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1. 发明公开

EP3412677A1 CYCLOBUTYL (S)-2-[[[(R)-2-(6-AMINOPURIN-9-YL)-1-METHYL-ETHOXY]METHYL-PHENOXY-PHOSPHORYL]AMINO]-PROPANOATES, AND METHOD FOR PRODUCING AND USING SAME 审中-公开
公开(公告)号：EP3412677A1
公开(公告)日：2018-12-12
申请号：EP17814304.6
申请日：2017-04-07
申请人： Alla Chem, LLC , Ivachtchenko, Alexandre Vasilievich , Ivashchenko, Andrey Alexandrovich , Ivachtchenko, Alena Alexandrovna , Savchuk, Nikolay Filippovich
发明人： IVACHTCHENKO, Alexandr Vasilievich , MITKIN, Oleg Dmitrievich
IPC分类号： C07F9/44
CPC分类号： A61K31/664 , A61K31/675 , C07C53/16 , C07C57/15 , C07F9/44 , C07F9/6561 , C07F9/65616
摘要： The present invention relates to chemotherapeutic agents for the treatment of viral and cancerous diseases. Said compounds are prodrugs of the inhibitors of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) of DNA polymerase and are intended for the treatment of human immunodeficiency virus, hepatitis B and co-infections HIV/HCV, HIV/ HBV, HIV/HCV/HBV, and HCV/HBV.

2. 发明公开

EP2236511A2 LIGANDS OF ALPHA-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF 审中-公开
标题翻译： ALPHA-肾上腺素和多巴胺，组胺，咪唑啉和血清素受体及其使用配体
公开(公告)号：EP2236511A2
公开(公告)日：2010-10-06
申请号：EP08864305.1
申请日：2008-12-19
申请人： Alla Chem, LLC. , Ivashchenko, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVASHCHENKO, Alexander Vasilievich , LAVROVSKY, Yan Vadimovich , MITKIN, Oleg Dmitrievich , SAVCHUK, Nikolay Filippovich , TKACHENKO, Sergey Yevgenievich , OKUN, Ilya Matusovich
IPC分类号： C07D471/04 , C07D487/04 , A61K31/43 , A61K31/519 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously α-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT 7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates,

wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C 1 -C 4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C 1 -C 4 alkyl, CF 3 , CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH 2 ) m group, optionally substituted CH=CH group, optionally substituted CH 2 -CH=CH group, C≡C group, SO 2 group; n = 1, 2; m = 1, 2, 3; solid line accompanied by dotted line, i.e. ( --- ) may represent single or double bond.
The invention also relates to active ingredients, pharmaceutical compositions comprising the said ligands as active ingredients; to novel medicaments useful for treatment of diseases and conditions of central nervous system (CNS) of humans and warm-blooded animals.
摘要翻译：本发明涉及新的配体的生物学活性的广谱都包括同时±肾上腺素能受体，多巴胺受体，组胺受体，咪唑啉受体和血清素受体，其中血清素5-HT 7种受体，它们是在通式1的化合物的游离碱，几何异构体，外消旋混合物或单独的光学异构体，药学上可接受的盐和/或水合物，形式worin：R 1是氨基，选自氢，任选取代的C 1 -C 4烷基，酰基，杂环基的取代基，烷氧基羰基，取代的磺酰基; R2是环体系，选自氢，卤素，任选取代的C 1个-C 4烷基，CF 3中选择的取代基，CN，烷氧基，烷氧基羰基，羧基，杂环基或取代的磺酰基; Ar是芳基OPTIONALLY substituiertem不一定安娜迟来与杂环基，或任选取代的芳族杂环基; W是任选substituiertem（CH 2）M基，任选substituiertem CH = CH基团，任选substituiertem CH 2 -CH = CH基团，C‰¡C组，SO 2基团; n = 1时，2; M = 1，2，3; solidLine陪同下虚线，即（---）可以代表单键或双键。因此，本发明涉及活性成分，药物组合物包含所述的配位体作为活性成分; 用于治疗的疾病和人类和温血动物的中枢神经系统（CNS）的条件下有用的新的药物。

