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1. 发明申请

WO2006089275A2 METHODS OF MAKING PHARMACOKINETICALLY IMPROVED COMPOUNDS COMPRISING FUNCTIONAL RESIDUES OR GROUPS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAID COMPOUNDS 审中-公开
标题翻译：制备包含功能性残留物或组合的药物动力学改进的化合物的方法和包含化合物的药物组合物
公开(公告)号：WO2006089275A2
公开(公告)日：2006-08-24
申请号：PCT/US2006006047
申请日：2006-02-21
申请人： SURFACE LOGIX INC , LUND FRANCES E , DUFFY DAVID , GROGAN MICHAEL , KATES STEVEN , OSTUNI EMANUELE , SCHUELLER OLIVIER , SWEETNAM PAUL
发明人： LUND FRANCES E , DUFFY DAVID , GROGAN MICHAEL , KATES STEVEN , OSTUNI EMANUELE , SCHUELLER OLIVIER , SWEETNAM PAUL
IPC分类号： A61K31/53
CPC分类号： A61K31/53
摘要： The present invention relates to methods of modulating the pharmacokinetic and/or pharmacodynamic properties of a compound by attaching at least one functional unit or group to the compound, thereby improving its non-specific binding characteristics and/or pharmacokinetic properties. Compounds comprising at least one functional residue are provided, as are pharmaceutical compositions comprising said compounds.
摘要翻译：本发明涉及通过将至少一个功能单元或基团连接到化合物上来调节化合物的药代动力学和/或药效学性质的方法，从而改善其非特异性结合特征和/或药代动力学性质。提供包含至少一个功能性残基的化合物，以及包含所述化合物的药物组合物。

2. 发明申请

WO2006089275A3 METHODS OF MAKING PHARMACOKINETICALLY IMPROVED COMPOUNDS COMPRISING FUNCTIONAL RESIDUES OR GROUPS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAID COMPOUNDS 审中-公开
公开(公告)号：WO2006089275A3
公开(公告)日：2006-08-24
申请号：PCT/US2006/006047
申请日：2006-02-21
申请人： SURFACE LOGIX, INC. , LUND, Frances, E. , DUFFY, David , GROGAN, Michael , KATES, Steven , OSTUNI, Emanuele , SCHUELLER, Olivier , SWEETNAM, Paul
发明人： LUND, Frances, E. , DUFFY, David , GROGAN, Michael , KATES, Steven , OSTUNI, Emanuele , SCHUELLER, Olivier , SWEETNAM, Paul
IPC分类号： A61K31/53 , C07D487/04 , A61P15/10
摘要： The present invention relates to methods of modulating the pharmacokinetic and/or pharmacodynamic properties of a compound by attaching at least one functional unit or group to the compound, thereby improving its non-specific binding characteristics and/or pharmacokinetic properties. Compounds comprising at least one functional residue are provided, as are pharmaceutical compositions comprising said compounds.

3. 发明申请

WO2006088951A9 CD38 MODULATED CHEMOTAXIS 审中-公开
标题翻译： CD38调节化学
公开(公告)号：WO2006088951A9
公开(公告)日：2007-10-18
申请号：PCT/US2006005314
申请日：2006-02-14
申请人： TRUDEAU INST , LUND FRANCES E , RANDALL TROY D , PARTIDA-SANDCHEZ SANTIAGO
发明人： LUND FRANCES E , RANDALL TROY D , PARTIDA-SANDCHEZ SANTIAGO
IPC分类号： C12P21/06 , C12N5/00 , G01N33/53
CPC分类号： G01N33/5047 , C07K16/2896 , G01N2333/70596 , G01N2333/924 , G01N2500/10
摘要： The present invention relates to methods for modulating the migratory activity of cells expressing CD38 for the treatment of disorders including, but not limited to, inflammation, ischemia, asthma, autoimmune disease, diabetes, arthritis, allergies, infection with pathogenic organisms, such as parasites, and transplant rejection. Such cells include, for example, neutrophils, lymphocytes, eosinophils, macrophages and dentritic cells. The invention further relates to drug screening assays designed to identify compounds that modulate the ADP- ribosyl cyclase activity of CD38 and the use of such, compounds in the treatment of disorders involving CD38 modulated cell migration. Additionally, the invention relates to the isolation and characterization of a CD38 homologue from the parasitic flatworm, Schistosoma mansoni.
摘要翻译：本发明涉及调节表达CD38的细胞的迁移活性的方法，用于治疗疾病，包括但不限于炎症，局部缺血，哮喘，自身免疫疾病，糖尿病，关节炎，过敏，病原体感染等寄生虫，移植排斥。这样的细胞包括例如嗜中性粒细胞，淋巴细胞，嗜酸性粒细胞，巨噬细胞和牙髓细胞。本发明还涉及设计用于鉴定调节CD38的ADP-核糖基环化酶活性的化合物的药物筛选试验，以及这些化合物在治疗涉及CD38调节的细胞迁移的病症中的用途。此外，本发明涉及从寄生扁丝虫曼氏血吸虫分离和表征CD38同系物。

