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1. 发明申请

WO2011008453A2 N-PHOSPHONOMETHYLGLYCINE GUANIDINE DERIVATIVE SALTS 审中-公开
标题翻译： N-膦酰基乙醇胺衍生物
公开(公告)号：WO2011008453A2
公开(公告)日：2011-01-20
申请号：PCT/US2010039745
申请日：2010-06-24
申请人： MONSANTO TECHNOLOGY LLC , FLAMEL TECHNOLOGIES S A , BRINKER RONALD J , SOULA OLIVIER , LEMERCIER ALAIN
发明人： BRINKER RONALD J , SOULA OLIVIER , LEMERCIER ALAIN
IPC分类号： C07F9/38 , A01N57/20 , C07C279/04 , C07C279/12 , C07C279/20
CPC分类号： A01N47/44 , A01N37/40 , A01N39/04 , A01N57/20 , C07C279/02 , C07C279/04 , C07C279/12 , C07C279/20 , C07F9/3813 , C07F9/3817 , C08G73/0206 , A01N2300/00
摘要： The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
摘要翻译：本发明提供N-膦酰基甲基甘氨酸胍盐。 N-膦酰基甲基甘氨酸胍盐具有比单独的草甘膦更好的除草效力。本发明还提供胍化合物及其盐。

2. 发明申请

WO2011008453A8 N-PHOSPHONOMETHYLGLYCINE GUANIDINE DERIVATIVE SALTS 审中-公开
标题翻译： N-PHOSPHONOMETHYLGLYCINE胍衍生物盐
公开(公告)号：WO2011008453A8
公开(公告)日：2011-05-19
申请号：PCT/US2010039745
申请日：2010-06-24
申请人： MONSANTO TECHNOLOGY LLC , FLAMEL TECHNOLOGIES S A , BRINKER RONALD J , SOULA OLIVIER , LEMERCIER ALAIN
发明人： BRINKER RONALD J , SOULA OLIVIER , LEMERCIER ALAIN
IPC分类号： C07F9/38 , A01N57/20 , C07C279/04 , C07C279/12 , C07C279/20
CPC分类号： A01N47/44 , A01N37/40 , A01N39/04 , A01N57/20 , C07C279/02 , C07C279/04 , C07C279/12 , C07C279/20 , C07F9/3813 , C07F9/3817 , C08G73/0206 , A01N2300/00
摘要： The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
摘要翻译：本发明提供N-膦酰基甲基甘氨酸胍盐。 N-膦酰基甲基甘氨酸胍盐与单独的草甘膦相比具有改进的除草效力。本发明还提供胍化合物及其盐。

3. 发明申请

WO2011098962A2 ANIONIC POLYSACCHARIDES FUNCTIONALISED BY AT LEAST TWO HYDROPHOBIC GROUPS SUPPORTED BY AN AT LEAST TRIVALENT SPACER 审中-公开
标题翻译：由至少两个间隔层支持的至少两个疏水组功能的绝对多糖
公开(公告)号：WO2011098962A2
公开(公告)日：2011-08-18
申请号：PCT/IB2011050554
申请日：2011-02-09
申请人： ADOCIA , CHARVET RICHARD , SOULA REMI , SOULA OLIVIER
发明人： CHARVET RICHARD , SOULA REMI , SOULA OLIVIER
IPC分类号： A61K31/70 , A61K38/00 , A61K38/18 , A61K47/36 , A61K47/48 , A61P19/00 , C07K14/51 , C08B11/12 , C08B15/00 , C08B37/00 , C08B37/02
CPC分类号： A61K47/36 , C08B11/12 , C08B11/14 , C08B37/0018 , C08B37/0021 , C08B37/0045 , C08B37/0072 , C08B37/0084
摘要： The present invention relates to novel anionic polysaccharide derivatives partially functionalised by at least two vicinal hydrophobic groups, said identical or different hydrophobic groups being supported by an at least trivalent radical or spacer. The invention also relates to methods for synthesising same. The invention further relates to the use of functionalised polysaccharides according to the invention for preparing pharmaceutical compositions including one of the polysaccharides according to the invention and at least one active principle.
摘要翻译：本发明涉及由至少两个邻位疏水基团部分官能化的新型阴离子多糖衍生物，所述相同或不同的疏水基团由至少三价基团或间隔基负载。本发明还涉及其合成方法。本发明还涉及根据本发明的官能化多糖用于制备包含根据本发明的多糖和至少一种活性成分之一的药物组合物的用途。