3. 发明公开

EP2062895A1 SUBSTITUTED AZEPINO[4,3-B]INDOLES, PHARMACOLOGICAL COMPOSITION AND A METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的氮杂并[4,3-B]吲哚，生产和使用的药物组合物和方法
公开(公告)号：EP2062895A1
公开(公告)日：2009-05-27
申请号：EP07834964.4
申请日：2007-08-08
申请人： Alla Chem, LLC. , Ivashchenko, Andrey, Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , FROLOV, Yevgeniy Borisovich , TKACHENKO, Sergey Yevgenievich , KHVAT, Alexander Viktorovich , MALYARCHUK, Sergey Viktorovich , MITKIN, Oleg Dmitrievich , OKUN, Ilya Matusovich , KYSELEV, Alexandr Sergeevich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Alexandr Vasilievich
IPC分类号： C07D487/04 , A61K31/55 , A61P3/14 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/06 , A61P25/08 , A61P25/14 , A61P25/28
CPC分类号： C07D487/04
摘要： The invention relates to novel chemical compounds, searching for novel physiologically active substanses, leader compounds, "molecular tools", and drug candidates obtained on the basis of screening of combinatorial and focused libraries of the said compounds, and also to pharmaceutical composition, methods for preparation and use thereof.
The invention proposes hydrogenated azepino[4,3-b]indoles of general formula 1 or racemates, optical isomers, geometrical isomers, mixtures of optical or geometrical isomers, pharmaceutically acceptable salts and/or hydrates thereof:

wherein: solid line together with the dotted line ( --- ) represents a single or double bond; R 1 and R 2 independently of each other are amino group substituents selected from hydrogen; optionally substituted C 1 -C 8 alkyl with substituents selected from optionally substituted aryl or 5-6-membered azaheterocyclyl; C 1 -C 8 alkoxycarbonyl; optionally substituted phenyl; optionally substituted carbonylamino or thiocarbonylamino; substituted acyl; C 1 -C 8 alkylsulfonyl; optionally substituted arylsulfonyl; upon that, the substituents in the said R 1 and R 2 independently selected from C 1 -C 8 alkyl, halogen atoms, nitro group, carboxy group, alkoxy, aryl; R i n represents one or more "substituents of cyclic structure" of the same or different structure selected from hydrogen, halogen, C 1 -C 8 alkyl, C 6 -C 10 aryl, 5-6-membered azaheterocyclyl.
摘要翻译：本发明涉及新化合物，搜寻新的生理活性substanses，前导化合物，“分子工具”，和药物候选物获得的组合筛选的基础上和聚焦在所述化合物的文库，并且因此药物组合物，用于方法及其制备方法和用途。本发明提出了氢化吖庚因并[4,3-B]通式1或种族配合，光学异构体，几何异构体，光学或几何异构体，药学上可接受的盐和/或它们的水合物的混合物的吲哚：用虚线实线一起：worin 线（---）表示单键或双键; R 1和R 2unabhängig海誓山盟是选自氢氨基的取代基; 任选取代的C 1 -C 8烷基，被选自任选取代的芳基或5-6元氮杂环基的取代基; C 1 -C 8烷氧基羰基; 任选取代的苯基; OPTIONALLY substituiertem羰或硫代羰; 取代的酰基; C 1 -C 8烷基磺酰基; 任选取代的芳基磺酰基; 时，在R 1和R 2。所述取代基独立地选自C 1个-C 8烷基，卤素原子，硝基，羧基，烷氧基，芳基; R IÑdarstellt一个或多个选自氢，卤素中选择的相同或不同结构的“环结构的取代基”取代，C 1 -C 8烷基，C 6 -C 10芳基，5-6元氮杂环基。

