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1. 发明公开

EP1315725A1 BICYCLIC ENAMIDE DERIVATIVES BEING INTEGRIN INHIBITORS 审中-公开
标题翻译：双环烯酰胺衍生物作为抑制剂研究整合
公开(公告)号：EP1315725A1
公开(公告)日：2003-06-04
申请号：EP01963216.5
申请日：2001-09-03
申请人： Celltech R & D Limited , Porter, John Robert , Head, John Clifford , Ratcliffe, Andrew James
发明人： PORTER, John, Robert,c/o Celltech R & D Limited , HEAD, John, Clifford,c/o Celltech R & D Limited , RATCLIFFE, Andrew, J.,c/o Celltech R & D Limited , NORMAN, Timothy, John,c/o Celltech R & D Limited
IPC分类号： C07D471/00 , A61K31/4375 , A61P29/00
CPC分类号： C07D471/04 , A61K31/4375
摘要： Enamide derivatives of formula (1) are described: (1) wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain -CH¿2?-CH(R)-, -CH=C(R)- or formula (II) in which r is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R?2¿ is a hydrogen atom or a C¿1-6?alkyl group; X is an O or S atom or the group NR?30¿ group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2. Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvantes, 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 including the inappropriate growth or migration of cells.

2. 发明专利

AU8424701A Bicyclic enamide derivatives being integrin inhibitors 未知
公开(公告)号：AU8424701A
公开(公告)日：2002-03-22
申请号：AU8424701
申请日：2001-09-03
申请人： CELLTECH R AND D LTD , PORTER JOHN ROBERT , HEAD JOHN CLIFFORD , RATCLIFFE ANDREW JAMES
发明人： PORTER JOHN ROBERT , HEAD JOHN CLIFFORD , RATCLIFFE ANDREW JAMES , NORMAN TIMOTHY JOHN
IPC分类号： A61K31/4375 , A61P29/00 , C07D471/04 , C07D471/00

3. 发明申请

WO2008138592A1 BICYCLIC AND HETEROBICYCLIC DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USES 审中-公开
标题翻译：双环和杂环衍生物，其制备方法及其用途
公开(公告)号：WO2008138592A1
公开(公告)日：2008-11-20
申请号：PCT/EP2008/003839
申请日：2008-05-13
申请人： UCB PHARMA, S.A. , DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , JONE, Mark, William
发明人： DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , JONE, Mark, William
IPC分类号： C07D215/52 , A61K31/4709 , A61P29/00
CPC分类号： C07D215/52
摘要： The present invention concerns bicyclic and heterobicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及双环和杂双环衍生物，它们的制备方法，含有它们的药物组合物以及它们作为药物的用途。

4. 发明申请

WO2008064823A1 BICYCLIC AND HETEROBICYCLIC DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USES 审中-公开
标题翻译：双相和间苯二酚衍生物，制备它们及其用途的方法
公开(公告)号：WO2008064823A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/010180
申请日：2007-11-23
申请人： UCB PHARMA, S.A. , DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , PERRY, Benjamin , PHILLIPS, David, Jonathan , JONES, MARK, William , DEMAUDE, Thierry , KNERR, Laurent
发明人： DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , PERRY, Benjamin , PHILLIPS, David, Jonathan , JONES, MARK, William , DEMAUDE, Thierry , KNERR, Laurent
IPC分类号： C07D471/04 , C07D401/12 , A61K31/4439 , A61K31/437 , A61K31/404
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention concerns bicyclic and heterobicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及双环和杂双环衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

