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1. 发明申请

US20230083960A1 BICYCLIC 1,4-DIAZEPANONES AND THERAPEUTIC USES THEREOF 有权
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.

2. 发明申请

US20210040050A1 COMBINATION COMPOSITIONS COMPRISING BISFLUOROALKYL-1,4- BENZODIAZEPINONE COMPOUNDS AND METHODS OF USE THEREOF 有权
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.

3. 发明授权

US10457652B2 3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors 有权
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.

4. 发明申请

US20190119228A1 3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS 审中-公开
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.

5. 发明申请

US20190112283A1 3-ALKYL BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS 审中-公开
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.

6. 发明授权

US10246460B2 Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[E]azulene and crytalline forms thereof 有权
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.

7. 发明授权

US10239845B2 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors 有权
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.

8. 发明授权

US09676760B2 Fused heterocyclic compounds as ion channel modulators 有权
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.

9. 发明授权

US09580394B2 Benzodiazepine derivative and method of producing the same 有权
标题翻译：苯并二氮杂衍生物及其制备方法
公开(公告)号：US09580394B2
公开(公告)日：2017-02-28
申请号：US14200393
申请日：2014-03-07
申请人： ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCH
发明人： Yu Chang , Ching-Yun Lee , Tsung-Hsien Chiang , Cheng-Fang Hsu
IPC分类号： C07D243/14 , C07D243/12
CPC分类号： C07D243/12
摘要： In a benzodiazepine derivative and a method of producing the derivative, isatoic anhydride or 5-chloroisatoic anhydride is reacted with amino acid ester hydrochloride for conducting a simple cyclization to obtain a produce with a low percentage of by-product directly without requiring the complicated separation and purification processes of column chromatography, and a chlorine-containing structure of the structure can improve the lipo-solubility and chlorine ion permeability and allow a functional group of a radioisotope to be modified to maximize the effects of the pharmacological properties such as the sedative, anticonvulsant and anti-spasmodic effects on the central nervous system or the benzodiazepine derivative can be used as a contrast agent of the system with excellent effects on applications.
摘要翻译：在苯并二氮杂衍生物和衍生物的制造方法中，将丙酸酐或5-氯代酸酐与氨基酸酯盐酸盐反应，进行简单的环化，直接得到副产物的百分比低的产物，无需复杂的分离，柱层析的纯化方法和结构的含氯结构可以改善脂溶性和氯离子渗透性，并允许改性放射性同位素的官能团以最大化药理学性质的影响，例如镇静剂，抗惊厥药对中枢神经系统或苯并二氮杂衍生物的抗痉挛作用可用作系统的造影剂，对应用效果优异。

10. 发明申请

US20160272596A1 TETRAHYDRO-BENZODIAZEPINONES 审中-公开
标题翻译：四氢苯并噻唑酮
公开(公告)号：US20160272596A1
公开(公告)日：2016-09-22
申请号：US15037240
申请日：2014-11-14
申请人： HOFFMANN-LA ROCHE AG
发明人： Shaoqing Chen , Andrew F. Donnell , Robert Francis Kester , Kang Le , Yan Lou , Christophe Michoud , Stacy Remiszewski , Kenneth C. Rupert , Martin Weisel
IPC分类号： C07D243/14 , C07D403/06 , C07D405/06 , C07D413/06 , C07D401/06 , C07D403/12
CPC分类号： C07D243/14 , C07D243/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/14 , C07D413/06 , C07D417/12 , C07D487/08
摘要： Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3, R4 and R5 are as described in this application, and methods of using said compounds in the treatment of cancer.

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