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公开(公告)号：US09227984B2
公开(公告)日：2016-01-05
申请号：US14239406
申请日：2012-08-15
申请人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
发明人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/04 , C07D513/04 , C07D519/00
CPC分类号： C07D495/04 , A61K31/519 , C07D513/04 , C07D519/00
摘要： A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
摘要翻译： 一系列单环或双环二胺取代的噻吩并[2,3-d]嘧啶和异噻唑并[5,4-d]嘧啶衍生物有助于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病 ; 病毒性疾病 和器官和细胞移植排斥反应。
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公开(公告)号：US20140309222A1
公开(公告)日：2014-10-16
申请号：US14239406
申请日：2012-08-15
申请人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
发明人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC分类号： C07D495/04 , C07D513/04
CPC分类号： C07D495/04 , A61K31/519 , C07D513/04 , C07D519/00
摘要： A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
摘要翻译： 一系列单环或双环二胺取代的噻吩并[2,3-d]嘧啶和异噻唑并[5,4-d]嘧啶衍生物有助于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病 ; 病毒性疾病 和器官和细胞移植排斥反应。
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公开(公告)号：US09029392B2
公开(公告)日：2015-05-12
申请号：US13821294
申请日：2011-09-02
申请人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Judi Charlotte Neuss , Joanna Rachel Quincey , Jackalyn Hinkins
发明人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
IPC分类号： A61K31/4709 , C07D215/12 , C07D471/04 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519
摘要： Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. The compounds are of general formula (I):
摘要翻译： 公开了一系列包含氟化乙基侧链的喹啉和喹喔啉衍生物，其是PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤， 伤害性或眼科疾病。 该化合物具有通式（I）：
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公开(公告)号：US20130296338A1
公开(公告)日：2013-11-07
申请号：US13821294
申请日：2011-09-02
申请人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
发明人： Andrew Harry Parton , Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Daniel James Ford , Richard Jeremy Franklin , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Quincey
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： A series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译： 包含氟化乙基侧链的一系列喹啉和喹喔啉衍生物是P13激酶的选择性抑制剂，因此在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害感受性或伤害性感受器 眼科病情。
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公开(公告)号：US08283359B2
公开(公告)日：2012-10-09
申请号：US12182931
申请日：2008-07-30
申请人： Martin Clive Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
发明人： Martin Clive Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
IPC分类号： A61K31/44 , C07D513/02
CPC分类号： C07D495/04
摘要： A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列被取代的苯胺基部分在2位被取代的噻吩并[2,3-b]吡啶衍生物是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗中 的炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害感受条件。
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公开(公告)号：US20100179124A1
公开(公告)日：2010-07-15
申请号：US12691842
申请日：2010-01-22
申请人： James Andrew Johnson , Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham , Judi Charlotte Neuss
发明人： James Andrew Johnson , Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham , Judi Charlotte Neuss
IPC分类号： A61K31/397 , C07D495/04 , A61K31/4365 , A61P35/02 , A61P35/00 , A61P9/12 , A61P7/02 , A61P11/06 , A61P17/06 , A61P19/02 , A61P1/00 , A61P37/06
CPC分类号： C07D495/04
摘要： A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列被取代的苯胺基部分在2位被取代的噻吩并[2,3-b]吡啶衍生物是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗中 的炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害感受条件。
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公开(公告)号：US08637491B2
公开(公告)日：2014-01-28
申请号：US12971590
申请日：2010-12-17
申请人： James Andrew Johnson , Daniel Christopher Brookings , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Thorne
发明人： James Andrew Johnson , Daniel Christopher Brookings , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Thorne
IPC分类号： A61K31/675 , C07D491/02
CPC分类号： C07D495/04 , C07D519/00
摘要： A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列噻吩并[2,3-b]吡啶衍生物，其在2-位连接到取代的苯胺基部分，其在3-位上被与吡咯烷-1-基环连接的羰基取代， 形成含有杂原子的稠合双环体系的一部分，其是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害性疾病 。
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公开(公告)号：US08394822B2
公开(公告)日：2013-03-12
申请号：US13604282
申请日：2012-09-05
申请人： Martin Clive Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
发明人： Martin Clive Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
IPC分类号： A61K31/44
CPC分类号： C07D495/04
摘要： A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列被取代的苯胺基部分在2位被取代的噻吩并[2,3-b]吡啶衍生物是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗中 的炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害感受条件。
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公开(公告)号：US20110172191A1
公开(公告)日：2011-07-14
申请号：US12971590
申请日：2010-12-17
申请人： James Andrew Johnson , Daniel Christopher Brookings , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Thorne
发明人： James Andrew Johnson , Daniel Christopher Brookings , Barry John Langham , Judi Charlotte Neuss , Joanna Rachel Thorne
IPC分类号： A61K31/675 , C07D495/04 , A61K31/4365 , C07D498/04 , A61K31/5365 , A61K31/66 , A61P35/00 , A61P25/04 , A61P9/00 , A61P19/02 , A61P1/00 , A61P11/06 , A61P37/06
CPC分类号： C07D495/04 , C07D519/00
摘要： A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列噻吩并[2,3-b]吡啶衍生物，其在2-位连接到取代的苯胺基部分，其在3-位上被与吡咯烷-1-基环连接的羰基取代， 形成含有杂原子的稠合双环体系的一部分，其是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害性疾病 。
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公开(公告)号：US20090149437A1
公开(公告)日：2009-06-11
申请号：US12182931
申请日：2008-07-30
申请人： Clive Martin Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
发明人： Clive Martin Hutchings , Sarah Catherine Archibald , Daniel Christopher Brookings , Jeremy Martin Davis , James Andrew Johnson , Barry John Langham , Judi Charlotte Neuss
IPC分类号： A61K31/4365 , C07D495/04 , A61P29/00 , A61P35/00 , A61P9/00
CPC分类号： C07D495/04
摘要： A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
摘要翻译： 一系列被取代的苯胺基部分在2位被取代的噻吩并[2,3-b]吡啶衍生物是人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗中 的炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害感受条件。
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