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1. 发明申请

WO2005030194A1 HCV INHIBITIING SULFONAMIDES 审中-公开
标题翻译： HCV抑制磺酰胺
公开(公告)号：WO2005030194A1
公开(公告)日：2005-04-07
申请号：PCT/EP2004/052388
申请日：2004-09-30
申请人： TIBOTEC PHARMACEUTICALS LTD. , SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
发明人： SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
IPC分类号： A61K31/18
CPC分类号： A61K45/06 , A61K31/18 , A61K31/421 , A61K31/426 , A61K2300/00
摘要： The present invention concerns sulfonamide derivatives having the general formula (I) and N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q 1 is -S- or -O-; R 1 is hydrogen, C 1-6 alkyl, hydroxy, amino, halogen, aminoC 1-4 alkyl and mono-or di(C 1-4 alkyl)amino; R 2 is hydrogen or C 1-6 alkyl; R 3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is hydrogen, C 1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C 1-4 alkyl)aminocarbonyl, C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 1-6 alkyl optionally substituted with one or more substituents each independently selected from aryl, Het 1 , Het 2 , C 3-7 cycloalkyl, C 1-4 alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C 1-4 alkyl)aminocarbonyl, aminosulfonyl, C 1-4 alkylS(=O) t , hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C 1-4 alkyl, aryl, arylC 1-4 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, Het 1 , Het 2 Het 1 C 1-4 alkyl and Het 2 C 1-4 alkyl; Q 2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.
摘要翻译：本发明涉及具有通式（I）和N-氧化物，盐，立体异构形式，外消旋混合物，前药和酯的磺酰胺衍生物，其中Q1是-S-或-O-; R 1是氢，C 1-6烷基，羟基，氨基，卤素，氨基C 1-4烷基和单或二（C 1-4烷基）氨基; R2是氢或C1-6烷基; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R4是氢，C1-4烷氧基羰基，羧基，任选的单取代或二取代的氨基羰基，单或二（C 1 -C 1-4烷基）氨基羰基，C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选被一个或多个取代基，各自独立地选自芳基，Het 1，Het 2，C 3-7环烷基，C 1-4烷氧基羰基，羧基，氨基羰基，一或二（C 1-4烷基）氨基羰基，氨基磺酰基， 4-烷基S（= O）t，羟基，氰基，卤素或氨基，其中取代基各自独立地选自C 1-4烷基，芳基，芳基C 1-4烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基， Het 1，Het 2 Het 1 C 1-4烷基和Het 2 C 1-4烷基; Q2是制备用于抑制HCV感染的哺乳动物的HCV活性的药物的式（III，IV，V，VI，VII）的基团。本发明还涉及所述磺酰胺在旨在治疗或对抗HCV和HIV感染综合症的药物组合物中的用途。此外，本发明涉及这种药物组合物的制备方法。本发明还涉及本发明磺酰胺与其它抗HCV剂和/或抗HIV剂的组合。

2. 发明申请

WO2007113337A1 A HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM 审中-公开
标题翻译：一个均衡的时间分辨率基于荧光的测试系统
公开(公告)号：WO2007113337A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053417
申请日：2007-04-06
申请人： TIBOTEC PHARMACEUTICALS LTD. , DAMS, Géry Karel Julia , VEREYCKEN, Inge , VAN ACKER, Koenraad Lodewijk August , GUSTIN, Emmanuel Marie Paul Ernest , VERSCHUEREN, Wim Gaston , OHAGEN, Asa Catrine
发明人： DAMS, Géry Karel Julia , VEREYCKEN, Inge , VAN ACKER, Koenraad Lodewijk August , GUSTIN, Emmanuel Marie Paul Ernest , VERSCHUEREN, Wim Gaston , OHAGEN, Asa Catrine
IPC分类号： G01N33/542 , G01N33/569
CPC分类号： G01N33/56988 , G01N33/542
摘要： The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six- helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.
摘要翻译：本发明涉及一种基于荧光共振能量转移的高通量测试系统来测量HIV gp41六螺旋束的形成。在第一个实施方案中，本发明涉及基于均匀时间分辨荧光的测试系统，其包含基本上由IQN36（SEQ ID NO：1）序列组成的第一螺旋多肽; 基本上由C34（SEQ ID NO：2）的序列组成的第二螺旋多肽，其中所述IQN36用发光荧光团标记，所述C34用紫外线可激发荧光团标记。

