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1.发明授权CARBOXYLIC ACIDS AND ACYLSULFONAMIDES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 有权碳氢酸和酰基磺酰胺，包含它们的筹备工作及治理方法
公开(公告)号：EP1216241B1
公开(公告)日：2005-12-07
申请号：EP00960258.2
申请日：2000-09-13
发明人： LACOMBE, Patrick , LABELLE, Marc , RUEL, Rejean
IPC分类号： C07D409/04 , A61K31/44 , A61P19/00 , A61P29/00
CPC分类号： C07D409/04
摘要： This invention encompasses the novel compounds of formula (A), which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases.
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2.发明公开IRREVERSIBLE CASPASE-3 INHIBITORS AS ACTIVE SITE PROBES 审中-公开不可逆的CASPASE-3-INHIBITOREN ALS SONDENFÜRAKTIVE ZENTREN
公开(公告)号：EP1594819A1
公开(公告)日：2005-11-16
申请号：EP04708291.2
申请日：2004-02-05
发明人： COLUCCI, John , GIROUX, Andre , HAN, Yongxin , METHOT, Nathalie , NICHOLSON, Donald, W. , ROY, Sophie , VAILLANCOURT, John, Paul , TAWA, Paul
IPC分类号： C07B59/00 , C07K5/00 , C12Q1/00 , G01N33/534 , C07C237/22
CPC分类号： C07D495/04 , C07B59/001 , C07C237/22 , C07C2601/08 , C07C2601/14 , C07K5/1021
摘要： The present invention encompasses a compound of Formula (I) useful as caspase active site probes. These probes can be used to determine whether a caspase has been activated, in cells or in tissues of animal models of various pathologies. Furthermore, through competition based assays, these caspase active site probes can be used to calculate the percentage of occupancy of active caspases by other, unlabeled inhibitors.
摘要翻译： 本发明包括可用作半胱天冬酶活性位点探针的式（I）化合物。 这些探针可以用于确定胱天蛋白酶是否已经在各种病态的动物模型的细胞或组织中被激活。 此外，通过基于竞争的测定，这些胱天蛋白酶活性位点探针可用于计算其他未标记的抑制剂占有活性半胱天冬酶的百分比。
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3.发明公开OXAZOLIDIN-2-ONE AND THIAZOLIDIN-2-ONE DERIVATIVES FOR USE AS EP4 RECEPTOR AGONISTS IN THE TREATMENT OF GLAUCOMA 审中-公开恶唑烷-2-酮和噻唑烷-2-酮衍生物FOR USE AS EP4受体激动剂治疗青光眼
公开(公告)号：EP1545517A1
公开(公告)日：2005-06-29
申请号：EP03790594.0
申请日：2003-08-25
IPC分类号： A61K31/422 , A61K31/427 , A61P27/06 , C07D277/14 , C07D417/06 , C07D417/14 , C07D263/24 , C07D413/06 , C07D413/14
CPC分类号： C07D263/20 , C07D263/24 , C07D277/14 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/10
摘要： This invention relates to compounds of formula (I) which are potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient.
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公开(公告)号：EP1130110A3
公开(公告)日：2005-02-23
申请号：EP01201784.4
申请日：1993-12-17
发明人： Cromlish, Wanda A. , Kennedy, Brian P. , O'Neill, Gary , Vickers, Philip J. , Wong, Elizabeth , Mancini, Joseph A.
CPC分类号： C12N9/0083 , C12Q1/48 , C12Q1/61 , C12Y114/99001 , G01N33/5005 , G01N33/88 , G01N2333/90241
摘要： An assay for determining the cyclooxygenase-2 activity of a sample comprising the steps of: (a) adding(1) a human osteosarcoma cell preparation,(2) a sample, said sample comprising a putative cyclooxygenase-2 inhibitor, and(3) arachidonic acid; and (b) determining the amount of prostaglandin E2 produced in step (a).
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5.发明公开FLUORO SUBSTITUTED CYCLOALKANOINDOLES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 有权氟取代CYCLOALKANINDOLE及其作为前列腺素D2受体拮抗剂
公开(公告)号：EP1470107A2
公开(公告)日：2004-10-27
申请号：EP03700740.8
申请日：2003-01-22
IPC分类号： C07D209/80 , A61K31/403 , A61P43/00 , C07D209/88
CPC分类号： C07D209/80 , C07D209/88
摘要： Fluoro substituted cycloalkanoindole derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein n is 0 or 1; m is 1, 2 or 3; R1 is H, C1-C3 alkyl, halogenated C1-C3 alkyl or cyclopropyl; R2 is 4-chlorophenyl or 2,4,6-trichlorophenyl are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
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公开(公告)号：EP1453503A2
公开(公告)日：2004-09-08
申请号：EP02784629.4
申请日：2002-11-27
发明人： OGIDIGBEN, Miller, J. , YOUNG, Robert, N. , BILLOT, Xavier , METTERS, Kathleen, M. , SLIPETZ, Deborah, M.
IPC分类号： A61K31/4015
CPC分类号： C07D403/12
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
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公开(公告)号：EP1012142B1
公开(公告)日：2004-08-11
申请号：EP98942432.0
申请日：1998-09-11
IPC分类号： C07D213/64 , A61K31/44 , C07D213/70 , C07D213/61
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70
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公开(公告)号：EP1441701A1
公开(公告)日：2004-08-04
申请号：EP02801836.4
申请日：2002-10-22
发明人： DOWN, Brian
IPC分类号： A61K9/16
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/1676
摘要： The present invention relates to oral granules of montelukast sodium.
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公开(公告)号：EP0839034B1
公开(公告)日：2004-06-02
申请号：EP96924537.2
申请日：1996-07-15
发明人： KARGMAN, Stacia , EVANS, Jilly , SIMON, Thomas, J.
CPC分类号： A61K31/603 , A61K31/00 , A61K31/12 , A61K31/18 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/34 , A61K31/365 , A61K31/405 , A61K31/407 , A61K31/54 , A61K31/5415 , A61K31/616
摘要： This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
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10.发明公开A METHOD TO INCREASE EXPRESSION OF PGD2 RECEPTORS AND ASSAYS FOR IDENTIFYING MODULATORS OF PROSTAGLANDIN D2 RECEPTORS 审中-公开受体PDG2方法受体PDG2的表达增加，调节剂的筛选
公开(公告)号：EP1412744A2
公开(公告)日：2004-04-28
申请号：EP02750700.3
申请日：2002-07-18
IPC分类号： G01N33/50
CPC分类号： G01N33/502 , G01N33/5008 , G01N33/5041 , G01N33/5044 , G01N33/88
摘要： The present invention provides cell lines expressing endogenous PGD2-specific receptors, methods for increasing expression of the receptors and assays utilizing the hereindisclosed cell lines for identifying modulators of the PGD2-specific receptors. Increasing expression of PGD2-specific receptors is achieved by treating the disclosed cell lines with an agent that induces differentiation.
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