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11. 发明授权

US5681839A Nitrogen heterocycles 失效
标题翻译：氮杂环
公开(公告)号：US5681839A
公开(公告)日：1997-10-28
申请号：US448453
申请日：1995-12-07
申请人： Roger Crossley , Albert Opalko , Barry John Langham
发明人： Roger Crossley , Albert Opalko , Barry John Langham
IPC分类号： C07C217/74 , C07C229/46 , C07D215/22 , C07D215/227 , C07D215/56 , A61K31/47
CPC分类号： C07D215/227 , C07C217/74 , C07C229/46 , C07D215/56 , C07C2101/14
摘要： This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds, R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl; R' represents one or more optional substituents the same or different, selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; R" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions selected from C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.sub.2 -C.sub.7 alkanoylamino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 hydroxyalkyl, and R" can also represent hydroxy in the 6 position when the optional bond is absent; oxo and methylene; which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.
摘要翻译： PCT No.PCT / GB95 / 00278 Sec。 371 1995年12月7日第 102（e）1995年12月7日，PCT提交1995年2月10日PCT公布。公开号WO95 / 21824 日期1995年8月17日本发明涉及通式（1）的化合物或其药学上可接受的盐，其中虚线表示任选的键，R 3是任选取代的C 6 -C 10芳基或杂芳基; R4代表氢或式-CRaRbRc基团，其中Ra，Rb和Rc独立地选自氢，C1-C6烷基C6-C10芳基，杂芳基，被任意取代的C6-C10芳基或杂芳基取代的C1-C6烷基; R'表示选自卤素，C 1 -C 6烷基，C 2 -C 7烷氧基羰基，C 1 -C 6羟基烷基，CN，氨基羰基，C 2 -C 7烷酰氧基（C 1 -C 6）烷基，羧基，C 2 -C 7烷氧基氨基，C 6 -C 10或杂芳基或（C 6 -C 10芳基）烷基或杂芳基烷基; R“表示选自C 1 -C 6烷基，C 2 -C 7烷酰氧基，羟基，氨基，C 2 -C 7烷酰基氨基，C 1 -C 6烷基氨基，C 1 -C 6烷基氨基， C6羟基烷基，当不含任选的键时，R“也可以表示6位的羟基; 氧代和亚甲基; 哪些化合物具有通过其阻断电压门控钾通道的能力而赋予的药物用途。

12. 发明申请

US20120095005A1 Fused Bicyclic Pyrazole Derivatives As Kinase Inhibitors 审中-公开
标题翻译：稠合双环吡唑衍生物作为激酶抑制剂
公开(公告)号：US20120095005A1
公开(公告)日：2012-04-19
申请号：US13321305
申请日：2010-05-19
申请人： Daniel Rees Allen , Julien Alistair Brown , Roland Burli , Alan Findlay Haughan , Barry John Langham , Mizio Matteucci , Andrew Pate Owens , Gilles Raphy , Andrew Sharpe
发明人： Daniel Rees Allen , Julien Alistair Brown , Roland Burli , Alan Findlay Haughan , Barry John Langham , Mizio Matteucci , Andrew Pate Owens , Gilles Raphy , Andrew Sharpe
IPC分类号： A61K31/53 , A61K31/519 , A61P35/00 , A61P29/00 , A61P37/06 , A61P9/00 , A61P25/28 , A61P3/00 , A61P27/02 , A61P11/06 , A61P1/00 , A61P25/00 , A61P17/06 , A61P7/02 , A61P9/12 , A61P9/04 , A61P25/16 , A61P3/04 , A61P3/10 , A61P35/02 , C07D487/04
CPC分类号： C07D487/04
摘要： A series of substituted pyrazolo[1,5-α][1,3,5]triazine and pyrazolo[1,5-αj-pyrimidine derivatives, 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. Formula (I).
摘要翻译：因此，一系列取代的吡唑并[1,5-α] [1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物是PI3激酶的选择性抑制剂，因此在医学中是有益的，例如在炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病的治疗。式（I）。

