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61. 发明申请

WO2007002433A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007002433A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024524
申请日：2006-06-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
发明人： IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
IPC分类号： C07D471/04 , A61K31/435 , C07C49/517 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. (Formula III).
摘要翻译：描述了对蛋白激酶有活性的式III化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。（式III）。

62. 发明申请

WO2006130426A2 MODULATORS OF CCR-5 ACTIVITY 审中-公开
标题翻译： CCR-5活性调节剂
公开(公告)号：WO2006130426A2
公开(公告)日：2006-12-07
申请号：PCT/US2006/020255
申请日：2006-05-25
申请人： KEMIA, INC. , BOMAN, Erik , DAHL, Russell , DELAET, Nancy, G. J. , ERNST, Justin , LUM, Christopher , SEBO, Lubomir , URBAN, Jan
发明人： BOMAN, Erik , DAHL, Russell , DELAET, Nancy, G. J. , ERNST, Justin , LUM, Christopher , SEBO, Lubomir , URBAN, Jan
CPC分类号： C07D295/32 , C07D249/08 , C07D451/02 , C07D451/04 , C07D487/08
摘要： The present invention relates to low molecular weight compounds, including compounds of Formulas I and II as defined herein, and pharmaceutical compositions thereof, useful as modulators of CCR- 5 activity. The invention further relates to the use of such compounds and compositions in treating disorders mediated by CCR-5 such as viral infections and inflammatory diseases.
摘要翻译：本发明涉及低分子化合物，包括本文定义的式I和II的化合物及其药物组合物，其可用作CCR-5活性的调节剂。本发明还涉及这些化合物和组合物在治疗由CCR-5介导的病症如病毒感染和炎性疾病中的用途。

63. 发明申请

WO2006078228A1 METHODS FOR THE DESIGN OF MOLECULAR SCAFFOLDS AND LIGANDS 审中-公开
标题翻译：分子标记和配体设计方法
公开(公告)号：WO2006078228A1
公开(公告)日：2006-07-27
申请号：PCT/US2003/006477
申请日：2003-03-03
申请人： PLEXXIKON, INC. , HIRTH, Klaus-Peter , MILBURN, Michael, V.
发明人： HIRTH, Klaus-Peter , MILBURN, Michael, V.
IPC分类号： C12Q1/00
CPC分类号： G06F19/16 , G01N33/6803 , G06F19/18 , G06F19/706
摘要： The present invention provides methods of designing ligands that specifically bind to target molecules by testing a set of distinct compounds to identify compound that bind to member of a molecular family of interest. Those compounds that show binding activity can be used as a starting point for ligand design. Unlike previous methods, even compounds that bind with only low affinity are of interest and can be used. Common chemical structures of binding molecules including low affinity binding molecules are identified, thereby providing molecular scaffolds. Co-crystals of the protein and the molecular scaffolds can be formed and analyzed by X-ray crystallography to determine the orientation of the scaffold compounds at the binding site of the molecule. Using the orientation information on a scaffold at the binding site of the molecule, chemically tractable structures of the scaffold are identified that are modified to provide ligands that bind to the target molecule with altered binding affinity or specificity to a target molecule or to members of a molecular family. New and useful ligands can therefore be designed in a rational manner and with a minimum investment of resources using the methods provided.
摘要翻译：本发明提供了通过测试一组不同的化合物来鉴定与感兴趣的分子家族成员结合的化合物来设计与靶分子特异性结合的配体的方法。那些显示结合活性的化合物可以用作配体设计的起点。与以前的方法不同，甚至仅以低亲和力结合的化合物是有意义的并且可以使用。鉴定包括低亲和力结合分子的结合分子的常见化学结构，从而提供分子支架。通过X射线晶体学可以形成和分析蛋白质和分子支架的共晶体，以确定支架化合物在分子结合位点的取向。使用分子的结合位点上的支架上的取向信息，鉴定出支架的化学易溶解结构，其被修饰以提供结合靶分子的配体，其具有改变的对靶分子的结合亲和力或特异性分子家族。因此，新的和有用的配体可以以合理的方式设计，并且使用所提供的方法以最小的资源投入。

64. 发明申请

WO2006060021A2 BIFUNCTIONAL FUSION PROTEINS CONTAINING THE FLT3 LIGAND 审中-公开
标题翻译：含FLT3 LIGAND的双功能融合蛋白
公开(公告)号：WO2006060021A2
公开(公告)日：2006-06-08
申请号：PCT/US2004/040912
申请日：2004-12-06
申请人： ONCOMAX ACQUISITION CORP. , MA, Jing , GUO, Yanjun
发明人： MA, Jing , GUO, Yanjun
IPC分类号： A61K39/00 , C07K14/82
CPC分类号： C07K16/2809 , C07K14/4747 , C07K14/475 , C07K16/2863 , C07K16/2896 , C07K16/30 , C07K16/32 , C07K2317/24 , C07K2317/31 , C07K2317/34 , C07K2317/52 , C07K2317/53 , C07K2317/622 , C07K2317/626 , C07K2317/73 , C07K2319/00 , C07K2319/01 , C07K2319/33
摘要： Provided herein is a chimeric protein, which chimeric protein comprises a Flt3 ligand, or a biologically active fragment thereof, and a proteinaceous or peptidyl tumoricidal agent, or a targeting agent which binds to a receptor expressed on a tumor, and uses thereof, particularly in the treatment of malignancy. Other embodiments and uses are disclosed.
摘要翻译：本文提供了一种嵌合蛋白，其嵌合蛋白包含Flt3配体或其生物活性片段，以及与肿瘤上表达的受体结合的蛋白质或肽基杀肿剂或靶向剂及其用途，特别是在治疗恶性肿瘤。公开了其它实施例和用途。