4. 发明申请

WO2010122385A1 FAST-ACTING INSULIN FORMULATION 审中-公开
标题翻译：速效胰岛素制剂
公开(公告)号：WO2010122385A1
公开(公告)日：2010-10-28
申请号：PCT/IB2010000711
申请日：2010-03-29
申请人： ADOCIA , SOULA GERARD , SOULA OLIVIER , SOULA REMI
发明人： SOULA GERARD , SOULA OLIVIER , SOULA REMI
IPC分类号： A61K38/28 , A61K47/36 , A61K47/48 , A61P5/50
CPC分类号： A61K38/28 , A61K9/0019
摘要： The invention relates to a complex of insulin and a polysaccharide comprising carboxylic functional groups, said polysaccharide being selected from among the polysaccharides functionalized by at least one phenylalanine derivative, in particular said phenylalanine derivative being selected from the group consisting of phenylalanine and the alkaline cation salts thereof, phenylalanine, phenylalaninamide, amine ethyl benzyl or from among the esters of phenylalanine and said insulin being either a human insulin or equivalent insulin. The invention also relates to a pharmaceutical composition including at least one complex according to the invention, particularly in the form of an injectable solution.
摘要翻译：本发明涉及胰岛素和含有羧基官能团的多糖的复合物，所述多糖选自由至少一种苯丙氨酸衍生物官能化的多糖，特别是所述苯丙氨酸衍生物选自苯丙氨酸和碱性阳离子盐其苯丙氨酸，苯丙氨酸酰胺，胺乙基苄基或苯丙氨酸的酯中，并且所述胰岛素是人胰岛素或等同的胰岛素。本发明还涉及包含至少一种根据本发明的复合物的药物组合物，特别是以可注射溶液的形式。

5. 发明申请

WO2007141344B1 PHARMACEUTICAL FORMULATIONS FOR THE SUSTAINED RELEASE OF ACTIVE INGREDIENT(S), AS WELL AS THEIR APPLICATIONS, ESPECIALLY THERAPEUTIC 审中-公开
标题翻译：持续释放有效成分的药物制剂，以及它们的应用，特别是治疗
公开(公告)号：WO2007141344B1
公开(公告)日：2008-05-22
申请号：PCT/EP2007055720
申请日：2007-06-11
申请人： FLAMEL TECH SA , BONNET GONNET CECILE , CHOGNOT DAVID , SOULA OLIVIER , CONSTANCIS ALAIN
发明人： BONNET GONNET CECILE , CHOGNOT DAVID , SOULA OLIVIER , CONSTANCIS ALAIN
IPC分类号： A61K9/00 , A61K9/10 , A61K9/16 , A61K9/19 , A61K38/21 , A61K38/27 , A61K38/28
CPC分类号： A61K38/212 , A61K9/0019 , A61K9/1676 , A61K9/19 , A61K38/27 , A61K38/28
摘要： The present invention concerns new pharmaceutical formulations based on aqueous colloidal suspensions for sustained release of active ingredient(s) -AI - in particular, protein(s) and peptide(s), as well as the applications, especially therapeutic, of these formulations. This formulation comprises an aqueous colloidal suspension with low viscosity based on micrometric particles of amphiphilic polymer PO that is biodegradable, hydrosoluble and carrying hydrophobic groups (HG) - alpha-tocopherol- and ionizable hydrophilic groups (IG) -Glu -, ionized at least in part, said particles being suitable for spontaneously combining non-covalently with an AI at pH = 7.0 under isotonic conditions; and with a size between 0.5 and 100 µm. This suspension contains multivalent ions (Mg ++ ) with a polarity opposite that of IH groups of the PO, the ratio r fulfilling the formula (A) where n is the valence of said multivalent ions, [MI] is the molar of multivalent ions, [IG] is the molar concentration of ionizable groups IG, is between 0.3 and 10.
摘要翻译：本发明涉及基于水性胶体悬浮液的新型药物制剂，用于持续释放活性成分-AI-特别是蛋白质和肽，以及这些制剂的应用，特别是治疗性应用。该制剂包含基于两亲聚合物PO的微米颗粒的低粘度胶态水性悬浮液，其是可生物降解的，水溶性的并带有疏水基团（HG）-α-生育酚和可电离的亲水基团（IG）-Glu-，其至少在部分，所述颗粒适于在等渗条件下在pH = 7.0时自发地与AI非共价结合; 尺寸在0.5到100微米之间。该悬浮液含有极性与PO的IH基团相反的多价离子（Mg ++ ++），其比例r满足式（A），其中n是所述多价离子的化合价[MI ]是多价离子的摩尔数，[IG]是可电离基团IG的摩尔浓度，在0.3和10之间。

