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1. 发明授权

US3953415A Process for the preparation of biologically active polypeptides containing aspartyl group 失效
标题翻译：制备含有天冬氨酰基的生物活性多肽的方法
公开(公告)号：US3953415A
公开(公告)日：1976-04-27
申请号：US360198
申请日：1973-05-14
申请人： Lajos Kisfaludy , Miklos Low , Istvan Schon , Tamas Szirtes , Maria Sz. Sarkozi , Sandor Bajusz , Andrae Turan , Rosa Beks , Attila Juhasz , Laszlo Graf , Kalman Medzihradszky , Laszlo Szporny
发明人： Lajos Kisfaludy , Miklos Low , Istvan Schon , Tamas Szirtes , Maria Sz. Sarkozi , Sandor Bajusz , Andrae Turan , Rosa Beks , Attila Juhasz , Laszlo Graf , Kalman Medzihradszky , Laszlo Szporny
IPC分类号： A61K38/00 , C07C67/00 , C07C231/00 , C07C231/12 , C07C271/22 , C07K1/06 , C07K1/08 , C07K7/08 , C07K14/575 , C07K14/695 , C07C103/52 , C07G7/00
CPC分类号： C07C271/22 , C07K1/066 , C07K1/088 , C07K14/695 , A61K38/00
摘要： The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.
摘要翻译：本发明涉及使用活性酯技术制备含有天冬氨酰基，特别是天冬氨酰 - 甘氨酸部分的生物活性多肽。

2. 发明授权

US5760235A Anticoagulant peptide derivatives and pharmaceutical compositions containing the same as well as a process for preparation thereof 失效
标题翻译：抗凝血肽衍生物和含有其的药物组合物及其制备方法
公开(公告)号：US5760235A
公开(公告)日：1998-06-02
申请号：US740009
申请日：1996-10-23
申请人： Sandor Bajusz , Daniel Bagdy , Eva Barabas , Andras Feher , Gabriella Szabo , Gyorgyne Szell , Belane Veghelyi , Gyula Horvath , Attila Juhasz , Janosne Lavich , Laszlone Mohai , Imre Moravcsik , Gaborne Szeker , Istvan Pallagi , Katalin Palne Aranyosi
发明人： Sandor Bajusz , Daniel Bagdy , Eva Barabas , Andras Feher , Gabriella Szabo , Gyorgyne Szell , Belane Veghelyi , Gyula Horvath , Attila Juhasz , Janosne Lavich , Laszlone Mohai , Imre Moravcsik , Gaborne Szeker , Istvan Pallagi , Katalin Palne Aranyosi
IPC分类号： A61K38/00 , A61P7/02 , C07D207/16 , C07D211/60 , C07D405/06 , C07K1/06 , C07K5/06 , C07K5/078 , A61K38/05
CPC分类号： C07D405/06 , C07D207/16 , C07D211/60
摘要： This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.
摘要翻译： PCT No.PCT / HU93 / 00013 Sec。 371日期1994年12月5日第 102（e）日期1994年12月5日PCT提交1993年3月4日PCT公布。出版物WO93 / 18060 PCT 日本公开专利文献1日本公开专利文献1日本公开专利文献1日本公开专利文献1：日本专利公开公报发明内容本发明涉及通式（I）A-Xaa-Arg-H的新型肽衍生物，其中A表示D-或L-异色满-1-羰基，D-或L-异色满-3 - 羰基，此外还有通式为D-或DL-A'-CH（OH）-CO的酰基，其中A'代表苯基，苄基，1-萘基，1-萘基甲基，2-萘基，2 - 萘基甲基，9-芴基，二苯甲基，环己基，环己基甲基，2-吡啶基，3-吡啶基或4-吡啶基，Xaa表示L-脯氨酰基或L-哌啶酸残基，Arg表示L-精氨酸残基，它们与有机或无机酸形成的酸加成盐和含有它们的药物组合物。此外，本发明涉及一种制备它们的方法。本发明的化合物具有有价值的治疗，特别是抗凝血剂的性质。

