公开(公告)号：BRPI0108664B8

公开(公告)日：2021-05-25

申请号：BR0108664

申请日：2001-02-21

Applicant: UCB BIOPHARMA SPRL ,  UCB PHARMA SA ,  UCB SA

Inventor： ALAIN MATAGNE ,  BENOÎT KENDA ,  BÉNÉDICTE LALLEMAND ,  EDMOND DIFFERDING ,  PATRICE TALAGA ,  PATRICK PASAU ,  PHILIPPE MICHEL

IPC: C07D207/00 ,  C07D401/04 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/541 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P27/16 ,  A61P37/08 ,  C07B61/00 ,  C07C237/06 ,  C07C237/12 ,  C07D207/26 ,  C07D207/27 ,  C07D207/273 ,  C07D207/277 ,  C07D307/33 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D495/04

Abstract: "composto, composição farmacêutica, uso de um composto e método para tratar epilepsia epileptogênese, distúrbios de ataque, convulsões e outros distúrbios neurológicos". a invenção diz respeito a derivados de 2-oxo-1-pirrolidina da fórmula (i) em que os substituintes são como definidos no relatório descritivo, bem como ao seu uso como produtos farmacêuticos. os compostos da invenção são particularmente adaptados para tratar distúrbios neurológicos tais como a epilepsia.

公开(公告)号：ZA200205837B

公开(公告)日：2003-11-04

申请号：ZA200205837

申请日：2002-07-22

Applicant: UCB SA

Inventor： DIFFERDING EDMOND ,  KENDA BENOIT ,  LALLEMAND BENEDICTE ,  MATAGNE ALAIN ,  PHILIPPE MICHEL ,  PASAU PATRICK ,  TALAGA PATRICE

IPC: C07D401/04 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/541 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P27/16 ,  A61P37/08 ,  C07B61/00 ,  C07C237/06 ,  C07C237/12 ,  C07D207/26 ,  C07D207/27 ,  C07D207/273 ,  C07D207/277 ,  C07D307/33 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D495/04 ,  C07D

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of general formula (B. geometrical isomers, enantiomers, diastereoisomers, mixtures of each of these and pharmaceutically acceptable salts thereof. whereinR 1 is methyl,R 2 and R 4 are hydrogen.R 3 is alkyl or haloalkenyl, andX is -COOH. -COOMe or -COOEt.

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.

公开(公告)号：CZ124794A3

公开(公告)日：1994-12-15

申请号：CZ124794

申请日：1994-05-20

Applicant: UCB SA

Inventor： PHILIPPE MICHEL ,  COSSEMENT ERIC ,  GOBERT JEAN ,  WULFERT ERNST

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61P27/02 ,  A61P27/06 ,  C07D233/54 ,  C07D233/56 ,  C07D233/64 ,  C07D403/10 ,  C07C257/18 ,  C07C257/22

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：ZA8903140B

公开(公告)日：1990-01-31

申请号：ZA8903140

申请日：1989-04-27

Applicant: UCB SA

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

IPC: C07D233/56 ,  A61K31/415 ,  A61K31/4164 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P29/00 ,  C07D233/54 ,  C07D233/64 ,  C07D ,  A61K

CPC classification number: C07D233/64

公开(公告)号：CZ9401247A3

公开(公告)日：1994-12-15

申请号：CZ124794

申请日：1994-05-20

Applicant: UCB SA

Inventor： PHILIPPE MICHEL ,  COSSEMENT ERIC ,  GOBERT JEAN ,  WULFERT ERNST

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61P27/02 ,  A61P27/06 ,  C07D233/54 ,  C07D233/56 ,  C07D233/64 ,  C07D403/10 ,  C07C257/18 ,  C07C257/22

CPC classification number: C07D233/64

公开(公告)号：ZA878170B

公开(公告)日：1989-07-26

申请号：ZA878170

申请日：1987-10-30

Applicant: UCB SA

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

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/495 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D405/06 ,  C07D413/06 ,  C07D ,  A61K

Abstract: New substituted 1H-imidazoles and their salts, processes for the preparation thereof and pharmaceutical compositions. These compounds have the formula wherein R1, R2, R3 and R5=hydrogen or C1-C4-alkyl; R4=hydrogen, C1-C4-alkyl or C1-C4-alkoxy; Y1=hydrogen and Y2=OZ2 or the reverse; Z1=Z2=hydrogen or C1-C4-alkyl or Z1 and Z2=-CH2- or -C(CH3)2-. These compounds are prepared either by reducing a corresponding imidazole compound having a hydroxyl or alkoxy group on the methyl bridge between the imidazole and phenyl rings, or by hydrolyzing a 4-[[2,2-dimethyl-4H-1,3-benzodioxin-6(or 8)-yl]methyl]-1H-imidazole, or yet by reducing an alkyl 3-[(1H-imidazol-4-yl)methyl]-2-hydroxybenzoate. These compounds have cardiac, cerebral and tissular anti-ischemic activities.

公开(公告)号：ZA200604410B

公开(公告)日：2008-09-25

申请号：ZA200604410

申请日：2004-11-29

Applicant: UCB SA

Inventor： BENOIT KENDA ,  PHILIPPE MICHEL ,  YANNICK QUESNEL

IPC: A61K20090101 ,  A61P20090101 ,  C07D20090101 ,  C07D207/26 ,  C07D207/263 ,  C07D207/27 ,  C07D403/06 ,  C07D403/08

Abstract: The present invention relates to imidazole derivatives of the formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

公开(公告)号：ZA893140B

公开(公告)日：1990-01-31

申请号：ZA893140

申请日：1989-04-27

Applicant: UCB SA

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

IPC: A61K31/415 ,  A61K31/4164 ,  C07D233/56 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P29/00 ,  C07D233/54 ,  C07D233/64 ,  C07D ,  A61K

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：ZA8708170B

公开(公告)日：1989-07-26

申请号：ZA8708170

申请日：1987-10-30

Applicant: UCB SA

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

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/495 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D405/06 ,  C07D413/06 ,  C07D ,  A61K

CPC classification number: C07D233/64 ,  C07D405/06