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11. 发明申请

US20100305066A1 Fused Thiophene Derivatives as Kinase Inhibitors 有权
标题翻译：稠合噻吩衍生物作为激酶抑制剂
公开(公告)号：US20100305066A1
公开(公告)日：2010-12-02
申请号：US12303713
申请日：2007-06-04
申请人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
发明人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
IPC分类号： A61K31/695 , C07D413/04 , A61K31/5377 , C07D413/14 , C07F7/08 , C07D495/04 , A61K31/55 , A61P3/00 , A61P13/00 , A61P9/00 , A61P25/00 , A61P27/02 , A61P37/00
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。

12. 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。

13. 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。

14. 发明授权

US06297264B1 Trisubstituted phenyl derivatives and process for their preparation 失效
标题翻译：三取代苯基衍生物及其制备方法
公开(公告)号：US06297264B1
公开(公告)日：2001-10-02
申请号：US09048594
申请日：1998-03-26
申请人： John Clifford Head , Graham John Warrellow , Rikki Peter Alexander
发明人： John Clifford Head , Graham John Warrellow , Rikki Peter Alexander
IPC分类号： A61K31435
CPC分类号： C07D213/30 , C07D213/32 , C07D213/38
摘要： Compounds of the general formula (1) are described wherein W is a ═N—, and Z and L are described in the specifications. These compounds are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：描述通式（1）的化合物，其中W是a = N-，Z和L在说明书中描述。这些化合物是IV型磷酸二酯酶抑制剂，可用于预防和治疗诸如哮喘的疾病，其中存在不希望的炎性反应或肌肉痉挛。

15. 发明授权

US5866593A Trisubstituted phenyl derivatives and processes for their preparation 失效
标题翻译：三取代苯基衍生物及其制备方法
公开(公告)号：US5866593A
公开(公告)日：1999-02-02
申请号：US964041
申请日：1997-11-04
申请人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
发明人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
IPC分类号： A61K31/41 , A61K31/44 , A61P1/04 , A61P11/00 , A61P29/00 , C07D413/10 , A61K31/42 , C07D213/24 , C07D401/06
CPC分类号： C07D413/10
摘要： Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.n Ar' where Ar' is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms or is Ar; R.sup.6 is hydrogen or optionally substituted alkyl; and R.sup.7 is hydrogen or optionally substituted alkyl; or a salt, solvate or hydrate thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：描述通式（1）的化合物（1）其中Y是卤素或-OR 1，其中R 1是任选取代的烷基; X是-O - ， - S-或-N（R 8） - ，其中R 8是氢或烷基; R2是任选取代的烷基，烯基，环烷基或环烯基; R3是氢，卤素或-OR9，其中R9是氢或任选取代的烷基，烯基，烷氧基烷基或烷酰基，或甲酰基，甲酰胺基或硫代羧酰胺基; R4是 - （CH2）nAr，其中Ar是任选地含有一个或多个选自氧，硫和氮原子的杂原子的单环或双环芳基，其中Ar被任选地含有一个或多个选自以下的杂原子的任选取代的C3-9环脂族基团取代：氧，硫或-N（R8） - ，n为零或整数1,2或3; R5是 - （CH2）nAr'，其中Ar'是任选含有一个或多个选自氧，硫或氮原子的杂原子的单环或二环芳基或Ar; R6是氢或任选取代的烷基; 并且R 7是氢或任选取代的烷基; 或其盐，溶剂合物或水合物。根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂，并且可用于预防和治疗诸如哮喘的疾病，其中存在不想要的炎症反应或肌肉痉挛。

16. 发明授权

US5780478A Tetra-substituted phenyl derivatives 失效
标题翻译：四取代苯基衍生物
公开(公告)号：US5780478A
公开(公告)日：1998-07-14
申请号：US493264
申请日：1995-06-21
申请人： Rikki Peter Alexander , Graham John Warrellow
发明人： Rikki Peter Alexander , Graham John Warrellow
IPC分类号： C07D213/30 , A61K31/44 , C07D213/34 , C07D213/64
CPC分类号： C07D213/30
摘要： Compounds of general formula (1): ##STR1## are described wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl, or --X.sup.a R.sup.1 group where X.sup.a is --O--, --S(O).sub.m -- �where m is zero or an integer of value 1 or 2!, or --N(R.sup.a)-- �where R.sup.a is a hydrogen atom or an optionally substituted alkyl group! and R.sup.1 is a hydrogen atom or an optionally substituted alkyl group or, (2) .dbd.N--; X is as described above for X.sup.a or is a chain --CR.dbd.C(R.sup.b)-- or �--CH(R)!.sub.q --CH(R.sup.b)-- where R is a hydrogen or a fluorine atom or a methyl group, R.sup.b is as described below for R.sup.2 and q is zero or the integer 1; R.sup.2 is (1) an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group when X is --O--, --S(O).sub.m -- or --N(R.sup.a)--; atoms or groups; R.sup.3 is an atom or group R.sup.13 ; R.sup.4 is a hydrogen atom or is as defined for R.sup.6 ; R.sup.5 is a hydrogen or a fluorine atom; R.sup.6 is a group --(CH.sub.2).sub.n Ar where Ar is an optionally and R.sup.8, which may be the same or different, is a hydrogen or a fluorine atom, or an optionally substituted straight or branched alkyl group; and the salts, solvates, prodrugs, hydrates and N-oxides thereof. Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：描述通式（1）的化合物：其中= W-是（1）= C（Y） - 其中Y是卤素原子，或烷基或-XaR1基团，其中Xa是-O - ， - S（O）m - [其中m为零或值为1或2的整数]或-N（R a） - [其中R a为氢原子或任选取代的烷基]，R 1为氢原子或任选取代的烷基，或（2）= N- X如上所述对于Xa或是链-CR = C（Rb） - 或[-CH（R）] q-CH（Rb） - 其中R是氢或氟原子或甲基，Rb是如下面对于R2所述，q是0或整数1; 当X是-O - ， - S（O）m - 或-N（R a） - 时，R 2是（1）任选取代的烷基，烯基，环烷基或环烯基; 原子或基团; R3是原子或基团R13; R 4是氢原子或如R6所定义; R5是氢或氟原子; R 6是 - （CH 2）n Ar基团，其中Ar是任选的，R 8可以相同或不同，是氢或氟原子，或任选取代的直链或支链烷基; 及其盐，溶剂合物，前体药物，水合物和N-氧化物。根据本发明的化合物是IV型磷酸二酯酶抑制剂，可用于预防和治疗诸如哮喘的疾病，其中存在不希望的炎性反应或肌肉痉挛。