3. 发明授权

US06593300B1 (3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta 失效
标题翻译：（3R）-3-氨基-4-羧基丁醛衍生物抑制白细胞介素-1 /β的释放
公开(公告)号：US06593300B1
公开(公告)日：2003-07-15
申请号：US09423006
申请日：2000-02-07
申请人： Sandor Bajusz , Iren Veghelyi , Klara Nemeth , Eva Barabas , Attila Juhasz , Jozsef Lango , Emilia Lavich , Zsuzsanna Mohai , Imre Moravcsik , Zsuzsanna Taschler , Gabor Toth
发明人： Sandor Bajusz , Iren Veghelyi , Klara Nemeth , Eva Barabas , Attila Juhasz , Jozsef Lango , Emilia Lavich , Zsuzsanna Mohai , Imre Moravcsik , Zsuzsanna Taschler , Gabor Toth
IPC分类号： A61K3800
CPC分类号： C07K7/02 , A61K38/00 , C07K5/0202
摘要： The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n=0, an &agr;-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an &agr;-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an &agr;-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q2-Q4 represent an acyl group selected from the following &agr;-hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1&bgr; converting enzyme.
摘要翻译：本发明涉及通式（I）的新的（3R）-3-氨基-4-羧基丁醛衍生物，其中X代表C1-4烷氧基羰基，任意取代的苯基 - （C 1-2烷氧基） - 羰基， 4烷基羰基或任选取代的苯基 - （C 1-3烷基） - 羰基，n表示1或0，Y表示在n = 1的情况下，通式Y4-Y3-Y2-Y1的四肽，三肽通式Y3-Y2-Y1或通式Y2-Y1的二肽或通式Y1的氨基酸残基，或在n = 0的情况下，通式为Q4-Y3-Y2的α-羟基酰基三肽 -Y1，通式为Q3-Y2-Y1的α-羟酰基二肽或通式为Q2-Y1的α-羟基酰基 - 酰基残基; 其中Y 1 -Y 4表示选自以下L-或D-氨基酸的残基：丙氨酸，异亮氨酸，环己基 - 甘氨酸，苯丙氨酸，谷氨酰胺，组氨酸，异亮氨酸，亮氨酸，赖氨酸，甲硫氨酸，哌可酸，脯氨酸，酪氨酸和缬氨酸; 和Q 2 -Q 4表示选自以下R或S构型的α-羟基酸的酰基：2-环庚基-2-羟基 - 乙酸，2-环己基-2-羟基乙酸，3-环己基乳酸，3-苯基乳酸，2-羟基-3-甲基丁酸，2-羟基-3-甲基戊酸，扁桃酸或乳酸，以及与有机或无机碱形成的盐，以及含有它们的药物组合物。本发明通式（I）的化合物是白细胞介素-1β转换酶的有价值的抑制剂。

