Condensation product of theanine derivative and carboxylic acid coumarin derivative, its intermediate, preparation method and use thereof
    45.
    发明授权
    Condensation product of theanine derivative and carboxylic acid coumarin derivative, its intermediate, preparation method and use thereof 有权
    茶氨酸衍生物和羧酸香豆素衍生物的缩合产物,其中间体,其制备方法和用途

    公开(公告)号:US09518038B2

    公开(公告)日:2016-12-13

    申请号:US14431707

    申请日:2013-09-25

    Abstract: The present invention relates to a compound as represented by formula (I), which is a condensation product of a theanine derivative and a carboxylic acid coumarin derivative, compounds as represented by formula (II) and formula (III), both of which are intermediates of the condensation product, a method for preparing these compounds, a pharmaceutical composition comprising the compounds, and a use thereof in preparing a medicament for prevention and treatment of tumors, inflammation, cardiovascular diseases, immune deficiency diseases and the like. Wherein, (Ia)R═CH3R1═HR2═H (Ib)R═CH2CH3R1═HR2═H (Ic)R═CH2CH3R1═ClR2═H (Id)R═CH2CH3R1═BrR2═H (Ie)R═CH2CH3R1═FR2═H (If)R═CH2CH3R1═NO2R2═H (Ig)R═CH2CH3R1═ClR2═Cl (Ih)R═CH2CH3R1═BrR2═Br (Ii)R═CH2CH3R1═NH2R2═H Wherein, (IIa)R═CH3 (IIb)R═CH2CH3 Wherein, (IIIc)R1═ClR2═H (IIId)R1═BrR2═H (IIIe)R1═FR2═H (IIIf)R1═NO2R2═H (IIIg)R1═ClR2═Cl (IIIh)R1═BrR2═Br

    Abstract translation: 本发明涉及由式(I)表示的化合物,其是茶氨酸衍生物和羧酸香豆素衍生物的缩合产物,由式(II)和式(III)表示的化合物,它们都是中间体 的缩合产物,制备这些化合物的方法,包含该化合物的药物组合物及其在制备用于预防和治疗肿瘤,炎症,心血管疾病,免疫缺陷疾病等的药物中的用途。 其中,其中,其中

    POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY
    46.
    发明申请
    POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY 审中-公开
    POLY(VINYL BENZOATE)NANOPARTICLES FOR MOLECULAR DELIVERY

    公开(公告)号:US20160338962A1

    公开(公告)日:2016-11-24

    申请号:US15228686

    申请日:2016-08-04

    Abstract: The present invention comprises poly(vinyl benzoate) nanoparticle suspensions as molecular carriers. These nanoparticles can be formed by nanoprecipitation of poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring about 200-250 nm in diameter which are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC50>1000 μg/mL) and primary bovine primary aortic endothelial cells (IC50>500 μg/mL), and exert non-observable bactericidal activity against a selection of representative test microbes (MIC>250 μg/mL). Poly(vinyl benzoate) nanoparticles are suitable carriers for molecular delivery of lipophilic small molecules such as drugs pharmaceutical and imaging agents.

    Abstract translation: 本发明包括作为分子载体的聚(苯甲酸乙烯酯)纳米颗粒悬浮液。 这些纳米颗粒可以通过使用Pluronic F68作为表面活性剂在水中的聚(乙烯基苯甲酸酯)的纳米沉淀形成,以产生直径约200-250nm的球形纳米结构,其在磷酸盐缓冲液和血清中是稳定的,并且在存在下仅缓慢降解 的酯酶。 在磷酸盐缓冲液中的动力学实验表明,78%的香豆素-6被包封在纳米颗粒的聚合物基质内,剩余的22%的香豆素-6被表面结合并迅速释放。 纳米颗粒在体外对人上皮细胞(IC50>1000μg/ mL)和原代牛主动脉内皮细胞(IC50>500μg/ mL)无毒性,并且对代表性测试微生物的选择施加不可观察的杀菌活性 (MIC>250μg/ mL)。 聚(苯甲酸乙烯酯)纳米颗粒是分子递送亲脂性小分子如药物药物和成像剂的合适的载体。

    CONDENSATION PRODUCT OF THEANINE DERIVATIVE AND CARBOXYLIC ACID COUMARIN DERIVATIVE, ITS INTERMEDIATE, PREPARATION METHOD AND USE THEREOF
    48.
    发明申请
    CONDENSATION PRODUCT OF THEANINE DERIVATIVE AND CARBOXYLIC ACID COUMARIN DERIVATIVE, ITS INTERMEDIATE, PREPARATION METHOD AND USE THEREOF 有权
    蒽衍生物和羧甲酸衍生物的缩合产物,其中间体,制备方法及其用途

    公开(公告)号:US20150239861A1

    公开(公告)日:2015-08-27

    申请号:US14431707

    申请日:2013-09-25

    Abstract: The present invention relates to a compound as represented by formula (I), which is a condensation product of a theanine derivative and a carboxylic acid coumarin derivative, compounds as represented by formula (II) and formula (III), both of which are intermediates of the condensation product, a method for preparing these compounds, a pharmaceutical composition comprising the compounds, and a use thereof in preparing a medicament for prevention and treatment of tumors, inflammation, cardiovascular diseases, immune deficiency diseases and the like. Wherein, (Ia)R═CH3R1═HR2═H (Ib)R═CH2CH3R1═HR2═H (Ic)R═CH2CH3R1═ClR2═H (Id)R═CH2CH3R1═BrR2═H (Ie)R═CH2CH3R1═FR2═H (If)R═CH2CH3R1═NO2R2═H (Ig)R═CH2CH3R1═ClR2═Cl (Ih)R═CH2CH3R1═BrR2═Br (Ii)R═CH2CH3R1═NH2R2═H Wherein, (IIa)R═CH3 (IIb)R═CH2CH3 Wherein, (IIIc)R1═ClR2═H (IIId)R1═BrR2═H (IIIe)R1═FR2═H (IIIf)R1═NO2R2═H (IIIg)R1═ClR2═Cl (IIIh)R1═BrR2═Br

    Abstract translation: 本发明涉及由式(I)表示的化合物,其是茶氨酸衍生物和羧酸香豆素衍生物的缩合产物,由式(II)和式(III)表示的化合物,它们都是中间体 的缩合产物,制备这些化合物的方法,包含该化合物的药物组合物及其在制备用于预防和治疗肿瘤,炎症,心血管疾病,免疫缺陷疾病等的药物中的用途。 其中,(Ia)R = CH 3 R 1 = H R 2 = H(Ib)R = CH 2 CH 3 R 1 = H R 2 = H(Ic)R = CH 2 CH 3 R 1 = Cl R 2 = H(Id)R = CH 2 CH 3 R 1 = (Ie)R = CH 2 CH 3 R 1 = R R 2 = H(If)R = CH 2 CH 3 R 1 = N 2 R 2 = H(Ig)R = CH 2 CH 3 R 1 = Cl R 2 = Cl(Ih)R = CH 2 CH 3 R 1 = R 2 R 2 = )R = CH 2 CH 3 R 1 = NH 2 R 2 = H其中,(IIa)R = CH 3(IIb)R = CH 2 CH 3其中,(IIIc)R 1 = Cl R 2 = H(IIId)R 1 = Br R 2 = H(IIIe) R2 = H(IIIf)R1 = NO2 R2 = H(IIIg)R1 = Cl R2 = C1(IIIh)R1 = Br R2 = Br

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