5. 发明申请

WO2003024967A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003024967A2
公开(公告)日：2003-03-27
申请号：PCT/EP2002/011131
申请日：2002-09-17
申请人： AVENTIS PHARMA S.A. , RATCLIFFE, Andrew, James , WALSH, Rodger, John, Aitchison , MAJID, Tahir, Nadeem , THURAIRATNAM, Sukanthini , AMENDOLA, Shelly , ALDOUS, David, John , SOUNESS, John, Edward , NEMECEK, Conception , WENTZLER, Sylvie , VENOT, Corinne
发明人： RATCLIFFE, Andrew, James , WALSH, Rodger, John, Aitchison , MAJID, Tahir, Nadeem , THURAIRATNAM, Sukanthini , AMENDOLA, Shelly , ALDOUS, David, John , SOUNESS, John, Edward , NEMECEK, Conception , WENTZLER, Sylvie , VENOT, Corinne
IPC分类号： C07D487/00
CPC分类号： A61K31/495 , C07D487/04 , Y02A50/411
摘要： The present invention concerns compounds of general formula (I): in which: R1 represents hydrogen, R4, -C(=Y)-NHR4, -SO2NHR4, -C(=Z1)-R4, -SO2-R4 or -C(=Z1)-OR4; R2 represents hydrogen, cyano, halogen or -C°C-R5;R3 represents hydrogen, acyl, alkoxycarbonyl, alkyl, aroyl, aryl, aryloxycarbonyl, carboxy, cycloalkenyl, cycloalkyl, heteroaroyl, heteroaryl, heterocycloalkyl or -C(=O)-NY1Y2; R4 represents optionally substituted alkyl, cycloalkyl, cycloalkenyl ,heterocycloalkyl, aryl or heteroaryl R5 represents hydrogen or alkyl;R6 represents alkyl, acyl, alkoxycarbonyl, alkylsulfonyl, aryl, arylsulfonyl, aroyl, cycloalkyl, cycloalkenyl, heteroaryl, heteroarylsulfonyl, heteroaroyl and heterocycloalkyl;R7 represents optionally substituted alkyl, cycloalkyl or cycloalkylalkyl, R8 represents hydrogen, alkyl, alkenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl;R9 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R10 represents hydrogen or lower alkyl;R11 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or alkyl optionally substituted by -NY1Y2;R12 represents aryl or heteroaryl; or alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl each optionally substituted Y represents O, S or NCN;Y1 and Y2 (Y3 and Y4) are independently in particular hydrogen, alkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycloalkyl; or the group -NY1Y2 may form 5-7 membered ring or the group -NY3Y4 (-NY5Y6) may form a cyclic amine;Z (Z1)represents O or S; Z2 represents O or S(O)p;n is zero or an integer 1 or 2; m is 1 or 2;p is 1 or 2;and their corresponding N-oxides, their prodrugs; their pharmaceutically acceptable salts and solvates (e.g. hydrates), also together with one or more pharmaceutically acceptable carriers or excipients, such novel indolizines derivatives with inhibitory effects towards kinase proteins and especially for use for preventing or treating diseases that may be modulated by the inhibition of such kinase proteins and particularly solid tumours.
摘要翻译：本发明涉及通式（I）的化合物：其中：R1表示氢，R4，-C（= Y）-NHR4，-SO2NHR4，-C（= Z1）-R4，-SO2-R4或-C = Z1）-OR 4; R 2表示氢，氰基，卤素或-C≡C-R 5; R 3表示氢，酰基，烷氧基羰基，烷基，芳酰基，芳基，芳氧基羰基，羧基，环烯基，环烷基，杂芳酰基，杂芳基，杂环烷基或-C（= O） - NY1Y2; R 4表示任选取代的烷基，环烷基，环烯基，杂环烷基，芳基或杂芳基R 5表示氢或烷基; R 6表示烷基，酰基，烷氧基羰基，烷基磺酰基，芳基，芳基磺酰基，芳酰基，环烷基，环烯基，杂芳基，杂芳基磺酰基，杂芳酰基和杂环烷基; R 8代表烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基烷基; R 9代表任选取代的烷基，环烷基或环烷基烷基，R 8代表氢，烷基，烯基，芳基， R 10表示氢或低级烷基; R 11表示烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基烷基; 或任选被-NY 1 Y 2取代的烷基; R 12表示芳基或杂芳基; 或任选被取代的Y代表O，S或NCN的烷基，环烷基，环烷基烷基，杂环烷基或杂环烷基烷基; Y 1和Y 2（Y 3和Y 4）独立地是氢，烷基，芳基，环烷基，环烯基，杂芳基或杂环烷基; 或-NY1Y2基可以形成5-7元环，或者-NY3Y4（-NY5Y6）可以形成环状胺; Z（Z1）表示O或S; Z2表示O或S（O）p; n为零或整数1或2; m为1或2; p为1或2;及其相应的N-氧化物，其前药; 其药学上可接受的盐和溶剂合物（例如水合物），还与一种或多种药学上可接受的载体或赋形剂一起，具有对激酶蛋白具有抑制作用的新型中氮茚衍生物，特别是用于预防或治疗可能受抑制作用这种激酶蛋白，特别是实体瘤。

6. 发明申请

WO1994027947A1 PHENYLCYCLOPROPANE COMPOUNDS AND THEIR USE AS cAMP AND TNF INHIBITORS 审中-公开
标题翻译：苯并环丙基化合物及其作为cAMP和TNF抑制剂的用途
公开(公告)号：WO1994027947A1
公开(公告)日：1994-12-08
申请号：PCT/GB1994001189
申请日：1994-06-01
申请人： RHONE-POULENC RORER LTD. , FENTON, Garry , MASON, Jonathan, Stephen , PALFREYMAN, Malcom, Norman , RATCLIFFE, Andrew, James
发明人： RHONE-POULENC RORER LTD.
IPC分类号： C07C47/47
CPC分类号： C07C311/07 , C07C43/235 , C07C43/243 , C07C43/253 , C07C45/71 , C07C47/47 , C07C47/575 , C07C49/577 , C07C62/12 , C07C69/007 , C07C225/20 , C07C233/23 , C07C235/40 , C07C251/42 , C07C259/08 , C07C271/24 , C07C271/28 , C07C275/34 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07C2601/08
摘要： This invention relates to substituted phenylcyclopropane derivatives, which carry various substituents on the cyclopropane ring, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for their use in the treatment of disease states, for example disease states associated with proteins that mediate cellular activity, for example by inhibiting tumour necrosis factor and/or by inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及在环丙烷环上携带各种取代基的取代的苯基环丙烷衍生物，其制备方法，含有它们的药物组合物及其用于治疗疾病状态的方法，例如与蛋白质相关的疾病状态介导细胞活性，例如通过抑制肿瘤坏死因子和/或抑制环AMP磷酸二酯酶。

