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1. 发明申请

WO2004089895A1 PROCESS FOR THE PREPARATION OF AMORPHOUS CALCIUM SALT OF ATORVASTATIN 审中-公开
标题翻译：制备ATORVASTATIN的无定形钙盐的方法
公开(公告)号：WO2004089895A1
公开(公告)日：2004-10-21
申请号：PCT/SI2004/000019
申请日：2004-04-09
申请人： LEK PHARMACEUTICALS D.D. , ANTONCIC, Ljubomir , SORSAK, Gorazd , COPAR, Anton
发明人： ANTONCIC, Ljubomir , SORSAK, Gorazd , COPAR, Anton
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

WO2009095431A1 NOVEL SALTS OF O-DESMETHYL-VENLAFAXINE 审中-公开
标题翻译： O-DESMETHYL-VENLAFAXINE的新口服
公开(公告)号：WO2009095431A1
公开(公告)日：2009-08-06
申请号：PCT/EP2009/050987
申请日：2009-01-29
申请人： LEK PHARMACEUTICALS D.D. , BORUT, Furlan , COPAR, Anton
发明人： BORUT, Furlan , COPAR, Anton
IPC分类号： C07C215/64 , A61K31/137 , A61P25/00
CPC分类号： C07C215/64 , C07C2601/12
摘要： The present invention relates to novel pharmaceutically acceptable salts of desvenlafaxine with physiologically ubiquitous ions selected from sugar acids and vitamins, to processes for their preparation, to pharmaceutical compositions containing them and to the use thereof.
摘要翻译：本发明涉及脱甲霜拉坦与选自糖酸和维生素的生理学上普遍存在的离子的新药学上可接受的盐，其制备方法，含有它们的药物组合物及其用途。

3. 发明申请

WO2009115585A1 CATALYZED CARBONYLATION IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译：合成二氧化钛拮抗剂中的催化羰基化
公开(公告)号：WO2009115585A1
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053269
申请日：2009-03-19
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , COPAR, Anton , CLUZEAU, Jerome , PREMRL, Andrej
发明人： CASAR, Zdenko , COPAR, Anton , CLUZEAU, Jerome , PREMRL, Andrej
IPC分类号： C07D403/04
CPC分类号： C07C17/263 , C07C17/14 , C07C17/2632 , C07D235/20 , Y10T436/147777 , C07C25/18
摘要： One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
摘要翻译：本发明公开的一个实施方案是通过格利雅化学及其用途有效地合成卤化联芳基原料。本发明的另一个实施方案是3' - （2'-卤代 - 联苯-4-基甲基）-1,7'-二甲基-2'-丙基-1H，3'H- [2， 5']联苯并咪唑基（TLMH），使用气态一氧化碳在含水的溶剂混合物中; 或甲酸盐任选地与乙酸一起在无水溶剂中。

4. 发明申请

WO2006050921A3 PREPARATION OF TELMISARTAN SALTS WITH IMPROVED SOLUBILITY 审中-公开
标题翻译：具有改善溶解性的电解质盐的制备
公开(公告)号：WO2006050921A3
公开(公告)日：2007-01-25
申请号：PCT/EP2005011980
申请日：2005-11-09
申请人： LEK PHARMACEUTICALS , ANTONCIC LJUBOMIR , COPAR ANTON
发明人： ANTONCIC LJUBOMIR , COPAR ANTON
IPC分类号： C07D235/20 , A61K31/4184 , 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 (I) 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（I）的新结晶钠盐。

5. 发明申请

WO2003101965A1 TWO CRYSTALLINE HYDRATE FORMS OF AMLODIPINE BENZENESULFONATE OF HIGH PURITY, PROCESSES FOR THEIR PREPARATION AND USE 审中-公开
标题翻译：高纯度亚油酸二苯酯的两水合液型，其制备和使用方法
公开(公告)号：WO2003101965A1
公开(公告)日：2003-12-11
申请号：PCT/EP2003/005632
申请日：2003-05-28
申请人： LEK PHARMACEUTICALS D.D. , HAM, Zoran , FURLAN, Borut , COPAR, Anton , URLEB, Uros
发明人： HAM, Zoran , FURLAN, Borut , COPAR, Anton , URLEB, Uros
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The novel crystalline amlodipine benzenesulfonate dihydrate of high purity is disclosed, as well as the process for preparation of the novel crystalline amlodipine benzenesulfonate dihydrate of high purity and the crystalline amlodipine benzenesulfonate monohydrate of high purity, suitable for the preparation of pharmaceutical formulations for the treatment of cardiac diseases or hypertension, and their use as intermediate compounds in the improved process of purification of the nonhydrate benzenesulfonate (besylate) salt of amlodipine.The process for preparation of the crystalline amlodipine benzenesulfonate dihydrate is carried in the way that from the C1-C5 alcoholic solution of amlodipine benzenesulfonate with water while stirring at a temperature of 20°C or lower the crystals of pure amlodipine benzenesulfonate dihydrate are separated, and isolated.The process for preparation of the crystalline amlodipine benzenesulfonate monohydrate is carried in the way that from the C1-C5 alcoholic solution of amlodipine benzenesulfonate with water while stirring at a temperature of 30°C or higher the crystals of pure amlodipine benzenesulfonate monohydrate are separated, and isolated.
摘要翻译：公开了高纯度的新型结晶氨氯地平苯磺酸盐二水合物，以及制备高纯度的新型结晶氨氯地平苯磺酸盐二水合物二水合物和高纯度结晶氨氯地平一水合物的方法，适用于制备用于治疗心脏病或高血压，以及它们作为中间体化合物用于改善氨氯地平的非水性苯磺酸盐（苯磺酸盐）盐的纯化方法。制备结晶氨氯地平苯磺酸盐二水合物的方法是以从C1-C5酒精在20℃或更低温度下搅拌的同时，分离苯磺酸氨氯地平与水的溶液，分离出纯氨基苯磺酸盐二水合物的晶体。分离出苯磺酸结晶氨氯地平一水合物的制备方法， C5 a 在30℃或更高的温度下搅拌的同时，将苯磺酸氨氯地平的醇溶液与水分离，分离出纯氨基苯磺酸一水合物的晶体。

