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1.发明授权公开(公告)号：US10208018B2
公开(公告)日：2019-02-19
申请号：US15320810
申请日：2015-07-02
申请人： Christopher M. Adams , Doug Bevan , Michael Paul Capparelli , Takeru Ehara , Luciana Ferrara , Nan Ji , Mitsunori Kato , Nello Mainolfi , Erik Meredith , Muneto Mogi , James J. Powers , Ganesh Prasanna
发明人： Christopher M. Adams , Doug Bevan , Michael Paul Capparelli , Takeru Ehara , Luciana Ferrara , Nan Ji , Mitsunori Kato , Nello Mainolfi , Erik Meredith , Muneto Mogi , James J. Powers , Ganesh Prasanna
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D401/10 , C07D401/12 , A61K9/00 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , C07D405/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US09475806B2
公开(公告)日：2016-10-25
申请号：US14774430
申请日：2014-03-13
申请人： Christopher Michael Adams , Charles Babu , Michael Paul Capparelli , Jian Ding , Takeru Ehara , Keith Jendza , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Liang Xue , Nello Mainolfi , James J. Powers , Michael H. Serrano-Wu , Chun Zhang
发明人： Christopher Michael Adams , Charles Babu , Michael Paul Capparelli , Jian Ding , Takeru Ehara , Keith Jendza , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Liang Xue , Nello Mainolfi , James J. Powers , Michael H. Serrano-Wu , Chun Zhang
IPC分类号： C07D401/14 , A61K31/4353 , A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.
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3.发明申请Piperidinyl-Indole Derivatives Complement Factor B Inhibitors and Uses Thereof 有权哌啶基 - 吲哚衍生物补体因子B抑制剂及其用途公开(公告)号：US20160152605A1
公开(公告)日：2016-06-02
申请号：US14904694
申请日：2014-07-14
申请人： Christopher ADAMS , Michael Paul CAPPARELLI , Takeru EHARA , Rajeshri Ganesh KARKI , Nello MAINOLFI , Chun ZHANG
发明人： Christopher Michael Adams , Michael Paul Capparelli , Takeru Ehara , Rajeshri Ganesh Karki , Nello Mainolfi , Chun Zhang
IPC分类号： C07D413/06 , A61K31/454 , C07D403/06 , A61K31/438 , C07D401/14 , A61K31/4439 , A61K31/5377 , A61K31/55 , C07D401/06 , A61K31/404
CPC分类号： C07D413/06 , A61K31/404 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/55 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitors of the complement alternative pathway, in particular of Factor B. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译： 本发明提供式I化合物：（I）制备本发明化合物的方法及其作为补体替代途径抑制剂，特别是因子B的治疗用途。本发明进一步提供了药理学上的组合 活性剂和药物组合物。
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4.发明申请公开(公告)号：US20170197940A1
公开(公告)日：2017-07-13
申请号：US15320810
申请日：2015-07-02
申请人： Christopher M. ADAMS , Doug BEVAN , Michael Paul CAPPARELLI , Takeru EHARA , Luciana FERRARA , Nan JI , Mitsunori KATO , Nello MAINOLFI , Erik MEREDITH , Muneto MOGI , James J. POWERS , Ganesh PRASANNA
发明人： Christopher M. ADAMS , Doug BEVAN , Michael Paul CAPPARELLI , Takeru EHARA , Luciana FERRARA , Nan JI , Mitsunori KATO , Nello MAINOLFI , Erik MEREDITH , Muneto MOGI , James J. POWERS , Ganesh PRASANNA
IPC分类号： C07D401/14 , C07D401/12 , A61K31/454 , C07D413/14 , A61K31/4725 , A61K31/4439 , C07D405/14 , A61K9/00 , A61K31/4545
CPC分类号： C07D401/14 , A61K9/0048 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , C07D401/10 , C07D401/12 , C07D405/14 , C07D413/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20120142685A1
公开(公告)日：2012-06-07
申请号：US12594728
申请日：2008-04-04
申请人： Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
发明人： Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
IPC分类号： A61K31/5377 , C07D471/10 , A61K31/444 , A61P7/10 , A61P9/04 , A61P35/00 , A61P3/04 , A61P3/10 , C07D471/04 , A61K31/496
CPC分类号： C07D471/04
摘要： The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译： 本发明提供式I化合物：（式I）所述化合物是属于AGC或钙调蛋白激酶家族的激酶选择性亚型的抑制剂，例如MARK1 / 2/3，PKD-1/2/3，PKN -1/2，CDK-9，CaMKII，ROCK-I / II，组蛋白脱乙酰酶（HDAC）磷酸化抑制剂或其他激酶抑制剂。 最后，本发明还提供药物组合物。
