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21. 发明专利

ZA200809208B Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 未知
公开(公告)号：ZA200809208B
公开(公告)日：2009-08-26
申请号：ZA200809208
申请日：2008-10-27
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G , VAN VLIET BERNARD J
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101

22. 发明专利

MX2009006411A INHIBIDORES SELECTIVOS DE ENZIMAS QUE DEGRADAN NEUROTENSINA. 未知
公开(公告)号：MX2009006411A
公开(公告)日：2009-06-23
申请号：MX2009006411
申请日：2007-12-12
申请人： SOLVAY PHARM BV
发明人： KRUSE CORNELIS G , SMID PIETER , FEENSTRA ROELOF W
IPC分类号： A61K38/05 , C07K5/06 , A61P1/00 , A61P9/12 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07F9/30 , C07K5/062 , C07K5/065 , C07K5/078
摘要： Esta invención se refiere a inhibidores selectivos de las enzimas que degradan la neurotensina, a composiciones farmacéuticas que contienen estos compuestos, a métodos para preparar los compuestos, métodos para preparar intermediarios novedosos útiles para su síntesis, y métodos para preparar composiciones; la invención también se refiere a los usos de dichos compuestos y composiciones, particularmente su uso en la fabricación de medicamentos para regular la presión sanguinea o el vaciado gástrico, o tratar la enfermedad de Parkinsor,, ansiedad, depresión o psicosis; los compuestos tienen la fórmula general (1) en donde los símbolos tienen los significados dados en la especificación. (ver fórmula (1)).

23. 发明专利

HRP20080689T3 IMIDAZOLINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 未知
公开(公告)号：HRP20080689T3
公开(公告)日：2009-05-31
申请号：HRP20080689
申请日：2008-12-31
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G , STUIVENBERG HERMAN H VAN
IPC分类号： C07D233/28
摘要： The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

24. 发明专利

SK286778B6 Piperazine and piperidine compounds, method for their preparation and pharmaceutical compositions comprising the same and their use 未知
公开(公告)号：SK286778B6
公开(公告)日：2009-05-07
申请号：SK15872002
申请日：2001-05-10
申请人： SOLVAY PHARM BV
发明人： FEENSTRA ROELOF W , VAN DER HEIJDEN JOHANNES A M , KRUSE CORNELIS G , LONG STEPHEN K , VAN SCHARRENBURG GUSTAAF J M
IPC分类号： C07D413/00 , C07D413/10 , A61K31/00 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D263/00 , C07D263/54 , C07D263/58 , C07D277/62 , C07D413/04 , C07D413/12 , C07D413/14
摘要： Compounds of the formula (I) wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents -C, = C or -N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors.

25. 发明专利

PL1725536T3 Pochodne imidazoliny mające czynność CB1-antagonistyczną 未知
公开(公告)号：PL1725536T3
公开(公告)日：2009-04-30
申请号：PL05716710
申请日：2005-02-16
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G , VAN STUIVENBERG HERMAN H
IPC分类号： C07D233/28

26. 发明专利

DE602005013424D1 未知
公开(公告)号：DE602005013424D1
公开(公告)日：2009-04-30
申请号：DE602005013424
申请日：2005-12-06
申请人： SOLVAY PHARM BV
发明人： VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS T M
IPC分类号： A61K31/496 , A61P25/00 , C07D405/12

27. 发明专利

AR064765A1 COMPUESTOS CON UNA COMBINACION DE ANTAGONISMO DE CB1 CANNABINOIDE E INHIBICION DE RECAPTACION DE SEROTONINA 未知
公开(公告)号：AR064765A1
公开(公告)日：2009-04-22
申请号：ARP080100048
申请日：2008-01-07
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G
IPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61P25/00 , C07D233/93 , C07D403/12
摘要： Reivindicacion 1: Compuestos con una combinacion de antagonismo de CB1 cannabinoide e inhibicion de la recaptacion de serotonina. Reivindicacion 3:Compuestos segun lo reivindicado en la reivindicacion 1 de la formula (1) o un tautomero, estereoisomero, N-oxido, análogo isotopicamente marcado o una sal, hidrato o solvato farmacologicamente aceptable de cualquiera de los anteriores, en donde: A representa un elemento estructural esencial de cualquier antagonista conocido de CB1 cannabinoide que contiene al menos dos anillos fenilo que están independientemente opcionalmente sustituidos con uno o más sustituyentes seleccionados de halogeno, metoxi y trifluorometilo, estando dicho elemento estructural esencial unido a un aceptor de enlace hidrogeno en dicho antagonista de CB1 cannabinoide, en donde el grupo molecular aceptor de enlace H es un grupo carbonilo, sulfonilo, o un átomo de N u O incorporado en una estructura de anillo heteroaromático; N representa un átomo de nitrogeno no básico; T representa una cadena de carbonos saturada o insaturada de 0-8 átomos, en donde un átomo de C puede estar reemplazado con un átomo de N, opcionalmente sustituido con un grupo alquilo C1-3 o CH2CF3, o reemplazado con un átomo de O o un átomo de S, y la cual cadena está opcionalmente sustituida con uno o más sustituyentes seleccionados de F, amino, ciano, alquilo C1-3, alcoxi C1-3 y trifluorometilo; R representa un átomo de H, o un grupo alquilo C1-3, o R junto con el átomo de N al cual está unido, y junto con una parte de T, forma un grupo heterocicloalquilo C4-7 o un grupo heteroarilo, B representa un elemento estructural esencial de cualquier inhibidor de la recaptacion de serotonina conocido.

28. 发明专利

NO20091485L 未知
公开(公告)号：NO20091485L
公开(公告)日：2009-04-17
申请号：NO20091485
申请日：2009-04-16
申请人： SOLVAY PHARM BV
发明人： KEIZER HISKIAS G , KRUSE CORNELIS G , BAKKER WOUTER I IWEMA , NEUT MARTINA A W VAN DER , LOEVEZIJN ARNOLD VAN , ZORGDRAGER JAN
IPC分类号： C07D231/06
摘要： This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.

29. 发明专利

AT425754T 未知
公开(公告)号：AT425754T
公开(公告)日：2009-04-15
申请号：AT05817508
申请日：2005-12-06
申请人： SOLVAY PHARM BV
发明人： VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS T M
IPC分类号： A61K31/496 , A61P25/00 , C07D405/12
摘要： The present invention relates to a group of novel 3 -(2-piperidin-4-yl-ethyl)-1H-indole derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D 2 receptors and to methods for the preparation of these compounds. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

30. 发明专利

DK1438296T3 未知
公开(公告)号：DK1438296T3
公开(公告)日：2009-03-30
申请号：DK02772314
申请日：2002-09-17
申请人： SOLVAY PHARM BV
发明人： KRUSE CORNELIS G , LANGE JOSEPHUS H M , HERREMANS A H J , VAN STUIVENBERG H H
IPC分类号： C07D233/90 , A61K31/4164 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P1/08 , A61P1/12 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/06 , A61P31/04 , A61P35/00 , A61P43/00 , C07C257/18 , C07D295/30 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12
摘要： The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R1-R4 have the meanings given in the specification.

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