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1. 发明授权

US06297256B1 Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands 失效
标题翻译：芳基和杂芳基取代的吡啶衍生物GABA脑受体配体
公开(公告)号：US06297256B1
公开(公告)日：2001-10-02
申请号：US09596031
申请日：2000-06-15
申请人： Guolin Cai , Gang Liu , Pamela A. Albaugh
发明人： Guolin Cai , Gang Liu , Pamela A. Albaugh
IPC分类号： G07D40104
CPC分类号： C07D401/14 , C07D495/04
摘要： Disclosed are aryl and heteroaryl substitated pyridino compounds. 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 and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了芳基和杂芳基取代的吡啶基化合物。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，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍，过量与苯二氮卓类药物和增强记忆。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

2. 发明授权

US06423711B1 Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands 失效
标题翻译：杂环氨基取代的杂芳基稠合吡啶; GABA脑受体配体
公开(公告)号：US06423711B1
公开(公告)日：2002-07-23
申请号：US09736497
申请日：2000-12-13
申请人： Guolin Cai , Gang Liu , Guoquing Chen , Pamela A. Albaugh
发明人： Guolin Cai , Gang Liu , Guoquing Chen , Pamela A. Albaugh
IPC分类号： C07D41304
CPC分类号： C07D471/04 , C07D495/04
摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido; W is (un)substituted alkyl, aryl, or heteroaryl; A and B are hydrogen or lower alkyl, 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中：n是0-3的整数; C环是芳基或杂芳基; X是CH，N或OZ表示电子对，氢或（取代的杂环，芳基或酰氨基; W是（未）取代的烷基，芳基或杂芳基; A和B是氢或低级烷基，该化合物是GABAa脑受体或前药的高选择性激动剂，拮抗剂或反向激动剂激动剂，拮抗剂或GABAa脑受体的反向激动剂。这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

3. 发明授权

US06448246B1 Substituted 4H-1,4-benzothiazine-2-carboxamide: GABA brain receptor ligands 失效
标题翻译：取代的4H-1,4-苯并噻嗪-2-甲酰胺：GABA脑受体配体
公开(公告)号：US06448246B1
公开(公告)日：2002-09-10
申请号：US09578928
申请日：2000-05-25
申请人： Guolin Cai , Gang Liu , Pamela A. Albaugh
发明人： Guolin Cai , Gang Liu , Pamela A. Albaugh
IPC分类号： C07D27916
CPC分类号： C07D417/12 , C07D279/16 , G01N33/948
摘要： Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. 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, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了4H-1,4-苯并噻嗪-2-甲酰胺。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，抑郁，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

4. 发明授权

US6166203A Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands 失效
公开(公告)号：US6166203A
公开(公告)日：2000-12-26
申请号：US259146
申请日：1999-02-26
申请人： Guolin Cai , Gang Liu , Guoquing Chen , Pamela A. Albaugh
发明人： Guolin Cai , Gang Liu , Guoquing Chen , Pamela A. Albaugh
IPC分类号： C07D471/04 , C07D495/04 , C07D413/04 , C07D241/04 , C07D471/02 , C07D513/04 , C07D515/04
CPC分类号： C07D471/04 , C07D495/04
摘要： Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3;the C ring is aryl or heteroaryl;X is CH, N, or OZ represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido;W is (un)substituted alkyl, aryl, or heteroaryl;A and B are hydrogen or lower alkyl,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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

5. 发明授权

US06723332B2 Oxomidazopyridine-carboxamides 失效
标题翻译：恶唑并吡啶 - 甲酰胺
公开(公告)号：US06723332B2
公开(公告)日：2004-04-20
申请号：US09864846
申请日：2001-05-24
申请人： Guolin Cai , Pamela A. Albaugh , Kenneth Shaw
发明人： Guolin Cai , Pamela A. Albaugh , Kenneth Shaw
IPC分类号： A01N2534
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: wherein: A, B, C, E, F, and G are substituents as defined herein, which compounds bind to the benzodiazepine site of GABAA receptors and are therefore useful in treatment of central nervous system (CNS) diseases.
摘要翻译：公开了下式的化合物：其中：A，B，C，E，F和G是如本文所定义的取代基，该化合物结合GABA A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病

