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1. 发明申请

WO2009093013A1 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：WO2009093013A1
公开(公告)日：2009-07-30
申请号：PCT/GB2009/000151
申请日：2009-01-20
申请人： UCB PHARMA S.A. , BROOKINGS, Daniel Christopher , LAING, Victoria Elizabeth , LANGHAM, Barry John
发明人： BROOKINGS, Daniel Christopher , LAING, Victoria Elizabeth , LANGHAM, Barry John
IPC分类号： C07D495/04 , A61K31/428 , A61K31/429 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04
摘要： A series of 7-oxo-4,5,6,7-tetrahydrothieno[2,3-c]pyridine 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：由2-取代的苯胺基部分取代的一系列7-氧代-4,5,6,7-四氢噻吩并[2,3-c]吡啶衍生物及其类似物是人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。

2. 发明申请

WO2009093008A1 THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS 审中-公开
标题翻译：作为MEK抑制剂的三苯基吡啶衍生物
公开(公告)号：WO2009093008A1
公开(公告)日：2009-07-30
申请号：PCT/GB2009/000144
申请日：2009-01-20
申请人： UCB PHARMA S.A. , BROOKINGS, Daniel Christopher , HUTCHINGS, Martin Clive , LANGHAM, Barry John
发明人： BROOKINGS, Daniel Christopher , HUTCHINGS, Martin Clive , LANGHAM, Barry John
IPC分类号： C07D495/04 , C07D519/00
CPC分类号： C07D495/04 , C07D519/00
摘要： The invention provides a series of thieno[2,3-b]pyridine derivatives wherein Y represents a linkage of formula C(O) or S(O) 2 ; R 1 represents hydrogen, halogen, cyano, nitro, C|-6 alkyl, trifluoromethyl, Ci.6 alkoxy, trifluoromethoxy, C 1-6 alkylthio, C 1-6 alkylsulphinyl or C 1-6 alkylsulphonyl; R 2 represents halogen, nitro, cyano, C 1-6 alkyl, C 2-6 alkynyl, hydroxy(C 1-6 )alkyl or formyl; and R 3 represents a group of formula (a), (b), (c), (d) or (e): wherein the asterisk (*) represents the point of attachment to the remainder of the molecule. The compounds of formula (I) are selective inhibitors of human MEK (MAPICIC) enzymes and 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：本发明提供了一系列噻吩并[2,3-b]吡啶衍生物，其中Y代表式C（O）或S（O）2的键; R 1表示氢，卤素，氰基，硝基，C 1-6烷基，三氟甲基，C 1-6烷氧基，三氟甲氧基，C 1-6烷硫基，C 1-6烷基亚磺酰基或C 1-6烷基磺酰基; R 2表示卤素，硝基，氰基，C 1-6烷基，C 2-6炔基，羟基（C 1-6）烷基或甲酰基; 并且R 3表示式（a），（b），（c），（d）或（e）的基团：其中星号（*）表示与分子剩余部分的连接点。式（I）化合物是人MEK（MAPICIC）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）中。

