专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

EP2287163B1 2-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：血清素5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶 - 嘧啶拮抗剂，其生产方法和用途
公开(公告)号：EP2287163B1
公开(公告)日：2014-08-06
申请号：EP09742910.4
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich , IVASHCHENKO, Andrey Alexandrovich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519

2. 发明公开

EP2036889A2 SUBSTITUTED INDOLES AND A METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：维多利亚独立电力公司
公开(公告)号：EP2036889A2
公开(公告)日：2009-03-18
申请号：EP07747937.6
申请日：2007-05-17
申请人： Alla Chem, LLC. , Ivashchenko, Andrey, Alexandrovich
发明人： IVASCHENKO, Andrey Alexandrovich , TKACHENKO, Sergey Yevgenievich , KHVAT, Alexander Viktorovich , MITKIN, Oleg Dmitrievich , OKUN, Ilya Matusovich , KYSELVEV, Alexandr Sergeevich , KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich
IPC分类号： C07D209/42 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/14 , C07D498/04 , A61K31/405 , A61K31/407 , A61K31/416 , A61K31/4439 , A61K31/4465 , A61K31/454 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/55
CPC分类号： C07D401/14 , C07D209/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/14 , C07D498/04
摘要： The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said compositions for the manufacture of medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (I) or racemates, optical isomers, pharmaceutically acceptable salts and/or hydrates thereof, wherein R 1 , R 1 4 and R 2 4 independently are an aminogroup substituent selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or R 1 4 and R 2 4 together with the nitrogen atom to which they are attached, form via R 1 4 and R 2 4 an optionally substituted azaheterocyclyl or guanidyl; R 2 is an alkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; R 3 is lower alkyl, R 5 is an hydrogen atom or R 5 together with the oxygen atom to which it is attached and R 2 4 together with the nitrogen atom to which it is attached close, via R 5 and R 2 4 an oxazine ring; R 6 is a cyclic system substituent selected from hydrogen, halogen atom, cyanogroup, optionally substituted aryl or substituted heterocyclyl.
摘要翻译：本发明涉及以药物组合物物质形式使用的新型取代的吲哚，以及所述组合物用于制备用于预防和治疗病毒性疾病的药物制剂的用途，特别是由感染性肝炎（HCV， HBV），人类免疫缺陷（HIV），非典型肺炎（SARS）和禽流感。本发明提出了通式（I）的新型取代的吲哚或其外消旋物，旋光异构体，药学上可接受的盐和/或水合物，其中R 1，R 14和R 24独立地是选自氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂环基，或R 14和R 24与它们所连接的氮原子一起经由R 14和R 24经任意取代的杂环基或胍基形成; R 2是选自氢，任选取代的巯基，任选取代的氨基和任选取代的羟基的烷基取代基; R 3为低级烷基，R 5为氢原子或R 5与连接的氧原子一起形成，R 2与其所连接的氮原子一起通过R 5和R 24接近恶嗪环; R 6是选自氢，卤素原子，氰基，任选取代的芳基或取代的杂环基的环系取代基。

3. 发明公开

EP2433939A1 SUBSTITUTED 8-SULFONYL-2,3,4,5-TETRAHYDRO-1H-GAMMA-CARBOLINES, LIGANDS AND PHARMACEUTICAL COMPOSITION; METHOD FOR THE PRODUCTION AND USE OF SAME 审中-公开
标题翻译： “取代的-8-磺酰-2,3,4,5- TETRA HYDRO-1H-GAMMA-CARBO LINE，配体和药物组合物的方法生产和使用THEREOF”
公开(公告)号：EP2433939A1
公开(公告)日：2012-03-28
申请号：EP10777998.5
申请日：2010-04-30
申请人： Alla Chem, LLC.
发明人： ALLA CHEM, LLC , IVASHCHENKO, Alexander Vasilievich , KYSIL, Volodymyr Mikhailovich , MITKIN, Oleg Dmitrievich , SAVCHUK Nikolay Filippovich
IPC分类号： C07D471/04 , A61K31/437 , A61K9/48 , A61K9/08 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/24
CPC分类号： A61K31/437 , A61K9/0019 , A61K9/2018 , A61K9/2059 , A61K9/4858 , A61K47/10 , C07D471/04
摘要： The invention relates to novel substituted 8-sulfonyl-2,3,4,5-tetrahydro-1 H -γ-carbolines of the general formula 1 and their pharmaceutically acceptable salt - ligands exhibiting biological activity simultaneously towards alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepinefrine receptors, serotonin receptors, to active components, pharmaceutical compositions, comprising as an active component novel ligands, to novel medicaments intended for treatment of conditions and diseases of central nervous system. In the general formula 1

R 1 represents a substituent selected from hydrogen, optionally substituted C 1 -C 3 alkyl or C 1 -C 4 alkyloxycarbonyl; R 2 represents a cyclic system substituent selected from hydrogen, optionally substituted C 1 -C 3 alkyl, optionally substituted C 2 -C 3 alkenyl or substituted sulfonyl; R 3 represents optionally substituted aryl or substituted amino group.
摘要翻译：本发明涉及新颖substituiertem -8-磺酰-2,3,4,5-四氢-1H-³咔啉的通式1的化合物及其药学上可接受的盐 - 同时参展的生物学活性向的α-肾上腺素能受体，多巴胺受体配体，组胺受体，咪唑啉受体，σ受体，norepinefrine受体，血清素受体，以活性成分，药物组合物，包含作为活性组分的新配体，旨在用于处理的条件和中枢神经系统疾病的新的药物。在通式1 R 1表示选自氢，任选取代的C 1 -C 3烷基或C 1 -C 4烷氧羰基中选出的取代基; R 2表示选自氢环状系统取代基，任选取代的C 1 -C 3烷基，任选取代的C 2 -C 3链烯基或取代的磺酰基; ，R 3 darstellt任选取代的芳基或取代的氨基。

