公开(公告)号：US20200002356A1

公开(公告)日：2020-01-02

申请号：US16567852

申请日：2019-09-11

申请人： EUTICALS SPA

发明人： Paride Grisenti ,  Maria Argese ,  Daniele Pengo ,  Maria Donata Grilli ,  Emanuela Fumagalli ,  Giuseppe Motta

IPC分类号： C07D498/22 ,  A61K9/20 ,  A61K9/28 ,  A61K31/437

摘要： A Rifaximin polymorphic mixture of α/β form in a relative ratio of 85/15±3 and a process for its preparation. The polymorphic mixture of Rifaximin is for use as a medicament, in particular in the treatment of traveler's diarrhea and hepatic encephalopathy. A pharmaceutical composition comprises the polymorphic mixture of Rifaximin as active ingredient, in particular, a solid formulation, more in particular, a film coated tablet. A polymorphic form of crude wet rifaximin and of purified wet rifaximin their use are used as intermediates in a process for the preparation of Rifaximin polymorphic mixture of α/β form in a relative ratio of 85/15±3.

公开(公告)号：US10519168B2

公开(公告)日：2019-12-31

申请号：US15639833

申请日：2017-06-30

申请人： Gilead Sciences, Inc.

发明人： John Enquist, Jr. ,  Nolan Griggs ,  Christopher Hale ,  Norihiro Ikemoto ,  Andrew W. Waltman

IPC分类号： C07D317/26 ,  C07C235/80 ,  C07C231/02 ,  C07C237/16 ,  C07D498/14 ,  C07D319/06 ,  C07C237/20 ,  C07D213/82 ,  C07D309/40 ,  C07D498/22 ,  C07C231/12

摘要： Methods of making compounds of Formula I are disclosed:

公开(公告)号：US20190330235A1

公开(公告)日：2019-10-31

申请号：US16507523

申请日：2019-07-10

申请人： Genentech, Inc.

发明人： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQing Wei

IPC分类号： C07D498/22 ,  C07D498/20 ,  A61K31/5377 ,  C07D471/14 ,  C07D498/14 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/395 ,  C07D491/147 ,  C07D495/14 ,  C07D491/14 ,  C07D487/14 ,  C07K16/22

摘要： Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

公开(公告)号：US20190330234A1

公开(公告)日：2019-10-31

申请号：US16404638

申请日：2019-05-06

申请人： JANSSEN SCIENCES IRELAND UNLIMITED COMPANY

发明人： Jean-François BONFANTI ,  Jérôme Michel Claude FORTIN ,  Frédéric Marc Maurice DOUBLET ,  Pierre Jean-Marie Bernard RABIOSSON ,  Eric Pierre Alexandre ARNOULT

IPC分类号： C07D498/22 ,  C07D487/22 ,  C07D487/16 ,  C07D498/16

摘要： This invention relates macrocyclic purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

公开(公告)号：US10377772B2

公开(公告)日：2019-08-13

申请号：US15511879

申请日：2015-09-17

申请人： Oncodesign S.A.

发明人： Jan Hoflack ,  Petra Blom ,  Olivier Lavergne ,  Sylvie Gomez

IPC分类号： C07D487/22 ,  C07D498/22

摘要： The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

公开(公告)号：US10364226B2

公开(公告)日：2019-07-30

申请号：US15021073

申请日：2014-09-10

申请人： Alios BioPharma, Inc.

发明人： Leonid Beigelman ,  Robert Than Hendricks ,  Antitsa Dimitrova Stoycheva ,  Jerome Deval ,  Sarah Katherine Stevens

IPC分类号： C07D237/20 ,  C07D237/24 ,  C07D403/12 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/06 ,  C07D471/04 ,  C07D498/22 ,  C07D471/22 ,  C07D498/10 ,  C07D519/00 ,  A61K31/245 ,  A61K31/50 ,  A61K31/501 ,  A61K31/504 ,  A61K31/506 ,  A61K31/529 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D487/18 ,  C07D487/22 ,  C07D498/08 ,  C07D498/18

摘要： Disclosed herein are pyridazinone compounds, pharmaceutical compositions that include one or more pyridazinone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with a pyridazinone compounds. Examples of an orthomyxovirus viral infection includes an influenza infection.

