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1. 发明授权

US07309800B2 Biphenylcarboxylic amide derivatives as p38 kinase inhibitors 失效
标题翻译：联苯羧酰胺衍生物作为p38激酶抑制剂
公开(公告)号：US07309800B2
公开(公告)日：2007-12-18
申请号：US11556285
申请日：2006-11-03
申请人： Richard Martyn Angell , Nicola Mary Aston , Paul Bamborough , Mark James Bamford , George Stuart Cockerill , Stephen Sean Flack , Dramane Ibrahim Lainé , Ann Louise Walker
发明人： Richard Martyn Angell , Nicola Mary Aston , Paul Bamborough , Mark James Bamford , George Stuart Cockerill , Stephen Sean Flack , Dramane Ibrahim Lainé , Ann Louise Walker
IPC分类号： C07C231/02 , C07D207/04 , C07D271/10 , C07D233/54 , C07D285/04 , C07D401/10 , C07D403/10 , C07D265/30
CPC分类号： C07D213/81 , C07D231/12 , C07D233/56 , C07D249/08 , C07D261/18 , C07D307/46 , C07D307/68 , C07D333/38 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12
摘要： Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的盐或溶剂合物，以及它们作为药物的用途，特别是作为p38激酶抑制剂。

2. 发明授权

US06391874B1 Fused heterocyclic compounds as protein tyrosine kinase inhibitors 有权
标题翻译：稠合杂环化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US06391874B1
公开(公告)日：2002-05-21
申请号：US09214267
申请日：1998-12-31
申请人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
发明人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
IPC分类号： A61K31506
CPC分类号： C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14
摘要： Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NRa wherein Ra is hydrogen or a C1-8 alkyl group; R1 represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R1 being optionally substituted by one or more R3;groups; P=0 to 3; U, R2, R3 are as defined in the application.
摘要翻译：取代的式（I）的杂芳族化合物，特别是取代的喹啉和喹唑啉是蛋白质酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣，或其盐或溶剂合物; 其中X是N或CH; Y是W（CH2），（CH2）W或W，其中W是O，S（O）m，其中m是0,1或2，或NRa，其中Ra是氢或C1-8烷基 ; R 1表示苯基或含有1至4个选自N，O或S（O）m的杂原子的5或6元杂环，其中m如上所定义，条件是该环不含有两个相邻的 O或S（O）m原子，并且其中环仅含有N作为杂原子的环，该环与喹唑啉或喹啉环C-连接，R 1任选被一个或多个R 3;基团取代; P = 0〜3; U，R2，R3如申请中所定义。

3. 发明授权

US06207669B1 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US06207669B1
公开(公告)日：2001-03-27
申请号：US09214261
申请日：1998-12-31
申请人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
发明人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07C217/86 , C07C317/36
摘要： Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds in which one ring is a pyridine or pyrimidine of formula (I) are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是其中一个环是式（I）的吡啶或嘧啶的取代的双环杂芳族化合物是蛋白质酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

4. 发明申请

US20110053934A1 COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：化合物和治疗方法
公开(公告)号：US20110053934A1
公开(公告)日：2011-03-03
申请号：US12691258
申请日：2010-01-21
申请人： RICHARD MARTYN ANGELL , IAN ROBERT BALDWIN , GEORGE STUART COCKERILL , STEPHEN SEAN FLACK , KAREN ELIZABETH LACKEY , PHILIP ALAN SKONE , KATHRYN JANE SMITH
发明人： RICHARD MARTYN ANGELL , IAN ROBERT BALDWIN , GEORGE STUART COCKERILL , STEPHEN SEAN FLACK , KAREN ELIZABETH LACKEY , PHILIP ALAN SKONE , KATHRYN JANE SMITH
IPC分类号： A61K31/5377 , C07D401/10 , A61K31/4709 , C07D413/12 , C07D413/14 , A61P35/00
CPC分类号： A61K31/4353 , A61K31/535
摘要： A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.
摘要翻译：本文描述了可用作ret激酶抑制剂的衍生物。所描述的发明还包括使用该方法治疗由不适当的ret激酶活性介导的疾病的方法。

