公开(公告)号：US07569549B2

公开(公告)日：2009-08-04

申请号：US10390573

申请日：2003-03-17

申请人： Miljenko Dumic ,  Mladen Vinkovic ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Zdravka Knezevic ,  Gorjana Lazarevski ,  Dominik Cincic ,  Darko Filic ,  Katica Lazaric ,  Dejan Kresimir Bucar

发明人： Miljenko Dumic ,  Mladen Vinkovic ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Zdravka Knezevic ,  Gorjana Lazarevski ,  Dominik Cincic ,  Darko Filic ,  Katica Lazaric ,  Dejan Kresimir Bucar

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/00 ,  C07H17/08

摘要： Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 Å, b=15.5-17.0 Å, and c=17.5-19.5 Å, and angles between the crystal axes of α=γ=90° and β=106°-112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

摘要翻译： 具有式I的9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的基本上纯的同态结构假多晶型物：其中S是与水至少部分混溶的有机溶剂，x为1,1.25,1.5或2 ，y为0,0.5或1，所述假多晶型物的特征在于单斜晶系空间群P21和平均晶胞参数，其包括：晶轴长度a =15.5-17.0，b =15.5-17.0，c = 17.5- α=γ= 90°和β= 106°-112°的晶轴之间的角度。 此外，本公开涉及制备式I的基本上纯的同态结构假多晶型物的方法; 包含基本上纯的式I的同态假多晶型物的药物组合物; 以及用于治疗细菌和原生动物感染以及炎症相关疾病的方法，其通过施用含有基本上纯的式I的同型结构假多晶型物的药物组合物。

公开(公告)号：US06936591B2

公开(公告)日：2005-08-30

申请号：US10624911

申请日：2003-07-21

申请人： Miljenko Dumić ,  Mladen Vinković ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Knezevic Zdravka ,  Gorjana Lazarevski ,  Darko Filic ,  Dominik Cincic ,  Katica Lazaric ,  Dejan-Kresimir Bucar

发明人： Miljenko Dumić ,  Mladen Vinković ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Knezevic Zdravka ,  Gorjana Lazarevski ,  Darko Filic ,  Dominik Cincic ,  Katica Lazaric ,  Dejan-Kresimir Bucar

IPC分类号： C07H17/08 ,  A61K31/70 ,  C07H1/00

CPC分类号： C07H17/08

摘要： Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I: wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P212121, with average unit cell parameters a=8.2 to 9.7 Å, b=11.5 to 13.5 Å, c=44.5 to 47.0 Å, α=β=γ=90°, wherein a, b and c represent the crystal axes lengths and α, β and γ represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.

摘要翻译： 基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A.此外，本发明涉及一种由9-脱氧-9a-氮杂-9a-甲基-9a- 通过通式I的9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的正交同构异构体假多晶型物的同型红霉素A：其中S表示水混溶性或水不混溶性有机溶剂，其特征在于正交空间群 其中平均单元电池参数a = 8.2至9.7，b = 11.5至13.5，c = 44.5 至47.0A，α=β=γ= 90°，其中a，b和c表示晶轴长度，α，β和γ表示晶轴之间的角度。 此外，公开了含有基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的药物组合物，以及用于治疗细菌和原生动物感染以及与人类发生炎症有关的疾病的方法 动物通过施用含有它们的药物组合物。

公开(公告)号：US20070276015A1

公开(公告)日：2007-11-29

申请号：US11822274

申请日：2007-07-03

申请人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Oresic ,  Jasna Horvat Mikulcic

发明人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Oresic ,  Jasna Horvat Mikulcic

IPC分类号： A61K31/44 ,  A61P11/00 ,  A61P25/08 ,  A61P27/06 ,  A61P7/10 ,  A61P9/00 ,  A61P9/12 ,  C07D213/74

CPC分类号： A61K31/44 ,  C07D213/53 ,  C07D213/71 ,  C07D213/74

摘要： The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.

摘要翻译： 本发明涉及托拉塞米的新晶体改性III的表征，其制备方法是通过使用托拉塞米的碱性溶液与无机或有机酸（有或没有加入晶种）将其酸化至其 用作制备托拉塞米和托拉塞米的药学上可接受的盐的晶体改性I的原料以及含有托拉塞米的这种新的结晶改性III的药物形式。

公开(公告)号：US20060205951A1

公开(公告)日：2006-09-14

申请号：US11357109

申请日：2006-02-21

申请人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Oresic ,  Jasna Horvat Mikulcic

发明人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Oresic ,  Jasna Horvat Mikulcic

IPC分类号： C07D213/75

CPC分类号： A61K31/44 ,  C07D213/53 ,  C07D213/71 ,  C07D213/74

摘要： The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.

公开(公告)号：US07037928B2

公开(公告)日：2006-05-02

申请号：US10416303

申请日：2001-01-31

申请人： Miljenko Dumic ,  Darko Filic ,  Bozena Klepic ,  Aleksandar Danilovski ,  Marijan Tudja

发明人： Miljenko Dumic ,  Darko Filic ,  Bozena Klepic ,  Aleksandar Danilovski ,  Marijan Tudja

IPC分类号： A61K31/44 ,  C07D213/02

CPC分类号： A61K31/44 ,  A61K31/715 ,  A61K31/724 ,  A61K45/06 ,  A61K47/6951 ,  B82Y5/00 ,  A61K2300/00

摘要： The invention relates to compositions of N-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyridylsul fonamide and cyclic oligosaccharides with increased release, to methods for their preparation, to pharmaceutical froms containing them as well as to their use.