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公开(公告)号：US20150250767A1
公开(公告)日：2015-09-10
申请号：US14715594
申请日：2015-05-19
申请人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Liang XUE , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
发明人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Liang XUE , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
IPC分类号： A61K31/4184 , A61K31/4439 , A61K31/4245
CPC分类号： A61K31/4184 , A61K31/423 , A61K31/4245 , A61K31/4439 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/14 , C07D413/06 , C07D413/14 , C07D487/04 , C07D491/048
摘要： The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20130296377A1
公开(公告)日：2013-11-07
申请号：US13826725
申请日：2013-03-14
申请人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Xue LIANG , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
发明人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Xue LIANG , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
IPC分类号： C07D491/048 , A61K31/4184 , C07D413/06 , A61K45/06 , C07D403/14 , C07D401/14 , A61K31/4439 , C07D403/06 , A61K31/423
CPC分类号： A61K31/4184 , A61K31/423 , A61K31/4245 , A61K31/4439 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/14 , C07D413/06 , C07D413/14 , C07D487/04 , C07D491/048
摘要： The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20110092505A1
公开(公告)日：2011-04-21
申请号：US12996901
申请日：2009-06-12
申请人： Robin Burgis , Michael Paul Capparelli , Lucian Dipietro , Gabriel G. Gamber , Charles Francis Jewell, JR. , Erik Meredith , Karl Miranda , Lauren G. Monovich , Chang Rao , Nicolas Soldermann , Taeyoung Yoon , Qingming Zhu
发明人： Robin Burgis , Michael Paul Capparelli , Lucian Dipietro , Gabriel G. Gamber , Charles Francis Jewell, JR. , Erik Meredith , Karl Miranda , Lauren G. Monovich , Chang Rao , Nicolas Soldermann , Taeyoung Yoon , Qingming Zhu
IPC分类号： A61K31/535 , A61K31/4985 , A61K31/501 , A61K31/497 , A61K31/437 , A61K31/4545 , C07D417/14 , C07D487/04 , C07D413/14 , C07D471/04 , C07D401/14 , A61P17/00 , A61P9/00 , A61P35/00 , A61P37/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
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公开(公告)号：US09682968B2
公开(公告)日：2017-06-20
申请号：US14904694
申请日：2014-07-14
申请人： Christopher Michael Adams , Michael Paul Capparelli , Takeru Ehara , Rajeshri Ganesh Karki , Nello Mainolfi , Chun Zhang
发明人： Christopher Michael Adams , Michael Paul Capparelli , Takeru Ehara , Rajeshri Ganesh Karki , Nello Mainolfi , Chun Zhang
IPC分类号： C07D401/06 , A61K31/55 , C07D413/06 , C07D401/14 , C07D413/14 , C07D403/06 , C07D417/14 , A61K31/404 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/5377
CPC分类号： C07D413/06 , A61K31/404 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/55 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitors of the complement alternative pathway, in particular of Factor B. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20160024079A1
公开(公告)日：2016-01-28
申请号：US14774430
申请日：2014-03-13
申请人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Liang XUE , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
发明人： Christopher Michael ADAMS , Charles BABU , Michael Paul CAPPARELLI , Jian DING , Takeru EHARA , Keith JENDZA , Nan JI , Rajeshri Ganesh KARKI , Toshio KAWANAMI , Liang XUE , Nello MAINOLFI , James J. POWERS , Michael H. SERRANO-WU , Chun ZHANG
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.
摘要翻译： 本发明提供了式（I）化合物：其中X为N或CH，Y为NH，O或S，制备这些化合物的方法及其作为因子B抑制剂用于治疗与补体相关的病症和疾病的用途 替代途径激活如年龄相关性黄斑变性，糖尿病性视网膜病变和相关眼科疾病。 本发明还提供药物组合物和药理活性剂的组合。
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