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1.发明申请公开(公告)号：US20090239896A1
公开(公告)日：2009-09-24
申请号：US12092385
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Tony Kwok-Kong Mong , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Tony Kwok-Kong Mong , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. The compounds include azaindoles of the formula below [insert FIG. 6c] in which at least one of CR4, CR5, CR6 and CR7 is replaced by N, and the groups R1-R7 are defined as in claim 1.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。 这些化合物包括下式的氮杂吲哚[ 6c]，其中CR4，CR5，CR6和CR7中的至少一个被N替代，基团R1-R7如权利要求1中所定义。
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2.发明申请INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS 审中-公开具有C4-酸性取代基的单一化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20090318492A1
公开(公告)日：2009-12-24
申请号：US12092380
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/437 , A61K31/40 , C07D471/02 , C07D209/04
CPC分类号： C07D209/32
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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3.发明授权Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors 有权多价吲哚化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US07666898B2
公开(公告)日：2010-02-23
申请号：US11593177
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/18 , C07D471/04 , C07D487/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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4.发明申请INDOLE COMPOUNDS HAVING C4-AMIDE SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS 审中-公开具有C4酰胺取代基的单一化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20090306171A1
公开(公告)日：2009-12-10
申请号：US12092388
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/404 , C07D209/20
CPC分类号： C07D209/22
摘要： Indole and indole-related compounds according to the formula (I) or (II) optionally having additional heteroatoms, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. Formula (I), formula (II). R4 being a moiety represented by formula (C4-II-C), R3 being a moiety represented by formula (C3-I or C3-II).
摘要翻译： 公开了根据式（I）或（II）的任选具有其它杂原子的吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。 式（I），式（II）。 R4是由式（C4-II-C）表示的部分，R3是由式（C3-I或C3-II）表示的部分。
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5.发明申请Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors 有权多价吲哚化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20070135385A1
公开(公告)日：2007-06-14
申请号：US11593177
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
IPC分类号： A61K31/675 , A61K31/404 , C07D209/36
CPC分类号： C07D209/18 , C07D471/04 , C07D487/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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公开(公告)号：US07488495B2
公开(公告)日：2009-02-10
申请号：US10965274
申请日：2004-10-13
申请人： Dominique Charmot , Han Ting Chang , Gerrit Klaerner , Michael James Cope , Mingjun Liu , Futian Liu , Jerry Buysse , Eric Connor , Tony Kwok-Kong Mong , Jun Shao , Deidre Madsen
发明人： Dominique Charmot , Han Ting Chang , Gerrit Klaerner , Michael James Cope , Mingjun Liu , Futian Liu , Jerry Buysse , Eric Connor , Tony Kwok-Kong Mong , Jun Shao , Deidre Madsen
CPC分类号： A61K31/74
摘要： The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.
摘要翻译： 本发明提供了用于治疗离子失衡的方法和组合物。 特别地，本发明提供了包含钾结合聚合物及其药物组合物的组合物。 本文公开了用于治疗和/或预防益处的聚合物和药物组合物的使用方法。 这些方法的实例包括治疗高钾血症，例如由肾衰竭引起的高钾血症和/或使用引起高钾血症的药物。
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7.发明申请Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors 审中-公开磷脂酶抑制剂，包括多价磷脂酶抑制剂及其用途，包括作为内腔定位的磷脂酶抑制剂公开(公告)号：US20070135383A1
公开(公告)日：2007-06-14
申请号：US11593176
申请日：2006-11-03
申请人： Han-Ting Chang , Dominque Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
发明人： Han-Ting Chang , Dominque Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
IPC分类号： A61K31/685 , A61K31/66 , A61K31/503 , A61K31/4745 , A61K31/405 , A61K31/365
CPC分类号： A61K31/404 , A61K9/0019 , A61K9/0095 , A61K31/41 , A61K31/66 , A61K47/10 , A61K47/20 , A61K47/55 , A61K47/58
摘要： The present invention provides methods and compositions for the treatment of phospholipase-related conditions. In particular, the invention provides a method of treating insulin-related, weight-related conditions and/or cholesterol-related conditions in an animal subject. The method generally involves the administration of a non-absorbed and/or effluxed phospholipase A2 inhibitor that is localized in a gastrointestinal lumen.
