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    • 11. 发明申请
    • Method for the production of aldehydes and ketones by oxidizing primary and secondary alcohols with alkylphosphonic acid anhydrides
    • 通过用烷基膦酸酐氧化伯醇和仲醇生产醛和酮的方法
    • US20070191645A1
    • 2007-08-16
    • US10592439
    • 2005-04-18
    • Andreas MeudtStefan SchererClaudius Boehm
    • Andreas MeudtStefan SchererClaudius Boehm
    • C07C45/37
    • C07C45/29C07B41/06C07C269/06C07C47/21C07C47/54C07C49/10C07C271/22
    • The invention relates to a method for the production of a.) aldehydes of formula (II): R1—CHO and b.) aldehydes of formula (III): R1—C(O)—R2 by reacting a.) primary alcohols (R1CH2—OH) or b.) secondary alcohols (R1—CH(OH)—R2) with cyclic phosphonic acid anhydrides in the presence of dialkyl-, diaryl- and/or alkyl-aryl sulphonic oxides at a temperature in the region of between −100 to +120° C., whereby R1 and/or R2 represent H, a substituted linear or branched C1-C12-alkyl radical, a substituted C3-C10 cycloalkyl-, alkenyl-, aryl- or heteroaryl radical. A cyclic phosphonic acid anhydride is used, preferably, as a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane of formula (I), wherein R′ independently represents allyl, aryl or open-chained or branched C1-C12-alkyl-radicals. Optionally, the reaction can be carried out in the presence of a tertiary amine base NR53.
    • 本发明涉及一种制备式(II)的醛的方法:R 1 -CHO和b)式(III)的醛:R 1〜 通过使a。)伯醇(R 1 CH 2 CH 2 -OH)或b。)二级(C 1 -C 4) 在二烷基 - ,二芳基 - 和/或烷基 - 芳基磺酸氧化物的存在下,与环状膦酸酐反应,得到醇(R 1 -CH 2(OH)-R 2) 在-100至+ 120℃之间的区域中的温度,其中R 1和/或R 2表示H,取代的直链或支链C 1〜 取代的C 3 -C 10 - 环烷基 - ,链烯基 - ,芳基 - 或杂芳基(C 1 -C 6) 激进。 优选使用环状膦酸酐作为式(I)的2,4,6-取代的1,3,5,2,4,6-三氧杂三磷杂环己烷,其中R'独立地表示烯丙基,芳基或开链 或支链C 1 -C 12 - 烷基 - 基团。 任选地,反应可以在叔胺碱NR 5 SO 3存在下进行。
    • 13. 发明授权
    • Process for preparing bisallylboranes and nonaromatic boronic acids
    • 制备双烯丙基硼烷和非芳族硼酸的方法
    • US06855848B2
    • 2005-02-15
    • US10650370
    • 2003-08-28
    • Stefan SchererAlexei KalininVictor Snieckus
    • Stefan SchererAlexei KalininVictor Snieckus
    • C07F5/02C07F5/04
    • C07F5/027
    • A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant: in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R114 R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).
    • 一种通过使二烯与硼氢化钠在氧化剂存在下反应来制备式(I)的双烯丙基硼烷的方法:在惰性溶剂中,所产生的硼烷与二烯选择性地反应生成二(烯丙基)硼烷, 式(I)和具有以下含义的取代基R 1至R 6具有以下含义:R 14 R 6为H,芳基或取代或未取代的C 1 -C 4 - 烷基或两个基团R可为 封闭以形成环状体系。作为氧化剂,可以使用例如烷基卤化物或二烷基硫酸盐。 在一个特别优选的实施方案中,所用的二烯是2,5-二甲基己-1,4-二烯(R 1,R 2,R 5,R 6 =甲基,R 3,R 4)= H)。
    • 17. 发明申请
    • RESPONSIVENESS TO ANGIOGENESIS INHIBITORS
    • 对血液生成抑制剂的反应
    • US20120195858A1
    • 2012-08-02
    • US13388840
    • 2010-08-03
    • Dorothee FoernzlerPaul DelmarStefan SchererDiether LambrechtsPeter Carmeliet
    • Dorothee FoernzlerPaul DelmarStefan SchererDiether LambrechtsPeter Carmeliet
    • A61K38/21A61P35/00C07H21/04A61K39/395C12Q1/68
    • C12Q1/6886C12Q2600/106C12Q2600/156
    • The present invention relates to methods for improving the overall survival of a patient suffering from a malignant disease or a disease involving physiological and pathological angiogenesis by treatment with an angiogenesis inhibitor, such as bevacizumab, by determining the presence of one or more variant alleles of the vascular endothelial growth factor receptor 1 (VEGFR-1) gene. The present invention further provides methods for improving the progression-free survival of a patient suffering from a malignant disease or a disease involving physiological and pathological angiogenesis by treatment with an angiogenesis inhibitor, such as bevacizumab, by determining the presence of one or more variant alleles of the VEGFR-1 gene. The present invention also provides for methods for assessing the responsiveness of a patient to an angiogenesis inhibitor by determining the presence of one or more variant alleles of the VEGFR-1 gene.
    • 本发明涉及通过用血管生成抑制剂如贝伐珠单抗治疗来改善患有恶性疾病或涉及生理和病理性血管发生的疾病的患者的整体存活的方法,通过确定一种或多种变异等位基因的存在, 血管内皮生长因子受体1(VEGFR-1)基因。 本发明进一步提供了通过用血管生成抑制剂如贝伐单抗进行治疗来改善患有恶性疾病或涉及生理和病理性血管发生的疾病的患者的无进展生存的方法,通过确定一种或多种变异等位基因的存在 的VEGFR-1基因。 本发明还提供了通过确定VEGFR-1基因的一个或多个变异等位基因的存在来评估患者对血管生成抑制剂的反应性的方法。