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1. 发明授权

US06949562B2 Heterocyclic compounds as ligands of the GABAA receptor 失效
标题翻译：杂环化合物作为GABA A受体的配体
公开(公告)号：US06949562B2
公开(公告)日：2005-09-27
申请号：US10670077
申请日：2003-09-23
申请人： Daniel Yohannes , George Maynard , Jun Yuan , Linghong Xie , Kyungae Lee , Manuka Ghosh , George Luke , Xiaojun Liu , Arthur Nagal , Lawrence Vincent , Kevin Currie , Zhe-Quing Wang
发明人： Daniel Yohannes , George Maynard , Jun Yuan , Linghong Xie , Kyungae Lee , Manuka Ghosh , George Luke , Xiaojun Liu , Arthur Nagal , Lawrence Vincent , Kevin Currie , Zhe-Quing Wang
IPC分类号： A61K31/4162 , A61K31/4178 , A61K31/4188 , A61K31/429 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4709 , A61K31/4745 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D403/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D498/04 , C07D513/04 , A61K31/4353
CPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D513/04
摘要： Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m 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 receptor.
摘要翻译：公开了下式的杂环化合物及其药学上可接受的盐，其中变量A，V，Y，J，E，X，T，G，Q，W，Z，b，n和m在本文中定义。这些化合物是高度选择性的激动剂，拮抗剂或反义激动剂，用于GABA A / A脑受体或GABA A A受体的激动剂，拮抗剂或反向激动剂的前药。

2. 发明授权

US06653471B2 Heterocyclic compounds as ligands of the GABAA receptor 失效
标题翻译：杂环化合物作为GABA A受体的配体
公开(公告)号：US06653471B2
公开(公告)日：2003-11-25
申请号：US09924174
申请日：2001-08-06
申请人： Daniel Yohannes , George Maynard , Jun Yuan , Linghong Xie , Kyungae Lee , Manuka Ghosh , George Luke , Xiaojun Liu , Arthur Nagal , Lawrence Vincent , Kevin Currie , Zhe-Quing Wang
发明人： Daniel Yohannes , George Maynard , Jun Yuan , Linghong Xie , Kyungae Lee , Manuka Ghosh , George Luke , Xiaojun Liu , Arthur Nagal , Lawrence Vincent , Kevin Currie , Zhe-Quing Wang
IPC分类号： C07D48700
CPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D513/04
摘要： Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m 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 receptor.
摘要翻译：公开了下式的杂环化合物及其药学上可接受的盐，其中变量A，V，Y，J，E，X，T，G，Q，W，Z，b，n和m在本文中定义。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。

3. 发明申请

US20060025425A1 Benzimidazole and pyridylimidazole derivatives 失效
标题翻译：苯并咪唑和吡啶基咪唑衍生物
公开(公告)号：US20060025425A1
公开(公告)日：2006-02-02
申请号：US11179458
申请日：2005-07-12
申请人： Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
IPC分类号： A61K31/506 , A61K31/4745 , A61K31/427 , A61K31/4184 , C07D471/02 , C07D403/02 , C07D417/02 , C07D413/02
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物， / SUB>受体。本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。公开了制备式I化合物的新方法。本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。

4. 发明申请

US20050277654A1 4,5-Disubstituted-2-aryl pyrimidines 失效
标题翻译： 4,5-二取代-2-芳基嘧啶
公开(公告)号：US20050277654A1
公开(公告)日：2005-12-15
申请号：US11123755
申请日：2005-05-06
申请人： George Maynard , Manuka Ghosh , Jun Yuan , Kevin Currie , Scott Mitchell , Qin Guo , He Zhao
发明人： George Maynard , Manuka Ghosh , Jun Yuan , Kevin Currie , Scott Mitchell , Qin Guo , He Zhao
IPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I和式II的4,5-二取代-2-芳基嘧啶：其中R 1，R 2，R 3，R 本文定义了R 8，R 9，A和Ar。这些化合物是C5a受体的配体。优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的4,5-二取代-2-芳基嘧啶，其可用作C5a受体定位的探针。

