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    Mixtures of polypeptides, compositions containing and processes for preparing same, for treating neurodegenerative diseases
    1.
    发明授权
    Mixtures of polypeptides, compositions containing and processes for preparing same, for treating neurodegenerative diseases 有权
    多肽混合物，含有它们的组合物及其制备方法，用于治疗神经变性疾病

    公开(公告)号：US07560100B2

    公开(公告)日：2009-07-14

    申请号：US11223408

    申请日：2005-09-09

    申请人： Irit Pinchasi ,  Ben-Zion Dolitzky ,  Anton Frenkel ,  Michal Schwartz ,  Ruth Arnon ,  Rina Aharoni

    发明人： Irit Pinchasi ,  Ben-Zion Dolitzky ,  Anton Frenkel ,  Michal Schwartz ,  Ruth Arnon ,  Rina Aharoni

    IPC分类号： A61K31/74

    CPC分类号： C07K14/001 ,  A61K38/02

    摘要： The invention provides a composition comprising a mixture of polypeptides, wherein each polypeptide (a) is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine, and L-lysine, and (b) may be in the form of a pharmaceutically acceptable salt; and wherein in the mixture (i) the polypeptides have an average molecular weight in the range 13,500 to 18,500 daltons, (ii) 13% to 38% of the polypeptides have a diethylamide group instead of a carboxyl group present at one end thereof, and (iii) 68% of the polypeptides have a molecular weight between 7,000 and 41,000 daltons. In an embodiment, the average molecular weight is 16,000 daltons. The invention also provides a method of treating a human subject afflicted with a neurodegenerative disease comprising administering to the human subject a therapeutically effective amount of any of the disclosed compositions so as to thereby treat the human subject.

    摘要翻译： 本发明提供包含多肽混合物的组合物，其中每个多肽（a）是L-谷氨酸，L-丙氨酸，L-酪氨酸和L-赖氨酸的氨基酸的共聚物，和（b）可以在 形式的药学上可接受的盐; 并且其中在所述混合物（i）中，所述多肽的平均分子量范围为13,500至18,500道尔顿，（ii）13％至38％的多肽具有二乙酰胺基团而不是存在于其一端的羧基，以及 （iii）68％的多肽具有7,000至41,000道尔顿的分子量。 在一个实施方式中，平均分子量为16,000道尔顿。 本发明还提供了治疗患有神经变性疾病的人类受试者的方法，包括向人类受试者施用治疗有效量的任何所公开的组合物，从而治疗人受试者。

    POLYMORPHS OF FEXOFENADINE HYDROCHLORIDE
    2.
    发明申请
    POLYMORPHS OF FEXOFENADINE HYDROCHLORIDE 审中-公开
    FEXOFENADINE HYDROCHLORIDE的聚合物

    公开(公告)号：US20090149497A1

    公开(公告)日：2009-06-11

    申请号：US12207372

    申请日：2008-09-09

    申请人： Ben-Zion DOLITZKY ,  Shlomit Wizel ,  Barnaba Krochmal ,  Dov Diller ,  Irwin Gross

    发明人： Ben-Zion DOLITZKY ,  Shlomit Wizel ,  Barnaba Krochmal ,  Dov Diller ,  Irwin Gross

    IPC分类号： A61K31/445 ,  C07D211/34

    CPC分类号： C07D211/22

    摘要： The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is anhydrous, but can be crystallized as a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.

    摘要翻译： 本发明提供盐酸非索非那定形式V，VI和VIII至XV的新型结晶形式及其制备和制备盐酸非索非那定的无定形形式和其它结晶形式的方法。 形式XIV和XV是乙酸乙酯的溶剂化物，而形式IX是无水的，但可以结晶为MTBE或环己烷的溶剂合物。 这些形式可用于给予人类和动物以减轻组胺引起的症状。 本发明还提供了新的结晶形式的药物组合物。

    Mixtures of polypeptides, compositions containing and processes for preparing same, and uses thereof
    7.
    发明申请
    Mixtures of polypeptides, compositions containing and processes for preparing same, and uses thereof 审中-公开
    多肽的组合物，含有的组合物及其制备方法及其用途

    公开(公告)号：US20070054857A1

    公开(公告)日：2007-03-08

    申请号：US11541263

    申请日：2006-09-29

    申请人： Irit Pinchasi ,  Ben-Zion Dolitzky ,  Anton Frenkel ,  Michal Schwartz ,  Ruth Arnon ,  Rina Aharoni

    发明人： Irit Pinchasi ,  Ben-Zion Dolitzky ,  Anton Frenkel ,  Michal Schwartz ,  Ruth Arnon ,  Rina Aharoni

    IPC分类号： A61K38/16

    CPC分类号： C07K14/001 ,  A61K38/02

    摘要： The invention provides a composition comprising a mixture of polypeptides, wherein each polypeptide (a) is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine, and L-lysine, and (b) may be in the form of a pharmaceutically acceptable salt; and wherein in the mixture (i) the polypeptides have an average molecular weight in the range 13,500 to 18,500 daltons, (ii) 13% to 38% of the polypeptides have a diethylamide group instead of a carboxyl group present at one end thereof, and (iii) 68% of the polypeptides have a molecular weight between 7,000 and 41,000 daltons. In an embodiment, the average molecular weight is 16,000 daltons, and processes for preparing and its uses.

    摘要翻译： 本发明提供包含多肽混合物的组合物，其中每个多肽（a）是L-谷氨酸，L-丙氨酸，L-酪氨酸和L-赖氨酸的氨基酸的共聚物，和（b）可以在 形式的药学上可接受的盐; 并且其中在所述混合物（i）中，所述多肽的平均分子量范围为13,500至18,500道尔顿，（ii）13％至38％的多肽具有二乙酰胺基团而不是存在于其一端的羧基，以及 （iii）68％的多肽具有7,000至41,000道尔顿的分子量。 在一个实施方案中，平均分子量为16,000道尔顿，其制备及其用途的方法。

    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    10.
    发明授权
    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide 失效
    制备6-羟基-3,4-二氢喹啉酮，西洛他唑和N-（4-甲氧基苯基）-3-氯丙酰胺的方法

    公开(公告)号：US06967209B2

    公开(公告)日：2005-11-22

    申请号：US10372201

    申请日：2003-02-25

    申请人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    发明人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    IPC分类号： C07C231/02 ,  C07C233/25 ,  C07D215/22 ,  C07D215/227 ,  A61K31/4704

    CPC分类号： C07D215/227 ,  C07C231/02 ,  C07C233/25

    摘要： A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxyphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.

    摘要翻译： 通过N-（4-甲氧基苯基）-3-氯丙酰胺的分子内Friedel-Crafts烷基化制备6-羟基-3,4-二氢喹啉酮的方法，其中将当量N-（4-甲氧基苯基）-3-氯丙酰胺与 提供了在约150℃至约220℃的高温下在DMSO中的路易斯酸或高沸点酰胺或胺。 该方法以高产率和高纯度产生6-HQ，使得其可用于随后的用于西洛他唑制备的反应，而无需中间纯化。 还提供了通过该方法制备西洛他唑的方法和改进的制备N-（4-甲氧基苯基）-3-氯丙酰胺的方法。