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1. 发明授权

US08367848B2 Process for the preparation of amorphous calcium salt of atorvastatin 有权
标题翻译：阿托伐他汀无定形钙盐的制备方法
公开(公告)号：US08367848B2
公开(公告)日：2013-02-05
申请号：US10552562
申请日：2004-04-09
申请人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
发明人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： Present invention refers to the process of preparing amorphous atorvastatin calcium without intermediate isolation of crystal or undefined mixture of crystal and amorphous atorvastatin calcium, respectively. Forming of calcium atorvastatin salt is carried out in a mixture of chlorinated organic solvent or cyclic hydrocarbon solvent, respectively, the non-hydroxylic organic solvent, and water, the source of calcium ions is calcium acetate or calcium chloride, respectively.
摘要翻译：本发明涉及制备无定形阿托伐他汀钙的方法，而不分别晶体或无定形阿托伐他汀钙混合物的中间分离。钙阿托伐他汀盐的形成分别在氯化有机溶剂或环烃溶剂，非羟基有机溶剂和水的混合物中进行，钙离子的来源分别是乙酸钙或氯化钙。

2. 发明申请

US20090208573A1 NOVEL POLYMORPH FORM OF IRBESARTAN 审中-公开
标题翻译： IRBESARTAN的新型POLYMORPH形式
公开(公告)号：US20090208573A1
公开(公告)日：2009-08-20
申请号：US11577725
申请日：2005-11-09
申请人： Ljubomir Antoncic
发明人： Ljubomir Antoncic
IPC分类号： A61K9/28 , C07D257/04 , A61K31/41 , A61K31/5415 , A61P9/00
CPC分类号： C07D403/10
摘要： New form of irbesartan having favourable chargeability is prepared from the alcoholic/etheric or ketonic solution of irbesartan after slow cooling with sporadic or light agitation and alternatively new crystalline form of an acid addition salt of irbesartan is prepared from the aqueous solution of a sodium salt of irbesartan after strongly acidifying aforesaid solution and subsequently adjusting pH with an alkali. Those are used in manufacturing a pharmaceutical composition.
摘要翻译：由缓慢冷却后偶尔或轻度搅动的厄贝沙坦的醇/乙醚或酮溶液制备具有良好带电性的新形式的厄贝沙坦，并且从盐酸钠盐的水溶液中制备厄贝沙坦的酸加成盐的新结晶形式厄贝沙坦在强酸化上述溶液后，随后用碱调节pH。这些用于制造药物组合物。

3. 发明授权

US07271269B2 Preparation of new pharmaceutically suitable salt of losartan and forms thereof with new purification and isolation methods 失效
标题翻译：用新的纯化和分离方法制备新的药物合适的氯沙坦盐及其形式
公开(公告)号：US07271269B2
公开(公告)日：2007-09-18
申请号：US10524993
申请日：2004-01-29
申请人： Ljubomir Antoncic , Anton Copar , Peter Svete , Breda Husu-Kovacevic , Zoran Ham , Boris Marolt
发明人： Ljubomir Antoncic , Anton Copar , Peter Svete , Breda Husu-Kovacevic , Zoran Ham , Boris Marolt
IPC分类号： C07D257/04
CPC分类号： C07D403/10
摘要： Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2′-(1 H-tetrazole-5-yl)[1.1′-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2′-(1H-tetrazole-5-yl)[1.1′-biphenyl]-44-yl]-1H-imidazole have been prepared.
摘要翻译： 2-正丁基-4-氯-5-羟基甲基-1 - [[2' - （1H-四唑-5-基）[1.1'-联苯]的药学上合适的结晶和无定形碱金属和碱土金属盐 ] -4-基] -1H-咪唑，并描述了高纯度的所述盐的新的制备，纯化和分离程序。含有2-正丁基-5-氯-5-羟基甲基-1 - [[2' - （1H-四唑-5-基）[1.1'-联苯] -44-基] -1H的新结晶钾盐的稳定药物组合物咪唑制备。

