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61. 发明专利

AU2005280366A1 Substituted biaryl piperazinyl-pyridine analogues 未知
公开(公告)号：AU2005280366A1
公开(公告)日：2006-03-09
申请号：AU2005280366
申请日：2005-08-13
申请人： NEUROGEN CORP
发明人： ZHENG XIAOZHANG , BRIELMANN HARRY , BLUM CHARLES A , CHENARD BERTRAND L
IPC分类号： C07D401/04 , A61K31/4427 , A61K31/506 , A61K31/53 , A61P11/00 , A61P11/06 , A61P13/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
摘要： Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

62. 发明专利

CA2567604A1 ARYL-SUBSTITUTED PIPERAZINE DERIVATIVES 未知
公开(公告)号：CA2567604A1
公开(公告)日：2006-01-26
申请号：CA2567604
申请日：2005-06-16
申请人： NEUROGEN CORP
发明人： PRINGLE WALLACE C , YOON TAEYOUNG , STEENSTRA CHERYL K , DOLLER DARIO , O'DONNELL MARY-MARGARET E , LUKE GEORGE P , LEE KYUNGAE , TARRANT JAMES G , PETERSON JOHN M , HODGETTS KEVIN J , HUTCHISON ALAN J , GHOSH MANUKA , CHENARD BERTRAND L , LI GUIYING
IPC分类号： C07D471/00
摘要： Aryl-substituted piperazine derivatives are provided. Such compounds may be used to modulate MCH receptor activity in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

63. 发明专利

CA2555867A1 ARYLALKYLAMINO-SUBSTITUTED QUINAZOLINE ANALOGUES 未知
公开(公告)号：CA2555867A1
公开(公告)日：2005-09-22
申请号：CA2555867
申请日：2005-03-01
申请人： NEUROGEN CORP
发明人： CHENARD BERTRAND L , PETERSON JOHN M , STEENSTRA CHERYL K , BAKTHAVATCHALAM RAJAGOPAL
IPC分类号： A61K31/395 , A61K31/505 , C07D215/16 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04 , C07D491/10
摘要： Arylalkylamino-substituted quinazoline analogues are provided, of the Formul a wherein variables are as described herein. Such compounds are ligands that m ay be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals a nd livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using suc h ligands for receptor localization studies.

64. 发明专利

AU2005221614A1 Arylalkylamino-substituted quinazoline analogues 未知
公开(公告)号：AU2005221614A1
公开(公告)日：2005-09-22
申请号：AU2005221614
申请日：2005-03-01
申请人： NEUROGEN CORP
发明人： BAKTHAVATCHALAM RAJAGOPAL , CHENARD BERTRAND L , STEENSTRA CHERYL K , PETERSON JOHN M
IPC分类号： A61K31/395 , A61K31/505 , C07D215/16 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04 , C07D491/10
摘要： Arylalkylamino-substituted quinazoline analogues are provided, of the Formula wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

65. 发明专利

CA2537331A1 IMIDAZO-PYRIMIDINES AND TRIAZOLO-PYRIMIDINES: BENZODIAZEPINERECEPTOR LIGANDS 未知
公开(公告)号：CA2537331A1
公开(公告)日：2005-02-10
申请号：CA2537331
申请日：2004-07-23
申请人： NEUROGEN CORP
发明人： XIE LINGHONG , XU YUELIAN , HAN BINGSONG , CHENARD BERTRAND L , GAO YANG , MAYNARD GEORGE , SHAW KENNETH
IPC分类号： C07D487/04 , A61K31/519
摘要： Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GAB AA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical composition s and methods for treating such disorders are provided, as are methods for usi ng such ligands for detecting GABAA receptors (e.g., receptor localization studies).

