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101 条记录 (耗时 0.044 秒)

    Preparation of alkyl cyanoacetates
    53.
    发明授权
    Preparation of alkyl cyanoacetates 失效
    氰基乙酸烷基酯的制备

    公开(公告)号：US4322369A

    公开(公告)日：1982-03-30

    申请号：US216363

    申请日：1980-12-15

    申请人： Michel Desbois ,  Gerard Soula

    发明人： Michel Desbois ,  Gerard Soula

    IPC分类号： C07C255/19 ,  C07C67/00 ,  C07C253/00 ,  C07C120/04

    CPC分类号： C07C255/00 ,  C07C253/14

    摘要： The alkyl cyanoacetates are prepared by reacting an alkyl chloracetate with an excess of an alkali metal cyanide, in an inert solvent and in the presence of at least one tertiary amine sequestering agent having the formula:N--CHR.sub.1 --CHR.sub.2 --O--CHR.sub.3 --CHR.sub.4 --O.sub.n R.sub.5 ].sub.3 (I).

    摘要翻译： 氰基乙酸烷基酯通过使氯代乙酸烷基酯与过量的碱金属氰化物在惰性溶剂中并在至少一种具有下式的叔胺螯合剂的存在下反应制备：N-CHR1-CHR2-O-CHR3-CHR4 -OnR5] 3（I）。

    Dextran functionalized by hydrophobic amino acids
    55.
    发明授权
    Dextran functionalized by hydrophobic amino acids 有权
    疏水性氨基酸功能化的葡聚糖

    公开(公告)号：US08629124B2

    公开(公告)日：2014-01-14

    申请号：US12078441

    申请日：2008-03-31

    申请人： Gerard Soula ,  Olivier Soula ,  Remi Soula

    发明人： Gerard Soula ,  Olivier Soula ,  Remi Soula

    IPC分类号： A01N43/04 ,  A01N61/00 ,  A61K31/715 ,  A61K31/00

    CPC分类号： A61K31/721 ,  C08B37/0021

    摘要： The invention relates to a dextran functionalized by at least one hydrophobic alpha-amino acid radical, said alpha-amino acid being grafted or bonded to the dextran by a bonding arm and a functional group. A hydrophobic amino acid radical is understood as being the product of coupling between the amine of the amino acid and an acid carried by the bonding arm, said dextran being amphiphilic at neutral pH. In an embodiment, the hydrophobic amino acid is selected from tryptophan derivatives, such as tryptophan, tryptophanol, tryptophanamide, 2-indole ethyl-amine and their alkaline cation salts. The present invention relates also to a pharmaceutical composition comprising one of the dextrans according to the invention.

    摘要翻译： 本发明涉及由至少一个疏水性α-氨基酸官能化的葡聚糖，所述α-氨基酸通过键合臂和官能团接枝或结合到葡聚糖上。 疏水性氨基酸被理解为是氨基酸的胺和由结合臂携带的酸之间的偶联的产物，所述葡聚糖在中性pH下是两亲性的。 在一个实施方案中，疏水性氨基酸选自色氨酸衍生物，例如色氨酸，色氨酸，色氨酰胺，2-吲哚乙基胺及其碱性阳离子盐。 本发明还涉及包含根据本发明的葡聚糖之一的药物组合物。

    Complex consisted of a polysaccharide and an HBP
    56.
    发明授权
    Complex consisted of a polysaccharide and an HBP 有权
    复合物由多糖和HBP组成

    公开(公告)号：US08367640B2

    公开(公告)日：2013-02-05

    申请号：US12585886

    申请日：2009-09-28

    申请人： Olivier Soula ,  Remi Soula ,  Martin Gaudier ,  Gerard Soula

    发明人： Olivier Soula ,  Remi Soula ,  Martin Gaudier ,  Gerard Soula

    IPC分类号： A01N43/04 ,  A01N61/00 ,  A61K31/715 ,  A61K31/00

    CPC分类号： A61K9/0019 ,  A61K9/19 ,  A61K38/1825 ,  A61K38/185 ,  A61K38/1866 ,  A61K38/27 ,  A61K38/29 ,  A61K47/42 ,  A61K47/61

    摘要： The invention relates to a complex consisted of a polysaccharide and an HBP, said polysaccharide being consisted from glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative. The invention also relates to a pharmaceutical composition comprising a complex according to the invention and to the use of a polysaccharide consisted of glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative, for the preparation of a pharmaceutical formulation of stable HBPs.

