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1. 发明申请

WO2004070653A3 IMAGE ANALYSIS SYSTEM AND METHOD 审中-公开
标题翻译：图像分析系统与方法
公开(公告)号：WO2004070653A3
公开(公告)日：2005-01-06
申请号：PCT/US2004002633
申请日：2004-01-30
申请人： DISCOVERY PARTNERS INTERNAT , AFFLECK RHETT L , LEVIN ROBERT K , LILLIG JOHN E , NEEPER ROBERT K , EWING WILLIAM R , DESIENO DUANE , HANSEN ERIC , BODNAR MIKE
发明人： AFFLECK RHETT L , LEVIN ROBERT K , LILLIG JOHN E , NEEPER ROBERT K , EWING WILLIAM R , DESIENO DUANE , HANSEN ERIC , BODNAR MIKE
IPC分类号： A47B88/48 , B01L9/00 , C30B7/00 , C30B29/58 , G01N1/40 , G01N15/14 , G01N21/25 , G01N35/00 , G01N35/02 , G01N35/04 , G02B21/00 , G06K9/00 , A61B5/00
CPC分类号： C30B29/58 , B01L9/523 , C30B7/00 , G01N15/1475 , G01N21/253 , G01N35/0099 , G01N35/028 , G01N2001/4027 , G01N2015/1493 , G01N2035/00356 , G01N2035/00455 , G01N2035/00881 , G01N2035/042 , G01N2035/0425 , G01N2035/0463 , G02B21/0016
摘要： An image analysis system (200) and related methods for automation of the monitoring of samples to determine crystal growth. Samples are imaged from time to time using a set of imaging parameters. The resulting images are evaluated to determine the contents of the samples. If the evaluation of the image indicates the presence of crystals, the sample may be re-imaged using a different set of imaging parameters, and the resulting image analyzed to determine its contents. The sample may also be evaluated by generating multiple images of a sample using various sets of imaging parameters, identifying pixels that depict regions of interest in a plurality of images, merging the pixels from each region of interest into a composite image and analyzing the composite image. An image of a sample can also be evaluated by classifying the pixels of the image based on the contents of the sample that they depict, color-coding the pixels using the classifications, and displaying the colored image for analysis.
摘要翻译：一种图像分析系统（200）及相关方法，用于监测样品的自动化，以确定晶体生长。使用一组成像参数不时地对样本进行成像。评估所得图像以确定样品的内容。如果图像的评估表明晶体的存在，则可以使用不同的成像参数集来重新成像样品，并且分析所得到的图像以确定其内容。也可以通过使用各种成像参数集合生成样本的多个图像来评估样本，识别在多个图像中描绘感兴趣区域的像素，将来自每个感兴趣区域的像素合并到合成图像中并分析合成图像。样本的图像也可以通过基于它们描绘的样本的内容，使用分类对像素进行颜色编码，并显示彩色图像进行分析来对图像的像素进行分类来评估。

2. 发明申请

WO2004092903A3 SPOT FINDING ALGORITHM USING IMAGE RECOGNITION SOFTWARE 审中-公开
标题翻译：使用图像识别软件的点搜索算法
公开(公告)号：WO2004092903A3
公开(公告)日：2005-09-15
申请号：PCT/US2004011282
申请日：2004-04-08
申请人： DISCOVERY PARTNERS INTERNAT , EWING WILLIAM R , DESIENO DUANE , AFFLECK RHETT L
发明人： EWING WILLIAM R , DESIENO DUANE , AFFLECK RHETT L
IPC分类号： G01N31/00 , G06F20060101 , G06K9/00 , G06T7/00
CPC分类号： G06T7/75 , G06T2207/30004
摘要： A plurality of samples are tested for their ability to enhance or inhibit a biological process in a multiplexed diffusive assay. The assay is imaged after the biological process has produced spots in a medium that indicate the tested enhancing or inhibiting ability of the samples. The image containing the resulting spots are evaluated to determine which samples caused the spots to form. The location of spots are identified by user selection or through a gradient triangulation technique that determines spot locations by analyzing the slope of pixel intensities in numerous subimages. The spots may also be analyzed by parametrically modeling the spots and comparing the spot characteristics in the image to a spot function, to determine the location of hit spots in the image. The hit spot locations, corresponding to the location of tested samples in the assay that enhanced or inhibited the biological process, are output to facilitate further analysis of the test samples.
摘要翻译：测试多个样品在多重扩散测定中增强或抑制生物过程的能力。在生物学过程在培养基中产生指示样品的增强或抑制能力的斑点之后，测定成像。评估含有所得斑点的图像，以确定哪些样品导致斑点形成。斑点的位置通过用户选择或通过梯度三角测量技术来识别，其通过分析许多子图像中像素强度的斜率来确定点位置。也可以通过对斑点进行参数建模和将图像中的斑点特征与斑点函数进行比较来分析斑点，以确定图像中命中点的位置。输出对应于增强或抑制生物过程的测定中测试样品的位置的命中点位置，以便于进一步分析测试样品。