6. 发明申请

WO2007051923A3 POLYGLUTAMIC ACIDS FUNCTIONALISED BY HISTIDINE DERIVATIVES AND HYDROPHOBIC GROUPS AND THE USES THEREOF IN PARTICULAR FOR THERAPEUTIC PURPOSES 审中-公开
标题翻译：西地丁衍生物和疏水基团作用的多聚谷氨酸及其用途，特别是用于治疗目的的用途
公开(公告)号：WO2007051923A3
公开(公告)日：2007-06-28
申请号：PCT/FR2006002443
申请日：2006-10-31
申请人： FLAMEL TECH SA , SOULA OLIVIER , SOULA REMI , BREYNE OLIVIER
发明人： SOULA OLIVIER , SOULA REMI , BREYNE OLIVIER
IPC分类号： C07K2/00 , A61K47/48 , C08G69/10
CPC分类号： C08G69/10 , A61K8/88 , A61K2800/57 , A61Q19/00 , C07K14/001
摘要： The invention relates to novel biodegradable materials based on modified polyomino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained by the invention which relates to novel polyglutomates modified by histidine derivatives and hydrophobic groups containing from 8 to 30 carbon atoms. Said polyglutomates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorisation particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7, 4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.
摘要翻译：本发明涉及基于改性的多酚酸的新型生物可降解材料，并且特别适用于载体活性物质（AS）。本发明还涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物保护组合物。本发明的目的是提供一种新型聚合物原料，其可用于载体AS并能最佳地满足该领域的所有规格：生物相容性，生物降解性，易与许多活性物质结合或溶解它们并释放所述物质体内活性物质。本发明通过涉及由组氨酸衍生物和含有8至30个碳原子的疏水基团修饰的新型多聚谷氨酸盐的发明达到目的。所述由组氨酸衍生物修饰的多聚谷氨酸盐在pH低于5时是可溶的，并且容易且经济地转化为能够形成稳定的含水胶态悬浮液的活性物质载体化颗粒。相反，所述改性聚谷氨酸盐不溶于具有生理pH（7,4）的水中，因此在皮下注射的情况下必须在注射部位沉淀。

