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    SUBSTITUTED HYDROGENATED THIENO-PYRROLO[3,2-C]PYRIDINE, LIGANDS, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR USING THE ABOVE
    1.
    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。

    SUBSTITUTED (2R, 3R, 5R)-3-HYDROXY-(5-PYRIMIDIN-1-YL) TETRAHYDROFURAN-2-YLMETHYL ARYL PHOSPHORAMIDATES
    5.
    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 (S)-(2R,3R,5R)-3-HYDROXY-(5-PYRIMIDIN-L-YL)TETRAHYDROFURAN-2- YLMETHYL ARYL PHOSPHORAMIDATE
    6.
    发明公开
    SUBSTITUTED (S)-(2R,3R,5R)-3-HYDROXY-(5-PYRIMIDIN-L-YL)TETRAHYDROFURAN-2- YLMETHYL ARYL PHOSPHORAMIDATE 审中-公开
    （S） - （2R，3R，5R）-3-羟基 - （5-嘧啶基-L-YL）四氢呋喃-2-亚甲基 - 甲基磺酰胺

    公开(公告)号：EP3055316A1

    公开(公告)日：2016-08-17

    申请号：EP14852129.7

    申请日：2014-12-10

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

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

    IPC分类号： C07F9/177

    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).

    摘要翻译： 本发明涉及一种新的化合物，其代表式（I）的取代的氨基磷酸 - 式（2R，3R，5R）-3-羟基 - （5-嘧啶-1-基）四氢呋喃-2-基）甲基芳基氨基磷酸酯 1或其药学上可接受的盐或立体异构体，其中：R 1是（i）氢，（CH 3）2 [（CH 3）3 C] Si，任选被NR 5取代的C 2 -C 6酰基 R 6基团，其中R 5和R 6独立地是氢或C 1 -C 4烷基; （ⅱ）1-吡咯-2-基羰基，哌啶-3-基羰基或哌啶-4-基羰基; R 2和R 3是F; 或R 3为CH 3且R 2为F或OH; R 4是氢或甲基; Ar是苯基，吡啶基或萘基，其中苯基，吡啶基或萘基任选被至少一个C 1-3烷基，C 2-4链烯基，C 2-4炔基，C 1-3烷氧基，F ，Cl，Br，I，硝基，氰基，-N（C 1-3烷基）2; Pm是2,4-二氧代-3,4-二氢-2H-嘧啶-1-基或4-（4-氨基-2-氧代-2H-嘧啶-1-基），其中氨基任选被 1-吡咯-2-基羰基，哌啶-3-基羰基，哌啶-4-基羰基或C（O）R 8基团，其中R 8为（i）任选被NR 6 R 7取代的C 1 -C 4烷基 基团，其中R 6和R 7独立地是氢或C 1 -C 4烷基; （ii）任选被苯基取代的C 1-3烷氧基; X是O或N-R 9，其中R 9是任选被OH或OCH 3取代的C 1 -C 4烷基; n = 1,2或3; 以及制备方法。 该新化合物用于具有至少一种药学上可接受的赋形剂以及肌苷5单磷酸脱氢酶抑制剂，HCV蛋白酶NS3抑制剂，HCV蛋白酶NS3 / 4A抑制剂和RNA聚合酶NS5A抑制剂的药物组合物。 该新型化合物可用作病毒聚合酶HCV NS5B抑制剂，可用于治疗丙型肝炎病毒（HCV）引起的疾病。

    SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF
    8.
    发明公开
    SUBSTITUTED AZOLES, ANTI-VIRAL ACTIVE INGREDIENT, PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
    取代唑类抗病毒活性，药物组合物，其制造方法相同，它们的用途

    公开(公告)号：EP2657231A2

    公开(公告)日：2013-10-30

    申请号：EP11844522.0

    申请日：2011-11-28

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

    发明人： BICHKO, Vadim Vasilievich ,  MITKIN, Oleg Dmitrievich

    IPC分类号： C07D403/04

    CPC分类号： C07D403/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    摘要： The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B , pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In general formulas 1A and 1B

    wherein: solid lines with accompanying dotted lines ( --- ) represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is - nitrogen, the other - oxygen, sulfur or NH group; R 1 and R 2 - optionally the same radicals selected from 2-(R)- and (S)- substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)- substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates. A represents aliphatic C 2 -C 8 biradical; dioxane, cyclo- and bicycloaliphatic, alkyloxyalkyl, alkyloxyalkylenoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl biradicals and their thioanaloges; aryl and thiophene alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, alkyloxyaryl, alkenyloxyaryl, alkynyloxyaryl, alkylthioaryl, alkenylthioaryl, alkynylthioaryl, cycloalkylthiophene, aryldioxane and thiophenyldioxane biradicals. B represents: aliphatic C 2 -C 8 radical, including 1,2 or 3 triple C≡C bonds; aryl and thiophene, alkynylcycloalkyl, alkynyldioxane, alkynylaryl, alkylthiophene, alkenylthiophene and alkynylthiophene, cycloalkylbenzene, 4-cycloalkylbiphenyl, bicycloalkylbenzene, 4-bicycloalkylbiphenyl, cycloalkylthiophene, aryldioxane and thiophenyldioxane radicals.

    摘要翻译： 本发明涉及新的吡咯，通式1A和图1B，药物组合物，抗病毒药物，用于预防和治疗病毒性疾病，由hepatisis肝炎病毒（HCV）引起的特别的方法的新的抗病毒活性组分。 在通式1A和1B worin：实线伴随虚线（---）表示普通键或双键，条件没有他们中的一个是一个普通的键，另外一个是双键; X和Y接受各种含义，它们中的一个是 - 氮，其他 - 氧，硫或NH基; R 1和R 2 - 任选地从2-（R）中选择的相同自由基 - 和（S） - 取代的N-酰基吡咯烷衍生物; N-甲基-N- [2-（R）和（S） - 取代的2,2-二取代的乙酰胺; 甲基[2-（R）和（S） - 取代的（（甲基）氨基） - （1-氧代丁-2-基）-2-（R） - ]和（S） - 异丙基）-carbamates。 甲darstellt脂族C 2 -C 8二价基团; 二恶烷，环和bicycloaliphatic，烷氧基烷基，alkyloxyalkylenoxyalkyl，链烯氧基烷基，alkynyloxyalkyl双自由基及其硫代类似物; 芳基和噻吩alkynylcycloalkyl，alkynyldioxane，炔，烷基噻吩，alkenylthiophene和alkynylthiophene，alkyloxyaryl，alkenyloxyaryl，alkynyloxyaryl，alkylthioaryl，alkenylthioaryl，alkynylthioaryl，cycloalkylthiophene，aryldioxane和thiophenyldioxane双自由基。 乙darstellt：脂肪族C 2 -C 8基团，包含1,2或3倍C‰¡C键; 芳基和噻吩，alkynylcycloalkyl，alkynyldioxane，炔，烷基噻吩，alkenylthiophene和alkynylthiophene，环烷基苯，4- cycloalkylbiphenyl，bicycloalkylbenzene，4- bicycloalkylbiphenyl，cycloalkylthiophene，aryldioxane和thiophenyldioxane自由基。

    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
    9.
    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.

    CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS AS ANDROGEN RECEPTOR ANTAGONISTS, ANTI-CANCER AGENT, METHOD FOR PRODUCING AND USING SAME
    10.
    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。