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公开(公告)号：US09963454B2
公开(公告)日：2018-05-08
申请号：US14978059
申请日：2015-12-22
Applicant: Arnab K. Chatterjee , Kelli L. Kuhen , Advait S. Nagle , David C. Tully , Tao Wu
Inventor： Arnab K. Chatterjee , Kelli L. Kuhen , Advait S. Nagle , David C. Tully , Tao Wu
IPC: C07D345/00 , C07D487/04 , C07D487/14 , C07D519/00 , A61K31/4985 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D495/04 , C07F5/02
CPC classification number: C07D487/04 , A61K31/4985 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D487/14 , C07D495/04 , C07D519/00 , C07F5/022 , Y02A50/409 , Y02A50/411 , Y02A50/414
Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
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2.发明申请公开(公告)号：US20140039007A1
公开(公告)日：2014-02-06
申请号：US13993231
申请日：2011-11-30
Applicant: David C. Tully , Donatella Chianelli
Inventor： David C. Tully , Donatella Chianelli
IPC: C07D413/14 , A61K31/4545 , A61K45/06 , A61K31/454
CPC classification number: C07D413/14 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D413/12
Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
Abstract translation: 本发明涉及式I化合物，其立体异构体，对映异构体，药学上可接受的盐或氨基酸缀合物; 其中变量如本文所定义; 和它们的药物组合物，其可用作Farnesiod X受体（FXR）活性的调节剂。
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公开(公告)号：US20130331349A1
公开(公告)日：2013-12-12
申请号：US13993138
申请日：2011-11-30
Applicant: David C. Tully , Paul Vincent Rucker , Phillip B. Alper , Daniel Mutnick , Donatella Chianelli
Inventor： David C. Tully , Paul Vincent Rucker , Phillip B. Alper , Daniel Mutnick , Donatella Chianelli
IPC: C07D451/06 , C07H17/00 , A61K45/06 , A61K31/46 , A61K31/706 , A61K31/497 , A61K31/501 , A61K31/4709 , A61K31/5025 , C07D519/00 , A61K31/506
CPC classification number: A61K31/46 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/706 , A61K45/06 , C07D451/06 , C07D471/04 , C07D487/04 , C07D519/00 , C07H17/00
Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
Abstract translation: 本发明涉及式（I）的化合物，其立体异构体，对映异构体，其药学上可接受的盐或氨基酸缀合物; 其中变量如本文所定义; 和它们的药物组合物，其可用作Farnesiod X受体（FXR）活性的调节剂。
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公开(公告)号：US08338469B2
公开(公告)日：2012-12-25
申请号：US13089973
申请日：2011-04-19
Applicant: David C. Tully , Amab K. Chatterjee , Agnes Vidal , Hank Michael James Petrassi , Zhiwei Wang , Badry Bursulaya , Glen Spraggon
Inventor： David C. Tully , Amab K. Chatterjee , Agnes Vidal , Hank Michael James Petrassi , Zhiwei Wang , Badry Bursulaya , Glen Spraggon
IPC: A61K31/423 , C07D413/12
CPC classification number: C07D417/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
Abstract translation: 本发明提供了可用于调节通道活化蛋白酶的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与通道活化蛋白酶（包括但不限于前列腺素PRSS22，TMPRSS11）相关的病症的方法 （例如TMPRSS11B，TMPRSS11E），TMPRSS2，TMPRSS3，TMPRSS4（MTSP-2），matriptase（MTSP-1），CAP2，CAP3，胰蛋白酶，组织蛋白酶A或嗜中性粒细胞弹性蛋白酶。
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公开(公告)号：US20110257077A1
公开(公告)日：2011-10-20
申请号：US13089973
申请日：2011-04-19
Applicant: David C. Tully , Amab K. Chatterjee , Agnes Vidal , Hank Michael James Petrassi , Zhiwei Wang , Badry Bursulaya , Glen Spraggon
Inventor： David C. Tully , Amab K. Chatterjee , Agnes Vidal , Hank Michael James Petrassi , Zhiwei Wang , Badry Bursulaya , Glen Spraggon
CPC classification number: C07D417/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
Abstract translation: 本发明提供了可用于调节通道活化蛋白酶的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与通道活化蛋白酶（包括但不限于前列腺素PRSS22，TMPRSS11）相关的病症的方法 （例如TMPRSS11B，TMPRSS11E），TMPRSS2，TMPRSS3，TMPRSS4（MTSP-2），matriptase（MTSP-1），CAP2，CAP3，胰蛋白酶，组织蛋白酶A或嗜中性粒细胞弹性蛋白酶。
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Patent Agency Ranking
公开(公告)号：US20110245243A1
公开(公告)日：2011-10-06
申请号：US13161555
