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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
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2.发明专利
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.
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公开(公告)号：DE69433802T2
公开(公告)日：2005-05-12
申请号：DE69433802
申请日：1994-03-09
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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
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公开(公告)号：AT198196T
公开(公告)日：2001-01-15
申请号：AT94870084
申请日：1994-05-19
Applicant: UCB SA
Inventor： MICHEL PHILIPPE , COSSEMENT ERIC , GOBERT JEAN , WUELFERT ERNST
IPC: A61K31/415 , A61K31/4164 , A61K31/4174 , 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.
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公开(公告)号：GR3034340T3
公开(公告)日：2000-12-29
申请号：GR20000402028
申请日：2000-09-06
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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
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Patent Agency Ranking
公开(公告)号：DE69424893T2
公开(公告)日：2000-10-12
申请号：DE69424893
申请日：1994-03-09
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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
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公开(公告)号：ES2147569T3
公开(公告)日：2000-09-16
申请号：ES94870043
申请日：1994-03-09
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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
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公开(公告)号：CZ287136B6
公开(公告)日：2000-09-13
申请号：CZ124794
申请日：1994-05-20
Applicant: UCB SA
Inventor： COSSEMENT ERIC , GOBERT JEAN , WUELFERT ERNST , PHILIPPE MICHEL
IPC: A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61P27/02 , A61P27/06 , C07D233/54 , C07D233/56 , C07D233/64 , C07D403/10
Abstract: In the present invention there are disclosed substituted 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidamides, their addition salts with non-toxic, and ophthalmologically acceptable acids, process of their preparation a their use for preparing a medicament for prevention and treatment of glaucoma. In the present invention there are also claimed pharmaceutical compositions containing those compounds. The invented substituted 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidamides correspond to the general formula I, in which Ri1 represents a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, Ri2 represents a hydrogen atom a hydroxyl group, an amine group or an alkyl group containing 1 to 4 carbon atoms, Ri3 represents a hydrogen atom or Ri2 and Ri3 together represent the group -CHi2-CHi2-. Active substances of the proposed pharmaceutical compositions exhibit stimulation properties to alphai2-m presynaptic receptors, are capable of reducing intra-ocular strain and are free of expressive side effects.
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公开(公告)号：PL178546B1
公开(公告)日：2000-05-31
申请号：PL30256594
申请日：1994-03-11
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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
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公开(公告)号：NO306616B1
公开(公告)日：1999-11-29
申请号：NO990351
申请日：1999-01-26
Applicant: UCB SA
Inventor： COSSEMENT ERIC , 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 , C07D295/15
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