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公开(公告)号：US09040706B2
公开(公告)日：2015-05-26
申请号：US14088110
申请日：2013-11-22
Applicant: Genentech, Inc.
Inventor： Frederick Cohen , Vickie Hsiao-Wei Tsui , Cuong Ly , John A. Flygare
IPC: C07D277/20 , C07D453/02 , C07D471/14 , C07D471/04 , C07D417/04 , C07D417/14
CPC classification number: C07D471/04 , C07D417/04 , C07D417/14
Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4′, R5, R6 and R6′ are as described herein.
Abstract translation: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式I：其中A，Q，X 1，X 2，Y，R 1，R 2，R 3，R 4，R 4'，R 5，R 6 和R6'如本文所述。
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公开(公告)号：US20180244694A1
公开(公告)日：2018-08-30
申请号：US15962333
申请日：2018-04-25
Applicant: Genentech, Inc.
Inventor： Yu Jiang , Guosheng Wu , Po-Wai Yuen , Elisia Villemure , Jacob Schwarz , Cuong Ly , Benjamin Sellers , Matthew Volgraf
IPC: C07D513/14 , C07D519/00 , C07D513/04 , C07D513/10
CPC classification number: C07D513/14 , C07D513/04 , C07D513/10 , C07D519/00
Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US20150080367A1
公开(公告)日：2015-03-19
申请号：US14550528
申请日：2014-11-21
Applicant: Genentech, Inc.
Inventor： Frederick Cohen , Malcolm Huestis , Cuong Ly , Snahel Patel , Michael Siu , Xianrui Zhao
IPC: C07D401/14 , C07D491/107 , C07D487/08 , C07D405/14
CPC classification number: C07D401/14 , C07D401/12 , C07D405/14 , C07D487/08 , C07D491/107
Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.
Abstract translation: 本发明提供式I化合物及其各种实施方案，以及包含式I化合物及其各种实施方案的组合物。 在式I化合物中，基团R 1，R 2，R 3，R 4，R 5，R 6，m，n和C连接的环具有如本文所述的含义。 本发明还提供使用式I化合物的方法和包含式I化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症。
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公开(公告)号：US10968203B2
公开(公告)日：2021-04-06
申请号：US15989008
申请日：2018-05-24
Inventor： Marie-Gabrielle Braun , Paul Gibbons , Wendy Lee , Cuong Ly , Joachim Rudolph , Jacob Schwarz , Avi Ashkenazi , Leo Fu , Tommy Lai , Fei Wang , Ramsay Beveridge , Liang Zhao
IPC: A61K31/506 , A61K45/06 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61P35/00
Abstract: Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I or I′ structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I or I′ compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号：US10647731B2
公开(公告)日：2020-05-12
申请号：US15962333
申请日：2018-04-25
Applicant: Genentech, Inc.
Inventor： Yu Jiang , Guosheng Wu , Po-Wai Yuen , Elisia Villemure , Jacob Schwarz , Cuong Ly , Benjamin Sellers , Matthew Volgraf
IPC: C07D513/14 , C07D513/04 , C07D513/10 , C07D519/00
Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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Patent Agency Ranking
公开(公告)号：US10392422B2
公开(公告)日：2019-08-27
申请号：US15312614
申请日：2015-05-19
Applicant: RQX PHARMACEUTICALS, INC. , GENENTECH, INC.
Inventor： Tucker Curran Roberts , Peter Andrew Smith , Robert I. Higuchi , Prasuna Paraselli , Philippe Bergeron , Michael F. T. Koehler , Huiyong Hu , Jacob Bradley Schwarz , Cuong Ly , James John Crawford
IPC: A61K38/00 , C07K5/103 , C07K7/06 , C07K7/08 , C07K5/02 , C07K5/087 , C07K5/09 , C07K5/11 , A61K45/06 , A61K31/395 , A61K31/407 , A61K31/4196 , A61K31/43 , A61K31/431 , A61K31/496 , A61K31/545 , A61K31/546 , A61K38/06 , A61K38/07 , A61K38/08 , C07K5/083 , A61K38/12
Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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7.发明申请公开(公告)号：US20180265497A1
公开(公告)日：2018-09-20
申请号：US15989008
申请日：2018-05-24
Inventor： Marie-Gabrielle Braun , Paul Gibbons , Wendy Lee , Cuong Ly , Joachim Rudolph , Jacob Schwarz , Avi Ashkenazi , Leo Fu , Tommy Lai , Fei Wang , Ramsay Beveridge , Liang Zhao
IPC: C07D401/14 , A61K31/506 , C07D401/04 , C07D405/14 , C07D417/14 , C07D413/14 , A61K45/06
CPC classification number: C07D401/14 , A61K31/506 , A61K45/06 , A61P35/00 , C07D401/04 , C07D405/14 , C07D413/14 , C07D417/14
Abstract: Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I or I′ structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I or I′ compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号：US09399636B2
公开(公告)日：2016-07-26
申请号：US14550528
申请日：2014-11-21
Applicant: Genentech, Inc.
Inventor： Frederick Cohen , Malcolm Huestis , Cuong Ly , Snahel Patel , Michael Siu , Xianrui Zhao
IPC: C07D401/14 , C07D401/12 , C07D405/14 , C07D487/08 , C07D491/107
CPC classification number: C07D401/14 , C07D401/12 , C07D405/14 , C07D487/08 , C07D491/107
Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.
Abstract translation: 本发明提供式I化合物及其各种实施方案，以及包含式I化合物及其各种实施方案的组合物。 在式I化合物中，基团R 1，R 2，R 3，R 4，R 5，R 6，m，n和C连接的环具有如本文所述的含义。 本发明还提供使用式I化合物的方法和包含式I化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症。
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公开(公告)号：US10351595B2
公开(公告)日：2019-07-16
申请号：US15312614
申请日：2015-05-19
Applicant: RQX PHARMACEUTICALS, INC. , GENENTECH, INC.
Inventor： Tucker Curran Roberts , Peter Andrew Smith , Robert I. Higuchi , Prasuna Paraselli , Philippe Bergeron , Michael F. T. Koehler , Huiyong Hu , Jacob Bradley Schwarz , Cuong Ly , James John Crawford
IPC: A61K38/00 , C07K5/103 , C07K7/06 , C07K7/08 , C07K5/02 , C07K5/087 , C07K5/09 , C07K5/11 , A61K45/06 , A61K31/395 , A61K31/407 , A61K31/4196 , A61K31/43 , A61K31/431 , A61K31/496 , A61K31/545 , A61K31/546 , A61K38/06 , A61K38/07 , A61K38/08 , C07K5/083 , A61K38/12
Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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公开(公告)号：US09988400B2
公开(公告)日：2018-06-05
申请号：US15094687
申请日：2016-04-08
Applicant: Genentech, Inc.
Inventor： Yu Jiang , Guosheng Wu , Po-Wai Yuen , Elisia Villemure , Jacob Schwarz , Cuong Ly , Benjamin Sellers , Matthew Volgraf
IPC: C07D513/04 , C07D513/10 , C07D513/14 , C07D519/00
CPC classification number: C07D513/14 , C07D513/04 , C07D513/10 , C07D519/00
Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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