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    VERFAHREN ZUR HERSTELLUNG VON AROMATISCHEN UND HETEROAROMATISCHEN CARBONSÄUREN, CARBONSÄUREESTERN UND CARBONSÄUREAMIDEN
    43.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON AROMATISCHEN UND HETEROAROMATISCHEN CARBONSÄUREN, CARBONSÄUREESTERN UND CARBONSÄUREAMIDEN 有权
    用于生产芳族和杂芳族羧酸，羧酸和羧酸酯的酰胺

    公开(公告)号：EP2282986A1

    公开(公告)日：2011-02-16

    申请号：EP09753852.4

    申请日：2009-05-25

    申请人： BASF SE

    发明人： CHALLAND, Nina ,  ALTENHOFF, Ansgar, Gereon ,  SCHMIDT-LEITHOFF, Joachim ,  WISSEL-STOLL, Kathrin ,  RACK, Michael ,  RHEINHEIMER, Joachim

    IPC分类号： C07C51/10 ,  C07C67/36 ,  C07C231/00 ,  C07C231/02 ,  C07C63/04 ,  C07C69/76 ,  C07C235/84

    CPC分类号： C07C231/10 ,  C07C51/10 ,  C07C67/36 ,  C07C63/04 ,  C07C69/76 ,  C07C235/84

    摘要： Method for producing aromatic and heteroaromatic carboxylic acids, carboxylic acid esters and carboxylic acid amides through the reacting of aromatic or heteroaromatic halogenides R-X
    n , where n = a whole number from 1 to 6, R = a substituted or unsubstituted, aromatic or heteroaromatic radical and X = a chlorine, bromine or iodine atom; with carbon monoxide and water, ammonia, alcohols or amines in the presence of bases and nonvalent or bivalent palladium compounds and bidentate diphosphanes or complexes of nonvalent or bivalent palladium with bidentate diphosphanes, in which bidentate diphosphanes are used (R
    1- )(R
    2- )P-Y-P(-R
    3 )(-R
    4 ), with R
    1 to R
    4 =, unsubstituted aryl radicals or aryl radicals that are substituted with at least one radical having a positive resonance effect or a positive inductive effect, or unsubstituted or substituted cycloalkyl radicals; and Y = hydrocarbon groups with a total of 2 to 20 carbon atoms, wherein at least one of the carbon atoms carried only one or no hydrogen atom as a substituent; excepting the reaction of 4-bromo-3-difluoromethyl-1 -methylpyrazol with 2-(3,4,5-trifluoorphenyl)aniline and carbon monoxide to form N-[2-(3,4,5-Trifluorophenyl)phenyl]-3- difluoromethyl-1 -methylpyrazol-4-carboxylic acid amide.

    摘要翻译： 过程用于制备芳族和杂芳族羧酸，羧酸酯和羧酰胺通过芳族或杂芳族卤化物R-Xn中的反应，其中n =整数1〜6，R = substituiertem奥德unsubstituiertem和芳族或杂芳族基团和X =氯，溴或碘原子，与一氧化碳和水，氨，在碱和零价或二价钯化合物和双齿diphosphanes或零价或二价钯与二齿diphosphanes的络合物的存在下的醇或cardamines，其中 使用了二齿diphosphanes（R1 - ）的（R 2）p-Y-P（-R 3）（ - R 4），其中R 1至R 4 =芳基unsubstituiertem自由基或芳基用至少一个基团表现出正的共振效应substituiertem 或正感应效应，或unsubstituiertem或substituiertem环烷基，和Y =烃基含总共2至20个碳原子，其中至少部分的碳原子中的一个仅携带一个或没有水合 罗根原子作为取代基; 除了4-溴-3-二氟甲基-1-甲基吡的反应与2-（3,4,5-三氟苯基）苯胺和一氧化碳，得到N- [2-（3,4,5-三氟苯基）苯基] -3-二氟甲基-1-甲基吡唑-4-甲酰胺。