3. 发明申请

WO0144194A3 PROPANOIC ACID DERIVATIVES AS INTEGRIN INHIBITORS 审中-公开
标题翻译：作为整合抑制剂的丙酸衍生物
公开(公告)号：WO0144194A3
公开(公告)日：2001-12-13
申请号：PCT/GB0004831
申请日：2000-12-15
申请人： CELLTECH R&D LTD , ALEXANDER RIKKI PETER , LANGHAM BARRY JOHN , REUBERSON JAMES THOMAS , TROWN EMMA LOUISE , WARRELLOW GRAHAM JOHN
发明人： ALEXANDER RIKKI PETER , LANGHAM BARRY JOHN , REUBERSON JAMES THOMAS , TROWN EMMA LOUISE , WARRELLOW GRAHAM JOHN
IPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , A61K31/44 , A61K31/4439 , A61K31/444 , A61P29/00 , A61P35/00
CPC分类号： C07D213/74 , C07D213/89 , C07D401/12
摘要： Propanoic acid derivatives of formula (1) are described: Ar-X -Ar -Z-R; in which Ar is a nitrogen base containing group; X is a linker atom or group; Ar is an optionally substituted pyridine or pyridine-N-oxide; Z is a group -CH(R )CH2- [in which R is R or Alk R , R is a hydrogen atom or an optionally substituted aliphatic, cycloaliphatic heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group and Alk is an optionally substituted C1-3alkylene chain], -C(R )(R )-CH(R )- [in which R and R together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or -C(R )=CH-; R is a carboxylic acid (-CO2H) or a derivative or biostere thereof; 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.
摘要翻译：式（1）的丙酸衍生物描述为：Ar-X 1 -Ar 1 -Z-R; 其中Ar是含氮碱基团; X 1是接头原子或基团; Ar 1是任选取代的吡啶或吡啶-N-氧化物; Z为基团-CH（R 13）CH 2 - [其中R 13为R 13a或Alk 1a R 13a，R 13a为氢原子或任选取代的脂族基团，脂环族杂脂族基，杂环脂族基，芳族或杂芳族基团且Alk 1a为任选取代的C 1-3亚烷基链]，-C（R 12a）（R 13）-CH（R 12b） - [ R 12a和R 12b与它们所连接的碳原子一起形成C 3-7环烷基]或-C（R 13）= CH-; R是羧酸（-CO 2 H）或其衍生物或生物等排物; 及其盐，溶剂化物，水合物和N-氧化物。该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。

4. 发明申请

WO2010133836A1 FUSED BICYCLIC PYRAZOLE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的熔融双相吡唑衍生物
公开(公告)号：WO2010133836A1
公开(公告)日：2010-11-25
申请号：PCT/GB2010/001000
申请日：2010-05-19
申请人： UCB PHARMA S.A. , ALLEN, Daniel, Rees , BROWN, Julien, Alistair , BÜRLI, Roland , HAUGHAN, Alan, Findlay , LANGHAM, Barry, John , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SHARPE, Andrew
发明人： ALLEN, Daniel, Rees , BROWN, Julien, Alistair , BÜRLI, Roland , HAUGHAN, Alan, Findlay , LANGHAM, Barry, John , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SHARPE, Andrew
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P25/28 , A61P37/00
CPC分类号： C07D487/04
摘要： A series of substituted pyrazolo[l,5-α][l,3,5]triazine and pyrazolo[l,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-a] [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）。

5. 发明申请

WO2007088345A1 THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS 审中-公开
标题翻译：作为MEK抑制剂的三苯基吡啶衍生物
公开(公告)号：WO2007088345A1
公开(公告)日：2007-08-09
申请号：PCT/GB2007/000310
申请日：2007-01-30
申请人： UCB PHARMA S.A. , HUTCHINGS, Martin, Clive , ARCHIBALD, Sarah, Catherine , BROOKINGS, Daniel, Christopher , DAVIS, Jeremy, Martin , JOHNSON, James, Andrew , LANGHAM, Barry, John , NEUSS, Judi, Charlotte
发明人： HUTCHINGS, Martin, Clive , ARCHIBALD, Sarah, Catherine , BROOKINGS, Daniel, Christopher , DAVIS, Jeremy, Martin , JOHNSON, James, Andrew , LANGHAM, Barry, John , NEUSS, Judi, Charlotte
IPC分类号： C07D495/04 , A61K31/4365
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取代在2-位的噻吩并[2,3-b]吡啶衍生物是人类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。

6. 发明申请

WO2004113348A1 THIENOPYRIDONE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：噻吗啉衍生物作为激酶抑制剂
公开(公告)号：WO2004113348A1
公开(公告)日：2004-12-29
申请号：PCT/GB2004/002644
申请日：2004-06-18
申请人： CELLTECH R & D LIMITED , BROOKINGS, Daniel Christopher , DAVIS, Jeremy Martin , LANGHAM, Barry John
发明人： BROOKINGS, Daniel Christopher , DAVIS, Jeremy Martin , LANGHAM, Barry John
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： A series of thieno[2,3- b ]pyridin-6(7 H )-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-3-yl, pyrrolidin-3-ylamino or related 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：通过羰基或磺酰基连接的吡咯烷-3-基，吡咯烷-3-基氨基或相关部分在2-位上取代的一系列噻吩并[2,3-b]吡啶-6（7H） - 酮衍生物，作为p38MAP激酶的抑制剂，因此在医学中有用，例如用于治疗和/或预防免疫或炎症性疾病。

