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1. 发明公开

EP1966226A2 AZACYTOSINE DERIVATIVES USEFUL AS ANTIVIRAL AGENTS 有权
标题翻译：作为抗病毒药剂的合适AZACYTOSINDERIVATE
公开(公告)号：EP1966226A2
公开(公告)日：2008-09-10
申请号：EP06828083.3
申请日：2006-12-08
申请人： K.U.Leuven Research & Development , INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY OF THE ACADEMY OF SCIENCES OF THE CZECH REPUBLIC
发明人： HOLY, Antonin , KRECMEROVÁ, Marcela , PISKALA, Alois , ANDREI, Graciela , SNOECK, Robert , DE CLERCQ, Erik , NEYTS, Johan , NAESENS, Lieve
IPC分类号： C07F9/38 , C07F9/6574 , A61K31/675 , A61P31/20
CPC分类号： C07F9/65181 , C07F9/657181
摘要： The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

2. 发明授权

EP1966226B1 AZACYTOSINE DERIVATIVES USEFUL AS ANTIVIRAL AGENTS 有权
标题翻译：作为抗病毒药剂的合适AZACYTOSINDERIVATE
公开(公告)号：EP1966226B1
公开(公告)日：2010-11-10
申请号：EP06828083.3
申请日：2006-12-08
申请人： K.U.Leuven Research & Development , INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY OF THE ACADEMY OF SCIENCES OF THE CZECH REPUBLIC
发明人： HOLY, Antonin , KRECMEROVÁ, Marcela , PISKALA, Alois , ANDREI, Graciela , SNOECK, Robert , DE CLERCQ, Erik , NEYTS, Johan , NAESENS, Lieve
IPC分类号： C07F9/38 , C07F9/6574 , A61K31/675 , A61P31/20
CPC分类号： C07F9/65181 , C07F9/657181
摘要： The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

3. 发明公开

EP2980095A1 PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION 审中-公开
标题翻译： PHOSPONATNUKLEOSIDE作为活性成分的药物组合物为他们的生产病毒感染和中间产品的处理
公开(公告)号：EP2980095A1
公开(公告)日：2016-02-03
申请号：EP15167795.2
申请日：2005-03-04
申请人： K.U.Leuven Research & Development
发明人： HERDEWIJN, Piet , PANNECOUQUE, Christophe , WU, Tongfei , DE CLERCQ, Erik
IPC分类号： C07H19/00 , C07H19/06 , C07H19/16 , A61K31/706
CPC分类号： C07H19/20 , C07F7/0812 , C07H1/00 , C07H15/04 , C07H17/02 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.
摘要翻译：本发明涉及新的核苷膦，更具体地涉及新颖phosponalkoxy substituiertem核苷。本发明进一步涉及一种具有HIV（人类免疫缺陷病毒）复制抑制性质，并化合物具有相对于其它病毒的抗病毒活性的化合物。因此本发明涉及一种用于制备所有测试的化合物和药物组合物，包含它们的方法。本发明还涉及作为药物和在制备用于从HIV感染的受试者的疾病的药物有用的制造，以及用于治疗其它病毒，逆转录病毒或慢病毒感染的和动物的治疗的用途。所述的化合物从FIV，病毒，逆转录病毒或慢感染的痛苦。

4. 发明授权

EP1521754B1 VIRAL INHIBITORS 有权转让
标题翻译：病毒抑制剂
公开(公告)号：EP1521754B1
公开(公告)日：2011-08-31
申请号：EP03762361.8
申请日：2003-07-03
申请人： K.U.Leuven Research & Development , GILEAD SCIENCES, INC. , Pürstinger, Gerhard
发明人： NEYTS, Johan , PÜRSTINGER, Gerhard , DE CLERCQ, Erik
IPC分类号： C07D471/04 , A61K31/437 , A61P31/12
CPC分类号： C07D471/04
摘要： The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

