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91. 发明申请

WO0010973A3 OXO-PYRIDOIMIDAZOLE-CARBOXAMIDES: GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：氧 - 吡啶并咪唑 - 羧酰胺类：GABA BRAIN RECEPTOR LIGANDS
公开(公告)号：WO0010973A3
公开(公告)日：2000-06-29
申请号：PCT/US9919400
申请日：1999-08-25
申请人： NEUROGEN CORP , RACHWAL BOGUMILA , ALBAUGH PAMELA , SHAW KENNETH
发明人： RACHWAL BOGUMILA , ALBAUGH PAMELA , SHAW KENNETH
IPC分类号： A61K31/437 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are compounds of formula (I), or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are 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, depression, sleep, cognitive and seizure disorders, overdose with benzodiazepine drugs and for enhancement of altertness.
摘要翻译：公开了式（I）化合物或其药学上可接受的无毒盐，其中R 1 -R 4和A在本文中定义，该化合物是GABAa脑受体的高度选择性激动剂，拮抗剂或反向激动剂或激动剂，拮抗剂或因此，可用于GABAa脑受体的反向激动剂，因此可用于诊断和治疗焦虑症，唐氏综合征，抑郁症，睡眠，认知和癫痫发作障碍，用苯二氮卓类药物过量并增强其改变。

92. 发明申请

WO9943661A2 SUBSTITUTED CYCLOALKYL-4-OXONICOTINIC CARBOXAMIDES; GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：取代的环己基-4-氧化碳酰胺; GABA脑接受者配偶
公开(公告)号：WO9943661A2
公开(公告)日：1999-09-02
申请号：PCT/US9904310
申请日：1999-02-26
申请人： NEUROGEN CORP , DESIMONE ROBERT W , ROSEWATER DANIEL L
发明人： DESIMONE ROBERT W , ROSEWATER DANIEL L
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/473 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/28 , A61P43/00 , C07D215/56 , C07D221/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/44 , C07D215/54 , C07D407/12
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）的化合物或其药学上可接受的无毒盐，其中：C环是（n）（un）取代的碳环; X是氢，羟基或低级烷基; 并且W是（未取代的）取代的烷基，芳基，芳烷基或杂芳基，该化合物是用于GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa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，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

93. 发明申请

WO9921848A2 NOVEL 1-(N'-(ARYLALKYLAMINOALKYL))AMINOISOINDOLES; A NEW CLASS OF DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS 审中-公开
标题翻译：新的1-（N' - （亚氨基亚氨基））氨基磺酸盐; 一类新的多巴胺受体亚型特异性配体
公开(公告)号：WO9921848A2
公开(公告)日：1999-05-06
申请号：PCT/US9822665
申请日：1998-10-26
申请人： NEUROGEN CORP , HE XIAO SHU , COSTA BRIAN DE , WASLEY JAN W F
发明人： HE XIAO-SHU , DE COSTA BRIAN , WASLEY JAN W F
IPC分类号： C07D209/44 , C07D217/22 , C07D401/12 , C07D403/12 , C07D401/00
CPC分类号： C07D401/12 , C07D209/44 , C07D217/22 , C07D403/12
摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl; Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl; L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11-membered ring with the nitrogen atoms to which they are bonded; CR'R'' represents a methylene group optionally substituted with lower alkyl; and k is an integer of from 1 to 3, which compounds are useful in treating various neuropsychological disorders including, for example, schizophrenia, dementia, depression, anxiety, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents, affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore, compounds of this invention may be useful in treating the extrapyramidyl side effects associated with the use of conventional neuroleptic agents. The interaction of 1-(N'-(arylalkylaminoalkyl)aminoisoindole derivatives of the invention with dopamine receptor subtypes is described. This interaction results in the pharmacological activities of these compounds.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，其中6元环可任选被至多四个独立地选自卤素，羟基，低级烷基或低级烷氧基的基团取代; Ar表示任选取代的芳基或杂芳基; Z表示碳或氮，条件是其中Z为碳，R11表示氢，卤素，羟基，低级烷基或低级烷氧基，或任选被一个或两个选自氢，卤素，羟基，低级烷基或低级烷氧基的基团取代的苯基 ; 并且其中Z是氮，R11表示电子对; R5是氢或低级烷基; L和m表示整数; n为0，或整数; R 12和R 13独立地表示低级烷基; 或一起可以与它们所键合的氮原子一起形成任选取代的5-11元环; CR'R“表示任选被低级烷基取代的亚甲基; 并且k是1至3的整数，该化合物可用于治疗各种神经心理障碍，包括例如精神分裂症，痴呆，抑郁症，焦虑症，帕金森样运动障碍和与使用精神安定药有关的运动障碍，情感性精神分裂症和抑郁症等疾病以及帕金森综合征等某些运动障碍。此外，本发明的化合物可用于治疗与常规精神抑制剂的使用相关的外贴剂副作用。描述了本发明的1-（N' - （芳基烷基氨基烷基）氨基异吲哚衍生物与多巴胺受体亚型的相互作用，这种相互作用导致这些化合物的药理活性。

