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1. 发明申请

WO2008031556A2 NOVEL 2 AMINO-PYRIMIDINE DERIVATIVES, PROCESSES FOR PREPARING THEM, PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译：新型二氨基吡啶衍生物，其制备方法及其药物组合物
公开(公告)号：WO2008031556A2
公开(公告)日：2008-03-20
申请号：PCT/EP2007/007898
申请日：2007-09-11
申请人： UCB PHARMA, S.A. , RAPHY, Gilles , WATSON, Robert, John , HANNAH, Duncan , PEGURIER, Cécile , ORTMANS, Isabelle , LOCK, Christopher, James , KNIGHT, Roland, Laurence , OWEN, David, Alan
发明人： RAPHY, Gilles , WATSON, Robert, John , HANNAH, Duncan , PEGURIER, Cécile , ORTMANS, Isabelle , LOCK, Christopher, James , KNIGHT, Roland, Laurence , OWEN, David, Alan
IPC分类号： C07D239/48 , C07D471/04 , C07D401/04 , C07D401/12 , C07D401/14 , A61P19/00 , A61K31/506
CPC分类号： C07D403/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D451/02 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/10
摘要： The present invention concerns novel 2 amino pyrimidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及新型2氨基嘧啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

2. 发明申请

WO1997037973A1 PEPTIDYL COMPOUNDS HAVING MMP AND TNF INHIBITORY ACTIVITY 审中-公开
标题翻译：具有MMP和TNF抑制活性的肽类化合物
公开(公告)号：WO1997037973A1
公开(公告)日：1997-10-16
申请号：PCT/GB1997000957
申请日：1997-04-04
申请人： CHIROSCIENCE LIMITED , BAXTER, Andrew, Douglas , OWEN, David, Alan , MONTANA, John, Gary , WATSON, Robert, John , KEILY, John, Fraser
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07C323/60 , C07C327/32
摘要： Compounds of formula (I) having MMP and TNF inhibitory activity.
摘要翻译：具有MMP和TNF抑制活性的式（I）化合物。

3. 发明申请

WO2004094381A1 CYCLIC QUATERNARY AMINO DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS 审中-公开
标题翻译：作为化合物受体的调节剂的循环季铵氨基转移酶
公开(公告)号：WO2004094381A1
公开(公告)日：2004-11-04
申请号：PCT/GB2004/001559
申请日：2004-04-08
申请人： CELLTECH R & D LIMITED , WATSON, Robert, John , MEISSNER, Johannes, Wilhelm, Georg , OWEN, David, Alan
发明人： WATSON, Robert, John , MEISSNER, Johannes, Wilhelm, Georg , OWEN, David, Alan
IPC分类号： C07D211/58
CPC分类号： C07D409/12 , C07D211/58
摘要： Compounds of formula (1) wherein,m,n,R 1 ,R 2 ,R a ,ALK 3 , E and Y are as defined in the claims, being potent and selective inhibitors of chemokine binding to the CXCR3 receptor, are accordingly of use in the treatment and/or prevention of conditions involving inappropriate T-cell trafficking, including inflammatory, autoimmune and immurforegulatory disorders such as rheumatoid arthritis.
摘要翻译：式（1）的化合物，其中m，n，R 1，R 2，R a，ALK 3，E和Y如权利要求中所定义，是趋化因子结合的有效和选择性抑制剂 CXCR3受体相应地用于治疗和/或预防涉及不适当的T细胞运输的病症，包括炎性，自身免疫和非前路外疾病如类风湿性关节炎。

4. 发明申请

WO2003087071A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO2003087071A1
公开(公告)日：2003-10-23
申请号：PCT/GB2003/001418
申请日：2003-04-01
申请人： CELLTECH R & D LIMITED , HAUGHAN, Alan, Findlay , DYKE, Hazel, Joan , WILLIAMS, Sophie, Caroline , LOWE, Christopher , DRAFFAN, Alistair, George , OWEN, David, Alan
发明人： HAUGHAN, Alan, Findlay , DYKE, Hazel, Joan , WILLIAMS, Sophie, Caroline , LOWE, Christopher , DRAFFAN, Alistair, George , OWEN, David, Alan
IPC分类号： C07D275/04
CPC分类号： C07D275/04 , C07D417/12 , C07D417/14 , C07D491/10
摘要： Sulfonamide derivatives of formula (1) are described wherein X is an O or S atom; Y is an 0 or S atom; A is a group -S0 2 NR 1 R 2 ; m is zero or the integer 1; n is zero or the integer 1; provided that at least one but not both of m and n are the integer 1; R 3 is a hydrogen atom or an alkyl or cycloalkyl group; and the salts, solvates, hydrates, tautomers, isomers, 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）的磺酰胺衍生物，其中X是O或S原子; Y是0或S原子; A是-SO 2 NR 1 R 2基团; m为零或整数1; n为零或整数1; 条件是m和n中的至少一个不是二者都是整数1; R 3是氢原子或烷基或环烷基; 及其盐，溶剂合物，水合物，互变异构体，异构体，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。

