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1. 发明申请

US20080206324A1 PELLETS HAVING AN ACTIVE COMPOUND MATRIX AND A POLYMER COATING, AND A PROCESS FOR THE PRODUCTION OF THE PELLETS 审中-公开
标题翻译：具有活性化合物基质和聚合物涂料的片剂以及生产小片剂的方法
公开(公告)号：US20080206324A1
公开(公告)日：2008-08-28
申请号：US12030377
申请日：2008-02-13
申请人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
发明人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
IPC分类号： A61K9/48 , A61K9/14 , A61K9/32
CPC分类号： A61K9/1635 , A61K9/5026 , A61K31/52
摘要： An active compound-containing pellet has a polymer coating of an anionic (meth)acrylate copolymer and a pharmaceutically active substance, embedded in a polymer matrix of one or more polymers, a particle size in the range from 300 to 1100 μm, a friability of at most 0.1%, measured using 200 g of pellets in a screening machine having a 200 μm screen, a screening diameter of 20 cm and 1.5 mm shaking amplitude at a shaking frequency of 50 l/sec for 10 min in the presence of six rubber cubes having a 1.8 cm edge length, with the proviso that the pellet releases no more than 10% of the active compound in a release test according to USP in artificial gastric juice at pH 1.2 after 120 min.
摘要翻译：含活性化合物的颗粒具有嵌入在一种或多种聚合物的聚合物基质中的阴离子（甲基）丙烯酸酯共聚物和药物活性物质的聚合物涂层，粒度在300至1100μm的范围内，脆性在具有200μm筛网的筛选机中使用200g粒料测量，至少0.1％，筛选直径为20cm和1.5mm，振荡频率为50l / sec，在六个橡胶存在下摇动10分钟具有1.8厘米边缘长度的立方体，条件是在120分钟后pH 1.2的人造胃液中，根据USP的释放试验中，颗粒释放不超过10％的活性化合物。

2. 发明申请

US20130096272A1 PROCESS FOR PREPARING A (METH)ACRYLATE COPOLYMER CONTAINING TERTIARY AMINO GROUPS BY FREE-RADICAL POLYMERIZATION IN SOLUTION 有权
标题翻译：通过溶液中的自由基聚合制备含有仲胺基团的（甲基）丙烯酸酯共聚物的方法
公开(公告)号：US20130096272A1
公开(公告)日：2013-04-18
申请号：US13805523
申请日：2010-10-13
申请人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
发明人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
IPC分类号： C08F2/06
CPC分类号： C08F2/06 , C08F220/12 , C08F220/34
摘要： The invention relates to a process for preparing a (meth)acrylate copolymer containing quaternary ammonium groups from a monomer mixture selected from: (a) 80 to 99% by weight of a C1-C4-alkyl ester of acrylic acid or methacrylic acid; and (b) 20 to 1% by weight of an alkyl ester of acrylic acid or methacrylic acid with a quaternary ammonium group in the alkyl radical; and (c) 0 to 10% of further copolymerizable vinyl monomers whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120 C over a period of 2 to 24 hours, where the polymerization mixture is polymerized to a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder and where the copolymer preparation is characterized by a molecular weight (Mw) of 25.000 to 50.000, a polydispersity index of 2.0 to 3.0 and a residual solvent concentration of less than 10.000 ppm by weight.
摘要翻译：本发明涉及一种从单体混合物制备含有季铵基的（甲基）丙烯酸酯共聚物的方法，所述单体混合物选自：（a）80-99重量％的丙烯酸或甲基丙烯酸的C 1 -C 4 - 烷基酯; 和（b）20至1重量％的烷基中具有季铵基团的丙烯酸或甲基丙烯酸的烷基酯; 和（c）0至10％的另外的可共聚的乙烯基单体，由此将一种或多种聚合引发剂，任选的一种或多种分子量调节剂和一种或多种溶剂或溶剂混合物加入到单体混合物中，得到聚合混合物，其中在2〜24小时的时间内在30〜120℃的温度下聚合，聚合混合物聚合成聚合浆料，其中单体向共聚物的转化率为至少99重量％，其中聚合糖浆为随后通过蒸馏或通过挤出脱气，并将脱气聚合糖浆进一步粉碎成颗粒或粉末形式的共聚物制剂，其中共聚物制剂的特征在于分子量（Mw）为25.000至50.000，多分散指数 2.0〜3.0，残留溶剂浓度小于10.000重量ppm。

