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    MEANS AND METHODS FOR ASSESSING LIVER TOXICITY
    5.
    发明申请
    MEANS AND METHODS FOR ASSESSING LIVER TOXICITY 审中-公开
    用于评估肝脏毒性的方法和方法

    公开(公告)号：WO2009153136A3

    公开(公告)日：2010-03-18

    申请号：PCT/EP2009056367

    申请日：2009-05-26

    Applicant: BASF SE ,  VAN RAVENZWAAY BENNARD ,  MELLERT WERNER ,  COELHO PALERMO CUNHA GEORGIA ,  FABIAN ERIC ,  STRAUSS VOLKER ,  KAMP HENNICKE ,  WALK TILMANN B ,  LOOSER RALF ,  HEROLD MICHAEL MANFRED ,  WIEMER JAN C ,  PROKOUDINE ALEXANDRE ,  LEIBOLD EDGAR

    Inventor： VAN RAVENZWAAY BENNARD ,  MELLERT WERNER ,  COELHO PALERMO CUNHA GEORGIA ,  FABIAN ERIC ,  STRAUSS VOLKER ,  KAMP HENNICKE ,  WALK TILMANN B ,  LOOSER RALF ,  HEROLD MICHAEL MANFRED ,  WIEMER JAN C ,  PROKOUDINE ALEXANDRE ,  LEIBOLD EDGAR

    IPC: G01N33/66 ,  G01N33/82 ,  G01N33/84 ,  G01N33/92

    CPC classification number: G01N33/92 ,  G01N2500/00 ,  G01N2560/00 ,  G01N2800/085 ,  G01N2800/60 ,  Y02A90/26

    Abstract: The present invention pertains to the field of toxicological assessments for risk stratification of chemical compounds. Specifically, it relates to a method for diagnosing liver toxicity. It also relates to a method of determining whether a compound is capable of inducing such liver toxicity in a subject and to a method of identifying a drug for treating liver toxicity. Furthermore, the present invention relates to a data collection comprising characteristic values of at least five metabolites, a data storage medium comprising said data collection, and a system and a device for diagnosing liver toxicity. Finally, the present invention- pertains to the use of a group of metabolites or means for the determination thereof for the manufacture of a diagnostic device or composition for diagnosing liver toxicity in a subject. For each sex, a different metabolome pattern, i.e. a different set of analytes is disclosed. The liver toxicity markers are mainly selected from free fatty acids, but also include various phosphatidylcholines, Hydroxyphenylpyruvic acid, alpha-Tocopherol, Cholesterol,myo-Inositol-2-monophosphate, 4-Hydroxysphinganine, Ceramide (dl8:1, C24:1), Ceramide (dl8:2, C24:0), Sphingomyelin (dl8:1, C16:0), 1, 2-Dioleoyl-sn-glycero-3-phosphatidyl-L-serine, 18:1 Lyso Phosphatidylcholine, CoenzymeQ9, Glucose, Glycerol, Glycerophosphates, Phosphate, 5-Methoxysphingosine, erythrosphingosine, Threonine, Diacylglycerides and Triacylglycerides.

    Abstract translation: 本发明涉及化学化合物危险分层的毒理学评估领域。 具体地说，涉及一种诊断肝毒性的方法。 它还涉及确定化合物是否能够在受试者中诱导这种肝毒性的方法以及鉴定用于治疗肝毒性的药物的方法。 此外，本发明涉及包含至少五种代谢物的特征值的数据收集，包括所述数据收集的数据存储介质，以及用于诊断肝脏毒性的系统和装置。 最后，本发明涉及一组代谢物或方法用于制备用于诊断受试者的肝脏毒性的诊断装置或组合物的用途。 对于每个性别，公开了不同的代谢组织模式，即不同的分析物组。 肝毒性标志物主要选自游离脂肪酸，还包括各种磷脂酰胆碱，羟基苯基丙酮酸，α-生育酚，胆固醇，肌醇-2-单磷酸，4-羟基鞘氨醇，神经酰胺（dl8：1，C24：1） 神经酰胺（dl8：2，C24：0），鞘磷脂（dl8：1，C16：0），1,2-二油酰-sn-甘油-3-磷脂酰-L-丝氨酸，18:1溶血磷脂酰胆碱，辅酶Q9，葡萄糖， 甘油，磷酸甘油酯，磷酸酯，5-甲氧基肌氨酸，红细胞素，苏氨酸，二酰基甘油酯和三酰基甘油酯。

    SULFONAMIDE COMPOUNDS
    9.
    发明申请
    SULFONAMIDE COMPOUNDS 审中-公开
    磺酰胺化合物

    公开(公告)号：WO2009153285A2

    公开(公告)日：2009-12-23

    申请号：PCT/EP2009057531

    申请日：2009-06-17

    Applicant: BASF SE ,  DEYN WOLFGANG VON ,  PUHL MICHAEL ,  POHLMAN MATTHIAS ,  RACK MICHAEL ,  PARRA RAPADO LILIANA ,  LANGEWALD JUERGEN ,  ANSPAUGH DOUGLAS D ,  OLOUMI-SADEGHI HASSAN ,  CULBERTSON DEBORAH L ,  RANKL NANCY B ,  KAMP HENNICKE ,  VAN RAVENZWAAY BENNARD

