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1. 发明申请

WO2002062372A3 TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM 审中-公开
公开(公告)号：WO2002062372A3
公开(公告)日：2002-08-15
申请号：PCT/EP2002/001182
申请日：2002-02-05
申请人： NEUROTELL AG , RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy formula (I), wherein X represents OH, (C 1-5 )alkoxy, NH 2 , NH-C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C 1-5 ) alkoxy group, a (C 1-5 ) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R 2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R 3 and R 4 independently represent H, OH, (C 1-5 ) alkyl, or (C 1-5 )alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 )alkoxy; R 5 represents H, OH, (C 1-5 )alkyl or (C 1-5 )alkoxy; and wherein R 0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.

2. 发明申请

WO2002062830A1 TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经病变性疾病的三肽衍生物
公开(公告)号：WO2002062830A1
公开(公告)日：2002-08-15
申请号：PCT/EP2002/001181
申请日：2002-02-05
申请人： TELL PHARM AG , RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： C07K5/08
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C 1-5 )alkoxy, NH 2 , NH-C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C 1-5 ) alkoxy group, a (C 1-5 ) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R 2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R 3 and R 4 independently represent H, OH, (C 1-5 )alkyl, or (C 1-5 )alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 )alkoxy; R 5 represents H, OH, (C 1-5 ) alkyl or (C 1-5 )alkoxy; and wherein R 0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及特异性三肽用于治疗神经变性疾病的用途。三肽衍生物满足下式（I）：其中X表示OH，（C 1-5）烷氧基，NH 2，NH-C 1-5 - 烷基，N（C 1-5烷基）2; R1是衍生自任何氨基酸Phe，Tyr，Trp，Pro的残基，其各自可以任选被（C 1-5）烷氧基，（C 1-5）烷基或卤素原子取代，和 Ala，Val，Leu或Ile; R2是衍生自任何氨基酸Gly，Ala，Ile，Val，Ser，Thr，His，Arg，Lys，Pro，Glu，Gln，pGlu，Asp，Leu和Asn的残基; R3和R4独立地表示H，OH，（C1-5）烷基或（C1-5）烷氧基，条件是R3和R4不同时为OH或（C1-5）烷氧基; R5表示H，OH，（C1-5）烷基或（C1-5）烷氧基; 并且其中R 0优选表示肉桂酰残基; 或其药学上可接受的盐。

3. 发明申请

WO2002062828A2 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：三萜类化合物和三萜类衍生物用于治疗神经退行性疾病
公开(公告)号：WO2002062828A2
公开(公告)日：2002-08-15
申请号：PCT/EP2002/001180
申请日：2002-02-05
申请人： TELL PHARM AG , RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： C07K5/00
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/08 , C07K5/0802
摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C 1-5 ) alkoxy, NH 2 , NH-C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one ormore (C 1-5 ) alkoxy groups, (C 1-5 ) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R 2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y 1 and Y 2 independently from each other represent H or (C 1-5 ) alkyl; R 3 and R 4 independently from each other represent H, OH, (C 1-5 ) alkyl or (C 1-5 ) alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 ) alkoxy; and R 5 represents H, OH, (C 1-5 ) alkyl or (C 1-5 ) alkoxy; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及特定三肽用于治疗神经变性疾病的用途，并涉及包含三肽的药物组合物。该三肽衍生物满足下式（I）：其中X代表OH，（C 1-5）烷氧基，NH 2，NH-C 1-5 N（C 1 -C 5烷基）2;以及N（C 1 -C 5）烷基。 R 1是来源于氨基酸Phe，Tyr，Trp，Pro中的一个的残基，其各自可任选被一个或多个（C 1-5）烷氧基（C 1 -C 5）烷基或卤素原子，以及Ala，Val，Leu或Ile; R 2是来自氨基酸Gly，Ala，Ile，Val，Ser，Thr，Leu和Pro之一的残基; Y 1和Y 2彼此独立地表示H或（C 1-5）烷基; R 3和R 4彼此独立地表示H，OH，（C 1-5）烷基或（C 1-4亚烷基） 5）烷氧基，条件是R 3和R 4不都是OH或（C 1-5）烷氧基; 且R5N表示H，OH，（C1-5）烷基或（C1-5）烷氧基; 或其药学上可接受的盐。