5. 发明授权

US06777422B2 Substituted tetrahydroisoquinolines as C5a receptor modulators 失效
标题翻译：取代的四氢异喹啉作为C5a受体调节剂
公开(公告)号：US06777422B2
公开(公告)日：2004-08-17
申请号：US10401135
申请日：2003-03-27
申请人： Kyungae Lee , Scott Mitchell , Robert Ohliger , Lu Yan Zhang , He Zhao , Kevin Currie
发明人： Kyungae Lee , Scott Mitchell , Robert Ohliger , Lu Yan Zhang , He Zhao , Kevin Currie
IPC分类号： C07D21700
CPC分类号： C07D221/20 , A61K31/47 , C07D211/14 , C07D211/70 , C07D217/04 , C07D217/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D417/12 , C07D495/04
摘要： Substituted tetrahydroisoquinolines and related compounds are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了取代的四氢异喹啉和相关化合物。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症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的方法。

6. 发明授权

US06559163B2 2,4-substituted quinoline derivatives 失效
标题翻译： 2,4-取代喹啉衍生物
公开(公告)号：US06559163B2
公开(公告)日：2003-05-06
申请号：US09931549
申请日：2001-08-16
申请人： Guolin Cai , Jun Yuan , Kevin Currie , Pamela Albaugh , Alan Hutchison
发明人： Guolin Cai , Jun Yuan , Kevin Currie , Pamela Albaugh , Alan Hutchison
IPC分类号： A61K314709
CPC分类号： C07D231/12 , C07D215/52 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D409/04
摘要： Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are 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：公开了式或其药学上可接受的盐的化合物，其中：表示：并且A，B，G，D，E，Ra，Rb，W和Z在本文中定义。这些化合物是GABAA脑受体的激动剂，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，睡眠和癫痫发作，过量与苯二氮卓类药物和增强记忆力。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

US06916827B2 Substituted ring-fused imidazole derivative: GABAA receptors ligands 失效
标题翻译：取代的环稠合咪唑衍生物：GABA A受体配体
公开(公告)号：US06916827B2
公开(公告)日：2005-07-12
申请号：US10438496
申请日：2003-05-15
申请人： George D. Maynard , Jun Yuan , George P. Luke , Kevin Currie
发明人： George D. Maynard , Jun Yuan , George P. Luke , Kevin Currie
IPC分类号： A61P25/00 , C07D471/04 , A61K31/437 , A61K31/4184 , A61K31/506 , C07D403/06
CPC分类号： C07D471/04
摘要： Substituted ring-fused 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 for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：提供了与GABA A A受体结合的取代的环稠合咪唑衍生物。这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物和牲畜。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

8. 发明申请

US20050054648A1 Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity 有权
标题翻译：某些8-杂芳基-6-苯基 - 咪唑并[1,2-a]吡嗪作为激酶活性的调节剂
公开(公告)号：US20050054648A1
公开(公告)日：2005-03-10
申请号：US10776002
申请日：2004-02-10
申请人： Scott Mitchell , Kevin Currie , Robert DeSimone , Douglas Pippin
发明人： Scott Mitchell , Kevin Currie , Robert DeSimone , Douglas Pippin
IPC分类号： A61P35/02 , A61P37/00 , C07D487/04 , A61K31/498
CPC分类号： C07D487/04
摘要： This invention pertains to compounds of Formula I: and all pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including of breast neoplasma, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound or salt of the invention to decrease the symptoms or slow the progression of these diseases or disorders. The invention also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an disease or disorder responsive to EphB4 modulation. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent. The invention also includes a method for determining the presence of EphB4 kinase in a sample, comprising contacting the sample with a compound of Formula I, or form thereof, and the detecting the amount of compound or form bound to EphB4 kinase, and therefrom determining the presence or absence of EphB4 kinase in the sample.
摘要翻译：本发明涉及式I化合物及其所有药学上可接受的形式。本文定义了式I中所示的变量R1，R2，R3，Z1，Z2，W和X. 本发明还提供含有一种或多种式I化合物或这些化合物的药学上可接受的形式的药物组合物和一种或多种药学上可接受的载体，赋形剂或稀释剂。本发明还包括治疗患有对EphB4激酶调节有反应的某些疾病和病症的患者的方法，其包括给予这样的患者一定数量的有助于减少疾病或病症的体征或症状的式I化合物。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈鳞状细胞癌。因此，治疗方法包括施用足量的本发明的化合物或盐，以减少症状或减缓这些疾病或病症的进展。本发明还包括治疗其它动物，包括患有对EphB4调节作用的疾病或病症的家畜和驯养的伴侣动物的方法。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。本发明还包括用于测定样品中EphB4激酶存在的方法，包括使样品与式I化合物或其形式接触，并检测与EphB4激酶结合的化合物或形式的量，并从中确定样品中存在或不存在EphB4激酶。

