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公开(公告)号：EP2780026A2
公开(公告)日：2014-09-24
申请号：EP12850713.4
申请日：2012-11-09
申请人： Merck Sharp & Dohme Corp. , Merck Canada Inc. , Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.
发明人： RUDD, Michael, T. , MCCAULEY, John , LIVERTON, Nigel , GRISE-BARD, Christiane , BROUCHU, Marie-Christine , CHARRON, Sylvie , AULAKH, Virender , BACHAND, Benoit , BEAULIEU, Patrick , ZAGHDANE, Helmi , HAN, Yongxin , FERRARA, Marco , HARPER, Steven , SUMMA, Vincenzo , CHACKALAMANNIL, Samuel , VENKATRAMAN, Srikanth , SHAH, Unmesh , VELAZQUEZ, Francisco
IPC分类号： A61K38/12
CPC分类号： C07K5/08 , A61K31/4745 , A61K31/5377 , A61K31/675 , A61K31/7056 , A61K38/005 , A61K38/06 , A61K38/12 , A61K38/21 , C07K5/0804 , C07K5/0808 , C07K5/0812 , C07K5/0821 , A61K2300/00
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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公开(公告)号：EP2550011A1
公开(公告)日：2013-01-30
申请号：EP11709969.7
申请日：2011-03-25
发明人： MONACI, Paolo , CARFI, Andrea
CPC分类号： A61K38/482 , A61K39/0005 , A61K2039/53 , C12N9/6408
摘要： The present invention relates to pharmaceutical compositions comprising PCSK9 DNA or PCSK9 proteins or PCSK9 peptides and CpG adjuvant; this composition is used to lower cholesterol levels specifically LDL cholesterol levels.
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3.发明授权NUCLEOSIDE CYCLIC PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 有权循环核苷氨基磷酸酯FOR RNA-依赖性RNA病毒感染的治疗
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公开(公告)号：EP2398483A1
公开(公告)日：2011-12-28
申请号：EP09840594.7
申请日：2009-12-18
申请人： Merck Sharp & Dohme Corp. , Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. , Indiana University Research&Technology Corporation
发明人： CARRINGTON, Paul, E. , EIERMANN, George, J. , MARSH, Donald, J. , METZGER, Joseph. M. , POCAI, Alessandro , SINHA ROY, Ranabir , BIANCHI, Elisabetta , INGALLINELLA, Paolo , PESSI, Antonello , SANTOPRETE, Alessia , CAPITO, Elena , DIMARCHI, Richard , WARD, Brian
IPC分类号： A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , C07K14/575
摘要： Peptide analogs of oxyntomodulin (OXM, glucagon-37), which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to act as a dual GLP-1/glucagon receptor (GCGR) agonist, are described. The peptide analogs are useful for treatment of metabolic disorders such as diabetes and obesity.
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公开(公告)号：EP2041159B1
公开(公告)日：2011-09-28
申请号：EP07733767.3
申请日：2007-06-21
发明人： CRESCENZI, Benedetta , DONGHI, Monica , FERRARA, Marco , GARDELLI, Cristina , HARPER, Steven , KOCH, Uwe , ROWLEY, Michael , SUMMA, Vincenzo
CPC分类号： C07K5/0827 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R1, R2, R3, R4, R5, Ra, M, Z and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical co mposit ions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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公开(公告)号：EP1765398B1
公开(公告)日：2011-07-13
申请号：EP05754872.9
申请日：2005-05-31
申请人： Merck Sharp & Dohme Corp. , WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH , Cambridge Antibody Technology LTD , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： SHIVER, John W. , MILLER, Michael D. , GELEZIUNAS, Romas , HAZUDA, Daria J. , KIM, Peter S. , ROOT, Michael J. , ECKERT, Debra M. , LENNARD, Simon N. , BIANCHI, Elisabetta
IPC分类号： A61K39/395 , C07K16/10 , A61P31/18
CPC分类号： G01N33/56988 , C07K16/1063 , C07K2317/21 , C07K2317/622 , C07K2317/76 , G01N2500/00
摘要： Human scFvs are disclosed which interact with a conformational epitope along the pre-hairpin, N-helix coiled coil structure within the heptad repeat 1 (HR1) region of gp41 of HIV. These antibodies, as well as IgG conversions, are shown to neutralize diverse HIV isolates. Isolated nucleic acid molecules are also disclosed which encode relevant portions of these antibodies, as well as the purified forms of the expressed antibodies or relevant antibody fragments, such as VH and VL chains. The antibody compositions disclosed within this specification may provide for a therapeutic treatment against HIV infection by reducing viral load levels within an infected individual, thus prolonging the asymptomatic phase of HIV infection. These antibodies will also be useful in assays to identify HIV antiviral compounds as well as allowing for the identification of candidate HIV vaccines, such as HIV peptide vaccines.
