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1. 发明申请

US20100120792A1 Substituted 2,3,4,5-Tetrahyrdo-1H-Pyrido[4,3-B]Indoles, Methods for the Production and Use Thereof 失效
标题翻译：取代的2,3,4,5-四氢-1H-吡啶并[4,3-B]吲哚，其生产和使用方法
公开(公告)号：US20100120792A1
公开(公告)日：2010-05-13
申请号：US12594453
申请日：2008-04-01
申请人： Andrey Alexandrovich Ivashchenko , Alexandre Vasilievich Ivachtchenko , Sergey Yevgenievich Tkachenko , Evgueni Borisovich Frolov , Oleg Dmitrievich Mitkin , llya Matusovich Okun , Nikolay Filippovich Savchuk , Yan Lavrovsky
发明人： Andrey Alexandrovich Ivashchenko , Alexandre Vasilievich Ivachtchenko , Sergey Yevgenievich Tkachenko , Evgueni Borisovich Frolov , Oleg Dmitrievich Mitkin , llya Matusovich Okun , Nikolay Filippovich Savchuk , Yan Lavrovsky
IPC分类号： A61K31/4427 , A61K31/4745 , C07D471/04 , A61P25/08 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/22 , A61P9/10
CPC分类号： A61K31/437 , A61K31/444 , C07D471/04
摘要： The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2, is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.
摘要翻译：本发明涉及同时调节细胞中Ca 2+离子的体内平衡的5-羟色胺5-HT6受体的拮抗剂，代表通式1的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚，其药学上可接受的盐和/或水合物。在通式1中：R 1表示选自任选取代的C 1 -C 5烷基的氨基取代基; R2是选自氢，卤素，C1-C3烷基，CF3，OCF3中的一个或多个取代基; Ar是任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或CF 3取代的苯基; 或在该循环中任选取代的包含1-2个氮原子的芳族6-元杂环; W表示亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C≡C-。本发明还涉及选自通式1的化合物，其制备方法，药物组合物及其用途的新化合物。

2. 发明授权

US08541437B2 Substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, methods for the production and use thereof 失效
标题翻译：取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚，其制备和使用方法
公开(公告)号：US08541437B2
公开(公告)日：2013-09-24
申请号：US12594453
申请日：2008-04-01
申请人： Andrey Alexandrovich Ivashchenko , Alexandre Vasilievich Ivachtchenko , Sergey Yevgenievich Tkachenko , Evgueni Borisovich Frolov , Oleg Dmitrievich Mitkin , Dmitri Vladimirovich Kravchenko , Ilya Matusovich Okun , Nikolay Filippovich Savchuk , Yan Lavrovsky
发明人： Andrey Alexandrovich Ivashchenko , Alexandre Vasilievich Ivachtchenko , Sergey Yevgenievich Tkachenko , Evgueni Borisovich Frolov , Oleg Dmitrievich Mitkin , Dmitri Vladimirovich Kravchenko , Ilya Matusovich Okun , Nikolay Filippovich Savchuk , Yan Lavrovsky
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： A61K31/437 , A61K31/444 , C07D471/04
摘要： The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2i is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.
摘要翻译：本发明涉及同时调节细胞中Ca 2+离子的体内平衡的5-羟色胺5-HT6受体的拮抗剂，代表通式1的取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚，其药学上可接受的盐和/或水合物。在通式1中：R 1表示选自任选取代的C 1 -C 5烷基的氨基取代基; R2i是一个或多个选自氢，卤素，C1-C3烷基，CF3，OCF3的取代基; Ar是任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或CF 3取代的苯基; 或在该循环中任选取代的包含1-2个氮原子的芳族6-元杂环; W表示亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C = C-。本发明还涉及选自通式1的化合物，其制备方法，药物组合物及其用途的新化合物。

3. 发明授权

US08618114B2 Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof 有权
标题翻译：取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，5-羟色胺5-HT 6受体拮抗剂及其生产和使用方法
公开(公告)号：US08618114B2
公开(公告)日：2013-12-31
申请号：US13122152
申请日：2009-10-06
申请人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko , Yan Lavrovsky , Oleg Dmitrievich Mitkin , Madina Georgievna Kadieva
发明人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko , Yan Lavrovsky , Oleg Dmitrievich Mitkin , Madina Georgievna Kadieva
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X=S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X=S or X=NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.
摘要翻译：本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍和肥胖。在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。