94. 发明申请

WO9212134A3 CERTAIN AMINOMETHYL PHENYLIMIDAZOLE DERIVATIVES; A NEW CLASS OF DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS 审中-公开
标题翻译：某些氨基甲基苯基咪唑衍生物; 一类新的多巴胺受体亚型特异性配体
公开(公告)号：WO9212134A3
公开(公告)日：1992-08-20
申请号：PCT/US9109816
申请日：1991-12-23
申请人： NEUROGEN CORP
发明人： THURKAUF ANDREW Y , HUTCHISON ALAN J
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/55 , A61P25/00 , A61P25/24 , A61P25/26 , C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention encompasses compounds of formulas (I), where R1, R3, R4, R6, X, Y, and Z and T are variables; and M is α or β, where R2 is a variable; or R1 and R2 together may represent -(CH2)n1 where n1 is 1, 2, or 3. These compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents.
摘要翻译：本发明包括式（I）的化合物，其中R 1，R 3，R 4，R 6，X，Y和Z和T是变量; M是α或β，其中R2是变量; 或者R1和R2一起可以代表 - （CH2）n1，其中n1是1,2或3.这些化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍，如帕金森综合征。此外，本发明的化合物可用于治疗与使用常规精神安定剂相关的extraparamidyl副作用。

95. 发明申请

WO2008066664A3 CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES 审中-公开
标题翻译： CIS-环己基取代的嘧啶酮衍生物
公开(公告)号：WO2008066664A3
公开(公告)日：2008-11-27
申请号：PCT/US2007023318
申请日：2007-11-05
申请人： NEUROGEN CORP , BLUM CHARLES A , GHOSH MANUKA , MARTINEZ ISAMIR , ZHANG XUECHUN , ZHENG XIAOZHANG
发明人： BLUM CHARLES A , GHOSH MANUKA , MARTINEZ ISAMIR , ZHANG XUECHUN , ZHENG XIAOZHANG
IPC分类号： C07D473/34 , A61K31/519 , A61K31/522 , A61P3/04 , A61P11/14 , A61P13/10 , A61P25/02 , A61P25/06 , A61P35/04 , C07D471/04 , C07D495/04 , C07D513/04
CPC分类号： C07D473/30 , C07D471/04 , C07D495/04 , C07D513/04
摘要： Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of Formula (I) 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.
摘要翻译：提供式（I）的顺式 - 环己基取代的嘧啶酮衍生物，其中变量如本文所述。此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。提供了用于使用这些化合物来治疗此类病症的药物组合物和方法，以及使用这些配体用于受体定位研究的方法。

96. 发明申请

WO2007146761A3 DIARYL PYRIMIDINONES AND RELATED COMPOUNDS 审中-公开
标题翻译：二元吡咯烷酮及相关化合物
公开(公告)号：WO2007146761A3
公开(公告)日：2008-10-30
申请号：PCT/US2007070676
申请日：2007-06-08
申请人： NEUROGEN CORP , LI HONGBIN , YUAN JUN , WUSTROW DAVID J
发明人： LI HONGBIN , YUAN JUN , WUSTROW DAVID J
IPC分类号： A01N43/58 , A01N43/66 , A61K31/50 , A61K31/55
CPC分类号： C07D401/04 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/04
摘要： Compounds of Formula (I) are provided. In which the variables are as described herein. Such compounds may be used to modulate CB 1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB 1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and dependency disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式（I）的化合物。其中变量如本文所述。这样的化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人类，驯养的伴侣动物和家畜动物（包括食欲障碍，肥胖症和依赖性疾病）中的CB 1调节有反应的病症。还提供了用于治疗这些疾病的药物组合物和方法，以及使用这些配体进行受体定位研究和各种体外测定的方法。