申请日：2011-06-16
Applicant: Hong LIU , David C. TULLY , Arnab CHATTERJEE , Phillip B. ALPER , David H. WOODMANSEE , Daniel MUTNICK
Inventor： Hong LIU , David C. TULLY , Arnab CHATTERJEE , Phillip B. ALPER , David H. WOODMANSEE , Daniel MUTNICK
IPC: A61K31/5377 , A61K31/5375 , A61K31/454 , A61K31/4245 , A61K31/423 , C07D413/12 , C07D265/30 , A61P43/00 , C07D417/12
CPC classification number: C07D263/56 , C07D211/66 , C07D273/02 , C07D277/64 , C07D295/185 , C07D307/30
Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
Abstract translation: 本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与组织蛋白酶S活性相关的疾病或病症的方法。
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公开(公告)号：US07939547B2
公开(公告)日：2011-05-10
申请号：US11749001
申请日：2007-05-15
Applicant: David C. Tully , Arnab K. Chatterjee , Hank Michael James Petrassi , Badry Bursulaya , Glen Spraggon
Inventor： David C. Tully , Arnab K. Chatterjee , Hank Michael James Petrassi , Badry Bursulaya , Glen Spraggon
IPC: A61K31/454 , C07D403/02
CPC classification number: C07K5/0806 , A61K38/00 , C07K5/06165
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
Abstract translation: 本发明提供了可用于调节通道活化蛋白酶的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与通道活化蛋白酶相关的病症的方法，包括但不限于前列腺素PRSS22，TMPRSS11（ 例如TMPRSS11B，TMPRSS11E），TMPRSS2，TMPRSS3，TMPRSS4（MTSP-2），matriptase（MTSP-1），CAP2，CAP3，胰蛋白酶，组织蛋白酶A或嗜中性粒细胞弹性蛋白酶。
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8.发明申请公开(公告)号：US20100239551A1
公开(公告)日：2010-09-23
申请号：US12525991
申请日：2008-01-04
Applicant: David C. Tully , Arnab K. Chatterjee , Agnes Vidal , Badry Bursulaya
Inventor： David C. Tully , Arnab K. Chatterjee , Agnes Vidal , Badry Bursulaya
IPC: A61K31/437 , C07D227/04 , A61K31/454 , C07D401/14 , A61K31/4545 , C07D471/04 , C07D263/58 , A61K31/423 , A61K38/43 , A61P11/00 , A61P35/00 , A61P29/00 , A61P37/08 , C12N5/071
CPC classification number: C07K5/06086 , C07D413/12 , C07D413/14 , C07K5/06191
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
Abstract translation: 本发明提供了可用于调节链激酶活化蛋白酶的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与通道活化蛋白酶相关的病症的方法，包括但不限于前列腺素PRSS22， TMPRSS11（例如TMPRSS11B，TMPRSSI1E），TMPRSS2，TMPRSS3，TMPRSS4（MTSP-2），matriptase（MTSP-1），CAP2，CAP3，胰蛋白酶，组织蛋白酶A或嗜中性粒细胞弹性蛋白酶。
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公开(公告)号：US20100204200A1
公开(公告)日：2010-08-12
申请号：US12764772
申请日：2010-04-21
Applicant: Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
Inventor： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
IPC: A61K31/5377 , C07D413/12 , C07D295/145 , C07D413/14 , C07C245/00 , C07D401/12 , C07D403/12 , A61K31/5375 , A61K31/54 , A61K31/496 , A61K31/404
CPC classification number: C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.
Abstract translation: 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供了具有式1的化合物：其中Q是任选取代的氮杂环丁烷基，吡咯烷基，哌啶基和二氢吲哚基; 或Q为NR25R26; A，R 5，R 6，R 7，R 8，R 9，R 25，R 26和Ar为取代基。
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公开(公告)号：US09469645B2
公开(公告)日：2016-10-18
申请号：US13912898
申请日：2013-06-07
Applicant: Arnab K. Chatterjee , Advait S. Nagle , Tao Wu , David C. Tully , Kelli L. Kuhen
Inventor： Arnab K. Chatterjee , Advait S. Nagle , Tao Wu , David C. Tully , Kelli L. Kuhen
IPC: A61K31/397 , C07D487/04 , C07D487/14 , C07D519/00 , A61K31/4985 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D495/04 , C07F5/02
CPC classification number: C07D487/04 , A61K31/4985 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D487/14 , C07D495/04 , C07D519/00 , C07F5/022 , Y02A50/409 , Y02A50/411 , Y02A50/414
Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
Abstract translation: 本发明提供一类化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防疟疾的方法。
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