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1. 发明申请

US20110293520A1 NEW DRUG FOR INHIBITING AGGREGATION OF PROTEINS INVOLVED IN DISEASES LINKED TO PROTEIN AGGREGATION AND/OR NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于抑制与蛋白质聚集和/或神经干细胞病变相关的疾病相关蛋白聚集的新药
公开(公告)号：US20110293520A1
公开(公告)日：2011-12-01
申请号：US12996833
申请日：2009-06-09
申请人： Armin Giese , Uwe Bertsch , Hans Kretzschmar , Mathias Habeck , Thomas Hirschberger , Paul Tavan , Christian Griesinger , Andrei Leonov , Sergey Ryazanov , Petra Weber , Markus Geissen , Martin H. Groschup , Jens Wagner
发明人： Armin Giese , Uwe Bertsch , Hans Kretzschmar , Mathias Habeck , Thomas Hirschberger , Paul Tavan , Christian Griesinger , Andrei Leonov , Sergey Ryazanov , Petra Weber , Markus Geissen , Martin H. Groschup , Jens Wagner
IPC分类号： A61K51/04 , C07D261/08 , C07D231/12 , C07D233/64 , C07D271/06 , A61K31/4155 , A61K31/42 , A61K31/415 , A61K31/4164 , A61K31/4245 , A61K49/00 , A61P25/16 , A61P25/00 , A61P25/28 , G01N33/566 , C07D405/10
CPC分类号： C07D231/12 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/42 , A61K31/4245 , C07D207/333 , C07D231/06 , C07D233/64 , C07D261/08 , C07D271/06 , C07D405/04 , C07D413/04 , G01N33/6896 , G01N2800/2828
摘要： The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)═, —N(R4)—, —N═, —N+(R5)═, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).
摘要翻译：本发明涉及由式（E）表示的化合物。本发明还涉及用于治疗或预防与蛋白质聚集和/或神经变性疾病相关的疾病的由式（E）表示的化合物。此外，本发明涉及包含本发明化合物以及试剂盒的药物和诊断组合物。此外，本发明涉及一种成像聚集蛋白沉积物的方法。还公开了用于制备本发明的可检测标记的化合物的试剂盒。式（E）其中X，Y和L分别独立地选自-C（R 1）（R 2） - ， - C（R 3）=，-N（R 4） - ， - N =，-N +（R 5） -O-和-S-; M和Z独立地选自式（I）和式（II）。

2. 发明申请

US20110296539A1 Mutant Alpha-Synuclein, and Methods Using Same 有权
标题翻译：突变型α-突触核蛋白，和使用相同的方法
公开(公告)号：US20110296539A1
公开(公告)日：2011-12-01
申请号：US13057680
申请日：2009-08-07
申请人： Markus Zweckstetter , Pinar Karpinar , Christian Griesinger
发明人： Markus Zweckstetter , Pinar Karpinar , Christian Griesinger
IPC分类号： G01N33/00 , C12N15/79 , C12N1/19 , A01K67/027 , C12Q1/02 , C07K14/435 , A01K67/033 , C12N15/12 , C12N5/10
CPC分类号： A01K67/0275 , A01K67/0336 , A01K67/0339 , A01K2227/105 , A01K2227/106 , A01K2227/703 , A01K2227/706 , A01K2267/03 , C07K14/47 , C12N15/102
摘要： The present invention relates to a mutant human alpha-synuclein with increased toxicity compared to wild-type alpha-synuclein, or a homologue thereof, wherein the mutant alpha-synuclein or homologue thereof comprises at least one amino acid substitution selected from the group consisting of a substitution at the alanine at position 56 (A56), at the alanine at position 76 (A76), at the methionine at position 127 (M127) and/or at the valine at position 118 (V118), as defined in the claims. Further, the invention relates to a polynucleotide encoding the mutant alpha-synuclein or homologue thereof, or an expression vector comprising said polynucleotide, a cell comprising the polynucleotide or expression vector, as defined in the claims. Also, a non-human animal comprising the cell of the invention is provided, as defined in the claims. Finally, the invention provides methods for identifying a substance that prevents or reduces toxicity of alpha-synuclein, as defined in the claims.
摘要翻译：本发明涉及与野生型α-突触核蛋白或其同源物相比具有增加的毒性的突变型人α-突触核蛋白，其中所述突变型α-突触核蛋白或其同源物包含至少一种选自以下的氨基酸取代：如在权利要求中定义的在位置56（A56）的丙氨酸，位置76（A76）的丙氨酸，位置127的甲硫氨酸（M127）和/或缬氨酸位置118（V118）处的取代。此外，本发明涉及编码突变型α-突触核蛋白或其同系物的多核苷酸，或包含所述多核苷酸的表达载体，包含如权利要求中所定义的多核苷酸或表达载体的细胞。而且，如权利要求中所定义的，提供包含本发明的细胞的非人动物。最后，本发明提供了鉴定如权利要求中所定义的预防或减少α-突触核蛋白毒性的物质的方法。