7. 发明申请

WO2004000846A1 ARYLAMINE SUBSTUTUTED BICYCLIC HETEROAROMATIC COMPOUNDS AS P38 KINASE INHIBITORS 审中-公开
标题翻译：作为P38激酶抑制剂的亚胺基亚基双环异构化合物
公开(公告)号：WO2004000846A1
公开(公告)日：2003-12-31
申请号：PCT/GB2003/002667
申请日：2003-06-20
申请人： CELLTECH R & D LIMITED , BROOKINGS, Daniel, Christopher , DAVIS, Jeremy, Martin , LANGHAM, Barry, John
发明人： BROOKINGS, Daniel, Christopher , DAVIS, Jeremy, Martin , LANGHAM, Barry, John
IPC分类号： C07D495/04
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(R a ) is present and represents a bond and A is a -N= atom or a -C(R b )= group, or the dashed line is absent and A is a -N(R b )-, or -C(R b )(R c )- group; X is an -O-, -S- or substituted nitrogen atom or a -S(O)-, -S(O 2 )- or -NH-group; Y is a nitrogen or substituted carbon atom or a -CH= group; n is zero or the integer 1; Alk 1 is an optionally substituted aliphatic or heteroaliphatic chain L 1 is a covalent bond or a linker atom or group; Cy 1 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是-N =原子或-C（R （b））=组，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。

8. 发明申请

WO2003033502A1 BICYCLIC OXOPYRIDINE AND OXOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：双羟基吡啶和氧代吡嗪衍生物
公开(公告)号：WO2003033502A1
公开(公告)日：2003-04-24
申请号：PCT/GB2002/004680
申请日：2002-10-16
申请人： CELLTECH R & D LIMITED , DAVIS, Jeremy, Martin , BROOKINGS, Daniel, Christopher , LANGHAM, Barry, John
发明人： DAVIS, Jeremy, Martin , BROOKINGS, Daniel, Christopher , LANGHAM, Barry, John
IPC分类号： C07D495/04
CPC分类号： C07D471/04 , C07D495/04
摘要： Compounds of formulae (1 a) and (1 b) are described: in which the dashed line represents an optional bond; A is a -N= atom or a -N(R b )-, -C(R b )= or -C(R b )(R C )- group; R a , R b and R c is each independently a hydrogen atom or an optionally substituted C 1-6 alkyl group; X is an -O- or -S- atom or -NH- group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk 1 is an optionally substituted aliphatic or heteroaliphatic chain L 1 is a covalent bond or a linker atom or group; Cy 1 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 salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase mediated diseases or disorders, such as rheumatoid arthritis.
摘要翻译：描述式（1a）和（1b）的化合物：其中虚线表示任选的键; A是-N =原子或-N（R b） - ， - C（R b）=或-C（R b）（R c） - 基团; R a，R b和R c各自独立地为氢原子或任选取代的C 1-6烷基; X是-O-或-S-原子或-NH-基团或取代的N原子; 每个Y独立地是N原子或CH基团或取代的C原子; 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; 及其盐，溶剂合物，水合物及其N-氧化物; 这些化合物是p38激酶的有效抑制剂，并且用于预防或治疗p38激酶介导的疾病或病症，例如类风湿性关节炎。