3. 发明申请

WO2004015393A3 SPOTTING PATTERN FOR PLACEMENT OF COMPOUNDS IN AN ARRAY 审中-公开
标题翻译：在阵列中放置化合物的喷射模式
公开(公告)号：WO2004015393A3
公开(公告)日：2004-11-11
申请号：PCT/US0325047
申请日：2003-08-08
申请人： DISCOVERY PARTNERS INTERNAT
发明人： EWING WILLIAM R , NEEPER ROBERT K , AFFLECK RHETT L , LILLIG JOHN E
IPC分类号： B01J33/00 , G01N20060101 , G01N15/06 , G01N21/00 , G01N31/22 , G01N33/00 , G01N33/48 , G01N33/53 , G01N33/543 , G01N35/00
CPC分类号： G01N33/543
摘要： A plurality of samples of different substances are tested for their ability to enhance or inhibit a biological process. The samples are deposited on a supporting surface, such as a ChemCard 110, in an array comprising at least two dots 130 of each sample, wherein at least one of the dots 130 of each sample is at least a predetermined distance from at least one of the dots 130 of each of the plurality of samples. One or more assay reagents in a gel sheet 120, for example, are then brought in contact with the compounds and reactions with certain of the compounds are evident as the active compounds diffuse into the one or more assay reagents. The concept of having unique neighbors for each occurrence of a dot 130 allows the definitive correlation of active compounds with the dot 130 (and the compound) that caused the biological activity.
摘要翻译：测试多种不同物质的样品增强或抑制生物过程的能力。样品以包含每个样品的至少两个点130的阵列的方式沉积在支撑表面（例如ChemCard 110）上，其中每个样品的至少一个点130距离至少一个多个样本中的每一个的点130。然后使例如凝胶片120中的一种或多种测定试剂与化合物接触，并且随着活性化合物扩散到一种或多种测定试剂中，某些化合物的反应是明显的。针对点130的每次出现具有唯一邻居的概念允许活性化合物与导致生物活性的点130（和化合物）的明确关联。

4. 发明申请

WO2004021984A3 HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
标题翻译：杂环芳族化合物可用作生长激素的秘密
公开(公告)号：WO2004021984A3
公开(公告)日：2004-11-25
申请号：PCT/US0327513
申请日：2003-09-02
申请人： SQUIBB BRISTOL MYERS CO , YU GUIXUE , LI JUN , EWING WILLIAM R , SULSKY RICHARD B , LI JAMES J , TINO JOSEPH A
发明人： YU GUIXUE , LI JUN , EWING WILLIAM R , SULSKY RICHARD B , LI JAMES J , TINO JOSEPH A
IPC分类号： A61K31/4025 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/00 , C07D231/56 , C07D261/20 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula (I) wherein R1, R1', R2, R3, R4, Xa, Y, Z, and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
摘要翻译：提供了可用于刺激生长激素的内源性产生或释放的新型杂环芳族化合物，所述具有式（I）的通式结构的化合物其中R1，R1'，R2，R3，R4，Xa，Y，Z和n 如本文所述。本文提供的化合物可用于治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量。

5. 发明申请

WO2006014287A8 HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开
标题翻译：人类GLUCAGON-PEPTIDE-1调节剂及其在治疗糖尿病及相关病症中的应用
公开(公告)号：WO2006014287A8
公开(公告)日：2006-05-26
申请号：PCT/US2005023076
申请日：2005-06-30
申请人： SQUIBB BRISTOL MYERS CO , EWING WILLIAM R , MAPELLI CLAUDIO , SULSKY RICHARD B , HAQUE TASIR S , LEE VING G , RIEXINGER DOUGLAS JAMES , MARTINEZ ROGELIO L , ZHU YEHENG
发明人： EWING WILLIAM R , MAPELLI CLAUDIO , SULSKY RICHARD B , HAQUE TASIR S , LEE VING G , RIEXINGER DOUGLAS JAMES , MARTINEZ ROGELIO L , ZHU YEHENG
IPC分类号： C07K14/605
CPC分类号： C07K7/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。本发明的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

6. 发明申请

WO2008076810A3 AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的偶氮异构体
公开(公告)号：WO2008076810A3
公开(公告)日：2008-08-14
申请号：PCT/US2007087404
申请日：2007-12-13
申请人： SQUIBB BRISTOL MYERS CO , EWING WILLIAM R , ZHU YEHENG , SULSKY RICHARD B
发明人： EWING WILLIAM R , ZHU YEHENG , SULSKY RICHARD B
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/04 , A61P25/04
CPC分类号： C07D487/04
摘要： The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) or (Ia), both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula (Ia), including all prodrugs, pharmaceutically acceptable salts and stereoisomer, thereof, wherein R 1 , R 2 , Ar 1 , Ar 2 are defined herein.
摘要翻译：本申请描述了根据式（I）和（Ia）的CB-1反向激动剂，包含至少一种根据式（I）或（Ia）的化合物的药物组合物，以及任选的一种或多种另外的治疗剂和治疗方法使用根据式（I）或（Ia）的化合物单独和与一种或多种另外的治疗剂组合。优选的化合物具有通式（Ia），包括其所有前药，药学上可接受的盐和立体异构体，其中R 1，R 2，Ar 1， / SUB>，这里定义为Ar 2。