4. 发明申请

WO2007082053A2 TRPM2-SPECIFIC INHIBITORS 审中-公开
标题翻译： TRPM2特异性抑制剂
公开(公告)号：WO2007082053A2
公开(公告)日：2007-07-19
申请号：PCT/US2007/000803
申请日：2007-01-10
申请人： TRUDEAU INSTITUTE , LUND, Frances, E. , PARTIDA-SANCHEZ, Santiago , WALSETH, Tim
发明人： LUND, Frances, E. , PARTIDA-SANCHEZ, Santiago , WALSETH, Tim
IPC分类号： E01C3/06
CPC分类号： C07K14/705 , A61K31/365 , G01N33/6872 , G01N2500/04
摘要： The present invention relates to methods and compositions for modulating ADPR- mediated migratory activity of cells through regulation of the TRPM2 cation channel. Such methods and compositions may be used for the treatment of disorders including, but not limited to, inflammation, ischemia, atherosclerosis, asthma, autoimmune disease, diabetes, arthritis, allergies, and transplant rejection. Such cells include, for example, neutrophils, lymphocytes, eosinophils, macrophages, monocytes and dendritic cells. The invention further relates to specific inhibition of TRPM2 by blocking the activity of ADPR. The invention also relates to drug screening assays designed to identify compounds that regulate TRPM2 and thereby also function to modulate ADPR-mediated cell migration. The invention is based on the discovery that, 8Br-ADPR, which specifically inhibits activation of TRPM2, acts to inhibit ADPR-mediated cell migration.
摘要翻译：本发明涉及通过调节TRPM2阳离子通道调节ADPR介导的细胞迁移活性的方法和组合物。这些方法和组合物可用于治疗疾病，包括但不限于炎症，缺血，动脉粥样硬化，哮喘，自身免疫性疾病，糖尿病，关节炎，过敏和移植排斥。这样的细胞包括例如嗜中性粒细胞，淋巴细胞，嗜酸性粒细胞，巨噬细胞，单核细胞和树突状细胞。本发明还涉及通过阻断ADPR的活性而对TRPM2的特异性抑制。本发明还涉及设计用于鉴定调节TRPM2的化合物并由此也可用于调节ADPR介导的细胞迁移的药物筛选测定。本发明基于以下发现：特异性抑制TRPM2激活的8Br-ADPR起抑制ADPR介导的细胞迁移的作用。

5. 发明申请

WO2007082053A3 TRPM2-SPECIFIC INHIBITORS 审中-公开
标题翻译： TRPM2特异性抑制剂
公开(公告)号：WO2007082053A3
公开(公告)日：2008-03-06
申请号：PCT/US2007000803
申请日：2007-01-10
申请人： TRUDEAU INST , LUND FRANCES E , PARTIDA-SANCHEZ SANTIAGO , WALSETH TIM
发明人： LUND FRANCES E , PARTIDA-SANCHEZ SANTIAGO , WALSETH TIM
IPC分类号： A61K31/70
CPC分类号： C07K14/705 , A61K31/365 , G01N33/6872 , G01N2500/04
摘要： The present invention relates to methods and compositions for modulating ADPR- mediated migratory activity of cells through regulation of the TRPM2 cation channel. Such methods and compositions may be used for the treatment of disorders including, but not limited to, inflammation, ischemia, atherosclerosis, asthma, autoimmune disease, diabetes, arthritis, allergies, and transplant rejection. Such cells include, for example, neutrophils, lymphocytes, eosinophils, macrophages, monocytes and dendritic cells. The invention further relates to specific inhibition of TRPM2 by blocking the activity of ADPR. The invention also relates to drug screening assays designed to identify compounds that regulate TRPM2 and thereby also function to modulate ADPR-mediated cell migration. The invention is based on the discovery that, 8Br-ADPR, which specifically inhibits activation of TRPM2, acts to inhibit ADPR-mediated cell migration.
摘要翻译：本发明涉及通过调节TRPM2阳离子通道调节ADPR介导的细胞迁移活性的方法和组合物。这些方法和组合物可用于治疗疾病，包括但不限于炎症，缺血，动脉粥样硬化，哮喘，自身免疫性疾病，糖尿病，关节炎，过敏和移植排斥。这样的细胞包括例如嗜中性粒细胞，淋巴细胞，嗜酸性粒细胞，巨噬细胞，单核细胞和树突状细胞。本发明还涉及通过阻断ADPR的活性而对TRPM2的特异性抑制。本发明还涉及设计用于鉴定调节TRPM2的化合物并由此也可用于调节ADPR介导的细胞迁移的药物筛选测定。本发明基于以下发现：特异性抑制TRPM2激活的8Br-ADPR起抑制ADPR介导的细胞迁移的作用。