3. 发明授权

US10308671B2 Water-soluble derivatives of 3,5-diphenyl-diazole compounds 有权
公开(公告)号：US10308671B2
公开(公告)日：2019-06-04
申请号：US16062258
申请日：2016-12-14
申请人： Max-Planck-Gesellschaft zur Förderung , Armin Giese , Felix Schmidt
发明人： Armin Giese , Felix Schmidt , Christian Griesinger , Andrei Leonov , Sergey Ryazanov
IPC分类号： C07F9/11 , A61P25/28 , A61P25/16
摘要： The present invention is concerned with derivatives of 3,5-diphenyl-diazole compounds, which are effective therapeutic agents for use in treating diseases linked to protein aggregation and/or neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and Transmissible spongiform encephalopathies (TSEs) such as Creutzfeldt-Jakob disease (CJD). The therapeutic effect is caused by the inhibition of the protein aggregation in the affected tissue, such as the brain. 3,5-Diphenyl-diazole derivatives have been shown to be effective in inhibiting aggregation of proteins but are also characterized by their poor solubility in aqueous solutions. The prodrugs of the invention are modified 3,5-diphenyl-diazole derivatives, which are characterized by their improved solubility in aqueous solutions, and by their increased bioavailability.

4. 发明授权

US5939527A Tetrapeptides as antitumor agents 失效
标题翻译：四肽作为抗肿瘤剂
公开(公告)号：US5939527A
公开(公告)日：1999-08-17
申请号：US688335
申请日：1996-07-30
申请人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky
发明人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K5/00
CPC分类号： C07K5/0205 , A61K38/00
摘要： The present invention provides anti-tumor peptides of Formula I,A--B--NR.sup.3 --CHD--CH(OCH.sub.3)--CH.sub.2 CO--E--K (I),and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N,N-dimethyl-2-ethylphenylglycyl, or an amino acid residue of the formula R.sup.1 R.sup.2 N--CHX--CO, wherein R.sup.1 is a-methyl group or an ethyl group, R.sup.2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R.sup.3 is a hydrogen atom or a methyl group. D is a normal or branched C.sub.2 -C.sub.5 -alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group.An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.
摘要翻译：本发明提供式I，A-B-NR3-CHD-CH（OCH3）-CH2CO-E-K（I）的抗肿瘤肽及其酸式盐。 A是选自N-甲基-D-脯氨酰基，N-甲基-D-正戊基和N，N-二甲基-2-乙基苯基甘氨酰或式R 1 R 2 N-CHX-的氨基酸残基的氨基酸残基， CO，其中R1是α-甲基或乙基，R2是氢原子，甲基或乙基，X是烷基。 B是选自缬氨酰基，异亮氨酰基，亮氨酰基和2-叔丁基甘氨酰基的氨基酸残基。 R3是氢原子或甲基。 D是正链或支链C 2 -C 5 - 烷基。 E是选自脯氨酰基，同环戊基，5-甲基脯氨酰基和苯丙氨酰基的氨基酸残基，或E是衍生自包含吡咯烷基的氨基酸的残基。 K是烷氧基或氨基。本发明的另一个实施方案是用于治疗哺乳动物（例如人）的恶性肿瘤的方法，包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式I化合物或化合物。

