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公开(公告)号:US07029695B2
公开(公告)日:2006-04-18
申请号:US09903442
申请日:2001-07-10
申请人: Thomas Redelmeier , Lawrence M. Kauvar , Robert T. Lum , Matthew H. Lyttle , Robert W. Macsata , Steven R. Schow , Hugo O. Villar , Michael R. Kozlowski
发明人: Thomas Redelmeier , Lawrence M. Kauvar , Robert T. Lum , Matthew H. Lyttle , Robert W. Macsata , Steven R. Schow , Hugo O. Villar , Michael R. Kozlowski
CPC分类号: A61K9/1075 , A61K9/127 , A61K38/063
摘要: Pharmaceutical compositions and methods of using them. Lipid formulations of a glutathione analog and methods of manufacturing them. Their use to stimulate hematopoiesis, protect hematopoietic cells from damage caused by radiation or chemotherapy, or potentiate the stimulatory action of one or a combination of cytokines on colony formation by hematopoietic progenitor cells, protect a subject from a destructive effect of a chemotherapeutic agent or irradiation, or to potentiate the effect of a chemotherapeutic agent.
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公开(公告)号:US06337338B1
公开(公告)日:2002-01-08
申请号:US09464360
申请日:1999-12-15
IPC分类号: A61K3147
CPC分类号: A61K31/4706 , A61K31/425 , A61K31/47 , A61K2300/00
摘要: Methods for treating diseases associated with the activity of the insulin growth factor-1 receptor (IGF-1R), such as cancer, are provided. Methods for inhibiting cell growth and proliferation, especially of tumor cells, and promoting apoptosis are also provided. Each of these methods employs the use of a heteroaryl-aryl urea compound as an antagonist for IGF-1R.
摘要翻译: 提供了治疗与胰岛素生长因子-1受体(IGF-1R)的活性相关的疾病如癌症的方法。 还提供了抑制细胞生长和增殖,特别是肿瘤细胞增殖和促进细胞凋亡的方法。 这些方法中的每一种都使用杂芳基 - 芳基脲化合物作为IGF-1R的拮抗剂。
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公开(公告)号:US5851988A
公开(公告)日:1998-12-22
申请号:US784854
申请日:1997-01-15
IPC分类号: C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/58 , A61K31/05 , A61K31/10 , A61K31/17 , A61K31/655
CPC分类号: G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译: 胰岛素受体的活性的调节,细胞的葡萄糖摄取的增强以及在糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现:式(1)+ TR< IMAGE>其中每个A是 独立地是质子接受取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个连接体独立地是-NHCONH-或-N = N-或-NHCO-的等离子体。 式(1)属中的化合物也可用于结构活性研究,以鉴定负责相关活性的特征。
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公开(公告)号:USRE39866E1
公开(公告)日:2007-10-02
申请号:US11167026
申请日:2005-06-23
IPC分类号: A61K31/655 , A61K31/17 , A61K31/10 , A61K31/015 , C07C245/00
CPC分类号: G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N═N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译: 胰岛素受体的活性调节,细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现:其中每个A独立地是质子受体取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个接头独立地是-NHCONH-或-N-N-或-NHCO-的等排物。 式(1)属中的化合物也可用于结构活性研究,以鉴定负责相关活性的特征。
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公开(公告)号:US5830918A
公开(公告)日:1998-11-03
申请号:US784857
申请日:1997-01-15
IPC分类号: C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/58 , A61K31/135
CPC分类号: C12Q1/48 , C07C309/34 , C12Q1/34 , G01N33/582 , G01N2333/62 , G01N2333/72 , G01N2333/9121
摘要: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## wherein each Ar is independently an aromatic moiety; each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; m is 0 or 1; n is 4-6; and each linker is independently an isostere of --CH.sub.2 --, --CH.dbd.CH-- or --NCHO--. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译: 胰岛素受体的活性的调节,细胞的葡萄糖摄取增强以及在糖尿病的控制和治疗中显着的其它作用使用式(1)的化合物来实现,其中每个Ar独立地是芳族部分; 每个A独立地是质子接受取代基; 每个R独立地是非干扰取代基; m为0或1; n为4-6; 并且每个连接体独立地是-CH 2 - , - CH = CH - 或-NCHO - 的等势线。 式(1)属中的化合物也可用于结构活性研究,以鉴定负责相关活性的特征。
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公开(公告)号:US5741653A
公开(公告)日:1998-04-21
申请号:US622693
申请日:1996-03-26
申请人: Lawrence M. Kauvar , Hugo O. Villar
发明人: Lawrence M. Kauvar , Hugo O. Villar
IPC分类号: G01N33/53 , G01N33/566 , G01N33/68 , G01N33/94
CPC分类号: G01N33/6845 , G01N33/53 , G01N33/5308 , G01N33/68 , G01N33/94
摘要: Panels which consist of individual members, said members comprising proteins, wherein at least one of the members of the panel is a protein other than an immunoglobulin (Ig) or fragment thereof and wherein the presence of said non-Ig protein enriches the panel are described herein. These panels can be tested for reactivity with an analyte to create a profile. Such profiles can be used in pattern matching, analysis of samples and other analyses. Illustrated herein using such panels is a method to determine reactivity of a candidate compound with a target "receptor" which method does not require the physical presence of the receptor. By providing a formula for treating data obtained from a reference panel of this type which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference panel, the formula applied, and reactivity with the actual target receptor may be predicted.
