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1. 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。

2. 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。

3. 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。

4. 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。

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

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。

8. 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。

9. 发明申请

WO2010112482A1 A PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS 审中-公开
标题翻译：活性甲基团的二甲基化方法
公开(公告)号：WO2010112482A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/054151
申请日：2010-03-30
申请人： LEK PHARMACEUTICALS D.D. , JENKO, Branko , COPAR, Anton
发明人： JENKO, Branko , COPAR, Anton
IPC分类号： C07C231/12 , C07C253/30 , C07C255/19 , C07C237/06 , A61K31/275 , A61K31/16
CPC分类号： C07C253/30 , C07C231/12 , C07C237/06 , C07C255/19
摘要： The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses aprocess for preparing3-amino-2,2- dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processesfor preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.
摘要翻译：本发明公开了一种活性亚甲基二甲基化方法。具体地说，本发明公开了3-氨基-2,2-二甲基丙酰胺的制备方法。通过本发明的二甲基化方法制备的化合物如3-氨基-2,2-二甲基丙酰胺可用作合成治疗，预防或诊断剂例如阿利吉仑或隐霉素的途径中的中间体。特别地，本发明涉及进一步延伸至制备包含所述治疗性预防或诊断剂的药物剂型的方法的实施方案。更具体地，本发明涉及通过本发明的二甲基化方法制备的化合物在制备治疗，预防或诊断剂中的用途，或用于制备包含所述治疗，预防或诊断剂的药物剂型。根据本发明的方法可有利地用于合成各种活性药物成分，例如阿利吉仑或crypthophycin。

10. 发明申请

WO2009115584A2 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译： 2-HALOBIPHENYL-4-YL中间体合成ANGIOTENSIN II拮抗剂
公开(公告)号：WO2009115584A2
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053267
申请日：2009-03-19
申请人： LEK PHARMACEUTICALS D.D. , COPAR, Anton , CASAR, Zdenko , PREMRL, Andrej
发明人： COPAR, Anton , CASAR, Zdenko , PREMRL, Andrej
IPC分类号： C07C17/26 , C07C25/18 , C07D235/18
CPC分类号： C07C17/263 , C07C17/14 , C07C17/2632 , C07D235/20 , Y10T436/147777 , C07C25/18
摘要： A process for obtaining 2'-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental halogen. In addition, the coupling of arised 2'-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1'-methylbenzimidazole-2-il)benzimidazole to afford 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament.
摘要翻译：描述了一种获得2'-卤代-4-甲基联苯的方法，其包括在元素金属如镁，锂或锌的存在下使4-卤代甲苯与1,2-二卤代苯反应，其中0至0.9摩尔，特别是0至使用0.2摩尔过量的4-卤代甲苯相对于1,2-二卤代苯，并且芳族有机金属中间体被元素卤素淬灭。另外，将2'-卤代-4-甲基联苯与2-（1-丙基）-4-甲基-6-（1'-甲基苯并咪唑-2-基）苯并咪唑的偶合得到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，其可进一步转化为有机金属化合物，并且所述有机金属化合物进一步反应与甲酸衍生物如N，N-二甲基甲酰胺，烷基甲酸酯或二氧化碳反应得到替米沙坦。进一步描述了在线分析用于监测上述反应的用途，制备药物组合物的方法和/或用于制备药物的剂量。

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