公开(公告)号：US10292972B1

公开(公告)日：2019-05-21

申请号：US15794665

申请日：2017-10-26

申请人： King Abdulaziz University

发明人： Jamal Sabir M. Sabir ,  Abdullah Y. Obaid ,  Nahid H. Hajrah ,  Waseem Mohammed ,  Zainab H. Abdul-Hameed ,  Walied M. Alarif ,  Roop Singh Bora ,  Seif-Eldin N. Ayyad ,  Nouf Saeed A. Al-Abbas ,  Abdulkader M. Shaikh Omer ,  Mohammed Zainy Mutawakil ,  Neil Hall ,  Kulvinder Singh Saini

IPC分类号： A61K31/439 ,  C07D498/22 ,  A61K36/24 ,  B01D11/02 ,  B01D15/12 ,  B01D15/42

摘要： A pharmaceutical composition containing an anticancer compound, named isopicrinine, isolated from the plant Rhazya Stricta. The pharmaceutical composition may contain a salt, an analog, a derivative, and/or the prodrug of isopicrinine. A method of treating cancer with the pharmaceutical composition is disclosed. A method of extracting isopicrinine is also disclosed.

公开(公告)号：US20190127376A1

公开(公告)日：2019-05-02

申请号：US16152827

申请日：2018-10-05

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Liangxing Wu ,  Colin Zhang ,  Chunhong He ,  Yaping Sun ,  Liang Lu ,  Ding-Quan Qian ,  Meizhong Xu ,  Jincong Zhuo ,  Wenqing Yao

IPC分类号： C07D471/14 ,  C07D491/22 ,  C07D471/22 ,  C07D495/14 ,  C07D498/14 ,  C07D471/20 ,  C07D498/22

摘要： The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

公开(公告)号：US20190125732A1

公开(公告)日：2019-05-02

申请号：US15794665

申请日：2017-10-26

申请人： King Abdulaziz University

发明人： Jamal Sabir M. SABIR ,  Abdullah Y. OBAID ,  Nahid H. HAJRAH ,  Waseem MOHAMMED ,  Zainab H. ABDUL-HAMEED ,  Walied M. ALARIF ,  Roop Singh BORA ,  Seif-Eldin N. AYYAD ,  Nouf Saeed A. AL-ABBAS ,  Abdulkader M. Shaikh OMER ,  Mohammed Zainy MUTAWAKIL ,  Neil HALL ,  Kulvinder Singh SAINI

IPC分类号： A61K31/439 ,  C07D498/22 ,  A61K36/24 ,  B01D11/02 ,  B01D15/42 ,  B01D15/12

摘要： A pharmaceutical composition containing an anticancer compound, named isopicrinine, isolated from the plant Rhazya Stricta. The pharmaceutical composition may contain a salt, an analog, a derivative, and/or the prodrug of isopicrinine. A method of treating cancer with the pharmaceutical composition is disclosed. A method of extracting isopicrinine is also disclosed.

公开(公告)号：US10266543B2

公开(公告)日：2019-04-23

申请号：US14781291

申请日：2014-03-28

申请人： Janssen Sciences Ireland UC

发明人： Jean-François Bonfanti ,  Jérôme Michel Claude Fortin ,  Philippe Muller ,  Frédéric Marc Maurice Doublet ,  Pierre Jean-Marie Bernard Raboisson ,  Eric Pierre Alexandre Arnoult

IPC分类号： C07D491/18 ,  C07D491/22 ,  C07D498/18 ,  C07D498/22 ,  C07D471/18

摘要： This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.