摘要翻译: 由单个成员构成的面板,所述成员包括蛋白质,其中该组成员中的至少一个成员是除免疫球蛋白(Ig)或其片段之外的蛋白质,并且其中描述富含该面板的所述非Ig蛋白质的存在被描述 这里。 可以测试这些面板与分析物的反应性以形成轮廓。 这种轮廓可用于模式匹配,样本分析和其他分析。 本文使用这种面板说明的是确定候选化合物与目标“受体”的反应性的方法,该方法不需要受体的物理存在。 通过提供一种治疗从预测与靶受体反应性的参考面板获得的数据的公式,待测试的化合物可以相对于参考面板,所应用的配方和与实际的反应性进行物理学评估 可以预测靶受体。
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公开(公告)号:US5587293A
公开(公告)日:1996-12-24
申请号:US177673
申请日:1994-01-06
申请人: Lawrence M. Kauvar , Hugo O. Villar
发明人: Lawrence M. Kauvar , Hugo O. Villar
CPC分类号: G01N33/53 , G01N33/5308 , G01N33/68 , G01N33/94 , G06F19/704 , G06F19/706 , Y10S436/809
摘要: A method to determine reactivity of a candidate compound with a target receptor which method does not require the physical presence of the receptor is disclosed. By providing a formula for treating data obtained from a reference set of receptors which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference receptors, the formula applied, and reactivity with the actual target receptor may be predicted.
摘要翻译: 公开了一种确定候选化合物与靶受体的反应性的方法,该方法不需要受体的物理存在。 通过提供一种治疗从预测与靶受体反应性的参考受体组获得的数据的公式,待测试的化合物可以相对于参考受体,所应用的配方和与实际目标的反应性进行物理学评估 受体可以被预测。
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公开(公告)号:US06329431B1
公开(公告)日:2001-12-11
申请号:US08916088
申请日:1997-08-21
IPC分类号: A01N4728
CPC分类号: C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/582 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , G06F17/30905 , H04N21/2356 , H04N21/2541 , H04N21/25875 , H04N21/25891 , H04N21/4622 , H04N21/4782 , H04N21/4786
摘要: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; m is 0 or 1; n is 0, 1, or 2; and each linker is independently —NHCNHNH—, —NHCOO—, OCOO—,—CH═CH—, —CH═N—, —CH2CH2—, —NHCH2—, —OCO— or —COO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译: 胰岛素受体的活性调节,细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用是使用アルフラフラ座的化合物,每个A独立地是质子受体取代基;每个R独立地是非干扰的 取代基; m为0或1; n为0,1或2; 连接体独立为-NHCNHNH-,-NHCOO-,OCOO - , - CH = CH - , - CH = N - , - CH2CH2 - , - NHCH2-,-OCO-或-COO-。 式(1)属中的化合物也可用于结构活性研究,以鉴定负责相关活性的特征。
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公开(公告)号:USRE38915E1
公开(公告)日:2005-12-06
申请号:US09748665
申请日:2000-12-21
IPC分类号: C07C309/34 , C12Q1/34 , C12Q1/48 , G01N33/58 , A61K31/05 , A61K31/10 , A61K31/17 , A61K31/655
CPC分类号: G01N33/582 , C07C309/34 , C12Q1/34 , C12Q1/48 , G01N2333/62 , G01N2333/72 , G01N2333/9121 , Y10S514/866
摘要: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N═N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要翻译: 胰岛素受体的活性调节,细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用使用下式的化合物来实现:其中每个A独立地是质子受体取代基; 每个R独立地是非干扰取代基; n为0,1或2; 并且每个接头独立地是-NHCONH-或-N-N-或-NHCO-的等排物。 式(1)属中的化合物也可用于结构活性研究,以鉴定负责相关活性的特征。
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公开(公告)号:US5798275A
公开(公告)日:1998-08-25
申请号:US308813
申请日:1994-09-19
申请人: Lawrence M. Kauvar , Hugo O. Villar
发明人: Lawrence M. Kauvar , Hugo O. Villar
CPC分类号: G01N33/53 , G01N33/5308 , G01N33/68 , G01N33/94 , G06F19/704 , G06F19/706 , Y10S436/809
摘要: Panels which consist of individual members, said members comprising proteins, wherein at least one of the members of the panel is a protein other than an immunoglobulin (Ig) or fragment thereof and wherein the presence of said non-Ig protein enriches the panel are described herein. These panels can be tested for reactivity with an analyte to create a profile. Such profiles can be used in pattern matching, analysis of samples and other analyses. Illustrated herein using such panels is a method to determine reactivity of a candidate compound with a target "receptor" which method does not require the physical presence of the receptor. By providing a formula for treating data obtained from a reference panel of this type which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference panel, the formula applied, and reactivity with the actual target receptor may be predicted.
摘要翻译: 由单个成员构成的面板,所述成员包括蛋白质,其中该组成员中的至少一个成员是除免疫球蛋白(Ig)或其片段之外的蛋白质,并且其中描述富含该面板的所述非Ig蛋白质的存在被描述 这里。 可以测试这些面板与分析物的反应性以形成轮廓。 这种轮廓可用于模式匹配,样本分析和其他分析。 本文使用这种面板说明的是确定候选化合物与目标“受体”的反应性的方法,该方法不需要受体的物理存在。 通过提供一种治疗从预测与靶受体反应性的参考面板获得的数据的公式,待测试的化合物可以相对于参考面板,所应用的配方和与实际的反应性进行物理学评估 可以预测靶受体。
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