4. 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。

5. 发明公开

EP2351756A1 SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，血清素5-HT6受体拮抗剂和方法的生产和使用
公开(公告)号：EP2351756A1
公开(公告)日：2011-08-03
申请号：EP09819452.5
申请日：2009-10-06
申请人： Ivashchenko, Andrey Alexandrovich , Alla Chem, LLC.
发明人： IVASHCHENKO, Alexander Vasilievich , SAVCHUK Nikolay Filippovich , LAVROVSKY Yan , MITKIN, Oleg Dmitrievich , KADIEVA Madina Georgievna
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P25/18 , A61P25/26 , A61P25/16 , A61P25/08 , A61P9/10 , A61P3/04 , A61P3/08 , A61K9/48 , A61K9/08
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-HT 6 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-HT 6 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; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R 2 represents hydrogen, halogen, optionally substituted C 1 -C 3 alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R 3 represents hydrogen, optionally substituted C 1 -C 3 alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X = S or X = NH, at least one of R 1 , R 2 or R 3 represent substituted C 1 -C 3 alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R 1 , R 2 or R 3 represent hydrogen; R 4 represents C 1 -C 3 alkyl; R 5 represents hydrogen, one or two halogens, C 1 -C 3 alkyl or optionally substituted hydroxyl.
摘要翻译：本发明涉及新颖的substituiertem 3-芳基磺酰基 - 吡唑并[1,5-A]通式1的嘧啶，其药学上可接受的盐和/或水合物，五羟色胺5-HT 6受体拮抗剂和药物组合物，并且因此方法用于特别是在人类和温血动物的所有发病预防和治疗中枢神经系统的各种疾病的，其与血清素5-HT 6个受体相关的疾病，阿尔茨海默氏症，帕金森氏病，亨廷顿氏病，精神分裂症，以及其它神经变性疾病，认知障碍和肥胖。在通式1：其中：X = S，SO或NH; 的R 1 darstellt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 darstellt氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，或aryldiazenyl任选取代的氨基; ，R 3 darstellt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基团，此外，在情况下，当X = S或X = NH，R 1，R中的至少一个2或R 3代表取代的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，aryldiazenyl，或至少两个R 1，R 2或R 3表示氢; ，R 4 darstellt C 1 -C 3烷基; 的R 5 darstellt氢，一个或两个卤素，C 1 -C 3烷基或任意取代的羟基。

6. 发明公开

EP2145887A2 SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND USE THEREOF 有权转让
标题翻译：替代物2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚，VERFAHRENFÜRIHRE HERSTELLUNG UND VERWENDUNG
公开(公告)号：EP2145887A2
公开(公告)日：2010-01-20
申请号：EP08753899.7
申请日：2008-04-01
申请人： Alla Chem, LLC. , Ivashchenko, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVACHTCHENKO, Alexandre Vasilievich , TKACHENKO, Sergey Yevgenievich , FROLOV, Evgueni Borisovich , MITKIN, Oleg Dmitrievich , KRAVCHENKO, Dmitri Vladimirovich , OKUN, Ilya Matusovich , SAVCHUK, Nikolay Filippovich , LAVROVSKY, Yan
IPC分类号： C07D471/04 , A61K31/437 , A61P37/08 , A61P37/02
CPC分类号： A61K31/437 , A61K31/444 , C07D471/04
摘要： The invention relates to antagonists of serotonin 5-HT 6 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:

R 1 represents amino group substituent selected from optionally substituted C 1 -C 5 alkyl; R 2 i is one or more substituents selected from hydrogen, halogen, C 1 -C 3 alkyl, CF 3 , OCF 3 ; Ar is phenyl optionally substituted with halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, substituted amino group, or CF 3 ; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group -CH 2 -CH 2 -, 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-HT 6受体的拮抗剂，代表通式中取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚 1，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; R 2 i是一个或多个选自氢，卤素，C 1 -C 3烷基，CF 3，OCF 3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型化合物。