5. 发明申请

WO2009047255A1 HETEROBICYCLIC COMPOUNDS AS HISTAMINE H4-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：异源化合物作为组胺H4受体拮抗剂
公开(公告)号：WO2009047255A1
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063413
申请日：2008-10-07
申请人： UCB PHARMA, S.A. , RAPHY, GILLES , PEGURIER, CECILE , MEISSNER, HANS , KNIGHT, ROLAND , OWEN, DAVID ALAN
发明人： RAPHY, GILLES , PEGURIER, CECILE , MEISSNER, HANS , KNIGHT, ROLAND , OWEN, DAVID ALAN
IPC分类号： C07D403/04 , C07D471/04 , C07D487/08 , A61K31/495 , A61P29/00 , C07D213/64 , C07D239/70 , C07D239/95 , C07C69/757
CPC分类号： C07D403/04 , C07C69/757 , C07D213/64 , C07D239/70 , C07D239/95 , C07D471/04 , C07D487/04
摘要： The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及式（I）的杂双环化合物，其制备方法，含有它们的药物组合物及其作为药物的用途。

6. 发明申请

WO2008031556A3 2 AMINO-PYRIMIDINE DERIVATIVES AS H4 RECEPTOR ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： 2氨基吡啶衍生物作为H4受体拮抗剂，其制备方法及其在药物组合物中的应用
公开(公告)号：WO2008031556A3
公开(公告)日：2008-06-12
申请号：PCT/EP2007007898
申请日：2007-09-11
申请人： UCB PHARMA SA , RAPHY GILLES , WATSON ROBERT JOHN , HANNAH DUNCAN , PEGURIER CECILE , ORTMANS ISABELLE , LOCK CHRISTOPHER JAMES , KNIGHT ROLAND LAURENCE , OWEN DAVID ALAN
发明人： RAPHY GILLES , WATSON ROBERT JOHN , HANNAH DUNCAN , PEGURIER CECILE , ORTMANS ISABELLE , LOCK CHRISTOPHER JAMES , KNIGHT ROLAND LAURENCE , OWEN DAVID ALAN
IPC分类号： C07D239/48 , A61K31/506 , A61P19/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04
CPC分类号： C07D403/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D451/02 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/10
摘要： The present invention concerns novel 2 amino pyrimidine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as harmaceuticals.
摘要翻译：本发明涉及式（I）的新型2氨基嘧啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

7. 发明申请

WO2005003127A1 BICYCLIC HETEROAROMATIC DERIVATIVES AS MODULATORS OF CXCR3 FUNCTION 审中-公开
标题翻译：作为CXCR3功能的调节剂的双相异构体衍生物
公开(公告)号：WO2005003127A1
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002735
申请日：2004-06-25
申请人： CELLTECH R & D LIMITED , OWEN, David, Alan , WATSON, Robert, John , MEISSNER, Johannes, Wilhelm, Georg , ALLEN, Daniel, Rees
发明人： OWEN, David, Alan , WATSON, Robert, John , MEISSNER, Johannes, Wilhelm, Georg , ALLEN, Daniel, Rees
IPC分类号： C07D413/12
CPC分类号： C07D401/12 , C07D413/12 , C07D417/12
摘要： A class of 1-substituted 4-(benzothiazol-2-ylamino) piperidine derivatives and related heterocyclic compounds, being potent and selective modulators of the interaction between CXCR3 and its chemokine ligands, are accordingly of use in the treatment and/or prevention of conditions involving inappropriate T-cell trafficking, including inflammatory, autoimmune and immunoregulatory disorders.
摘要翻译：一类1-取代的4-（苯并噻唑-2-基氨基）哌啶衍生物和相关的杂环化合物是CXCR3与其趋化因子配体之间相互作用的有效和选择性调节剂，因此可用于治疗和/或预防病症涉及不适当的T细胞运输，包括炎症，自身免疫和免疫调节性疾病。

8. 发明申请

WO1997037974A1 PEPTIDYL COMPOUNDS HAVING MMP AND TNF INHIBITORY ACTIVITY 审中-公开
标题翻译：具有MMP和TNF抑制活性的肽化合物
公开(公告)号：WO1997037974A1
公开(公告)日：1997-10-16
申请号：PCT/GB1997000959
申请日：1997-04-04
申请人： CHIROSCIENCE LIMITED , BAXTER, Andrew, Douglas , OWEN, David, Alan , MONTANA, John, Gary , WATSON, Robert, John , KEILY, John, Fraser
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07D209/48
CPC分类号： C07C323/60 , C07C327/32
摘要： Compounds of formula (I) having MMP and TNF inhibitory activity.
摘要翻译：式（I）化合物，具有基质金属蛋白酶抑制剂（MMP）和肿瘤坏死因子（TNF）活性。