17. 发明授权

US5776958A Trisubstituted phenyl derivatives and processes for their preparation 失效
标题翻译：三取代苯基衍生物及其制备方法
公开(公告)号：US5776958A
公开(公告)日：1998-07-07
申请号：US360563
申请日：1994-12-21
申请人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander , Michael Anthony William Eaton
发明人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander , Michael Anthony William Eaton
IPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4418 , A61P11/08 , A61P29/00 , A61P43/00 , C07D213/64 , C07D231/20 , C07D261/12 , C07D211/86
CPC分类号： C07D213/64 , C07D231/20 , C07D261/12
摘要： Compounds of general formula (1): ##STR1## wherein Y is a halogen atom or a group --OR.sup.1 where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 is a hydrogen or halogen atom or an --OR.sup.9 group, where R.sup.9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group; R.sup.4 is a group --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3; R.sup.5 is a C.sub.3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.6 is a hydrogen atom or an optionally substituted alkyl group; R.sup.7 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：通式（1）的化合物：其中Y是卤素原子或基团-OR1，其中R1是任意取代的烷基; X是-O - ， - S-或-N（R 8） - ，其中R 8是氢原子或烷基; R2是任选取代的烷基，烯基，环烷基或环烯基; R3是氢或卤原子或-OR9基团，其中R9是氢原子或任选取代的烷基，烯基，烷氧基烷基或烷酰基，或甲酰基，甲酰氨基或硫代羧酰胺基; R4是 - （CH2）nAr基团，其中Ar是任选地含有一个或多个选自氧，硫或氮原子的杂原子的单环或双环芳基，n是0或1,2或3的整数; R5是任选地含有一个或多个选自氧，硫或氮原子的杂原子的C3-9碳环酮; R6是氢原子或任选取代的烷基; R7是氢原子或任选取代的烷基; 及其盐，溶剂合物，水合物和N-氧化物。根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂，并且可用于预防和治疗诸如哮喘的疾病，其中存在不想要的炎症反应或肌肉痉挛。

18. 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。

19. 发明授权

US06245774B1 Tri-substituted phenyl or pyridine derivatives 失效
公开(公告)号：US06245774B1
公开(公告)日：2001-06-12
申请号：US08492855
申请日：1995-06-20
申请人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
发明人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
IPC分类号： C07D21338
CPC分类号： C07D213/30 , C07D409/12
摘要： Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12C(S)—, —C(S)NR12—, —C≡C—, —NR12SO2—, or —SO2NR12—; Alk is an optionally substituted straight or branched alkyl chain optionally interrupted by an atom or group X; t is zero or an integer of value 1, 2 or 3; R3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group or an OR11 group [where R11 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group]; R4 is a hydrogen atom or an optionally substituted alkyl, —CO2R8, —CSNR9R10, —CN, —CH2CN, or —(CH2)tAr group where t is zero or an integer of value 1, 2 or 3 and Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; provided that when L is a group of type (2) or (3) above then Z is a group of type (A) or type (B) in which R4 is a —(CH2)tAr group; R5 is a group —(CH2)tAr; R6 is a hydrogen or a fluorine atom, or an optionally substituted alkyl or —CO2R8, —CONR9R10, —CSNR9R10, —CN or —CH2CN group; R7 is a hydrogen or a fluorine atom, an optionally substituted straight or branched alkyl group, or an ORc group where Rc is a hydrogen atom or an optionally substituted alkyl or alkenyl group, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where unwanted inflammatory response or muscular spasm is present.

20. 发明授权

US07795256B2 Thieno-pyridinone derivatives as kinase inhibitors 失效
标题翻译：噻吩并吡啶酮衍生物作为激酶抑制剂
公开(公告)号：US07795256B2
公开(公告)日：2010-09-14
申请号：US10576731
申请日：2004-10-22
申请人： Rikki Peter Alexander , Jeremy Martin Davis , Martin Clive Hutchings , Victoria Elizabeth Laing , Graham Peter Trevitt
发明人： Rikki Peter Alexander , Jeremy Martin Davis , Martin Clive Hutchings , Victoria Elizabeth Laing , Graham Peter Trevitt
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4365 , C07D495/04
CPC分类号： C07D495/04
摘要： A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 3-position by an arylcarbonyl or heteroaryl-carbonyl moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
摘要翻译：一系列由芳基羰基或杂芳基 - 羰基部分在3-位被取代为p38 MAP激酶的抑制剂的噻吩并[2,3-b]吡啶-6（7H） - 酮衍生物，因此可用于医药，例如在治疗和/或预防免疫或炎性疾病中。

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