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61. 发明申请

US20060142324A1 Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 审中-公开
公开(公告)号：US20060142324A1
公开(公告)日：2006-06-29
申请号：US11355439
申请日：2006-02-15
申请人： Jun Yuan , George Maynard , Alan Hutchison
发明人： Jun Yuan , George Maynard , Alan Hutchison
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , C07D495/04
摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

62. 发明授权

US07003512B1 System and method for multiple pass cooperative processing 有权
标题翻译：多通道协同处理系统和方法
公开(公告)号：US07003512B1
公开(公告)日：2006-02-21
申请号：US10912174
申请日：2004-08-06
申请人： Jeffrey A. Bedell , William Hurwood , Benjamin Z. Li , Sadanand Sahasrabudhe , Xinyi Wang , Jun Yuan
发明人： Jeffrey A. Bedell , William Hurwood , Benjamin Z. Li , Sadanand Sahasrabudhe , Xinyi Wang , Jun Yuan
IPC分类号： G06F17/30
CPC分类号： G06F17/30595 , G06F17/30592 , G06Q10/10 , Y10S707/99932 , Y10S707/99933 , Y10S707/99934 , Y10S707/99935
摘要： A system for collaborative processing, comprising a controlling module with access to at least one relational database capable of performing a first set of functions on the data in the database and at least one external analytical engine, the external analytical engine being external to the relational database and being capable of a second set of functions on the data in the database. The controlling module is capable of iteratively processing a multi-step calculation including generating SQL statements to the relational database, passing preliminary results to an external analytical engine and saving data back into the relational database for further processing until the multi-step calculation is performed.
摘要翻译：一种用于协同处理的系统，包括控制模块，该控制模块可访问至少一个能够对数据库中的数据执行第一组功能的关系数据库和至少一个外部分析引擎，所述外部分析引擎在关系数据库外部并且能够对数据库中的数据进行第二组功能。控制模块能够迭代处理多步计算，包括生成SQL语句到关系数据库，将初步结果传递给外部分析引擎，并将数据保存回关系数据库进行进一步处理，直到执行多步计算。

63. 发明申请

US20050261193A1 Antimicrobial theta defensins and methods of using same 审中-公开
标题翻译：抗微生物θ防御素及其使用方法
公开(公告)号：US20050261193A1
公开(公告)日：2005-11-24
申请号：US11126468
申请日：2005-05-10
申请人： Michael Selsted , Yi-Quan Tang , Jun Yuan , Andre Ouellette
发明人： Michael Selsted , Yi-Quan Tang , Jun Yuan , Andre Ouellette
IPC分类号： A61K38/00 , A61K38/10 , A61K38/12 , C07K7/08 , C07K14/47 , C12N15/12 , C12P21/00
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.
摘要翻译：本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5，其中Xaa1至Xaa8是定义其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。例如，本发明提供具有氨基酸序列Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。本发明还涉及特异性结合θ防御素和编码θ防御素的分离的核酸分子的抗体。此外，本发明涉及使用θ防御素或θ防御素类似物以通过使环境与θ防御素接触来在能够维持微生物生长或存活的环境中减少或抑制微生物生长或存活的方法。

64. 发明申请

US20050148601A1 Neurokinin-3 receptor modulators: diaryl imidazole derivatives 审中-公开
标题翻译：神经激肽-3受体调节剂：二芳基咪唑衍生物
公开(公告)号：US20050148601A1
公开(公告)日：2005-07-07
申请号：US11007652
申请日：2004-12-07
申请人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
发明人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
IPC分类号： A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/498 , A61K31/506 , A61K31/538 , C07D233/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/12 , C07D413/02 , C07D413/04 , C07D417/02 , C07D417/04 , C07D43/02
CPC分类号： C07D233/90 , C07D233/64 , C07D405/04
摘要： The invention relates to compounds of general Formula I: wherein the variables are as defined herein. Also provided are pharmaceutical compositions comprising such compounds, and methods for treating patients suffering from a disorder responsive to neurokinin-3 receptor modulation. NK-3 receptor modulators provided herein are also useful as probes for the localization of NK-3 receptors.
摘要翻译：本发明涉及通式I的化合物：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，以及用于治疗患有对神经激肽-3受体调节有响应的病症的患者的方法。本文提供的NK-3受体调节剂也可用作NK-3受体定位的探针。