摘要翻译： 本发明提供了治疗磷脂酶相关病症的方法和组合物。 特别地，本发明提供了一种在动物受试者中治疗胰岛素相关，体重相关病症和/或胆固醇相关病症的方法。 该方法通常涉及施用定位在胃肠腔中的未吸收和/或流出的磷脂酶A2抑制剂。
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公开(公告)号：US07718746B2
公开(公告)日：2010-05-18
申请号：US12471220
申请日：2009-05-22
申请人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
发明人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
IPC分类号： C08F26/06 , C07C211/11
CPC分类号： C08G73/02 , A61K31/13 , A61K31/785 , C08G73/0206 , C08L39/02 , C08L79/02 , C08L2666/02
摘要： Anion-binding polymers are described. The anion-binding polymers in some cases are low swelling anion-binding polymers. In some cases, the anion-binding polymers have a pore volume distribution such that a fraction of the polymer is not available for non-interacting solutes above a certain percentage of the MW of the target ion for the polymer. In some cases, the anion-binding polymers are characterized by low ion-binding interference, where the interference is measured in, for example, a gastrointestinal simulant, relative to non-interfering buffer. Pharmaceutical composition, methods of use, and kits are also described.
摘要翻译： 描述了阴离子结合聚合物。 阴离子结合聚合物在某些情况下是低溶胀阴离子结合聚合物。 在一些情况下，阴离子结合聚合物具有孔体积分布，使得聚合物的分数不能用于高于聚合物的目标离子的一定百分比MW的非相互作用溶质。 在一些情况下，阴离子结合聚合物的特征在于低离子结合干扰，其中相对于非干扰缓冲液在例如胃肠模拟物中测量干扰。 还描述了药物组合物，使用方法和试剂盒。
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9.发明授权Pharmaceutical compositions comprising cross-linked small molecule amine polymers 失效包含交联的小分子胺聚合物的药物组合物公开(公告)号：US07608674B2
公开(公告)日：2009-10-27
申请号：US10980991
申请日：2004-11-03
申请人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
发明人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
CPC分类号： C08G73/02 , A61K31/13 , A61K31/785 , C08G73/0206 , C08L39/02 , C08L79/02 , C08L2666/02
摘要： Anion-binding polymers are described. The anion-binding polymers in some cases are low swelling anion-binding polymers. In some cases, the anion-binding polymers have a pore volume distribution such that a fraction of the polymer is not available for non-interacting solutes above a certain percentage of the MW of the target ion for the polymer. In some cases, the anion-binding polymers are characterized by low ion-binding interference, where the interference is measured in, for example, a gastrointestinal simulant, relative to non-interfering buffer. Pharmaceutical composition, methods of use, and kits are also described.
摘要翻译： 描述了阴离子结合聚合物。 阴离子结合聚合物在某些情况下是低溶胀阴离子结合聚合物。 在一些情况下，阴离子结合聚合物具有孔体积分布，使得聚合物的分数不可用于高于聚合物的靶离子MW的一定百分比的非相互作用溶质。 在一些情况下，阴离子结合聚合物的特征在于低离子结合干扰，其中相对于非干扰缓冲液在例如胃肠模拟物中测量干扰。 还描述了药物组合物，使用方法和试剂盒。
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公开(公告)号：US20100029897A1
公开(公告)日：2010-02-04
申请号：US12471220
申请日：2009-05-22
申请人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
发明人： Eric Connor , Dominique Charmot , Han-Ting Chang , Florence Roger , Gerrit Klaerner , Son Hoai Nguyen , Jonathan Mills , Jerry M. Buysse , Angela Lee , Deidre Madsen , Jun Shao , Michael J. Cope , John Fordtran
IPC分类号： C08G73/00
CPC分类号： C08G73/02 , A61K31/13 , A61K31/785 , C08G73/0206 , C08L39/02 , C08L79/02 , C08L2666/02
摘要： Anion-binding polymers are described. The anion-binding polymers in some cases are low swelling anion-binding polymers. In some cases, the anion-binding polymers have a pore volume distribution such that a fraction of the polymer is not available for non-interacting solutes above a certain percentage of the MW of the target ion for the polymer. In some cases, the anion-binding polymers are characterized by low ion-binding interference, where the interference is measured in, for example, a gastrointestinal simulant, relative to non-interfering buffer. Pharmaceutical composition, methods of use, and kits are also described.
摘要翻译： 描述了阴离子结合聚合物。 阴离子结合聚合物在某些情况下是低溶胀阴离子结合聚合物。 在一些情况下，阴离子结合聚合物具有孔体积分布，使得聚合物的分数不可用于高于聚合物的靶离子MW的一定百分比的非相互作用溶质。 在一些情况下，阴离子结合聚合物的特征在于低离子结合干扰，其中相对于非干扰缓冲液在例如胃肠模拟物中测量干扰。 还描述了药物组合物，使用方法和试剂盒。
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