7. 发明申请

WO2010041138A2 COMPLEX BETWEEN HUMAN INSULIN AND AN AMPHIPHILIC POLYMER, AND USE OF SAID COMPLEX FOR PREPARING A QUICK HUMAN INSULIN FORMULATION 审中-公开
标题翻译：人胰岛素和人血浆聚合物之间的复合物，以及使用复合物制备快速人胰岛素制剂
公开(公告)号：WO2010041138A2
公开(公告)日：2010-04-15
申请号：PCT/IB2009007106
申请日：2009-10-12
申请人： ADOCIA , SOULA OLIVIER , SOULA REMI , SOULA GERARD
发明人： SOULA OLIVIER , SOULA REMI , SOULA GERARD
IPC分类号： A61K47/48 , A61K31/721 , A61K38/28 , A61K47/36 , A61P3/10 , C07K14/62 , C08B37/00
CPC分类号： C08L89/00 , A61K31/721 , A61K38/28 , A61K47/61 , C08B37/0021 , C08K3/20 , C08K3/32 , C08K5/13 , C08K5/15 , C08K5/175 , C08L5/02 , A61K2300/00
摘要： The invention relates to a complex between human insulin and an amphiphilic polymer containing carboxyl functional groups, said amphiphilic polymer being selected from among the functionalised polysaccharides mostly made up of glycosidic monomers bonded by (1,6) glycosidic bonds functionalised by at least one tryptophan derivative. The invention also relates to a pharmaceutical composition including at least one complex according to the invention, said formulation capable of being in the form of an injectable solution. The invention relates, more particularly, to the use of a complex according to the invention for the preparation of a formulation of human insulin with a concentration of around 600 µM (100 UI/mL), with the onset of action being in less than 30 minutes, preferably in less than 20 minutes, and more preferably in less than 15 minutes and/or with the glycaemic nadir being in less than 120 minutes, preferably in less than 105 minutes, and more preferably in less than 90 minutes.
摘要翻译：本发明涉及人胰岛素与含有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至少一种色氨酸衍生物官能化的（1,6）糖苷键结合的糖苷单体组成的官能化多糖中。本发明还涉及包含至少一种根据本发明的复合物的药物组合物，所述制剂能够以可注射溶液的形式存在。本发明更具体地涉及根据本发明的复合物用于制备浓度为约600μM（100 UI / mL）的人胰岛素制剂的用途，起始作用小于30 分钟，优选小于20分钟，更优选小于15分钟，和/或血糖最低点在小于120分钟内，优选小于105分钟，更优选小于90分钟。

8. 发明申请

WO2008120085A3 ANGIOGENIC COMPOSITION 审中-公开
标题翻译：生物成分
公开(公告)号：WO2008120085A3
公开(公告)日：2009-09-11
申请号：PCT/IB2008000762
申请日：2008-03-31
申请人： ADOCIA , SOULA OLIVIER , SOULA GERARD , SOULA REMI , ELOY ROSY
发明人： SOULA OLIVIER , SOULA GERARD , SOULA REMI , ELOY ROSY
IPC分类号： A61K47/48 , A61K9/00 , A61K38/18 , A61P9/10
CPC分类号： A61K9/0014 , A61K38/1858 , A61K47/61
摘要： The invention relates to the use of an amphiphilic polymer for the preparation of a therapeutic composition that is intended to promote angiogenesis at the administration site thereof, comprising a complex between a polymer and a platelet-derived growth factors (PDGF), characterised in that the polymer is amphiphilic. In one embodiment of the invention, the PDGF is selected from the PDGF group and the amphiphilic polymer is selected from the group comprising amphiphilic polymers formed by a hydrophilic polymer backbone functionalised with hydrophobic substituents and hydrophilic groups having general formula (I). The invention also relates to the use of same in accordance with these claims, characterised in that the therapeutic composition takes the form of a gel, cream, solution, spray, paste, patch or bandage.
摘要翻译：本发明涉及两亲性聚合物在制备治疗组合物中的用途，所述治疗组合物旨在促进其施用部位的血管发生，其包含聚合物与血小板衍生生长因子（PDGF）之间的复合物，其特征在于，聚合物是两亲性的。在本发明的一个实施方案中，PDGF选自PDGF基团，两亲性聚合物选自由疏水取代基官能化的亲水性聚合物骨架和具有通式（I）的亲水基团形成的两亲聚合物。本发明还涉及根据权利要求的用途，其特征在于治疗组合物采取凝胶，霜剂，溶液，喷雾剂，糊剂，贴剂或绷带的形式。

