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41. 发明专利

DE602005009180D1 未知
公开(公告)号：DE602005009180D1
公开(公告)日：2008-10-02
申请号：DE602005009180
申请日：2005-05-26
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , WALS HENDERIK C , KRUSE CORNELIS G
IPC分类号： C07D233/90 , A61K31/4164 , A61K31/454 , A61P25/00

42. 发明专利

AR061808A1 DERIVADOS DE AZAINDOL CON UNA COMBINACION DE AGONISMO PARCIAL DEL RECEPTOR NICOTINICO ACETILCOLINA E INHIBICION DE LA REABSORCION DE DOPAMINA 未知
公开(公告)号：AR061808A1
公开(公告)日：2008-09-24
申请号：ARP070102976
申请日：2007-07-03
申请人： SOLVAY PHARM BV
发明人： VAN DER NEUT MARTINA A W , COOLEN HEIN K A C , STOIT AXEL , KRUSE CORNELIS G
IPC分类号： C07D471/04 , A61K31/40 , A61K31/445 , A61P25/16 , A61P25/28 , A61P25/30 , C07D487/04 , C07D519/00
摘要： Estos compuestos tienen una combinacion de agonismo parcial del receptor nicotínico acetilcolina e inhibicion de la reabsorcion de dopamina. También se refiere a composiciones farmacéuticas que contienen estos compuestos, a métodos para prepararlos, métodos para preparar compuestos intermedios utiles para su síntesis, métodos para preparar composiciones y usos de tales compuestos y composiciones, particularmente su uso en la administracion a pacientes para lograr un efecto terapéutico en trastornos en los que están implicados receptores nicotínicos y/o transportadores de dopamina o que pueden ser tratados vía la manipulacion de tales receptores. Reivindicacion 1: Compuestos derivados de azaindol, caracterizados por la formula general (1) donde X, Y y Z representan independientemente N o C, con la condicion de que el anillo contiene al menos un átomo de N, y no más de 2; m y n son independientemente ya sea 0 (cero) o 1, con la condicion de que cuando Y y Z representan carbono y X representa nitrogeno, m es 0 (cero); R2 y R3 representan independientemente hidrogeno, halogeno, alquilo C1-3, alquinilo C1-3, NH-alquilo C1-3, CF2, hidroxilo, alquil C1-3oxi o un grupo piperidinilo, pirrolidinilo, tetrahidropiridinilo, morfolinilo, azepanilo, 1-aza-biciclo[2.2.2]octanilo o 1-aza-biciclo[2.2.2]oct-2-enilo, grupo que está o insubstituido o substituido con uno o más sustituyentes seleccionados entre halogeno, alquilo C1-3, fenilo o bencilo; R4, R5 y R6 representan independientemente hidrogeno, halogeno, alquilo C1-3, alquinilo C2-3, NH-alquilo C1-3, hidroxilo o alquil C1-3oxi, con la condicion de que R4 existe solo cuando Y = C, R5 solo cuando Z = C; y tautomeros, estereoisomeros y N-oxidos de los mismos, como así también sales farmacologicamente aceptables, hidratos y solvatos de dichos compuestos de formula (1) y sus tautomeros, estereoisomeros y N-oxidos, compuestos que tienen una combinacion de agonismo parcial del receptor nicotínico acetilcolina e inhibicion de reabsorcion de dopamina.

43. 发明专利

DE602005008471D1 未知
公开(公告)号：DE602005008471D1
公开(公告)日：2008-09-04
申请号：DE602005008471
申请日：2005-12-06
申请人： SOLVAY PHARM BV
发明人： FEENSTRA ROELOF W , STOIT AXEL , TERPSTRA JAN-WILLEM , PRAS-RAVES MARIA L , MCCREARY ANDREW C , VAN VLIET BERNARD J , HESSELINK MAYKE B , KRUSE CORNELIS G , VAN SCHARRENBURG GUSTAAF J M
IPC分类号： A61K31/423 , A61P25/00 , C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. 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.

44. 发明专利

ZA200704151B Phenylpiperazines with a combination of affinity for dopamine - D2 receptors and serotonin reuptake sites 未知
公开(公告)号：ZA200704151B
公开(公告)日：2008-08-27
申请号：ZA200704151
申请日：2007-05-22
申请人： SOLVAY PHARM BV
发明人： ROELOF VAN HES , KRUSE CORNELIS G , PIETER SMID , TULP MARTINUS TH M
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D2 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.

