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公开(公告)号：US09796742B2
公开(公告)日：2017-10-24
申请号：US15228945
申请日：2016-08-04
IPC分类号： C07F9/6558 , C07F9/6568 , A61K31/675 , A61K31/695 , C07D213/68 , C07D231/14 , C07D239/22 , C07F7/08 , C07F9/28 , C07F9/30 , C07F9/6512 , C07F9/6503
CPC分类号： C07F9/65583 , A61K31/675 , A61K31/695 , C07D213/68 , C07D231/14 , C07D239/22 , C07F7/0803 , C07F9/28 , C07F9/304 , C07F9/65031 , C07F9/6512 , C07F9/65685
摘要： There are provided compounds of formula I, wherein R1 to R5, X1, X2, Ar, L, A, A1, E and G 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.
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公开(公告)号：US10392346B2
公开(公告)日：2019-08-27
申请号：US16035502
申请日：2018-07-13
IPC分类号： C07D213/74 , C07D213/80 , C07D401/12 , C07D239/47 , C07D413/12 , C07D405/12 , C07D453/02 , C07F9/6512 , C07H19/048 , C07H13/08 , C07H15/26 , C07F9/6558 , A61K31/44 , A61K31/506 , A61K31/675 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/706 , A61K31/553 , A61K31/551 , A61K31/541 , C07F9/58 , C07F9/59 , A61K31/4412 , A61K31/7052 , A61K31/4375 , A61K31/635 , A61K45/06 , A61K31/444 , A61K31/505 , C07F9/6503
摘要： There are provided compounds of formula IIb, wherein: LG1 represents imidazolyl, chloro, or aryloxy; and Z1 represents a structural fragment of formula V: wherein R2 to R4, R5a, L and X1 to X3 have meanings given in the description, or a salt or protected derivative thereof, wherein said protected derivative is a compound in which the carboxyl moiety of R4 is protected as a C1-8 alkyl ester. The compounds have antiinflammatory activity, for example 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.
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公开(公告)号：US20160376232A1
公开(公告)日：2016-12-29
申请号：US15261174
申请日：2016-09-09
发明人： Stephen Malcolm Thom
IPC分类号： C07C317/48 , C07D233/90 , C07C317/28
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.
摘要翻译： 其中LG1表示咪唑基，氯或芳氧基，该化合物可用于制备具有抗炎活性的化合物（例如通过抑制p38丝裂原活化蛋白激酶的家族中的一种或多种成员; Syk激酶;和成员 的Src家族酪氨酸激酶），并且用于治疗，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。
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公开(公告)号：US20150218137A1
公开(公告)日：2015-08-06
申请号：US14422158
申请日：2013-08-16
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 。
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公开(公告)号：US10435361B2
公开(公告)日：2019-10-08
申请号：US15726241
申请日：2017-10-05
发明人： Thomas Matthew Baker , Matthew Colin Thor Fyfe , Gareth William Harbottle , Vedran Hasimbegovic , Premji Meghani , Aaron Rigby , Colin Sambrook-Smith , Stephen Malcolm Thom
IPC分类号： C07D295/096 , C07C317/48 , 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 , C07C317/28 , C07D233/90
摘要： There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 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.
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公开(公告)号：US09790174B2
公开(公告)日：2017-10-17
申请号：US15261174
申请日：2016-09-09
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.
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公开(公告)号：US09732063B2
公开(公告)日：2017-08-15
申请号：US14443351
申请日：2013-11-15
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.
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公开(公告)号：US09701670B2
公开(公告)日：2017-07-11
申请号：US14422158
申请日：2013-08-16
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.
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公开(公告)号：US10125100B2
公开(公告)日：2018-11-13
申请号：US15604258
申请日：2017-05-24
IPC分类号： C07D213/74 , C07D213/80 , C07D401/12 , C07D239/47 , C07D413/12 , C07H13/08 , C07H15/26 , C07F9/58 , C07F9/6512 , C07F9/6558 , C07H19/048 , A61K31/4412 , A61K31/44 , A61K31/506 , A61K31/675 , A61K31/7052 , C07D453/02 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/553 , A61K31/635 , A61K31/706 , C07D405/12 , A61K45/06 , A61K31/444 , A61K31/505
摘要： There are provided compounds of formulas III and VIIa: or a salt or protected derivative thereof, wherein Z2 represents a structural fragment of formula V, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity, for example 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.
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公开(公告)号：US10072034B2
公开(公告)日：2018-09-11
申请号：US15480689
申请日：2017-04-06
IPC分类号： C07D213/79 , C07D239/47 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/44 , A61K31/501 , A61K31/505 , C07F9/58 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/675 , C07D213/73 , C07D403/12 , A61K31/506 , C07D213/74
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 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.
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