3. 发明授权

US08822613B2 Process for preparing a (meth)acrylate copolymer containing quaternary ammonium groups by free-radical polymerization in solution 有权
标题翻译：在溶液中通过自由基聚合制备含有季铵基团的（甲基）丙烯酸酯共聚物的方法
公开(公告)号：US08822613B2
公开(公告)日：2014-09-02
申请号：US13805523
申请日：2010-10-13
申请人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
发明人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
IPC分类号： C08F2/06
CPC分类号： C08F2/06 , C08F220/12 , C08F220/34
摘要： The invention relates to a process for preparing a (meth)acrylate copolymer containing quaternary ammonium groups from a monomer mixture selected from: (a) 80 to 99% by weight of a C1-C4-alkyl ester of acrylic acid or methacrylic acid; and (b) 20 to 1% by weight of an alkyl ester of acrylic acid or methacrylic acid with a quaternary ammonium group in the alkyl radical; and (c) 0 to 10% of further copolymerizable vinyl monomers whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120 C over a period of 2 to 24 hours, where the polymerization mixture is polymerized to a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder and where the copolymer preparation is characterized by a molecular weight (Mw) of 25.000 to 50.000, a polydispersity index of 2.0 to 3.0 and a residual solvent concentration of less than 10.000 ppm by weight.
摘要翻译：本发明涉及一种从单体混合物制备含有季铵基的（甲基）丙烯酸酯共聚物的方法，所述单体混合物选自：（a）80-99重量％的丙烯酸或甲基丙烯酸的C 1 -C 4 - 烷基酯; 和（b）20至1重量％的烷基中具有季铵基团的丙烯酸或甲基丙烯酸的烷基酯; 和（c）0至10％的另外的可共聚的乙烯基单体，由此将一种或多种聚合引发剂，任选的一种或多种分子量调节剂和一种或多种溶剂或溶剂混合物加入到单体混合物中，得到聚合混合物，其中在2〜24小时的时间内在30〜120℃的温度下聚合，聚合混合物聚合成聚合浆料，其中单体向共聚物的转化率为至少99重量％，其中聚合糖浆为随后通过蒸馏或通过挤出脱气，并将脱气聚合糖浆进一步粉碎成颗粒或粉末形式的共聚物制剂，其中共聚物制剂的特征在于分子量（Mw）为25.000至50.000，多分散指数 2.0〜3.0，残留溶剂浓度小于10.000重量ppm。