13. 发明授权

US07456286B2 Bicyclic heteroaromatic compounds as kinase inhibitors 失效
标题翻译：双环杂芳族化合物作为激酶抑制剂
公开(公告)号：US07456286B2
公开(公告)日：2008-11-25
申请号：US10529413
申请日：2003-09-30
申请人： Daniel Christopher Brookings , Rachel Jane Cubbon , Jeremy Martin Davis , Barry John Langham
发明人： Daniel Christopher Brookings , Rachel Jane Cubbon , Jeremy Martin Davis , Barry John Langham
IPC分类号： C07D471/02 , A01N43/90
CPC分类号： C07D471/04
摘要： A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 5-oxo-4,5-dihydro-1H-pyrrolo[3,2-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
摘要翻译：基于5-氧代-4,5-二氢-1H-吡咯并[3,2-b]吡啶环体系的一系列5-6稠环双环杂芳族衍生物是p38激酶的抑制剂，因此是用于医学中，例如用于治疗和/或预防免疫或炎性疾病。

14. 发明授权

US06610700B2 Enamine derivatives 失效
标题翻译：使用衍生物
公开(公告)号：US06610700B2
公开(公告)日：2003-08-26
申请号：US09835656
申请日：2001-04-16
申请人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
发明人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
IPC分类号： A61K31435
CPC分类号： C07D213/81 , C07C229/36 , C07C2601/10 , C07D217/22 , C07D471/04
摘要： Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了式（1）的胺衍生物：其中R1是Ar1，其中Ar1是芳族或杂芳基，L2是共价键或连接原子或基团，Ar2是亚芳基或亚杂芳基，Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸或其衍生物或生物试剂; R 2是氢原子或C 1-6烷基; Cy是脂环族或杂环脂族环，其中X是N原子或C（Rw）基团; Rx是氧代，硫代或亚氨基; Rw和Rz各自是氢原子或任选的取代基;条件是Cy不是环丁烯二酮基团;并且盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当生长或迁移的病症。

15. 发明授权

US08637491B2 Thieno-pyridine derivatives as MEK inhibitors 有权
标题翻译：噻吩并吡啶衍生物作为MEK抑制剂
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。

16. 发明申请

US20130296338A1 Quinoline and Quinoxaline Derivatives as Kinase Inhibitors 有权
标题翻译：喹啉和喹喔啉衍生物作为激酶抑制剂
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。

17. 发明授权

US08394822B2 Thieno-pyridine derivatives as MEK inhibitors 有权
标题翻译：噻吩并吡啶衍生物作为MEK抑制剂
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。

18. 发明申请

US20110172191A1 THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS 有权
标题翻译：作为MEK抑制剂的三苯基吡啶衍生物
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。

19. 发明授权

US07763729B2 Bicyclic heteroaromatic derivatives 失效
标题翻译：双环杂芳族衍生物
公开(公告)号：US07763729B2
公开(公告)日：2010-07-27
申请号：US12187936
申请日：2008-08-07
申请人： Daniel Christopher Brookings , Jeremy Martin Davis , Barry John Langham
发明人： Daniel Christopher Brookings , Jeremy Martin Davis , Barry John Langham
IPC分类号： C07D513/04 , A61K31/4365
CPC分类号： C07D495/04
摘要： Bicyclic heteroaromatic derivatives of formula (1) are described: F(1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a —N═ atom or a —C(Rb)═ group, or the dashed line is absent and A is a —N(Rb)—, or —C(Rb)(Rc)— group; X is an —O—, —S— or substituted nitrogen atom or a —S(O)—, —S(O2)— or —NH-group; Y is a nitrogen or substituted carbon atom or a —CH═ group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述式（1）的双环杂芳族衍生物：F（1）其中：连接A和C（R a）的虚线表示键，A为-N =原子或-C（Rb）=基团，或虚线不存在，A为-N（Rb） - 或-C（Rb）（Rc） - 基团; X是-O-，-S-或取代的氮原子或-S（O） - ， - S（O 2） - 或-NH-基团; Y是氮或取代的碳原子或-CH =基团; n为零或整数1; Alk1是任选取代的脂族或杂脂族链，L1是共价键或连接原子或基团; Cy1是氢原子或任选取代的脂环族，多环脂族，杂脂环族，多杂环脂族，芳族或杂芳族基团; Ar是任选取代的芳族或杂芳族基团; 并且其余的取代基在说明书中定义。这些化合物是p38激酶的有效和选择性抑制剂，可用于预防和治疗免疫或炎症性疾病。

20. 发明申请

US20090149437A1 THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS 有权
标题翻译：作为MEK抑制剂的三苯基吡啶衍生物
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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