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1. 发明授权

US06569834B1 Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides 失效
标题翻译：抗肿瘤四肽w-氨基烷基酰胺的阐释和合成
公开(公告)号：US06569834B1
公开(公告)日：2003-05-27
申请号：US07985697
申请日：1992-12-03
申请人： George R. Pettit , Jozsef Barkoczy
发明人： George R. Pettit , Jozsef Barkoczy
IPC分类号： A61K3800
CPC分类号： C07K7/06 , A61K38/07 , C07K5/101
摘要： Dolastatin 10, a linear pentapeptide, has shown potent antineoplastic activity profiles against various experimental cancer systems. The synthesis of structural modifications of dolastatin 10 having significant antineoplastic activity against human cancer cell lines has been accomplished; namely antineoplastic tetrapeptide w-amino alkyl amides related to dolastatin 10, which have been found to demonstrate effective antineoplastic activity against various human cancer cell lines. Members of this have demonstrated significant antineoplastic activity against human cancer cell lines. The human cancer cell lines against which the substances of the present invention have yielded the significant antineoplastic activity are: Ovarian OVCAR-3; Central Nervous System (“CNS”) SF295; Renal A498; Lung NCI460; Colon KM20L2 and Melanoma SK-MEL-3.
摘要翻译：线性五肽Dolastatin 10已经显示出针对各种实验性癌症系统的有效的抗肿瘤活性。已经完成了对人癌细胞系具有显着抗肿瘤活性的多拉司他汀10的结构修饰的合成; 即与多拉司他汀10相关的抗肿瘤四肽w-氨基烷基酰胺，已被发现证明对各种人类癌细胞系具有有效的抗肿瘤活性。其成员已经证明对人类癌细胞系具有显着的抗肿瘤活性。本发明的物质产生显着的抗肿瘤活性的人类癌细胞系是：卵巢OVCAR-3; 中枢神经系统（“CNS”）SF295; 肾A498; 肺NCI460; 结肠KM20L2和黑色素瘤SK-MEL-3。

2. 发明授权

US5635483A Tumor inhibiting tetrapeptide bearing modified phenethyl amides 失效
标题翻译：具有改性苯乙基酰胺的肿瘤抑制四肽
公开(公告)号：US5635483A
公开(公告)日：1997-06-03
申请号：US985827
申请日：1992-12-03
申请人： George R. Pettit , Jozsef Barkoczy
发明人： George R. Pettit , Jozsef Barkoczy
IPC分类号： A61K38/00 , A61P35/00 , A61P35/02 , C07K5/02 , C07K5/027 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/0205 , A61K38/00
摘要： New tetrapeptides bearing modified phenethyl amides are elucidated and syesized and found to exhibit tumor inhibiting effects when measured against the NCI screen for six major types of human cancer and against the murine P388 lymphocytic cell line. The new modified tetrapeptides phenethyl amides are 6(a-k).
摘要翻译：当对六种主要类型的人类癌症和针对小鼠P388淋巴细胞细胞系的NCI筛选进行测量时，阐明并合成具有改性的苯乙基酰胺的新四肽，显示出肿瘤抑制作用。新修饰的四肽苯乙酰胺为6（a-k）。

3. 发明授权

US6034065A Elucidation and synthesis of antineoplastic tetrapeptide phenethylamides of dolastatin 10 失效
标题翻译：多卡他汀10抗肿瘤四肽苯乙胺的阐释和合成
公开(公告)号：US6034065A
公开(公告)日：2000-03-07
申请号：US985831
申请日：1992-12-03
申请人： George R. Pettit , Jozsef Barkoczy
发明人： George R. Pettit , Jozsef Barkoczy
IPC分类号： A61K38/00 , A61P35/00 , C07K5/02 , C07K5/023
CPC分类号： C07K5/0205 , A61K38/00
摘要： Dolastatin 10, a linear pentapeptide, has shown potent antineoplastic activity profiles against various experimental cancer systems.The design and synthesis of structural modifications of dolastatin 10 having significant antineoplastic activity against human cancer cell lines has been accomplished. Members of this group have demonstrated significant antineoplastic activity against selected human cancer cell lines. Especially: Ovarian OVSCAR-3; Central Nervous System ("CNS") SF295; Renal A498; Lung NCI460; Colon KM20L2 and Melanoma SK-MEL-3.
摘要翻译：线性五肽Dolastatin 10已经显示出针对各种实验性癌症系统的有效的抗肿瘤活性。已经完成了对人癌细胞系具有显着抗肿瘤活性的多拉司他汀10的结构修饰的设计和合成。该组的成员已经证明对选定的人类癌细胞系具有显着的抗肿瘤活性。特别是：卵巢OVSCAR-3; 中枢神经系统（“CNS”）SF295; 肾A498; 肺NCI460; 结肠KM20L2和黑色素瘤SK-MEL-3。