7. 发明公开

EP3978503A1 ANNELATED 9-HYDROXY-1,8-DIOXO-1,3,4,8-TETRAHYDRO-2H-PYRIDO[1,2-a]PYRAZINE-7-CARBOXAMIDES AS HIV INTEGRASE INHIBITORS 无效
公开(公告)号：EP3978503A1
公开(公告)日：2022-04-06
申请号：EP20818731.0
申请日：2020-03-05
申请人： Ivachtchenko, Alena Alexandrovna , Alla Chem, LLC , Ivachtchenko, Alexandre Vasilievich , Savchuk, Nikolay Filippovich , Ivashchenko, Andrey Alexandrovich
发明人： MITKIN, Oleg Dmitrievich , IVACHTCHENKO, Alexandre Vasilievich , SAVCHUK, Nikolay Filippovich , IVASHCHENKO, Andrey Alexandrovich
IPC分类号： C07D498/14 , C07D498/18 , A61K31/5365 , A61K31/537 , A61K31/553 , A61K31/4985 , A61P31/18
摘要： The present invention relates to a novel compound that has antiviral activity, in particular, inhibitory activity against the integrase of the human immunodeficiency virus (HIV).
The subject of this invention is a novel annelated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxamide of general formula 1 or 2, or any stereoisomer, any pharmaceutically acceptable salt, any solvate, or any crystalline or polycrystalline form thereof

wherein
ring A 1 is an optionally methyl-substituted 5-7 membered saturated heterocycle or heterobicycle;
ring A 2 is a 5-6 membered optionally methyl-substituted saturated or partially saturated monocyclic heterocycle;
ring A 3 is a 5-6 membered monocyclic saturated cycloalkane or tetrahydro-2H-pyran;
R is a 5-7 membered optionally substituted with one, two, or three optionally identical substituents monocyclic or bicyclic heterocyclic radical comprising 1-4 heteroatoms selected from the series O, S, and N except (2 S ,5 R ,13a S )-8-hydroxy-7,9-dioxo- N -{[3-(trifluoromethyl)-pyridin-2-yl]methyl}-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopurido[1',2':4,5]pyrazino[2,1- b ][1,3]oxazepine-10-carboxamide (formula A4) and (1 R ,4 S ,12a R )- N -[(3,5-difluoropyridin-2-yl)methyl]-7-hydroxy-6,8-dioxo-1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2- a :1',2'- d ]pyrazine-9-carboxamide (formula A5).

8. 发明公开

EP3400946A1 ANTIVIRAL COMPOSITION AND METHOD FOR USING SAME 有权
公开(公告)号：EP3400946A1
公开(公告)日：2018-11-14
申请号：EP17844595.3
申请日：2017-04-07
申请人： Alla Chem, LLC , Ivachtchenko, Alexandre Vasilievich , Ivashchenko, Andrey Alexandrovich , Ivachtchenko, Alena Alexandrovna , Savchuk, Nikolay Filippovich
发明人： IVACHTCHENKO, Alexandr Vasilievich , MITKIN, Oleg Dmitrievich
IPC分类号： A61K31/7072 , A61P31/12 , A61K9/08 , A61K9/20 , A61K9/48
CPC分类号： A61K9/08 , A61K9/20 , A61K9/48 , A61K31/7072
摘要： The present invention relates to an antiviral composition and a method for application thereof in the treatment of hepatitis C virus.
Said antiviral composition comprises the HCV NS5B inhibitor of general formula 1, or a stereoisomer, an isotopically enriched analog, or crystalline or polycrystalline forms thereof.

