximidamides and their salts, processes for their preparation and ophthalmic compositions containing them. These new compounds correspond to the general formula: in which R1 = hydrogen or C1-4 alkyl; R2 = hydrogen, hydroxyl, amino or C1-4 alkyl; R3 = hydrogen; or R2 and R3 = -CH2-CH2-. These are new compounds which are capable of lowering intraocular pressure and which can be used in the treatment and prevention of glaucoma.

公开(公告)号：NO922922D0

公开(公告)日：1992-07-23

申请号：NO922922

申请日：1992-07-23

Applicant: UCB SA

Inventor： KEULEN BEREND JAN VAN ,  GOLDSTEIN SOLO ,  COSSEMENT ERICK ,  GOBERT JEAN ,  WUELFERT ERNST

IPC: A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61P11/00 ,  A61P11/06 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  C07D251/12 ,  C07D251/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D401/04 ,  C07D403/04 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04 ,  C07D498/08 ,  C07D417/00 ,  C07D403/00 ,  C07D413/00 ,  C07D251/00

Abstract: New cyclopropylamino-1,3,5-triazines and their salts, processes for their preparation and therapeutic compositions. These compounds correspond to the formula in which R1 = alkyl, cycloalkyl or alkylcycloalkyl, R2 = bis(2-hydroxyethyl)amino, 3-hydroxy-1-azetidinyl, 3-methoxy-1-azetidinyl, 3-oxo-1-azetidinyl, morpholino, 4-hydroxypiperidino, thiomorpholino, thiomorpholino S-oxide, thiomorpholino S,S-dioxide, 3-thiazolidinyl, 3-thiazolidinyl S-oxide, 3-thiazolidinyl S,S-dioxide or 8-oxa-3-azabicyclo[3.2.1]oct-3-yl. These compounds are useful in the treatment of disorders associated with Alzheimer's disease, Alzheimer-type senile dementias and all evolutive cognitive pathologies and in the treatment of depression, anxiety, mood disorders, inflammatory phenomena and asthma.