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1. 发明申请

WO2003001206A1 METHOD OF MASS SPECTROMETRY 审中-公开
标题翻译：质谱法
公开(公告)号：WO2003001206A1
公开(公告)日：2003-01-03
申请号：PCT/GB2002/002921
申请日：2002-06-25
申请人： GLAXO GROUP LIMITED , MCKEOWN, Stephen, Carl
发明人： MCKEOWN, Stephen, Carl
IPC分类号： G01N33/532
CPC分类号： G01N33/6803 , C12Q1/37 , G01N30/7233
摘要： A method of analysing the cleavage of a polymer wherein the polymer is differentially labelled with an isotope and the cleaved fragments of the polymer are analysed by mass spectrometry is disclosed. The method is particularly useful for analysing the cleavage of proteins and more particularly for determining substrate specificity for enzymes such as proteases.
摘要翻译：公开了通过质谱分析分析其中聚合物用同位素差异标记的聚合物裂解的方法和聚合物的切割的片段。该方法特别可用于分析蛋白质的切割，更特别地用于确定酶如蛋白酶的底物特异性。

2. 发明申请

WO0020357A3 CHEMICAL CONSTRUCTS 审中-公开
标题翻译：化学结构
公开(公告)号：WO0020357A3
公开(公告)日：2000-10-26
申请号：PCT/GB9903286
申请日：1999-10-05
申请人： GLAXO GROUP LTD , CARR ROBIN ARTHUR ELLIS , GEHANNE SYLVIE , KAY CORINNE , MCKEOWN STEPHEN CARL , MURRAY PETER JOHN , PAIO ALFREDO , SCICINSKI JAN JOSEF , WATSON STEPHEN PAUL , WILLIAMS GEOFFREY MARTYN , ZARAMELLA ALESSIO
发明人： CARR ROBIN ARTHUR ELLIS , GEHANNE SYLVIE , KAY CORINNE , MCKEOWN STEPHEN CARL , MURRAY PETER JOHN , PAIO ALFREDO , SCICINSKI JAN JOSEF , WATSON STEPHEN PAUL , WILLIAMS GEOFFREY MARTYN , ZARAMELLA ALESSIO
IPC分类号： G01N27/62 , A61K45/00 , B01J20/281 , C07B61/00 , C07C235/20 , C07C271/20 , C07C311/18 , C07D239/42 , G01N30/88 , G01N33/531 , C07C237/18 , C07D239/38
CPC分类号： C40B50/16 , B01J2219/005 , B01J2219/00581 , B01J2219/0072 , C07B2200/05 , C07B2200/11 , C07C235/20 , C07C311/18 , C40B20/08 , C40B30/04 , C40B40/04 , C40B70/00
摘要： The invention provides a chemical construct for use in solid phase synthesis comprising a solid support Q having linked thereto via a connecting group Y a substrate R; the connecting group Y having first and second cleavage sites which are orthogonally and selectively cleavable; the second cleavage site being selectively cleavable to release the substrate; and the first cleavage site being located at a position between the second cleavage site and the solid support and being selectively cleavable to release a fragment Fr comprising the substrate and at least a portion of the connecting group Y; characterised in that cleavage at the first cleavage site forms or introduces on the chemical fragment Fr at the first cleavage site a moiety comprising a sensitising group G (such as an amino group) which sensitises the chemical fragment Fr to instrumental, e.g. mass spectroscopic, analysis. Also provided are methods of analysis employing the constructs, as well as intermediate constructs.
摘要翻译：本发明提供了用于固相合成的化学构建体，其包括通过连接基团Y与基底R连接的固体支持物Q; 连接基团Y具有正交和可选择性切割的第一和第二切割位点; 第二切割位点是可选择性切割的以释放底物; 并且所述第一切割位点位于所述第二切割位点和所述固体支持物之间的位置，并且可选择性地切割以释放包含所述基底和所述连接基团Y的至少一部分的片段Fr; 其特征在于，第一切割位点处的切割在第一切割位点处的化学片段Fr上形成或引入包含使化学片段Fr致敏的器官的致敏基团G（例如氨基）的部分。质谱分析。还提供了使用构建体的分析方法以及中间构建体。

