公开(公告)号：US11364211B2

公开(公告)日：2022-06-21

申请号：US15564863

申请日：2016-04-08

申请人： MEDICAL RESEARCH COUNCIL

发明人： Anne Bertolotti ,  Indrajit Das ,  Agnieszka Krzyzosiak ,  Adrien Rousseau ,  Kim Schneider ,  Anna Gudny Sigurdardottir

IPC分类号： A61K31/155 ,  C07C281/18 ,  C07D213/61 ,  A61P21/00 ,  A61P25/14 ,  C12Q1/42 ,  C07D239/30 ,  A61P25/28 ,  G01N33/573 ,  C12N11/14 ,  G01N21/31 ,  G01N33/53

摘要： The present invention discloses a method to discover selective inhibitors of phosphatases. Thus the invention provides a method for screening a test compound to determine whether the compound binds a holophosphatase selectively or non-selectively comprising: i) providing a first holophosphatase wherein said holophosphatase is captured/immobilised; ii) testing a test compound for its ability to bind to the first holophosphatase; iii) providing a second holophosphatase wherein said second holophosphatase is captured/immobilised; iv) testing the same test compound for its ability to bind to the second holophosphatase; v) comparing the binding of the test compound to said first holophosphatase with the binding to said second phosphatase wherein a compound that binds a holophosphatase selectively will bind to said first holophosphatase but not said second holophosphatase; or will bind to said second holophosphatase but not said first; or wherein a compound that binds a holophosphatase non-selectively will bind to both said first holophosphatase and said second holophosphatase.

公开(公告)号：US11084783B2

公开(公告)日：2021-08-10

申请号：US16700327

申请日：2019-12-02

申请人： INFLECTIS BIOSCIENCE

发明人： Philippe Guedat

IPC分类号： C07C281/18 ,  C07C317/18 ,  C07C323/12 ,  C07D213/61 ,  C07D295/108 ,  A61K31/155 ,  A61K31/44 ,  C07D295/088

摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.

公开(公告)号：US10954198B2

公开(公告)日：2021-03-23

申请号：US16694694

申请日：2019-11-25

申请人： United Kingdom Research and Innovation ,  InFlectis BioScience

发明人： Philippe Guedat ,  Anne Bertolotti

IPC分类号： C07D253/075 ,  A61K31/155 ,  A61K31/44 ,  A61K31/53 ,  C07C281/18 ,  C07D213/61 ,  A61K45/06 ,  A61K31/165 ,  A61K31/216 ,  C07C281/16

摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

公开(公告)号：US10752606B2

公开(公告)日：2020-08-25

申请号：US16699476

申请日：2019-11-29

申请人： Neoculi Pty Ltd.

发明人： Stephen Page ,  Andrew Stevens ,  Adam McCluskey ,  Martine Keenan ,  Rebecca Abraham

IPC分类号： A61K31/155 ,  A61K31/505 ,  C07C251/24 ,  C07D239/48 ,  C07D333/58 ,  A61K31/381 ,  C07C281/18 ,  C07D239/50 ,  C07D295/135 ,  A61K31/17 ,  A61K31/341 ,  A61K31/4045 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/498 ,  C07C47/565 ,  C07C211/29 ,  C07D209/14 ,  C07D241/20 ,  C07D249/14 ,  C07D251/54 ,  C07D307/56 ,  C07D311/58 ,  C07D401/14 ,  A61K9/00 ,  A61K31/404 ,  A61K31/496 ,  A61K45/06 ,  C07C335/40 ,  C07D209/08

摘要： The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.

公开(公告)号：US10717704B2

公开(公告)日：2020-07-21

申请号：US16389008

申请日：2019-04-19

申请人： Rgenix, Inc.

发明人： Eduardo J. Martinez ,  Sohail F. Tavazoie

IPC分类号： A61K31/7105 ,  A61K31/704 ,  A61K31/337 ,  A61K31/155 ,  A61K31/53 ,  A61K31/7068 ,  A61K45/06 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4168 ,  A61K31/4402 ,  A61K31/4427 ,  A61K31/505 ,  C07C279/14 ,  C07C279/16 ,  C07C313/34 ,  C07F9/48 ,  C07F9/09 ,  C07F9/24 ,  C07F9/38 ,  C07F9/40 ,  A61K31/00 ,  C07D213/76 ,  C07C257/14 ,  C07C259/14 ,  C07C279/26 ,  C07C279/36 ,  C07C281/16 ,  C07C281/18 ,  C07D231/12 ,  C07C309/15 ,  C07D233/26 ,  C07D233/46 ,  C07D233/52 ,  C07D233/64 ,  C07D233/88 ,  C07D401/04 ,  C07D239/06 ,  C07D405/04 ,  C07D239/14 ,  C07D249/08 ,  C07D249/14 ,  C07D253/06 ,  C07D257/08 ,  C07D487/04 ,  C07D205/04 ,  C07D207/16 ,  C07D207/22 ,  C07D295/32 ,  C07F9/568 ,  C07F9/572 ,  C07F9/6506 ,  C07C275/70 ,  C07D205/08 ,  C07D213/74 ,  C07H19/06

摘要： This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

公开(公告)号：US10544093B2

公开(公告)日：2020-01-28

申请号：US15316797

申请日：2015-07-02

申请人： INFLECTIS BIOSCIENCE

发明人： Philippe Guedat

IPC分类号： C07C281/18 ,  C07C317/18 ,  C07C323/12 ,  C07D213/61 ,  C07D295/088

摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof Formula (I), and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.