6. 发明授权

US06413956B1 Substituted 4-oxo-quinoline-3-carboxamides 失效
标题翻译：取代的4-氧代 - 喹啉-3-甲酰胺
公开(公告)号：US06413956B1
公开(公告)日：2002-07-02
申请号：US09565529
申请日：2000-05-05
申请人： Pamela A. Albaugh , Kevin S. Currie , Dan Rosewater , Guolin Cai
发明人： Pamela A. Albaugh , Kevin S. Currie , Dan Rosewater , Guolin Cai
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D215/56 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D487/04
摘要： Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. 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 and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了式I的化合物或其药学上可接受的盐，其中R1，R2和W如本文所定义。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，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和发作障碍，过量与苯二氮卓类药物和增强记忆。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

7. 发明授权

US06646124B2 Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands 失效
标题翻译：取代的4-氧代 - 萘啶-3-甲酰胺：GABA脑受体配体
公开(公告)号：US06646124B2
公开(公告)日：2003-11-11
申请号：US10114743
申请日：2002-04-02
申请人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
发明人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
IPC分类号： C07D41300
CPC分类号： C07D471/04
摘要： The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：本发明包括式的药学上可接受的无毒盐的结构，其中：X是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 和Y是（未）取代的烷基，芳基或杂芳基，该化合物是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症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

8. 发明授权

US06399604B1 Substituted 4-OXO-napthyridine-3-carboxamides; GABA brain receptor ligands 失效
标题翻译：取代的4-OXO-萘啶-3-甲酰胺; GABA脑受体配体
公开(公告)号：US06399604B1
公开(公告)日：2002-06-04
申请号：US09634093
申请日：2000-08-08
申请人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
发明人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
IPC分类号： A61K31535
CPC分类号： C07D471/04
摘要： The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：本发明包括式的药学上可接受的无毒盐的结构，其中：X是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 和Y是（未）取代的烷基，芳基或杂芳基，该化合物是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症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

9. 发明授权

US6143760A Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands 失效
标题翻译：取代的4-氧代 - 萘啶-3-甲酰胺：GABA脑受体配体
公开(公告)号：US6143760A
公开(公告)日：2000-11-07
申请号：US139456
申请日：1998-08-25
申请人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
发明人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
IPC分类号： C07D471/04 , A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; andY is (un)substituted alkyl, aryl, 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：本发明包括式或其药学上可接受的无毒盐的结构，其中：x是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 并且Y是（未）取代的烷基，芳基或杂芳基，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症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

10. 发明申请

US20110166133A1 FUSED NITROGEN CONTAINING HETEROCYCLES AND COMPOSITIONS THEREOF AS KINASE INHIBITORS 有权
标题翻译：含氮杂环化合物及其作为激酶抑制剂的组合物
公开(公告)号：US20110166133A1
公开(公告)日：2011-07-07
申请号：US12992027
申请日：2009-05-07
申请人： Pamela A. Albaugh , Ha-Soon Choi , Gregory Chopiuk , Yi Fan , Paul Vincent Rucker , Zhicheng Wang
发明人： Pamela A. Albaugh , Ha-Soon Choi , Gregory Chopiuk , Yi Fan , Paul Vincent Rucker , Zhicheng Wang
IPC分类号： A61K31/5377 , C07D295/02 , C07D487/04 , A61K31/5025 , A61P35/00 , A61P17/00 , A61P25/00 , A61P11/06
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.
摘要翻译：本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调激酶活性相关的疾病或病症的方法，特别是Ros，KDR，FMS，C-FMS，FLT3，c-Kit，JAK2， JAK3，Aurora，PDGFR，Lck，TrkA，TrkB，TrkC，IGF-1R，ALK4，ALK5和ALK或其组合。

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