公开(公告)号：EP1112003B2

公开(公告)日：2011-09-14

申请号：EP99946084.3

申请日：1999-08-31

申请人： SMITHKLINE BEECHAM PLC

发明人： BAKER, Nicola SmithKline Beecham Consumer Brands ,  PARKER, David SmithKline Beecham Consumer Brands

IPC分类号： A23L1/05 ,  A23L2/52 ,  A61Q11/00 ,  A61K8/73

CPC分类号： A23L2/385 ,  A23L2/62 ,  A23L29/231 ,  A23L29/238 ,  A23L29/256 ,  A23L29/262 ,  A23L29/27 ,  A61K8/73 ,  A61K8/733 ,  A61K8/8176 ,  A61K2800/52 ,  A61Q11/00 ,  Y10S514/901

摘要： The use of viscosity modifying polymer materials, commonly used as stabilisers, thickeners and emulsifiers, as tooth erosion inhibitors in acidic compositions for oral administration, especially in acidic beverages such as fruit drinks and oral healthcare products such as mouthwashes, in which the effective pH of the composition is less than or equal to 4.5.

公开(公告)号：EP1686119B1

公开(公告)日：2009-07-29

申请号：EP06075890.1

申请日：2001-02-13

申请人： SMITHKLINE BEECHAM PLC

发明人： Hickey, Deidre, Mary, B. c/o GlaxoSmithKline ,  Ife, Robert, John c/o GlaxoSmithKline ,  Leach, Colin, Andrew c/o GlaxoSmithKline ,  Pinto, Ivan, Leo c/o GlaxoSmithKline ,  Smith, Stephen, Allan c/o GlaxoSmithKline ,  Stanway, Steven, James c/o GlaxoSmithKline

IPC分类号： C07D239/56 ,  C07D401/12 ,  C07D239/70 ,  C07D239/26 ,  C07D213/06 ,  C07D213/54 ,  C07C15/14 ,  A61K31/505 ,  A61P3/06

CPC分类号： C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12 ,  C07D495/04

摘要： Pyrimidinone compounds of formula (I) are inhibitors of the enzyme LpPLA2 and are useful in the treatment of atherosclerosis

公开(公告)号：EP1274321B1

公开(公告)日：2008-08-20

申请号：EP01925499.4

申请日：2001-03-23

申请人： SMITHKLINE BEECHAM PLC

发明人： BAKER, Nicola, Jane ,  PARKER, David, Myatt

IPC分类号： A23L1/304 ,  A23L2/52 ,  A61Q11/00

CPC分类号： A61Q11/00 ,  A23L2/39 ,  A23L2/52 ,  A23L33/16 ,  A23V2002/00 ,  A61K8/24 ,  A23V2250/046 ,  A23V2250/1578 ,  A23V2250/50

摘要： The use of polyphosphate in acidic oral compositions, especially acid beverages with a pH between 2.2 and 5.5, to alleviate or prevent the tooth damage associated with the consumption of acid. The invention may be practised using polyphosphate alone or in combination with calcium and/or viscosity modifying polymers.

摘要翻译： 在酸性口服组合物中使用多磷酸盐，特别是pH在2.2和5.5之间的酸性饮料，以减轻或防止与消耗酸相关的牙齿损伤。 本发明可以单独使用多磷酸盐或与钙和/或粘度改性聚合物组合来实施。

公开(公告)号：EP1075539B1

公开(公告)日：2008-08-06

申请号：EP99923518.7

申请日：1999-04-28

申请人： SMITHKLINE BEECHAM PLC

发明人： CLARKE, Stephen, Edward

IPC分类号： C12Q1/26 ,  C07D311/16

CPC分类号： C07D311/16 ,  C12Q1/26

摘要： Coumarin derivatives as substrates for cytochrome P450 enzyme.

摘要翻译： 香豆素衍生物作为细胞色素P450酶的底物。

公开(公告)号：EP1930330A1

公开(公告)日：2008-06-11

申请号：EP08152170.0

申请日：1998-10-27

申请人： SMITHKLINE BEECHAM PLC ,  SmithKline Beecham Corporation

发明人： Berry, Valerie ,  Dabbs, Stephen ,  Frydrych, Colin, Henry ,  Hunt, Eric ,  Woodnutt, Gary ,  Sanderson, Francis, Dominic

IPC分类号： C07D453/02 ,  A61K31/435 ,  C07D451/02 ,  C07D471/08 ,  C07D487/08 ,  C07D211/62 ,  A61K31/445

CPC分类号： C07D451/02 ,  C07D211/20 ,  C07D211/54 ,  C07D451/04 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

摘要： Derivatives of pleuromutilin in which the glycolic ester moiety at position 14 is replaced by R 2 (CH 2 ) m X(CH 2 ) n CH 2 COO are of use in antimicrobial therapy. In which: each of n and m is independently 0, 1 or 2; X is selected from -O-, -S-, -S(O)-, -SO 2 -, -CO.O-, -NH-, -CONH-, -NHCONH- and a bond;R 1 is vinyl or ethyl;R 2 is a non-aromatic monocyclic or bicyclic group containing one or two basic nitrogen atoms and attached through a ring carbon atom; R 3 is H or OH; or the moiety R 2 (CH 2 ) m X(CH 2 ) n CH 2 COO at position 14 of (IA) or (IB) is replaced by R a R b C=CHCOO in which one of R a and R b is hydrogen and the other is R 2 or R a and R b together form R 2 ; or a pharmaceutically acceptable salt thereof

