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    PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR
    2.
    发明申请
    PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR 审中-公开
    血小板生成素受体激动剂的制备方法

    公开(公告)号：WO2014177517A1

    公开(公告)日：2014-11-06

    申请号：PCT/EP2014/058610

    申请日：2014-04-28

    申请人： ESTEVE QUÍMICA, S.A. ,  GALCHIMIA, S.A.

    发明人： BARTRA SANMARTÍ, Martí ,  SOLSONA ROCABERT, Joan Gabriel ,  CRUCES COLADO, Jacobo ,  ENJO BABIO, Juan ,  PAMPÍN CASAL, María Begoña

    IPC分类号： C07C205/59 ,  C07C201/12 ,  C07D231/22 ,  C07C227/04 ,  C07C249/16

    CPC分类号： C07C201/12 ,  C07C205/59 ,  C07C227/04 ,  C07C249/16 ,  C07D231/22 ,  C07C229/70 ,  C07C251/76

    摘要： It relates to a preparation process of 2'-(benzyloxy)-3'-nitro-1,1'-biphenyl-3- carboxylic acid or a salt thereof comprising reacting 2-(benzyloxy)-1-bromo- 3-nitrobenzene with a either 3-carboxyphenylboronic acid or a salt thereof or a (C 1 -C 4 )-alkyl ester thereof in the presence of Pd(OAc) 2 , tricydohexylphosphine, a base, an appropriate solvent, and at an appropriate temperature; if appropriate, submitting the compound thus obtained to a hydrolysis reaction; and isolating the compound thus obtained in form of a salt of compound of formula (VI) or in form of the free acid by adding an acid. It also comprises the further preparation to eltrombopag or its salts from the new intermediate thus obtained by subsequent reduction of the nitro group and deprotection of the phenol, conversion of the amine intermediate obtained in a diazonium derivative, and either (1) subsequent reaction with ethyl acetoacetate and with (3,4-dimethylphenyl)hydrazine or a salt thereof, occurring the pyrazole ring formation by intermolecular cyclization, or (2) introduction of the pyrazole ring by reaction with 1-(3,4-dimethylphenyl)-3-methyl-3-pyrazolin-5-one.

    摘要翻译： 本发明涉及2' - （苄氧基）-3'-硝基-1,1'-联苯-3-甲酸或其盐的制备方法，其包括使2-（苄氧基）-1-溴-3-硝基苯与 在Pd（OAc）2，三羟基己基膦，碱，适当的溶剂和适当的温度存在下，3-羧基苯基硼酸或其盐或其（C 1 -C 4） - 烷基酯; 如果合适，将由此获得的化合物提交至水解反应; 并通过添加酸分离由式（VI）化合物的盐形成的化合物或游离酸形式的化合物。 它还包括通过随后还原硝基和脱保护苯酚得到的新中间体进一步制备埃曲波帕或其盐，以及在重氮衍生物中获得的胺中间体的转化，以及（1）随后的反应与乙基 乙酰乙酸酯和（3,4-二甲基苯基）肼或其盐，通过分子间环化形成吡唑环，或（2）通过与1-（3,4-二甲基苯基）-3-甲基 -3-吡唑啉-5-酮。

    METHOD OF PRODUCING THERAPEUTIC AGENT
    3.
    发明申请
    METHOD OF PRODUCING THERAPEUTIC AGENT 审中-公开
    生产治疗剂的方法

    公开(公告)号：WO2014172326A1

    公开(公告)日：2014-10-23

    申请号：PCT/US2014/034109

    申请日：2014-04-15

    申请人： WARNER, Deborah

    发明人： WARNER, Deborah

    IPC分类号： A01N37/30 ,  A61K31/205

    CPC分类号： C07C51/43 ,  C07B2200/13 ,  C07C227/42 ,  C07C59/255 ,  C07C229/70

    摘要： A method for producing a therapeutic agent [10] and the agent [10] thus produced. This therapeutic agent [10], referred to as D-boramine [10], has the following chemical formula: [(CH 3 ) 3 NCH 2 CHOHCH 2 CO 2 H] 2 [O 2 CCHOHCHOHCO 2 ] and has the following empirical formula: C 18 H 36 N 2 O 12 . The D-boramine [10] is produced by allowing a reaction between approximately 500mg of L-carnitine and approximately 2.5 mg of pyridoxal 5 phosphate in the presence of approximately 10 mg of fumaric acid. The reaction creates the D-boramine [10] molecule as the reaction product. The D-boramine [10] molecule has an orthorhombic crystalline structure and has been shown to be useful as a therapeutic agent in treating a variety of human cancers, ailments and diseases.

