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    Process for preparing synthetic intermediates of peripherally-selective inhibitors of dopamine-β-hydroxylase involving catalytic asymmetric hydrogenation
    1.
    发明授权
    Process for preparing synthetic intermediates of peripherally-selective inhibitors of dopamine-β-hydroxylase involving catalytic asymmetric hydrogenation 有权
    制备涉及催化不对称氢化的多巴胺与bgr-羟化酶周期选择性抑制剂合成中间体的方法

    公开(公告)号：US08710239B2

    公开(公告)日：2014-04-29

    申请号：US12990918

    申请日：2009-05-06

    申请人： Alexander Beliaev ,  David Alexander Learmonth

    发明人： Alexander Beliaev ,  David Alexander Learmonth

    IPC分类号： C07D405/04 ,  C07D233/84 ,  C07D487/04

    CPC分类号： C07D405/04 ,  C07D233/84 ,  C07D311/04 ,  C07D487/04

    摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.

    摘要翻译： 一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性催化剂和氢源（其中X为CH 2，氧或硫）存在下使式B化合物进行不对称氢化; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 并且R 4是烷基或芳基，其中术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

    1,3-dihydroimidazole-2-thione derivatives as inhibitors of dopamine-beta-hydroxylase
    3.
    发明授权
    1,3-dihydroimidazole-2-thione derivatives as inhibitors of dopamine-beta-hydroxylase 有权
    1,3-二氢咪唑-2-硫酮衍生物作为多巴胺-β-羟化酶的抑制剂

    公开(公告)号：US08481582B2

    公开(公告)日：2013-07-09

    申请号：US12599014

    申请日：2008-05-06

    申请人： Patrício Manuel Vieira Araújo Soares Da Silva ,  David Alexander Learmonth ,  Alexander Beliaev

    发明人： Patrício Manuel Vieira Araújo Soares Da Silva ,  David Alexander Learmonth ,  Alexander Beliaev

    IPC分类号： A61K31/4178 ,  C07D207/48

    CPC分类号： C07D405/04 ,  A61K31/4178 ,  A61K45/06

    摘要： Compounds of formula I and a method for their preparation are described: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or -alkyl-heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

    摘要翻译： 描述式I化合物及其制备方法：其中R1，R2和R3相同或不同，表示氢，卤素，烷基，硝基，氨基，烷基羰基氨基，烷基氨基或二烷基氨基; R 4表示 - 烷基 - 芳基或 - 烷基 - 杂芳基; X表示CH2，氧原子或硫原子; n为2或3; 包括单体（R） - 和（S） - 对映异构体或其对映异构体的混合物; 并且包括其药学上可接受的盐和酯。 这些化合物具有用于治疗心血管疾病如高血压和慢性心力衰竭的潜在有价值的药物性质。

    NOVEL PRECURSORS
    6.
    发明申请
    NOVEL PRECURSORS 审中-公开
    新一代前辈

    公开(公告)号：US20100292482A1

    公开(公告)日：2010-11-18

    申请号：US12739669

    申请日：2008-10-24

    申请人： David Alexander Learmonth ,  Laszlo Erno Kiss

    发明人： David Alexander Learmonth ,  Laszlo Erno Kiss

    IPC分类号： C07D213/12 ,  C07C229/30 ,  C07C255/17 ,  C07D213/80 ,  C07D213/84 ,  C07D213/78

    CPC分类号： C07D213/80 ,  C07D213/85 ,  C07D213/89 ,  Y02P20/55

    摘要： The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR′2, wherein R′ represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.

    摘要翻译： 本发明涉及式（I）化合物，其中X表示CN，COOR，其中R表示氢或羧基保护基，CONR'2，其中R'表示氢或羧基保护基，或硝基; R 1，R 2，R 3，R 4，R 5彼此独立地表示氢，C 1 -C 6烷基，卤素，三氟甲基，氰基，硝基，取代的芳基或取代的杂芳基; Y表示氢，C1-C6烷基，C3-C7环烷基，C7-C13烷芳基，三氟甲基，氰基，硝基，取代的芳基或取代的杂芳基; 并且其中上述式（I）中的立体化学未指定的双键表示E，E; E，Z; Z，E或Z，Z配置。

    1,3-Dihydroimidazole-2-Thione Derivatives as Inhibitors of Dopamine-Beta-Hydroxylase
    9.
    发明申请
    1,3-Dihydroimidazole-2-Thione Derivatives as Inhibitors of Dopamine-Beta-Hydroxylase 有权
    1,3-二氢咪唑-2-硫酮衍生物作为多巴胺-β-羟化酶抑制剂

    公开(公告)号：US20100137390A1

    公开(公告)日：2010-06-03

    申请号：US12599014

    申请日：2008-05-06

    申请人： Patricio Manuel Vieira Araüjo Soares Da Silva ,  David Alexander Learmonth ,  Alexander Beliaev

    发明人： Patricio Manuel Vieira Araüjo Soares Da Silva ,  David Alexander Learmonth ,  Alexander Beliaev

    IPC分类号： A61K31/4178 ,  C07D405/04 ,  A61P25/22 ,  A61P9/00 ,  A61P25/06 ,  A61P9/04

    CPC分类号： C07D405/04 ,  A61K31/4178 ,  A61K45/06

    摘要： Compounds of formula I and a method for their preparation are described, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or alkyl heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

    摘要翻译： 描述了式I化合物及其制备方法，其中R 1，R 2和R 3相同或不同，表示氢，卤素，烷基，硝基，氨基，烷基羰基氨基，烷基氨基或二烷基氨基; R4表示烷基 - 芳基或烷基杂芳基; X表示CH2，氧原子或硫原子; n为2或3; 包括单体（R） - 和（S） - 对映异构体或其对映异构体的混合物; 并且包括其药学上可接受的盐和酯。 这些化合物具有用于治疗心血管疾病如高血压和慢性心力衰竭的潜在有价值的药物性质。