66. 发明专利

CA2504941C 3-SUBSTITUTED-6-ARYL PYRIDINES 未知
公开(公告)号：CA2504941C
公开(公告)日：2012-06-26
申请号：CA2504941
申请日：2003-11-07
申请人： NEUROGEN CORP
发明人： HUTCHISON ALAN , YUAN JUN , LEE KYUNGAE , MAYNARD GEORGE , CHENARD BERTRAND L , LIU NIAN , GUO QIN , GUO ZIHONG , HRNCIAR PETER
IPC分类号： C07D213/60 , A61K31/4418 , A61K31/5377 , A61P9/00 , A61P29/00 , C07B61/00 , C07D213/24 , C07D213/30 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , G01N33/58
摘要： 3-substituted-6-aryl pyridines of Formula (I) are provided: Formula (I) wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

67. 发明专利

NZ553388A Substituted biaryl piperazinyl-pyridine analogues as capsaicin receptor (VR1) modulators 未知
公开(公告)号：NZ553388A
公开(公告)日：2011-01-28
申请号：NZ55338805
申请日：2005-08-13
申请人： NEUROGEN CORP
发明人： BLUM CHARLES A , BRIELMANN HARRY , CHENARD BERTRAND L , ZHENG XIAOZHANG
IPC分类号： A61K31/4427 , A61K31/506 , A61K31/53 , A61P11/00 , A61P11/06 , A61P13/10 , C07D401/04 , C07D401/14 , C07D403/00 , C07D403/14 , C07D413/04 , C07D413/14
摘要： Disclosed is a list of substituted biaryl piperazinyl-pyridine derivatives, or salts thereof, which all fall within formula I, as listed in the specification. Also disclosed are compounds of formula I or salts thereof where the substituents are as defined in the specification. These compounds are capsaicin receptor (VR1) modulators. Also disclosed is the use of the compounds to treat pain.

68. 发明专利

SV2009003173A ANALOGOS DE 2-FENOXIPIRIMIDINONAS REF. 66513-SV (72021) 未知
公开(公告)号：SV2009003173A
公开(公告)日：2010-08-10
申请号：SV2009003173
申请日：2009-02-20
申请人： NEUROGEN CORP
发明人： BAKTHAVATCHALAM RAJAGOPAL , CAPITOSTI SCOTT MICHAEL , XU JIANJUN , CHENARD BERTRAND L , GHOSH MANUKA , BLUM CHARLES A
IPC分类号： A61K31/519
摘要： SE PROVEEN ANÁLOGOS DE 2-FENOXIPIRIMIDINONA, DE LA FORMULA: (VER FORMULA); EN DONDE LAS VARIABLES SON COMO SE DESCRIBE AQUÍ; DICHOS COMPUESTOS SON LIGANDOS QUE SE PUEDEN USAR PARA MODULAR ACTIVIDAD DE RECEPTOR ESPECIFICA IN VIVO O IN VITRO, Y SON PARTICULARMENTE ÚTILES EN EL TRATAMIENTO DE CONDICIONES ASOCIADAS CON ACTIVACIÓN DE RECEPTOR PATOLÓGICA EN HUMANOS, ANIMALES DE COMPAÑÍA DOMESTICADOS Y ANIMALES DE GANADO; SE PROVEEN COMPOSICIONES FARMACÉUTICAS Y MÉTODOS PARA USAR DICHOS COMPUESTOS PARA TRATAR ESOS TRASTORNOS, COMO LO SON LOS MÉTODOS PARA USAR DICHOS LIGANDOS PARA ESTUDIOS DE LOCALIZACIÓN DE RECEPTOR

