Preparation of N-(1-alkoxyalkyl)formamide and bis formamides
    11.
    发明授权
    Preparation of N-(1-alkoxyalkyl)formamide and bis formamides 失效
    制备N-(1-烷氧基烷基)甲酰胺和双甲酰胺

    公开(公告)号:US5117056A

    公开(公告)日:1992-05-26

    申请号:US631597

    申请日:1990-12-21

    CPC分类号: C07C231/08 Y02P20/582

    摘要: This invention relates to an improved process for the formation of N-(1-alkoxyalkyl)amides with coproduction of alkylidene bisamides. The N-(1-alkoxyalkyl)formamides of this invention are prepared by reacting formamide with an acetal or hemiacetal carboxylate ester represented by the formulas: ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, aralkyl or aryl; R.sub.1 and R.sub.2 are C.sub.1 -C.sub.8 alkyl, or aryl; and R.sub.3 is secondary or tertiary alkyl having from 3-8 carbon atoms.The reaction is carried out in the presence of an acid catalyst such as a strong acid ion exchange resin.

    摘要翻译: 本发明涉及通过共生产亚烷基双酰胺形成N-(1-烷氧基烷基)酰胺的改进方法。 本发明的N-(1-烷氧基烷基)甲酰胺通过使甲酰胺与下式表示的缩醛或半缩醛羧酸酯反应来制备:其中R是C 1 -C 8烷基,芳烷基或芳基; R1和R2是C1-C8烷基或芳基; 并且R 3是具有3-8个碳原子的仲或叔烷基。 反应在酸催化剂如强酸离子交换树脂存在下进行。

    Phenylcarboxylic acid derivatives
    12.
    发明授权
    Phenylcarboxylic acid derivatives 失效
    苯基羧酸衍生物

    公开(公告)号:US4999378A

    公开(公告)日:1991-03-12

    申请号:US372336

    申请日:1989-06-20

    摘要: Phenylcarboxylic acid derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, --O--D--R.sup.5 (D is alkylene, R.sup.5 is H, amino, morpholino, carboxyl, phthalimido, phenyl, epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl, or both form alkylenedioxy; R.sup.3 is H, --E--R.sup.6 (E is alkylene, R.sup.6 is H, carboxyl, cyano, OH, phenylalkoxy, or halogen-substituted phenyl, or phenylcarbamoyl), --CO--G--R.sup.7 (G is alkylene, R.sup.7 is H, substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl, or halophenyl; R.sup.4 is H or alkyl; A is alkylene, alkylene condensed with cycloalkyl ring, or alkenylene; B is alkylene or alkenylene; l is 0 or 1. Said compounds have fatty acid synthesis-inhibitory activity, cholesterol synthesis-inhibitory activity and are useful as antilipidemic agent, prophylactic and treating agent of artherosclerosis, prophylactic and treating agent of obesity, antidiabetics.

    摘要翻译: 具有下式的苯基羧酸衍生物:其中R1和R2各自为H,卤素,烷基,卤代烷基,烷酰基,环烷基,硝基,氨基,-OD-R5(D为亚烷基,R5为H,氨基,吗啉代,羧基 苯二甲酰亚氨基,苯基,环氧基),取代或未取代的苯氧基,取代或未取代的苯基烷基氨基,羧基烯基或二者形成亚烷基二氧基; R3是H,-E-R6(E是亚烷基,R6是H,羧基,氰基,OH,苯基烷氧基或卤素取代的苯基或苯基氨基甲酰基),-CO-G-R7(G是亚烷基,R7是H, 取代或未取代的苯基氨基甲酰基),取代或未取代的苯甲酰基,烯基,氨基甲酰基,苯基或卤代苯基; R4是H或烷基; A是亚烷基,与环烷基环稠合的亚烷基或亚烯基; B是亚烷基或亚烯基; l是0或1.所述化合物具有脂肪酸合成抑制活性,胆固醇合成抑制活性,可用作抗血脂药物,动脉粥样硬化的预防和治疗剂,肥胖症的预防和治疗剂,抗糖尿病药。

    Multifunctional carrier for the delivery of a pharmacological agent or genetic material into a cell
    18.
    发明授权
    Multifunctional carrier for the delivery of a pharmacological agent or genetic material into a cell 失效
    用于将药剂或遗传物质递送到细胞中的多功能载体

    公开(公告)号:US07314956B2

    公开(公告)日:2008-01-01

    申请号:US10137355

    申请日:2002-05-03

    摘要: The present invention provides a drug delivery vehicle that can improve the pharmacokinetics of pharmacological agents. The invention relates to a multifunctional carrier capable of delivering a carried material such as a pharmacological agent or genetic material to a recipient. The multifunctional carrier includes a multifunctional core and a plurality of adduct molecules bonded thereto. The molecular carrier has surface functional groups which can be associated with a carried material. The carried material can be associated with the molecular carrier through covalent interactions or ionic interactions. The polyvalent core can be ethylene-diamine tetraacetic acid (EDTA) or succinic acid. The invention also relates to methods for producing and using such molecules.

    摘要翻译: 本发明提供能够改善药理学药剂的药代动力学的药物输送载体。 本发明涉及一种能够将诸如药物学或遗传物质的载体材料递送到接受者的多功能载体。 多功能载体包括多功能核心和与其键合的多个加合物分子。 分子载体具有可与载体材料相关的表面官能团。 携带的材料可以通过共价相互作用或离子相互作用与分子载体结合。 多价核可以是乙二胺四乙酸(EDTA)或琥珀酸。 本发明还涉及生产和使用这些分子的方法。