65. 发明申请

WO2006017292A1 CONSTRAINED CYANO COMPOUNDS 审中-公开
标题翻译：约束氰化合物
公开(公告)号：WO2006017292A1
公开(公告)日：2006-02-16
申请号：PCT/US2005/024695
申请日：2005-07-12
申请人： PHENOMIX CORPORATION , CAMPBELL, David, Alan , BETANCORT, Juan, M. , WINN, David
发明人： CAMPBELL, David, Alan , BETANCORT, Juan, M. , WINN, David
IPC分类号： A61K31/40
CPC分类号： C07D513/04
摘要： Certain constrained cyano compounds are useful as inhibitors of post-proline/alanine cleaving amino-dipeptidases. Accordingly, these compounds can be employed, , alone or with another therapeutic agent, to treat diabetes (especially, Type II diabetes), hyperglycemia, Syndrome X, diabetic complications, hyperinsulinemia, obesity, atherosclerosis and related diseases, as well as various immunomodulatory diseases and chronic inflammatory bowel disease.
摘要翻译：某些受限的氰基化合物可用作后脯氨酸/丙氨酸切割氨基二肽酶的抑制剂。因此，这些化合物可单独或与其它治疗剂一起用于治疗糖尿病（特别是II型糖尿病），高血糖症，综合征X，糖尿病并发症，高胰岛素血症，肥胖，动脉粥样硬化及相关疾病以及各种免疫调节疾病和慢性炎性肠病。

66. 发明申请

WO2006017257A2 AZETIDINONE DERIVATIVES 审中-公开
标题翻译： AZETIDINONE衍生物
公开(公告)号：WO2006017257A2
公开(公告)日：2006-02-16
申请号：PCT/US2005/024624
申请日：2005-07-11
申请人： PHENOMIX CORPORATION , CAMPBELL, David, A. , BETANCORT, Juan , KARANEWSKY, Donald, S.
发明人： CAMPBELL, David, A. , BETANCORT, Juan , KARANEWSKY, Donald, S.
CPC分类号： C07D405/04 , C07D403/04 , C07D417/04
摘要： Novel azetidinone-containing compounds are useful in the treatment or prevention of various human diseases. For example, they can be employed in lowering plasma levels of a sterol, such as cholesterol. Thus, these compounds can be administered in the contexts of methods for treating and/or preventing diabetes, obesity, and atherosclerosis, respectively.
摘要翻译：新的含氮杂环丁酮的化合物可用于治疗或预防各种人类疾病。例如，它们可以用于降低诸如胆固醇的固醇的血浆水平。因此，这些化合物可以分别在用于治疗和/或预防糖尿病，肥胖和动脉粥样硬化的方法的情况下给药。

67. 发明申请

WO2005113834A3 SINGLE LABEL COMPARATIVE HYBRIDIZATION 审中-公开
公开(公告)号：WO2005113834A3
公开(公告)日：2005-12-01
申请号：PCT/US2005/017986
申请日：2005-05-19
申请人： QUEST DIAGNOSTICS INVESTMENTS INCORPORATED , MOHAMMED, Mansoor, S. , DZIDIC, Natasa , MCCASKILL, Christopher , KIM, Jaeweon
发明人： MOHAMMED, Mansoor, S. , DZIDIC, Natasa , MCCASKILL, Christopher , KIM, Jaeweon
IPC分类号： C12Q1/68
摘要： The present invention provides methods of detecting and mapping chromosomal or genetic abnormalities associated with various diseases or with predisposition to various diseases, or to detecting the phenomena of large scale copy number variants. In particular, the present invention provides advanced methods of performing array-based comparative hybridization that allow reproducibility between samples and enhanced sensitivity by using the same detectable label for both test sample and reference sample nucleic acids. Invention methods are useful for the detection or diagnosis of particular disease conditions such as cancer, and detecting predisposition to cancer based on detection of chromosomal or genetic abnormalities and gene expression level. Invention methods are also useful for the detection or diagnosis of hereditary genetic disorders or predisposition thereto, especially in prenatal samples. Moreover, invention methods are also useful for the detection or diagnosis of de novo genetic aberrations associated with post-natal developmental abnormalities.

68. 发明申请

WO2004033397A3 ACTIVITY-BASED PROBES, AND METHODS OF THEIR PREPARATION AND USE 审中-公开
公开(公告)号：WO2004033397A3
公开(公告)日：2004-04-22
申请号：PCT/US2003/032152
申请日：2003-10-08
申请人： ACTIVX BIOSCIENCES, INC. , WINN, David , CAMPBELL, David, Alan
发明人： WINN, David , CAMPBELL, David, Alan
IPC分类号： C07K1/00
摘要： The present invention provides compositions and methods for assessing profiles of catalytically active enzymes in compositions containing a plurality of proteins. In preferred embodiments, the enzyme is a hydrolase, most preferably a cysteine protease. The methods described herein use activity based probes ("ABPs") that have an affinity moiety for directing the binding of the ABP to one or more catalytically active target enzymes, a reactive group for forming a covalent bond at an active site of the target enzyme(s), and a TAG (e.g., a detectable label, preferably a fluorophore). One or more ABPs may be combined with a protein-containing sample under conditions for binding and reaction of the ABP(s) with target enzyme(s) that are present in the sample. The resulting products may then be used to assess the active enzyme profile of the sample, and can be correlated to the presence, amount, or activity of one or more target enzyme(s) present in the original complex protein mixture.

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