公开(公告)号：US11046672B2

公开(公告)日：2021-06-29

申请号：US16066043

申请日：2016-12-23

申请人： RESPIVERT LIMITED

发明人： Iain Walters ,  Louise Birch ,  Joseph Hill-Cousins ,  Stephen Paul Collingwood ,  Christopher Scott Stevenson

IPC分类号： C07D403/12 ,  C07D209/34 ,  C07D401/12 ,  C07D471/08 ,  C07D487/08 ,  A61P11/00

摘要： The present invention relates inter alia to a compound of formula (I) Wherein R1, R2, R3 and Z are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

公开(公告)号：US20180305383A1

公开(公告)日：2018-10-25

申请号：US16021519

申请日：2018-06-28

申请人： Respivert Limited ,  Topivert Pharma Limited

发明人： Matthew Colin Thor FYFE ,  Stephen Malcolm THOM

IPC分类号： C07F9/58 ,  C07D213/74 ,  A61K31/44 ,  C07D403/12 ,  C07D213/73 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/505 ,  A61K31/675 ,  C07D239/47 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/506

CPC分类号： C07F9/58 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/675 ,  A61K45/06 ,  C07D213/73 ,  C07D213/74 ,  C07D239/47 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K2300/00

摘要： There are provided compounds of: wherein T, A, Q, Z, R4, R5a, R5b, n, r, Het1 and Rx have meanings given in the description, which compounds are useful in synthesizing compounds that 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：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：US09884845B2

公开(公告)日：2018-02-06

申请号：US15118708

申请日：2015-02-13

申请人： Respivert Limited ,  Topivert Pharma Limited

发明人： Alistair Ian Longshaw ,  Euan Alexander Fraser Fordyce ,  Stuart Thomas Onions ,  John King-Underwood ,  Jennifer Diane Venable ,  Iain Walters

IPC分类号： A61K31/4427 ,  C07D401/14 ,  C07D409/14 ,  A61K31/497 ,  C07D401/12 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D413/14 ,  C07D487/04

CPC分类号： A61K31/497 ,  A61K9/0075 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K47/26 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04

摘要： There are provided compounds of formula (I) as defined in the specification, which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of inflammatory diseases.

公开(公告)号：US09790174B2

公开(公告)日：2017-10-17

申请号：US15261174

申请日：2016-09-09

申请人： Respivert Limited ,  Topivert Pharma Limited

发明人： Stephen Malcolm Thom

IPC分类号： C07C317/48 ,  C07C317/28 ,  C07D233/90 ,  A61K31/5377 ,  C07D239/47 ,  C07D211/86 ,  A61K31/44 ,  A61K31/506 ,  C07D405/12 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4427 ,  A61K31/505 ,  A61K31/541 ,  A61K31/551 ,  A61K31/553 ,  C07C311/08 ,  C07D403/12 ,  C07D213/74 ,  C07D401/12 ,  C07D413/12

CPC分类号： C07C317/48 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/553 ,  C07C311/08 ,  C07C317/28 ,  C07D211/86 ,  C07D213/74 ,  C07D233/90 ,  C07D239/47 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

摘要： There are provided compounds of formula IIb, wherein LG1 represents imidazolyl, chloro or aryloxy, which compounds are useful in the preparation of compounds that 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：US20170291917A1

公开(公告)日：2017-10-12

申请号：US15480689

申请日：2017-04-06

申请人： Respivert Limited ,  Topivert Pharma Limited

发明人： Matthew Colin Thor FYFE ,  Stephen Malcolm THOM

IPC分类号： C07F9/58 ,  C07D239/47 ,  C07D401/12 ,  C07D413/12 ,  C07D409/12 ,  A61K31/443 ,  A61K31/44 ,  A61K31/505 ,  A61K31/501 ,  A61K31/4439 ,  A61K31/4436 ,  A61K31/675 ,  C07D213/73 ,  C07D405/12

CPC分类号： C07F9/58 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/675 ,  C07D213/73 ,  C07D213/74 ,  C07D239/47 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： There are provided compounds of formula I, wherein T, A, Q, Z, G, R4, R5a, R5b and n 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：US20170239256A1

公开(公告)日：2017-08-24

申请号：US15588845

申请日：2017-05-08

申请人： Respivert Limited

发明人： Rudy Laurent Maria Broeckx ,  Walter Ferdinand Maria Filliers ,  Patrick Hubert, J Nieste ,  Alex Herman Copmans ,  Filip Marcel Vanhoutte ,  Carina Leys

IPC分类号： A61K31/519 ,  A61K9/00 ,  A61K47/12

CPC分类号： A61K31/519 ,  A61K9/0073 ,  A61K9/0075 ,  A61K31/52 ,  A61K47/12 ,  A61K47/26 ,  C07D487/04

摘要： There is provided inter alia 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-di hydroquinazolin-5-yl)-N, N-bis(2-methoxyethyl)hex-5-ynamide in the form of a solid crystalline hydrate and in solid crystalline anhydrous form. There are also provided dry powder pharmaceutical compositions for inhalation containing such solid crystalline forms.

公开(公告)号：US09732063B2

公开(公告)日：2017-08-15

申请号：US14443351

申请日：2013-11-15

申请人： RESPIVERT LIMITED ,  TOPIVERT PHARMA LIMITED

发明人： Fritz-Frieder Frickel ,  Matthew Colin Thor Fyfe ,  Premji Meghani ,  Stephen Malcolm Thom

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/506 ,  C07D401/14 ,  A61K31/5377 ,  C07D403/02

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/12 ,  C07D403/02 ,  C07D403/12

摘要： In compounds of formula I: R1 to R5, Ar and X1 to X3 have defined meanings. The compounds have anti-inflammatory 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：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.