-
1.发明公开ARYL AND HETEROARYL FUSED AMINOALKYL-IMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIDIABETICS 审中-公开芳基和杂凝聚AMINOALKYLIMIDAZOLDERIVATE及其作为抗糖尿病
公开(公告)号：EP1165519A1
公开(公告)日：2002-01-02
申请号：EP00919947.2
申请日：2000-03-31
申请人： NEUROGEN CORPORATION
IPC分类号： C07D235/14 , C07D471/04 , A61K31/4184 , A61K31/4188 , A61P3/10 , G01N33/50
CPC分类号： C07D471/04 , C07D235/14 , G01N2333/72
摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein X, R1, R2, R3, R4, R5, R6, R7, A, B, C, and D are variables defined herein. Such compounds useful in treatment of obesity and diabetes. The invention also provides labeled probes for the localization of cellular receptors that are involved in the modulation of blood glucose levels.
-
2.发明公开BENZIMIDAZOLE AND IMIDAZOLOPYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS SELECTIVE MODULATORS OF BRADYKININ B2 (= BK-2) RECEPTORS 审中-公开苯并咪唑和咪唑并吡啶衍生物，其制备和血管舒缓激肽B2的它们作为选择性调节剂（= BK-2）受体
公开(公告)号：EP1165518A2
公开(公告)日：2002-01-02
申请号：EP00919946.4
申请日：2000-03-31
申请人： NEUROGEN CORPORATION
发明人： DESIMONE, Robert, W. , HUTCHISON, Alan , SHAW, Kenneth , MAYNARD, George, D. , PETERSON, John, M. , LEW, Richard , BRIELMANN, Harry, L.
IPC分类号： C07D235/14 , C07D471/04 , C07D403/10 , C07D401/06 , A61K31/415 , A61K31/495 , A61K31/535 , A61K31/44
CPC分类号： C07D471/04
摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable salts thereof wherein: R1 is not 3-fluorobenzyl and represents (C2-C6) alkenyl, aryl (C1-C6)alkyl or heteroaryl (C1-C6)alkyl, OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R2 represents hydrogen, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, amino (C1-C6)alkyl, mono- or di(C1-C6)alkylamino (C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R3 represents (C1-C6)alkyl; R4 represents halogen or trifluoromethyl; R5 and R6 represent hydrogen, trifluoromethyl, triluoromethoxy, cyano, (C1-C6)alkyl, halogen, (C1-C6)alkylamino(C1-C6)alkyl, mono or di(C1-C6)alkylamino(C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or together form a 5 or 6 membered aromatic ring which is optionally substituted. X represents a bond or CH2 which is optionally mono- or disubstituted with a (C1-C6)alkyl or (C1-C6)alkoxy; and A, B, C and D are the same or different and represent CRp or N with the proviso that not more than two of A,B, C and D represent N; which compounds are selective modulators of Bradykinin B2 receptors.
-
3.发明公开ARYL AND HETEROARYL FUSED AMINOALKYL-IMIDAZOLE DERIVATIVES: SELECTIVE MODULATORS OF GABAa RECEPTORS 有权芳基和杂芳基氨基烷基者浓缩咪唑衍生物：GABA受体的选择性调节剂
公开(公告)号：EP1165557A1
公开(公告)日：2002-01-02
申请号：EP00919975.3
申请日：2000-03-31
申请人： NEUROGEN CORPORATION
IPC分类号： C07D471/04 , C07D235/14 , A61K31/437 , A61K31/4184 , A61P25/00
CPC分类号： C07D235/14 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of formula (I), or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
-
4.发明公开NOVEL SUBSTITUTED ARYL AND CYCLOALKYL IMIDAZOLONES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 失效取代的芳基和环烷基咪唑啉酮，配体GABA受体在脑中的一类
公开(公告)号：EP0830359A1
公开(公告)日：1998-03-25
申请号：EP96919393.0
申请日：1996-06-04
申请人： NEUROGEN CORPORATION
CPC分类号： C07D413/04 , C07D417/04
摘要： Disclosed are compounds of formula (I) wherein: T is NH, O, or S; X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide; the W ring is an optionally substituted aryl or heteroaryl group; and (a) represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compouns are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
-
5.发明授权ARYL AND HETEROARYL FUSED AMINOALKYL-IMIDAZOLE DERIVATIVES: SELECTIVE MODULATORS OF GABAa RECEPTORS 有权芳基和杂芳基氨基烷基者浓缩咪唑衍生物：GABA受体的选择性调节剂
公开(公告)号：EP1165557B1
公开(公告)日：2004-09-29
申请号：EP00919975.3
申请日：2000-03-31
申请人： NEUROGEN CORPORATION
IPC分类号： C07D471/04 , C07D235/14 , A61K31/437 , A61K31/4184 , A61P25/00
CPC分类号： C07D235/14 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of formula (I), or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
-
6.发明授权SUBSTITUTED CYCLOALKYL-4-OXONICOTINIC CARBOXAMIDES; GABA BRAIN RECEPTOR LIGANDS 有权取代的环烷基-4-氧杂环丁烷羧酰胺; GABA脑受体配体
公开(公告)号：EP1056724B1
公开(公告)日：2005-05-25
申请号：EP99908533.5
申请日：1999-02-26
申请人： NEUROGEN CORPORATION
IPC分类号： C07D221/04 , C07D215/54 , C07D417/12 , C07D407/12 , C07D401/12 , C07D409/12 , A61K31/44
CPC分类号： C07D221/04 , C07D215/56 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Disclosed are compounds of Formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译： 公开了式（a）化合物或其药学上可接受的无毒盐，其中：C环为（n）（未）取代的碳环; X是氢，羟基或低级烷基; 并且W为（未）取代的烷基，芳基，芳烷基或杂芳基，所述化合物为GABAα脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAα脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑症，睡眠和癫痫症，苯二氮卓类药物过量用药和增强记忆力。
-
7.发明公开SUBSTITUTED CYCLOALKYL-4-OXONICOTINIC CARBOXAMIDES; GABA BRAIN RECEPTOR LIGANDS 有权取代的环烷基-4- OXONICOTINISCHE KARBOXAMIDE; GABA脑REZEPTORLIGANDE
公开(公告)号：EP1056724A2
公开(公告)日：2000-12-06
申请号：EP99908533.5
申请日：1999-02-26
申请人： NEUROGEN CORPORATION
IPC分类号： C07D221/04 , C07D215/54 , C07D417/12 , C07D407/12 , C07D401/12 , C07D409/12 , A61K31/44
CPC分类号： C07D221/04 , C07D215/56 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Disclosed are compounds of Formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
-
-
-
-
-
-
搜索结果
7 条记录 (耗时 0.012 秒)
