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公开(公告)号：US20080176891A1
公开(公告)日：2008-07-24
申请号：US11858144
申请日：2007-09-20
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D221/04 , A61P29/00 , A61P19/02 , A61P11/06
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof.The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
摘要翻译： 本发明涉及某些新化合物。 具体地，本发明涉及根据式（I）的化合物及其盐。 本发明的化合物是激酶活性的抑制剂，特别是IKK2活性。
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![PYRROLO[2,3-B]PYRIDIN-4-YL-BENZENESULFONAMIDE COMPOUNDS AS 1KK2 INHIBITORS](/abs-image/US/2010/02/11/US20100035917A1/abs.jpg.150x150.jpg)
2.发明申请PYRROLO[2,3-B]PYRIDIN-4-YL-BENZENESULFONAMIDE COMPOUNDS AS 1KK2 INHIBITORS 审中-公开作为1KK2抑制剂的吡咯并[2,3-B]吡啶-4-基 - 苯甲酰胺化合物公开(公告)号：US20100035917A1
公开(公告)日：2010-02-11
申请号：US12442012
申请日：2007-09-20
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to Formula (1) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular 1KK2 activity.
摘要翻译： 本发明涉及某些新化合物。 具体地，本发明涉及根据式（1）的化合物及其盐。 本发明的化合物是激酶活性的抑制剂，特别是1KK2的活性。
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公开(公告)号：US20080146606A1
公开(公告)日：2008-06-19
申请号：US11858143
申请日：2007-09-20
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D221/04 , A61P11/06 , A61P19/02 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof.The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
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4.发明申请PYRROLOPYRIDINE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS MEDICAMENTS 审中-公开吡咯啉化合物，其制备方法及其作为药物的用途公开(公告)号：US20100179139A1
公开(公告)日：2010-07-15
申请号：US12602619
申请日：2008-05-29
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D471/04 , A61K31/506 , A61K31/541 , A61P11/02 , A61P11/06 , A61P11/00 , A61P29/00 , A61P19/10 , A61P31/18 , A61P25/00 , A61P3/10 , A61P9/10 , A61P25/28 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof.The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
摘要翻译： 本发明涉及某些新化合物。 具体地，本发明涉及根据式（I）的化合物及其盐。 本发明的化合物是激酶活性的抑制剂，特别是IKK2活性。
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公开(公告)号：US20080214581A1
公开(公告)日：2008-09-04
申请号：US11995921
申请日：2006-07-17
IPC分类号： A61K31/52 , C07D473/00 , A61P29/00
CPC分类号： C07H19/16
摘要： A compound of formula (I): wherein R1-R3 are as defined in the specification, and compositions, combinations, and methods of manufacture, and methods of treatment of inflammatory diseases, using the same.
摘要翻译： 式（I）化合物：其中R 1 -R 3如说明书中所定义，组合物，组合和制备方法以及治疗方法 炎性疾病，使用相同。
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公开(公告)号：US07985740B2
公开(公告)日：2011-07-26
申请号：US11995921
申请日：2006-07-17
CPC分类号： C07H19/16
摘要： The invention provides novel compounds which are agonists of the adenosine 2A receptor along with pharmaceutical compositions thereof, and methods of administering such compounds.
摘要翻译： 本发明提供了作为腺苷2A受体的激动剂及其药物组合物的新化合物，以及施用这些化合物的方法。
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公开(公告)号：US06426337B1
公开(公告)日：2002-07-30
申请号：US09331526
申请日：1999-08-20
申请人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
发明人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
IPC分类号： A61K3170
CPC分类号： C07D473/00 , C07H19/16 , Y10S514/826 , Y10S514/851 , Y10S514/885 , Y10S514/921 , Y10S514/925
摘要： There are provided according to the invention novel compounds of formula (I) wherein R1, R2, and R3 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要翻译： 根据本发明提供新的式（I）化合物，其中R 1，R 2和R 3如说明书中所述，其制备方法，含有它们的制剂及其在治疗炎性疾病中的用途。
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公开(公告)号：US06528494B2
公开(公告)日：2003-03-04
申请号：US10025678
申请日：2001-12-19
申请人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
发明人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
IPC分类号： A01N4304
CPC分类号： C07D473/00 , C07H19/16 , Y10S514/826 , Y10S514/851 , Y10S514/885 , Y10S514/921 , Y10S514/925
摘要： There are provided according to the invention novel compounds of formula I wherein R1, R2 and R3 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要翻译： 根据本发明提供新的式I化合物，其中R 1，R 2和R 3如说明书中所述，其制备方法，含有它们的制剂及其在治疗炎性疾病中的应用。
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公开(公告)号：US09127003B2
公开(公告)日：2015-09-08
申请号：US14416937
申请日：2012-07-26
申请人： Stephen John Atkinson , Michael David Barker , Matthew Campbell , Hawa Diallo , Clement Douault , Neil Stuart Garton , John Liddle , Robert John Sheppard , Ann Louise Walker , Christopher Wellaway , David Matthew Wilson
发明人： Stephen John Atkinson , Michael David Barker , Matthew Campbell , Hawa Diallo , Clement Douault , Neil Stuart Garton , John Liddle , Robert John Sheppard , Ann Louise Walker , Christopher Wellaway , David Matthew Wilson
IPC分类号： C07D471/04 , A61K31/407 , A61K31/4184
CPC分类号： A61K31/4545 , A61K31/407 , A61K31/4184 , C07D471/04
摘要： Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
摘要翻译： 式（I）的化合物：其中; R1是氢或C1-6烷基; R 2是氢，C 1-6烷基，全卤代甲基C 0-5烷基-O-或C 1-6烷氧基; R3是氢，C1-6烷基或C1-6烷氧基C1-6烷基; R 4是氢，C 1-6烷基，全卤代甲基C 1-6烷基; 或未取代的C 3-6环烷基C 1-6烷基; A为C-R5或N; B为C-R6或N; D为C-R7或N; 条件是A，B和D中的至少一个为N; R5是氢或C1-6烷基; R6是氢或C1-6烷基; R7是氢，C1-6烷基，C1-6烷氧基或羟基; R8是氢或C1-6烷基，条件是R4和R8中的一个是氢; R9是氢或羟基; R 10是氢或C 1-6烷基; 其盐是PAD4抑制剂，并且可用于治疗各种疾病，例如类风湿性关节炎，血管炎，系统性红斑狼疮，溃疡性结肠炎，癌症，囊性纤维化，哮喘，皮肤红斑狼疮和牛皮癣。
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![PYRIDO[3,4-B]PYRAZINE DERIVATIVES AS SYK INHIBITORS](/abs-image/US/2014/01/02/US20140005188A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140005188A1
公开(公告)日：2014-01-02
申请号：US14004375
申请日：2012-03-08
申请人： Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
发明人： Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译： 式（I）的化合物或其盐; 其是脾脏酪氨酸激酶（Syk）的抑制剂，因此潜在地用于治疗由肥大细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎性疾病和/或过敏性疾病 ，以及癌症治疗，特别是血红素恶性肿瘤和自身免疫病症。
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