9. 发明申请

WO2007141344A2 PHARMACEUTICAL FORMULATIONS FOR THE SUSTAINED RELEASE OF ACTIVE INGREDIENT(S), AS WELL AS THEIR APPLICATIONS, ESPECIALLY THERAPEUTIC 审中-公开
标题翻译：活性成分持续释放的药物制剂，作为其应用，特别是治疗
公开(公告)号：WO2007141344A2
公开(公告)日：2007-12-13
申请号：PCT/EP2007055720
申请日：2007-06-11
申请人： FLAMEL TECH SA , BONNET GONNET CECILE , CHOGNOT DAVID , SOULA OLIVIER , CONSTANCIS ALAIN
发明人： BONNET GONNET CECILE , CHOGNOT DAVID , SOULA OLIVIER , CONSTANCIS ALAIN
IPC分类号： A61K9/16 , A61K9/10 , A61K9/19 , A61K38/21 , A61K38/27 , A61K38/28
CPC分类号： A61K38/212 , A61K9/0019 , A61K9/1676 , A61K9/19 , A61K38/27 , A61K38/28
摘要： The present invention concerns new pharmaceutical formulations based on aqueous colloidal suspensions for sustained release of active ingredient(s) - AI - in particular, protein(s) and peptide(s), as well as the applications, especially therapeutic, of these formulations. This formulation comprises an aqueous colloidal suspension with low viscosity based on micrometric particles of amphiphilic polymer PO that is biodegradable, hydrosoluble and carrying hydrophobic groups (HG) - alpha-tocopherol- and ionizable hydrophilic groups (IG) - Glu -, ionized at least in part, said particles being suitable for spontaneously combining non-covalently with an AI at pH = 7.0 under isotonic conditions; and with a size between 0.5 and 100 µm. This suspension contains multivalent ions (Mg ++ ) with a polarity opposite that of IH groups of the PO, the ratio r fulfilling the formula (A) where - n is the valence of said multivalent ions - [MI] is the molar of multivalent ions, [IG] is the molar concentration of ionizable groups IG, is between 0.3 and 10.
摘要翻译：本发明涉及基于水性胶体悬浮液的新型药物制剂，其用于持续释放活性成分（特别是蛋白质和肽）以及这些制剂的应用，特别是治疗性的用途。该制剂包含基于两亲性聚合物PO的微米颗粒的低粘度的水性胶体悬浮液，其是可生物降解的，可溶解的和携带疏水基团（HG）-α-生育酚和可离子化的亲水基团（IG）-Glu-，至少在所述颗粒适合于在等渗条件下在pH = 7.0下非共价与AI共价组合; 并且尺寸在0.5和100μm之间。该悬浮液含有极性与PO的IH基团相反极性的多价离子（Mg ++），满足式（A）的比率r其中，n是所述多价离子的化合价[ MI]是多价离子的摩尔数[IG]是可电离基团IG的摩尔浓度，在0.3和10之间。

10. 发明申请

WO2007034320A3 PDGF AMPHIPHILIC POLYMER COMPLEX 审中-公开
公开(公告)号：WO2007034320A3
公开(公告)日：2007-10-04
申请号：PCT/IB2006002666
申请日：2006-09-26
申请人： PROTEINS & PEPTIDES MAN , DUBREUCQ GUY , DAHRI-CORREIA LATIFA , CORREIA JOSE , DURACHER DAVID , SOULA REMI , SOULA OLIVIER , SOULA GERARD
发明人： DUBREUCQ GUY , DAHRI-CORREIA LATIFA , CORREIA JOSE , DURACHER DAVID , SOULA REMI , SOULA OLIVIER , SOULA GERARD
IPC分类号： A61K38/18 , A61K47/36 , A61P17/02
CPC分类号： A61K47/36 , A61K38/1858
摘要： The invention concerns novel platelet-derived growth factor (PDGF) complexes associated with amphiphilic polymers for enhancing the physical and chemical in vitro and in vivo stability of the therapeutic protein for pharmaceutical applications. The invention also concerns a method for preparing the PDGF-amphiphilic polymer complex characterized in that it consists in preparing said polymer/PDGF-BB complex in an aqueous medium and in the absence of organic solvent likely to cause denaturation of the protein and the use of said PDGF-amphiphilic polymer complex for preparing a therapeutic wound-healing composition for topically treating ulcers.
摘要翻译：本发明涉及与两亲聚合物相关的新型血小板衍生生长因子（PDGF）复合物，用于增强用于药物应用的治疗性蛋白质的物理和化学体外和体内稳定性。本发明还涉及一种制备PDGF-两亲性聚合物复合物的方法，其特征在于其包括在水性介质中制备所述聚合物/ PDGF-BB复合物，并且在不存在可能引起蛋白质变性的有机溶剂的情况下以及使用所述PDGF-两亲性聚合物复合物用于制备用于局部治疗溃疡的治疗性伤口愈合组合物。

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