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1. 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。

2. 发明申请

WO2004007494A1 PHENYLALANINE ENAMIDE DERIVATIVES 审中-公开
标题翻译：苯乙烯胺衍生物
公开(公告)号：WO2004007494A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/003104
申请日：2003-07-16
申请人： CELLTECH R & D LIMITED , BROWN, Julien, Alistair , BAILEY, Stuart , BRAND, Stephen
发明人： BROWN, Julien, Alistair , BAILEY, Stuart , BRAND, Stephen
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Phenylalanine enamide derivatives of formula (1) are described, wherein R 1 is a -CH(CH 3 ) 2 , -(CH 2 ) 2 CH 3 ; -CH 2 C(CH 3 ) 3 , -CH 2 CH 2 OH, -CH 2 CH 2 OCH 3 , -CH 2 CH 2 OCH 2 CH 2 OH, -CH 2 CH 2 OCH 2 CH 2 OCH 3 , formula (A) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of α4 integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.
摘要翻译：描述了式（1）的苯丙氨酸烯酰胺衍生物，其中R 1是-CH（CH 3）2， - （CH 2）2 CH 3; -CH 2 C（CH 3）3，-CH 2 CH 2 OH，-CH 2 CH 2 OCH 3，-CH 2 CH 2 OCH 2 CH 2 OH，-CH 2 CH 2 OCH 2 CH 2 OCH 3，式（A）及其盐，溶剂化物和N-氧化物。根据本发明的化合物是α4整联蛋白的有效和选择性抑制剂。这些化合物可用于调节细胞粘附，特别是用于预防和治疗疾病或病症，包括其中白细胞外渗起作用的炎症，本发明延伸到这种用途和使用该化合物用于制备用于治疗这些疾病或病症的药物。

3. 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）。

4. 发明申请

WO2010092340A1 FUSED PYRIDINE AND PYRAZINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：熔融吡啶和吡嗪衍生物作为激酶抑制剂
公开(公告)号：WO2010092340A1
公开(公告)日：2010-08-19
申请号：PCT/GB2010/000243
申请日：2010-02-11
申请人： UCB PHARMA S.A. , ALLEN, Daniel, Rees , BROWN, Julien, Alistair , BÜRLI, Roland , HAUGHAN, Alan, Findlay , MACDONALD, Jonathan, David , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SAVILLE-STONES, Elizabeth, Anne , SHARPE, Andrew
发明人： ALLEN, Daniel, Rees , BROWN, Julien, Alistair , BÜRLI, Roland , HAUGHAN, Alan, Findlay , MACDONALD, Jonathan, David , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SAVILLE-STONES, Elizabeth, Anne , SHARPE, Andrew
IPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/4709 , A61K31/52 , A61P29/00 , A61P37/00
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline 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：一系列氨基取代的稠合吡啶和吡嗪衍生物，特别是氨基取代的喹啉和喹喔啉衍生物，作为PI3激酶的选择性抑制剂，因此在医学上有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害感受或眼科疾病。

5. 发明申请

WO2004006918A1 PHENYLALANINE ENAMIDE DERIVATIVES CONTAINING A SPIRO`3.5!NON-1-ENE RING FOR USE AS INTEGRIN INHIBITORS 审中-公开
标题翻译：含有SPIRO®3.5！NON-1-ENE环的苯乙烯胺衍生物用作INTEGRIN抑制剂
公开(公告)号：WO2004006918A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/003100
申请日：2003-07-16
申请人： CELLTECH R & D LIMITED , BROWN, Julien, Alistair , BAILEY, Stuart , BRAND, Stephen
发明人： BROWN, Julien, Alistair , BAILEY, Stuart , BRAND, Stephen
IPC分类号： A61K31/44
CPC分类号： C07D213/81
摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 is a -CH 3 , -(CH 2 ) 3 CH 3 , -CH 2 CH 2 0H, -CH 2 CH 2 0CH 3 , -CH 2 CH 2 0CH 2 CH 2 0H, -CH 2 CH 2 0CH 2 CH 2 0CH 3 , Formula (II) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of oA integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.
摘要翻译：描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R 1是-CH 3， - （CH 2）3 CH 3，-CH 2 CH 2 OH，-CH 2 CH 2 OCH 3，-CH 2 CH 2 OCH 2 CH 2 OH，-CH 2 CH 2 CH 2 CH 2 CH 3，式（II）及其盐，溶剂化物和N-氧化物。根据本发明的化合物是oA整联蛋白的有效和选择性抑制剂。这些化合物可用于调节细胞粘附，特别是用于预防和治疗疾病或病症，包括其中白细胞外渗起作用的炎症，本发明延伸到这种用途和使用该化合物用于制备用于治疗这些疾病或病症的药物。

