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1. 发明申请

US20130012531A1 TREATMENT METHOD 审中-公开
标题翻译：治疗方法
公开(公告)号：US20130012531A1
公开(公告)日：2013-01-10
申请号：US13518407
申请日：2011-01-05
申请人： Andrew G King , Albert B. Suttle , Valeriu Damian-Iordache , Megan M Mclaughlin
发明人： Andrew G King , Albert B. Suttle , Valeriu Damian-Iordache , Megan M Mclaughlin
IPC分类号： A61K31/506 , A61K31/404 , A61P27/02 , A61K31/44
CPC分类号： A61K31/52
摘要： The present invention is directed to methods of treating disorders of ocular angiogenesis or vascular leakage in a patient by administration of suitable inhibitors, including pazopanib or pharmaceutically acceptable salts or hydrates thereof.
摘要翻译：本发明涉及通过给予合适的抑制剂（包括吡罗他尼或其药学上可接受的盐或水合物）来治疗患者眼血管发生或血管渗漏的疾病的方法。

2. 发明授权

US06306583B1 Human brain phosphodiesterase 失效
标题翻译：人脑磷酸二酯酶
公开(公告)号：US06306583B1
公开(公告)日：2001-10-23
申请号：US08445474
申请日：1995-05-22
申请人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
发明人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
IPC分类号： C12Q168
CPC分类号： C12N9/16
摘要： Isolated cDNA clones from human brain (frontal cortex) cDNA libraries that encode a unique subtype of the low Km, cAMP-specific phosphodiesterases (PDE IVs) are disclosed. Analysis of the distribution of hPDE IVB mRNA expression in various human tissues using a nonconserved fragment of the cDNA as a probe revealed a restricted pattern of expression, with an ˜4-kb mRNA detected in brain, heart, lung and skeletal muscle and not in placenta, liver, kidney or pancreas. Furthermore, an additional ˜5-kb hPDE IVB-related mRNA species was detected in brain tissue. Expression of hPDE IVB in a genetically-engineered PDE-deficient strain of the yeast Saccharomym cerevisiae resulted in the overproduction of cAMP PDE activity which displayed the expected kinetic characteristics for a PDE IV: 1) low Km (4.3 &mgr;M) for cAMP, 2) high Km (>3 mM) for cGMP, and 3) sensitivity to rolipram (Ki=0.085 &mgr;M), a selective inhibitor of PDE IV. Recombinant hPDE IVB also bound [3H] R-rolipram saturably and with a high affinity. Analysis of [3H] R-rolipram binding data revealed curvilinear Scatchard plots, suggesting the presence of two non-interacting high affinity rolipram binding sites (Kd=0.4 and 6 nM) or a negatively cooperative interaction among multiple binding sites. This novel enzyme is particularly useful for screening candidate compounds for their ability to serve as potential anti-depressant, antiasthmatic or anti-inflammatory agents.
摘要翻译：公开了编码低Km，cAMP特异性磷酸二酯酶（PDE IV）的独特亚型的来自人脑（额叶皮质）cDNA文库的分离的cDNA克隆。使用cDNA的非保守片段作为探针分析各种人体组织中hPDE IVB mRNA表达的分布，显示出限制性表达模式，在脑，心脏，肺和骨骼肌中检测到〜4-kb mRNA，而不是在胎盘，肝，肾或胰腺。此外，在脑组织中检测到另外约5kb的hPDE IVB相关mRNA种类。在酵母酿酒酵母的遗传工程化PDE缺陷菌株中表达hPDE IVB导致过量产生cAMP PDE活性，其显示PDE IV的预期动力学特征：1）cAMP低Km（4.3μM），2）对于cGMP，高Km（> 3mM），以及3）灵敏度为咯利普兰（Ki =0.085μM），PDE IV的选择性抑制剂。重组hPDE IVB也以饱和和高亲和力结合[3H] R-咯利普兰。 [3H] R-咯利普兰结合数据的分析显示曲线Scatchard图，表明存在两个非相互作用的高亲和力咯利普兰结合位点（Kd = 0.4和6nM）或多个结合位点之间的负配位相互作用。该新型酶特别用于筛选候选化合物作为潜在的抗抑郁剂，抗哮喘或抗炎剂的能力。