    摘要翻译： 本发明涉及由多糖和HBP组成的复合物，所述多糖由（1,6）和/或（1,4）和/或（1,3）和/或（1,2）的糖苷键组成 ）类型并用至少一种可成盐或盐化的色氨酸衍生物官能化。 本发明还涉及包含根据本发明的复合物和由（1,6）和/或（1,4）和/或（1,3）和/或（1,3）的糖苷键组成的多糖和/ 或（1,2）型，并用至少一种可成盐或盐化的色氨酸衍生物官能化，用于制备稳定HBP的药物制剂。

    Fast-acting insulin formulation
    57.
    发明申请
    Fast-acting insulin formulation 有权
    速效胰岛素制剂

    公开(公告)号：US20100249020A1

    公开(公告)日：2010-09-30

    申请号：US12662036

    申请日：2010-03-29

    申请人： Remi Soula ,  Gerard Soula ,  Olivier Soula

    发明人： Remi Soula ,  Gerard Soula ,  Olivier Soula

    IPC分类号： A61K38/28 ,  C07K17/10 ,  A61P3/10

    CPC分类号： A61K38/28 ,  A61K9/0019

    摘要： The invention relates to a complex between an insulin and a polysaccharide comprising carboxyl functional groups, said polysaccharide being chosen from polysaccharides functionalized with at least one phenylalanine derivative, noted Phe, said phenylalanine derivative being chosen from the group consisting of phenylalanine and its alkali metal cation salts, phenylalaninol, phenylalaninamide and ethylbenzylamine or from phenylalanine esters, and said insulin being either a human insulin or an insulin analog. The invention also relates to a pharmaceutical composition comprising at least one complex according to the invention, especially in the form of an injectable solution.

    摘要翻译： 本发明涉及胰岛素和包含羧基官能团的多糖之间的复合物，所述多糖选自用至少一种苯丙氨酸衍生物（所述Phe）官能化的多糖，所述苯丙氨酸衍生物选自苯丙氨酸及其碱金属阳离子 盐，苯丙氨酸，苯丙氨酰胺和乙基苄胺或苯丙氨酸酯，所述胰岛素是人胰岛素或胰岛素类似物。 本发明还涉及包含至少一种根据本发明的复合物，特别是可注射溶液形式的药物组合物。

    Complex between human insulin and an amphiphilic polymer and use of this complex in the preparation of a fast-acting human insulin formulation
    58.
    发明申请
    Complex between human insulin and an amphiphilic polymer and use of this complex in the preparation of a fast-acting human insulin formulation 审中-公开
    人胰岛素与两亲性聚合物之间的复合物，以及该配合物在制备快速作用的人胰岛素制剂中的用途

    公开(公告)号：US20100167984A1

    公开(公告)日：2010-07-01

    申请号：US12588349

    申请日：2009-10-13

    申请人： Olivier Soula ,  Remi Soula ,  Gerard Soula

    发明人： Olivier Soula ,  Remi Soula ,  Gerard Soula

    IPC分类号： A61K38/28 ,  C07K14/62

    CPC分类号： A61K38/28 ,  A61K9/0019 ,  C07K14/62

    摘要： The invention relates to a complex between human insulin and an amphiphilic polymer comprising carboxyl functional groups, said amphiphilic polymer being chosen from functionalized polysaccharides predominantly composed of glycoside monomers bonded via glycoside bonds of (1,6) type which are functionalized by at least one tryptophan derivative.It also relates to a pharmaceutical composition comprising at least one complex according to the invention, it being possible for said formulation to be in the form of an injectable solution.It more particularly relates to the use of a complex according to the invention in the preparation of a human insulin formulation at a concentration of approximately 600 μM (100 IU/ml), the onset of action of which is less than 30 minutes, preferably less than 20 minutes and more preferably less than 15 minutes and/or the glycemic nadir of which is at less than 120 minutes, preferably less than 105 minutes and more preferably less than 90 minutes.

