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1. 发明申请

WO2011054783A3 PROCESSES FOR THE PREPARATION OF 5 - LIPOOXYGENASE ACTIVATING PROTEIN INHIBITORS AND THEIR INTERMEDIATES 审中-公开
标题翻译：制备5-LIPOOXYGENASE激活蛋白抑制剂及其中间体的方法
公开(公告)号：WO2011054783A3
公开(公告)日：2011-07-07
申请号：PCT/EP2010066577
申请日：2010-11-02
申请人： GLAXO GROUP LTD , AMIRA PHARMACEUTICALS INC , CRAWFORD CLAIRE FRANCES , GARCIA SANDRINE , GRAHAM JONATHAN PAUL , HARLING SANDRA JANE , HENLEY NICHOLAS PAUL , HERMITAGE STEPHEN ANDREW , HUTCHINSON JOHN HOWARD , KEEL TREVOR RAYMOND , KENNEDY ANDREW , MASON ANDREW MCMURTRIE , SCOTT MARK SIMON , SMITH NEIL MICHAEL , STOCK NICHOLAS SIMON , TATENO YUICHI , TROUW LEONTINE SASKIA , TURNER PETER GRAHAM , WALLIS CHRISTOPHER JOHN , WILLACY ROBERT DAVID
发明人： CRAWFORD CLAIRE FRANCES , GARCIA SANDRINE , GRAHAM JONATHAN PAUL , HARLING SANDRA JANE , HENLEY NICHOLAS PAUL , HERMITAGE STEPHEN ANDREW , HUTCHINSON JOHN HOWARD , KEEL TREVOR RAYMOND , KENNEDY ANDREW , MASON ANDREW MCMURTRIE , SCOTT MARK SIMON , SMITH NEIL MICHAEL , STOCK NICHOLAS SIMON , TATENO YUICHI , TROUW LEONTINE SASKIA , TURNER PETER GRAHAM , WALLIS CHRISTOPHER JOHN , WILLACY ROBERT DAVID
IPC分类号： C07D403/14
CPC分类号： C07D403/14
摘要： The present invention provides processes useful for preparing 5-lipoxygenase activating protein (FLAP) inhibitors and their intermediates. In particular, processes for preparing 3-[3-(tert-butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, the anhydrous Form C polymorph of sodium 3-[3- (tert-butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1H- indol-2-yl]-2,2-dimethyl-propionate, and intermediates useful in said processes are provided.
摘要翻译：本发明提供了可用于制备5-脂氧合酶活化蛋白（FLAP）抑制剂及其中间体的方法。特别地，制备3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-3-基）苄基] -5-（5-甲基 - 吡啶-2-基 - 甲氧基）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸，3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-2-基）（5-甲基 - 吡啶-2-基 - 甲氧基）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸酯，以及可用于所述方法的中间体。

2. 发明申请

WO2006085112A1 ANTHRANILIC ACID DERIVATIVES AS HM74A RECEPTOR AGONISTS 审中-公开
标题翻译：作为HM74A受体激动剂的ANTHRANILIC酸性衍生物
公开(公告)号：WO2006085112A1
公开(公告)日：2006-08-17
申请号：PCT/GB2006/000508
申请日：2006-02-14
申请人： SMITHKLINE BEECHAM CORPORATION , HATLEY, Richard , MASON, Andrew, Mcmurtrie , PINTO, Ivan, Leo , SMITH, Ian, Edward, David
发明人： HATLEY, Richard , MASON, Andrew, Mcmurtrie , PINTO, Ivan, Leo , SMITH, Ian, Edward, David
IPC分类号： C07D253/08 , C07D401/04 , C07D271/06 , C07C235/24 , A61K31/53 , A61K31/4245 , A61K31/196 , A61P9/10
CPC分类号： C07C235/24 , C07D253/10 , C07D271/06 , C07D401/04
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R 1 , R 2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：其中R 1，R 2和W的式（I）的治疗活性的邻氨基苯甲酸衍生物如说明书中所定义，用于制备所述衍生物，药物制剂含有活性化合物和化合物在治疗中的用途，特别是在治疗其中HM74A受体的活化不足有助于疾病或其中受体的活化将是有益的疾病方面。