69. 发明专利

CO6150167A2 ANALOGOS DE 2-FENOXIPIRIMIDINONA 未知
公开(公告)号：CO6150167A2
公开(公告)日：2010-04-20
申请号：CO09028167
申请日：2009-03-18
申请人： NEUROGEN CORP
发明人： BAKTHAVATCHALAM RAJAGOPAL , CAPITOSTI SCOTT MICHAEL , XU JIANJUN , CHENARD BERTRAND L , GHOSH MANUKA , BLUM CHARLES A
IPC分类号： C07D473/34
摘要： 1.- Un compuesto de la fórmula: o una sal farmacéuticamente aceptable o hidrato del mismo, en donderepresenta un heteroarilo de 5 ó 6 miembros fusionado que contiene 1, 2 ó 3 heteroátomos independientemente escogidos de O, N y S, con los átomos de anillo restantes siendo carbono, en donde el heteroarilo fusionado es sustituido con de 0 a 3 sustituyentes independientemente escogidos de amino, hidroxi, alquilo de C1-C6, hidroxialquilo de C1-C6, (cicloalquilo de C3-C7)alquilo de C0-C2, halogenoalquilo de C1-C6, alcoxi de C1-C6, éter alquílico de C2-C6, alcanoiloxi de C1-C6, alquilsulfonilamino de C1-C6, alcanoilamino de C1-C6, y mono- o di-(alquilo de C1-C6)amino; Ar es fenilo o un heteroarilo de 5 ó 6 miembros, cada uno de los cuales es sustituido con de 0 a 4 sustituyentes que son independientemente escogidos de halógeno, ciano, amino, nitro, alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, halogenoalquilo de C1-C6, hidroxialquilo de C1-C6, alcoxi de C1-C6, halogenoalcoxi de C1-C6, (cicloalquilo de C3-C7)alquilo de C0-C4, y mono- o di- (alquilo de C1-C6)amino; y R3 representa de 0 a 4 sustituyentes que son independientemente escogidos de halógeno, hidroxi, ciano, amino, nitro, alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, halogenoalquilo de C1-C6, hidroxialquilo de C1-C6, alcoxi de C1-C6, halogenoalcoxi de C1-C6, (cicloalquilo de C3-C7)alquilo de C0-C4, mono- o di-(alquilo de C1-C6)amino, y mono- o di-(alquilo de C1-C6)aminosulfonilo.

70. 发明专利

MA30720B1 ANALOGUES DE 2-PHENOXYPYRIMIDINONE 未知
公开(公告)号：MA30720B1
公开(公告)日：2009-09-01
申请号：MA31732
申请日：2009-03-23
申请人： NEUROGEN CORP
发明人： BAKTHAVATCHALAM RAJAGOPAL , CAPITOSTI SCOTT MICHAEL , XU JIANJUN , CHENARD BERTRAND L , GHOSH MANUKA , BLUM CHARLES A
IPC分类号： C07D473/34 , A61K31/519 , A61K31/522 , A61P11/14 , A61P13/10 , A61P25/02 , A61P3/04 , A61P35/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要： L'INVENTION CONCERNE DES ANALOGUES DE LA 2-PHÉNOXYPYRIMIDINONE, DE FORMULE : DANS LAQUELLE LES VARIABLES SONT TELLES QUE DÉCRITES ICI. DE TELS COMPOSÉS SONT DES LIGANDS QUI PEUVENT ÊTRE UTILISÉS POUR MODULER L'ACTIVITÉ DE RÉCEPTEURS PARTICULIERS IN VIVO OU IN VITRO ET QUI SONT PARTICULIÈREMENT UTILES DANS LE TRAITEMENT D'AFFECTIONS ASSOCIÉES À L'ACTIVATION PATHOLOGIQUE DE RÉCEPTEURS CHEZ DES HUMAINS, DES ANIMAUX DE COMPAGNIE DOMESTIQUÉS ET LE BÉTAIL. L'INVENTION CONCERNE ÉGALEMENT DES COMPOSITIONS PHARMACEUTIQUES ET DES PROCÉDÉS D'UTILISATION DE TELS COMPOSÉS POUR TRAITER DE TELS TROUBLES, AINSI QUE DES PROCÉDÉS D'UTILISATION DE TELS LIGANDS POUR DES ÉTUDES DE LOCALISATION DE RÉCEPTEURS.

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