9. 发明申请

US20050054649A1 Certain 8-heteroaryl-6-phenyl-imidazo[1,2-A]pyrazines as modulators of Hsp90 complex activity 有权
标题翻译：某些8-杂芳基-6-苯基 - 咪唑并[1,2-A]吡嗪作为Hsp90复合物活性的调节剂
公开(公告)号：US20050054649A1
公开(公告)日：2005-03-10
申请号：US10776631
申请日：2004-02-10
申请人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
发明人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
IPC分类号： A61P35/02 , A61P37/00 , C07D487/04 , A61K31/498
CPC分类号： C07D487/04
摘要： This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders. The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent. The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.
摘要翻译：本发明涉及式I化合物及其药学上可接受的形式。本文定义了式I中所示的变量R1，R2，R3，Z1，Z2，W和X. 本发明还提供含有一种或多种式I化合物或这些化合物的药学上可接受的形式的药物组合物和一种或多种药学上可接受的载体，赋形剂或稀释剂。本发明还包括治疗患有对Hsp90复合物调节有反应的某些疾病和病症的患者的方法，其包括向所述患者施用一定量的有助于减少疾病或病症的体征或症状的式I化合物。这些疾病包括癌症，包括慢性骨髓性白血病，黑素瘤，乳腺癌，卵巢癌，脑，甲状腺，结肠直肠癌，前列腺癌和膀胱癌，心脏病，中风，自身免疫/炎性疾病和神经变性疾病。因此，治疗方法包括施用足量的式I化合物或其形式以减少症状或减缓这些疾病或病症的进展。本发明还包括治疗患有针对Hsp90复合调节的疾病或病症的非人类患者，包括家畜和驯养伴侣动物的方法。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。本发明还包括用于测定样品中某些激酶或Hsp90复合物的存在的方法，包括使样品与式I化合物或其形式接触并检测样品中的Hsp9O复合物活性。

10. 发明申请

US20060178367A1 Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof 审中-公开
标题翻译：某些咪唑并[1,2-a]吡嗪-8-基胺，制备方法及其使用方法
公开(公告)号：US20060178367A1
公开(公告)日：2006-08-10
申请号：US11270837
申请日：2005-11-10
申请人： Kevin Currie , Jeffrey Kropf , James Darrow , Robert Desimone
发明人： Kevin Currie , Jeffrey Kropf , James Darrow , Robert Desimone
IPC分类号： A61K31/53 , A61K31/498 , C07D487/04 , A61K31/506 , A61K31/501
CPC分类号： C07D487/04
摘要： Chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are described herein. Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell proliferation are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了选自式1化合物的化学实体及其可药用盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。描述了包含至少一种式1的化学实体的药物组合物，以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对抑制Btk活性和/或B细胞增殖有响应的疾病的方法。描述了确定样品中Btk的存在的方法。

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