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1. 发明申请

WO1997026243A1 NOVEL FUSED PYRROLECARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：新型融合吡咯烷新类型的GABA脑受体配体
公开(公告)号：WO1997026243A1
公开(公告)日：1997-07-24
申请号：PCT/US1997000519
申请日：1997-01-14
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , LIU, Gang , SHAW, Kenneth , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D401/12 , C07D209/42 , C07D209/52 , C07D405/12 , C07D413/12
摘要： The present invention encompasses structures of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein G represents (1) where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with substituents on Q; (2), (3) and (4) independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3; R3, R4, R5, and R6 are the same or different and represent organic or inorganic substituents. 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 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：本发明包括式（I）或其药学上可接受的无毒盐的结构，其中G表示（1）其中Q是任选被羟基或卤素单取代或二取代的芳基取代基; T是卤素，氢，羟基，氨基或具有1-6个碳原子的烷氧基; W是氧，氮，硫或任选取代的亚甲基; X是氢，羟基或烷基; Z是任选地在Q上形成具有取代基的环的有机或无机取代基; （2），（3）和（4）独立地代表任选取代的碳链; 其中k，m和n独立地为0或1-3的整数; R3，R4，R5和R6相同或不同，表示有机或无机取代基。这些化合物是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。

2. 发明申请

WO1998002420A1 CERTAIN FUSED PYRROLECARBOXANILIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔融的吡咯烷酮; 新类型的GABA脑受体配体
公开(公告)号：WO1998002420A1
公开(公告)日：1998-01-22
申请号：PCT/US1997012153
申请日：1997-07-14
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , HUTCHISON, Alan , LIU, Gang
发明人： NEUROGEN CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D209/08 , A61K31/404 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention encompasses structures of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein (a) represents (b) or (c) or (d) or (e) wherein: W represents substituted or unsubstituted phenyl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R3 is hydrogen or an organic group; R4 is hydrogen or substituted or unsubstituted organic substituent; R5 and R6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4, 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：本发明包括式（I）的结构或其药学上可接受的无毒盐，其中（a）表示（b）或（c）或（d）或（e）其中：W表示取代或未取代的苯基; X是氢，羟基或低级烷基; T是氢，卤素，羟基，硝基，氨基或烷基; R3是氢或有机基团; R4是氢或取代或未取代的有机取代基; R5和R6代表有机和无机取代基; 和n为1,2,3或4，这些化合物是用于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。

3. 发明申请

WO1998002433A1 CERTAIN FUSED PYRROLECARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔融的吡咯烷新类型的GABA脑受体配体
公开(公告)号：WO1998002433A1
公开(公告)日：1998-01-22
申请号：PCT/US1997007830
申请日：1997-05-09
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , LIU, Gang , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D401/12
CPC分类号： C07D209/08 , A61K31/404 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention encompasses structures of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein (a) represents (i) or (ii) or (iii) or (iv) wherein W represents substituted or unsubstituted heteroaryl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R3 is hydrogen or an organic group; R4 is hydrogen or substituted or unsubstituted organic substituent; R5 and R6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4, 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：本发明包括式（I）的结构或其药学上可接受的无毒盐，其中（a）表示（i）或（ii）或（iii）或（iv）其中W表示取代或未取代的杂芳基; X为氢，羟基或低级烷基; T是氢，卤素，羟基，硝基，氨基或烷基; R3是氢或有机基团; R4是氢或取代或未取代的有机取代基; R5和R6代表有机和无机取代基; 和n为1,2,3或4，这些化合物是用于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。

4. 发明申请

WO1997034870A1 CERTAIN FUSED PYRROLECARBOXAMIDES AS GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔化的吡咯类抗生素作为GABA脑受体配体
公开(公告)号：WO1997034870A1
公开(公告)日：1997-09-25
申请号：PCT/US1997004623
申请日：1997-03-20
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , LIU, Gang , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D401/12 , C07D209/42 , C07D409/12 , C07D471/04
摘要： Diclosed are compounds of formula (I), or the pharmaceutically acceptable non-toxic salts thereof, wherein W represents substituted or unsubstituted phenyl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. 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 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：被称为式（I）化合物或其药学上可接受的无毒盐，其中W表示取代或未取代的苯基; T是氢，卤素，羟基，氨基或烷基; X是氢，羟基或低级烷基; m为0,1或2; n为0,1或2; 并且R 3和R 4表示取代或未取代的有机残基。这些化合物是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。

5. 发明申请

WO1995011885A1 CERTAIN FUSED PYRROLECARBOXANILIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些熔融的吡咯烷酮; 新类型的GABA脑受体配体
公开(公告)号：WO1995011885A1
公开(公告)日：1995-05-04
申请号：PCT/US1994012300
申请日：1994-10-26
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D405/12 , C07D209/08 , C07D209/42 , C07D209/52 , C07D307/84 , C07D413/04 , C07D471/04
摘要： The present invention encompasses structures of formula (I) and the pharmaceutically acceptable non-toxic salts thereof wherein (a) represents (b), (c), (d) or (e), wherein W represents substituted or unsubstituted aryl groups; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxyl, amino or alkyl; R3 is hydrogen or an organic group; R4 is hydrogen or substituted or unsubstituted organic substituent; R5 and R6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4. 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 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：本发明包括式（I）的结构及其药学上可接受的无毒盐，其中（a）代表（b），（c），（d）或（e），其中W表示取代或未取代的芳基; X是氢，羟基或低级烷基; T是氢，卤素，羟基，氨基或烷基; R3是氢或有机基团; R4是氢或取代或未取代的有机取代基; R5和R6代表有机和无机取代基; 这些化合物是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。