97. 发明申请

WO2008097483A3 METHODS FOR PREPARING ARYL-SUBSTITUTED KETOPHOSPHONATES 审中-公开
标题翻译：制备芳基取代的酮膦酸酯的方法
公开(公告)号：WO2008097483A3
公开(公告)日：2008-10-02
申请号：PCT/US2008001393
申请日：2008-02-01
申请人： NEUROGEN CORP , CHENARD BERTRAND , LUKE GEORGE P
发明人： CHENARD BERTRAND , LUKE GEORGE P
IPC分类号： A01N57/18 , A61K31/66
CPC分类号： C07F9/655345 , C07F9/4006 , C07F9/65515
摘要： Methods are provided for the synthesis of aryl-substituted ketophosphonates of the Formula (I): wherein variables are as described herein. Such compounds are useful as reagents for olefination reactions, and as intermediates in the synthesis of certain biologically active agents.
摘要翻译：提供了式（I）的芳基取代的酮基膦酸酯的合成方法：其中变量如本文所述。这类化合物可用作烯化反应的试剂，并作为合成某些生物活性剂的中间体。

98. 发明申请

WO2008066789A3 HETEROARYL AMIDE DERIVATIVES 审中-公开
标题翻译：杂芳基酰胺衍生物
公开(公告)号：WO2008066789A3
公开(公告)日：2008-08-21
申请号：PCT/US2007024396
申请日：2007-11-27
申请人： NEUROGEN CORP , HUTCHISON ALAN J , LI HONGBIN , MAO JIANMIN , WUSTROW DAVID J , YUAN JUN , ZHAO HE
发明人： HUTCHISON ALAN J , LI HONGBIN , MAO JIANMIN , WUSTROW DAVID J , YUAN JUN , ZHAO HE
IPC分类号： A01N55/02 , A61K31/555
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/113 , C07D519/00
摘要： Heteroaryl amide derivatives 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.
摘要翻译：提供具有下式的杂芳基酰胺衍生物：其中变量如本文所述。此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。提供了用于使用这些化合物来治疗此类病症的药物组合物和方法，以及使用这些配体用于受体定位研究的方法。

99. 发明申请

WO2008024433A2 HALOALKYL-SUBSTITUTED PYRIMIDINONE DERIVATIVES 审中-公开
标题翻译：卤代烷基取代的嘧啶酮衍生物
公开(公告)号：WO2008024433A2
公开(公告)日：2008-02-28
申请号：PCT/US2007018635
申请日：2007-08-22
申请人： NEUROGEN CORP , BLUM CHARLES A , ZHENG XIAOZHANG , MARTINEZ ISAMIR , CHENARD BERTRAND L
发明人： BLUM CHARLES A , ZHENG XIAOZHANG , MARTINEZ ISAMIR , CHENARD BERTRAND L
IPC分类号： A61K31/519 , A61K31/522 , A61P5/00 , A61P11/06 , A61P11/14 , A61P13/00 , A61P29/00 , C07D409/02 , C07D417/04
CPC分类号： C07D473/30 , C07D471/04 , C07D495/04 , C07D513/04
摘要： Haloalkyl-substituted pyrimidinone derivatives are provided, of the Formula (I): 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.
摘要翻译：提供式（I）卤代烷基取代的嘧啶酮衍生物：其中变量如本文所述。此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。提供了用于使用这些化合物来治疗此类病症的药物组合物和方法，以及使用这些配体用于受体定位研究的方法。

100. 发明申请

WO2007133820A2 DIARYL TRIAZOLONES AS CB1 ANTAGONISTS 审中-公开
标题翻译： DIARYL TRIAZOLONES作为CB1拮抗剂
公开(公告)号：WO2007133820A2
公开(公告)日：2007-11-22
申请号：PCT/US2007060599
申请日：2007-01-17
申请人： NEUROGEN CORP , HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
发明人： HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
IPC分类号： A61F9/00
CPC分类号： C07D401/14 , C07D249/12 , C07D401/04 , C07D403/04 , C07D413/14
摘要： Diaryl triazolones of Formula I are provided, in which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using diaryl traizolones of Formula I to treat such disorders are provided, as are methods for using such compounds as ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式I的二芳基三唑酮，其中变量如本文所述。这些化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了使用式I的二芳基特里诺酮来治疗这些疾病的药物组合物和方法，以及使用这些化合物作为受体定位研究的配体和各种体外测定的方法。

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