4. 发明授权

US06214969B1 Luteinizing hormone releasing hormone analogs with cytotoxic moiety 失效
标题翻译：具有细胞毒性部分的促黄体激素释放激素类似物
公开(公告)号：US06214969B1
公开(公告)日：2001-04-10
申请号：US08008186
申请日：1993-01-25
申请人： Tamas Janaky , Attila Juhasz , Sandor Bajusz , Andrew V. Schally
发明人： Tamas Janaky , Attila Juhasz , Sandor Bajusz , Andrew V. Schally
IPC分类号： C07K723
CPC分类号： C07K7/23 , A61K38/00 , Y10S530/81 , Y10S530/816 , Y10S930/11
摘要： The present invention deals with LHRH analogs which contain cytotoxic moieties, have influence on the release of gonadotropins from the pituitary in mammals (possess high agonistic or antagonistic activity) and have antineoplastic effect. The compounds of this invention are represented by Formula I: X-R1-R2-R3-Ser-R5-R6(Q)-Leu-Arg-Pro-R10-NH2, wherein R1 is pGlu or D-Nal(2), R2 is His or D-Phe(4Cl), R3 is Trp, D-Trp or D-Pal(3), R5 is Tyr or Arg, R6 is D-Lys or D-Orn, R10 is Gly or D-Ala, X is hydrogen or a lower alkanoyl group of 2-5 carbon atoms, Q is a cytotoxic moiety having the formula —Q4 or —A(Q3) or —B(Q1)2 or —B(AQ2)2, wherein A is —NH—(CH2)n—CO— or —OC—(CH2)n—CO— where n is 2-6, B is —NH—CH2—(CH2)m—CH(NH)—(CH2)n—CO— where m is 0 or 1, n is 0 or 1, the —CO moiety of A— and of B— being bonded to an amino group on R6, and in the group B(AQ2)2, the —CO moiety of A— and of B— being bonded to the episilon or delta amino group of R6 when R6 is Lys or Orn respectively, and in the group B(AQ2)2, the —CO moiety of A being bonded to an amino group on B, Q1 is D or L-Mel, cyclopropanealkanoyl, aziridine-2-carbonyl, epoxyalkyl or 1,4-naphthoquinone-5-oxy-carbonyl-ethyl, Q2 is Q1, 2-anthraquinonyl-methylenoxy or doxorubicinyl, Q3 is Q2, mitomicinyl, esperamycinyl or methotrexoyl, Q4 is Q1 or methotrexoyl and pharmaceutically acceptable salts thereof and methods of use pertaining these compounds.
摘要翻译：本发明涉及含有细胞毒素部分的LHRH类似物，对哺乳动物垂体中促性腺激素的释放具有影响（具有高激动作用或拮抗作用）并具有抗肿瘤作用。本发明的化合物由式I表示：X-R1-R2-R3-Ser-R5-R6（Q）-Leu-Arg-Pro-R10-NH2，其中R1是pGlu或D-Nal（2）， R2是His或D-Phe（4Cl），R3是Trp，D-Trp或D-Pal（3），R5是Tyr或Arg，R6是D-Lys或D-Orn，R10是Gly或D-Ala， X是氢或2-5个碳原子的低级烷酰基，Q是具有式-Q4或-A（Q3）或-B（Q1）2或-B（AQ2）2的细胞毒性部分，其中A是 - NH-（CH 2）n -CO-或-OC-（CH 2）n -CO-，其中n为2-6，B为-NH-CH 2 - （CH 2）m -CH（NH） - （CH 2）n -CO - 其中m为0或1，n为0或1，A和B的-CO部分键合到R6上的氨基上，B组（AQ2）2中的-CO部分 - 当R6分别为Lys或Orn时，B-与R6的游离或δ氨基结合，在B组（AQ2）2中，A的-CO部分键合到B上的氨基，Q1 是D或L-Mel，环丙烷基酰基，氮丙啶-2-羰基，环氧烷基或1,4-萘醌-5-氧羰基 - 乙基，Q2是Q1，2-蒽醌基 - 亚甲基氧基或多柔比星 Q 3是Q2，线粒体蛋白，埃曲肽或甲氨蝶呤，Q4是Q1或甲氨蝶呤及其药学上可接受的盐，以及这些化合物的使用方法。

