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公开(公告)号:HK95693A
公开(公告)日:1993-09-24
申请号:HK95693
申请日:1993-09-16
Applicant: UCB SA
Inventor: COSSEMENT ERIC , GOBERT JEAN , BOYDENS ROLAND , MATHIEU JACQUES
IPC: C07D413/04 , A61K31/53 , A61K31/535 , A61K31/5377 , A61P21/02 , A61P25/28 , A61P27/06 , C07D251/18
Abstract: New 2-amino-4-morpholino-6-propyl-1,3,5-triazines having the formula (I) wherein R1 is hydrogen, alkyl, aralkyl or acetyl, R2 is hydroxyl, hydroxyalkyl, alkoxyalkyl, dialkylamino, arylhydroxyalkyl, (hydroxy-cycloalkyl)alkyl, alkanoyloxyalkyl, benzoyloxyalkyl, phenylacetyloxyalkyl, aminocarbonyloxyalkyl, COR3 or CONR4R5, or NR1R2=(hydroxyalkyl)alkyleneimino, R3=alkyl, aryl, haloaryl, alkylaryl, alkoxyaryl, aralkyl or aryloxy, R4=R5=hydrogen or alkyl, alkyl, alkoxy and alkanoyloxy having 1 to 4 carbon atoms, cycloalkyl and alkyleneimino having 4 to 6 carbon atoms. Moreover, when R1 is acetyl, R2 is acetoxyalkyl. Processes for the preparation thereof and pharmaceutical compositions containing the same are also given. In particular, these compounds are useful for the treatment of cognitive and behavioral disorders associated with aging and dementia syndromes, e.g. those associated with Alzheimer's disease.
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公开(公告)号:NO173331B
公开(公告)日:1993-08-23
申请号:NO891760
申请日:1989-04-27
Applicant: UCB SA
Inventor: COSSEMENT ERIC , GEERTS JEAN-PIERRE , GOBERT JEAN , MICHEL PHILIPPE , WUELFERT ERNST
IPC: A61K31/415 , A61K31/4164 , C07D233/56 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P29/00 , C07D233/54 , C07D233/64 , C07D403/10
Abstract: New substituted 1-(1H-imidazol-4-yl)alkyl-benzamides and their salts, processes for the preparation thereof and pharmaceutical compositions. These compounds have the formula wherein R1, R2=hydrogen or C1-C4-alkyl, R3=hydrogen, amino, hydroxyl, C1-C4-alkyl or C1-C4-hydroxyalkyl, R4=hydrogen or C1-C4-alkyl, or R3R4N=pyrrolidino, piperidino or morpholino, R5 and R6=hydrogen, hydroxyl, C1-C4-alkyl or C1-C4-alkoxy, at least one of R5 and R6 being other than hydrogen. These compounds are prepared either by reacting a nitrogen compound with an alkyl 1-(1H-imidazol-4-yl)alkyl-benzoate or with a 1-(1H-imidazol-4-yl)alkyl-benzoic acid, or by hydrolyzing in an acid medium a 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzonitrile. The compounds have anti-ischemic and alpha 2-adrenoceptor agonist activities.
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公开(公告)号:PL161591B1
公开(公告)日:1993-07-30
申请号:PL28360389
申请日:1989-08-11
Applicant: UCB SA
Inventor: COSSEMENT ERIC , GOBERT JEAN , BOYDENS ROLAND , MATHIEU JACQUES
IPC: A61K31/53 , C07D413/04 , A61K31/535 , A61K31/5377 , A61P21/02 , A61P25/28 , A61P27/06 , C07D251/18
Abstract: New 2-amino-4-morpholino-6-propyl-1,3,5-triazines having the formula (I) wherein R1 is hydrogen, alkyl, aralkyl or acetyl, R2 is hydroxyl, hydroxyalkyl, alkoxyalkyl, dialkylamino, arylhydroxyalkyl, (hydroxy-cycloalkyl)alkyl, alkanoyloxyalkyl, benzoyloxyalkyl, phenylacetyloxyalkyl, aminocarbonyloxyalkyl, COR3 or CONR4R5, or NR1R2=(hydroxyalkyl)alkyleneimino, R3=alkyl, aryl, haloaryl, alkylaryl, alkoxyaryl, aralkyl or aryloxy, R4=R5=hydrogen or alkyl, alkyl, alkoxy and alkanoyloxy having 1 to 4 carbon atoms, cycloalkyl and alkyleneimino having 4 to 6 carbon atoms. Moreover, when R1 is acetyl, R2 is acetoxyalkyl. Processes for the preparation thereof and pharmaceutical compositions containing the same are also given. In particular, these compounds are useful for the treatment of cognitive and behavioral disorders associated with aging and dementia syndromes, e.g. those associated with Alzheimer's disease.
