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1.发明授权Isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A 有权9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的异构体假多晶型物公开(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
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。
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2.发明授权Amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, process for preparing the same, and uses thereof 失效无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A，其制备方法及其用途公开(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
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。
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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
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。
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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.
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