7. 发明申请

WO1994002465A1 INHIBITORS OF c-AMP PHOSPHODIESTERASE AND TNF 审中-公开
标题翻译： c-AMP磷酸二酯酶和TNF的抑制剂
公开(公告)号：WO1994002465A1
公开(公告)日：1994-02-03
申请号：PCT/GB1993001597
申请日：1993-07-28
申请人： RHONE-POULENC RORER LIMITED , FENTON, Garry , MORLEY, Andrew, David , PALFREYMAN, Malcolm, Norman , RATCLIFFE, Andrew, James , SHARP, Brian, William , STUTTLE, Keith, Alfred, James , THURAIRATNAM, Sukanthini , VACHER, Bernard, Yvon, Jack
发明人： RHONE-POULENC RORER LIMITED
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D213/50 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

8. 发明申请

WO2010046639A1 FUSED PYRIDINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：熔融吡啶衍生物作为激酶抑制剂
公开(公告)号：WO2010046639A1
公开(公告)日：2010-04-29
申请号：PCT/GB2009/002504
申请日：2009-10-21
申请人： UCB PHARMA S.A. , JENKINS, Kerry , LOCK, Christopher, James , RATCLIFFE, Andrew, James
发明人： JENKINS, Kerry , LOCK, Christopher, James , RATCLIFFE, Andrew, James
IPC分类号： C07D495/04 , A61P29/00 , A61K31/4365
CPC分类号： C07D495/04
摘要： A series of heteroaryl-substituted fused pyridine derivatives, in particular heteroaryl-substituted thieno[3,2-6]pyridine derivatives, being selective inhibitors of PO 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：一系列杂芳基取代的稠合吡啶衍生物，特别是杂芳基取代的噻吩并[3,2-6]吡啶衍生物，是PO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。

9. 发明申请

WO2009081105A2 QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹诺酮和喹啉衍生物作为激酶抑制剂
公开(公告)号：WO2009081105A2
公开(公告)日：2009-07-02
申请号：PCT/GB2008004171
申请日：2008-12-17
申请人： UCB PHARMA SA , ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
发明人： ALLEN DANIEL REES , BUCKLEY GEORGE MARTIN , BUERLI ROLAND , DAVENPORT RICHARD JOHN , KINSELLA NATASHA , LOCK CHRISTOPHER JAMES , LOWE CHRISTOPHER , MACK STEPHEN ROBERT , PITT WILLIAM ROSS , RATCLIFFE ANDREW JAMES , RICHARD MARIANNA DILANI , SABIN VERITY MARGARET , SHARPE ANDREW , TAIT LAURA JANE , WARRELOW GRAHAM JOHN , WILLIAMS SOPHIE CAROLINE
IPC分类号： C07D401/14 , A61K31/395 , A61P35/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
CPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
摘要： A series of heteroaryl-substituted quinoxaline and quinoline 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：因此，作为PI3激酶的选择性抑制剂的一系列杂芳基取代的喹喔啉和喹啉衍生物在医学中是有益的，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，伤害感受性或眼科疾病中。

10. 发明申请

WO2008138591A2 BICYCLIC AND HETEROBICYCLIC DERIVATIVES,PROCESSES FOR PREPARING THEM AND THEIR USES 审中-公开
标题翻译：双相和间苯二酚衍生物，制备它们及其用途的方法
公开(公告)号：WO2008138591A2
公开(公告)日：2008-11-20
申请号：PCT/EP2008/003838
申请日：2008-05-13
申请人： UCB PHARMA, S.A. , DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , JONES, Mark, William
发明人： DAVENPORT, Richard, John , RATCLIFFE, Andrew, James , JONES, Mark, William
IPC分类号： C07D263/56 , C07D277/66 , C07D413/12 , C07D417/12 , A61K31/41 , A61P35/00
CPC分类号： C07D263/56 , C07D277/66 , C07D413/12 , C07D417/12
摘要： The present invention concerns bicyclic and heterobicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及双环和杂双环衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

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