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1. 发明申请

WO2009054952A3 SMALL MOLECULE INHIBITORS OF PARP ACTIVITY 审中-公开
标题翻译：小分子抑制剂PARP活性
公开(公告)号：WO2009054952A3
公开(公告)日：2009-08-06
申请号：PCT/US2008011990
申请日：2008-10-22
申请人： ANGION BIOMEDICA CORP , PANICKER BIJOY , JUNG DAWOON , ZHU XIAOKANG , SMITH DAVID E , LIM DONG SUNG
发明人： PANICKER BIJOY , JUNG DAWOON , ZHU XIAOKANG , SMITH DAVID E , LIM DONG SUNG
IPC分类号： A61K31/44 , A61K31/522 , C07D237/32 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D237/32 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Componds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such componds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
摘要翻译：提供了抑制聚ADP-核糖合成酶（PARP）的活性的组合物和药物组合物。这样的化合物可用于治疗各种疾病，病症和损伤，例如中风，心肌梗死，各种器官中的缺血灌注损伤，创伤性脑损伤，动脉粥样硬化，炎性疾病和癌症。

2. 发明申请

WO2009054952A2 SMALL MOLECULE INHIBITORS OF PARP ACTIVITY 审中-公开
标题翻译：小分子PARP活性分子抑制剂
公开(公告)号：WO2009054952A2
公开(公告)日：2009-04-30
申请号：PCT/US2008/011990
申请日：2008-10-22
申请人： ANGION BIOMEDICA CORP. , PANICKER, Bijoy , JUNG, Dawoon , ZHU, Xiaokang , SMITH, David, E. , LIM, Dong Sung
发明人： PANICKER, Bijoy , JUNG, Dawoon , ZHU, Xiaokang , SMITH, David, E. , LIM, Dong Sung
IPC分类号： A61K31/44 , A61K31/52
CPC分类号： C07D237/32 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Componds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such componds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
摘要翻译：提供了抑制多聚ADP-核糖合成酶（PARP）活性的化合物和药物组合物。这些化合物可用于治疗各种疾病，病症和损伤，例如中风，心肌梗塞，各种器官的缺血 - 灌注损伤，创伤性脑损伤，动脉粥样硬化，炎性疾病和癌症。

3. 发明申请

WO2007081978A3 MODULATORS OF HEPATOCYTE GROWTH FACTOR / C-MET ACTIVITY 审中-公开
标题翻译：肝细胞生长因子/ C-MET活性的调节剂
公开(公告)号：WO2007081978A3
公开(公告)日：2007-11-29
申请号：PCT/US2007000584
申请日：2007-01-10
申请人： ANGION BIOMEDICA CORP , ZEMBOWER DAVID E , SINGH JASBIR , MISHRA RAMA K , JUNG DAWOON , ZHU XIAOKANG
发明人： ZEMBOWER DAVID E , SINGH JASBIR , MISHRA RAMA K , JUNG DAWOON , ZHU XIAOKANG
IPC分类号： A61K39/395 , C07K16/22
CPC分类号： C07D239/95 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/04
摘要： This invention is directed to compounds and compositions that have biological properties useful for modulating HGF/SF activity. In certain embodiments, said compounds and compositions may be used in the treatment and prophylaxis of cancer or other dysproliferative diseases, as well as inflammatory diseases such as rheumatoid arthritis.
摘要翻译：本发明涉及具有可用于调节HGF / SF活性的生物学特性的化合物和组合物。在某些实施方案中，所述化合物和组合物可用于治疗和预防癌症或其它增生性疾病，以及炎性疾病如类风湿性关节炎。

4. 发明申请

WO2011153192A2 CYTOCHROME P450 INHIBITORS AND USES THEREOF 审中-公开
标题翻译：细胞色素P450抑制剂及其用途
公开(公告)号：WO2011153192A2
公开(公告)日：2011-12-08
申请号：PCT/US2011038695
申请日：2011-06-01
申请人： ANGION BIOMEDICA CORP , PANICKER BIJOY , OEHLEN LAMBERTUS J W M , TARRANT JAMES G , LIM DONG SUNG , ZHU XIAOKANG , JUNG DAWOON , MISHRA RAMA K
发明人： PANICKER BIJOY , OEHLEN LAMBERTUS J W M , TARRANT JAMES G , LIM DONG SUNG , ZHU XIAOKANG , JUNG DAWOON , MISHRA RAMA K
IPC分类号： C07D417/04 , A61K31/428 , A61P9/10 , A61P35/00
CPC分类号： C07D417/06 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
摘要翻译：本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本课程和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。

5. 发明申请

WO2006094230A3 SCREENING METHODS FOR PROTEIN KINASE B INHIBITORS EMPLOYING VIRTUAL DOCKING APPROACHES AND COMPOUNDS AND COMPOSITIONS DISCOVERED THEREBY 审中-公开
公开(公告)号：WO2006094230A3
公开(公告)日：2006-09-08
申请号：PCT/US2006/007730
申请日：2006-03-02
申请人： THE BURNHAM INSTITUTE FOR MEDICAL RESEARCH , PELLECCHIA, Maurizio , FORTINO, Martino , JUNG, Dawoon
发明人： PELLECCHIA, Maurizio , FORTINO, Martino , JUNG, Dawoon
IPC分类号： G06F17/00 , G06F17/30
摘要： The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1 ) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1 , a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions.