4. 发明授权

US5410024A Human cancer inhibitory pentapeptide amides 失效
标题翻译：人类癌抑制五肽酰胺
公开(公告)号：US5410024A
公开(公告)日：1995-04-25
申请号：US6465
申请日：1993-01-21
申请人： George R. Pettit , Jozsef Barkoczy , Darko Kantoci
发明人： George R. Pettit , Jozsef Barkoczy , Darko Kantoci
IPC分类号： A61K38/00 , A61P35/00 , C07K1/00 , C07K1/113 , C07K5/02 , C07K5/06 , C07K7/00 , C07K7/06
CPC分类号： C07K5/0205 , A61K38/00 , Y02P20/55
摘要： The synthesis of useful peptides presents a promising approach to new theeutic agents. The Dolastatins, a series of linear and cyclic antineoplastic and/or cytostatic peptides isolated from Indian Ocean sea hare Dolabella auricularia represent excellent leads for synthetic modification.The extraordinary inhibition of cell growth shown by the pentapeptideamides against six major types of human cancer has been presented. The intermediates of these reaction also show anticancer activity against the murine P388 lymphocytic leukemia cell line.
摘要翻译：有用的肽的合成为新的治疗剂提供了有希望的方法。 Dolastatins，一系列线性和环状抗肿瘤和/或细胞生长抑制肽，分离自印度洋海洋，海豚耳朵，代表了合成改性的优秀引线。已经提出了五肽对六种主要类型的人类癌症表现出的细胞生长的非凡抑制作用。这些反应的中间体也显示对鼠P388淋巴细胞白血病细胞系的抗癌活性。

5. 发明授权

US07960375B2 8-chloro-2,3-benzodiazepine derivatives 失效
标题翻译： 8-氯-2,3-苯并二氮杂衍生物
公开(公告)号：US07960375B2
公开(公告)日：2011-06-14
申请号：US10567598
申请日：2004-07-29
申请人： Jozsef Barkoczy , Istvan Ling , Gyula Simig , Gabor Szenasi , Gabor Gigler , Szabolcs Kertesz , Gyula Szücs , Geza Szabo , Miklos Vegh , Laszlo Gabor Harsing
发明人： Jozsef Barkoczy , Istvan Ling , Gyula Simig , Gabor Szenasi , Gabor Gigler , Szabolcs Kertesz , Gyula Szücs , Geza Szabo , Miklos Vegh , Laszlo Gabor Harsing
IPC分类号： A61P9/10 , A61K31/55 , C07D243/02
CPC分类号： C07D243/02
摘要： The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R′, wherein R′ stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.
摘要翻译：本发明涉及通式（I）的新的8-氯-2,3-苯并二氮杂衍生物，其中R代表低级烷基或通式-NH-R'基团，其中R'代表低级烷基或低级环烷基）及其药学上可接受的酸加成盐。本发明还包括制备所述化合物的方法，含有它们的药物组合物和可用于制备新的8-氯-2,3-苯并二氮杂衍生物的新中间体。根据本发明的化合物具有AMPA /红藻氨酸受体抑制活性。