5. 发明申请

US20100120804A1 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 有权
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US20100120804A1
公开(公告)日：2010-05-13
申请号：US12691784
申请日：2010-01-22
申请人： Malcom Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
发明人： Malcom Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
IPC分类号： A61K31/517 , C07D239/86 , A61P35/00
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： A process for the preparation of a compound of formula (I) comprising the steps:(a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups,with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译：一种制备式（I）化合物的方法，包括以下步骤：（a）将其中L和L'是合适的离去基团的式（II）化合物与式（III）化合物UNH2（III）制备式（Ⅳ）化合物，随后（b）用置换基团L'代替基团R 1。

6. 发明授权

US08513262B2 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 有权
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US08513262B2
公开(公告)日：2013-08-20
申请号：US12691784
申请日：2010-01-22
申请人： Malcolm Clive Carter , George Stuart Cockerill , Karen Elizabeth Lackey
发明人： Malcolm Clive Carter , George Stuart Cockerill , Karen Elizabeth Lackey
IPC分类号： A01N43/90 , A61K31/519 , C07D239/72
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译：一种制备式（I）化合物的方法，包括以下步骤：（a）将其中L和L'是合适的离去基团的式（II）化合物与式（III）化合物UNH2（III）制备式（Ⅳ）化合物，随后（b）用置换基团L'代替基团R 1。

7. 发明授权

US07432289B2 5-Acylamino-1,1′-biphenyl-4-carboxamide derivatives and their use as P38 kinase inhibitors 失效
标题翻译： 5-酰氨基-1,1'-联苯-4-甲酰胺衍生物及其作为P38激酶抑制剂的用途
公开(公告)号：US07432289B2
公开(公告)日：2008-10-07
申请号：US10492605
申请日：2002-10-16
申请人： Richard Martyn Angell , Nicola Mary Aston , Paul Bamborough , Mark James Bamford , George Stuart Cockerill , Stephen Sean Flack , Dramane Ibrahim Lainé , Suzanne Joy Merrick , Kathryn Jane Smith , Ann Louise Walker
发明人： Richard Martyn Angell , Nicola Mary Aston , Paul Bamborough , Mark James Bamford , George Stuart Cockerill , Stephen Sean Flack , Dramane Ibrahim Lainé , Suzanne Joy Merrick , Kathryn Jane Smith , Ann Louise Walker
IPC分类号： A61K31/44 , A61K31/04 , A61K31/34 , A61K33/44 , C07D307/02 , C07C241/00
CPC分类号： C07D207/27 , C07C237/42 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/327 , C07D213/81 , C07D213/82 , C07D215/50 , C07D239/28 , C07D239/42 , C07D241/24 , C07D241/26 , C07D261/18 , C07D277/56 , C07D307/24 , C07D307/54 , C07D307/68 , C07D309/08 , C07D333/38 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的盐或溶剂合物，以及它们作为药物的用途，特别是作为p38激酶抑制剂。

8. 发明授权

US07384963B2 2′-Methyl-5-(1,3,4-oxadiazol-2-yl)1, 1′-biphenyl-4-carboxaide derivatives and their use as p38 kinase 失效
标题翻译： 2'-甲基-5-（1,3,4-恶二唑-2-基）1,1'-联苯-4-羧酸衍生物及其作为p38激酶的用途
公开(公告)号：US07384963B2
公开(公告)日：2008-06-10
申请号：US10492713
申请日：2002-10-16
申请人： Richard Martyn Angell , Paul Bamborough , George Stuart Cockerill , Ann Louise Walker
发明人： Richard Martyn Angell , Paul Bamborough , George Stuart Cockerill , Ann Louise Walker
IPC分类号： A61K31/4245 , C07D271/10
CPC分类号： C07D271/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12
摘要： Compounds of formula (I), wherein R1 is a phenyl group which may be optionally substituted; R2 is selected from hydrogen, C1-6 alkyl and (CH2)p—C3-7cycloalkyl; R3 is the group: (Formula II), R4 is selected from hydrogen and C1-4 alkyl; U is selected from methyl and halogen; X and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4, and may be optionally substituted with up to two groups selected independently from C1-6 alkyl; n is selected from 0, 1 and 2; p is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors
摘要翻译：式（I）的化合物，其中R 1是可任意取代的苯基; R 2选自氢，C 1-6烷基和（CH 2 CH 2）n-C≡S<！ - SIPO < > 3-7环烷基; R 3是下列基团：（式II），R 4选自氢和C 1-4烷基; U选自甲基和卤素; X和Y各自独立地选自氢，甲基和卤素; m选自0,1,2,3和4，并且可以任选地被至多两个独立地选自C 1-6烷基的基团取代; n选自0,1和2; p选自0，1和2; 或其药学上可接受的盐或溶剂化物，以及它们作为药物的用途，特别是作为p38激酶抑制剂

