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1. 发明授权

US08283359B2 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：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。

2. 发明申请

US20110021558A1 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：US20110021558A1
公开(公告)日：2011-01-27
申请号：US12839752
申请日：2010-07-20
申请人： Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham
发明人： Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham
IPC分类号： A61K31/4365 , C07D495/04 , A61P35/00 , A61P29/00 , A61P9/12 , A61P7/02 , A61P9/04 , A61P9/00 , A61P19/02 , A61P25/00 , A61P11/06 , A61P17/06
CPC分类号： C07D495/04 , C07D519/00
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。

3. 发明申请

US20100179124A1 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：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。

4. 发明授权

US07592455B2 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：US07592455B2
公开(公告)日：2009-09-22
申请号：US10524199
申请日：2003-08-11
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： C07D513/02
CPC分类号： C07D495/04
摘要： A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-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：一系列基于6-氧代-6,7-二氢噻吩并[2,3-b]吡啶环体系的5-6稠环双环杂芳族衍生物是p38激酶的抑制剂，因此可用于医药，例如在治疗和/或预防免疫或炎性疾病中。

5. 发明授权

US07423047B2 Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors 失效
标题翻译：芳胺取代的双环杂芳族化合物作为p38激酶抑制剂
公开(公告)号：US07423047B2
公开(公告)日：2008-09-09
申请号：US10518725
申请日：2003-06-20
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： 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：描述了式（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是-N-原子或或者虚线不存在，A是-N（R b） - 或-C（R b）（R c）） - 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; Alk 1是任选取代的脂族或杂脂族链L 1是共价键或连接原子或基团; Cy 1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。

6. 发明授权

US06740654B2 Squaric acid derivatives 失效
标题翻译：方酸衍生物
公开(公告)号：US06740654B2
公开(公告)日：2004-05-25
申请号：US09899488
申请日：2001-07-05
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07D23514
CPC分类号： C07D495/04 , C07D235/30
摘要： Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl 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：描述式（1）的方酸衍生物：其中Het是任选取代的双环稠环杂芳族基团; L 2是共价键或-O - ， - S - ， - C（O） - ， -C（S） - ， - S（O） - ， - S（O）2，-N（R 8） - 或-C（R 8）（R 8a） - ; Ar 2 >是任选取代的芳族或杂芳族基团; Alk是一种链霉素，其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; R 1是氢原子或C 1-6烷基; L 1，是共价键或连接原子或基团; Alk 1是任选取代的脂族链; n是0或整数1; R 2是氢原子或任选取代的杂脂肪族，脂环族，杂脂族，多环烷基，除2,6-二氮杂萘-1-基，异喹啉-1-基，2,7-萘啶-1-基或喹唑啉-4-基之外的杂多环脂族，芳族或杂芳族基;以及盐，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。

7. 发明授权

US06403608B1 3-Substituted isoquinolin-1-yl derivatives 失效
标题翻译： 3-取代的异喹啉-1-基衍生物
公开(公告)号：US06403608B1
公开(公告)日：2002-06-11
申请号：US09867060
申请日：2001-05-29
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07D21708
CPC分类号： C07D401/12 , C07D217/22 , C07D217/24 , C07D417/12 , C07D487/08
摘要： 3-Substituted isoquinoline containing squaric acids of formula (1) are described: wherein Ar1 is a 3-substituted isoquinolin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic 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 disordes or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了含有式（1）的方酸的3-取代的异喹啉：其中Ar1是3-取代的异喹啉-1-基; L2是共价键或连接原子或基团; Ar2是任选取代的芳族或杂芳族链; Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链霉素; R 1是氢原子或C 1-6烷基; L 1是共价键或连接原子或基团; Alk1是任选取代的脂族链; n为零或整数1; R 2为氢原子或任选取代的杂脂族，脂环族，杂环脂族，多环芳族，杂多环脂族，芳族或杂芳族基团;及其盐，溶剂合物，水合物和N-氧化物。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涉及细胞不适当生长或迁移的免疫或炎症性紊乱或紊乱。

8. 发明授权

US08487101B2 Thieno-pyridine derivatives as MEK inhibitors 有权
公开(公告)号：US08487101B2
公开(公告)日：2013-07-16
申请号：US12839752
申请日：2010-07-20
申请人： Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham
发明人： Daniel Christopher Brookings , Martin Clive Hutchings , Barry John Langham
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D519/00
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.

9. 发明申请

US20090264411A1 FUSED THIOPHENE DERIVATIVES AS MEK INHIBITORS 审中-公开
标题翻译：熔化的THIOPHENE衍生物作为MEK抑制剂
公开(公告)号：US20090264411A1
公开(公告)日：2009-10-22
申请号：US12371124
申请日：2009-02-13
申请人： Victoria Elizabeth Laing , Daniel Christopher Brookings , Rachel Jane Carbery , Jose Miguel Gascon Simorte , Martin Clive Hutchings , Barry John Langham , Martin Alexander Lowe
发明人： Victoria Elizabeth Laing , Daniel Christopher Brookings , Rachel Jane Carbery , Jose Miguel Gascon Simorte , Martin Clive Hutchings , Barry John Langham , Martin Alexander Lowe
IPC分类号： A61K31/55 , A61K31/4365 , A61K31/381 , C07D513/04 , C07D333/52
CPC分类号： C07D495/04
摘要： A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, 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4,5,6,7-四氢噻吩并[2,3-c]吖庚因-8-酮衍生物及其类似物，其在2-位被取代的苯胺基部分取代，是人MEK的选择性抑制剂（MAPKK）酶相应地在医学中有益，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）中。

10. 发明授权

US06455539B2 Squaric acid derivates 失效
标题翻译：方酸衍生物
公开(公告)号：US06455539B2
公开(公告)日：2002-09-24
申请号：US09742038
申请日：2000-12-21
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07C22914
CPC分类号： C07D471/04 , C07C229/34 , C07C229/36 , C07C2601/04
摘要： Squaric acid derivatives of formula (1) are described: wherein R1 is a group Ar1Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6 alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic 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：描述式（1）的方酸衍生物：其中R1是Ar1Ar2Alk-基团，其中Ar1是任选取代的芳族或杂芳族基团; Ar2是任选取代的亚苯基或含氮六元杂亚芳基; 并且Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸（-CO 2 H）或其衍生物或生物固体; R 2是氢原子或C1- 6烷基; L1是共价键或连接原子或基团; n为零或整数1; Alk1为任选取代的脂族链; R3为氢原子或任选取代的杂脂肪族，脂环族，杂环脂族，多环脂族，杂多环脂族，芳族或杂芳族基团：及其盐，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的生长或迁移。

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