3. 发明申请

WO1997013760A1 TRICYCLIC FUSED COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：三聚体熔融化合物和含有它们的药物组合物
公开(公告)号：WO1997013760A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004396
申请日：1996-10-10
申请人： GLAXO GROUP LIMITED , McKEOWN, Stephen, Carl , PAGE, Martin, John , VILE, Sadie , WALKER, Ann, Louise , HUDSON, Alan, Thomas , BARRACLOUGH, Paul , FRANZMANN, Karl, Witold
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D239/70
CPC分类号： C07D495/04 , C07D239/70
摘要： Substituted heteroaromatic compounds, in particular substituted tricyclic fused compounds in which one terminal ring is pyridine or pyrimidine, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：取代的杂芳族化合物，特别是其中一个末端环是吡啶或嘧啶的取代的三环稠合化合物是蛋白质酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，过敏，哮喘，移植排斥反应，炎症，血栓形成，神经系统疾病和癌症。

4. 发明申请

WO2012007539A9 IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2012007539A9
公开(公告)日：2012-01-19
申请号：PCT/EP2011/062028
申请日：2011-07-14
申请人： NOVARTIS AG , CHARLTON, Steven, John , LEBLANC, Catherine , MCKEOWN, Stephen, Carl
发明人： CHARLTON, Steven, John , LEBLANC, Catherine , MCKEOWN, Stephen, Carl
IPC分类号： C07D471/04 , A61K31/4375 , A61P9/00 , A61P11/00
摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.

5. 发明申请

WO2012007539A1 IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译： IP受体激动剂杂环化合物
公开(公告)号：WO2012007539A1
公开(公告)日：2012-01-19
申请号：PCT/EP2011/062028
申请日：2011-07-14
申请人： NOVARTIS AG , CHARLTON, Steven, John , LEBLANC, Catherine , MCKEOWN, Stephen, Carl
发明人： CHARLTON, Steven, John , LEBLANC, Catherine , MCKEOWN, Stephen, Carl
IPC分类号： C07D471/04 , A61K31/4375 , A61P9/00 , A61P11/00
CPC分类号： A61K31/4985 , A61K31/4375 , C07D471/04
摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.
摘要翻译：本发明提供活化IP受体的杂环衍生物。激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。还包括包含这些衍生物的药物组合物。

6. 发明申请

WO2005040128A1 HETEROCYCLYL COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2005040128A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011964
申请日：2004-10-21
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , LEWELL, Xiao, Qing , LORTHIOIR, Olivier, Eric , MCKEOWN, Stephen, Carl , SCOCCITTI, Tiziana , WATSON, Stephen, Paul
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , LEWELL, Xiao, Qing , LORTHIOIR, Olivier, Eric , MCKEOWN, Stephen, Carl , SCOCCITTI, Tiziana , WATSON, Stephen, Paul
IPC分类号： C07D231/14
CPC分类号： C04B35/632 , C07D207/34 , C07D231/14 , C07D401/12 , C07D409/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein W, X, Y, Z, R 1 , R 2a , R 2b , and R x , R 8 , and R 9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中W，X，Y，Z，R 1，R 2a，R 2b和R x，R 8和R 本说明书中定义，制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

7. 发明申请

WO1997013771A1 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的双相异构化合物
公开(公告)号：WO1997013771A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004399
申请日：1996-10-10
申请人： GLAXO GROUP LIMITED , COCKERILL, George, Stuart , GUNTRIP, Stephen, Barry , McKEOWN, Stephen, Carl , PAGE, Martin, John , SMITH, Kathryn, Jane , VILE, Sadie , HUDSON, Alan, Thomas , BARRACLOUGH, Paul , FRANZMANN, Karl, Witold
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D495/04
摘要： Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R is a group ZR wherein Z is joined to R through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR'), V(CHR) or V where R and R' are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NR where R is hydrogen or R is C1-4 alkyl; and R is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R is a group ZR in which Z is NR , and NR and R together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：取代的式（A）的杂芳族化合物，其中X是N或CH; 其中（a）表示稠合的5,6或7元杂环，R 3是基团ZR 4，其中Z通过（CH 2）p基团与R 4连接，其中p为0 ，1或2，Z表示V（CH2），V（CF2），（CH2）V，（CF2）V，V（CRR'），V（CHR）或V，其中R和R' -4-烷基，其中V是含有0,1或2个碳原子的烃基，羰基，二羰基，CH（OH），CH（CN），磺酰胺，酰胺，O，S（O）其中R b是氢或R b是C 1-4烷基; 和R 4是任选取代的C 3-6环烷基或任选取代的5,6,7,8,9或10元碳环或杂环部分; 或R 3是Z Z 4，其中Z是NR b，NR b和R 4一起形成任选取代的5,6,7,8,9或10元碳环或杂环部分是蛋白质酪氨酸激酶抑制剂。描述了这些化合物，以及其制备方法，包括这些化合物的药物组合物及其在医学中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，过敏，哮喘，移植排斥，炎症，血栓形成，神经系统疾病和癌症。