5. 发明授权

US5741892A Pentapeptides as antitumor agents 失效
标题翻译：五肽作为抗肿瘤剂
公开(公告)号：US5741892A
公开(公告)日：1998-04-21
申请号：US688334
申请日：1996-07-30
申请人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky , George R. Pettit
发明人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky , George R. Pettit
IPC分类号： A61K38/00 , A61P1/00 , A61P11/00 , A61P15/00 , A61P35/00 , C07K7/02 , C07K7/00
CPC分类号： C07K7/02 , A61K38/00
摘要： The present invention provides anti-tumor peptides of Formula I, A-B-N (CH.sub.3)-CHD-CH(OCH.sub.3)-CH.sub.2 CO-Pro-Pro-K (I), and the acid salts thereof. A is an amino acid residue of the formula (CH.sub.3).sub.2 N--CHX--CO, wherein X is a normal or branched alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. D is a normal or branched C.sub.3 -C.sub.4 -alkyl group. K is a t-butoxy group or a substituted amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.
摘要翻译：本发明提供式I，A-B-N（CH 3）-CHD-CH（OCH 3）-CH 2 CO-Pro-Pro-K（I）的抗肿瘤肽及其酸式盐。 A是式（CH 3）2 N-CHX-CO的氨基酸残基，其中X是正或支链烷基。 B是选自缬氨酰基，异亮氨酰基，亮氨酰基和2-叔丁基甘氨酰基的氨基酸残基。 D是正链或支链C 3 -C 4 - 烷基。 K为叔丁氧基或取代氨基。本发明的另一个实施方案是用于治疗哺乳动物（例如人）的恶性肿瘤的方法，包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式I化合物或化合物。

6. 发明授权

US08809505B2 Mutant alpha-synuclein, and methods using same 有权
标题翻译：突变型α-突触核蛋白，以及使用其的方法
公开(公告)号：US08809505B2
公开(公告)日：2014-08-19
申请号：US13057680
申请日：2009-08-07
申请人： Markus Zweckstetter , Pinar Karpinar , Christian Griesinger
发明人： Markus Zweckstetter , Pinar Karpinar , Christian Griesinger
IPC分类号： C12N15/12 , A61K38/00
CPC分类号： A01K67/0275 , A01K67/0336 , A01K67/0339 , A01K2227/105 , A01K2227/106 , A01K2227/703 , A01K2227/706 , A01K2267/03 , C07K14/47 , C12N15/102
摘要： The present invention relates to a mutant human alpha-synuclein with increased toxicity compared to wild-type alpha-synuclein, or a homologue thereof, wherein the mutant alpha-synuclein or homologue thereof comprises at least one amino acid substitution selected from the group consisting of a substitution at the alanine at position 56 (A56), at the alanine at position 76 (A76), at the methionine at position 127 (M127) and/or at the valine at position 118 (V118), as defined in the claims. Further, the invention relates to a polynucleotide encoding the mutant alpha-synuclein or homologue thereof, or an expression vector comprising said polynucleotide, a cell comprising the polynucleotide or expression vector, as defined in the claims. Also, a non-human animal comprising the cell of the invention is provided, as defined in the claims. Finally, the invention provides methods for identifying a substance that prevents or reduces toxicity of alpha-synuclein, as defined in the claims.
摘要翻译：本发明涉及与野生型α-突触核蛋白或其同源物相比具有增加的毒性的突变型人α-突触核蛋白，其中所述突变型α-突触核蛋白或其同源物包含至少一种选自以下的氨基酸取代：如在权利要求中定义的在位置56（A56）的丙氨酸，位置76（A76）的丙氨酸，位置127的甲硫氨酸（M127）和/或缬氨酸位置118（V118）处的取代。此外，本发明涉及编码突变型α-突触核蛋白或其同系物的多核苷酸，或包含所述多核苷酸的表达载体，包含如权利要求中所定义的多核苷酸或表达载体的细胞。而且，如权利要求中所定义的，提供包含本发明的细胞的非人动物。最后，本发明提供了鉴定如权利要求中所定义的预防或减少α-突触核蛋白毒性的物质的方法。

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