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1. 发明授权

EP1471884B1 PHARMACEUTICAL FORMULATION COMPRISING AN ANDROSTANE DERIVATIVE AND A SOLUBILISING AGENT IN AN AQUEOUS LIQUID CARRIER 有权转让
标题翻译：含有ANDROSTANE衍生物和溶解剂的药物制剂在水性液体载体中的应用
公开(公告)号：EP1471884B1
公开(公告)日：2017-10-18
申请号：EP03702727.3
申请日：2003-02-04
申请人： Glaxo Group Limited
发明人： BIGGADIKE, Keith, GlaxoSmithKline , BUXTON, Ian, GlaxoSmithKline Inc. , DALEY-YATES, Peter, Terence, GlaxoSmithKline , FONG, Bettina, GlaxoSmithKline Inc. , HO, Elita, Y., GlaxoSmithKline Inc. , REED, Kenton, Lewis, GlaxoSmithKline Inc. , SAYANI, Amyn, GlaxoSmithKline Inc.
IPC分类号： A61K45/06 , A61P11/00 , A61K47/10 , A61K9/00 , A61K47/32 , A61P11/02 , A61K31/56 , A61K31/58 , A61K47/24 , A61K47/26 , A61K47/34 , A61K47/44
CPC分类号： A61K31/56 , A61K9/0043 , A61K31/58 , A61K45/06 , A61K47/10 , A61K47/24 , A61K47/26 , A61K47/34 , A61K47/44 , Y10S514/826 , A61K2300/00
摘要： There is provided according to the invention a pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) an ester of fluticasone or a solvate thereof as medicament and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.

2. 发明授权

EP1775305B1 6.Alpha.,9.alpha.-difluoro-17.alpha.-'(2-furanylcarboxyl) oxy]-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothiotic acid s-fluoromethyl ester as an anti-inflammatory agent 有权
标题翻译： 6α，9α-二氟-17α' - （2-呋喃基羧基）氧基]-11β-羟基-16α-甲基-3-氧代 - 雄甾-1,4， - 二烯-17-碳泊三烯酸s-氟甲基酯作为抗炎剂
公开(公告)号：EP1775305B1
公开(公告)日：2014-09-17
申请号：EP07101269.4
申请日：2001-08-03
申请人： Glaxo Group Limited
发明人： Biggadike, Keith , Coote, Steven, John , Nice, Rosalyn, Kay
IPC分类号： C07J31/00 , A61K31/58 , A61P5/44 , A61P11/06 , A61P11/08 , C07J17/00
CPC分类号： C07J31/006

3. 发明公开

EP2720719A2 METHOD OF SELECTING THERAPEUTIC INDICATIONS 审中-公开
标题翻译：一种用于选择治疗适应症
公开(公告)号：EP2720719A2
公开(公告)日：2014-04-23
申请号：EP12800675.6
申请日：2012-06-15
申请人： Glaxosmithkline Intellectual Property (No. 2) Limited
发明人： AGARWAL, Pankaj , CARDON, Lon, R. , MOOSER, Vincent, Eugene , SANSEAU, Philippe
IPC分类号： A61K39/395
CPC分类号： C12Q1/6883 , A61K31/215 , A61K31/4152 , A61K31/7072 , C12Q2600/106
摘要： Methods are provided for repositioning a pharmaceutical, comprising the steps of: a. selecting at least one target gene or gene product associated with the treatment of at least one first disease, trait and/or phenotype by said pharmaceutical, b. identifying at least one second disease, trait and/or phenotype for at least one target gene of pharmaceutical mentioned in (a) using genome- wide associated studies, and c. selecting at least one second disease, trait and/or phenotype based on step (b) for treatment with said pharmaceutical compound in step (a). Methods are provided for treating Crohn's disease in a human in need thereof, comprising administering denosumab to said human.

