公开(公告)号：US10508128B2

公开(公告)日：2019-12-17

申请号：US15548713

申请日：2016-02-09

申请人： INDOCO REMEDIES LIMITED

发明人： Ranjeet Nair ,  Palangat Vayalileveetil Ramesan ,  Sandip Kacharu Deshmukh ,  Aditi Milind Panandikar

IPC分类号： C07H7/04 ,  C07H1/00

摘要： The present invention DISCLOSES a novel process for preparing sodium glucose transporters 2 (SGLT2) inhibitor compounds of Formula IX. Wherein, R is halogen, alkyl or alkoxy group; and Ar is aryl group, substituted or unsubstituted monocyclic polycyclic or heterocyclic ring selected from the residues A, B, C or D as given below,

公开(公告)号：US20190284220A1

公开(公告)日：2019-09-19

申请号：US16317636

申请日：2017-07-21

申请人： Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

发明人： Xiang LI ,  Jun YU ,  Haizhou YU ,  Jinjia WANG ,  Lei HE ,  Zuyin DU

IPC分类号： C07H7/04

摘要： Disclosed are a crystal form of a dapagliflozin intermediate and a preparation method therefor, and specifically disclosed are a crystal form of the dapagliflozin intermediate (2S,3R,4S,5S,6R)-2-(4-chloro-3 -(4-ethoxybenzyOphenyl)-2-ethoxy-6-(methylhydroxyl) tetrahydro-2H-pyran-3,4,5-triol and a preparation method therefor. The advantages thereof lie in that an intermediate can be highly purified to obtain a sample with a purity of 99.3% or more, which has an important significance for improving the quality of the dapagliflozin, and the preparation process is simple and suitable for industrial production.

公开(公告)号：US20190106450A1

公开(公告)日：2019-04-11

申请号：US15945221

申请日：2018-04-04

申请人： Vertex Pharmaceuticals Incorporated

发明人： Yeeman K. Ramtohul ,  Sanjoy Kumar Das ,  Caroline Cadilhac ,  Thumkunta Jagadeeswar Reddy ,  Louis Vaillancourt ,  Michel Gallant ,  Bingcan Liu ,  Evelyne Dietrich ,  Frederic Vallee ,  Julien Martel ,  Carl Poisson

IPC分类号： C07H7/02 ,  A61K31/7064 ,  C07D405/14 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7028 ,  C07D495/04 ,  C07D407/14 ,  C07D413/14 ,  C07H19/02 ,  C07H7/06 ,  C07H7/04 ,  C07D417/14 ,  C07H19/056 ,  C07D409/14 ,  C07H15/26 ,  C07D309/10

摘要： The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

公开(公告)号：US20180346502A1

公开(公告)日：2018-12-06

申请号：US15990860

申请日：2018-05-29

申请人： Emmennar Pharma Private Limited

发明人： Maha Vishnu Mundla ,  Sridhar Malyala ,  Chandra Prakash Narani ,  Laxmi Narasimha Varaprasad Chintaginjala ,  Suresh Kumar Gunukula ,  Bala Yellaiah Chittiboyina ,  Prabhakar Bellam ,  Hemalatha Reddy Samireddy ,  Sowmya Dantham ,  Prasad Vure ,  Pooja Kale

IPC分类号： C07H7/04 ,  C07C41/18 ,  C07H7/06 ,  A61K9/10 ,  A61K47/38 ,  C07D307/20

CPC分类号： C07H7/04 ,  A61K9/10 ,  A61K9/146 ,  A61K47/38 ,  C07B2200/07 ,  C07C41/18 ,  C07D307/20 ,  C07H7/06 ,  C07C43/225

摘要： The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

公开(公告)号：US10011627B2

公开(公告)日：2018-07-03

申请号：US14917792

申请日：2014-08-19

申请人： YOUNGENE THERAPEUTICS CO., LTD

发明人： Huijuan Zhong ,  Jianchun Liao ,  Hongping Yu ,  Yaochang Xu ,  Qing Li ,  Jianghua Chen ,  Peng Gao ,  Songliang Tan ,  Shaobao Wang

IPC分类号： C07H7/06 ,  C07H9/04 ,  C07D409/10 ,  C07D409/14 ,  A61K31/00 ,  C07H7/04 ,  A61K31/7048 ,  C07D493/08

CPC分类号： C07H7/06 ,  A61K31/00 ,  A61K31/7048 ,  C07D409/10 ,  C07D409/14 ,  C07D493/08 ,  C07H7/04 ,  C07H9/04

摘要： C-aryl glucoside derivatives, preparation methods thereof, and medical applications thereof are described. Specifically, compounds represented by formula I, and, tautomers, enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts of the compounds, preparation methods thereof, pharmaceutical compositions containing the compounds, and applications thereof are described. Compounds of formula (I) are useful as therapeutic agents, and particularly as sodium-dependent glucose contransporter protein (SGLT) inhibitors.