4. 发明申请

US20110178078A1 SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，丝氨酸5-HT6受体拮抗剂及其生产和使用方法
公开(公告)号：US20110178078A1
公开(公告)日：2011-07-21
申请号：US13122152
申请日：2009-10-06
申请人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko , Yan Lavrovsky , Oleg Dmitrievich Mitkin , Madina Georgievna Kadieva
发明人： Andrey Alexandrovich Ivashchenko , Nikolay Filippovich Savchuk , Alexander Vasilievich Ivashchenko , Yan Lavrovsky , Oleg Dmitrievich Mitkin , Madina Georgievna Kadieva
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/519 , C07D487/04 , A61P3/04 , A61P25/28 , A61P25/16 , A61P25/18 , A61P3/10
CPC分类号： C07D487/04
摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X═S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X═S or X═NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.
摘要翻译：本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍和肥胖。在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。

5. 发明授权

US07179593B1 Estrogen receptor site-specific ribozymes and uses thereof for estrogen dependent tumors 失效
标题翻译：雌激素受体位点特异性核酶及其用于雌激素依赖性肿瘤的用途
公开(公告)号：US07179593B1
公开(公告)日：2007-02-20
申请号：US10009420
申请日：2000-06-02
申请人： Arun K. Roy , Yan Lavrovsky , Rakesh K. Tyagi , Chung S. Song , Bandana Chatterjee , Shuo Chen
发明人： Arun K. Roy , Yan Lavrovsky , Rakesh K. Tyagi , Chung S. Song , Bandana Chatterjee , Shuo Chen
IPC分类号： C12Q1/68 , C12P19/34 , C12N15/88 , C07H21/02 , C07H21/04
CPC分类号： C12Q1/6886 , C12Q2600/156 , C12Q2600/158
摘要： Highly specific hammerhead ribozymes are provided that human target estrogen receptor mRNA. These ribozymes, designated RZ1 through RZ7 provide predictable mRNA cleavage products. Methods for inhibiting estrogen-dependent tumor growth, such as that characteristic of breast cancer, are also provided employing these ribozymes. One or both of the ribozymes may be used together or separately with equal efficiency. The ribozymes possess a sequence region with a catalytic core that provides the attributed catalytic activity to these ribozymes.
摘要翻译：提供了高度特异性的锤头核酶，人类靶向雌激素受体mRNA。这些指定为RZ1至RZ7的核酶可提供可预测的mRNA裂解产物。使用这些核酶也提供了抑制雌激素依赖性肿瘤生长的方法，例如乳腺癌的特征。一个或两个核酶可以一起使用或以相同的效率单独使用。核酶具有带有催化核心的序列区域，其提供对这些核酶的归属催化活性。

6. 发明授权

US08283307B2 Treatment of fibrotic disease 失效
标题翻译：治疗纤维化疾病
公开(公告)号：US08283307B2
公开(公告)日：2012-10-09
申请号：US10570122
申请日：2004-09-07
申请人： Christine Power , Yan Lavrovsky
发明人： Christine Power , Yan Lavrovsky
IPC分类号： A61K38/00 , A61K38/18 , A61K38/19 , C07K14/475 , C07K14/52
CPC分类号： A61K38/215 , A61K38/00 , A61K38/177 , C07K14/52 , C07K2319/21 , A61K2300/00
摘要： The invention relates to the use of INSP035 for treatment and/or prevention of fibrotic diseases, in particular of scleroderma.
摘要翻译：本发明涉及INSP035用于治疗和/或预防纤维化疾病，特别是硬皮病的用途。