4. 发明授权

EP1841780B1 ANDROSTANE 17-ALPHA-CARBONATE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC AND INFLAMMATORY CONDITIONS 有权
标题翻译：雄甾烷-17-α-碳酸酯衍生物FOR USE在治疗过敏性和炎性病症
公开(公告)号：EP1841780B1
公开(公告)日：2011-07-27
申请号：EP06704092.3
申请日：2006-01-09
申请人： GLAXO GROUP LIMITED
发明人： BIGGADIKE, Keith, GlaxoSmithKline , NEEDHAM, Deborah, GlaxoSmithKline
IPC分类号： C07J41/00 , C07J3/00 , A61P5/44 , A61P37/00 , A61K31/56
CPC分类号： C07J3/005 , C07J41/0094
摘要： The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydrogen, a methyl group, which may be in either the α or β configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; represents a single or a double bond; and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

5. 发明公开

EP2295408A1 Matrix metalloproteinase inhibitors 审中-公开
标题翻译：基质金属蛋白酶
公开(公告)号：EP2295408A1
公开(公告)日：2011-03-16
申请号：EP10176905.7
申请日：2004-09-10
申请人： GLAXO GROUP LIMITED
发明人： Gaines, Simon , Holmes, Ian Peter , Martin, Stephen Lewis , Watson, Stephen Paul
IPC分类号： C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00
CPC分类号： C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要： Compounds of Formula (I):

Wherein: A represents bond, C 1-6 alkyl or CH=CH-C 1-4 alkyl;
B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ),
N(SO 2 R 14 )(COR 15 ) or NR 14 R 15 ;
D represents bond, or C 1-6 alkyl;
E represents substituted aryl or substituted or unsubstituted heteroaryl;
Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring;
X represents O, S, SO, SO 2 , CO, CNR 5 , CNOR 5 , CNNR 5 R 6 , NR 11 or CR 7 R 8 ;
Y represents CR 5 OR 11 , CR 5 SR 11 , NOR 5 , CR 5 NR 6 R 11 , SO, SO 2 , CO, CNR 5 , CNOR 5 or CS;
R 1 and R 1' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl;
R 2 represents CO 2 R 12 , CH 2 OR 12 or CONR 12 R 13 , CONR 12 OR 13 , NR 12 COR 13 , SR 12 , PO(OH) 2 ,
PONHR 12 or SONHR 12 ;
R 3 represents H, C 1-6 alkyl or C 1-4 alkylaryl;
R 4 represents optionally substituted aryl or heteroaryl;
Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 5 , OCR 5 R 6 , CR 9 R 10 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group;
R 5 and R 6 each independently represent H, C 1-6 alkyl or C 1-4 alkylaryl;
R 7 and R 8 each independently represent H, halo, C 1-6 alkyl or C 1-4 alkylaryl;
R 9 and R 10 each independently represents H, C 1-6 alkyl optionally substituted by halo, cyano,
OR 11 or NR 6 R 11 , C 1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR 6 R 11 , OR 11 or, together with the N to which they are attached, R 9 and R 10 form a heterocyclic group:
R 11 represents H, C 1-6 alkyl, C 1-4 alkylaryl or COR 5 ;
R 12 and R 13 each independently represent H, C 1-3 alkyl, C 1-3 alkylaryl or C 1-3 alkylheteroaryl or, together with the functionality to which they are attached, R 12 and R 13 form a heterocyclic group:
R 14 and R 15 each independently represent H, C 1-6 alkyl, C 1-4 alkylaryl or C 1-4 alkylheteroaryl or together with the functionality to which they are attached R 14 and R 15 form a heterocyclic or fused heterocyclic group: and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.

6. 发明公开

EP2012797A2 NOVEL FORMULATIONS 审中-公开
标题翻译：新型制剂
公开(公告)号：EP2012797A2
公开(公告)日：2009-01-14
申请号：EP07758963.8
申请日：2007-03-21
申请人： GLAXO GROUP LIMITED , 3M Innovative Properties Company
发明人： CAPECCHI, John , STEFELY, James , RILEY, Trevor
IPC分类号： A61K31/58 , A61L2/23
CPC分类号： A61K9/008 , A61K31/58 , A61K47/34
摘要： The present invention relates to novel pharmaceutical aerosol formulations, processes for their preparation, their use in therapy, metered dose inhalers containing said formulations and the use of biocompatible polymers in reducing the variability in the content uniformity and/or in providing enhanced fine particle fraction (FPF) in said formulations.