6. 发明申请

US20080153814A1 8-Chloro-2,3-Benzodiazepine Derivatives 失效
标题翻译： 8-氯-2,3-苯并二氮杂衍生物
公开(公告)号：US20080153814A1
公开(公告)日：2008-06-26
申请号：US10567598
申请日：2004-07-29
申请人： Jozsef Barkoczy , Istvan Ling , Gyula Simig , Gabor Szenasi , Gabor Gigler , Szabolcs Kertesz , Gyula Szucs , Geza Szabo , Miklos Vegh , Laszio Gabor Harsing
发明人： Jozsef Barkoczy , Istvan Ling , Gyula Simig , Gabor Szenasi , Gabor Gigler , Szabolcs Kertesz , Gyula Szucs , Geza Szabo , Miklos Vegh , Laszio Gabor Harsing
IPC分类号： A61K31/551 , C07D243/02 , A61P25/00
CPC分类号： C07D243/02
摘要： The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R′, wherein R′ stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.
摘要翻译：本发明涉及通式（I）的新的8-氯-2,3-苯并二氮杂衍生物，其中R代表低级烷基或通式-NH-R'基团，其中R'代表低级烷基或低级环烷基）及其药学上可接受的酸加成盐。本发明还包括制备所述化合物的方法，含有它们的药物组合物和可用于制备新的8-氯-2,3-苯并二氮杂衍生物的新中间体。根据本发明的化合物具有AMPA /红藻氨酸盐受体抑制活性。

7. 发明申请

US20050215560A1 Piperidinyl-alkylamino-pyridazinone derivatives, a process for the preparation thereof and pharmaceutical compositions containing said compounds 失效
标题翻译：哌啶基 - 烷基氨基 - 哒嗪酮衍生物，其制备方法和含有所述化合物的药物组合物
公开(公告)号：US20050215560A1
公开(公告)日：2005-09-29
申请号：US10508676
申请日：2002-12-28
申请人： Jozsef Barkoczy , Istvan Gacsalyi , Laszlo Harsing , Peter Kotay Nagy , Gyorgy Levay , Iva Schmidt
发明人： Jozsef Barkoczy , Istvan Gacsalyi , Laszlo Harsing , Peter Kotay Nagy , Gyorgy Levay , Iva Schmidt
IPC分类号： C07D401/12 , A61K31/501 , A61P25/22 , C07B61/00 , C07D401/06 , C07D43/02
CPC分类号： C07D401/06
摘要： The invention relates to new piperidinyl-alkylamino-pyridazinone derivatives of the general Formula (I) (wherein R is hydrogen or C1-4-alkyl; one of X and Y stands for hydrogen and the other represents a group of the general Formula (II) Hal stands for halogen; and n is 1 or 2) and pharmaceutically acceptable acid addition salts thereof a process for the preparation thereof and pharmaceutical compositions comprising said compounds. The compounds of the general Formula I exhibit anxiolytic effect and are useful in the treatment of anxiety.
摘要翻译：本发明涉及通式（I）的新的哌啶基 - 烷基氨基 - 哒嗪酮衍生物（其中R是氢或C 1-4 - 烷基; X和Y之一代表氢，另一个代表一般式（II）Hal代表卤素; n为1或2）及其药学上可接受的酸加成盐作为其制备方法和包含所述化合物的药物组合物。通式Ⅰ化合物具有抗焦虑作用，可用于治疗焦虑症。

