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    IMPROVED PROCESS FOR THE PRODUCTION OF HIGH-PURITY SULFATED HA
    4.
    发明申请
    IMPROVED PROCESS FOR THE PRODUCTION OF HIGH-PURITY SULFATED HA 审中-公开
    改进的生产高纯度硫化氢的方法

    公开(公告)号：WO2017085622A1

    公开(公告)日：2017-05-26

    申请号：PCT/IB2016/056868

    申请日：2016-11-15

    Applicant: FIDIA FARMACEUTICI S.P.A.

    Inventor： GUARISE, Cristian ,  PAVAN, Mauro

    IPC: C08B37/08 ,  A61K31/728 ,  A61K31/737

    CPC classification number: C08B37/0072 ,  A61K31/737

    Abstract: The present invention relates to an improved process for the production of sulfated hyaluronic acid (HA), sulfated HA-derivatives and/or mixtures thereof, having a high purity and a sulfation degree ranging from 1 to 3, which comprises the following steps: a) solubilization of HA-Na or HA-derivative-Na, in an aprotic solvent in the presence of an organic sulfonic acid; b) sulfation of the solution obtained by the addition of an excess of sulfating agents; c) precipitation in ethanol until a precipitate is obtained; d) solubilization of the precipitate thus obtained in a mixture of water and the aprotic solvent used in step a), in the presence of an excess of NaCl, with a pH adjustment within a range of 3 to 4; e) further precipitation with ethanol until a powder is obtained; f) washings of the powder coming from step e) and drying the product thus obtained under vacuum. The present invention also relates to sulfated HA, sulfated HA derivatives and/or mixtures thereof, having a high purity and sulfation degree ranging from 1 to 3, thus prepared, and the relative pharmaceutical mixtures.

    Abstract translation: 本发明涉及用于生产硫酸化透明质酸（HA），硫酸化HA-衍生物和/或其混合物的改进方法，其具有高纯度和1至3范围内的硫酸化度 其包括以下步骤：a）在有机磺酸存在下，在非质子传递溶剂中溶解HA-Na或HA-衍生物-Na; b）通过加入过量的硫酸化剂获得的溶液的硫酸化; c）在乙醇中沉淀直至获得沉淀; d）将如此获得的沉淀物在步骤a）中使用的水和非质子溶剂的混合物中，在过量的NaCl存在下溶解，其中pH调节在3至4的范围内; e）用乙醇进一步沉淀，直至获得粉末; f）洗涤来自步骤e）的粉末，并在真空下干燥由此获得的产物。 本发明还涉及如此制备的具有1至3的高纯度和硫酸化度的硫酸化HA，硫酸化HA衍生物和/或其混合物，以及相关的药物混合物。

    PROCESS FOR THE SYNTHESIS OF CONJUGATES OF GLYCOSAMINOGLYCANES (GAG) WITH BIOLOGICALLY ACTIVE MOLECULES, POLYMERIC CONJUGATES AND RELATIVE USES THEREOF
    7.
    发明申请
    PROCESS FOR THE SYNTHESIS OF CONJUGATES OF GLYCOSAMINOGLYCANES (GAG) WITH BIOLOGICALLY ACTIVE MOLECULES, POLYMERIC CONJUGATES AND RELATIVE USES THEREOF 审中-公开
    合成具有生物活性分子的糖蛋白氨基酸（GAG）结合的方法，聚合物共聚物及其相关用途

    公开(公告)号：WO2010145821A1

    公开(公告)日：2010-12-23

    申请号：PCT/EP2010/003634

    申请日：2010-06-04

    Applicant: FIDIA FARMACEUTICI S.P.A. ,  D'ESTE, Matteo ,  RENIER, Davide ,  PASUT, Gianfranco ,  ROSATO, Antonio

    Inventor： D'ESTE, Matteo ,  RENIER, Davide ,  PASUT, Gianfranco ,  ROSATO, Antonio

    IPC: C08B37/00

    CPC classification number: C08B37/0072 ,  A61K31/726 ,  C08B37/0063 ,  C08B37/0069 ,  C08B37/0075

    Abstract: The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones. An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.

