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1.发明申请公开(公告)号：US20190048005A1
公开(公告)日：2019-02-14
申请号：US16165506
申请日：2018-10-19
Inventor： Niall Andrew ANDERSON , Ian Baxter CAMPBELL , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , Seble LEMMA , Simon John Fawcett MACDONALD , John Martin PRITCHARD , Panayiotis Alexandrou PROCOPIOU
IPC: C07D471/04 , C07B59/00
CPC classification number: C07D471/04 , C07B59/002 , C07B2200/05
Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected from a hydrogen atom, a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
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公开(公告)号：US20190112306A1
公开(公告)日：2019-04-18
申请号：US16087320
申请日：2017-03-20
Inventor： Niall Andrew ANDERSON , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , Seble LEMMA , John Martin PRITCHARD , Panayiotis Alexandrou PROCOPIOU , Steven Leslie SOLLIS
IPC: C07D471/04 , A61P11/00
Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the description and claims, or pharmaceutically acceptable salts thereof, having αvβ6 integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an αvβ6 integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.
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Patent Agency Ranking
3.发明申请公开(公告)号：US20170291899A1
公开(公告)日：2017-10-12
申请号：US15514416
申请日：2015-09-22
Inventor： Niall Andrew ANDERSON , Ian Baxter CAMPBELL , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , Seble LEMMA , Simon John Fawcett MACDONALD , John Martin PRITCHARD , Panayiotis Alexandrou PROCOPIOU
IPC: C07D471/04 , C07B59/00
CPC classification number: C07D471/04 , C07B59/002 , C07B2200/05
Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, Ri does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
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公开(公告)号：US20170290818A1
公开(公告)日：2017-10-12
申请号：US15514414
申请日：2015-09-22
Inventor： Niall Andrew ANDERSON , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , Seble LEMMA , Simon John Fawcett MACDONALD , John Martin PRITCHARD , Panayiotis Alexandrou PROCOPIOU , Stephen SWANSON
IPC: A61K31/4375 , C07D207/04 , C07D471/04
CPC classification number: A61K31/4375 , C07D207/04 , C07D471/04
Abstract: A compound according to formula (I) wherein R1 is hydrogen, cyclopropyl, or pyrazolyl, wherein said pyrazolyl is optionally substituted by one or two methyl groups; or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20210206758A1
公开(公告)日：2021-07-08
申请号：US16087349
申请日：2017-03-20
Inventor： Niall Andrew ANDERSON , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , Seble LEMMA , John Martin PRITCHARD , Panayiotis Alexandrou PROCOPIOU , Joanna Mary REDMOND , Steven Leslie SOLLIS
IPC: C07D471/04
Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the description and claims, or pharmaceutically acceptable salts thereof, having αvβ6 integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof, in therapy, including in the treatment of a disease or condition for which an αvβ6 integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.
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公开(公告)号：US20190275016A1
公开(公告)日：2019-09-12
申请号：US16423455
申请日：2019-05-28
Inventor： Niall Andrew ANDERSON , Matthew Howard James CAMPBELL-CRAWFORD , Ashley Paul HANCOCK , John Martin PRITCHARD , Joanna Mary REDMOND
IPC: A61K31/4375 , C07D471/04
Abstract: A compound of formula (I): being 4-(3-Fluoro-3-(2-(5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-2-yl) ethyl) pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy) phenyl) butanoic acid, or a salt thereof.
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公开(公告)号：US20180291022A1
公开(公告)日：2018-10-11
申请号：US16007584
申请日：2018-06-13
Inventor： Niall Andrew ANDERSON , Brendan John FALLON , John Martin PRITCHARD
IPC: C07D471/04 , A61P11/00
CPC classification number: C07D471/04 , A61P11/00
Abstract: A compound of formula (I) or a salt thereof wherein R1 represents a hydrogen atom, a methyl group or a ethyl group R2 represents a hydrogen atom or a fluorine atom R3 represents a hydrogen atom, a methyl group or an ethyl group.
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