3. 发明授权

US6150150A Human brain phosphodiesterase 有权
标题翻译：人脑磷酸二酯酶
公开(公告)号：US6150150A
公开(公告)日：2000-11-21
申请号：US192702
申请日：1998-11-16
申请人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
发明人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
IPC分类号： G01N33/53 , C07H21/04 , C07K14/47 , C07K16/40 , C07K19/00 , C08L101/16 , C12N1/19 , C12N1/21 , C12N9/16 , C12N15/09 , C12N15/55 , C12P21/08 , C12Q1/02 , C12Q1/44 , C12R1/865 , G01N33/573 , C12N9/22
CPC分类号： C12N9/16
摘要： Isolated cDNA clones from human brain (frontal cortex) cDNA libraries that encode a unique subtype of the low K.sub.m, cAMP-specific phosphodiesterases (PDE IVs) are disclosed. Analysis of the distribution of hPDE IV.sub.B mRNA expression in various human tissues using a nonconserved fragment of the cDNA as a probe revealed a restricted pattern of expression, with an .about.4-kb mRNA detected in brain, heart, lung and skeletal muscle and not in placenta, liver, kidney or pancreas. Furthermore, an additional .about.5-kb hPDE IV.sub.B.sup.- related mRNA species was detected in brain tissue. Expression of hPDE IV.sub.B in a genetically-engineered PDE-deficient strain of the yeast Saccharomyces cerevisiae resulted in the overproduction of cAMP PDE activity which displayed the expected kinetic characteristics for a PDE IV: 1) low K.sub.m (4.3 .mu.M) for cAMP, 2) high K.sub.m (>3 mM) for cGMP, and 3) sensitivity to rolipram (K.sub.i =0.085 .mu.M), a selective inhibitor of PDE IV. Recombinant hPDE IV.sub.B also bound [.sup.3 H] R-rolipram saturably and with a high affinity. Analysis of [.sup.3 H] R-rolipram binding data revealed curvilinear Scatchard plots, suggesting the presence of two non-interacting high affinity rolipram binding sites (K.sub.d =0.4 and 6 nM) or a negatively cooperative interaction among multiple binding sites.This novel enzyme is particularly useful for screening candidate compounds for their ability to serve as potential anti-depressant, antiasthmatic or anti-inflammatory agents.
摘要翻译：公开了编码低Km，cAMP特异性磷酸二酯酶（PDE IV）的独特亚型的来自人脑（额叶皮质）cDNA文库的分离的cDNA克隆。使用cDNA的非保守片段作为探针分析各种人体组织中hPDE IVB mRNA表达的分布，显示出限制性表达模式，在脑，心脏，肺和骨骼肌中检测到差异4-kb mRNA，而不是在胎盘，肝，肾或胰腺。此外，在脑组织中检测到另外的DIFFERENCE 5-kb hPDE IVB相关mRNA种类。在酵母酿酒酵母的遗传工程化PDE缺陷菌株中表达hPDE IVB导致cAMP PDE活性过度产生，其显示PDE IV的预期动力学特征：1）cAMP低的Km（4.3μM），2 ）对于cGMP高Km（> 3mM），和3）灵敏度对咯利普兰（Ki =0.085μM），PDE IV的选择性抑制剂。重组hPDE IVB也以饱和和高亲和力结合[3H] R-咯利普兰。 [3H] R-咯利普兰结合数据的分析显示曲线Scatchard图，表明存在两个非相互作用的高亲和力咯利普兰结合位点（Kd = 0.4和6nM）或多个结合位点之间的负配位相互作用。这种新型酶特别可用于筛选候选化合物作为潜在的抗抑郁剂，抗哮喘或抗炎药的能力。

4. 发明申请

US20120165354A1 TREATMENT METHOD 审中-公开
标题翻译：治疗方法
公开(公告)号：US20120165354A1
公开(公告)日：2012-06-28
申请号：US13383935
申请日：2010-07-16
申请人： Megan M. McLaughlin , John Irving Wurzelmann , Chun-Fang Xu
发明人： Megan M. McLaughlin , John Irving Wurzelmann , Chun-Fang Xu
IPC分类号： A61K31/506 , A61P27/02
CPC分类号： A61K31/415
摘要： The present invention relates to methods of treating age-related macular degeneration in a patient by administration of pazopanib or pharmaceutically acceptable salts or solvates thereof.
摘要翻译：本发明涉及通过给予吡罗他尼或其药学上可接受的盐或溶剂化物来治疗患者年龄相关性黄斑变性的方法。

