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91. 发明授权

US07317032B2 Imidazolyl inhibitors of 15-lipoxygenase 有权
标题翻译： 15-脂氧合酶的咪唑基抑制剂
公开(公告)号：US07317032B2
公开(公告)日：2008-01-08
申请号：US10932594
申请日：2004-09-01
申请人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
发明人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C04B35/632 , C07D233/64 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/10 , C07D487/08
摘要： The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本发明提供15-LO的咪唑基抑制剂，含有这种抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。

92. 发明授权

US07317024B2 Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的杂环调节剂及其用途
公开(公告)号：US07317024B2
公开(公告)日：2008-01-08
申请号：US11330511
申请日：2006-01-12
申请人： Bingwei V. Yang
发明人： Bingwei V. Yang
IPC分类号： A61K31/47 , A61K31/445 , A61K31/426 , A61K31/415 , A61K31/4168 , A61K31/4196 , A61K31/421 , C07D215/02 , C07D277/20 , C07D263/30 , C07D249/08 , C07D231/10 , C07D233/54
CPC分类号： C07D277/56 , A61K31/135 , C07D233/88 , C07D277/46 , C07D417/10 , A61K2300/00
摘要： The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：本发明涉及一类新型非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性调节有关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）的结构或其立体异构体或前药或溶剂合物或其药学上可接受的盐，其中Z，R，R 4，R 5，R a，本文定义的，其中R b，R b，R c和R d都在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

93. 发明授权

US07262289B2 KCNQ potassium channels and methods of modulating same 有权
标题翻译： KCNQ钾通道及其调节方法
公开(公告)号：US07262289B2
公开(公告)日：2007-08-28
申请号：US10131685
申请日：2002-04-24
申请人： Michael A. Blanar , Wen-Pin Yang , Paul C. Levesque , Michael G. Neubauer , Wayne A. Little
发明人： Michael A. Blanar , Wen-Pin Yang , Paul C. Levesque , Michael G. Neubauer , Wayne A. Little
IPC分类号： C12N14/705
CPC分类号： C07K14/705 , A61K48/00
摘要： The present invention relates to KCNQ proteins defining potassium channels. In particular, the invention concerns the human KCNQ2, human KCNQ3, murine KCNQ2, and rat KCNQ2 proteins reported herein. KCNQ2 and KCNQ3 proteins are nervous system-selective and may be involved in neurotransmission and neuroprotection. The KCNQ2 and KCNQ3 of the present invention can be used to assay for modulators of the proteins, which would be useful in treatment of such disorders as ataxia, myokymia, seizures, Alzheimer's disease, Parkinson's disease, age-associated memory loss, learning deficiencies, motor neuron diseases, epilepsy, stroke, and the like.
摘要翻译：本发明涉及定义钾通道的KCNQ蛋白。特别地，本发明涉及本文报道的人KCNQ2，人类KCNQ3，鼠KCNQ2和大鼠KCNQ2蛋白。 KCNQ2和KCNQ3蛋白是神经系统选择性的，可能参与神经传递和神经保护。本发明的KCNQ2和KCNQ3可用于测定蛋白质的调节剂，其可用于治疗诸如共济失调，myokymia，癫痫发作，阿尔茨海默氏病，帕金森病，年龄相关记忆丧失，学习缺陷，运动神经元疾病，癫痫，中风等。

94. 发明授权

US07211593B2 C12-cyano epothilone derivatives 有权
标题翻译： C12-氰基埃坡霉素衍生物
公开(公告)号：US07211593B2
公开(公告)日：2007-05-01
申请号：US10386059
申请日：2003-03-11
申请人： Gregory D. Vite , Alicia Regueiro-Ren
发明人： Gregory D. Vite , Alicia Regueiro-Ren
IPC分类号： A61K31/427 , C07D277/30
CPC分类号： C07D417/06 , C07D493/04
摘要： The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula wherein: R1, R2, R3, R4, R5 are hydrogen or lower alkyl; R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; X is hydrogen and Y is hydroxy, or X and Y taken together represent a carbon-carbon bond; and pharmaceutically acceptable salts, solvates, or hydrates thereof. Also included are therapeutic compositions containing the compounds represented by formula I as active ingredients, alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.
摘要翻译：本发明涉及可用于治疗由下式表示的癌症或其它增殖性疾病的化合物：其中：R 1，R 2，R 3， >，R 4，R 5是氢或低级烷基; R 6选自氢，烷基，取代的烷基，芳基，取代的芳基，环烷基或杂环; X是氢，Y是羟基，X或Y一起代表碳 - 碳键; 及其药学上可接受的盐，溶剂化物或水合物。还包括含有式I表示的化合物作为活性成分的治疗组合物，单独或与用于治疗癌症或其它增殖性疾病的其它治疗剂组合。