4. 发明申请

US20130190468A1 PROCESS FOR PREPARING A (METH)ACRYLATE COPOLYMER CONTAINING TERTIARY AMINO GROUPS BY FREE-RADICAL POLYMERIZATION IN SOLUTION 有权
标题翻译：通过溶液中的自由基聚合制备含有仲胺基团的（甲基）丙烯酸酯共聚物的方法
公开(公告)号：US20130190468A1
公开(公告)日：2013-07-25
申请号：US13876277
申请日：2010-10-13
申请人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
发明人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
IPC分类号： C08F2/04
CPC分类号： C08F2/04 , C08F220/18 , C08F220/34
摘要： The invention relates to a process for preparing a (meth)acrylate copolymer containing tertiary amino groups by free-radical polymerization in solution from a monomer mixture selected from a) 30 to 70% by weight of a C1-C4-alkyl ester of acrylic acid or methacrylic acid and b) 70 to 30% by weight of an alkyl ester of acrylic acid or methacrylic acid with a tertiary amino group in the alkyl radical and c) 0 to 10% of further copolymerizable vinyl monomers, whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120° C. over a period of 2 to 24 hours, where the polymerization mixture is finally polymerized to give a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder, where the copolymer preparation is characterized by a molecular weight (Mw) of 25.000 to 75.000 g/mol a polydispersity index of 2.1 to 2.9 and a residual solvent concentration of less than 1.000 ppm by weight.
摘要翻译：本发明涉及一种通过自由基聚合制备含有叔氨基的（甲基）丙烯酸酯共聚物的方法，该方法是从选自a）30至70重量％的丙烯酸C 1 -C 4烷基酯的单体混合物或甲基丙烯酸，b）70〜30重量％的烷基中丙烯酸或甲基丙烯酸与叔氨基的烷基酯，和c）0〜10％的其它可共聚乙烯基单体，由此一个或多个聚合引发剂，任选地将一种或多种分子量调节剂和一种或多种溶剂或溶剂混合物加入到单体混合物中，得到聚合混合物，其在30至120℃的温度下在2至24小时的时间内聚合其中聚合混合物最终聚合以得到聚合浆料，其中单体向共聚物的转化率至少为99重量％，其中聚合糖浆随后通过蒸馏脱气或通过挤出，并将脱气的聚合糖浆进一步粉碎成颗粒或粉末形式的共聚物制剂，其中共聚物制剂的特征在于分子量（Mw）为25.000至75.000g / mol，多分散指数为2.1至 2.9，残留溶剂浓度小于1.000重量ppm。

5. 发明授权

US08859697B2 Process for preparing a (meth)acrylate copolymer containing tertiary amino groups by free-radical polymerization in solution 有权
标题翻译：在溶液中通过自由基聚合制备含有叔氨基的（甲基）丙烯酸酯共聚物的方法
公开(公告)号：US08859697B2
公开(公告)日：2014-10-14
申请号：US13876277
申请日：2010-10-13
申请人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
发明人： Christian Meier , Andreas Weber , Johannes Vorholz , Alpertunga Kueksal , Andreas Klosendorf , Pamela Boehmann , Marcus Denger , Norbert Hoffmann , Nikolaos Papadopoulos
IPC分类号： C08F2/06 , C08F220/34 , C08F2/04 , C08F220/18
CPC分类号： C08F2/04 , C08F220/18 , C08F220/34
摘要： The invention relates to a process for preparing a (meth)acrylate copolymer containing tertiary amino groups by free-radical polymerization in solution from a monomer mixture selected from a) 30 to 70% by weight of a C1-C4-alkyl ester of acrylic acid or methacrylic acid and b) 70 to 30% by weight of an alkyl ester of acrylic acid or methacrylic acid with a tertiary amino group in the alkyl radical and c) 0 to 10% of further copolymerizable vinyl monomers, whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120° C. over a period of 2 to 24 hours, where the polymerization mixture is finally polymerized to give a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder, where the copolymer preparation is characterized by a molecular weight (Mw) of 25.000 to 75.000 g/mol a polydispersity index of 2.1 to 2.9 and a residual solvent concentration of less than 1.000 ppm by weight.
摘要翻译：本发明涉及一种通过自由基聚合制备含有叔氨基的（甲基）丙烯酸酯共聚物的方法，该方法是从选自a）30至70重量％的丙烯酸C 1 -C 4烷基酯的单体混合物或甲基丙烯酸，b）70〜30重量％的烷基中丙烯酸或甲基丙烯酸与叔氨基的烷基酯，和c）0〜10％的其它可共聚乙烯基单体，由此一个或多个聚合引发剂，任选地将一种或多种分子量调节剂和一种或多种溶剂或溶剂混合物加入到单体混合物中，得到聚合混合物，其在30至120℃的温度下在2至24小时的时间内聚合其中聚合混合物最终聚合以得到聚合浆料，其中单体向共聚物的转化率至少为99重量％，其中聚合糖浆随后通过蒸馏脱气或通过挤出，并将脱气的聚合糖浆进一步粉碎成颗粒或粉末形式的共聚物制剂，其中共聚物制剂的特征在于分子量（Mw）为25.000至75.000g / mol，多分散指数为2.1至 2.9，残留溶剂浓度小于1.000重量ppm。

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