摘要翻译： 其中第14位的乙醇酸酯部分被R 2（CH 2）m X（CH 2）n CH 2 COO代替的去促胰岛素的衍生物在抗微生物治疗中是有用的。 其中：n和m各自独立地为0,1或2; X选自-O - ， - S - ， - S（O） - ， - SO 2 - ， - COO - ， - NH - ， - CONH - ， - NHCONH-和键; R 1是乙烯基或 乙基; R 2是含有一个或两个碱性氮原子并通过环碳原子连接的非芳族单环或双环基团; R 3是H或OH; 或（IA）或（IB）的第14位上的部分R 2（CH 2）m X（CH 2）n CH 2 COO被R a R b C = CHCOO代替，其中R a和R b之一为 氢，另一个是R 2或R a和R b一起形成R 2; 或其药学上可接受的盐

公开(公告)号：EP1913945A3

公开(公告)日：2008-04-30

申请号：EP07120386.3

申请日：2000-11-16

申请人： SMITHKLINE BEECHAM PLC

发明人： Lewis, Karen ,  Lilliott, Nicola, Jayne ,  Mackenzie, Donald, Colin

IPC分类号： A61K31/425 ,  A61K9/20 ,  A61K9/50 ,  A61K31/155 ,  A61P3/10

CPC分类号： A61K31/425 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2077 ,  A61K9/209 ,  A61K9/5084 ,  A61K31/155 ,  A61K31/427 ,  A61K31/4439 ,  Y10S514/866 ,  Y10S514/96 ,  Y10S514/961 ,  Y10S514/962 ,  A61K2300/00

摘要： A pharmaceutical composition, comprising a thiazolidinedione, such as Compound (I), metformin hydrochloride and a pharmaceutically acceptable carrier, wherein the thiazolidinedione and metformin hydrochloride are each dispersed within its own pharmaceutically acceptable carrier in the pharmaceutical composition for use in the treatment of conditions associated with the pre-diabetic state.

公开(公告)号：EP1305312B1

公开(公告)日：2008-04-23

申请号：EP01954162.2

申请日：2001-08-03

申请人： SMITHKLINE BEECHAM PLC

发明人： CHOUDARY, Bernadette Marie ,  CRAIG, Andrew Simon ,  HO, Tim Chien Ting ,  MACKENZIE, Donald, Colin ,  O'KEEFFE, Deirdre

IPC分类号： C07D417/12 ,  A61K31/44 ,  A61P3/08

CPC分类号： C07D417/12

摘要： A novel pharmaceutical compound 5-[4-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione D(-) Tartrate or a solvate thereof, a process for preparing such a compound, a pharmaceuitcal composition comprising such a compound and the use of such a compound in medicine.

摘要翻译： 一种新的药物化合物5- [4-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基]噻唑烷-2,4-二酮D（ - ）酒石酸盐或其溶剂化物，制备这种 化合物，包含这种化合物的药物组合物以及这种化合物在药物中的用途。

公开(公告)号：EP1900736A1

公开(公告)日：2008-03-19

申请号：EP07150376.7

申请日：2002-11-19

申请人： SMITHKLINE BEECHAM PLC

发明人： Leonard, Graham, Stanley ,  Lewis, Karen, Jane ,  Mackenzie, Donald, Colin

IPC分类号： C07D417/12

CPC分类号： C07D417/12 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/2077 ,  A61K31/4439

摘要： A compound, 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione ('Compound (I)'), or a pharmaceutically acceptable form thereof, in particulate form wherein the median value of the volume mean diameter of the particles is within the range 500nm to 5 micrometres and medicinal uses thereof.

摘要翻译： 化合物5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基]噻唑烷-2,4-二酮（'化合物（I）'）或药学上可接受的形式 其颗粒形式，其中颗粒的体积平均直径的中值在500nm至5微米的范围内及其药用用途。

公开(公告)号：EP1385845B1

公开(公告)日：2008-01-09

申请号：EP02722482.3

申请日：2002-05-02

申请人： SMITHKLINE BEECHAM PLC

发明人： BRANCH, Clive, Leslie, c/o GlaxoSmithKline ,  COULTON, Steven, c/o GlaxoSmithKline ,  JOHNS, Amanda, c/o GlaxoSmithKline ,  JOHNSON, Christopher, Norbert, c/o GlaxoSmithKlin ,  PORTER, Roderick, Alan, c/o GlaxoSmithKline ,  STEMP, Geoffrey, c/o GlaxoSmithKline ,  THEWLIS, Kevin, c/o GlaxoSmithKline

IPC分类号： C07D417/14 ,  A61K31/445 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12 ,  A61K31/505 ,  C07D471/04 ,  A61K31/5377 ,  C07D401/14 ,  C07D498/04 ,  C07D403/14 ,  A61P25/20 ,  A61P9/10 ,  A61P3/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents O or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C¿1-4?)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; when Ar?1¿ is aryl p is not 1; or a pharmaceutical acceptable salt thereof.

公开(公告)号：EP1335915B1

公开(公告)日：2008-01-02

申请号：EP01996537.5

申请日：2001-11-12

申请人： SMITHKLINE BEECHAM PLC

发明人： HADLEY, Michael, Stewart, GlaxoSmithKline ,  LIGHTFOOT, Andrew, P., GlaxoSmithKline ,  MACDONALD, Gregor, James, GlaxoSmithKline ,  STEMP, Geoffrey, GlaxoSmithKline

IPC分类号： C07D403/12

CPC分类号： C07D223/16 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

摘要： The invention provides compounds of formula (I), wherein R1-R4, A, B and t are as defined in claim 1. The compounds are modulators of dopamine D¿3? receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.