3. 发明申请

WO2006085111A1 ANTHRANILIC ACID DERIVATIVES ACTIVE AT THE HM74A RECEPTOR 审中-公开
标题翻译： HM74A受体活性的氨基酸衍生物
公开(公告)号：WO2006085111A1
公开(公告)日：2006-08-17
申请号：PCT/GB2006/000506
申请日：2006-02-14
申请人： SMITHKLINE BEECHAM CORPORATION , MASON, Andrew, Mcmurtrie , PINTO, Ivan, Leo , RAHMAN, Shahzad, Sharooq
发明人： MASON, Andrew, Mcmurtrie , PINTO, Ivan, Leo , RAHMAN, Shahzad, Sharooq
IPC分类号： C07C235/24 , C07D257/04 , A61K31/167 , A61K31/41 , A61P3/10
CPC分类号： C07D257/04 , C07C235/24
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) or of Formula (Ia) wherein R, R 1 , R 2 and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：其中R，R 1，R 2和Z如式（I）或式（Ia）的治疗活性的邻氨基苯甲酸衍生物如说明书中所定义，所述衍生物的制备，含有活性化合物的药物制剂和该化合物在治疗中的用途，特别是用于治疗HM74A受体的未激活有助于该疾病或受体的活化将是有益的疾病，被披露。

4. 发明申请

WO2002064564A1 BENZO'F!ISOINDOLE DERIVATIVES WITH AFFINITY TO THE EP4 RECEPTOR 审中-公开
标题翻译： BENZO'F！具有对EP4受体的亲和力的ISOINDOLE衍生物
公开(公告)号：WO2002064564A1
公开(公告)日：2002-08-22
申请号：PCT/GB2002/000522
申请日：2002-02-07
申请人： GLAXO GROUP LIMITED , CONGREVE, Miles, Stuart , GIBLIN, Gerard, Martin, Paul , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , ROOMANS, Susan , WALKER, Ann, Louise
发明人： CONGREVE, Miles, Stuart , GIBLIN, Gerard, Martin, Paul , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , ROOMANS, Susan , WALKER, Ann, Louise
IPC分类号： C07D209/64
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) wherein R 1 and R 3 are the same or different and represent =O, hydrogen, C 1-6 alkyl, C 1-6 dialkyl, =CHC 1 -C 5 alkyl, =S, or a 5- or 6-membered anyl; R 4 to R 9 are the same or different and represent hydrogen, C 1-6 alkoxy, OCF 3 , OCH 2 CF 3 , O-cyclopropyl, OCH 2 -cyclopropyl, C 1 -C 6 alkyl, S-alkyl, NR 2 10¿ where R 10 is hydrogen or C 1-6 alkyl, halogen, NO 2 , OH, CH 2 OC 1 -C 6 alkly, CH 2 OH, or CF 3 ; Q 1 is hydrogen, C 1-6 alkyl, C 1-6 dialkyl, C 1-6 alkoxy, NHAc, NR 2 10¿ where R 10 is hydrogen is hydrogen or C 1-6 alkyl, difluoro, fluoro, =O, or OH; Q 2 , Q 3 , Q 4 and Q 5 are the same or different and represent hydrogen, C 1-6 alkoxy, OCF 3 , OCH 2 CF 3 , O-cyclopropyl, OCH 2 -cyclopropyl, C 1 -C 6 alkyl, S-alkyl, NR 2 10¿ where R 10 is hydrogen or C 1-6 alkyl, halogen, NO 2 , OH, CH 2 OC 1 -C 6 alkyl, CH 2 OH, or a 5-or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.
摘要翻译：式（I）化合物，其中R 1和R 3相同或不同，表示= O，氢，C 1-6烷基，C 1-6二烷基，= CHCl-C 5烷基，= S或5-或 6元芳基; R 4至R 9相同或不同，表示氢，C 1-6烷氧基，OCF 3，OCH 2 CF 3，O-环丙基，OCH 2 - 环丙基，C 1 -C 6烷基，S-烷基，NR 2 10，其中R 10为氢或C1- 6烷基，卤素，NO 2，OH，CH 2 OC 1 -C 6烷基，CH 2 OH或CF 3; Q 1是氢，C 1-6烷基，C 1-6二烷基，C 1-6烷氧基，NHAc，NR 2 10，其中R 10是氢或C 1-6烷基，二氟，氟，= O或OH; Q 2，Q 3，Q 4和Q 5相同或不同，表示氢，C 1-6烷氧基，OCF 3，OCH 2 CF 3，O-环丙基，OCH 2 - 环丙基，C 1 -C 6烷基，烷基，NR210，其中R10是氢或C1-6烷基，卤素，NO2，OH，CH2OC1-C6烷基，CH2OH或5-或6-元芳基; 条件是化合物[4-（1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基] -2-丙酸钠盐和[4-（4,9 - 二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基]乙酸; 及其药学上可接受的衍生物。