4. 发明申请

US20070179308A1 Process for preparing amophous (4r-cis)-6-[2-[3-phenyl-4-(Phenylcarbamoyl)-2-4-Fluorophenyl)-5-(1-Methylethyl)-Pyrrol-1-YL]-Ethyl]-2,2-Dimethyl-[1,3]-Dioxane-4-YL-Acetic Acid 有权
标题翻译：（4r顺式）-6- [2- [3-苯基-4-（苯基氨基甲酰基）-2-4-氟苯基）-5-（1-甲基乙基） - 吡咯-1-基] - 乙基] -2,2-二甲基 - [1,3] - 二氧杂环己烷-4-YL-乙酸
公开(公告)号：US20070179308A1
公开(公告)日：2007-08-02
申请号：US10584638
申请日：2004-12-27
申请人： Ljubomir Antoncic
发明人： Ljubomir Antoncic
IPC分类号： C07C255/00
CPC分类号： C07D405/06 , C07D207/34
摘要： The invention relates to a process of preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid-tertiary butyl ester which is a useful pharmaceutical intermediate in the preparation of atorvastatin salts.
摘要翻译：本发明涉及制备无定形（4R-顺式）-6- [2- [3-苯基-4-（苯基氨基甲酰基）-2-（4-氟苯基）-5-（1-甲基乙基） - 吡咯-1-基] - 基] - 乙基] -2,2-二甲基 - [1,3] - 二恶烷-4-基 - 乙酸叔丁酯，其是制备阿托伐他汀盐的有用药物中间体。

5. 发明授权

US08697741B2 Process for the preparation of amorphous calcium salt of atorvastatin 失效
标题翻译：阿托伐他汀无定形钙盐的制备方法
公开(公告)号：US08697741B2
公开(公告)日：2014-04-15
申请号：US12397981
申请日：2009-03-04
申请人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
发明人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34
摘要： A process for the preparation of amorphous atorvastatin calcium. The process includes providing a reaction mixture having a pH between 6.5 and 8.0 containing a sodium salt of atorvastatin and tetrahydrofuran. A non-cyclic chlorinated organic solvent selected from the group consisting of dichloromethane, trichloroethane, tetrachloroethane and chloroform or addition of cyclic hydrocarbon solvent selected from the group consisting of cyclohexane, cyclopentane and methyl cyclohexane is added to provide a mixture of organic solvents. An equivalent or an excess quantity of a source of calcium ions selected from the group consisting of calcium acetate and calcium chloride is added. Amorphous atorvastatin calcium is isolated from an organic phase comprising the mixture of organic solvents.
摘要翻译：一种制备无定形阿托伐他汀钙的方法。该方法包括提供pH为6.5至8.0的含有阿托伐他汀和四氢呋喃的钠盐的反应混合物。加入选自二氯甲烷，三氯乙烷，四氯乙烷和氯仿的非环状氯化有机溶剂或加入选自环己烷，环戊烷和甲基环己烷的环状烃溶剂以提供有机溶剂的混合物。加入等量或过量的钙离子源，其选自乙酸钙和氯化钙。从包含有机溶剂的混合物的有机相中分离无定形阿托伐他汀钙。

6. 发明申请

US20090012140A1 Preparation of Telmisartan Salts with Improved Solubility 审中-公开
标题翻译：改善溶解度的替米沙坦盐的制备
公开(公告)号：US20090012140A1
公开(公告)日：2009-01-08
申请号：US11718838
申请日：2005-11-09
申请人： Ljubomir Antoncic , Anton Copar
发明人： Ljubomir Antoncic , Anton Copar
IPC分类号： A61K31/4184 , C07D403/04 , A61P9/12
CPC分类号： C07D235/20
摘要： New alkali and earth-alkali salts of telmisartan in amorphous form and a new crystalline sodium salt of telmisartan have been prepared by preparing a solution despite low solubility of telmisartan and rapidly vacuum evaporating to dryness.
摘要翻译：通过制备溶液，尽管替米沙坦的溶解度低，并且迅速真空蒸发至干，已经制备了无定形形式的替米沙坦替代米沙坦的新碱和碱 - 碱盐和替米沙坦的新结晶钠盐。

7. 发明申请

US20060287538A1 Process for the preparation of amorphous calcium salt of atorvastatin 有权
公开(公告)号：US20060287538A1
公开(公告)日：2006-12-21
申请号：US10552562
申请日：2004-04-09
申请人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
发明人： Ljubomir Antoncic , Gorazd Sorsak , Anton Copar
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： Present invention refers to the process of preparing amorphous atorvastatin calcium without intermediate isolation of crystal or undefined mixture of crystal and amorphous atorvastatin calcium, respectively. Forming of calcium atorvastatin salt is carried out in a mixture of chlorinated organic solvent or cyclic hydrocarbon solvent, respectively, the non-hydroxylic organic solvent, and water, the source of calcium ions is calcium acetate or calcium chloride, respectively.