公开(公告)号：US20180127391A1

公开(公告)日：2018-05-10

申请号：US15571112

申请日：2016-05-04

申请人： Glenmark Pharmaceuticals Limited

发明人： Shekhar Bhaskar Bhirud ,  Kumar Hari BHUSHAN ,  Raghu Ram SURAPARAJU ,  Nandkumar GAIKWAD ,  Sharad GORE ,  Rajendra JAGDHANE ,  Mandar KULKARNI

IPC分类号： C07D309/10 ,  C07C31/20 ,  C07H7/04 ,  C07B51/00 ,  C07B63/04 ,  B01D9/00

CPC分类号： C07D309/10 ,  A61K31/70 ,  B01D9/0054 ,  C07B51/00 ,  C07B63/04 ,  C07C31/207 ,  C07H7/04

摘要： The present invention relates to a process for the preparation of amorphous dapagliflozin. The present invention relates to 2,3-butanediol solvate of dapagliflozin and process for its preparation.

公开(公告)号：US09902751B2

公开(公告)日：2018-02-27

申请号：US15105620

申请日：2014-12-29

申请人： Mylan Laboratories Ltd.

发明人： Vipin Kumar Kaushik ,  Jagan Mohana Chary Tummanepally ,  Jayaram Pothani ,  Ramarao Dodda

IPC分类号： C07H7/06 ,  C07H1/00 ,  C07H7/04 ,  C07H15/04 ,  C07D407/12 ,  C07H23/00 ,  C07D307/20

CPC分类号： C07H7/06 ,  C07D307/20 ,  C07D407/12 ,  C07H1/00 ,  C07H7/04 ,  C07H15/04 ,  C07H23/00 ,  Y02P20/55

摘要： An improved process for the preparation of empagliflozin is disclosed. Novel intermediates of formulas (13) and (14) for the preparation of empagliflozin are also disclosed, wherein R1 and R2 are independently hydrogen or hydroxyl protecting groups.

公开(公告)号：US09834573B2

公开(公告)日：2017-12-05

申请号：US14627693

申请日：2015-02-20

申请人： Theracos Sub, LLC

发明人： Mengzhuang Cai ,  Qian Liu ,  Ge Xu ,  Binhua Lv ,  Brian Seed ,  Jacques Y. Roberge

IPC分类号： C07H7/04 ,  C07H1/06 ,  C07D309/10

CPC分类号： C07H1/06 ,  C07D309/10 ,  C07H7/04

摘要： Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.

公开(公告)号：US09598454B2

公开(公告)日：2017-03-21

申请号：US14132662

申请日：2013-12-18

申请人： Vertex Pharmaceuticals Incorporated

发明人： Yeeman K. Ramtohul ,  Sanjoy Kumar Das ,  Caroline Cadilhac ,  Thumkunta Jagadeeswar Reddy ,  Louis Vaillancourt ,  Michel Gallant ,  Bingcan Liu ,  Evelyne Dietrich ,  Frederic Vallee ,  Julien Martel ,  Carl Poisson

IPC分类号： C07H19/02 ,  C07H7/04 ,  C07H7/06 ,  C07H7/02 ,  C07D405/14 ,  C07D309/10 ,  C07H15/26 ,  C07D409/14 ,  C07H19/056 ,  C07D417/14 ,  C07D413/14 ,  C07D407/14 ,  C07D495/04

CPC分类号： C07H7/02 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7064 ,  C07D309/10 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04 ,  C07H7/04 ,  C07H7/06 ,  C07H15/26 ,  C07H19/02 ,  C07H19/056

摘要： The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

公开(公告)号：US09243019B2

公开(公告)日：2016-01-26

申请号：US14383557

申请日：2013-06-08

申请人： ZHEJIANG YONGNING PHARMACEUTICAL CO LTD

发明人： Fengqi Ye ,  Ben Cai ,  Min Lu ,  Yongling Chen

IPC分类号： C07H7/04 ,  C07H15/207 ,  C07D309/04

CPC分类号： C07H15/207 ,  C07D309/04 ,  C07H7/04

摘要： A hydroxysafflor yellow A sodium compound as shown in a formula (I) and preparation as well as medicinal application thereof are provided. According to the present invention, the safflower is utilized as a raw material. A monomer pharmaceutical compound, the hydroxysafflor yellow A sodium, is obtained by sufficient processes, and a purity thereof is surely above 98.5%. Therefore, the hydroxysafflor yellow A sodium is a monomer compound, which is safer, more effective, more stable and more controllable than hydroxysafflor yellow A, for treating blood circulation disorders such as platelet aggregation, coronary heart disease, angina pectoris and acute cerebral ischemia. Furthermore, the hydroxysafflor yellow A sodium has sufficient solubility and human tolerance.