    摘要翻译： 本发明涉及人胰岛素与包含羧基官能团的两亲聚合物之间的复合物，所述两亲性聚合物选自主要由通过（1,6）型糖苷键键合的糖苷单体组成的官能化多糖，其由至少一种色氨酸官能化 衍生物。 它还涉及包含至少一种根据本发明的复合物的药物组合物，所述制剂可以是可注射溶液的形式。 更具体地涉及根据本发明的复合物在制备浓度为约600μM（100IU / ml）的人胰岛素制剂时的用途，其作用开始小于30分钟，优选较少 20分钟以上，更优选小于15分钟，和/或血糖最低值低于120分钟，优选小于105分钟，更优选小于90分钟。

    Anti-Misuse Microparticulate Oral Drug Form
    59.
    发明申请
    Anti-Misuse Microparticulate Oral Drug Form 审中-公开
    反滥用微量口服药物形式

    公开(公告)号：US20090041838A1

    公开(公告)日：2009-02-12

    申请号：US11883935

    申请日：2006-02-08

    申请人： Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

    发明人： Florence Guimberteau ,  Remi Meyrueix ,  Gerard Soula

    IPC分类号： A61K9/50 ,  A61K9/14 ,  A61K9/22

    CPC分类号： A61K9/5047 ,  A61K9/5078 ,  A61K31/196 ,  A61K31/522

    摘要： The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form. More specifically, the invention relates to a solid oral drug form comprising anti-misuse means and at least one active ingredient, which is characterized in that: at least part of the active ingredient is contained in microparticles; and the anti-misuse means comprise anti-crushing means (a) which enable the microparticles of the active ingredient to resist crushing, such as to prevent the misuse thereof. According to the invention, the drug form can also comprise means (b) for preventing the misuse of the active ingredient following a possible liquid extraction process.

    摘要翻译： 本发明涉及具有防止滥用其中所含的活性药物成分（API）的组合物的固体微粒口服剂型。 本发明的目的是防止不适当地使用固体口服药物以用于由适当的公共卫生当局正式批准的治疗用途以外的任何用途。 本发明的另一个目的是提供新的止痛药，其可用于：防止某些止痛剂的滥用和成瘾和/或控制血浆浓度变异性和/或促进口服; 行政; 和/或将镇痛药彼此和/或以相同口服形式的一种或多种活性成分组合。 更具体地，本发明涉及包含抗滥用手段和至少一种活性成分的固体口服药物形式，其特征在于：至少部分活性成分包含在微粒中; 并且防误用手段包括能够使活性成分的微粒抵抗破碎的抗破碎装置（a），以防止其误用。 根据本发明，药物形式还可以包括用于防止在可能的液体提取过程后滥用活性成分的装置（b）。

    Solid, Oral, Microparticulate Dosage Form Which Has Been Designed To Prevent Misuse
    60.
    发明申请
    Solid, Oral, Microparticulate Dosage Form Which Has Been Designed To Prevent Misuse 审中-公开
    坚实，口服，微量的剂型，旨在防止误用

    公开(公告)号：US20080260844A1

    公开(公告)日：2008-10-23

    申请号：US11791471

    申请日：2005-11-21

    申请人： Gerard Soula ,  Florence Guimberteau

    发明人： Gerard Soula ,  Florence Guimberteau

    IPC分类号： A61K9/14 ,  A61K31/522

    CPC分类号： A61K31/196 ,  A61K9/0053 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047 ,  A61K9/5078

    摘要： The invention relates to the field of solid, oral, microparticulate dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient contained therein. The aim of the invention is to prevent the improper use of solid oral medicaments for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. More specifically, the invention relates to a solid, oral drug form which is characterised in that at least one part of the active pharmaceutical ingredient is contained in the microparticles thereof and in that the inventive form comprises anti-crushing means which are intended to impede or completely prevent the crushing of the microparticles of the active pharmaceutical ingredient, such as to preclude the misuse thereof.

    摘要翻译： 本发明涉及具有防止其中含有的活性药物成分的滥用的组合物的固体，口服，微粒剂型的领域。 本发明的目的是防止固体口服药物用于除适当的公共卫生当局正式批准的治疗用途以外的任何用途。 更具体地，本发明涉及固体口服药物形式，其特征在于活性药物成分的至少一部分包含在其微粒中，并且本发明形式包括抗破碎装置，其旨在阻止或 完全防止活性药物成分的微粒的破碎，排除其滥用。