7. 发明申请

US20070104723A1 Treatment of fibrotic disease 失效
标题翻译：治疗纤维化疾病
公开(公告)号：US20070104723A1
公开(公告)日：2007-05-10
申请号：US10570122
申请日：2004-09-07
申请人： Christine Power , Yan Lavrovsky
发明人： Christine Power , Yan Lavrovsky
IPC分类号： A61K48/00 , A61K38/21 , A61K31/573 , A61K31/192
CPC分类号： A61K38/215 , A61K38/00 , A61K38/177 , C07K14/52 , C07K2319/21 , A61K2300/00
摘要： The invention relates to the use of INSP035 for treatment and/or prevention of fibrotic diseases, in particular of scleroderma.
摘要翻译：本发明涉及INSP035用于治疗和/或预防纤维化疾病，特别是硬皮病的用途。

8. 发明授权

US08486945B2 Heterocyclic inhibitors of an Hh-signal cascade, medicinal compositions based thereon and methods for treating diseases caused by the aberrant activity of an Hh-signal system 失效
标题翻译： Hh信号级联的杂环抑制剂，基于其的医药组合物和用于治疗由Hh信号系统的异常活性引起的疾病的方法
公开(公告)号：US08486945B2
公开(公告)日：2013-07-16
申请号：US12808152
申请日：2008-12-12
申请人： Andrey Ivashchenko , Yan Lavrovsky , Sergey Malyarchuk , Ilya Okun , Nikolay Savchuk , Sergey Tkachenko , Alexander Khvat , Alexander Ivashchenko
发明人： Andrey Ivashchenko , Yan Lavrovsky , Sergey Malyarchuk , Ilya Okun , Nikolay Savchuk , Sergey Tkachenko , Alexander Khvat , Alexander Ivashchenko
IPC分类号： A01N43/58 , A61K31/50 , C07D487/00
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/2018 , A61K9/205 , A61K9/2059 , A61K9/4858 , C07D215/58 , C07D401/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]N-acidylated 3-azole derivatives.
摘要翻译：本发明涉及新颖的杂环化合物及其用途，含有所述化合物作为活性成分的药物组合物及其用于生产用于治疗由异常活性引起的疾病的人和温血动物的药物制剂的用途刺猬（Hh） - 信号系统，特别是肿瘤疾病。本发明还涉及以“分子药理学工具”形式的上述化合物用于检查（体外和体内）Hh信号系统的生化特征的用途，特别是Hh蛋白和跨膜蛋白，即抑制剂Patched（Ptc）和原癌蛋白。所要求保护的八个化合物组包括2,6-二氢-7H-吡唑并[3,4-d]哒嗪-7-酮和1,4-二氢吡唑并[3,4-b] [1,4] 噻嗪-5-酮; N-酸化的4-咪唑并[1,2-a]嘧啶-2-基]苯胺; （[4H-噻吩并[3,2-b]吡咯-5-基）羰基]哌啶-4-碳酸酰胺; 2-（4-氰基吡啶-1-基） - 异烟酰胺; N-磺酰基-1,2,3,4-四氢喹啉-6-碳酸酰胺; 和吡啶2-氨基-4,5,6,7-四氢噻吩并[2,3-c] N-酸化的3-唑衍生物。

9. 发明申请

US20100048467A1 Cystine-Knot Fold Cytokine 审中-公开
标题翻译：胱氨酸结折叠细胞因子
公开(公告)号：US20100048467A1
公开(公告)日：2010-02-25
申请号：US12159541
申请日：2006-01-12
申请人： Mark Douglas Davies , Christopher Benjamin Phelps , Richard Joseph Fagan , Christine Power , Melanie Yorke , Mark Ibberson , Yan Lavrovsky
发明人： Mark Douglas Davies , Christopher Benjamin Phelps , Richard Joseph Fagan , Christine Power , Melanie Yorke , Mark Ibberson , Yan Lavrovsky
IPC分类号： A61K38/16 , A61K31/7088 , A61P35/00
CPC分类号： A61K38/18
摘要： This invention relates to a novel protein (INSP002), herein identified as a secreted protein that is a member of the Dan family of the cystine-knot fold cytokine superfamily and to the use of this protein and nucleic acid sequences from the encoding genes in the diagnosis, prevention and treatment of disease.
摘要翻译：本发明涉及一种新型蛋白质（INSP002），其被鉴定为分泌型蛋白质，其是胱氨酸 - 结折叠细胞因子超家族的丹氏家族的成员，并且使用该蛋白质和来自编码基因的核酸序列诊断，预防和治疗疾病。

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