公开(公告)号：US20180134687A1

公开(公告)日：2018-05-17

申请号：US15812425

申请日：2017-11-14

申请人： RESPIVERT LIMITED

发明人： Kazuhiro Ito ,  Catherine Elisabeth Charron ,  John King-Underwood ,  Stuart Thomas Onions ,  Alistair Ian Longshaw ,  Rudy Broeckx ,  Walter Filliers ,  Alex Copmans

IPC分类号： C07D403/12 ,  A61K31/351 ,  A61K31/513 ,  A61K31/506 ,  A61K31/215 ,  C07D491/10 ,  A61K31/4155

CPC分类号： C07D403/12 ,  A61K31/215 ,  A61K31/351 ,  A61K31/4155 ,  A61K31/506 ,  A61K31/513 ,  C07B2200/13 ,  C07D491/10 ,  Y02A50/406

摘要： There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

公开(公告)号：US20170202841A1

公开(公告)日：2017-07-20

申请号：US15474059

申请日：2017-03-30

申请人： Respivert Limited

发明人： John King-Underwood ,  Kazuhiro Ito ,  Peter John Murray ,  George Hardy ,  Frederick Arthur Brookfield ,  Christopher John Brown

IPC分类号： A61K31/519 ,  A61K9/00 ,  A61K47/26 ,  A61K9/14

CPC分类号： A61K31/519 ,  A61K9/0075 ,  A61K9/14 ,  A61K47/26 ,  C07D487/04

摘要： The present invention relates to the compound of formula (I) and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compound.

公开(公告)号：US09701670B2

公开(公告)日：2017-07-11

申请号：US14422158

申请日：2013-08-16

申请人： RESPIVERT LIMITED ,  TOPIVERT PHARMA LIMITED

发明人： Claire Anne Marie Cariou ,  Catherine Elisabeth Charron ,  Euan Alexander Fraser Fordyce ,  Daniel Hamza ,  Matthew Colin Thor Fyfe ,  Kazuhiro Ito ,  John King-Underwood ,  Peter John Murray ,  Stuart Thomas Onions ,  Stephen Malcolm Thom ,  Hayley Tegan Angela Watson ,  Jonathan Gareth Williams

IPC分类号： A61K31/506 ,  A61K31/5377 ,  C07D409/14 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06 ,  C07D405/14

CPC分类号： C07D409/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

摘要： There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

公开(公告)号：US09475796B2

公开(公告)日：2016-10-25

申请号：US14349356

申请日：2012-10-03

申请人： RESPIVERT LIMITED

发明人： Kazuhiro Ito ,  Catherine Elisabeth Charron ,  John King-Underwood ,  Stuart Thomas Onions ,  Alistair Ian Longshaw

IPC分类号： C07D403/12 ,  A61K31/506 ,  A61K45/06 ,  A61K31/215 ,  A61K31/351

CPC分类号： A61K31/506 ,  A61K9/0075 ,  A61K31/215 ,  A61K31/351 ,  A61K45/06 ,  C07D403/12 ,  A61K2300/00

摘要： There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

摘要翻译： 提供了作为p38丝裂原活化蛋白激酶的家族的抑制剂的式（I）化合物，以及它们在治疗中的应用，包括药物组合，特别是治疗炎性疾病，包括肺炎性疾病 ，如哮喘和COPD。

公开(公告)号：US20160045512A1

公开(公告)日：2016-02-18

申请号：US14883464

申请日：2015-10-14

申请人： RESPIVERT LIMITED

发明人： Catherine Elisabeth Charron ,  Robert Fenton ,  Scott Crowe ,  Kazuhiro Ito ,  Peter Strong ,  William Garth Rapeport

IPC分类号： A61K31/5377 ,  A61K31/496 ,  G01N33/50 ,  C12N15/113 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/506

CPC分类号： A61K31/5377 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06 ,  C12N15/1137 ,  C12N2310/141 ,  G01N33/5023 ,  G01N33/56983 ,  G01N2333/11 ,  G01N2333/91205 ,  G01N2333/91215 ,  G01N2500/04 ,  G01N2500/10 ,  A61K2300/00

摘要： The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.