    摘要翻译： 由此制备治疗剂[10]和药剂[10]的方法。 这种称为D-硼胺[10]的治疗剂[10]具有以下化学式：[（CH3）3NCH2CHOHCH2CO2H] 2 [O2CCHOHCHCOCO2]，具有以下经验式：C 18 H 36 N 2 O 12。 在大约10mg富马酸的存在下，通过允许大约500mg左旋肉碱和约2.5mg吡哆醛5磷酸酯之间的反应来制备D-硼胺[10]。 该反应产生作为反应产物的D-硼胺[10]分子。 D-boramine [10]分子具有斜方晶体结构，已被证明可用作治疗各种人类癌症，疾病和疾病的治疗剂。

    NAPHTHALENESULPHONIC OR CARBOXYLIC ACIDS AND THEIR USE AS ATYPICAL BETA-ADRENOCEPTOR AGONISTS
    5.
    发明申请
    NAPHTHALENESULPHONIC OR CARBOXYLIC ACIDS AND THEIR USE AS ATYPICAL BETA-ADRENOCEPTOR AGONISTS 审中-公开
    萘二酚或羧酸及其作为原位β-受体激动剂的用途

    公开(公告)号：WO98043953A1

    公开(公告)日：1998-10-08

    申请号：PCT/EP1998/001845

    申请日：1998-03-31

    IPC分类号： C07C229/70 ,  C07C309/47 ,  C07C309/35 ,  A61K31/185 ,  A61K31/19 ,  C07C229/68

    CPC分类号： C07C229/70 ,  C07C309/47

    摘要： The invention relates to a compound of formula (I) wherein the groups N(R ) and R are separated by at least 4 ring carbon atoms; R represents a phenyl, naphthyl, phenoxymethyl, thiazolyl, pyridyl or pyrimidyl group, optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, NR R , and NHSO2R ; R represents hydrogen or C1-6alkyl; R represents hydrogen or C1-4alkyl; R represents CO2R or SO3H; R represents one or more groups independently selected from hydrogen, C1-6alkyl, halogen, trifluoromethyl and C1-6alkoxy; n represents an integer from 1-6; R and R independently represent hydrogen or C1-4alkyl; or pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.

    摘要翻译： 本发明涉及式（I）化合物，其中基团N（R 3）和R 4被至少4个环碳原子分开; R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基，三氟甲基，硝基， 6> R 7和NHSO 2 R 6; R 2表示氢或C 1-6烷基; R 3表示氢或C 1-4烷基; R 4表示CO 2 R 6或SO 3 H; R 5表示一个或多个独立地选自氢，C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的基团; n表示1-6的整数; R 6和R 7独立地表示氢或C 1-4烷基; 或其药学上可接受的衍生物，其制备方法及其用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

    NEW COMPOUNDS
    9.
    发明申请
    NEW COMPOUNDS 审中-公开
    新化合物

    公开(公告)号：WO1994019315A1

    公开(公告)日：1994-09-01

    申请号：PCT/SE1994000152

    申请日：1994-02-22

    申请人： AKTIEBOLAGET ASTRA ,  THE UNIVERSITY OF MARYLAND ,  BJÖRK, Susanna, Karin, Maria ,  GOTTHAMMAR, Kristina, Birgitta ,  LINDERBERG, Mats, Torbjörn ,  LUTHMAN, Per, Johan ,  PERSSON, Kerstin, Margareta, Irma ,  SCHWARCZ, Robert

    发明人： AKTIEBOLAGET ASTRA ,  THE UNIVERSITY OF MARYLAND

    IPC分类号： C07C229/64

    CPC分类号： C07C205/59 ,  C07C205/26 ,  C07C205/37 ,  C07C229/64 ,  C07C229/70 ,  C07C255/59 ,  C07C2602/10

    摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of general formula (I), wherein R and R are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R , R are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z-R wherein Z is selected from CHn, NHm, O, S, SO2 and CO wherein n = 1 or 2; m = 0 or 1 and R is selected from alkyl, aryl and fluoroalkyl; or R and R together form a saturated or unsaturated ring system Y-V-Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C1-C3 alkylene or alkenylene, -N = , -N = N- and (a), wherein R7 = H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.

    摘要翻译： 本发明涉及通式（I）的3-羟基邻氨基苯甲酸3-HANA的新衍生物，其中R 1和R 2相同或不同并且选自H和烷基; X选自烷硫基，芳硫基，芳氧基，卤素和氰基; R 3，R 4相同或不同，并且选自卤素，甲基，氟烷基，氰基和ZR 5，其中Z选自CH n，NH m，O，S，SO 2和CO，其中n = 1或 2; m = 0或1，R 5选自烷基，芳基和氟烷基; 或R 3和R 4一起形成饱和或不饱和的环系YVZ，其中Y和Z彼此独立地如上述Z所定义，V选自C 1 -C 3亚烷基或亚烯基，-N = ，-N = N-和（a），其中R7 = H或烷基; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责产生内源性神经毒素喹啉酸QUIN的3-羟基 - 邻氨基苯甲酸加氧酶3-HAO的用途。