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1. 发明申请

WO2009081105A3 QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2009081105A3
公开(公告)日：2009-07-02
申请号：PCT/GB2008/004171
申请日：2008-12-17
申请人： UCB PHARMA S.A. , ALLEN, Daniel, Rees , BUCKLEY, George, Martin , BÜRLI, Roland , DAVENPORT, Richard, John , KINSELLA, Natasha , LOCK, Christopher, James , LOWE, Christopher , MACK, Stephen, Robert , PITT, William, Ross , RATCLIFFE, Andrew, James , RICHARD, Marianna, Dilani , SABIN, Verity, Margaret , SHARPE, Andrew , TAIT, Laura, Jane , WARRELOW, Graham, John , WILLIAMS, Sophie, Caroline
发明人： ALLEN, Daniel, Rees , BUCKLEY, George, Martin , BÜRLI, Roland , DAVENPORT, Richard, John , KINSELLA, Natasha , LOCK, Christopher, James , LOWE, Christopher , MACK, Stephen, Robert , PITT, William, Ross , RATCLIFFE, Andrew, James , RICHARD, Marianna, Dilani , SABIN, Verity, Margaret , SHARPE, Andrew , TAIT, Laura, Jane , WARRELOW, Graham, John , WILLIAMS, Sophie, Caroline
IPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36 , A61K31/395 , A61P35/00
摘要： A series of heteroaryl-substituted quinoxaline and quinoline 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.

2. 发明申请

WO2003053958A1 QUINAZOLINEDIONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2003053958A1
公开(公告)日：2003-07-03
申请号：PCT/GB2002/005770
申请日：2002-12-18
申请人： CELLTECH R & D LIMITED , DYKE, Hazel, Joan , RICHARD, Marianna, Dilani , HAUGHAN, Alan, Findlay , SHARPE, Andrew
发明人： DYKE, Hazel, Joan , RICHARD, Marianna, Dilani , HAUGHAN, Alan, Findlay , SHARPE, Andrew
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： A compound of formula (1): wherein: X and Y, which may be the same or different, is each an O or S atom; R 1 is an aliphatic, cylcoaliphatic or cycloalkyl-akyl-group; R 2 is an optionally substituted heteroaromatic group; R 3 is the group Alk 1 -L 1 -Alk 2 -R 4 in which Alk 1 is a covalent bond or an optionally substituted aliphatic or heteroaliphatic chain, L 1 is a covalent bond or a linker atom or group, Alk 2 is a covalent bond or an optionally substituted aliphatic or thereoaliphatic chain and R 4 is a hydrogen atom or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates, tautomers, isomers or N- oxides thereof. The compounds of the present invention are potent inhibitors of IMPDH.
摘要翻译：式（1）的化合物：其中：X和Y可以相同或不同，各自为O或S原子; R 1是脂族，环脂肪族或环烷基 - 烷基; R 2是任选取代的杂芳族基团; R 3是Alk 1 -L 1 -Alk 2 -R 4，其中Alk 1是共价键或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，Alk 2是共价键或任选取代的脂族或脂环族链，R 4是氢原子或任选取代的脂环族，杂脂族，芳族或杂芳族基团; 及其盐，溶剂合物，水合物，互变异构体，异构体或N-氧化物。本发明的化合物是IMPDH的有效抑制剂。

3. 发明申请

WO2009081105A2 QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹诺酮和喹啉衍生物作为激酶抑制剂
公开(公告)号：WO2009081105A2
公开(公告)日：2009-07-02
申请号：PCT/GB2008004171
申请日：2008-12-17
申请人： UCB PHARMA SA , ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
发明人： ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
IPC分类号： C07D401/14 , A61K31/395 , A61P35/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
CPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
摘要： A series of heteroaryl-substituted quinoxaline and quinoline 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.
摘要翻译：因此，作为PI3激酶的选择性抑制剂的一系列杂芳基取代的喹喔啉和喹啉衍生物在医学中是有益的，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，伤害感受性或眼科疾病中。