5. 发明公开

EP1546331A2 INTEGRASE COFACTOR 有权
标题翻译：整合相关蛋白
公开(公告)号：EP1546331A2
公开(公告)日：2005-06-29
申请号：EP03757548.7
申请日：2003-09-26
申请人： K.U.Leuven Research & Development
发明人： DEBYSER, Zeger , CHEREPANOV, Peter , DE CLERCQ, Erik
IPC分类号： C12N15/11 , C07K14/16 , C07K14/47 , C12N15/62 , C12Q1/68 , G01N33/50 , A61K38/16 , A61K38/17 , A61K48/00
CPC分类号： C07K14/47 , A61K38/00 , A61K48/00 , C07K14/005 , C07K14/475 , C12N5/0641 , C12N9/22 , C12N2740/16222
摘要： In a study of HIV-1 integrase (IN) complexes derived from nuclei of human cells stably expressing the viral protein from a synthetic gene it was demonstrated that in the nuclear extracts IN exists as part of a large distinct complex with apparent Stokes radius of 61Å, which dissociates upon dilution yielding a core molecule of 41 Å. The IN complexes were isolated from cells expressing FLAG-tagged IN. By present invention it was demonstrated that the 41Å core is tetramer of IN, whereas 61 Å molecules are composed of IN tetramers associated with a cellular protein with an apparent molecular weight of 76 kDa. This integrase interacting protein (Inip76) was found to be identical to LEDGF/DFS70/p75 a protein implicated in regulation of gene expression and cellular stress-response. HIV-1 IN and Inip76 co-localized in the nuclei of human cells stably expressing IN. Furthermore, it has been demonstrated by present invention that recombinant Inip76 strongly promoted strand-transfer activity of HIV-1 IN in vitro. Our findings reveal that the minimal IN molecule in human cells is a tetramer and clearly demonstrates that Inip76 is plays a role in retroviral integration. Therefore the present invention provides integrase interacting proteins and more particularly cofactors which promote strand transfer activity of viral integrase, more particularly HIV integrase, and methods and uses relating thereto. The present invention relates to a cellular protein that associates with integrase ( integrase interacting protein-Inip), to molecules interacting with Inip and their use as an antiviral. The present invention also relates to antibodies, RNA interference, antigen therapy, gene silencing or antisense inhibition of said integrase interacting protein. The novel integrase interaction protein is a target for HIV replication prevention or inhibition.

6. 发明授权

EP1546331B1 INTEGRASE COFACTOR 有权
标题翻译：整合相关蛋白
公开(公告)号：EP1546331B1
公开(公告)日：2012-08-29
申请号：EP03757548.7
申请日：2003-09-26
申请人： K.U.Leuven Research & Development
发明人： DEBYSER, Zeger , CHEREPANOV, Peter , DE CLERCQ, Erik
IPC分类号： C12N15/11 , C07K14/16 , C07K14/47 , C12N15/62 , C12Q1/68 , G01N33/50 , A61K38/16 , A61K38/17 , A61K48/00
CPC分类号： C07K14/47 , A61K38/00 , A61K48/00 , C07K14/005 , C07K14/475 , C12N5/0641 , C12N9/22 , C12N2740/16222

7. 发明公开

EP1720890A2 PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION 有权
标题翻译：作为活性成分的药物组合物用于治疗病毒感染SUITABLE PHOSPONATNUKLEOSIDE和中间产品用于其生产治疗
公开(公告)号：EP1720890A2
公开(公告)日：2006-11-15
申请号：EP05714381.0
申请日：2005-03-04
申请人： K.U.Leuven Research & Development
发明人： HERDEWIJN, Piet , PANNECOUQUE, Christophe , WU, Tongfei , DE CLERCQ, Erik
IPC分类号： C07H19/00
CPC分类号： C07H19/20 , C07F7/0812 , C07H1/00 , C07H15/04 , C07H17/02 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.

8. 发明授权

EP1546331B2 INTEGRASE COFACTOR 有权
标题翻译：整合相关蛋白
公开(公告)号：EP1546331B2
公开(公告)日：2016-01-13
申请号：EP03757548.7
申请日：2003-09-26
申请人： K.U.Leuven Research & Development
发明人： DEBYSER, Zeger , CHEREPANOV, Peter , DE CLERCQ, Erik
IPC分类号： C12N5/078
CPC分类号： C07K14/47 , A61K38/00 , A61K48/00 , C07K14/005 , C07K14/475 , C12N5/0641 , C12N9/22 , C12N2740/16222

9. 发明授权

EP1720890B1 PHOSPONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION 有权
标题翻译：作为活性成分的药物组合物用于治疗病毒感染SUITABLE PHOSPONATNUKLEOSIDE和中间产品用于其生产治疗
公开(公告)号：EP1720890B1
公开(公告)日：2015-05-20
申请号：EP05714381.0
申请日：2005-03-04
申请人： K.U.Leuven Research & Development
发明人： HERDEWIJN, Piet , PANNECOUQUE, Christophe , WU, Tongfei , DE CLERCQ, Erik
IPC分类号： C07H19/00
CPC分类号： C07H19/20 , C07F7/0812 , C07H1/00 , C07H15/04 , C07H17/02 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/16

10. 发明公开

EP1521754A2 VIRAL INHIBITORS 有权转让
标题翻译：病毒抑制剂
公开(公告)号：EP1521754A2
公开(公告)日：2005-04-13
申请号：EP03762361.8
申请日：2003-07-03
申请人： K.U.Leuven Research & Development , GILEAD SCIENCES, INC. , Pürstinger, Gerhard
发明人： NEYTS, Johan , PÜRSTINGER, Gerhard , DE CLERCQ, Erik
IPC分类号： C07D471/04 , A61K31/437 , A61P31/12
CPC分类号： C07D471/04
摘要： The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

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