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    SUBSTITUTED 3,4,12,12A-TETRAHYDRO-1H-[1,4]OXAZINO[3,4-C]PYRIDO[2,1-F][1,2,4]TRIAZINE-6,8-DIONE, PHARMACEUTICAL COMPOSITION, AND METHODS FOR PREPARING AND USING SAME
    4.
    发明公开
    SUBSTITUTED 3,4,12,12A-TETRAHYDRO-1H-[1,4]OXAZINO[3,4-C]PYRIDO[2,1-F][1,2,4]TRIAZINE-6,8-DIONE, PHARMACEUTICAL COMPOSITION, AND METHODS FOR PREPARING AND USING SAME 审中-公开

    公开(公告)号：EP3763718A1

    公开(公告)日：2021-01-13

    申请号：EP20781429.4

    申请日：2020-03-27

    申请人： Ivachtchenko, Alexandre Vasilievich ,  Ivashchenko, Andrey Alexandrovich ,  Savchuk, Nikolay Filippovich ,  Ivachtchenko, Alena Alexandrovna ,  Asavi, LLC

    发明人： MITKIN, Oleg Dmitrievich ,  IVACHTCHENKO, Alexandre Vasilievich ,  IVASHCHENKO, Andrey, Alexandrovich

    IPC分类号： C07D498/14 ,  A61K31/5383 ,  A61P31/16

    摘要： Influenza is an acute infectious respiratory disease caused by the influenza virus. It is part of the group of Acute Respiratory Viral Infections (ARVI). It occasionally spreads in the form of epidemics and pandemics. Currently, more than 2000 variants of the influenza virus differing in the antigen spectrum have been identified. Given that influenza is a serious threat to public health (worldwide, these annual epidemics lead to 3-5 million cases of severe illness, millions of hospitalizations, and up to 650,000 deaths), it seems appropriate to search for new anti-influenza drugs with improved characteristics.
    The inventors surprisingly found out that the previously unknown substituted 3,4,12,12a-tetrahydro-1 H-[1,4] oxazino[3,4-c]pyrido[2,1-f] [1,2,4]triazine-6,8-dione of general formula 1, its stereoisomer, their prodrug, pharmaceutically acceptable salt, solvate, hydrate, and a crystalline or polycrystalline form thereof are effective agents for prophylaxis and treatment of viral diseases, including influenza

    where
    R 1 is (6,7-difluoro-5,10-dihydrothieno[3,2- c ][2]benzothiepin-10-yl, (7,8-difluoro-4,9-dihydrothieno[2,23- c ][2]benzothiepin-4-yl, (3,4-difluorophenyl)(phenyl)methyl, (3,4-difluorophenyl)(2-methylsulfanylphenyl)methyl, diphenylmethyl, bis(4-fluorophenyl)-methyl; R 2 is hydrogen or a protective group selected from a series comprising (C1-C3 alkyl) oxycarbonyloxy, {[(C1-C3 alkyl)oxycarbonyl]-oxy}methoxy, {[2-(C1-C3 alkyl) oxyethoxy]carbonyl}oxy, ({[(1 R )-2-[(C1-C3alkyl)oxy]-1-methylethoxy}carbonyl)oxy, {[(3 S )-ethoxyfuran-3-yloxy]-carbonyl}oxy, [(ethoxy-2 H -pyran-4-yloxy)carbonyl]oxy,{[(1-acetylazetidine)-3-yloxy]carbonyl}oxy, {[(C1-C3alkyl) oxycarbonyl] -oxy}methoxy, ({[2-(C1-C3 alkyl)oxyethoxy]carbonyl}oxy) methoxy.

    PHOSPHORAMIDATE NUCLEOSIDE PRODRUG FOR TREATING VIRAL DISEASES AND CANCER, PROCESSES FOR THEIR PREPARATION AND THEIR USE
    5.
    发明公开
    PHOSPHORAMIDATE NUCLEOSIDE PRODRUG FOR TREATING VIRAL DISEASES AND CANCER, PROCESSES FOR THEIR PREPARATION AND THEIR USE 审中-公开

    公开(公告)号：EP3331354A1

    公开(公告)日：2018-06-13

    申请号：EP17834922.1

    申请日：2017-06-21

    申请人： Asavi, LLC ,  Ivashchenko, Andrey Alexandrovich ,  Savchuk, Nikolay Filippovich ,  Mitkin, Oleg Dmitrievich ,  Ivachtchenko, Alexandre Vasilievich ,  Ivachtchenko, Alena Alexandrovna

    发明人： IVACHTCHENKO, Alexandre Vasilievich ,  IVASHCHENKO, Andrey Alexandrovich ,  SAVCHUK, Nikolay Filippovich ,  MITKIN, Oleg Dmitrievich ,  IVACHTCHENKO, Alena Alexandrovna