4. 发明申请

WO2004022554A1 QUINAZOLINONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2004022554A1
公开(公告)日：2004-03-18
申请号：PCT/GB2003/003878
申请日：2003-09-05
申请人： CELLTECH R & D LIMITED , HAUGHAN, Alan, Findlay , BUCKLEY, George, Martin , DAVIES, Natasha , DYKE, Hazel, Joan , HANNAH, Duncan, Robert , MORGAN, Trevor , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
发明人： HAUGHAN, Alan, Findlay , BUCKLEY, George, Martin , DAVIES, Natasha , DYKE, Hazel, Joan , HANNAH, Duncan, Robert , MORGAN, Trevor , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D239/70 , C07D471/10 , C07D487/10 , C07D491/10
摘要： A compound of formula (1), wherein: X is an oxygen or sulfur atom; R 1 is an aliphatic, cycloaliphatic or cycloalkyl-alkyl- group; R 2 is an optionally substituted heteroaromatic group or a -CN group; R 3 is a group -(Alk 1 ) m L 1 (AIk 2 ) n R 4 in which m and n, which may be the same or different, is each zero or the integer 1, Alk 1 and AIk 2 , which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L 1 is a covalent bond or a linker atom or group and R 4 is a hydrogen atom or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; A is an optionally substituted cycloaliphatic or heterocycloaliphatic group optionally fused to an optionally substituted aryl or heteroaryl group; R 5 , which may be attached to any available C or N atom present in the cycloaliphatic or heterocycloaliphatic, or where fused, aryl or heteroaryl group, is a group -(AIk 3 ) t L 2 (AIk 4 ) v R 6 in which t and v, which may be the same or different, is each zero or the integer 1, Alk 3 and AIk 4 , which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L 2 is a covalent bond or a linker atom or group and R 6 is a hydrogen or halogen atom or a -CN group or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates, tautomers, isomers or N-oxides thereof. The compounds of the present invention are potent inhibitors of IMPDH.
摘要翻译：式（1）的化合物，其中：X是氧或硫原子; R 1是脂族，脂环族或环烷基 - 烷基; R 2是任选取代的杂芳基或-CN基; R 3是基团 - （Alk 1）mL -1（Alk 2）n R 4，其中m和n可以相同或不同，分别为零或整数1， Alk 1和Alk 2可以相同或不同，各自为任选取代的脂族或杂脂族链，L 1为共价键或连接原子或基团，R 4为氢原子或任选取代的脂环族，杂脂族，芳族或杂芳族基团; A是任选地与任选取代的芳基或杂芳基稠合的任选取代的脂环族或杂环脂族基; R 5可以连接在存在于脂环族或杂环脂族基中的任何可用的C或N原子上，或者其中稠合的，芳基或杂芳基是基团 - （Alk 3）tL 2（Alk <4） >）vR <6>其中可以相同或不同的t和v各自为零或整数1，Alk 3和Alk 4可以相同或不同，各自为任选地取代的脂族或杂脂族链，L 2是共价键或连接原子或基团，R 6是氢或卤素原子或-CN基团或任选取代的脂环族，杂脂族，芳族或杂芳族基团; 及其盐，溶剂合物，水合物，互变异构体，异构体或N-氧化物。本发明的化合物是IMPDH的有效抑制剂。

5. 发明申请

WO2007141504A1 FUSED THIOPHENE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：熔化的噻吩衍生物作为激酶抑制剂
公开(公告)号：WO2007141504A1
公开(公告)日：2007-12-13
申请号：PCT/GB2007/002051
申请日：2007-06-04
申请人： UCB PHARMA S.A. , ALEXANDER, Rikki Peter , BAILEY, Stuart , BRAND, Stephen , BROOKINGS, Daniel Christopher , BROWN, Julien Alistair , HAUGHAN, Alan Findlay , KINSELLA, Natasha , LOWE, Christopher , MACK, Stephen Robert , PITT, William Ross , RICHARD, Marianna Dilani , SHARPE, Andrew , TAIT, Laura Jane
发明人： ALEXANDER, Rikki Peter , BAILEY, Stuart , BRAND, Stephen , BROOKINGS, Daniel Christopher , BROWN, Julien Alistair , HAUGHAN, Alan Findlay , KINSELLA, Natasha , LOWE, Christopher , MACK, Stephen Robert , PITT, William Ross , RICHARD, Marianna Dilani , SHARPE, Andrew , TAIT, Laura Jane
IPC分类号： C07D333/66 , C07D333/68 , C07D409/12 , C07D409/14 , C07D451/04 , C07D453/02 , C07D471/04 , C07D495/04 , A61K31/55 , A61K31/5377 , A61P3/00
CPC分类号： C07D333/66 , C07D333/68 , C07D333/76 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D453/02 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, 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.
摘要翻译：一系列5位二氢-1-苯并噻吩-7（4H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4-基部分取代，为PI3激酶的选择性抑制剂酶在医学上有益，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，伤害性感受性或眼科疾病中。