摘要翻译： 本发明特别涉及使用抑制p59的活性的化合物治疗或预防流感病毒感染（包括亚型甲型流感病毒，乙型流感病毒，禽类H5N1，A / H1N1，H3N2和/或大流行性流感） HCK以及用于筛选用于预防或治疗受试者的流感病毒感染的候选药物的方法，所述方法包括鉴定能够抑制p59-HCK活性的测试物质。

公开(公告)号：US20150203475A1

公开(公告)日：2015-07-23

申请号：US14424361

申请日：2013-08-28

申请人： RESPIVERT LIMITED ,  TOPIVERT PHARMA LIMITED

发明人： Lorna Anne Duffy ,  John King-Underwood ,  Alistair Ian Longshaw ,  Peter John Murray ,  Stuart Thomas Onions ,  David Michael Adrien Taddei ,  Jonathan Gareth Williams ,  Kazuhiro Ito ,  Catherine Elisabeth Charron

IPC分类号： C07D403/14 ,  A61K31/5377 ,  C07D413/14 ,  C07D409/14 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14 ,  A61K31/506 ,  C07D471/04

CPC分类号： C07D403/14 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula (I): wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.

摘要翻译： 公开了式（I）化合物：其中R1，R2，J，Q，V，X，Y和Z如本文所定义。 这些化合物是p38丝裂原活化蛋白激酶（家系本文中称为p38 MAP激酶抑制剂），特别是其α亚型以及Syk激酶和酪氨酸激酶的Src家族的抑制剂。 这些化合物可以用于治疗，包括药物组合，特别是治疗炎性疾病，特别是肺的炎性疾病，如哮喘和COPD，以及胃肠道炎症性疾病如溃疡性结肠炎和克罗恩病 疾病和眼睛，如葡萄膜炎。

公开(公告)号：US10738032B2

公开(公告)日：2020-08-11

申请号：US16285762

申请日：2019-02-26

申请人： RESPIVERT LIMITED

发明人： Kazuhiro Ito ,  Catherine Elisabeth Charron ,  John King-Underwood ,  Stuart Thomas Onions ,  Alistair Ian Longshaw ,  Rudy Broeckx ,  Walter Filliers ,  Alex Copmans

IPC分类号： C07D403/12 ,  A61K31/4155 ,  C07D491/10 ,  A61K31/215 ,  A61K31/351 ,  A61K31/513 ,  A61K31/506

摘要： There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

公开(公告)号：US10266519B2

公开(公告)日：2019-04-23

申请号：US15812425

申请日：2017-11-14

申请人： RESPIVERT LIMITED

发明人： Kazuhiro Ito ,  Catherine Elisabeth Charron ,  John King-Underwood ,  Stuart Thomas Onions ,  Alistair Ian Longshaw ,  Rudy Broeckx ,  Walter Filliers ,  Alex Copmans

IPC分类号： C07D401/14 ,  C07D403/12 ,  A61K31/4155 ,  C07D491/10 ,  A61K31/215 ,  A61K31/351 ,  A61K31/513 ,  A61K31/506

摘要： There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

公开(公告)号：US20150218137A1

公开(公告)日：2015-08-06

申请号：US14422158

申请日：2013-08-16

申请人： RESPIVERT LIMITED ,  TOPIVERT PHARMA LIMITED

发明人： Claire Anne Marie Cariou ,  Catherine Elisabeth Charron ,  Euan Alexander Fraser Fordyce ,  Daniel Hamza ,  Matthew Colin Thor Fyfe ,  Kazuhiro Ito ,  John King-Underwood ,  Peter John Murray ,  Stuart Thomas Onions ,  Stephen Malcolm Thom ,  Hayley Tegan Angela Watson ,  Jonathan Gareth Williams

IPC分类号： C07D409/14 ,  A61K31/5377 ,  C07D405/14 ,  C07D403/12 ,  A61K31/506 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06

CPC分类号： C07D409/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

摘要： There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

摘要翻译： 提供了式I化合物，其中R，R 1，R a，R b，Q，X和Y具有说明书中给出的含义，哪些化合物具有抗炎活性（例如，通过抑制下列成员中的一个或多个： p38丝裂原活化蛋白激酶; Syk激酶;以及Src家族酪氨酸激酶的成员），并用于治疗，包括药物组合，特别是治疗炎性疾病，包括肺，眼和肠的炎性疾病 。

公开(公告)号：US20180000830A1

公开(公告)日：2018-01-04

申请号：US15706152

申请日：2017-09-15

申请人： Respivert Limited

发明人： Catherine Elisabeth Charron ,  Robert Fenton ,  Scott Crowe ,  Kazuhiro Ito ,  Peter Strong ,  William Garth Rapeport ,  Keith Ray

IPC分类号： A61K31/5377 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4155 ,  A61K45/06 ,  C12N15/113 ,  G01N33/569 ,  G01N33/50 ,  A61K31/506

CPC分类号： A61K31/5377 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06 ,  C12N15/1137 ,  C12N2310/141 ,  G01N33/5023 ,  G01N33/56983 ,  G01N2333/11 ,  G01N2333/91205 ,  G01N2333/91215 ,  G01N2500/04 ,  G01N2500/10 ,  A61K2300/00

摘要： The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.