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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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5.发明授权7-(1H-pyrazol-4-yl)-1,6-naphthyridine compounds as Syk inhibitors 失效7-（1H-吡唑-4-基）-1,6-萘啶化合物作为Syk抑制剂公开(公告)号：US08633319B2
公开(公告)日：2014-01-21
申请号：US13642338
申请日：2011-04-27
申请人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
发明人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： The present invention relates to 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 and/or basophil 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, chronic spontaneous urticaria and autoimmune conditions.
摘要翻译： 本发明涉及式（I）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桅杆和/或嗜碱性粒细胞，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，慢性自发性荨麻疹和自身免疫性疾病。
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6.发明申请PYRIDINYL- AND PYRAZINYL-METHYLOXY-ARYL DERIVATIVES USEFUL AS INHIBITORS OF SPLEEN TYROSINE KINASE (SYK) 审中-公开作为缓冲型酪氨酸激酶（SYK）的抑制剂有用的吡啶基 - 和吡嗪并 - 甲基衍生物公开(公告)号：US20140005177A1
公开(公告)日：2014-01-02
申请号：US14004388
申请日：2012-03-08
IPC分类号： C07D401/12 , A61K31/4725 , A61K31/55 , C07D403/12 , A61K45/06 , C07D401/14
CPC分类号： C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
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 diseases and/or allergic conditions, 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，例如炎症性疾病和/或过敏性疾病 ，在癌症治疗中，特别是血红素恶性肿瘤和自身免疫病症。
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公开(公告)号：US20120232061A1
公开(公告)日：2012-09-13
申请号：US13414873
申请日：2012-03-08
IPC分类号： A61K31/55 , A61P37/06 , A61P19/04 , A61P19/02 , A61P7/00 , A61P17/00 , A61P13/12 , A61P29/00 , C07D401/12 , A61P9/00
CPC分类号： C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
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 diseases and/or allergic conditions, 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，例如炎症性疾病和/或过敏性疾病 ，在癌症治疗中，特别是血红素恶性肿瘤和自身免疫病症。
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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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10.发明申请7-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS 失效7-（1H-吡唑-4-基）-1,6-萘啶化合物作为SYK抑制剂公开(公告)号：US20130040984A1
公开(公告)日：2013-02-14
申请号：US13642338
申请日：2011-04-27
申请人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
发明人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
IPC分类号： A61K31/4545 , A61P37/06 , A61P17/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to 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 and/or basophil 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, chronic spontaneous urticaria and autoimmune conditions.
摘要翻译： 本发明涉及式（I）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桅杆和/或嗜碱性粒细胞，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，慢性自发性荨麻疹和自身免疫性疾病。
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