    Inventor： VON DEYN WOLFGANG ,  PUHL MICHAEL ,  POHLMAN MATTHIAS ,  RACK MICHAEL ,  PARRA RAPADO LILIANA ,  LANGEWALD JUERGEN ,  ANSPAUGH DOUGLAS D ,  OLOUMI-SADEGHI HASSAN ,  CULBERTSON DEBORAH L ,  RANKL NANCY B ,  KAMP HENNICKE ,  VAN RAVENZWAAY BENNARD

    IPC: C07D417/06 ,  A01N43/80 ,  C07D417/14

    CPC classification number: C07D417/06 ,  A01N43/80 ,  C02F1/001 ,  C02F2209/03 ,  C02F2303/16 ,  C07D417/14

    Abstract: The present invention relates to sulfonamide compounds of formula (I) wherein R1 is H, halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylthio, C2-C6-alkenylthio, C2-C6-alkynylthio, C1-C6-haloalkyl or C1-C6-haloalkoxy; R2 and R3 are H, halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylthio, C2-C6-alkenylthio, C2-C6-alkynylthio, C1-C6-haloalkyl or C1-C6-haloalkoxy; or R2 together with R3 form a fused 5 or 6-membered carbocycle or heterocycle; R4 is halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, C1-C6-haloalkyl, C1-C6-haloalkoxy, C1-C6-haloalkylthio, C1-C6-haloalkylsulfinyl or C1-C6-haloalksulfonyl; n is 0, 1, 2 or 3; R5 is phenyl or a 5- or 6-membered heterocycle; X is O or NRx, wherein Rx is H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylcarbonyl or C1-C6-alkylcarbonyloxy; Y is N or C(Ry), wherein Ry is H, halogen, CN, C1-C6-alkyl,C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C3-7-cycloalkyl- C1-C4-alkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylthio, C2-C6-alkenylthio, C2-C6-alkynylthio, C1-C6-haloalkyl and C1-C6-haloalkoxy; and Z is a chemical bond, O or N(Rz), wherein Rz is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C1-C6-alkylcarbonyl or C1-C6-alkylcarbonyloxy; as well as to the N-oxides and salts thereof. These compounds are useful for combating animal pests. The invention also relates to a process for the preparation of these compounds and to intermediate compounds used in said process. The invention further relates to a method for controlling animal pests by using the compounds of formula (I), the N-oxides or the salts thereof, to plant propagation material and to an agricultural and veterinary composition comprising said compounds, the N-oxides or the salts thereof.

    Abstract translation: 本发明涉及式（I）的磺酰胺化合物，其中R1是H，卤素，CN，C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，C3-C7-环烷基，C3-C7-环烷基 C 1 -C 4 - 烷基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烯氧基，C 2 -C 6 - 炔氧基，C 1 -C 6 - 烷硫基，C 2 -C 6 - 烯硫基，C 2 -C 6 - 炔硫基，C 1 -C 6 - 卤代烷基或C 1 1 -C 6 - 卤代烷氧基; R2和R3是H，卤素，CN，C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，C3-C7-环烷基，C3-C7-环烷基-C1-C4-烷基，C1-C6- 烷氧基，C 2 -C 6 - 烯氧基，C 2 -C 6 - 炔氧基，C 1 -C 6 - 烷硫基，C 2 -C 6 - 烯硫基，C 2 -C 6炔硫基，C 1 -C 6卤代烷基或C 1 -C 6卤代烷氧基; 或R 2与R 3一起形成稠合的5或6元碳环或杂环; R4是卤素，CN，C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，C1-C6-烷氧基，C1-C6-烷硫基，C1-C6-烷基亚磺酰基，C1-C6-烷基磺酰基，C1- C 1 -C 6卤代烷基，C 1 -C 6卤代烷硫基，C 1 -C 6卤代烷基亚磺酰基或C 1 -C 6卤代磺酰基; n为0,1,2或3; R5是苯基或5-或6-元杂环; X是O或NR x，其中Rx是H，C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烯氧基，C 2 -C 6 - 炔基氧基，C 1 -C 6 - 烷基羰基或C 1 -C 6烷基羰基氧基; Y是N或C（Ry），其中R y是H，卤素，CN，C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，C 3 -C 7 - 环烷基，C 3-7 - C 1 -C 6烷基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烯氧基，C 2 -C 6 - 炔氧基，C 1 -C 6 - 烷硫基，C 2 -C 6 - 烯硫基，C 2 -C 6 - 炔硫基， 卤代烷氧基; Z为化学键，O或N（Rz），其中Rz为C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，C3-C7-环烷基，C1-C6-烷氧基，C2-C6 - 烯氧基，C1-C6-烷基羰基或C1-C6-烷基羰基氧基; 以及N-氧化物及其盐。 这些化合物可用于对抗动物害虫。 本发明还涉及制备这些化合物的方法和用于所述方法的中间体化合物。 本发明还涉及通过使用式（I）化合物，其N-氧化物或其盐来植物繁殖材料以及包含所述化合物，N-氧化物或其盐的农业和兽医组合物来控制动物害虫的方法 其盐。

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