45. 发明专利

UA83862C2 ПРОИЗВОДНЫЕ ТИАЗОЛА КАК МОДУЛЯТОРЫ РЕЦЕПТОРОВ КАНАБИНОИДОВ 未知
公开(公告)号：UA83862C2
公开(公告)日：2008-08-26
申请号：UAA200604048
申请日：2004-09-20
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G , VAN STUIVENBERG HERMAN H , SLIEDREGT LEONARDUS A J M
IPC分类号： C07D277/24 , A61K31/426 , A61K31/427 , A61K31/4439 , A61P25/00 , C07D277/38 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Изобретениекасаетсягруппыпроизводныхтиазола, способовполученияэтихсоединений, фармацевтическихкомпозиций, которыесодержат, покрайнеймере, одноизэтихсоединенийв качестведействующеговещества, атакжепримененияэтихсоединенийдлялеченияпсихическихи нервныхрасстройстви другихболезней, связанныхс нейротрансмиссиейканабиноидаСВ. ПроизводныетиазолапоизобретениюявляютсяилиантагонистамирецепторовканабиноидовСВ, илиагонистамирецепторовСВ, илиобратнымиагонистамирецепторовСВ, иличастичнымиагонистамирецепторовСВ.Соединенияимеютобщуюформулу (І), (I)где R, RиХ имеютзначения, приведенныев описании.

46. 发明专利

CA2671554A1 COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB, ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION 未知
公开(公告)号：CA2671554A1
公开(公告)日：2008-07-17
申请号：CA2671554
申请日：2008-01-09
申请人： SOLVAY PHARM BV
发明人： KRUSE CORNELIS G , LANGE JOSEPHUS H M
IPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61P25/00 , C07D233/90 , C07D403/12
摘要： This invention relates to compounds with a combination of cannabinoid-CB1 antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods fo r preparing compositions. The invention also relates to the uses of such com pounds and compositions, particularly their use in administering them to pat ients to achieve a therapeutic effect in psychosis, anxiety, depression, att ention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the ge neral formula (I): wherein the symbols have the meanings given in the specif ication.

47. 发明专利

ZA200704211B Aryloxyethylamine and phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 未知
公开(公告)号：ZA200704211B
公开(公告)日：2008-05-28
申请号：ZA200704211
申请日：2007-05-23
申请人： SOLVAY PHARM BV
发明人： FEENSTRA ROELOF W , JAN-WILLEM TERPSTRA , MCCREARY ANDREW C , HESSELINK MAYKE B , VAN SCHARRANBURG GUSTAAF J M , AXEL STOIT , PRAS-RAVES MARIA L , VAN VLIET BERNARD J , KRUSE CORNELIS G
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. 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, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.

48. 发明专利

AU2003219165B2 Neurotensin active 2,3-diaryl-pyrazolidine derivatives 未知
公开(公告)号：AU2003219165B2
公开(公告)日：2008-03-13
申请号：AU2003219165
申请日：2003-03-17
申请人： SOLVAY PHARM BV
发明人： KRUSE CORNELIS G , PRAS-RAVES MARIA L , FEENSTRA ROELOF W , KEIZER HISKIAS G , STUIVENBERG HERMAN H VAN , LANGE JOSEPHUS H M , TUINSTRA TINKA
IPC分类号： C07D231/04 , A61K31/415 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P43/00 , C07D401/04
摘要： The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.

49. 发明专利

AU2007267097A1 Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 未知
公开(公告)号：AU2007267097A1
公开(公告)日：2007-12-06
申请号：AU2007267097
申请日：2007-05-29
申请人： SOLVAY PHARM BV
发明人： LANGE JOSEPHUS H M , VLIET BERNARD J VAN , KRUSE CORNELIS G
IPC分类号： C07D231/18 , A61K31/4155 , A61P25/30
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB 1 receptor antagonists having a high CB 1 /CB 2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, 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.

50. 发明专利

MX2007006818A DERIVADOS DE FENILPIPERAZINA CON UNA COMBINACION DE AGONISMO PARCIAL DEL RECEPTOR DE DOPAMINA-D2 E INHIBICION DE LA REABSORCION DE SEROTONINA. 未知
公开(公告)号：MX2007006818A
公开(公告)日：2007-11-09
申请号：MX2007006818
申请日：2005-12-06
申请人： SOLVAY PHARM BV
发明人： KRUSE CORNELIS G , TERPSTRA JAN-WILLEM , SCHARRENBURG GUSTAAF J M VAN , FEENSTRA ROELOF W , STOIT AXEL , PRAS-RAVES MARIA L , MCCREARY ANDREW C , VLIET BERNARD J VAN , HESSELINK MAYKE B
IPC分类号： A61K31/00 , C07D413/12 , A61P25/00
摘要： La invencion se refiere a un grupo de nuevos derivados de fenilpiperazina con un doble modo de accion; inhibicion de la reabsorcion de serotonina y agonismo parcial de receptores de dopamina-D2; la invencion tambien se refiere al uso de un compuesto descrito en la misma para la fabricacion de un medicamento que tiene un efecto benefico; los compuestos tienen la formula general (1): (ver formula (1)) donde los simbolos tienen los significados dados en la memoria descriptiva.

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