    IPC分类号： A01K43/04 ,  A61K31/70

    CPC分类号： C07H19/16 ,  C07F9/65586 ,  C07F9/65616 ,  C07H19/06

    摘要： The present invention pertains to chemotherapeutic agents and their use for treating viral and cancerous diseases. These compounds are inhibitors of HCV NS5B polymerase, HBV DNA polymerase and, HIV-1 reverse transcriptase (RT) inhibitor, and for treatment of hepatitis B and C infection in mammals. These compounds are also of interest for the treatment of cancer. The phosphoramidate nucleoside prodrug of the general formula (1), a stereoisomer, isotope-enriched analogue, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, formula (1) wherein: Ar is aryl or hetaryl; R1 is H or CH3, R2 is the substituent selected from OCH2CH=CH2, OCH2CH≡CH, OCH2CH2CH2OCH3, formula (2), formula (3) or formula (4), R3 is H or CH3; R4 is OH, OR5, NR6R7; R5 is C1-C4-alkyl; R6 and R7 are not necessarily the same substituents selected from H or CH3, Z = O, or NH; an arrow (→) indicates the place of substituent connection; Nuc is formula (5) or (6); R8 and R9 are not necessarily the same substituents selected from H, F, Cl, CH3 or OH provided when continuous line and its accompanying dotted line ( ) together are the single carbon-carbon (C-C) bond or R8 and R9 are hydrogen provided when continuous line and its accompanying dotted line ( ) together are the double carbon-carbon bond (C=C); R10 is the substituent selected from R10.1- R10.5; R10.1 R10.2 R10.4 R10.5 ; R11 is the substituent selected from H, F, CI, CH3, or CF3; R12 is hydrogen, C1-C4-alkyl or C3-C6-cycloalkyl; X is oxygen or ethanediyl-1,1 (C=CH2); Y is O, S, CH2, or HO-CH group provided when continuous line and its accompanying dotted line (formula 7) together are the single carbon-carbon (C-C) bond or Y is CH group provided when continuous line and its accompanying dotted line (formula 7) together are the double carbon-carbon bond (C=C), and compound of the general formula (1), stereoisomers, isotope-enriched analogues, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, wherein: Ar is aryl or hetaryl; R1 is H or CH3; R2 is isopropyl; Nuc is formula (8), (9) or (10).

    CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS AS ANDROGEN RECEPTOR ANTAGONISTS, ANTI-CANCER AGENT, METHOD FOR PRODUCING AND USING SAME
    6.
    发明公开
    CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS AS ANDROGEN RECEPTOR ANTAGONISTS, ANTI-CANCER AGENT, METHOD FOR PRODUCING AND USING SAME 审中-公开
    骑行N，N'- DIARYLTHIOHARNSTOFFE和N，N'-二芳基雄激素受体拮抗剂，抗癌药在生产和使用ORDER AND METHOD

    公开(公告)号：EP2597086A1

    公开(公告)日：2013-05-29

    申请号：EP11809933.2

    申请日：2011-07-01

    申请人： Ivachtchenko, Alexandre Vasilievich ,  Ivashchenko, Andrey Alexandrovich ,  Savchuk, Nikolay Filippovich

    发明人： MITKIN, Oleg Dmitrievich

    IPC分类号： C07D239/10 ,  C07D239/22 ,  C07D233/86 ,  C07D233/72 ,  C07D471/10 ,  C07D491/107 ,  C07D249/12 ,  A61K31/4196 ,  A61K31/513 ,  A61K31/4166 ,  A61K31/4188 ,  A61K31/527 ,  A61K9/20 ,  A61K9/48 ,  A61K9/08 ,  A61P35/00

    CPC分类号： C07D233/86 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/2095 ,  A61K9/4858 ,  C07D233/72 ,  C07D239/10 ,  C07D239/22 ,  C07D249/12 ,  C07D471/10 ,  C07D491/107

    摘要： The present invention relates to novel cyclic N,N'-diarylureas and N,N'-diarylthioureas - androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.
    Cyclic N,N' -diarylthioureas or N,N' -diarylureas of the general formula 1, their optical (R)- and (S)- isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed,

    wherein: X represents oxygen or sulfur;
    m = 0 or 1;
    R1 represents C 1 -C 3 alkyl;
    R2 and R3 represent hydrogen; or
    R2 and R3 together with C-atom they are attached to form C = O group; R4 and R5 represent hydrogen; or
    R4 represents hydrogen, R5 represents methyl; or
    R4 represents methyl, R5 represents CH 2 R6 group in which R6 represents C 1 -C 3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or
    R4 and R5 together with C-atom they are attached to form 5- or 6- membered heterocycle comprising at least one oxygen atom or nitrogen atom optionally substitutd with methyl; or
    R4 and R5 together with C-atom they are attached to form NH group.

