公开(公告)号：US11185531B2

公开(公告)日：2021-11-30

申请号：US16801290

申请日：2020-02-26

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro

IPC分类号： A61K31/415 ,  C07D231/12 ,  C07D401/04 ,  C07D413/08 ,  A61K31/454 ,  A61K31/5377 ,  C07D401/02 ,  C07D231/10 ,  C07D413/02 ,  C07D405/04 ,  C12N9/10 ,  A61K31/4155

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

公开(公告)号：US11084810B2

公开(公告)日：2021-08-10

申请号：US16749412

申请日：2020-01-22

申请人： Centrexion Therapeutics Corporation

发明人： Doris Riether ,  Florian Paul Christian Binder ,  Henri Doods ,  Stephan Georg Mueller ,  Janet Rachel Nicholson ,  Achim Sauer

IPC分类号： C07D417/12 ,  C07D413/12 ,  C07D261/14 ,  C07D413/14 ,  C07D413/02 ,  C07D261/04 ,  A61K31/422

摘要： This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

公开(公告)号：US20210032256A1

公开(公告)日：2021-02-04

申请号：US17010089

申请日：2020-09-02

申请人： Grünenthal GmbH

发明人： Sven KUEHNERT ,  Rene KOENIGS ,  Achim KLESS ,  Anita WEGERT ,  Ingo KONETZKI ,  Paul RATCLIFFE ,  Ruth JOSTOCK ,  Thomas KOCH ,  Klaus LINZ ,  Wolfgang SCHROEDER

IPC分类号： C07D487/04 ,  C07D403/04 ,  C07D235/02 ,  C07D401/04 ,  C07D409/14 ,  C07D405/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/04 ,  C07D405/14 ,  C07D401/14 ,  C07D471/04 ,  C07D405/02 ,  C07D401/02 ,  C07D413/02 ,  C07D409/04

摘要： The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US20190375754A1

公开(公告)日：2019-12-12

申请号：US16450331

申请日：2019-06-24

申请人： Grünenthal GmbH

发明人： Sven KUEHNERT ,  Rene KOENIGS ,  Achim KLESS ,  Anita WEGERT ,  Ingo KONETZKI ,  Paul RATCLIFFE ,  Ruth JOSTOCK ,  Thomas KOCH ,  Klaus LINZ ,  Wolfgang SCHROEDER

IPC分类号： C07D487/04 ,  C07D409/04 ,  C07D413/02 ,  C07D401/02 ,  C07D405/02 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D413/14 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D401/04 ,  C07D235/02 ,  C07D403/04

摘要： The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US20190106429A1

公开(公告)日：2019-04-11

申请号：US16207854

申请日：2018-12-03

申请人： GRUENENTHAL GMBH

发明人： Sven Kuehnert ,  Rene Koenigs ,  Achim Kless ,  Anita Wegert ,  Ingo Konetzki ,  Paul Ratcliffe ,  Ruth Jostock ,  Thomas Koch ,  Klaus Linz ,  Wolfgang Schroeder

IPC分类号： C07D487/04 ,  C07D409/04 ,  C07D401/02 ,  C07D405/02 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D413/14 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D401/04 ,  C07D235/02 ,  C07D403/04 ,  C07D413/02

摘要： The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US20180201616A1

公开(公告)日：2018-07-19

申请号：US15923948

申请日：2018-03-16

申请人： Gruenenthal GmbH

发明人： Sven Kuehnert ,  Rene Koenigs ,  Achim Kless ,  Anita Wegert ,  Ingo Konetzki ,  Paul Ratcliffe ,  Ruth Jostock ,  Thomas Koch ,  Klaus Linz ,  Wolfgang Schroeder

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D235/02 ,  C07D413/14 ,  C07D413/02 ,  C07D409/14 ,  C07D409/04 ,  C07D405/14 ,  C07D405/06 ,  C07D405/02 ,  C07D403/14 ,  C07D403/04 ,  C07D401/14 ,  C07D401/04 ,  C07D401/02 ,  C07D417/04

CPC分类号： C07D487/04 ,  C07D235/02 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/02 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/02 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

摘要： The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3 -diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US20170320868A1