5. 发明申请

WO2011054783A2 NOVEL PROCESSES 审中-公开
标题翻译：新进程
公开(公告)号：WO2011054783A2
公开(公告)日：2011-05-12
申请号：PCT/EP2010/066577
申请日：2010-11-02
申请人： GLAXO GROUP LIMITED , AMIRA PHARMACEUTICALS, INC. , CRAWFORD, Claire Frances , GARCIA, Sandrine , GRAHAM, Jonathan Paul , HARLING, Sandra Jane , HENLEY, Nicholas Paul , HERMITAGE, Stephen Andrew , HUTCHINSON, John Howard , KEEL, Trevor Raymond , KENNEDY, Andrew , MASON, Andrew McMurtrie , SCOTT, Mark Simon , SMITH, Neil Michael , STOCK, Nicholas Simon , TATENO, Yuichi , TROUW, Leontine Saskia , TURNER, Peter Graham , WALLIS, Christopher John , WILLACY, Robert David
发明人： CRAWFORD, Claire Frances , GARCIA, Sandrine , GRAHAM, Jonathan Paul , HARLING, Sandra Jane , HENLEY, Nicholas Paul , HERMITAGE, Stephen Andrew , HUTCHINSON, John Howard , KEEL, Trevor Raymond , KENNEDY, Andrew , MASON, Andrew McMurtrie , SCOTT, Mark Simon , SMITH, Neil Michael , STOCK, Nicholas Simon , TATENO, Yuichi , TROUW, Leontine Saskia , TURNER, Peter Graham , WALLIS, Christopher John , WILLACY, Robert David
CPC分类号： C07D403/14
摘要： The present invention provides processes useful for preparing 5-lipoxygenase activating protein (FLAP) inhibitors and their intermediates. In particular, processes for preparing 3-[3-( tert -butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1 H -indol-2-yl]-2,2-dimethyl-propionic acid, the anhydrous Form C polymorph of sodium 3-[3- ( tert -butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1 H - indol-2-yl]-2,2-dimethyl-propionate, and intermediates useful in said processes are provided.
摘要翻译：本发明提供了可用于制备5-脂氧合酶活化蛋白（FLAP）抑制剂及其中间体的方法。特别地，制备3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-3-基）苄基] -5-（5-甲基 - 吡啶-2-基 - 甲氧基）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸，3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-2-基）（5-甲基 - 吡啶-2-基 - 甲氧基）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸酯，以及可用于所述方法的中间体。

6. 发明申请

WO2006000399A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006000399A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006760
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
发明人： BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
IPC分类号： C07D401/06
CPC分类号： A61K31/5377 , C07D401/06 , C07D413/14
摘要： Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2, 6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：式（I）的化合物，其中R 1是2-茚满基，R 2是1-甲基丙基，R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团，R 4表示甲基和R 5 表示氢或甲基，或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物，其制备方法，含有它们的药物组合物及其在药物中的用途，特别是其用作催产素拮抗剂。

7. 发明申请

WO2003053443A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2003053443A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014823
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译：一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的哺乳动物施用有效量的式I化合物和/或其生理上可接受的衍生物，其中所述取代基具有给定的含义在说明中。公开了式I的新化合物及其制备方法。

