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    • 1. 发明申请
    • CHIRAL LIGANDS
    • US20110251416A1
    • 2011-10-13
    • US13128710
    • 2009-11-13
    • Benoit PuginAdrian Wyss
    • Benoit PuginAdrian Wyss
    • C07F15/02
    • C07F17/02
    • Process for preparing ligands of the formula (1), in which R1 is C1-C8-alkyl, unsubstituted cyclopentyl, cyclohexyl, norbornyl or adamantyl, or cyclopentyl or cyclohexyl, substituted by 1 to 3 C1-C4-alkyl or C1-C4-alkoxy, or benzyl, phenyl, naphthyl and anthryl which are unsubstituted or substituted by 1 to 3 C1-C4-alkyl, C1-C4-alkoxy, C1-C4-fluoroalkyl or C1-C4-fluoroalkoxy, F and Cl, each of R2 and R3 is independently a C-bonded hydrocarbon radical or a heterohydrocarbon radical, and R4 is C1-C4-alkyl, cyclopentyl, cyclohexyl, phenyl, methylphenyl, methylbenzyl or benzyl, which comprises (a) stereoselective metallation in ortho position to the amine side-chain of a compound of formula (A) in which R4 is as defined above, reaction with a dihalide of formula R1—PX2 in which R1 is as defined above and X is Cl or Br, stereoselective hydrolysis to give a compound containing an SPO group, and reaction with a secondary phosphine of formula H—PR2R3 in which R2 and R3 are as defined above, to give the compounds of formula (1). New ligands obtained by that process and metal complexes thereof.
    • 制备式(1)配体的方法,其中R 1是被1至3个C 1 -C 4 - 烷基或C 1 -C 4 - 烷基取代的C 1 -C 8 - 烷基,未被取代的环戊基,环己基,降冰片基或金刚烷基或环戊基或环己基, 烷氧基或苄基,未被取代或被1至3个C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 氟代烷基或C 1 -C 4 - 氟烷氧基,F和Cl各自取代的苯基,萘基和蒽基,每个R 2 并且R 3独立地是C键合的烃基或杂烃基,R 4是C 1 -C 4 - 烷基,环戊基,环己基,苯基,甲基苯基,甲基苄基或苄基,其包括(a)在邻近位置的立体选择性金属化 - 其中R 4如上定义的式(A)化合物与式R1-PX2的二卤化物反应,其中R 1如上定义,X​​是Cl或Br,立体选择性水解,得到含有SPO的化合物 并与式H-PR2R3的仲膦反应,其中R2和R3如上定义 得到式(1)的化合物。 通过该方法获得的新配体及其金属络合物。
    • 9. 发明申请
    • NOVEL NUTRACEUTICAL COMPOSITIONS AND USE THEREOF
    • 新型营养组合物及其用途
    • US20100166859A1
    • 2010-07-01
    • US12160823
    • 2006-12-29
    • Luppo EdensRegina GoralczykAdrian Wyss
    • Luppo EdensRegina GoralczykAdrian Wyss
    • A61K38/06C07K4/00A61P25/24A61P25/28A61K9/28
    • A61K45/06A23L33/18A61K38/06
    • The invention relates to a novel nutraceutical composition containing at least one tripeptide as active ingredient. The term “nutraceutical' as used herein denotes a usefulness in both the nutritional and pharmaceutical field of application. Thus, the novel nutraceutical compositions can find use as supplement to food and beverages, and as pharmaceutical formulations for enteral or parenteral application which may be solid formulations such as capsules or tablets, or liquid formulations, such as solutions or suspensions. As will he evident from the foregoing, the term nutraceutical composition also comprises food and beverages containing the above-specified active ingredients, for example protein hydrolysates which are rich in tripeptides according to the invention. The compositions are useful to improve cognitive functions such as learning, memory and alertness and for the treatment of a disorder connected to impaired neurotransmission and of conditions resulting from hypoxia and for alleviating neuropathic pain.
    • 本发明涉及含有至少一种三肽作为活性成分的新型营养组合物。 本文所用的术语“营养制品”表示在营养和制药领域中的有用性。 因此,新型营养食品组合物可以用作食品和饮料的补充剂,以及用作肠内或肠胃外应用的药物制剂,其可以是固体制剂如胶囊或片剂,或液体制剂,例如溶液或悬浮液。 从上文可以看出,术语营养药物组合物还包含含有上述活性成分的食品和饮料,例如富含根据本发明的三肽的蛋白质水解产物。 该组合物可用于改善认知功能,例如学习,记忆和警觉性,以及治疗与受损的神经传递相关的病症以及由缺氧引起的疾病和减轻神经性疼痛。