4. 发明申请

WO2002062373A2 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM 审中-公开
标题翻译：三萜类化合物和三萜类衍生物治疗神经系统疾病的研究
公开(公告)号：WO2002062373A2
公开(公告)日：2002-08-15
申请号：PCT/EP2002/001183
申请日：2002-02-05
申请人： TELL PHARM AG , RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C 1 - 5 ) alkoxy, NH 2 , NH-C 1 - 5 -alkyl, N(C 1 - 5 alkyl) 2 ; R 1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C 1 - 5 ) alkoxy groups, (C 1 - 5 ) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R 2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y1 and Y2 independently from each other represent H or (C 1 - 5 ) alkyl; R 3 and R 4 independently from each other represent H, OH, (C 1 - 5 ) alkyl or (C 1 - 5 ) alkoxy, provided that R 3 and R 4 are not both OH or (C 1 - 5 ) alkoxy; and R 5 represents H, OH, (C1-5) alkyl or (C 1 - 5 ) alkoxy; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及特定三肽用于治疗局部缺血性，创伤性或毒性来源的病后疾病的用途。所述三肽衍生物满足下式（I）：（其中X代表OH，（C 1 - ）5 - 烷氧基，NH _{NH-C 1 -C 5 - 烷基，N（C 1 -C 5） - 烷基，烷基）<子> 2 ; R 1是来源于氨基酸Phe，Tyr，Trp，Pro之一的残基，其各自可以任选被一个或多个（C 1〜（C 1〜5）烷基或卤素原子，以及Ala，Val，Leu或Ile; R 2是来自氨基酸Gly，Ala，Ile，Val，Ser，Thr和Pro之一的残基; Y 1和Y 2彼此独立地代表H或（C 1 - 5 - ）烷基; R 3和R 4彼此独立地代表H，OH，（C 1〜5）烷基或（C 1 -C 5）烷氧基，条件是R 3和R 4不都是OH或（C 1 - ） - 烷氧基; 和R 5表示H，OH，（C 1-5）烷基或（C 1 -C 5）烷氧基; 或其药学上可接受的盐。}

5. 发明申请

WO2002062372A2 TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM 审中-公开
标题翻译：治疗神经系统疾病的三肽衍生物
公开(公告)号：WO2002062372A2
公开(公告)日：2002-08-15
申请号：PCT/EP2002/001182
申请日：2002-02-05
申请人： TELL PHARM AG , RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy formula (I), wherein X represents OH, (C 1-5 )alkoxy, NH 2 , NH-C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C 1-5 ) alkoxy group, a (C 1-5 ) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R 2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R 3 and R 4 independently represent H, OH, (C¿1 -C 5?) alkyl, or (C 1-5 )alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 )alkoxy; R 5 represents H, OH, (C 1-5 )alkyl or (C 1-5 )alkoxy; and wherein R 0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及特异性三肽用于治疗缺血性，创伤性或毒性起源性的postsional疾病的用途。三肽衍生物满足式（I），其中X表示OH，（C 1-5）烷氧基，NH 2，NH-C 1-5 - 烷基，N（C 1-5烷基）2; R1是衍生自任何氨基酸Phe，Tyr，Trp，Pro的残基，其各自可以任选被（C 1-5）烷氧基，（C 1-5）烷基或卤素原子取代，和 Ala，Val，Leu或Ile; R2是衍生自任何氨基酸Gly，Ala，Ile，Val，Ser，Thr，His，Arg，Lys，Pro，Glu，Gln，pGlu，Asp，Leu和Asn的残基; R3和R4独立地表示H，OH，（C1-C5）烷基或（C1-5）烷氧基，条件是R3和R4不同时为OH或（C1-5）烷氧基; R5表示H，OH，（C1-5）烷基或（C1-5）烷氧基; 并且其中R 0优选表示肉桂酰残基; 或其药学上可接受的盐。

6. 发明授权

EP1363656B1 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM 有权
标题翻译：三肽及其衍生物对postlesional神经疾病的治疗
公开(公告)号：EP1363656B1
公开(公告)日：2004-12-22
申请号：EP02719767.2
申请日：2002-02-05
申请人： Neurotell AG
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C1-5) alkoxy, NH2, NH-C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

7. 发明公开

EP1358204A1 TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：三肽用于治疗神经变性疾病
公开(公告)号：EP1358204A1
公开(公告)日：2003-11-05
申请号：EP02716727.9
申请日：2002-02-05
申请人： Neurotell AG
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： C07K5/08 , A61K38/06 , A61P25/28
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5)alkoxy, NH2, NH-C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C1-5) alkoxy group, a (C1-5) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R3 and R4 independently represent H, OH, (C1-5)alkyl, or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; R5 represents H, OH, (C1-5) alkyl or (C1-5)alkoxy; and wherein R0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.

8. 发明公开

EP1363656A2 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM 有权
标题翻译：三肽及其衍生物对postlesional神经疾病的治疗
公开(公告)号：EP1363656A2
公开(公告)日：2003-11-26
申请号：EP02719767.2
申请日：2002-02-05
申请人： Neurotell AG
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： A61K38/06
摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C1-5) alkoxy, NH2, NH-C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

9. 发明公开

EP1359934A2 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权
标题翻译： TRIPEPIDE和TRIPEPDID-DERIVTE用于治疗神经退行性疾病
公开(公告)号：EP1359934A2
公开(公告)日：2003-11-12
申请号：EP02711833.0
申请日：2002-02-05
申请人： Neurotell AG
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/08 , C07K5/0802
摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5) alkoxy, NH2, NH-C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one ormore (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

10. 发明授权

EP1359934B1 TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权
标题翻译： TRIPEPIDE和TRIPEPDID-DERIVTE用于治疗神经退行性疾病
公开(公告)号：EP1359934B1
公开(公告)日：2006-11-08
申请号：EP02711833.0
申请日：2002-02-05
申请人： Neurotell AG
发明人： RAPIN, Jean , WITZMANN, Hans, Klaus , GRUMEL, Jean-Marie , GONELLA, Jacques
IPC分类号： A61K38/06
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/08 , C07K5/0802
摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5) alkoxy, NH2, NH-C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one ormore (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

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