9. 发明申请

WO0179173A2 ENAMINE DERIVATIVES 审中-公开
标题翻译： ENAMINE衍生物
公开(公告)号：WO0179173A2
公开(公告)日：2001-10-25
申请号：PCT/GB0101682
申请日：2001-04-12
申请人： CELLTECH R&D LTD , NORMAN TIMOTHY JOHN , PORTER JOHN ROBERT , HUTCHINSON BRIAN WOODSIDE , RATCLIFFE ANDREW JAMES , HEAD JOHN CLIFFORD , ALEXANDER RIKKI PETER , LANGHAM BARRY JOHN , WARRELLOW GRAHAM JOHN , ARCHIBALD SARAH CATHERINE , LINSLEY JANEEN MARSHA
发明人： NORMAN TIMOTHY JOHN , PORTER JOHN ROBERT , HUTCHINSON BRIAN WOODSIDE , RATCLIFFE ANDREW JAMES , HEAD JOHN CLIFFORD , ALEXANDER RIKKI PETER , LANGHAM BARRY JOHN , WARRELLOW GRAHAM JOHN , ARCHIBALD SARAH CATHERINE , LINSLEY JANEEN MARSHA
IPC分类号： A61K31/198 , A61K31/223 , A61K31/4375 , A61K31/4409 , A61K31/4436 , A61K31/4545 , A61K31/472 , A61P1/04 , A61P3/10 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/28 , A61P29/00 , A61P37/06 , A61P43/00 , C07C229/36 , C07D213/81 , C07D217/22 , C07D409/12 , C07D471/04 , A61K31/44 , C07C225/20
CPC分类号： C07D213/81 , C07C229/36 , C07C2601/10 , C07D217/22 , C07D471/04
摘要： Enamine derivatives of formula (1) are described. In said formula , R a group Ar L Ar Alk- in which Ar is an aromatic or heteroaromatic group, L is a covalent bond or a linker atom or group, Ar is an arylene or heteroarylene group and Alk is a chain -CH2-CH(R)-, -CH=C(R)- or (a) in which R is a carboxylic acid or a derivative or biostere thereof; R 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(R ) group; R is a oxo, thioxo, or imino group; R and R are 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：描述式（1）的烯胺衍生物。在所述式中，R 1，Ar 1，Ar 2，Ar 2 Al，其中Ar 1是芳族或杂芳族基团，L 2是共价键或连接原子或基团，Ar 2是亚芳基或亚杂芳基，Alk是链-CH 2 -CH（R） - ， - CH = C（R） - 或（a）其中R是羧酸或衍生物或生物固体物; R 2是氢原子或C 1-6烷基; Cy是其中X是N原子或C（R））基团的脂环族或杂脂环族环; R x是氧代，硫代或亚氨基; R w和R z各自为氢原子或任选的取代基; 只要Cy不是环丁烯二酮基团; 及其盐，溶剂合物，水合物和N-氧化物。这些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。

10. 发明申请

WO2010146351A1 INDOLYLMETHYL-MORPHOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的吲哚基甲基吗啉衍生物
公开(公告)号：WO2010146351A1
公开(公告)日：2010-12-23
申请号：PCT/GB2010/001171
申请日：2010-06-15
申请人： UCB PHARMA S.A. , ALI, Mezher, Hussein , BROWN, Julien, Alistair , DE CANDOLE, Benjamin, Charles , HUTCHINSON, Brian, Woodside , LANGHAM, Barry, John , NEUSS, Judi, Charlotte , QUINCEY, Joanna, Rachel , TREVITT, Graham, Peter
发明人： ALI, Mezher, Hussein , BROWN, Julien, Alistair , DE CANDOLE, Benjamin, Charles , HUTCHINSON, Brian, Woodside , LANGHAM, Barry, John , NEUSS, Judi, Charlotte , QUINCEY, Joanna, Rachel , TREVITT, Graham, Peter
IPC分类号： C07D413/06 , C07D413/14 , A61K31/5355 , A61P35/00 , A61P29/00 , A61P9/00 , A61P25/00
CPC分类号： C07D413/06 , C07D413/14
摘要： A series of morpholine derivatives, substituted in the 4-position by a substituted carbonyl or sulfonyl moiety, and in the 3-position by an optionally substituted indol-3-ylmethyl group, 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：一系列通过取代的羰基或磺酰基部分在4-位取代的吗啉衍生物，以及3-任选取代的吲哚-3-基甲基，作为PI3激酶的选择性抑制剂，因此有益于药物，例如治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

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