7. 发明授权

EP1383786B1 ANTI-INFLAMMATORY 17.BETA.-CARBOTHIOATE ESTER DERIVATIVES OF ANDROSTANE WITH A CYCLIC ESTER GROUP IN POSITION 17.ALPHA 有权
标题翻译： WITH A 17.ALPHA.环酯基雄甾抗炎7.BETA.，硫代羧酸酯衍生物
公开(公告)号：EP1383786B1
公开(公告)日：2008-10-15
申请号：EP02722463.3
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED
发明人： BIGGADIKE, Keith , JONES, Paul , PAYNE, Jeremy John
IPC分类号： C07J31/00 , A61K31/56 , A61P5/44 , A61P11/06 , A61P17/00
CPC分类号： C07J31/006
摘要： There are provided compound of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents C3-8 cycloalkyl or C3-8 cycloalkenyl either of which may optionally be substituted by one or more groups selected from oxo, methyl, methylene and halogen; R3 represents hydrogen, methyl (which may be in either the alpha or beta configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and (AA) represents a single or a double bond; and solvates thereof, processes for preparing them and their use in therapy.

8. 发明授权

EP1539796B1 ANTI-INFLAMMATORY OR ANTI-ALLERGIC ANDROSTANE COMPLEXES 有权
标题翻译：抗炎药或 ANTI过敏性ANDROSTANKOMPLEXE
公开(公告)号：EP1539796B1
公开(公告)日：2007-02-14
申请号：EP03765110.6
申请日：2003-07-21
申请人： GLAXO GROUP LIMITED
发明人： BIGGADIKE, Keith, GlaxoSmithKline , CHETINA, Olga, University Of Durham , COOTE, Steven John, GlaxoSmithKline , CRAIG, Andrew Simon, GlaxoSmithKline , JACEWICZ, Victor Witold, GlaxoSmithKline , MILLAN, Michael John, GlaxoSmithKline , SEAGER, John Frederick, GlaxoSmithKline , THEOPHILUS, Andrew Lewis, GlaxoSmithKline
IPC分类号： C07J31/00 , A61K31/58 , A61P29/00
CPC分类号： A61K45/06 , A61K31/58 , C07J17/00
摘要： There is provided a crystalline chemical complex comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in that the crystalline complex is of space group P212121 having unit cell dimensions of about 7.6 ± 0.6 Å, 12.7 ± 0.7 Å, and 33 ± 3 Å when determined at 120K.

9. 发明公开

EP1713775A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：EP1713775A2
公开(公告)日：2006-10-25
申请号：EP05712794.6
申请日：2005-01-28
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： DREWRY, David, Harold, c/o GlaxoSmithKline , JUNG, David, Kendall, c/o GlaxoSmithKline , LINN, James, Andrew, c/o GlaxoSmithKline , HUNTER, Robert, Neil, III, c/o GlaxoSmithKline , LEE, Dennis, c/o GlaxoSmithKline , STAVENGER, Robert, A, c/o GlaxoSmithKline , SEHON, Clark, c/o GlaxoSmithKline
IPC分类号： C07D213/56 , C07D231/12 , C07D239/42 , A61K31/415 , A61K31/416 , A61K31/4418 , A61K31/505
CPC分类号： C07D213/56 , C07D231/12 , C07D231/56 , C07D239/26 , C07D239/42 , C07D403/04
摘要： There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: Formula (I).
摘要翻译：提供式（I）的化合物及其盐，溶剂合物和生理学功能衍生物：式（I）。

10. 发明公开

EP1641766A2 NOVEL CHEMICAL COMPOUNDS 审中-公开
标题翻译：新化学化合物
公开(公告)号：EP1641766A2
公开(公告)日：2006-04-05
申请号：EP04777657.0
申请日：2004-07-07
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： SATO, Hideyuki , TAKADA, Mio , WASHIO, Yoshiaki
IPC分类号： C07D239/70 , A61K31/517
CPC分类号： C07D471/04
摘要： This invention relates to newly identified inhibitors of kinases for treating various disorders.
摘要翻译：本发明涉及用于治疗各种病症的新鉴定的激酶抑制剂。

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