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7.发明公开Combinations containing amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors 有权聚合酶（ADP-核糖） - 聚合酶（PARP） - 聚合酶
公开(公告)号：EP2336120A1
公开(公告)日：2011-06-22
申请号：EP11157369.7
申请日：2008-01-08
IPC分类号： C07D401/10 , A61K31/4439 , A61P35/00 , A61P29/00
CPC分类号： C07D401/10 , A61K31/4439
摘要： The present invention relates to combinations of compounds of formula I:
and other anti-cancer agents which are useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage and skin senescence and UV-induced skin damage.摘要翻译： 本发明涉及式I化合物与其它可用于治疗癌症，炎性疾病，再灌注损伤，缺血性疾病，中风，肾衰竭，心血管疾病，心血管疾病以外的血管疾病的抗癌剂的组合 ，糖尿病，神经变性疾病，逆转录病毒感染，视网膜损伤和皮肤衰老以及紫外线诱发的皮肤损伤。
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8.发明公开Method for shielding functional sites or epitopes on proteins 审中-公开Verfahren zur Abschirmung von funktionalen Stellen oder Epitopen von Proteinen
公开(公告)号：EP2314320A2
公开(公告)日：2011-04-27
申请号：EP10183132.9
申请日：2006-03-31
CPC分类号： C07K14/005 , A61K39/00 , A61K47/60 , C12N2740/16122
摘要： Methods of site-specifically shielding one or more binding sites within a polypeptide are disclosed, comprising attaching at least one small molecular weight, water-soluble polymer to said polypeptide such that the binding site is masked by said polymer. The shielding of a binding site ( e.g ., epitope) as per the disclosed methods acts to either eliminate or substantially reduce the biological response induced by the interaction between said binding site and its cognate receptor, helping to refocus the biological response toward unmasked portions of the polypeptide. Pharmaceutical products generated as per the methods described herein ( e.g ., polymer-modified antigens and vaccine compositions comprising them), as well as the use thereof, induce a specific immune response against unmasked portions of the polypeptides when directly introduced into living vertebrate tissue, preferably a mammalian host such as a human or a non-human mammal of commercial or domestic veterinary importance, generating selective immunoprotection in said mammal.
摘要翻译： 公开了特异性屏蔽多肽内的一个或多个结合位点的方法，包括将至少一种小分子量的水溶性聚合物连接到所述多肽上，使得结合位点被所述聚合物掩蔽。 根据所公开的方法，结合位点（例如，表位）的屏蔽用于消除或显着降低由所述结合位点与其同源受体之间的相互作用诱导的生物反应，有助于将生物反应重新聚焦到未被掩蔽的部分 多肽。 根据本文所述的方法（例如，聚合物修饰的抗原和包含它们的疫苗组合物）产生的药物产品及其用途在直接引入活的脊椎动物组织时诱导针对多肽的未掩蔽部分的特异性免疫应答， 优选哺乳动物宿主，例如商业或家庭兽医重要的人或非人哺乳动物，在所述哺乳动物中产生选择性免疫保护。
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公开(公告)号：EP1704167B1
公开(公告)日：2011-01-12
申请号：EP04820430.9
申请日：2004-12-10
CPC分类号： C07K14/005 , C12N2740/16122 , C12N2760/16122
摘要： The present invention provides a method for making a peptide-carrier conjugate. The method comprises modifying a first peptide to produce a second peptide so that the pI of the second peptide is in a favorable range or closer to the range than the pI of the first peptide, and conjugating a plurality of the second peptide to OMPC to obtain a peptide-carrier conjugate. The peptide load, or the solubility of the conjugate, or both of them are increased by the modification.
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公开(公告)号：EP1444523B1
公开(公告)日：2010-12-15
申请号：EP02802643.3
申请日：2002-11-01
IPC分类号： G01N33/576
CPC分类号： G01N33/5767 , G01N2333/18 , G01N2500/02
摘要： The present invention features methods of screening for compounds that inhibit HCV binding to a cell, methods of inhibiting HCV entry into a cell, and methods of actively or prophylactically treating against an HCV infection. The different methods are based on the identification of the scavenger receptor class B type I as a target site for HCV E2 binding to a cell.
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