6. 发明申请

WO2012062918A1 PROCESS FOR THE PREPARATION OF 3-AROYL-5-AMINOBENZOFURAN DERIVATIVES 审中-公开
标题翻译：制备3-氨基-5-氨基苯并呋喃衍生物的方法
公开(公告)号：WO2012062918A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069974
申请日：2011-11-11
申请人： LEK PHARMACEUTICALS D.D. , RICHTER, Frank , SCHREINER, Erwin , PIRC, Samo , COPAR, Anton
发明人： RICHTER, Frank , SCHREINER, Erwin , PIRC, Samo , COPAR, Anton
IPC分类号： C07D307/84
CPC分类号： C07D307/81 , A61K31/343 , C07D307/82 , C07D307/84
摘要： The present invention relates to a process for the preparation of 3-aroyl -5- aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
摘要翻译：本发明涉及一种制备可用作抗心律失常药物的3-芳酰基-5-氨基苯并呋喃衍生物的方法，其避免使用硝基中间体。

7. 发明申请

WO2005090359A3 SYNTHESIS OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL)-10H-THIENO[2, 3-B][1,5]BENZODIAZEPINE AND SALTS THEREOF 审中-公开
标题翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-B] [1,5]苯并咪唑及其盐的合成
公开(公告)号：WO2005090359A3
公开(公告)日：2007-04-26
申请号：PCT/EP2005002876
申请日：2005-03-17
申请人： LEK PHARMACEUTICALS , MESAR TOMAZ , COPAR ANTON , STURM HUBERT , LUDESCHER JOHANNES
发明人： MESAR TOMAZ , COPAR ANTON , STURM HUBERT , LUDESCHER JOHANNES
IPC分类号： C07D495/04 , A61K31/5513 , A61P25/00
CPC分类号： C07D495/04
摘要： The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.
摘要翻译：本发明属于有机化学领域，涉及一种用于纯化奥氮平的新方法，包括制备奥氮平的酸加成盐及其转化为药学上可接受的纯和变色的最终产物。本发明还涉及制备纯奥氮平的新方法。

8. 发明申请

WO2007017087A1 PROCESS FOR THE PREPARATION OF CRYSTALLINE PERINDOPRIL 审中-公开
标题翻译：制备结晶白蛋白的方法
公开(公告)号：WO2007017087A1
公开(公告)日：2007-02-15
申请号：PCT/EP2006/007258
申请日：2006-07-24
申请人： LEK PHARMACEUTICALS D.D. , JENKO, Branko , COPAR, Anton
发明人： JENKO, Branko , COPAR, Anton
IPC分类号： C07D209/42 , C07K1/00 , A61K31/404 , A61P9/00
CPC分类号： C07K5/06026 , C07D209/42
摘要： The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.
摘要翻译：本发明涉及一种制备结晶培哚普利的新方法。本发明还涉及培哚普利的新的烷基铵盐及其制备方法。

9. 发明申请

WO2006103068A1 A SYNTHESIS OF 4-BROMOMETHYL-2'-FORMYLBIPHENYL AND 4-BROMOMETHYL-2'- HYDROXYMETHYLBIPHENYL AND ITS USE IN PREPARATION OF ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译： 4-溴甲基-2'-甲酰苯胺和4-溴甲基-2'-羟基甲基苯乙烯的合成及其在血管紧张素II拮抗剂的制备中的应用
公开(公告)号：WO2006103068A1
公开(公告)日：2006-10-05
申请号：PCT/EP2006/002897
申请日：2006-03-30
申请人： LEK PHARMACEUTICALS D.D. , COPAR, Anton , ANTONCIC, Ljubomir , ANTONCIC, Matej
发明人： COPAR, Anton , ANTONCIC, Ljubomir , ANTONCIC, Matej
IPC分类号： C07D403/04 , C07D235/02 , C07D417/08
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，使用所选氢化物试剂。

10. 发明申请

WO2005090359A2 SYNTHESIS OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL)-10H-THIENO[2, 3-B][1,5]BENZODIAZEPINE AND SALTS THEREOF 审中-公开
标题翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-B] [1,5]苯并咪唑及其盐的合成
公开(公告)号：WO2005090359A2
公开(公告)日：2005-09-29
申请号：PCT/EP2005/002876
申请日：2005-03-17
申请人： LEK PHARMACEUTICALS D.D. , MESAR, Tomaz , COPAR, Anton , STURM, Hubert , LUDESCHER, Johannes
发明人： MESAR, Tomaz , COPAR, Anton , STURM, Hubert , LUDESCHER, Johannes
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.
摘要翻译：本发明属于有机化学领域，涉及一种用于纯化奥氮平的新方法，包括制备奥氮平的酸加成盐及其转化为药学上可接受的纯和变色的最终产物。本发明还涉及制备纯奥氮平的新方法。

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