    Abstract translation: 本发明涉及一种用于合成糖胺聚糖（GAG）与不同性质的生物活性分子的缀合物的方法，其包含小分子和大分子。 特别地，本发明涉及透明质酸（HA）及其衍生物与具有生物作用的多肽和蛋白质（例如干扰素，促红细胞生成素，生长因子，胰岛素，细胞因子，抗体和激素）的缀合。 本发明的目的还涉及通过上述共轭方法中GAG与被保护的氨基醛的部分或全部反应获得的可分离的中间体。

    A PROCESS FOR THE PREPARATION OF ROTIGOTINE
    9.
    发明申请
    A PROCESS FOR THE PREPARATION OF ROTIGOTINE 审中-公开
    制备ROTIGOTINE的方法

    公开(公告)号：WO2010035111A1

    公开(公告)日：2010-04-01

    申请号：PCT/IB2009/006934

    申请日：2009-09-24

    Applicant: FIDIA FARMACEUTICI S.P.A. ,  BANFI, Aldo ,  BELOGI, Gianluca ,  FUGANTI, Claudio ,  PIZZOCARO, Roberta

    Inventor： BANFI, Aldo ,  BELOGI, Gianluca ,  FUGANTI, Claudio ,  PIZZOCARO, Roberta

    IPC: C07C215/48 ,  C07D333/20 ,  A61K31/381 ,  A61P25/00

    CPC classification number: C07D333/08 ,  C07C211/38 ,  C07C213/08 ,  C07C215/64 ,  C07C2602/10 ,  C07D333/20

    Abstract: A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid- sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II) The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-l-methoxy- naphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.

    Abstract translation: 一种制备罗替戈汀（I）及其药学上可接受的盐的方法，其包括用2-噻吩基乙酸 - 硼氢化钠络合物还原胺化式6的胺并使用氢溴酸盐5作为中间体（ II）从工业观点来看，该方法是有利的，因为它允许从光学活性的5,6,7,8-四氢-6-（S）-N-丙基氨基-1-甲氧基，得到具有高对映体纯度的罗替高汀 - 萘（2），避免使用危险的反应物，难以进行层析分离或形成副产物。 此外，公开了两种新的结晶形式。

    PROCESS FOR THE PREPARATION AND ISOLATION OF PHOSPHATIDES
    10.
    发明申请
    PROCESS FOR THE PREPARATION AND ISOLATION OF PHOSPHATIDES 审中-公开
    磷酸盐的制备和分离方法

    公开(公告)号：WO2006128639A2

    公开(公告)日：2006-12-07

    申请号：PCT/EP2006/005030

    申请日：2006-05-26

    Applicant: FIDIA FARMACEUTICI S.P.A. ,  ZANELLATO, Anna, Maria ,  PITTARELLO, Mara ,  GAMBILLARA, Antonio ,  VACCARO, Susanna

    Inventor： ZANELLATO, Anna, Maria ,  PITTARELLO, Mara ,  GAMBILLARA, Antonio ,  VACCARO, Susanna

    IPC: A61K31/685 ,  A61K8/14 ,  A61K47/48 ,  A23J7/00 ,  C07F9/10 ,  C12P9/00

    CPC classification number: A23J7/00 ,  A61K8/14 ,  A61K8/553 ,  A61Q19/00 ,  C07F9/10 ,  C12P9/00 ,  C12P13/06

    Abstract: Process for the preparation of phosphatidylserine of formula (I) wherein R 1 and R 2 independently represent a saturated, mono-unsaturated or polyunsaturated acyl C 10 -C 30 , X=OH or OM where M=alkaline or alkaline earth metal, ammonium, alkylammonium (including the inner salt) including the transphosphatidylation reaction between phosphatidylcholine of the general formula (II) wherein R 1 and R 2 and X have the above specified meanings, R 3 =CH 2 -CH 2 - NH 2 o CH 2 -CH 2 -N + (CH 3 ) 3 and Serine in D, L or racemic form catalysed by the phospholipase D enzyme (PLD), characterised in that said reaction is carried out in a hydroalcoholic medium containing an aliphatic alcohol and in the presence of bivalent metal oxide.

    Abstract translation: 式（I）的磷脂酰丝氨酸的制备方法其中R 1和R 2独立地表示饱和的，单不饱和的或多不饱和的酰基C 10 其中M =碱金属或碱土金属，铵，烷基铵（包括内盐），包括通式（II）的磷脂酰胆碱之间的磷脂酰化反应，其中R R 1，R 2和R 2具有上述含义，R 3 = CH 2 -CH 2， 2 CH 2 -CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 - 3）3和由磷脂酶D酶（PLD）催化的D，L或外消旋形式的丝氨酸，其特征在于所述反应在含有脂肪醇的水醇介质中进行， 在二价金属氧化物存在下。

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