9. 发明申请

WO1996035711A1 PEPTIDE COMPOUNDS WHICH INHIBIT METALLOPROTEINASE AND TNF LIBERATION, AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：抑制金属蛋白酶和TNF释放的肽化合物及其治疗用途
公开(公告)号：WO1996035711A1
公开(公告)日：1996-11-14
申请号：PCT/GB1996001136
申请日：1996-05-10
申请人： CHIROSCIENCE LIMITED , BAXTER, Andrew, Douglas , MONTANA, John , OWEN, David, Alan
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07K05/023
CPC分类号： C07K5/06052 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06043 , C07K5/0806 , Y10S530/868
摘要： Peptidyl compounds have therapeutic utility via MMP/TNF inhibition.
摘要翻译：肽基化合物通过MMP / TNF抑制具有治疗效用。

10. 发明申请

WO1995013289A1 PEPTIDYL COMPOUNDS AND THEIR THERAPEUTIC USE AS INHIBITORS OF METALLOPROTEINASES 审中-公开
标题翻译：肽类化合物及其治疗用途作为金属蛋白酶抑制剂
公开(公告)号：WO1995013289A1
公开(公告)日：1995-05-18
申请号：PCT/GB1994002471
申请日：1994-11-10
申请人： CHIROSCIENCE LIMITED , MONTANA, John , DICKENS, Jonathon , OWEN, David, Alan , BAXTER, Andrew, Douglas
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07K05/062
CPC分类号： C07K5/0606 , A61K38/00 , C07K5/06043 , Y02A50/411 , Y10S530/868
摘要： A compound of formula (I), wherein R is C1-6 alkyl, C2-6 alkenyl, aryl, (C1-6 alkyl)aryl or C1-6 alkyl-AR where A is O, NR or S(O)m, where m = 0-2, and the or each R is H, C1-4 alkyl, aryl or (C1-4 alkyl)aryl; R is H or C1-6 alkyl; either R is H or C1-6 alkyl optionally substituted by amino (NH2), arylamino, protected amino, aryl, di(C1-6 alkyl)amino, mono(C1-6 alkyl)amino, CO2H, protected carboxyl, carbamoyl, mono(C1-6 alkyl)carbamoyl or di(C1-6 alkyl)carbamoyl, and R is H or C1-6 alkyl, or NR4R5 is pyrrolidino, piperidino or morpholino; R is optionally-substituted C3-6 cycloalkyl, C3-6 cycloalkenyl, C1-6 alkyl, benzyl, (C1-6 alkoxy)benzyl, benzyloxybenzyl or 3-indolylmethyl; Alk is C1-6 alkyl or C2-6 alkenyl and n = 0 or 1; R is H or R CO where R is C1-4 alkyl, (C1-4 alkyl)aryl, C3-6 cycloalkyl, (C3-6 cycloalkyl)C1-4 alkyl, C2-6 alkenyl or (C2-6 alkenyl)aryl; and R is H, C1-4 alkyl, (C1-4 alkyl)aryl or aryl; or a salt, solvate or hydrate thereof. Such compounds may be used to treat conditions associated with metalloproteinase, TNF and/or other activity.
摘要翻译：式（I）化合物，其中R 1为C 1-6烷基，C 2-6烯基，芳基，（C 1-6烷基）芳基或C 1-6烷基-Ar 9，其中A为O， 9或S（O）m，其中m = 0-2，并且每个R 9是H，C 1-4烷基，芳基或（C 1-4烷基）芳基; R 2是H或C 1-6烷基; R 4是H或任选被氨基（NH 2），芳基氨基，保护的氨基，芳基，二（C 1-6烷基）氨基，单（C 1-6烷基）氨基，CO 2 H，被保护的羧基取代的C 1-6烷基，氨基甲酰基，单（C 1-6烷基）氨基甲酰基或二（C 1-6烷基）氨基甲酰基，R 5为H或C 1-6烷基，或NR 4 R 5为吡咯烷子基，哌啶子基或吗啉代; R 6是任选取代的C 3-6环烷基，C 3-6环烯基，C 1-6烷基，苄基，（C 1-6烷氧基）苄基，苄氧基苄基或3-吲哚甲基; Alk是C 1-6烷基或C 2-6烯基，n = 0或1; R 7是H或R 10 CO，其中R 10是C 1-4烷基，（C 1-4烷基）芳基，C 3-6环烷基，（C 3-6环烷基）C 1-4烷基，C 2-6 烯基或（C 2-6烯基）芳基; 和R 8是H，C 1-4烷基，（C 1-4烷基）芳基或芳基; 或其盐，溶剂合物或水合物。这些化合物可用于治疗与金属蛋白酶，TNF和/或其他活性相关的病症。

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