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1. 发明公开

EP2398483A1 OXYNTOMODULIN ANALOGS 有权转让
标题翻译：泌酸调节素类似物
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.

2. 发明授权

EP2041159B1 MACROCYCLIC COMPOUNDS AS ANTIVIRAL AGENTS 有权转让
标题翻译：万家乐环状化合物作为抗病毒剂
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
申请人： Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
发明人： CRESCENZI, Benedetta , DONGHI, Monica , FERRARA, Marco , GARDELLI, Cristina , HARPER, Steven , KOCH, Uwe , ROWLEY, Michael , SUMMA, Vincenzo
IPC分类号： C07K5/08 , A61K38/06 , A61P31/00
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.

3. 发明授权

EP1765398B1 HUMAN ANTIBODIES INTERACTING WITH HIV GP41 有权
标题翻译：艾滋病毒GP41相互作用有关的人类抗体
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.

4. 发明公开

EP2314320A2 Method for shielding functional sites or epitopes on proteins 审中-公开
标题翻译： 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
申请人： Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
发明人： Bianchi, Elisabetta , Pessi, Antonello
IPC分类号： A61K47/48 , C07K14/16
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。

5. 发明授权

EP1704167B1 A METHOD TO MAKE A PEPTIDE-CARRIER CONJUGATE WITH A HIGH IMMUNOGENICITY 有权
标题翻译：用于生产肽载体结合体与高免疫原性
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
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： BIANCHI, Elisabetta , FINOTTO, Marco , INGALLINELLA, Paolo , PESSI, Antonello
IPC分类号： C07K19/00 , C07K14/16 , C07K14/11 , A61K39/12 , G01N33/68
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.

6. 发明授权

EP1444523B1 SCREENING FOR HEPATITIS C VIRUS ENTRY INHIBITORS 有权
标题翻译：筛选丙型肝炎病毒抑制剂入侵
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
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： CORTESE, Riccardo, c/o IRBM , SCARSELLI, Elisa, c/o IRBM , VITELLI, Alessandra, c/o IRBM
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.

7. 发明授权

EP1578748B1 TETRAHYDRO-4H-PYRIDO[1,2-A]PYRIMIDINES AND RELATED COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS 有权
标题翻译：四氢-4H-吡啶并[1,2-A]嘧啶和相关化合物的AS HIV整合缝边
公开(公告)号：EP1578748B1
公开(公告)日：2010-09-15
申请号：EP03768014.7
申请日：2003-12-18
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： CRESCENZI, Benedetta, IRBM , KINZEL, Olaf, IRBM , MURAGLIA, Ester, IRBM , ORVIETO, Federica, IRBM , PESCATORE, Giovanna, IRBM , ROWLEY, Michael, IRBM , SUMMA, Vincenzo, IRBM
IPC分类号： C07D471/04 , A61K31/519 , A61P31/18 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

8. 发明授权

EP1758857B1 INDOLE DERIVATIVES AS ANTIVIRAL AGENTS 有权
标题翻译：吲哚衍生物ALS杀病毒
公开(公告)号：EP1758857B1
公开(公告)日：2010-08-18
申请号：EP05811114.7
申请日：2005-06-08
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： COLARUSSO, Stefania, c/o IRBM , CONTE, Immacolata, c/o IRBM , HABERMANN, Joerg, c/o IRBM , NARJES, Frank, c/o IRBM , PONZI, Simona, c/o IRBM
IPC分类号： C07D209/42 , C07D413/12 , C07D403/12 , C07D401/04 , C07D413/04 , A61K31/4045 , A61P31/12
CPC分类号： C07D209/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.

9. 发明公开

EP2178902A1 MACROCYCLIC COMPOUNDS AS ANTIVIRAL AGENTS 有权转让
标题翻译：大环化合物的杀病毒ALS
公开(公告)号：EP2178902A1
公开(公告)日：2010-04-28
申请号：EP08776220.9
申请日：2008-07-17
申请人： Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. , Merck Sharp & Dohme Corp.
发明人： LIVERTON, Nigel , SUMMA, Vincenzo , MCCAULEY, John , HARPER, Steven , BUTCHER, John , DI FILIPPO, Marcello , DI FRANCESCO, Maria Emilia , FERRARA, Marco , ROMANO, Joseph J. , RUDD, Michael
IPC分类号： C07K5/08 , C07K5/12 , A61K38/00 , A61K31/00
CPC分类号： C07K5/0812 , C07K5/0808
摘要： A class of macrocyclic compounds offormula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W,n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use ofsuch macrocyclic compounds for treating or preventing HCV infection. Formula (I):

10. 发明公开

EP2124555A2 NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 失效转让
标题翻译： NUKLEOSIDARYLPHOSPHORAMIDATE FOR RNA依赖性RNA病毒感染的治疗
公开(公告)号：EP2124555A2
公开(公告)日：2009-12-02
申请号：EP07868112.9
申请日：2007-12-28
申请人： Merck & Co., Inc. , Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A.
发明人： NARJES, Frank , GARDELLI, Cristina , DONGHI, Monica , ATTENNI, Barbara , DURETTE, Philippe, L.
IPC分类号： A01N43/04 , A61K31/70 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/048
CPC分类号： C07H19/04 , C07H19/048 , C07H19/10 , C07H19/20
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention. (I)

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