    摘要翻译： 本发明涉及新的环状N，N'- diarylureas和N，N'-diarylthioureas - 雄激素受体拮抗剂，抗肿瘤剂，药物组合物，药物，以及用于治疗癌性疾病，其中的前列腺癌的方法。 环状N，N“-diarylthioureas或N，N”，通式1中，其光学（R）的-diarylureas - 和（S） - 异构体及其参展雄激素受体拮抗剂的性质药学上可接受的盐已被提出，worin：X darstellt氧或硫; M = 0或1; R1 darstellt C 1 -C 3烷基; R2和R3代表氢; 或者R2和R3一起与碳原子它们连接形成C = O基团; R4和R5表示氢; 或氢R4 darstellt，R5 darstellt甲基; 或R4 darstellt甲基，R5 darstellt CH 2 R 6基团，其中R6 darstellt C 1 -C 3烷氧基羰基，羧基，羟基基团任选地用甲基或苄基substituiertem; 或R4和R5一起与碳原子它们连接形成5-或6-元杂环，其包含至少一个氧原子或氮原子与甲基OPTIONALLY substitutd; 或R4和R5一起与碳原子它们附接以形成NH基团。

    SUBSTITUTED (2R, 3R, 5R)-3-HYDROXY-(5-PYRIMIDIN-1-YL) TETRAHYDROFURAN-2-YLMETHYL ARYL PHOSPHORAMIDATES
    7.
    发明公开
    SUBSTITUTED (2R, 3R, 5R)-3-HYDROXY-(5-PYRIMIDIN-1-YL) TETRAHYDROFURAN-2-YLMETHYL ARYL PHOSPHORAMIDATES 审中-公开
    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).

    SUBSTITUTED HYDROGENATED THIENO-PYRROLO[3,2-C]PYRIDINE, LIGANDS, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR USING THE ABOVE
    9.
    发明公开
    SUBSTITUTED HYDROGENATED THIENO-PYRROLO[3,2-C]PYRIDINE, LIGANDS, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR USING THE ABOVE 审中-公开
    取代的噻吩并氢化吡咯并[3,2-c]吡啶，配体，药物组合物和方法中使用

    公开(公告)号：EP2660243A2

    公开(公告)日：2013-11-06

    申请号：EP11853469.2

    申请日：2011-12-13

    申请人： Ivachtchenko, Alexandre Vasilievich ,  Alla Chem, LLC.

    发明人： MITKIN, Oleg Dmitrievich

    IPC分类号： C07D495/14 ,  C07D495/22 ,  C07D451/02 ,  A61K31/46 ,  A61K31/439 ,  A61K31/4365 ,  A61P25/24 ,  A61P25/28

    CPC分类号： C07D495/14 ,  C07D471/04 ,  C07D495/22

    摘要： The present invention relates to novel substituted tetrahydro-4 H -thieno-pyrrolo[3,2-c]pyridines of the general formula 1, geometrical isomers, mixtures of geometrical isomers, and pharmaceutically acceptable salts thereof,

    wherein:
    Th represents annelated thienic cycle;
    W represents odinary bond (in this case R3 is bound directly to N-atom of pyrrole cycle), methylene, 1,2-ethylene, 1,2-vinyl, 1,2-ethynylene, 1,3-propanediyl or 1,3-propenylene, optionally substituted with hydroxy group;
    R1 and R2 represent hydrogen, C 1 -C 4 alkyl, halogen or -CH 2 OH;
    R3 represents hydrogen, optionally substituted phenyl, optionally substituted azaheteroaryl;
    R4 represents C 1 -C 4 alkyl, CO 2 C 2 H 5 or CO 2 C(CH 3 ) 3 ;
    R5, R6, R7 independently of each other represent hydrogen or C 1 -C 4 alkyl, or
    R5 and R6 form together ethylene bridge, and R7 represents hydrogen, or R5 and R7 form together ethylene bridge, and R6 represents hydrogen.
    And also to synthesis of novel chemical compounds, novel physiologically active compounds, "molecular tools", to pharmaceutical composition, methods for preparation thereof and to method of treatment and prophylaxis of various diseases including diseases of central nervous system (CNS).

    摘要翻译： 本发明涉及新的substituiertem四氢-4H-噻吩并吡咯并[3,2-C]通式1中，几何异构体，几何异构体的混合物，以及它们的药学上可接受的盐，吡啶类worin：钍darstellt安迟来thienic周期 ; W¯¯darstellt odinary键（在这种情况下R 3是直接结合到N-原子吡咯周期的），亚甲基，1,2-亚乙基，1,2-乙烯基，1,2-亚乙炔基，1,3-丙二基或1,3- -propenylene，任选被羟基基团substituiertem; R1和R2表示氢，C 1 -C 4烷基，卤素或-CH 2 OH; R3 darstellt氢，任选取代的苯基，任选substituiertem azaheteroaryl; R4 darstellt C 1个-C 4烷基，CO 2 C 2 H 5或CO 2 C（CH 3）3; R5，R6，R7彼此独立地表示氢或C 1 -C 4烷基，或R 5和R 6一起形成亚乙基桥，和R7 darstellt氢，或R 5和R 7一起形成亚乙基桥，和R 6表示氢。 并且还新的化学化合物，新的生理活性化合物，“分子工具”，药物组合物，其制备和治疗和各种疾病，包括中枢神经系统（CNS）疾病的预防的方法的方法合成。