65. 发明授权

US06828329B2 Aryl fused substituted 4-oxy-pyridines 失效
标题翻译：芳基稠合取代的4-氧 - 吡啶
公开(公告)号：US06828329B2
公开(公告)日：2004-12-07
申请号：US09892024
申请日：2001-06-26
申请人： Guolin Cai , Pamela Albaugh , Jun Yuan
发明人： Guolin Cai , Pamela Albaugh , Jun Yuan
IPC分类号： A61K3144
CPC分类号： C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04
摘要： Disclosed are compounds of the formula: wherein X, Q, W and are as 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：公开了下式的化合物：其中X，Q，W和如本文所定义。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。

66. 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。

67. 发明授权

US06511987B1 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US06511987B1
公开(公告)日：2003-01-28
申请号：US09709887
申请日：2000-11-10
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
IPC分类号： C07D47104
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合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）疾病和作为组织样品中GABA A受体定位的探针。还公开了可用于制备这些化合物的中间体。

68. 发明授权

US06440969B2 Certain isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands 失效
标题翻译：某些异喹啉胺和酞嗪胺衍生物：促肾上腺皮质激素释放因子受体CRF1特异性配体
公开(公告)号：US06440969B2
公开(公告)日：2002-08-27
申请号：US09852991
申请日：2001-05-10
申请人： Jun Yuan , Taeyoung Yoon
发明人： Jun Yuan , Taeyoung Yoon
IPC分类号： C07D23730
CPC分类号： C07D401/12 , C07D217/22 , C07D237/34
摘要： Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that 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. The compounds have the formula or the pharmaceutically acceptable salts thereof wherein Ar, R1, R2, R3, R4 and W are various organic and inorganic substituents.
摘要翻译：公开了在人CRF1受体上是高选择性部分激动剂或拮抗剂的化合物，其可用于治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁症，头痛和焦虑症的诊断和治疗。所述化合物具有其药学上可接受的盐，其中Ar，R 1，R 2，R 3，R 4和W是各种有机和无机取代基。

69. 发明授权

US06281359B1 Aminomethyl phenyl pyridine derivatives 失效
标题翻译：氨基甲基苯基吡啶衍生物
公开(公告)号：US06281359B1
公开(公告)日：2001-08-28
申请号：US08457409
申请日：1995-06-01
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D40106
CPC分类号： C07D239/42 , C07C211/27 , C07D211/14 , C07D211/70 , C07D295/096 , C07D401/06
摘要： Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R 1 X，Y，Z和T是有机或无机取代基; 且R 2和R 3表示氢或有机取代基; 或NRR2R3一起表示杂环系统;及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此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。

70. 发明授权

US06239179B1 N-aminoalkyl-2-anthracenecarboxamides; new dopamine receptor subtype specific ligands 失效
标题翻译： N-氨基烷基-2-蒽基甲酰胺; 新的多巴胺受体亚型特异性配体
公开(公告)号：US06239179B1
公开(公告)日：2001-05-29
申请号：US09497989
申请日：2000-02-04
申请人： Jun Yuan , Xi Chen
发明人： Jun Yuan , Xi Chen
IPC分类号： A61K31166
CPC分类号： C07D295/13 , C07C2603/24 , C07D211/14 , C07D211/70
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and R9 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4, R5, R6, R7, R8 and R9 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R10 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group; which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
摘要翻译：公开了下式的化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6，R7，R8和R9相同或不同，代表氢，C1-C6烷基，卤素，羟基，氨基，氰基，硝基，三氟甲基，三氟甲氧基，C 1 -C 6烷氧基，-O 2 CR'， - NHCOR'，-COR'，-SO m R'，其中R'是C 1 -C 6烷基，其中m是0,1或 2; 或R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R10 是氢或C 1 -C 6烷基; R代表氨基烷基;这些化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默氏病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的药物滥用和强迫症。此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

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