公开(公告)号：US11939302B2

公开(公告)日：2024-03-26

申请号：US17505250

申请日：2021-10-19

申请人： The Governors of the University of Alberta

发明人： James A. Nieman ,  Jack Jhamandas ,  Bing Bai ,  Alexandr Belovodskiy ,  Wen Fu ,  Mostofa Hena ,  Michael Houghton ,  Appan Srinivas Kandadai ,  Ryoichi Kimura ,  Kamlesh Kumar Sahu ,  D. Lorne Tyrrell

IPC分类号： A61K31/55 ,  A61P25/28 ,  C07D241/44 ,  C07D243/12 ,  C07D243/14 ,  C07D403/12

CPC分类号： C07D243/12 ,  A61P25/28 ,  C07D241/44 ,  C07D243/14 ,  C07D403/12

摘要： The present disclosure provides compounds that are amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.

公开(公告)号：US20240002353A1

公开(公告)日：2024-01-04

申请号：US18252039

申请日：2021-10-25

申请人： NINGBO COMBIREG PHARMACEUTICAL TECHNOLOGY CO., LTD.

发明人： Gang LIU ,  Yao MA ,  Wenjun YU

IPC分类号： C07D243/14 ,  A61P35/00

CPC分类号： C07D243/14 ,  A61P35/00 ,  C07B2200/05

摘要： Disclosed are a deuterated 1,4-benzodiazepine-2,5-dione compound and the use thereof. Provided is a compound as represented by formula I or a pharmaceutically acceptable salt thereof. The disclosed 1,4-benzodiazepine-2,5-dione active compound maintains the activity of inhibiting tumor cells and tumor stem cells, and prolongs the degradation function of in-vitro human liver microsomes on the compound, such that the half-life period is significantly prolonged, which provides a safer and more reliable candidate for developing new anti-tumor drugs.

公开(公告)号：US20230083960A1

公开(公告)日：2023-03-16

申请号：US17453761

申请日：2021-11-05

申请人： Cytokinetics, Inc.

发明人： Bradley P. MORGAN ,  Chris Evans ,  Pu-Ping Lu ,  Makoto Yamasaki ,  Wenyue Wang ,  Scott Collibee ,  Takuya Makino ,  Kazuyuki Tsuchiya ,  Toshio Kurosaki ,  Susumu Yamaki ,  Eriko Honjo ,  Yuka Koizumi ,  Naoto Katoh ,  Ryuichi Sekioka ,  Ikumi Kuriwaki ,  Denise Andersen

IPC分类号： C07D243/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D405/14 ,  C07D401/12 ,  C07D403/14 ,  C07D519/00 ,  C07D413/12 ,  C07D471/10 ,  C07D417/12 ,  C07D413/08

摘要： Provided herein are compounds of formula (I): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X1, X2, Ry, Rz, R1, R2, R3, and R4 are as defined herein.
Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing.
Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.

公开(公告)号：US20210040050A1

公开(公告)日：2021-02-11

申请号：US17077857

申请日：2020-10-22

申请人： Ayala Pharmaceuticals Inc.

发明人： Matti Davis

IPC分类号： C07D243/14 ,  A61K9/00 ,  A61P35/00

摘要： The present invention provides compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds, including compounds of Formula (I) or prodrugs thereof; in combination with an additional cancer therapeutic agent, and methods of use thereof for treating diseases and disorders such as cancer.

公开(公告)号：US10457652B2

公开(公告)日：2019-10-29

申请号：US16219648

申请日：2018-12-13

申请人： FORMA Therapeutics, Inc.

发明人： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Heather Davis ,  Aleksandra Rudnitskaya ,  David R. Lancia, Jr. ,  Kenneth W. Bair ,  David S. Millan ,  Matthew W. Martin

IPC分类号： A61K31/5513 ,  C07D243/14 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D413/06 ,  C07D417/06 ,  C07D267/14 ,  C07D413/12 ,  C07D413/04 ,  C07D291/08 ,  C07D405/06 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/08 ,  C07D493/08 ,  C07D413/08 ,  C07D491/107 ,  C07D495/10 ,  C07D267/12

摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20190119228A1

公开(公告)日：2019-04-25

申请号：US16219592

申请日：2018-12-13

申请人： FORMA Therapeutics, Inc.

发明人： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Heather Davis ,  Aleksandra Rudnitskaya ,  David R. Lancia, Jr. ,  Kenneth W. Bair ,  David S. Millan ,  Matthew W. Martin

IPC分类号： C07D267/14 ,  C07D413/04 ,  C07D267/12 ,  C07D413/06 ,  C07D401/06 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D243/14 ,  C07D291/08 ,  C07D498/08 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D495/10 ,  C07D491/107 ,  C07D413/08 ,  C07D493/08 ,  C07D413/12

摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20190112283A1

公开(公告)日：2019-04-18

申请号：US16218132

申请日：2018-12-12

申请人： FORMA Therapeutics, Inc.

发明人： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR. ,  David S. Millan ,  Matthew W. Martin ,  Kenneth W. Bair

IPC分类号： C07D267/14 ,  C07D413/04 ,  C07D267/12 ,  C07D413/06 ,  C07D401/06 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D243/14 ,  C07D291/08 ,  C07D498/08 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D495/10 ,  C07D491/107 ,  C07D413/08 ,  C07D493/08 ,  C07D413/12

摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US10246460B2

公开(公告)日：2019-04-02

申请号：US15172542

申请日：2016-06-03

申请人： Hoffmann-La Roche Inc.

发明人： Benno Rothenhaeusler ,  Rene Trussardi ,  Fabienne Hoffmann-Emery ,  Urs Schwitter ,  Jean-Michel Adam ,  Olaf Grassmann ,  Thomas Hartung ,  Frederic Ran ,  Ralph Diodone ,  Christophe Pfleger ,  Bjorn Bartels

IPC分类号： C07D487/04 ,  C07D243/14

摘要： The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.

公开(公告)号：US10239845B2

公开(公告)日：2019-03-26

申请号：US15013816

申请日：2016-02-02

申请人： Forma Therapeutics, Inc.

发明人： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Aleksandra Rudnitskaya ,  David R. Lancia, Jr. ,  David S. Millan ,  Matthew W. Martin

IPC分类号： A61K31/553 ,  C07D267/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/04 ,  C07D243/14 ,  C07D291/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/08 ,  C07D493/08 ,  C07D413/08 ,  C07D491/107 ,  C07D495/10 ,  C07D267/12

摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US09676760B2

公开(公告)日：2017-06-13

申请号：US15152231

申请日：2016-05-11

申请人： Gilead Sciences, Inc.

发明人： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC分类号： C07D413/06 ,  A61K31/553 ,  A61K31/5513 ,  C07D267/08 ,  C07D243/24 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/12 ,  C07D413/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D243/14 ,  C07B59/00 ,  C07D413/04 ,  C07D417/14

CPC分类号： C07D413/06 ,  A61K31/5513 ,  A61K31/553 ,  C07B59/002 ,  C07B2200/05 ,  C07D243/14 ,  C07D243/24 ,  C07D267/08 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.