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公开(公告)号:CA1320732C
公开(公告)日:1993-07-27
申请号:CA614708
申请日:1989-09-29
Applicant: UCB SA
Inventor: BODSON GUY , COSSEMENT ERIC , GOBERT JEAN
IPC: C07D295/08 , C07D295/088 , C07D295/15
Abstract: A process for the preparation of 2-¢2-¢4¢(4-chlorophenyl)phenylmethyl!-1-piperazinyl!ethoxy!-acetic acid and its dihydrochloride, wherein 2¢4-¢(4-chlorophenyl-phenylmethyl!-1-piperazinyl!-ethanol is reacted with an alkali metal halogenoacetate in the presence of an alkali metal alcoholate, the alkali metal salt thus obtained is converted into the corresponding acid and, if appropriate, into its dihydrochloride.
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公开(公告)号:HK45493A
公开(公告)日:1993-05-21
申请号:HK45493
申请日:1993-05-13
Applicant: UCB SA
Inventor: COSSEMENT ERIC , GOBERT JEAN , BODSON GUY
IPC: C07D295/08 , C07D295/088
Abstract: A process for the preparation of 2-[2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid and its dihydrochloride, wherein 2-[4-[(4-chlorophenyl-phenylmethyl]-1-piperazinyl]1-1ethanol is reacted with an alkali metal halogenoacetate in the presence of an alkali metal alcoholate, the alkali metal salt thus obtained is converted into the corresponding acid and, if appropriate, into its dihydrochloride.
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公开(公告)号:NO172287B
公开(公告)日:1993-03-22
申请号:NO894650
申请日:1989-11-22
Applicant: UCB SA
Inventor: BODSON GUY , COSSEMENT ERIC , GOBERT JEAN
IPC: C07D295/08 , C07D295/088
Abstract: A process for the preparation of 2-[2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid and its dihydrochloride, wherein 2-[4-[(4-chlorophenyl-phenylmethyl]-1-piperazinyl]1-1ethanol is reacted with an alkali metal halogenoacetate in the presence of an alkali metal alcoholate, the alkali metal salt thus obtained is converted into the corresponding acid and, if appropriate, into its dihydrochloride.
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公开(公告)号:IE922422A1
公开(公告)日:1993-01-27
申请号:IE922422
申请日:1992-07-24
Applicant: UCB SA
Inventor: KEULEN BEREND JAN VAN , GOLDSTEIN SOLO , COSSEMENT ERIC , GOBERT JEAN , WULFERT 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 , C07D251/00 , C07D417/00 , C07D403/00 , C07D498/00 , C07D401/00
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.
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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
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公开(公告)号:FI923314A
公开(公告)日:1993-01-26
申请号:FI923314
申请日:1992-07-21
Applicant: UCB SA
Inventor: VAN KEULEN BEREND JAN , GOLDSTEIN SOLO , COSSEMENT ERIC , 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
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.
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公开(公告)号:DK163501C
公开(公告)日:1992-07-27
申请号:DK212985
申请日:1985-05-14
Applicant: UCB SA
Inventor: GOBERT JEAN , GEERTS JEAN-PIERRE , BODSON GUY
IPC: C07D207/26 , A61K31/40 , A61K31/4015 , A61P7/06 , A61P9/00 , A61P9/10 , C07D207/12 , C07D207/27 , C07D207/277 , C07D295/185
Abstract: (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-amino-butanamide of the formula X-CH2CH2-NHCH (C2H5)CONH2 wherein Y is a -CH2-radical when X represents a ZOOC-radical and Y is a -CO- radical when X represents a HalCH2-radical, Z being a C1-C4 alkyl radical and Hal a halogen atom. This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
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