公开(公告)日：2017-11-09

申请号：US15491035

申请日：2017-04-19

申请人： Centrexion Therapeutics Corporation

发明人： Doris Riether ,  Florian Paul Christian Binder ,  Henri Doods ,  Stephan Georg Mueller ,  Janet Rachel Nicholson ,  Achim Sauer

IPC分类号： C07D417/12 ,  C07D413/02 ,  C07D261/04 ,  C07D261/14 ,  C07D413/14 ,  C07D413/12

CPC分类号： C07D417/12 ,  C07D261/04 ,  C07D261/14 ,  C07D413/02 ,  C07D413/12 ,  C07D413/14

摘要： This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

公开(公告)号：US09724332B2

公开(公告)日：2017-08-08

申请号：US14808290

申请日：2015-07-24

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro

IPC分类号： A61K31/415 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/4155 ,  C07D231/12 ,  C07D401/04 ,  C07D413/08 ,  C07D401/02 ,  C07D231/10 ,  C07D413/02 ,  C07D405/04 ,  C12N9/10

CPC分类号： A61K31/415 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/5377 ,  C07D231/10 ,  C07D231/12 ,  C07D401/02 ,  C07D401/04 ,  C07D405/04 ,  C07D413/02 ,  C07D413/08 ,  C12N9/1007 ,  C12Y201/01125

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

公开(公告)号：US09586905B2

公开(公告)日：2017-03-07

申请号：US14438920

申请日：2013-12-26

申请人： SANWA KAGAKU KENKYUSHO CO., LTD.

发明人： Katsunori Kitamoto ,  Nobuyoshi Kasugai ,  Hiroyo Kataoka ,  Yasushi Ohsawa ,  Yuka Kuno ,  Hiroki Fujieda ,  Keita Sakai ,  Hiroki Nagano ,  Naoki Takahashi ,  Toru Izuchi ,  Mitsuaki Takeuchi ,  Daisuke Kurumazuka ,  Toshiyuki Miyazawa ,  Satoko Harada ,  Izumi Gotoh ,  Yukiyasu Asano ,  Yurie Yamada ,  Morio Okabe

IPC分类号： A61K31/55 ,  C07D223/16 ,  C07D403/02 ,  C07D403/14 ,  C07D413/02 ,  C07D413/14 ,  C07D403/10 ,  C07D413/10 ,  C07D403/12 ,  C07D413/12

CPC分类号： C07D223/16 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： A compound having a V2 receptor agonistic activity is provided. Providing a pharmaceutical composition which contains, as an active ingredient, a compound represented by general formula (I) described below: [R1 is formula described below: (A is a lower alkylene group which may be substituted with lower alkyl group; R6 is a hydrogen atom; R7 is a hydroxyl group, an aromatic heterocyclic group which may be substituted with lower alkyl group, carbamoyl group); R2 is a hydrogen atom or lower alkyl group; R3 is lower alkyl group which may be substituted with 1-3 fluorine atoms, or halogen atom; R4 is a five-membered aromatic monocyclic heterocyclic group, five-membered non-aromatic monocyclic heterocyclic group, (provided each heterocyclic groups contain at least one nitrogen atom and may be substituted with a lower alkyl group); and R5 is a lower alkyl group, halogen atom], or pharmacologically acceptable salt thereof.

摘要翻译： 本发明的目的是提供具有V2受体激动活性的化合物。 本发明提供含有下述通式（I）表示的化合物作为活性成分的药物组合物：[式中，R 1为下述通式：（式中，A为低级亚烷基，可以被 低级烷基等; R 6为氢原子等; R 7为羟基，可被低级烷基取代的芳香族杂环基，氨基甲酰基等）; R 2为氢原子或低级烷基; R 3为可被1〜3个氟原子取代的低级烷基或卤原子; R 4为五元芳族单环杂环基，五元非芳香族单环杂环基等（条件是这些杂环基各自含有至少一个氮原子，并可被低级烷基取代 ）; R 5为低级烷基，卤素原子等]或其药理学上可接受的盐。

公开(公告)号：US09365493B2

公开(公告)日：2016-06-14

申请号：US14063868

申请日：2013-10-25

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07C237/26 ,  C07D413/02 ,  C07C231/10 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D261/20 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

CPC分类号： C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.