8. 发明授权

US06646133B1 Process for the preparation of amorphous atorvastatin calcium 失效
标题翻译：制备无定形阿托伐他汀钙的方法
公开(公告)号：US06646133B1
公开(公告)日：2003-11-11
申请号：US10110874
申请日：2002-07-03
申请人： Zoltan Greff , Peter Kotay Nagy , Jozsef Barkoczy , Gyula Simig , Laszlo Balazs , Imre Doman , Zoltan Ratkai , Peter Seres , Zsuzsa Szent Kirallyi , Ferenc Barta , Gyorgyi Vereczkeyne Donath , Kalman Nagy
发明人： Zoltan Greff , Peter Kotay Nagy , Jozsef Barkoczy , Gyula Simig , Laszlo Balazs , Imre Doman , Zoltan Ratkai , Peter Seres , Zsuzsa Szent Kirallyi , Ferenc Barta , Gyorgyi Vereczkeyne Donath , Kalman Nagy
IPC分类号： C07D207337
CPC分类号： C07D207/337
摘要： The invention relates to a process for the preparation of amorphous atorvastatin calcium by recrystallization of crude atorvastatin from an organic solvent which comprises dissolving crude amorphous atorvastatin calcium in a lower alkanol containing 2-4 carbon atoms or a mixture of such alkanols under heating and isolating the amorphous atorvastatin calcium precipitated after cooling. The atorvastatin calcium obtained is a known valuable agent useful in treating hyperlipidemia and hypercholestrolemia.
摘要翻译：本发明涉及通过从有机溶剂中重结晶粗阿托伐他汀来制备无定形阿托伐他汀钙的方法，其包括将粗无定形阿托伐他汀钙溶解在含有2-4个碳原子的低级链烷醇或加热下将这些链烷醇的混合物分离无定形阿托伐他汀钙冷却后沉淀。获得的阿托伐他汀钙是可用于治疗高脂血症和高胆固醇血症的已知有价值的药剂。

9. 发明申请

US20130338360A1 METHOD FOR THE PREPARATION OF HIGH-PURITY PHARMACEUTICAL INTERMEDIATES 有权
标题翻译：制备高纯度药物中间体的方法
公开(公告)号：US20130338360A1
公开(公告)日：2013-12-19
申请号：US13990283
申请日：2011-11-29
申请人： Gyorgyi Kovanyine Lax , Gyula Simig , Balazs Volk , Ferenc Lorant Bartha , Gyorgy Krasznai , Gyorgy Ruzsics , Eva Sipos , Kalman Nagy , Gyorgy Morovjan , Jozsef Barkoczy , Adrienn Keszthelyi , Janos Imre , Gabor Bagyinszki
发明人： Gyorgyi Kovanyine Lax , Gyula Simig , Balazs Volk , Ferenc Lorant Bartha , Gyorgy Krasznai , Gyorgy Ruzsics , Eva Sipos , Kalman Nagy , Gyorgy Morovjan , Jozsef Barkoczy , Adrienn Keszthelyi , Janos Imre , Gabor Bagyinszki
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , A61K31/505
摘要： The present invention is related to intermediates useful in the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid and polymorphs of said intermediates, methods for preparation thereof and use thereof.
摘要翻译：本发明涉及可用于制备（+） - 7- [4-（4-氟苯基）-6-异丙基-2-（甲磺酰基 - 甲基 - 氨基） - 嘧啶-5-基的药用盐的中间体 ] - （3R，5S） - 二羟基 - 庚-6-烯酸和所述中间体的多晶型物，其制备方法和用途。

10. 发明申请

US20100168087A1 BENZO[1,2,3]THIADIAZINE DERIVATES 审中-公开
标题翻译：苯并[1,2,3]噻二嗪衍生物
公开(公告)号：US20100168087A1
公开(公告)日：2010-07-01
申请号：US12377771
申请日：2007-08-13
申请人： Marta Porcs-Makkay , Gyula Lukacs , Gabor Kapus , Istvan Gacsalyi , Gyula Simig , Gyoergy Levay , Tibor Mezei , Miklos Vegh , Szabolcs Kertesz , Jozsef Barkoczy , Csilla Leveleki , Laszlo Gabor Harsing
发明人： Marta Porcs-Makkay , Gyula Lukacs , Gabor Kapus , Istvan Gacsalyi , Gyula Simig , Gyoergy Levay , Tibor Mezei , Miklos Vegh , Szabolcs Kertesz , Jozsef Barkoczy , Csilla Leveleki , Laszlo Gabor Harsing
IPC分类号： A61K31/5415 , C07D285/16 , A61P25/00
CPC分类号： C07D285/16
摘要： The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system.
摘要翻译：本发明涉及通式（I）的新的苯并[1,2,3]噻二嗪-1,1-二氧化物衍生物，含有这些化合物的药物及其在药物中的用途。通式（I）的苯并[1,2,3]噻二嗪-1,1-二氧化物衍生物适用于预防或治疗中枢神经系统疾病。

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