7. 发明申请

WO2008076810A2 AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的偶氮异构体
公开(公告)号：WO2008076810A2
公开(公告)日：2008-06-26
申请号：PCT/US2007087404
申请日：2007-12-13
申请人： SQUIBB BRISTOL MYERS CO , EWING WILLIAM R , ZHU YEHENG , SULSKY RICHARD B
发明人： EWING WILLIAM R , ZHU YEHENG , SULSKY RICHARD B
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/04 , A61P25/04
CPC分类号： C07D487/04
摘要： The present application describes compounds according to Formula I and Ia, pharmaceutical compositions comprising at least one compound according to Formula I or Ia, and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I or Ia, both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula Ia below; including all prodrugs, pharmaceutically acceptable salts and stereoisomers thereof, wherein R 1 , R 2 , Ar 1 , Ar 2 are defined herein.
摘要翻译：本申请描述了根据式I和Ia的化合物，包含至少一种根据式I或Ia的化合物的药物组合物，以及任选的一种或多种另外的治疗剂和使用根据式I或Ia的化合物单独治疗的方法并与一种或多种另外的治疗剂组合。优选的化合物具有以下通式Ia; 包括其所有前药，药学上可接受的盐和立体异构体，其中R 1，R 2，Ar 1，Ar 2， >在本文中定义。

8. 发明申请

WO2006044359A3 HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
标题翻译：杂环芳族化合物可用作生长激素的秘密
公开(公告)号：WO2006044359A3
公开(公告)日：2006-06-22
申请号：PCT/US2005036495
申请日：2005-10-12
申请人： SQUIBB BRISTOL MYERS CO , EWING WILLIAM R , LI JUN , SULSKY RICHARD B , HERNANDEZ ANDRES S
发明人： EWING WILLIAM R , LI JUN , SULSKY RICHARD B , HERNANDEZ ANDRES S
IPC分类号： A61K31/415 , C07D231/12
CPC分类号： C07D231/12 , C07D231/20 , C07D249/08 , C07D261/04 , C07D261/08 , C07D271/10 , C07D271/107 , C07D403/12 , C07D413/12
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R 1 , R la , R 6 , X a , X b and Y are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
摘要翻译：提供了新颖的杂环芳族化合物，其可用于刺激生长激素的内源性产生或释放，所述具有通式结构的化合物其中R 1，R 2，其中，X 1，X 2，X 2和X 2如本文所述。本文提供的化合物可用于治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量。

9. 发明申请

WO2006044362A2 N-SULFONYLPIPERIDINE CANNABINOID RECEPTOR 1 ANTAGONISTS 审中-公开
标题翻译： N-磺酰胆碱卡那霉素受体1拮抗剂
公开(公告)号：WO2006044362A2
公开(公告)日：2006-04-27
申请号：PCT/US2005036498
申请日：2005-10-12
申请人： SQUIBB BRISTOL MYERS CO , SHER PHILIP M , WU GANG , EWING WILLIAM R
发明人： SHER PHILIP M , WU GANG , EWING WILLIAM R
IPC分类号： A61K31/454 , C07D401/02
CPC分类号： C07D401/12 , C07D211/96 , C07D409/12
摘要： The present application describes compounds according to Formula (I), wherein R
摘要翻译：本申请描述了根据式（I）的化合物，其中R

10. 发明申请

WO2007140284A3 N-TERMINALLY MODIFIED GLP-1 RECEPTOR MODULATORS 审中-公开
标题翻译： N-末端修饰的GLP-1受体调节剂
公开(公告)号：WO2007140284A3
公开(公告)日：2008-12-31
申请号：PCT/US2007069703
申请日：2007-05-25
申请人： SQUIBB BRISTOL MYERS CO , EWING WILLIAM R , MAPELLI CLAUDIO , RIEXINGER DOUGLAS JAMES , LEE VING G , SULSKY RICHARD B , ZHU YEHENG
发明人： EWING WILLIAM R , MAPELLI CLAUDIO , RIEXINGER DOUGLAS JAMES , LEE VING G , SULSKY RICHARD B , ZHU YEHENG
IPC分类号： C07K7/06 , A61K38/08 , A61K38/26
CPC分类号： A61K33/30 , A61K33/26 , A61K33/32 , A61K38/08 , A61K38/26 , A61K45/06 , C07K14/605 , A61K2300/00
摘要： The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that may stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本文所述的主题提供具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1）受体调节剂，因此可用于治疗或预防与GLP相关的疾病或病症活动。所述化合物包括可刺激II型糖尿病患者胰岛素分泌的化学修饰的肽，但也产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。所公开和要求保护的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

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