6. 发明申请

WO2004018462A1 QUINAZOLINONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2004018462A1
公开(公告)日：2004-03-04
申请号：PCT/GB2003/003600
申请日：2003-08-18
申请人： CELLTECH R & D LIMITED , HAUGHAN, Alan, Findlay , BUCKLEY, George, Martin , DYKE, Hazel, Joan , HANNAH, Duncan, Robert , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
发明人： HAUGHAN, Alan, Findlay , BUCKLEY, George, Martin , DYKE, Hazel, Joan , HANNAH, Duncan, Robert , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： A compound of formula (1): wherein: X is an oxygen or sulfur atom; R 1 is an aliphatic, cycloaliphatic or cycloalkyl-alkyl-group; R 2 is an optionally substituted heteroaromatic group or a -CN group; R 3 is a group -(Alk 1 ) m L 1 (Alk 2 ) n R 6 in which m and n, which may be the same or different, is each zero or the integer 1, Alk 1 and Alk 2 , which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L 1 is a covalent bond or a linker atom or group and R 6 is a hydrogen atom or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; R 4 is a group -(Alk 3 ) p L 2 (Alk 4 ) q R 7 in which p and q, which may be the same or different, is each zero or the integer 1, Alk 3 and Alk 4 , which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L 2 is a covalent bond or a linker atom or group and R 7 is a hydrogen or halogen atom or a -CN group or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; R 5 is a hydrogen atom or an optionally substituted aliphatic group; and the salts, solvates, hydrates, tautomers, isomers or N-oxides thereof. The compounds of the present invention are potent inhibitors of IMPDH.
摘要翻译：式（1）的化合物：其中：X是氧或硫原子; R 1是脂族，脂环族或环烷基 - 烷基; R 2是任选取代的杂芳基或-CN基; R 3是基团 - （Alk 1）·mL -1（Alk 2）n R 6，其中m和n可以相同或不同，分别为零或整数1， Alk 1和Alk 2可以相同或不同，各自为任选取代的脂族或杂脂族链，L 1为共价键或连接原子或基团，R 6为氢原子或任选取代的脂环族，杂脂族，芳族或杂芳族基团; R 4是基团 - （Alk 3）pL 2（Alk 4）q R 7，其中可以相同或不同的p和q各自为零或整数1， Alk 3和Alk 4可以相同或不同，各自为任选取代的脂族或杂脂族链，L 2为共价键或连接原子或基团，R 7为氢或卤素原子或-CN基团或任选取代的脂环族，杂脂族，芳族或杂芳族基团; R 5是氢原子或任选取代的脂族基团; 及其盐，溶剂合物，水合物，互变异构体，异构体或N-氧化物。本发明的化合物是IMPDH的有效抑制剂。

7. 发明申请

WO2003035066A1 2-AMINOQUINOLONE DERIVATIVES FOR USE AS IMPDH INHIBITORS 审中-公开
标题翻译：用作IMPDH抑制剂的2-氨基喹啉衍生物
公开(公告)号：WO2003035066A1
公开(公告)日：2003-05-01
申请号：PCT/GB2002/004754
申请日：2002-10-22
申请人： CELLTECH R & D LIMITED , HAUGHAN, Alan, Findlay , DYKE, Hazel, Joan , BUCKLEY, George, Martin , DAVIES, Natasha , HANNAH, Duncan, Robert , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
发明人： HAUGHAN, Alan, Findlay , DYKE, Hazel, Joan , BUCKLEY, George, Martin , DAVIES, Natasha , HANNAH, Duncan, Robert , RICHARD, Marianna, Dilani , SHARPE, Andrew , WILLIAMS, Sophie, Caroline
IPC分类号： A61K31/422
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/04 , C07D413/14
摘要： Quinolone derivatives of formula (1) are described; wherein: X is an O or S atom; R 1 is an aliphatic, cycloaliphatic, or cycloalkyl-alkyl-group; R 2 is a -CN group or an optionally substituted heteroaromatic group; R 3 is a hydrogen atom or an alkyl, -CN, -CO 2 H, -CO 2 R 6 or -CONR 7 R 8 group; R 4 is a chain -Alk 1 -L 1 -Alk 2 -R 9 ; R 5 is a hydrogen atom or an alkyl group; or NR 4 R 5 forms an optionaly substituted heterocycloaliphatic ring optionally fused to an optionally substituted monocylcic C 6-12 aromatic group or an optionally substituted monocyclic C 1-9 heteroaromatic group; and the salts, solvates, hydrates, tautomers, isomers or N -oxides thereof. The compounds are potent inhibitors of IMPDH and are of use as immunosuppressants, anti-cancer agents, anti-inflammatory agents, antipsoriatic and anti-viral agents.
摘要翻译：描述了式（1）的喹诺酮衍生物; 其中：X是O或S原子; R 1是脂族，脂环族或环烷基 - 烷基; R 2是-CN基团或任选取代的杂芳族基团; R 3是氢原子或烷基，-CN，-CO 2 S，H，-CO 2 s，R 6，sp >或-CONR R 8 组; R 4 是链-Alk -L 1 -Alk SP>; R 5是氢原子或烷基; 或任选地与任选取代的单环C 6-12芳族基团或任选取代的单环的稠合的任选的杂环脂族环杂芳族基团; 及其盐，溶剂合物，水合物，互变异构体，异构体或其N-氧化物。这些化合物是IMPDH的有效抑制剂，可用作免疫抑制剂，抗癌剂，抗炎剂，抗牛皮癣和抗病毒剂。

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