8. 发明申请

US20060004207A1 Preparation of new pharmaceutically suitable salt of losartan and forms thereof with new purification and isolation methods 失效
标题翻译：用新的纯化和分离方法制备新的药物合适的氯沙坦盐及其形式
公开(公告)号：US20060004207A1
公开(公告)日：2006-01-05
申请号：US10524993
申请日：2004-01-29
申请人： Ljubomir Antoncic , Anton Copar , Peter Svete , Breda Husu-Kovacevic , Zoran Ham , Boris Marolt
发明人： Ljubomir Antoncic , Anton Copar , Peter Svete , Breda Husu-Kovacevic , Zoran Ham , Boris Marolt
IPC分类号： C07D403/02 , A61K31/4184
CPC分类号： C07D403/10
摘要： Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2′-(1H-tetrazole-5-yl)[1.1′-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2′-(1H-tetrazole-5-yl)[1.1′-biphenyl]-44-yl]-1H-imidazole have been prepared.
摘要翻译： 2-正丁基-4-氯-5-羟基甲基-1 - [[2' - （1H-四唑-5-基）[1.1'-联苯]]酮的药学上合适的结晶和无定形碱金属和碱土金属盐， -4-基] -1H咪唑，并描述了高纯度的所述盐的新的制备，纯化和分离程序。含有2-正丁基-5-氯-5-羟基甲基-1 - [[2' - （1H-四唑-5-基）[1.1'-联苯] -44-基] -1H的新结晶钾盐的稳定药物组合物咪唑制备。

9. 发明授权

US07968727B2 Synthesis of 4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl and its use in preparation of angiotensin II antagonists 失效
标题翻译： 4-溴甲基-2'-甲酰基联苯和4-溴甲基-2'-羟甲基联苯的合成及其在制备血管紧张素II拮抗剂中的应用
公开(公告)号：US07968727B2
公开(公告)日：2011-06-28
申请号：US11887637
申请日：2006-03-30
申请人： Anton Copar , Ljubomir Antoncic , Matej Antoncic
发明人： Anton Copar , Ljubomir Antoncic , Matej Antoncic
IPC分类号： C07D235/06 , C07C255/03 , C07C47/54 , C07C33/24
CPC分类号： C07D235/02 , C07C33/46 , C07C45/44 , C07C47/55 , C07D403/04 , C07D417/08 , C07C47/546
摘要： 4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2′-cyanobiphenyl or 4′-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
摘要翻译： 4-溴甲基-2'-甲酰基联苯和4-溴甲基-2'-羟甲基联苯是用于制备各种血管紧张素II拮抗剂的起始原料，其由4-溴甲基-2'-氰基联苯或4'-溴甲基联苯羧基衍生物制备，使用所选择的氢化物试剂。

10. 发明授权

US07943786B2 Process for preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid 有权
标题翻译：制备无定形（4R-顺式）-6- [2- [3-苯基-4-（苯基氨基甲酰基）-2-（4-氟苯基）-5-（1-甲基乙基） - 吡咯-1-基] - 乙基 ] -2,2-二甲基 - [1,3] - 二恶烷-4-基 - 乙酸
公开(公告)号：US07943786B2
公开(公告)日：2011-05-17
申请号：US10584638
申请日：2004-12-27
申请人： Ljubomir Antoncic , Gorazd Sorsak
发明人： Ljubomir Antoncic , Gorazd Sorsak
IPC分类号： C07D405/00
CPC分类号： C07D405/06 , C07D207/34
摘要： The invention relates to a process of preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid-tertiary butyl ester which is a useful pharmaceutical intermediate in the preparation of atorvastatin salts.
摘要翻译：本发明涉及制备无定形（4R-顺式）-6- [2- [3-苯基-4-（苯基氨基甲酰基）-2-（4-氟苯基）-5-（1-甲基乙基） - 吡咯-1-基] - 基] - 乙基] -2,2-二甲基 - [1,3] - 二恶烷-4-基 - 乙酸叔丁酯，其是制备阿托伐他汀盐的有用药物中间体。

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