9. 发明公开

EP3078669A1 SUBSTITUTED (2R, 3R, 5R)-3-HYDROXY-(5-PYRIMIDIN-1-YL) TETRAHYDROFURAN-2-YLMETHYL ARYL PHOSPHORAMIDATES 审中-公开
标题翻译：取代的（2R，3R，5R）-3-羟基 - （5-嘧啶-1-基） - 四氢-2-基甲基 - 芳基磷酸酯
公开(公告)号：EP3078669A1
公开(公告)日：2016-10-12
申请号：EP14852462.2
申请日：2014-10-06
申请人： Ivashchenko, Andrey Alexandrovich , Ivachtchenko, Alexandre Vasilievich , Alla Chem, LLC.
发明人： MITKIN, Oleg Dmitrievich
IPC分类号： C07F9/6558 , C07F9/44 , C07F9/6596 , A61K31/665 , A61K31/664 , A61K31/675 , A61K31/695 , A61P31/12
CPC分类号： C07F9/65586 , A61K31/665 , A61K31/675 , A61K31/695 , A61K31/7068 , A61K31/7072 , A61K45/06 , C07H19/067 , Y02A50/385 , Y02A50/387 , Y02A50/393 , A61K2300/00
摘要： The instant invention relates to a novel compound representing a substituted phosphoramidic acid - a (2 R ,3 R ,5 R )-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 1 or a pharmaceutically acceptable salt or a stereoisomer thereof,

wherein:
R 1 is (i) hydrogen, a (CH 3 ) 2 [(CH 3 ) 3 C]Si, a C 2 -C 6 acyl, optionally substituted with NR 5 R 6 group, wherein R 5 and R 6 are independently hydrogen or a C 1 -C 4 alkyl; (ii) 1-pyrrole-2-ylcarbonyl, piperidin-3-ylcarbonyl or piperidin-4-ylcarbonyl;
R 2 and R 3 are F; or R 3 is CH 3 and R 2 is F or OH; R 4 is hydrogen or methyl; Ar is a phenyl, a pyridyl or a naphthyl, wherein phenyl, pyridyl or naphthyl are optionally substituted with at least one of C 1-3 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-3 alkoxy, F, Cl, Br, I, nitro, cyano, -N(C 1-3 alkyl) 2 ;
Pm is 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl or 4-(4-amino-2-oxo-2H-pyrimidin-1-yl), in which amino group is optionally substituted with 1-pyrrole-2-ylcarbonyl, piperidin-3-ylcarbonyl, piperidin-4-ylcarbonyl or radical C(O)R 8 , wherein R 8 is (i) a C 1 -C 4 alkyl, optionally substituted with NR 6 R 7 group, wherein R 6 and R 7 are independently hydrogen or C 1 -C 4 alkyl; (ii) a C 1-3 alkoxy optionally substituted with a phenyl; X is O or N-R 9 , wherein R 9 is a C 1 -C 4 alkyl, optionally substituted with OH or OCH 3 ; n = 1, 2 or 3; and methods for the preparation as well.
The novel compound is used for a pharmaceutical composition with at least one pharmaceutically acceptable excipient as well as with an inosine 5 monophosphate dehydrogenase inhibitor, HCV protease NS3 inhibitor, HCV protease NS3/4A inhibitor, and RNA polymerase NS5A inhibitor. The novel compound is useful as viral polymerase HCV NS5B inhibitor and can be used for treating a disease caused by hepatitis C virus (HCV).

10. 发明授权

EP2145887B1 SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND USE THEREOF 有权转让
标题翻译：取代的2,3,4,5-四氢-1H-吡啶并[4,3-B]吲哚，PROCESS FOR其生产和使用
公开(公告)号：EP2145887B1
公开(公告)日：2016-04-27
申请号：EP08753899.7
申请日：2008-04-01
申请人： Alla Chem, LLC. , Ivashchenko, Andrey Alexandrovich
发明人： IVASHCHENKO, Andrey Alexandrovich , IVACHTCHENKO, Alexandre Vasilievich , TKACHENKO, Sergey Yevgenievich , FROLOV, Evgueni Borisovich , MITKIN, Oleg Dmitrievich , KRAVCHENKO, Dmitri Vladimirovich , OKUN, Ilya Matusovich , SAVCHUK, Nikolay Filippovich , LAVROVSKY, Yan
IPC分类号： C07D471/04 , A61K31/437 , A61P37/08 , A61P37/02
CPC分类号： A61K31/437 , A61K31/444 , C07D471/04

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