6. 发明申请

WO1994005665A1 CERTAIN ARYL AND CYCLOALKYL FUSED IMIDAZOPYRAZINOLS; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些亚甲基和环丙基氟化咪唑并吡嗪; 新类型的GABA脑受体配体
公开(公告)号：WO1994005665A1
公开(公告)日：1994-03-17
申请号：PCT/US1993008042
申请日：1993-08-24
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , HUTCHISON, Alan , BLUM, Charles
发明人： NEUROGEN CORPORATION
IPC分类号： C07D471/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention encompasses structures of formula (I) and the pharmaceutically acceptable non-toxic salts thereof wherein (a) represents (b); (c); (d) or (e) or (f), where W represents an aromatic group substituted with various organic and inorganic substituents; X, Y are hydrogen, halogen, hydroxy or amino with the proviso that at least X or Y is hydroxy; A, B, C and D represent nitrogen or a carbon atom substituted with various organic and inorganic substituents; E represents oxygen, sulfur or substituted nitrogen; R3, R4, R12 and R13 are variables representing various organic and inorganic substituents; and n is 0, 1 or 2.
摘要翻译：本发明包括式（I）的结构及其药学上可接受的无毒盐，其中（a）代表（b）; （C）; （d）或（e）或（f），其中W表示被各种有机和无机取代基取代的芳族基团; X，Y是氢，卤素，羟基或氨基，条件是至少X或Y是羟基; A，B，C和D表示氮或被各种有机和无机取代基取代的碳原子; E表示氧，硫或取代的氮; R3，R4，R12和R13是表示各种有机和无机取代基的变量; n为0,1或2。

7. 发明申请

WO1993004066A1 CERTAIN IMIDAZOQUINOXALINOLS; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些IMIDAZOQUINOXALINOLS; GABA脑受体配体一类新
公开(公告)号：WO1993004066A1
公开(公告)日：1993-03-04
申请号：PCT/US1992007080
申请日：1992-08-27
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela , HUTCHISON, Alan, J.
发明人： NEUROGEN CORPORATION
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention encompasses compounds of formula (I) and the pharmaceutically acceptable non-toxic salts thereof wherein: X and Y are hydrogen, halogen, hydroxy or amino with the proviso that at least X or Y is hydroxy; and R1-R4 are variables representing various organic and inorganic substituents; and W represents phenyl, 2- or 3-thienyl, or 2-, 3-, or 4-pyridyl; or phenyl, 2- or 3-thienyl, or 2-, 3-, or 4-pyridyl, each of which is mono or disubstituted with various organic or inorganic substituents. These compounds or prodrugs thereof are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

8. 发明申请

WO1994026742A1 CERTAIN ARYL FUSED IMIDAZOPYRIMIDINES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些ARYL融合了咪唑并嘧啶; 新类型的GABA脑受体配体
公开(公告)号：WO1994026742A1
公开(公告)日：1994-11-24
申请号：PCT/US1993004095
申请日：1993-05-06
申请人： NEUROGEN CORPORATION , THURKAUF, Andrew , HUTCHISON, Alan, J. , ALBAUGH, Pamela
发明人： NEUROGEN CORPORATION
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： The present invention encompasses compounds of formula (I) and the phamaceutically acceptable non-toxic salts thereof wherein ( alpha ) represents (a); (b); (c); (d); X is oxygen or sulfur; W is phenyl, thienyl, or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents; A, B, C and D represent carbon or nitrogen, each of which may be substituted with various organic or inorganic groups; E is oxygen, sulfur, or substituted or unsubstituted nitrogen; and R3 and R4 are the same or different and represent various organic or inorganic substituents; which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory structures.
摘要翻译：本发明包括式（I）化合物及其药物学上可接受的无毒盐，其中（α）代表（a）; （B）; （C）; （D）; X是氧或硫; W是苯基，噻吩基或吡啶基，它们各自可以是未被取代的或被有机或无机取代基单取代或二取代; A，B，C和D表示碳或氮，各自可以被各种有机或无机基团取代; E是氧，硫或取代或未取代的氮; R3和R4相同或不同，代表各种有机或无机取代基; 哪些化合物是GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且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，以及增强记忆结构。

9. 发明申请

WO1992000296A1 CERTAIN AZACYCLOALKYL IMIDAZOPYRIMIDINES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS 审中-公开
标题翻译：某些亚油酸吗咪唑嗪; 新类型的GABA脑受体配体
公开(公告)号：WO1992000296A1
公开(公告)日：1992-01-09
申请号：PCT/US1991004254
申请日：1991-06-24
申请人： NEUROGEN CORPORATION , ALBAUGH, Pamela
发明人： NEUROGEN CORPORATION
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： The invention encompasses compounds of formula (I) and the pharmaceutically acceptable non-toxic salts thereof wherein n is 0, 1, or 2, X is -N=C-R3 or -NR4-C=T, Z is H2, oxygen or sulfur, and R1, R2, R3, R4, T, W, and Y are defined variables. These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

10. 发明申请

WO1996035689A1 NOVEL DEAZAPURINE DERIVATIVES; A NEW CLASS OF CRF1 SPECIFIC LIGANDS 审中-公开
标题翻译：新型二氮杂萘衍生物一类新的CRF1特殊配置
公开(公告)号：WO1996035689A1
公开(公告)日：1996-11-14
申请号：PCT/US1996006708
申请日：1996-05-09
申请人： NEUROGEN CORPORATION , YUAN, Jun , HUTCHISON, Alan
发明人： NEUROGEN CORPORATION
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of formula (I), wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：公开了式（I）的化合物，其中Ar表示芳基或杂芳基; 并且R1，R2，R3，R4和R5代表有机或无机取代基，这些化合物是人CRF1受体的高选择性部分激动剂或拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁，头痛和焦虑。

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