95. 发明授权

US07145040B2 Process for the preparation of amino acids useful in the preparation of peptide receptor modulators 有权
标题翻译：用于制备可用于制备肽受体调节剂的氨基酸的方法
公开(公告)号：US07145040B2
公开(公告)日：2006-12-05
申请号：US11172488
申请日：2005-06-30
申请人： Arvind Mathur , K. Selva Kumar
发明人： Arvind Mathur , K. Selva Kumar
IPC分类号： C07F5/02 , C07C229/00
CPC分类号： C07C227/20 , C07C229/36 , C07C271/22 , C07F5/025
摘要： The present invention provides process useful for the preparation of intermediates which are useful in the preparation of amino acids useful in preparing peptide receptor modulators, for example agonists or partial agonists of such peptide receptors. Such peptide receptor modulators include, for example glucagon like peptide-1 receptor modulators which are useful for the amelioration of the diabetic condition.
摘要翻译：本发明提供了可用于制备可用于制备可用于制备肽受体调节剂的氨基酸的中间体的方法，例如这种肽受体的激动剂或部分激动剂。这样的肽受体调节剂包括例如可用于改善糖尿病状况的胰高血糖素样肽-1受体调节剂。

96. 再颁专利

USRE39251E1 Polymorphs of an epothilone analog 有权
公开(公告)号：USRE39251E1
公开(公告)日：2006-08-29
申请号：US11076589
申请日：2005-03-09
申请人： Zhenrong Guo
发明人： Zhenrong Guo
IPC分类号： C07D493/04 , A61K31/42 , A61P35/00
CPC分类号： C07D491/04 , C07D417/06
摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

97. 发明授权

US07087614B2 Pyrimidine inhibitors of phosphodiesterase (PDE) 7 有权
标题翻译：磷酸二酯酶抑制剂（PDE）7
公开(公告)号：US07087614B2
公开(公告)日：2006-08-08
申请号：US10173442
申请日：2002-06-17
申请人： Junqing Guo , Joseph Barbosa , William John Pitts , Marianne Carlsen , Claude Quesnelle , Marco Dodier
发明人： Junqing Guo , Joseph Barbosa , William John Pitts , Marianne Carlsen , Claude Quesnelle , Marco Dodier
IPC分类号： A61K31/513 , A61K31/506 , A61K31/505 , C07D43/02 , C07D277/42
CPC分类号： C07D417/14 , A61K31/00 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/522 , C07D403/12 , C07D417/12 , C07D471/04 , C07D473/00 , C07D473/16 , C07D487/04 , C07D491/10
摘要： Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, Z, J and L are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.
摘要翻译：其中R 1，R 2，Z，J和L的嘧啶磷酸二酯酶7（PDE 7）抑制剂其中R 1，R 2，Z，J和L如本文所述，并且提供其类似物是有用的在治疗T细胞介导的疾病。

98. 发明授权

US07053111B2 Inhibitors of IMPDH enzyme 有权
公开(公告)号：US07053111B2
公开(公告)日：2006-05-30
申请号：US10465425
申请日：2003-06-19
申请人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
发明人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
IPC分类号： A61K31/421 , A61K31/422 , C07D263/32 , C07D413/12
CPC分类号： C07D413/12 , C07D263/32 , C07D307/20 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

99. 发明授权

US07022849B2 Quinazoline and pyrido[2,3-d]pyrimidine inhibitors of phosphodiesterase (PDE) 7 有权
公开(公告)号：US07022849B2
公开(公告)日：2006-04-04
申请号：US10173322
申请日：2002-06-17
申请人： William J. Pitts , Joseph Barbosa
发明人： William J. Pitts , Joseph Barbosa
IPC分类号： C07D237/02 , A01N43/58 , A61K31/50
CPC分类号： C07D403/12 , A61K31/00 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/522 , C07D401/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/16 , C07D487/04 , C07D491/10
摘要： Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.

100. 发明授权

US06968037B2 High throughput X-ray diffraction filter sample holder 失效
$High throughput X-ray diffraction filter sample holder$
标题翻译：高通量X射线衍射滤光片样品架
公开(公告)号：US06968037B2
公开(公告)日：2005-11-22
申请号：US10410910
申请日：2003-04-10
申请人： Victor W. Rosso , Glen Young , Joseph Nolfo , Imre M. Vit z , John J. Venit
发明人： Victor W. Rosso , Glen Young , Joseph Nolfo , Imre M. Vit z , John J. Venit
IPC分类号： B01L3/00 , G01N1/28 , G01N23/20
CPC分类号： G01N1/4077 , B01L3/50255 , B01L2200/026 , B01L2300/0829 , B01L2400/049 , G01N23/20 , G01N23/20025
摘要： Multiple samples are prepared in slurry form and deposited through a funnel plate by a multiprobe liquid handler into an array of inserts situated in openings in a housing. Each insert has a recess that extends through the insert body and a filter disc situated in the recess to support the sample. The filter is held in place by an annular part which defines a channel providing access to the filter through the lower portion of the recess. A pressure differential is created across each of the filters by attaching a vacuum manifold to the bottom of the housing to simultaneously remove the liquid from each of the samples, leaving the samples in powder form. The housing is then placed in the X-ray diffractometer for sequential analysis of each of the samples, while the samples are situated in the inserts.
摘要翻译：多个样品以浆料形式制备并通过漏斗板通过多孔液体处理器沉积到位于壳体中的开口中的插入物阵列中。每个插入件具有延伸穿过插入体的凹部和位于凹部中以支撑样品的过滤盘。过滤器通过环形部分保持在适当位置，该环形部分限定了通过凹部的下部进入过滤器的通道。通过将真空歧管连接到壳体的底部，同时从每个样品中移除液体，使样品成粉末形式，在每个过滤器上形成压差。然后将壳体放置在X射线衍射仪中，以顺序分析每个样品，而样品位于插入物中。

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