5. 发明授权

US6121241A Anticoagulant peptide aldehyde derivatives 失效
标题翻译：抗凝血肽醛衍生物
公开(公告)号：US6121241A
公开(公告)日：2000-09-19
申请号：US11001
申请日：1999-04-02
申请人： Sandor Bajusz , Attila Juhasz , Eva Barabas , Andras Feher , Gabriella Szabo , Erzsebet Szell nee Hasenohrl , Iren Veghelyi nee Fauszt , Emilia Lavich nee Oszko , Eva Kaszas , Jozsef Lango , Imre Moravcsik , Agnes Szeker nee Peszeky , Zsuzsanna Taschler nee Pasztor , Gabor Toth , Zsuzsanna Mohai nee Nagy , Anna Maria Szalkay nee Hollosi , Klara Makk nee Ocskay
发明人： Sandor Bajusz , Attila Juhasz , Eva Barabas , Andras Feher , Gabriella Szabo , Erzsebet Szell nee Hasenohrl , Iren Veghelyi nee Fauszt , Emilia Lavich nee Oszko , Eva Kaszas , Jozsef Lango , Imre Moravcsik , Agnes Szeker nee Peszeky , Zsuzsanna Taschler nee Pasztor , Gabor Toth , Zsuzsanna Mohai nee Nagy , Anna Maria Szalkay nee Hollosi , Klara Makk nee Ocskay
IPC分类号： C07D207/16 , A61K38/05 , C07K5/00
CPC分类号： C07D207/16 , Y10S514/822
摘要： This invention relates to peptide aldehyde derivatives of formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represent a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents an L-prolyl residue and Arg represents an L-arginyl residue, their acid-additon salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) of the invention have therapeutic, particularly anticoagulant, antiplatelet and antithrombotic properties.
摘要翻译： PCT No.PCT / HU97 / 00027 Sec。一九九九年四月二日 102（e）1999年4月2日PCT 1997年6月5日PCT公布。第WO97 / 46523号公报日期1997年12月11日本发明涉及式（I）的肽醛衍生物：D-Xaa-Pro-Arg-H，其中Xaa表示2-环庚基-2-羟基乙酰基或2-环戊基-2-羟基乙酰基，Pro 代表L-脯氨酰残基，Arg表示L-精氨酰残基，它们与有机或无机酸形成的酸加成盐和含有它们的药物组合物。本发明式（I）的化合物具有治疗性，特别是抗凝血，抗血小板和抗血栓形成的特性。

6. 发明申请

US20090287811A1 Configuration of network's nodes in a telecommunication system 有权
标题翻译：网络节点在电信系统中的配置
公开(公告)号：US20090287811A1
公开(公告)日：2009-11-19
申请号：US11813726
申请日：2005-01-12
申请人： Attila Juhasz , Andras Veres
发明人： Attila Juhasz , Andras Veres
IPC分类号： G06N5/02 , G06F11/07 , G06F15/173
CPC分类号： H04L41/00
摘要： The idea of the present invention providing a solution for configuration problems of a node is based on the following components. A problem recognition system, which analyses performance indicators and identifies root causes, so that signatures can be attached to a found problems. Furthermore there is a signature based filtering system, which looks for transactions satisfying signatures. A customer identification system labels the transactions with the subscriber identify. A solution feedback system generates feedback event to the end node according to the rule of the signature.
摘要翻译：为节点的配置问题提供解决方案的本发明的思想基于以下组件。问题识别系统，分析绩效指标并确定根本原因，以便签署可以附加到发现的问题。此外，还有一个基于签名的过滤系统，可以查找满足签名的交易。客户识别系统将用户识别的交易标记出来。解决方案反馈系统根据签名规则向终端节点生成反馈事件。

7. 发明授权

US08086724B2 Configuration of network's nodes in a telecommunication system 有权
标题翻译：网络节点在电信系统中的配置
公开(公告)号：US08086724B2
公开(公告)日：2011-12-27
申请号：US11813726
申请日：2005-01-12
申请人： Attila Juhasz , Andras Veres
发明人： Attila Juhasz , Andras Veres
IPC分类号： G06N5/02 , G06F11/07 , G06F15/173
CPC分类号： H04L41/00
摘要： The idea of the present invention providing a solution for configuration problems of a node is based on the following components. A problem recognition system, which analyses performance indicators and identifies root causes, so that signatures can be attached to a found problems. Furthermore there is a signature based filtering system, which looks for transactions satisfying signatures. A customer identification system labels the transactions with the subscriber identify. A solution feedback system generates feedback event to the end node according to the rule of the signature.
摘要翻译：为节点的配置问题提供解决方案的本发明的思想基于以下组件。问题识别系统，分析绩效指标并确定根本原因，以便签署可以附加到发现的问题。此外，还有一个基于签名的过滤系统，可以查找满足签名的交易。客户识别系统将用户识别的交易标记出来。解决方案反馈系统根据签名规则向终端节点生成反馈事件。

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