4. 发明公开

EP2305678A1 TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：四氢[1,5-A]吡啶并嘧啶AS拮抗剂的血清素5-HT6受体，方法用于生产及其用途
公开(公告)号：EP2305678A1
公开(公告)日：2011-04-06
申请号：EP09742911.2
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519
摘要： The present invention relates to serotonin 5-HT 6 receptor antagonists - novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT 6 receptors.
In formulas 1 and 2

Ar represents optionally substituted aryl or optionally substituted heterocyclyl; R 1 represents hydrogen, optionally substituted lower C 1 -C 3 alkyl, substituted hydroxyl group, substituted sulfahyl group; R 2 represents hydrogen or optionally substituted C 1 -C 3 alkyl; R 3 represents hydrogen, optionally substituted C 1 -C 3 alkyl or tert .-butyloxycarbonyl.
摘要翻译：本发明涉及对血清素5-HT 6受体拮抗剂 - 新颖substituiertem -3-磺酰基-6,7,8,9-四氢[1,5-α] [4,3-E]嘧啶和substituiertem -3-磺酰 5,6,7,8-四氢[1,5-α] [4,3-D]嘧啶，药物物质和药物组合物，包含药物物质如上述的化合物和各种病症的预防和治疗的方法中所提到的和在人类和温血动物的所有发病中枢神经系统的疾病，其与血清素5-HT 6个受体相关的。在式1个2中的Ar darstellt任选取代的芳基或任选取代的杂环; 的R 1 darstellt氢，任选取代的低级C 1 -C 3烷基，取代的羟基，取代sulfahyl基; R 2 darstellt氢或任选取代的C 1 -C 3烷基; ，R 3 darstellt氢，任选取代的C 1 -C 3烷基或叔丁氧基羰基。

5. 发明授权

EP2305678B8 TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：四氢[1,5-A]吡啶并嘧啶AS拮抗剂的血清素5-HT6受体，方法用于生产及其用途
公开(公告)号：EP2305678B8
公开(公告)日：2014-03-05
申请号：EP09742911.2
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich , IVASHCHENKO, Andrey Alexandrovich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519

6. 发明授权

EP2305678B1 TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：四氢[1,5-A]吡啶并嘧啶AS拮抗剂的血清素5-HT6受体，方法用于生产及其用途
公开(公告)号：EP2305678B1
公开(公告)日：2013-12-25
申请号：EP09742911.2
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519
摘要： The invention relates to serotonin 5-HT 6 receptor antagonists - novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT 6 receptors including cognitive and neurodegenerative diseases. Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar represents optionally substituted aryl or optionally substituted heteroaryl; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, C 1 -C 4 alkyloxycarbonyl; R 2 represents hydrogen, halogen or optionally substituted C 1 -C 3 alkyl ; R 1 3 and R 2 3 represent optionally alike: hydrogen, optionally substituted C 1 -C 3 alkyl or R 1 3 and R 2 3 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.

7. 发明公开

EP2287163A1 2-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
标题翻译：血清素5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶 - 嘧啶拮抗剂，其生产方法和用途
公开(公告)号：EP2287163A1
公开(公告)日：2011-02-23
申请号：EP09742910.4
申请日：2009-04-30
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： KYSIL, Volodymyr Mikhailovich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexander Vasilievich
IPC分类号： C07D471/14 , A61P25/22 , A61K31/519 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/08 , A61P3/08 , A61P25/26 , A61P9/10 , A61P25/16 , A61P3/04
CPC分类号： C07D471/14 , A61K31/519
摘要： The invention relates to serotonin 5-HT 6 receptor antagonists - novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT 6 receptors including cognitive and neurodegenerative diseases.
Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof.

wherein: Ar represents optionally substituted aryl or optionally substituted heteroaryl; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, C 1 -C 4 alkyloxycarbonyl; R 2 represents hydrogen, halogen or optionally substituted C 1 -C 3 alkyl ; R 1 3 and R 2 3 represent optionally alike: hydrogen, optionally substituted C 1 -C 3 alkyl or R 1 3 and R 2 3 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.
摘要翻译：本发明涉及血清素5-HT 6受体拮抗剂 - 新的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基 -3-芳基磺酰基-5,6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，含有所述药物作为所述化合物的药物和药物组合物，预防和治疗人和动物中中枢神经系统的各种疾病的发病机理与血清素5-HT 6受体相关，包括认知和神经退行性疾病。通式1的取代的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基-3-芳基磺酰基-5 ，通式2的6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶及其药学上可接受的盐和/或水合物。其中：Ar代表任选取代的芳基或任选取代的杂芳基; R 1代表氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2代表氢，卤素或任选取代的C1-C3烷基; R13和R23任选相同：氢，任选取代的C1-C3烷基或R13和R23与它们所连接的氮原子一起形成任选取代的氮杂杂环。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式