摘要翻译： 本发明涉及N-（1-甲基乙基氨基羰基）-4-（3-甲基苯基氨基）-3-吡啶基磺酰胺和释放增加的环状寡糖，其制备方法，含有它们的药物以及它们的用途的组合物 。

公开(公告)号：US20060100439A1

公开(公告)日：2006-05-11

申请号：US10521609

申请日：2003-07-07

申请人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Marinkovic ,  Jasna Horvat-Mikulcic

发明人： Darko Filic ,  Miljenko Dumic ,  Aleksandar Danilovski ,  Bozena Klepic ,  Ines Fistric ,  Marina Marinkovic ,  Jasna Horvat-Mikulcic

IPC分类号： C07D213/75

CPC分类号： C07D213/74

摘要： The invention relates to a new process for the preparation of modification I of torasemide by precipitation with acids from an alkaline extract of the original reaction mixture of the last phase in the synthesis of torasemide.

摘要翻译： 本发明涉及一种通过在合成托拉塞米的最后阶段的原始反应混合物的碱性提取物中用酸沉淀制备托拉塞米的修饰I的新方法。

公开(公告)号：US20070238759A1

公开(公告)日：2007-10-11

申请号：US11763156

申请日：2007-06-14

申请人： Darko Filic ,  Miljenko Dumic ,  Bozena Klepic ,  Aleksandar Danilovski ,  Marijan Tudja

发明人： Darko Filic ,  Miljenko Dumic ,  Bozena Klepic ,  Aleksandar Danilovski ,  Marijan Tudja

IPC分类号： C07D213/74 ,  A61K31/44

CPC分类号： C07D213/74

摘要： The invention relates to a novel polymorph V of torasemide, to a process for its preparation, to its use as a raw material for the preparation of crystalline modifications I and III of torasemide, to amorphous torasemide modifications and to pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the said novel polymorph V of torasemide as the active ingredient as well as to its use.

摘要翻译： 本发明涉及托拉塞米的新型多晶型V，其制备方法，其用作制备托拉塞米的晶体修饰I和III的原料，其用于无定形托拉塞米改性和托拉塞米的药学上可接受的盐， 含有所述新型多晶型V的托拉塞米作为活性成分的药物形式及其用途。

公开(公告)号：US20050004172A1

公开(公告)日：2005-01-06

申请号：US10847900

申请日：2004-05-17

申请人： Darko Filic ,  Nada Hulita ,  Aleksandar Danilovski ,  Zvonimir Siljkovic ,  Helena Ceric ,  Miljenko Dumic ,  Miroslav Zegarac

发明人： Darko Filic ,  Nada Hulita ,  Aleksandar Danilovski ,  Zvonimir Siljkovic ,  Helena Ceric ,  Miljenko Dumic ,  Miroslav Zegarac

IPC分类号： A61K31/4439 ,  A61P1/04 ,  C07D401/12 ,  C07

CPC分类号： C07D401/12

摘要： The present disclosure relates to new solid-state forms of 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium aqua complexes, and to processes for their preparation. The disclosure is also directed to pharmaceutical compositions containing the solid-state forms, and the methods of treatment using the solid-state forms.

摘要翻译： 本公开涉及5-（二氟甲氧基）-2 - [[（3,4-二甲氧基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑钠水溶液复合物的新型固体形式及其制备方法 。 本公开还涉及含有固态形式的药物组合物和使用固态形式的治疗方法。

公开(公告)号：US20110184030A1

公开(公告)日：2011-07-28

申请号：US12309260

申请日：2007-07-13

申请人： Aleksandar Danilovski ,  Maja Devcic ,  Marina Marinkovic ,  Ernest Mestrovic ,  Tina Mundorfer ,  Iva Tunjic

发明人： Aleksandar Danilovski ,  Maja Devcic ,  Marina Marinkovic ,  Ernest Mestrovic ,  Tina Mundorfer ,  Iva Tunjic

IPC分类号： A61K31/44 ,  C07D213/75 ,  A61P25/04 ,  A61P25/16 ,  A61P21/02

CPC分类号： C07D213/75

摘要： The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.

摘要翻译： 本发明涉及马来酸氟吡汀的新型多晶型物，新型多晶型物的制备方法，含有它们的药物组合物，其治疗用途和使用它们的治疗方法。

公开(公告)号：US20090137613A1

公开(公告)日：2009-05-28

申请号：US12293239

申请日：2007-03-06

申请人： Helena Ceric ,  Zvonimir Siljkovic ,  Iva Tunjic ,  Aleksandar Danilovski ,  Ernest Mestrovic

发明人： Helena Ceric ,  Zvonimir Siljkovic ,  Iva Tunjic ,  Aleksandar Danilovski ,  Ernest Mestrovic

IPC分类号： A61K31/522

CPC分类号： C07D473/32

摘要： The present invention is concerned with new pharmaceutically acceptable salts of valacyclovir, polymorphic forms, processes for preparing the new pharmaceutically acceptable salts and new polymorphic forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same.

摘要翻译： 本发明涉及新的可待因的伐昔洛韦盐，多晶型物，制备新的药学上可接受的盐和新的多晶型物的方法，含有它们的药物组合物，其治疗用途和使用该盐的治疗方法。