9. 发明申请

US20080114008A1 Quinazoline Derivatives as Antiviral Agents 审中-公开
标题翻译：喹唑啉衍生物作为抗病毒剂
公开(公告)号：US20080114008A1
公开(公告)日：2008-05-15
申请号：US11883191
申请日：2006-01-30
申请人： George Stuart Cockerill , Stephen Sean Flack , Neil Mathews , James Iain Salter
发明人： George Stuart Cockerill , Stephen Sean Flack , Neil Mathews , James Iain Salter
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07C255/61 , C07D239/94
摘要： Compounds of formula (I) are found to be active in inhibiting replication of flaviviridac Formula (I) wherein: X represents a direct bond or a moiety -L-NR—, wherein R is hydrogen or C1-C4 alkyl, and L represents a C1-C4alkylene, C6-C10 aryl or 5- to 10-membered heteroaryl moiety; either R1 and R2, together with the N atom to which they are attached, form a 5- to 10-membered heterocyclyl group or a 5- to 10-membered heteroaryl group, or R1 represents hydrogen, C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl and R2 represents C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl; and R3 represents a C6-C10 aryl, C3-C6 carbocyclyl, 5- to 10-membered heteroaryl or 5- to 10-membered heterocyclyl moiety, said aryl, carbocyclyl, heteroaryl and heterocyclyl groups being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxy, thiol, —NH2, C1-C4 hydroxyalkyl, C1-C4 thioalkyl and C1-C4aminoalkyl substituents.
摘要翻译：发现式（I）化合物在抑制黄病毒复方（I）中具有活性，其中：X表示直接键或部分-L-NR-，其中R为氢或C 1〜 -C 4烷基，L表示C 1 -C 4亚烷基，C 6 -C 3亚烷基 > 10 芳基或5至10元杂芳基部分; R 1和R 2 2与它们所连接的N原子一起形成5-至10-元杂环基或5-至10-元杂芳基或R 1代表氢，C 6 -C 10芳基，C 1 -C 3 > 4个C 1 -C 4烷基或C 1 -C 4羟基烷基，R 2表示C 6 -C C 1 -C 10芳基，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 羟烷基和R 3表示C 6 -C 10芳基，C 3 -C 6 - 所述芳基，碳环基，杂芳基和杂环基是未被取代的或被1,2或3个选自卤素，C 1 -C 6烷基的取代基取代的杂芳基， C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 3亚烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，卤代烷基，C 1 -C 4卤代烷氧基，羟基，硫醇，-NH 2，C 1， C 1 -C 4 - 羟基烷基，C 1 -C 4硫代烷基和C 1 -C 3 - 4个氨基烷基取代基。

10. 发明授权

US07265123B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US07265123B2
公开(公告)日：2007-09-04
申请号：US11562047
申请日：2006-11-21
申请人： George Stuart Cockerill , Karen Elizabeth Lackey
发明人： George Stuart Cockerill , Karen Elizabeth Lackey
IPC分类号： C07D521/00 , A61K31/519
CPC分类号： C07D405/04 , C07D239/94 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/02
摘要： Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
摘要翻译：描述了杂芳族化合物，其制备方法，含有它们的药物组合物，使用方法及其在药物中的用途。特别地，本发明涉及蛋白酪氨酸激酶抑制的喹唑啉和吡啶并嘧啶衍生物。

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