8. 发明申请

WO2002100886A1 PYRROLIDIN-2-ONE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译：吡咯烷-2-酮衍生物作为因子XA的抑制剂
公开(公告)号：WO2002100886A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002586
申请日：2002-06-06
申请人： GLAXO GROUP LIMITED , CHAN, Chuen , HAMBLIN, Julie, Nicole , KELLY, Henry, Andreson , KING; Nigel, Paul , MASON, Andrew, McMurtrie , PATEL, Vipulkumar, Kantibhai , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , WESTON, Helen, Elisabeth , WHITWORTH, Caroline , YOUNG, Robert, John
发明人： CHAN, Chuen , HAMBLIN, Julie, Nicole , KELLY, Henry, Andreson , KING; Nigel, Paul , MASON, Andrew, McMurtrie , PATEL, Vipulkumar, Kantibhai , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , WESTON, Helen, Elisabeth , WHITWORTH, Caroline , YOUNG, Robert, John
IPC分类号： C07K5/06
CPC分类号： A61K9/0031 , A61K9/0019 , A61K9/0024 , A61K9/0043 , A61K9/0056 , A61K9/0073 , A61K9/0095 , A61K9/02 , A61K9/12 , A61K31/4025 , A61K31/454 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（Ic）化合物的制备方法，含有它们的药物组合物及其在药物中的用途，特别是用于改善指定因子Xa抑制剂的临床病症。

9. 发明申请

WO2005016867A3 ANTHRANILIC ACID DERIVATIVES AND THEIR USE AS ACTIVATORS OF THE HM74A RECEPTOR 审中-公开
公开(公告)号：WO2005016867A3
公开(公告)日：2005-02-24
申请号：PCT/GB2004/003516
申请日：2004-08-13
申请人： SMITHKLINE BEECHAM CORPORATION , CAMPBELL, Mathew , HATLEY, Richard, Jonathan , HEER, Jag, Paul , MASON, Andrew, McMurtrie , PINTO, Ivan, Leo , RAHMAN, Shahzad, Sharooq , SMITH, Ian, Edward, David
发明人： CAMPBELL, Mathew , HATLEY, Richard, Jonathan , HEER, Jag, Paul , MASON, Andrew, McMurtrie , PINTO, Ivan, Leo , RAHMAN, Shahzad, Sharooq , SMITH, Ian, Edward, David
IPC分类号： C07C233/55
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R 1 , R 2 and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.

10. 发明申请

WO2005016867A2 ANTHRANILIC ACID DERIVATIVES AND THEIR USE AS ACTIVATORS OF THE HM74A RECEPTOR 审中-公开
标题翻译：壬二酸衍生物及其作为HM74A受体的激活剂使用
公开(公告)号：WO2005016867A2
公开(公告)日：2005-02-24
申请号：PCT/GB2004003516
申请日：2004-08-13
申请人： SMITHKLINE BEECHAM CORP , CAMPBELL MATHEW , HATLEY RICHARD JONATHAN , HEER JAG PAUL , MASON ANDREW MCMURTRIE , PINTO IVAN LEO , RAHMAN SHAHZAD SHAROOQ , SMITH IAN EDWARD DAVID
发明人： CAMPBELL MATHEW , HATLEY RICHARD JONATHAN , HEER JAG PAUL , MASON ANDREW MCMURTRIE , PINTO IVAN LEO , RAHMAN SHAHZAD SHAROOQ , SMITH IAN EDWARD DAVID
IPC分类号： C07C233/55 , C07C235/24 , C07C235/38 , C07C237/22 , C07D209/18 , C07D217/12 , C07D217/24 , C07D317/60 , C07D333/60 , A61K31/196 , A61K31/33 , C07D215/36 , C07D217/14
CPC分类号： C07D209/18 , C07C233/55 , C07C235/24 , C07C235/38 , C07C237/22 , C07C2602/08 , C07C2602/10 , C07D217/12 , C07D217/24 , C07D317/60 , C07D333/60
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：式（I）的治疗活性的邻氨基苯甲酸衍生物，其中R1，R2和Z如说明书中所定义，所述衍生物的制备方法，含有活性化合物的药物制剂以及该化合物在治疗中的用途，特别是在治疗中公开了其中HM74A受体的未激活有助于疾病或受体激活将是有益的疾病。

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