公开(公告)号：FI923314A0

公开(公告)日：1992-07-21

申请号：FI923314

申请日：1992-07-21

Applicant: UCB SA

Inventor： VAN KEULEN BEREND JAN ,  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 ,  C07D

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：DE68901511D1

公开(公告)日：1992-06-17

申请号：DE68901511

申请日：1989-07-28

Applicant: UCB SA

Inventor： WUELFERT ERNST ,  GOBERT JEAN ,  COSSEMENT ERIC

IPC: C07D251/18 ,  A61K31/53 ,  A61K31/535 ,  A61P25/04

Abstract: A method for the treatment of cognitive and behavioral disorders associated with aging and with dementia syndromes, for example senile dementia, Alzheimer's type, by administering a 2-amino-4-morpholino-6-propyl-1,3,5-triazine of the formula in which R1=hydrogen, alkyl, aralkyl or acetyl, R2=hydrogen, hydroxyl, alkyl, hydroxyalkyl, alkoxyalkyl, dialkylamino, aryl-hydroxyalkyl, (hydroxycycloalkyl)alkyl, alkanoyloxyalkyl, benzoyloxyalkyl, phenylacetyloxyalkyl, aminocarbonyloxyalkyl, COR3, where R3=alkyl, aryl, halogenoaryl, alkylaryl, alkoxyaryl, aralkyl or aryloxy, CONR4R5, where R4 and R5=hydrogen or alkyl, or R1 and R2 form an alkyleneimino substituted by hydroxyalkyl, and in addition when R1=acetyl, R2=acetoxyalkyl, or a salt thereof.

公开(公告)号：BG50272A3

公开(公告)日：1992-06-15

申请号：BG7023785

申请日：1985-05-14

Applicant: UCB SA

Inventor： GOBERT JEAN ,  GIURGEA CORNELIU ,  GEERTS JEAN-PIERRE ,  BODSON GUY

IPC: C07D207/26 ,  A61K31/40 ,  A61K31/4015 ,  A61P25/28 ,  C07D207/27 ,  C07D295/185

公开(公告)号：AT75942T

公开(公告)日：1992-05-15

申请号：AT89870119

申请日：1989-07-28

Applicant: UCB SA

Inventor： WUELFERT ERNST ,  GOBERT JEAN ,  COSSEMENT ERIC

IPC: C07D251/18 ,  A61K31/53 ,  A61K31/535 ,  A61P25/04

公开(公告)号：PH25982A

公开(公告)日：1992-01-13

申请号：PH39570

申请日：1989-11-23

Applicant: UCB SA

Inventor： COSSEMENT ERIC ,  MOTTE GENEVIEVE ,  BODSON GUY ,  GOBERT JEAN

IPC: C07D295/088 ,  C07D295/08 ,  C07D295/14

Abstract: A process for the preparation of 2-[2-4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid and its dihydrochloride, wherein 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetonitrile is hydrolysed in an aqueous, alcoholic or aqueous-alcoholic medium by a base or by an acid, and, if desired, the acid thus obtained is converted into its dihydrochloride. The compound is claimed per se.o

公开(公告)号：AU614247B2

公开(公告)日：1991-08-22

申请号：AU3991789

申请日：1989-08-15

Applicant: UCB SA

Inventor： COSSEMENT ERIC ,  MATHIEU JACQUES ,  BOYDENS ROLAND ,  GOBERT JEAN

IPC: C07D413/04 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5377 ,  A61P21/02 ,  A61P25/28 ,  A61P27/06 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04

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.

公开(公告)号：HK52391A

公开(公告)日：1991-07-19

申请号：HK52391

申请日：1991-07-11

Applicant: UCB SA

Inventor： GOBERT JEAN ,  GEERTS JEAN-PIERRE ,  BODSON GUY

IPC: A61K31/40 ,  A61K31/4015 ,  C07D207/26 ,  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.

公开(公告)号：AU610796B2

公开(公告)日：1991-05-23

申请号：AU3373089

申请日：1989-04-27

Applicant: UCB SA

Inventor： GEERTS JEAN-PIERRE ,  COSSEMENT ERIC ,  GOBERT JEAN ,  MICHEL PHILIPPE ,  WULFERT ERNST

IPC: C07D233/56 ,  A61K31/415 ,  A61K31/4164 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P29/00 ,  C07D233/54 ,  C07D233/64 ,  A61K31/44 ,  A61K31/445 ,  A61K31/535

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.

公开(公告)号：GR890100771A

公开(公告)日：1990-12-31

申请号：GR89100771

申请日：1989-11-20

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.

公开(公告)号：GR890100769A

公开(公告)日：1990-12-31

申请号：GR89100769

申请日：1989-11-20

Applicant: UCB SA

Inventor： COSSEMENT ERIC ,  MOTTE GENEVIEVE ,  GEERTS JEAN-PIERRE ,  GOBERT JEAN

IPC: C07D207/26 ,  C07D207/27

Abstract: S- alpha -Ethyl-2-oxo-1-pyrrolidineacetamide prepared by hydrogenolysis of (S)- alpha - [2-(methylthio)ethyl]-2-oxo-1- pyrrolidineacetamide in the presence of a desulphurizing reagent such as NaBH4/NiCl2.6H2O, Raney nickel W-2 or, preferably, Raney nickel T-1. (S)- alpha -ethyl-2-oxo-1-pyrrolidineacetamide is useful in the treatment and prevention of hypoxic and ischemic type aggressions of the central nervous system.