6. 发明申请

WO2011153192A3 CYTOCHROME P450 INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：WO2011153192A3
公开(公告)日：2011-12-08
申请号：PCT/US2011/038695
申请日：2011-06-01
申请人： ANGION BIOMEDICA CORP. , PANICKER, Bijoy , OEHLEN, Lambertus ., J.W.M. , TARRANT, James, G. , LIM, Dong, Sung , ZHU, Xiaokang , JUNG, Dawoon , MISHRA, Rama, K.
发明人： PANICKER, Bijoy , OEHLEN, Lambertus ., J.W.M. , TARRANT, James, G. , LIM, Dong, Sung , ZHU, Xiaokang , JUNG, Dawoon , MISHRA, Rama, K.
IPC分类号： C07D417/04 , A61K31/428 , A61P35/00 , A61P9/10
摘要： The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

7. 发明申请

WO2007081978A2 MODULATORS OF HEPATOCYTE GROWTH FACTOR / C-MET ACTIVITY 审中-公开
标题翻译：肝细胞生长因子/ C-MET活性的调节剂
公开(公告)号：WO2007081978A2
公开(公告)日：2007-07-19
申请号：PCT/US2007/000584
申请日：2007-01-10
申请人： ANGION BIOMEDICA CORPORATION , ZEMBOWER, David, E. , SINGH, Jasbir , MISHRA, Rama, K. , JUNG, Dawoon , ZHU, Xiaokang
发明人： ZEMBOWER, David, E. , SINGH, Jasbir , MISHRA, Rama, K. , JUNG, Dawoon , ZHU, Xiaokang
IPC分类号： A61K31/517
CPC分类号： C07D239/95 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/04
摘要： This invention is directed to compounds and compositions that have biological properties useful for modulating HGF/SF activity. In certain embodiments, said compounds and compositions may be used in the treatment and prophylaxis of cancer or other dysproliferative diseases, as well as inflammatory diseases such as rheumatoid arthritis.
摘要翻译：本发明涉及具有可用于调节HGF / SF活性的生物学特性的化合物和组合物。在某些实施方案中，所述化合物和组合物可用于治疗和预防癌症或其他增生不良疾病，以及炎性疾病如类风湿性关节炎。

8. 发明申请

WO2006094230A2 SCREENING METHODS FOR PROTEIN KINASE B INHIBITORS EMPLOYING VIRTUAL DOCKING APPROACHES AND COMPOUNDS AND COMPOSITIONS DISCOVERED THEREBY 审中-公开
标题翻译：使用虚拟锁定方法的蛋白激酶B抑制剂的筛选方法及其发现的化合物和组合物
公开(公告)号：WO2006094230A2
公开(公告)日：2006-09-08
申请号：PCT/US2006007730
申请日：2006-03-02
申请人： BURNHAM INST MEDICAL RESEARCH , PELLECCHIA MAURIZIO , FORTINO MARTINO , JUNG DAWOON
发明人： PELLECCHIA MAURIZIO , FORTINO MARTINO , JUNG DAWOON
IPC分类号： G06F19/00
CPC分类号： G06F19/706 , G06F19/16 , G06F19/18
摘要： The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1 ) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1 , a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions.
摘要翻译：本发明描述了一种用于筛选化合物以抑制Akt1蛋白激酶（也称为蛋白激酶B）的酶活性的活性的改进方法，该酶被认为在抑制细胞凋亡中起着关键作用，因此在病因癌症等病症，包括神经退行性疾病。通常，该方法包括：（1）提供疑似具有Akt1激酶抑制活性的多种化合物; （2）将来自多个化合物的每个化合物与由Akt1，不可水解的ATP类似物和源自生理学AKT底物的肽底物衍生自三元复合物的晶体结构的靶结合位点进行建模，使得蛋白质定义活性位点，包括距离不可水解的ATP类似物限定距离内的那些残基; （3）通过拟合优点对准对接化合物; （4）通过使用一个或多个筛选标准进一步选择化合物，所述化合物通过拟合优先顺序进行对接; （5）任选地，目视分析在步骤（4）中选择的化合物的结构以除去具有不可能的对接几何形状的任何化合物; （6）如果进行步骤（5），则从步骤（4）或步骤（5）中选出的化合物进行实验测试，以确定其对Akt1的抑制活性，以选择具有Akt1抑制活性的化合物。本发明还包括药物组合物，其包括通过筛选方法发现对Akt1的抑制活性的化合物，以及药物组合物用于治疗癌症和其它病症的方法。

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