8. 发明申请

WO2014125413A1 IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译： IP受体激动剂杂环化合物
公开(公告)号：WO2014125413A1
公开(公告)日：2014-08-21
申请号：PCT/IB2014/058905
申请日：2014-02-11
申请人： NOVARTIS AG , BUTLER, Rebecca , LEBLANC, Catherine , MCKEOWN, Stephen Carl , CHARLTON, Steven John
发明人： BUTLER, Rebecca , LEBLANC, Catherine , MCKEOWN, Stephen Carl , CHARLTON, Steven John
IPC分类号： C07D471/04 , A61K31/4375 , A61P7/02 , A61P9/10 , A61P11/06 , A61P3/10 , A61P29/00 , A61P19/04
CPC分类号： C07D471/04 , A61K31/4375
摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.
摘要翻译：本发明提供活化IP受体的杂环衍生物。激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。还包括包含这些衍生物的药物组合物。

9. 发明申请

WO2006114313A1 PYRAZOLE COMPOUNDS AS PROSTAGLANDIN RECEPTORS LIGANDS 审中-公开
标题翻译：作为PROSTAGLANDIN受体配体的吡咯化合物
公开(公告)号：WO2006114313A1
公开(公告)日：2006-11-02
申请号：PCT/EP2006/003919
申请日：2006-04-24
申请人： GLAXO GROUP LIMITED , CONWAY, Elizabeth, Ann , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HALL, Adrian , HAYHOW, Thomas, George, Christopher , HEALY, Mark, Patrick , HURST, David, Nigel , KILFORD, Ian, Reginald , MCKEOWN, Stephen, Carl , NAYLOR, Alan , PRICE, Helen Susanne , RAWLINGS, Derek Anthony
发明人： CONWAY, Elizabeth, Ann , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HALL, Adrian , HAYHOW, Thomas, George, Christopher , HEALY, Mark, Patrick , HURST, David, Nigel , KILFORD, Ian, Reginald , MCKEOWN, Stephen, Carl , NAYLOR, Alan , PRICE, Helen Susanne , RAWLINGS, Derek Anthony
IPC分类号： A61K31/4155 , C07D231/14 , C07D231/20 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12
CPC分类号： C07D231/40 , C07D231/14 , C07D231/20 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R 1 ,R 2a , R 2b , R 10 , R 11 and R x are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中Z，R 1，R 2a，R 2b，R 2b， 10，R 11和R x如本说明书中所定义，制备这些化合物的方法，包含这些化合物的药物组合物和使用药物中的这种化合物。

10. 发明申请

WO2005051890A1 AMINOPHENYLCYCLOPROPYL CARBOXYLIC ACIDS AND DERIVATIVES AS AGONISTS TO GPR40 审中-公开
标题翻译：氨基苯甲酰基羧酸和衍生物作为GPR40的激素
公开(公告)号：WO2005051890A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/038126
申请日：2004-11-15
申请人： SMITHKLINE BEECHAM CORPORATION , CORBETT, David, Francis , DWORNIK, Kate, Anna , GARRIDO, Dulce, Maria , MCKEOWN, Stephen, Carl , MILLS, Wendy, Yoon , PEAT, Andrew, James , SMALLEY, Terrence, Lee, Jr.
发明人： CORBETT, David, Francis , DWORNIK, Kate, Anna , GARRIDO, Dulce, Maria , MCKEOWN, Stephen, Carl , MILLS, Wendy, Yoon , PEAT, Andrew, James , SMALLEY, Terrence, Lee, Jr.
IPC分类号： C07C229/46
CPC分类号： C07C229/46 , C07C237/24 , C07C323/37 , C07C2601/02 , C07D213/38 , C07D277/28 , C07D277/34 , C07D295/13 , C07D307/52 , C07D333/20 , C07D407/12
摘要： The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.
摘要翻译：本发明一般涉及新的治疗化合物，更具体地涉及新化合物，它们作为GPR40激动剂的用途，其制备方法和用于其制备的中间体。

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