3. 发明申请

WO2008071723A1 A HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM FOR PARAMYXOVIRIDAE 审中-公开
标题翻译：基于荧光的荧光检测系统的均匀时间分辨
公开(公告)号：WO2008071723A1
公开(公告)日：2008-06-19
申请号：PCT/EP2007/063753
申请日：2007-12-12
申请人： TIBOTEC PHARMACEUTICALS LTD. , ROYMANS, Dirk André E. , VAN ACKER, Koenraad Lodewijk August , VEREYCKEN, Inge , DAMS, Géry Karel Julia
发明人： ROYMANS, Dirk André E. , VAN ACKER, Koenraad Lodewijk August , VEREYCKEN, Inge , DAMS, Géry Karel Julia
IPC分类号： G01N33/542 , G01N33/569 , C07K14/115
CPC分类号： G01N21/6428 , C07K14/005 , C12N2760/18522 , G01N21/6408 , G01N33/542 , G01N2021/6441 , G01N2333/135
摘要： The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the RSV F1 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN57 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C45 (SEQ ID NO: 2) wherein said IQN57 is labeled with a light emitting fluorophore and said C45 is labeled with an ultra-violet excitable fluorophore.
摘要翻译：本发明涉及一种基于荧光共振能量转移的高通量测试系统来测量RSV F1六螺旋束的形成。在第一实施方案中，本发明涉及基于均匀时间分辨荧光的测试系统，其包含基本上由IQN57（SEQ ID NO：1）序列组成的第一螺旋多肽; 基本上由C45（SEQ ID NO：2）的序列组成的第二螺旋多肽，其中所述IQN57用发光荧光团标记，所述C45用紫外线可激发的荧光团标记。

4. 发明公开

EP1670448A1 HCV INHIBITIING SULFONAMIDES 有权
标题翻译： HCV耐磺胺
公开(公告)号：EP1670448A1
公开(公告)日：2006-06-21
申请号：EP04766871.0
申请日：2004-09-30
申请人： Tibotec Pharmaceuticals Ltd.
发明人： SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
IPC分类号： A61K31/18 , A61K31/426 , A61K31/421 , A61P31/14
CPC分类号： A61K45/06 , A61K31/18 , A61K31/421 , A61K31/426 , A61K2300/00
摘要： The present invention concerns sulfonamide derivatives having the general formula (I) and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is -S- or -O-; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono-or di(C1-4 alkyl)amino; R2 is hydrogen or C1-6 alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4 alkyl, or arylC1-4 alkyl; R4 is hydrogen, C1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4 alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(=O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2 Het1C1-4alkyl and Het2C1-4 alkyl; Q2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.

5. 发明公开

EP2005177A1 A HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM 有权
标题翻译：均相时间分辨荧光基于测试方法
公开(公告)号：EP2005177A1
公开(公告)日：2008-12-24
申请号：EP07727885.1
申请日：2007-04-06
申请人： Tibotec Pharmaceuticals Ltd.
发明人： DAMS, Géry Karel Julia , VEREYCKEN, Inge , VAN ACKER, Koenraad Lodewijk August , GUSTIN, Emmanuel Marie Paul Ernest , VERSCHUEREN, Wim Gaston , OHAGEN, Asa Catrine
IPC分类号： G01N33/542 , G01N33/569
CPC分类号： G01N33/56988 , G01N33/542
摘要： The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six- helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.

6. 发明公开

EP2092335A1 A HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM FOR PARAMYXOVIRIDAE 有权转让
标题翻译：基于时间齐测试系统分辨荧光FOR副粘病毒
公开(公告)号：EP2092335A1
公开(公告)日：2009-08-26
申请号：EP07848070.4
申请日：2007-12-12
申请人： Tibotec Pharmaceuticals Ltd.
发明人： ROYMANS, Dirk André E. , VAN ACKER, Koenraad Lodewijk August , VEREYCKEN, Inge , DAMS, Géry Karel Julia
IPC分类号： G01N33/542 , G01N33/569 , C07K14/115
CPC分类号： G01N21/6428 , C07K14/005 , C12N2760/18522 , G01N21/6408 , G01N33/542 , G01N2021/6441 , G01N2333/135
摘要： The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the RSV F1 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN57 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C45 (SEQ ID NO: 2) wherein said IQN57 is labeled with a light emitting fluorophore and said C45 is labeled with an ultra-violet excitable fluorophore.

7. 发明授权

EP1670448B1 HCV INHIBITING SULFONAMIDES 有权
标题翻译： HCV-HEMMENDE磺酰胺
公开(公告)号：EP1670448B1
公开(公告)日：2007-11-21
申请号：EP04766871.0
申请日：2004-09-30
申请人： Tibotec Pharmaceuticals Ltd.
发明人： SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
IPC分类号： A61K31/18 , A61K31/426 , A61K31/421 , A61P31/14
CPC分类号： A61K45/06 , A61K31/18 , A61K31/421 , A61K31/426 , A61K2300/00
摘要： The present invention concerns sulfonamide derivatives having the general formula (I) and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is -S- or -O-; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono-or di(C1-4 alkyl)amino; R2 is hydrogen or C1-6 alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4 alkyl, or arylC1-4 alkyl; R4 is hydrogen, C1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het , Het , C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4 alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(=O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het , Het Het C1-4alkyl and Het C1-4 alkyl; Q2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.

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