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    • 61. 发明授权
    • Preparation of hydrogenosilanes by redistribution
    • 通过再分配制备氢硅烷
    • US4746752A
    • 1988-05-24
    • US837053
    • 1986-03-06
    • Jean-Luc LepageGerard Soula
    • Jean-Luc LepageGerard Soula
    • C01B33/04B01J20/26B01J31/00C01B33/107C07F7/12C09K3/00C07F7/08C07F7/18
    • C07F7/125
    • Hydrogenated silanes are facilely prepared by redistribution, by reacting (1) a silane having the formula H.sub.m SiX.sub.4-m in which X is halogen or an alkoxy group and m is an integer equal to 0, 1, 2 or 3, with (2) an alkyl or aryl hydrosilane having the formula R.sub.n H.sub.p SiX'.sub.4-(n+p) in which X' is halogen or an alkoxy group, R is an alkyl or aryl group and n and p, which may be identical or different, are integers equal to 1, 2 or 3, with the proviso that n+p.ltoreq.4, in the presence of (3) a catalytically effective amount of a catalyst comprising (i) a quaternary ammonium salt having the formula R'.sub.4 NY or a quaternary phosphonium salt having the formula R'.sub.4 PY, in which formulae R', which may be identical or different, are each a monovalent hydrocarbon radical and Y is halogen, (ii) a tertiary amine of the general formula NR'R"R"', in which R', R" and R"', which may be identical or different, are monovalent hydrocarbon radicals, or (iii) an ion exchange resin comprising tertiary amine or quaternary ammonium groups.
    • 氢化硅烷通过重新分布,通过使(1)具有式HmSiX4-m的硅烷(其中X是卤素或烷氧基,m是等于0,1,2或3的整数)与(2) 具有式RnHpSiX'4-(n + p)的烷基或芳基氢硅烷,其中X'为卤素或烷氧基,R为烷基或芳基,n和p可相同或不同,为等于 1,2或3,条件是在(3)催化有效量的催化剂存在下,n + p = 4,其包含(i)具有式R'4NY的季铵盐或季鏻 具有式R'4PY的盐,其中可以相同或不同的式R'各自为一价烃基,Y为卤素,(ii)通式NR'R''R“'的叔胺 ',其中可以相同或不同的R',R“和R”'是一价烃基,或(iii)包含叔胺或四氢呋喃的离子交换树脂 铵基团。
    • 67. 发明授权
    • Dextran functionalized by hydrophobic amino acids
    • 疏水性氨基酸功能化的葡聚糖
    • US08629124B2
    • 2014-01-14
    • US12078441
    • 2008-03-31
    • Gerard SoulaOlivier SoulaRemi Soula
    • Gerard SoulaOlivier SoulaRemi Soula
    • A01N43/04A01N61/00A61K31/715A61K31/00
    • A61K31/721C08B37/0021
    • 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.
    • 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。
    • 69. 发明申请
    • Fast-acting insulin formulation
    • 速效胰岛素制剂
    • US20100249020A1
    • 2010-09-30
    • US12662036
    • 2010-03-29
    • Remi SoulaGerard SoulaOlivier Soula
    • Remi SoulaGerard SoulaOlivier Soula
    • A61K38/28C07K17/10A61P3/10
    • A61K38/28A61K9/0019
    • 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.
    • 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。
    • 70. 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
    • 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
    • US20100167984A1
    • 2010-07-01
    • US12588349
    • 2009-10-13
    • Olivier SoulaRemi SoulaGerard Soula
    • Olivier SoulaRemi SoulaGerard Soula
    • A61K38/28C07K14/62
    • A61K38/28A61K9/0019C07K14/62
    • 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.
    • 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。