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41. 发明专利

SI1648899T1 Imidazo-pirimidini in triazolo-pirimidini: benzodiazepinski receptorski ligandi 未知
公开(公告)号：SI1648899T1
公开(公告)日：2007-08-31
申请号：SI200430193
申请日：2004-07-23
申请人： NEUROGEN CORP
发明人： XIE LINGHONG , HAN BINGSONG , XU YUELIAN , MAYNARD GEORGE , CHENARD BERTRAND L , SHAW KENNETH , GAO YANG
IPC分类号： C07D487/00

42. 发明专利

DK1648899T3 未知
公开(公告)号：DK1648899T3
公开(公告)日：2007-04-02
申请号：DK04779031
申请日：2004-07-23
申请人： NEUROGEN CORP
发明人： HAN BINGSONG , SHAW KENNETH , MAYNARD GEORGE , GAO YANG , XIE LINGHONG , XU YUELIAN , CHENARD BERTRAND L
IPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z 1 , Z 2 , Z 3 , R 4 , R 5 , R 6 , R 7 , R 8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABA A receptors (e.g., receptor localization studies).

43. 发明专利

ES2268488T3 DERIVADOS DE 4-IMIDAZOL-1-ILMETIL-PIRIMIDINA COMO LIGANDOS PARA RECEPTORES DE GABAA. 未知
公开(公告)号：ES2268488T3
公开(公告)日：2007-03-16
申请号：ES03810562
申请日：2003-11-04
申请人： NEUROGEN CORP
发明人： XIE LINGHONG , HAN BINGSONG , XU YUELIAN , MAYNARD GEORGE
IPC分类号： C07D401/14 , A61K31/506 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D403/06 , C07D417/14
摘要： Compuesto que tiene la fórmula: o una sal farmacéuticamente aceptable del mismo, en el que: R1 se selecciona de: (a) hidrógeno, halógeno, nitro y ciano; y (b) grupos de fórmula: en los que: G es un enlace, alquilo C1-C8, -N(RB)-, -O-, -C(=O)-, - C(=O)N(RB)-, -N(RB)C(=O)-, -S(O)m-, -CH2C(=O)-, -S(O)mN(RB)- o -N(RB)S(O)m-; en los que m es 0, 1 ó 2; y RA y cada RB se seleccionan independientemente de: (a) hidrógeno; y (b) alquilo C1-C8, alquenilo C2-C8, alquinilo C2-C8 y heterociclos y carbociclos de 3 a 12 miembros, cada uno de los cuales está sustituido con desde 0 hasta 4 sustituyentes seleccionados independientemente de halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C4, alcoxilo C1- C4, alcanoílo C1-C4, mono y di(alquil C1-C4)amino, haloalquilo C1-C4 y haloalcoxilo C1-C4; R2 es hidrógeno, halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C4, haloalquilo C1-C4, alcoxilo C1-C4, haloalcoxilo C1-C4, cicloalquilo C3-C7, o mono o di(alquil C1-C4)amino; R3 es hidrógeno, halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C8, alquenilo C2-C8, alquinilo C2-C8, cicloalquilo C3-C7, haloalquilo C1-C8, alcoxilo C1-C8, haloalcoxilo C1-C8, alquil éter C2-C8, haloalquil éter C2-C8, o mono o di(alquil C1-C8)amino; R4 representa 0, 1 ó 2 sustituyentes escogidos independientemente de halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C4, alcoxilo C1-C4, mono y di(alquil C1- C4)amino, cicloalquilo C3-C7, haloalquilo C1-C2 y haloalcoxilo C1-C2; Ar representa fenilo, naftilo o heteroarilo de 5 a 10 miembros, cada uno de los cuales está sustituido con desde 0 hasta 4 sustituyentes seleccionados independientemente de halógeno, hidroxilo, nitro, ciano, amino, alquilo C1-C8, alquenilo C1-C8, alquinilo C1-C8, cicloalquil C3-C7(alquilo C0-C8), haloalquilo C1-C8, alcoxilo C1-C8, cicloalquil C3-C7 (alcoxilo C1-C8), haloalcoxilo C1-C8, alquil éter C1-C8, alcanona C1-C8, alcanoílo C1-C8, heterocicloalquil(alquilo C0-C8) de 3 a 7 miembros, oxo, hidroxialquilo C1-C8, aminoalquilo C1-C8, y mono ydi(alquil C1-C8)amino(alquilo C0-C8); y R5 y R6 son independientemente hidrógeno, halógeno, metilo o etilo.

44. 发明专利

AU2006275568A1 Dipiperazinyl ketones and related analogues 未知
公开(公告)号：AU2006275568A1
公开(公告)日：2007-02-08
申请号：AU2006275568
申请日：2006-07-28
申请人： NEUROGEN CORP
发明人： PETERSON JOHN M , OCHTERSKI JOSEPH W , CALDWELL TIMOTHY M , XIE LINGHONG , XU YUELIAN , OHLIGER ROBERT , HAN BINGSONG , GAO YANG , GE PING
IPC分类号： A61K31/551 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/55 , C07D403/02
摘要： Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

45. 发明专利

CA2485093A1 SUBSTITUTED IMIDAZOLE DERIVATIVES: GABAA RECEPTOR LIGANDS 未知
公开(公告)号：CA2485093A1
公开(公告)日：2003-11-13
申请号：CA2485093
申请日：2003-05-02
申请人： NEUROGEN CORP
发明人： GUSTAVSON LINDA M , MAYNARD GEORGE D , HAN BINGSONG
IPC分类号： G01N33/53 , A61K31/4178 , A61K31/4439 , A61P9/10 , A61P25/08 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , A61P31/18 , A61P43/00 , C07D233/64 , C07D401/14 , C07D403/14 , G01N33/534 , A61K31/4164
摘要： Substituted imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA 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 compositions and methods f or treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies). (Formul a I)

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