    CONTRAST AGENTS
    45.
    发明公开
    CONTRAST AGENTS 审中-公开
    对比剂

    公开(公告)号：EP2245003A2

    公开(公告)日：2010-11-03

    申请号：EP09715655.8

    申请日：2009-02-26

    申请人： GE Healthcare AS ,  Priebe, Hanno

    发明人： PRIEBE, Hanno

    IPC分类号： C07C235/66 ,  C07C235/84 ,  C07D309/10 ,  C07C233/09 ,  A61K49/04

    CPC分类号： A61K49/04 ,  A61K49/0438 ,  B22D11/1287 ,  B23K9/048 ,  B23K35/02 ,  B23K35/0261 ,  B23K35/30 ,  B23K35/3086 ,  B23K2201/04 ,  B23K2203/04 ,  C07C235/66 ,  C07C235/84 ,  C07D309/10 ,  C22C38/18 ,  C22C38/26

    摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula R-N(CO-CH
    3 ) — X— N(CO-CH
    3 )- R and salts or optical active isomers thereof, wherein X denotes a divalent linking moiety with 5 to 10 bridge elements of carbon, oxygen, sulphur and nitrogen separating the acetylated nitrogen atoms, and which may be further substituted by hydroxyl groups, by C
    1 to C
    4 alkyl moieties optionally substituted by hydroxyl groups, by C
    1 to C
    4 alkoxy groups, by amino groups and by C
    1 to C
    4 alkylamino groups, and wherein 2 or 3 carbon bridge elements together with alkyl or alkoxy groups form a cyclopentane, cyclohexane, pentahydropyran or tetrahydrofuran entity which may be alkyl- or hydroxyalkyl- substituted and each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

    摘要翻译： 本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。 更具体地说，含碘化合物是含有两个通式为RN（CO-CH 3）-X-N（CO-CH 3）-R的连接碘化苯基的化合物及其盐或光学活性异构体，其中X表示 二价连接部分与碳原子，氧原子，硫原子和氮原子的5至10个桥联元素分隔乙酰化的氮原子，并且可以被羟基进一步取代，被C 1至C 4烷基部分任选地被羟基取代，被C 1 至C 4烷氧基，氨基和C 1至C 4烷基氨基，并且其中2或3个碳桥基与烷基或烷氧基一起形成环戊烷，环己烷，五氢吡喃或四氢呋喃实体，其可以是烷基或羟烷基 - 取代的并且每个R表示进一步被亲水部分取代的三碘代苯基残基。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中，特别是在X射线成像中的用途，以及含有这种化合物的造影剂。

    NEW COMPOUNDS I
    49.
    发明公开
    NEW COMPOUNDS I 审中-公开
    新化合物我

    公开(公告)号：EP1881950A1

    公开(公告)日：2008-01-30

    申请号：EP06733400.3

    申请日：2006-05-08

    申请人： AstraZeneca AB

    发明人： JONASSON, Catrin ,  MOLIN, Håkan ,  ROTTICCI, Didier

    IPC分类号： C07C43/253 ,  A61K31/22 ,  A61K31/275 ,  A61K31/41 ,  A61P29/00 ,  C07C235/58 ,  C07C235/84 ,  C07C255/56 ,  C07C257/04

    CPC分类号： C07C255/56 ,  C07C43/2055 ,  C07C235/58 ,  C07C235/84

    摘要： A compound of formula (I), or pharmaceutically acceptable salts thereof wherein X is selected from hydrogen, halo, -CN, -CON2, -CON(C1-6alkyl)H, -CON(C1-6alkyl)2 and heterocyclic groups; R1 is selected from C1-6alkyl and C3-6cycloalkyl; whereby Z is -OH, M is selected from C(O)- , -CH(ORa) , N(Ra) , and S(O)r-, wherein Ra is hydrogen or C1-6alkyl and r is 0, 1 or 2, R2 is selected from C1-6alkyl, C3-6cycloalkyl, heterocycloalkyl, aryl, alkylaryl, and heteroaryl, R2 is substituted with halo, -NO2, -CN, -OH, -CF3, -OCF3, -NH2, and/or -CONH2, when Y is -C1-6alkyl; or Z is -C1-6alkoxy, M is bond, R2 is selected from C1-6alkyl, C3-6cycloalkyl, heterocycloalkyl, aryl, alkylaryl, and heteroaryl, when Y is -C1-6alkoxy.