6. 发明申请

WO2012032334A1 QUINOLINE AND QUINOXALINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹啉和喹啉衍生物作为激酶抑制剂
公开(公告)号：WO2012032334A1
公开(公告)日：2012-03-15
申请号：PCT/GB2011/051647
申请日：2011-09-02
申请人： UCB PHARMA S.A. , PARTON, Andrew Harry , ALI, Mezher Hussein , BROOKINGS, Daniel Christopher , BROWN, Julien Alistair , FORD, Daniel James , FRANKLIN, Richard Jeremy , LANGHAM, Barry John , NEUSS, Judi Charlotte , QUINCEY, Joanna Rachel
发明人： PARTON, Andrew Harry , ALI, Mezher Hussein , BROOKINGS, Daniel Christopher , BROWN, Julien Alistair , FORD, Daniel James , FRANKLIN, Richard Jeremy , LANGHAM, Barry John , NEUSS, Judi Charlotte , QUINCEY, Joanna Rachel
IPC分类号： C07D471/04 , A61K31/519 , A61P9/00 , A61P25/28 , A61P29/00
CPC分类号： C07D471/04 , A61K31/519
摘要： A series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of P13 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：包含氟化乙基侧链的一系列喹啉和喹喔啉衍生物是P13激酶的选择性抑制剂，因此在医学中是有益的，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，伤害感受性或伤害性感受器眼科病情。

7. 发明申请

WO2010001126A1 THIOPHENE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：噻诺衍生物作为激酶抑制剂
公开(公告)号：WO2010001126A1
公开(公告)日：2010-01-07
申请号：PCT/GB2009/001659
申请日：2009-07-02
申请人： UCB PHARMA S.A. , ALEXANDER, Rikki, Peter , BAILEY, Stuart , BROOKINGS, Daniel, Christopher , BROWN, Julien, Alistair , CALLAGHAN, Sacha , POLLARD, Faye, Charlotte
发明人： ALEXANDER, Rikki, Peter , BAILEY, Stuart , BROOKINGS, Daniel, Christopher , BROWN, Julien, Alistair , CALLAGHAN, Sacha , POLLARD, Faye, Charlotte
IPC分类号： C07D333/36 , C07D409/04 , C07D413/04 , A61K31/381 , A61P29/00
CPC分类号： C07D333/36 , C07D409/04 , C07D413/04
摘要： A series of thiophene derivatives which are substituted in the 2 -position by a morphoIin-4-yl substituent, and in the 3 -position by a substituted ethynyl 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：一系列噻吩衍生物在2-位被吗啉-4-基取代基取代，而在3位被取代的乙炔基部分取代，作为PI3激酶的选择性抑制剂，因此在医学上是有益的例如治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

8. 发明申请

WO2009071890A1 TRICYCLIC KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC激酶抑制剂
公开(公告)号：WO2009071890A1
公开(公告)日：2009-06-11
申请号：PCT/GB2008/004002
申请日：2008-12-03
申请人： UCB PHARMA S.A. , ALEXANDER, Rikki Peter , AUJLA, Pavandeep Singh , BROWN, Julien Alistair , DE CANDOLE, Benjamin Charles , TREVITT, Graham Peter
发明人： ALEXANDER, Rikki Peter , AUJLA, Pavandeep Singh , BROWN, Julien Alistair , DE CANDOLE, Benjamin Charles , TREVITT, Graham Peter
IPC分类号： C07D513/04 , A61K31/425 , A61P29/00
CPC分类号： C07D513/04
摘要： A series of fused tricyclic thiazole and thiophene derivatives which are substituted in the 2-position of the thiazole or thiophene ring 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：在噻唑或噻吩环的2-位被任选取代的吗啉-4-基部分取代的一系列稠合的三环噻唑和噻吩衍生物是PI3激酶的选择性抑制剂，因此在医学上是有益的例如治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

9. 发明申请

WO2009071888A1 PYRROLOTHIAZOLES AS PI3-KINASE INHIBITORS 审中-公开
标题翻译： PYRROLOTHIAZOLES作为PI3-激酶抑制剂
公开(公告)号：WO2009071888A1
公开(公告)日：2009-06-11
申请号：PCT/GB2008/004000
申请日：2008-12-03
申请人： UCB PHARMA S.A. , BROWN, Julien Alistair , DE CANDOLE, Benjamin Charles , MORGAN, Trevor
发明人： BROWN, Julien Alistair , DE CANDOLE, Benjamin Charles , MORGAN, Trevor
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A series of 4,5-dihydro-6H-pyrrolo[3,4-d][1,3]thiazol-6-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4,5-二氢-6H-吡咯并[3,4-d] [1,3]噻唑-6-酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，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。

10. 发明申请

WO2008047109A1 THIAZOLE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：噻唑衍生物作为激酶抑制剂
公开(公告)号：WO2008047109A1
公开(公告)日：2008-04-24
申请号：PCT/GB2007/003949
申请日：2007-10-16
申请人： UCB PHARMA S.A. , ALEXANDER, Rikki Peter , BROWN, Julien Alistair , CRÉPY, Karen Viviane Lucile , MACK, Stephen Robert
发明人： ALEXANDER, Rikki Peter , BROWN, Julien Alistair , CRÉPY, Karen Viviane Lucile , MACK, Stephen Robert
IPC分类号： C07D417/04 , A61K31/427 , A61P29/00
CPC分类号： C07D417/04
摘要： A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 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：在2-位被取代的吗啉-4-基部分取代的一系列噻唑衍生物是P13激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

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