6. 发明申请

WO2006088951A3 CD38 MODULATED CHEMOTAXIS 审中-公开
公开(公告)号：WO2006088951A3
公开(公告)日：2007-03-15
申请号：PCT/US2006005314
申请日：2006-02-14
申请人： TRUDEAU INST , LUND FRANCES E , RANDALL TROY D , PARTIDA-SANDCHEZ SANTIAGO
发明人： LUND FRANCES E , RANDALL TROY D , PARTIDA-SANDCHEZ SANTIAGO
IPC分类号： C12P21/06 , C12N5/00 , G01N33/53
CPC分类号： G01N33/5047 , C07K16/2896 , G01N2333/70596 , G01N2333/924 , G01N2500/10
摘要： The present invention relates to methods for modulating the migratory activity of cells expressing CD38 for the treatment of disorders including, but not limited to, inflammation, ischemia, asthma, autoimmune disease, diabetes, arthritis, allergies, infection with pathogenic organisms, such as parasites, and transplant rejection. Such cells include, for example, neutrophils, lymphocytes, eosinophils, macrophages and dentritic cells. The invention further relates to drug screening assays designed to identify compounds that modulate the ADP- ribosyl cyclase activity of CD38 and the use of such, compounds in the treatment of disorders involving CD38 modulated cell migration. Additionally, the invention relates to the isolation and characterization of a CD38 homologue from the parasitic flatworm, Schistosoma mansoni.
摘要翻译：本发明涉及调节表达CD38的细胞的迁移活性以治疗疾病的方法，所述疾病包括但不限于炎症，局部缺血，哮喘，自身免疫性疾病，糖尿病，关节炎，变态反应，病原体如寄生虫和移植排斥反应。这样的细胞包括例如嗜中性粒细胞，淋巴细胞，嗜酸性粒细胞，巨噬细胞和树突细胞。本发明进一步涉及设计用于鉴定调节CD38的ADP-核糖基环化酶活性的化合物的药物筛选测定法以及这种化合物在治疗涉及CD38调节的细胞迁移的病症中的用途。另外，本发明涉及从寄生性扁平虫曼氏血吸虫中分离和表征CD38同系物。

7. 发明申请

WO2006088951A2 CD38 MODULATED CHEMOTAXIS 审中-公开
标题翻译： CD38调节化学
公开(公告)号：WO2006088951A2
公开(公告)日：2006-08-24
申请号：PCT/US2006/005314
申请日：2006-02-14
申请人： TRUDEAU INSTITUTE , LUND, Frances, E. , RANDALL, Troy, D. , PARTIDA-SANDCHEZ, Santiago
发明人： LUND, Frances, E. , RANDALL, Troy, D. , PARTIDA-SANDCHEZ, Santiago
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C12N9/10 , C12N9/22 , C12N9/24
CPC分类号： G01N33/5047 , C07K16/2896 , G01N2333/70596 , G01N2333/924 , G01N2500/10
摘要： The present invention relates to methods for modulating the migratory activity of cells expressing CD38 for the treatment of disorders including, but not limited to, inflammation, ischemia, asthma, autoimmune disease, diabetes, arthritis, allergies, infection with pathogenic organisms, such as parasites, and transplant rejection. Such cells include, for example, neutrophils, lymphocytes, eosinophils, macrophages and dentritic cells. The invention further relates to drug screening assays designed to identify compounds that modulate the ADP- ribosyl cyclase activity of CD38 and the use of such, compounds in the treatment of disorders involving CD38 modulated cell migration. Additionally, the invention relates to the isolation and characterization of a CD38 homologue from the parasitic flatworm, Schistosoma mansoni.
摘要翻译：本发明涉及调节表达CD38的细胞的迁移活性的方法，用于治疗疾病，包括但不限于炎症，局部缺血，哮喘，自身免疫疾病，糖尿病，关节炎，过敏，病原体感染等寄生虫，移植排斥。这样的细胞包括例如嗜中性粒细胞，淋巴细胞，嗜酸性粒细胞，巨噬细胞和牙髓细胞。本发明还涉及设计用于鉴定调节CD38的ADP-核糖基环化酶活性的化合物的药物筛选试验，以及这些化合物在治疗涉及CD38调节的细胞迁移的病症中的用途。此外，本发明涉及从寄生扁丝虫曼氏血吸虫分离和表征CD38同系物。

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