公开(公告)号：US10253002B2

公开(公告)日：2019-04-09

申请号：US14888306

申请日：2014-05-01

申请人： Neoculi Pty Ltd.

发明人： Stephen Page ,  Sanjay Garg ,  Martine Keenan ,  Adam McCluskey ,  Andrew Stevens

IPC分类号： C07D239/50 ,  C07D239/48 ,  C07D251/48 ,  C07D251/54 ,  C07D251/66 ,  C07D281/16 ,  C07C281/18 ,  C07C281/16 ,  C07D333/58 ,  A61K31/155 ,  A61K31/381 ,  C07D209/14 ,  C07D295/125 ,  C07C281/08 ,  A61K45/06 ,  A61K31/14 ,  A61K31/17 ,  A61K31/175 ,  A61K31/404 ,  A61K31/505 ,  C07C323/45 ,  C07C337/08 ,  C07D215/12 ,  C07D209/40 ,  C07D213/53 ,  C07D307/56 ,  A01N43/54 ,  A01N47/44 ,  C07F9/6512

摘要： The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

公开(公告)号：US09663458B2

公开(公告)日：2017-05-30

申请号：US15114025

申请日：2014-03-19

申请人： GUANGZHOU INSIGHTER BIOTECHNOLOGY CO., LTD.

发明人： Xianfeng Peng ,  Zonghua Qin ,  Fang Li ,  Xiaolan Ye

IPC分类号： C07C281/18 ,  A23K20/111 ,  A23K50/75 ,  A23K50/30

CPC分类号： C07C281/18 ,  A23K20/111 ,  A23K50/30 ,  A23K50/75 ,  C07C2601/08

摘要： Diaminoguanidine derivatives in preparation of animal growth promoters used in feed. The diaminoguanidine derivatives have a structural formula as shown in formula (I), wherein R1 is methyl, ethyl, isopropyl, n-butyl, n-propyl, n-pentyl, n-octyl, n-tetradecyl, sec-butyl, 3-pentyl, cyclopentyl or benzyl. The diaminoguanidine compounds significantly improve the productivity of ducks if they are fed with the diaminoguanidine compounds. Productivity of pigs or chickens is also improved with such diaminoguanidine compounds.

公开(公告)号：US09550000B2

公开(公告)日：2017-01-24

申请号：US14343627

申请日：2012-09-07

申请人： Simon P. Robinson ,  Ming Yu

发明人： Simon P. Robinson ,  Ming Yu

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07C279/04 ,  C07D233/46 ,  C07D209/14 ,  C07C257/14 ,  C07C279/06 ,  C07C279/08 ,  C07C279/12 ,  C07C279/14 ,  C07C281/18 ,  C07C217/70

CPC分类号： A61K51/0459 ,  A61K51/04 ,  A61K51/041 ,  A61K51/0453 ,  A61K51/0497 ,  C07B2200/05 ,  C07C217/70 ,  C07C257/14 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/12 ,  C07C279/14 ,  C07C281/18 ,  C07D209/14 ,  C07D233/46

摘要： The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

摘要翻译： 本发明涉及用于合成和使用成像剂或其前体的体系，组合物和方法。 成像剂前体可以使用本文所述的方法转化成成像剂。 在某些情况下，成像剂富集于18F。 在一些情况下，成像剂可用于对受试者感兴趣的区域进行成像，包括但不限于心脏，心血管系统，心脏血管，脑和其他器官。 在一些实施例中，提供了用于评估受试者的一部分中的灌注和神经支配失配的方法和组合物。

公开(公告)号：US20160340299A1

公开(公告)日：2016-11-24

申请号：US15114025

申请日：2014-03-19

申请人： GUANGZHOU INSIGHTER BIOTECHNOLOGY CO., LTD.

发明人： Xianfeng Peng ,  Zonghua Qin ,  Fang Li ,  Xiaolan Ye

IPC分类号： C07C281/18 ,  A23K50/75 ,  A23K50/30 ,  A23K20/111

CPC分类号： C07C281/18 ,  A23K20/111 ,  A23K50/30 ,  A23K50/75 ,  C07C2601/08

摘要： Diaminoguanidine derivatives in preparation of animal growth promoters used in feed. The diaminoguanidine derivatives have a structural formula as shown in formula (I), wherein R1 is methyl, ethyl, isopropyl, n-butyl, n-propyl, n-pentyl, n-octyl, n-tetradecyl, sec-butyl, 3-pentyl, cyclopentyl or benzyl. The diaminoguanidine compounds significantly improve the productivity of ducks if they are fed with the diaminoguanidine compounds. Productivity of pigs or chickens is also improved with such diaminoguanidine compounds.

摘要翻译： 乙基，异丙基，正丁基，正丙基，正戊基，正辛基，正十四烷基，仲丁基，3-戊基，环戊基或苄基。 当在饲料实验中首次使用该化合物时，发现应用于鸭子的生产率明显提高。 通过类似的喂养实验，猪和鸡的生产力也得到提高。 二氨基胍衍生物可用于制备动物饲料生长促进剂。