5. 发明授权

US5932477A Polynucleotides encoding human brain phosphodiesterase 失效
标题翻译：编码人脑磷酸二酯酶的多核苷酸
公开(公告)号：US5932477A
公开(公告)日：1999-08-03
申请号：US942521
申请日：1997-10-02
申请人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
发明人： George P. Livi , Megan M. McLaughlin , Theodore J. Torphy
IPC分类号： G01N33/53 , C07H21/04 , C07K14/47 , C07K16/40 , C07K19/00 , C08L101/16 , C12N1/19 , C12N1/21 , C12N9/16 , C12N15/09 , C12N15/55 , C12P21/08 , C12Q1/02 , C12Q1/44 , C12R1/865 , G01N33/573 , C12N5/10 , C12N1/15 , C12N15/12
CPC分类号： C12N9/16
摘要： Isolated cDNA clones from human brain (frontal cortex) cDNA libraries that encode a unique subtype of the low K.sub.m, cAMP-specific phosphodiesterases (PDE IVs) are disclosed. Analysis of the distribution of hPDE IV.sub.B mRNA expression in various human tissues using a nonconserved fragment of the cDNA as a probe revealed a restricted pattern of expression, with an .about.4-kb MRNA detected in brain, heart, lung and skeletal muscle and not in placenta, liver, kidney or pancreas. Furthermore, an additional .about.5-kb hPDE IV.sub.B.sup.- related mRNA species was detected in brain tissue. Expression of hPDE IV.sub.B in a genetically-engineered PDE-deficient strain of the yeast Saccharomyces cerevisiae resulted in the overproduction of cAMP PDE activity which displayed the expected kinetic characteristics for a PDE IV: 1) low K.sub.m (4.3 .mu.M) for cAMP, 2) high K.sub.m (>3 mM) for cGMP, and 3) sensitivity to rolipram (K.sub.i =0.085 .mu.M), a selective inhibitor of PDE IV. Recombinant HPDE IV.sub.B also bound �.sup.3 H!R-rolipram saturably and with a high affinity. Analysis of �.sup.3 H!R-rolipram binding data revealed curvilinear Scatchard plots, suggesting the presence of two non-interacting high affinity rolipram binding sites (K.sub.d =0.4 and 6 nM) or a negatively cooperative interaction among multiple binding sites. This novel enzyme is particularly useful for screening candidate compounds for their ability to serve as potential anti-depressant, antiasthmatic or anti-inflammatory agents.
摘要翻译：公开了编码低Km，cAMP特异性磷酸二酯酶（PDE IV）的独特亚型的来自人脑（额叶皮质）cDNA文库的分离的cDNA克隆。使用cDNA的非保守片段作为探针分析各种人体组织中hPDE IVB mRNA表达的分布，显示了在脑，心脏，肺和骨骼肌中检测到差异4-kb MRNA的限制性表达模式，而不是在胎盘，肝，肾或胰腺。此外，在脑组织中检测到另外的DIFFERENCE 5-kb hPDE IVB相关mRNA种类。在酵母酿酒酵母的遗传工程化PDE缺陷菌株中表达hPDE IVB导致cAMP PDE活性过度产生，其显示PDE IV的预期动力学特征：1）cAMP低的Km（4.3μM），2 ）对于cGMP高Km（> 3mM），和3）灵敏度对咯利普兰（Ki =0.085μM），PDE IV的选择性抑制剂。重组HPDE IVB还以饱和的和高亲和力结合[3H] R-咯利普兰。 [3H] R-咯利普兰结合数据的分析显示曲线Scatchard图，表明存在两个非相互作用的高亲和力咯利普兰结合位点（Kd = 0.4和6nM）或多个结合位点之间的负配位相互作用。这种新型酶特别可用于筛选候选化合物作为潜在的抗抑郁剂，抗哮喘或抗炎药的能力。

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