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11. 发明申请

WO2004066997A3 PREPARATION OF NEW PHARMACEUTICALLY SUITABLE SALT OF LOSARTAN AND FORMS THEREOF WITH NEW PURIFICATION AND ISOLATION METHODS 审中-公开
标题翻译：用新的纯化和分离方法制备新药物洛索坦的盐及其形式
公开(公告)号：WO2004066997A3
公开(公告)日：2004-11-11
申请号：PCT/SI2004000001
申请日：2004-01-29
申请人： LEK PHARMACEUTICALS , ANTONCIC LJUBOMIR , COPAR ANTON , SVETE PETER , HUSU-KOVACECIC BREDA , HAM ZORAN , MAROLT BORIS
发明人： ANTONCIC LJUBOMIR , COPAR ANTON , SVETE PETER , HUSU-KOVACECIC BREDA , HAM ZORAN , MAROLT BORIS
IPC分类号： A61P9/12 , C07D403/10 , A61K31/4178
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-h idroxymethyl-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-4-chloro-5hidroxymethyl-1-[[2'-(1 H-tetrazole-5-yl)[1.1'-biphenyl]-4-yl]-1 H-imidazole have been prepared.
摘要翻译： 2-正丁基-4-氯-5H-异丙基甲基-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，纯化和分离方法。含有2-正丁基-4-氯-5-甲基甲基-1 - [[2' - （1H-四唑-5-基）[1.1'-联苯] -4-基] -1H-咪唑已经制备。

12. 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。

13. 发明申请

WO2009115584A3 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译： 2'-卤代苯基-4-炔丙基中间体合成血管紧张素Ⅱ拮抗剂
公开(公告)号：WO2009115584A3
公开(公告)日：2009-11-12
申请号：PCT/EP2009053267
申请日：2009-03-19
申请人： LEK PHARMACEUTICALS , 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：描述了获得2'-卤代-4-甲基联苯的方法，该方法包括使4卤代甲苯与1,2-二卤代苯在单质金属如镁，锂或锌存在下反应，其中0至0.9摩尔，特别是0至0摩尔在1,2-二卤代苯中使用0.2摩尔过量的4-卤代甲苯，产生的有机金属中间体被元素卤素猝灭。此外，产生的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）苯并咪唑的偶联得到3' - （2'- 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，其可以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也描述了与甲酸衍生物如N，N-二甲基甲酰胺，烷基甲酸酯或二氧化碳反应以获得替米沙坦。进一步描述了用于监测上述反应的在线分析法，用于制备药物组合物的过程和/或用于制备药物的剂量或用于制备药物的用途。

14. 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。

15. 发明申请

WO2006050921A2 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：WO2006050921A2
公开(公告)日：2006-05-18
申请号：PCT/EP2005/011980
申请日：2005-11-09
申请人： LEK PHARMACEUTICALS D.D. , 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 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。

16. 发明申请

WO2006048237A1 NOVEL POLYMORPH FORMS OF CANDESARTAN CILEXETIL 审中-公开
标题翻译： CANDESARTAN CILEXETIL的新型POLYMORPH形式
公开(公告)号：WO2006048237A1
公开(公告)日：2006-05-11
申请号：PCT/EP2005/011689
申请日：2005-11-02
申请人： LEK PHARMACEUTICALS D.D. , ANTONCIC, Ljubomir , COPAR, Anton , JERIHA, Alenka
发明人： ANTONCIC, Ljubomir , COPAR, Anton , JERIHA, Alenka
IPC分类号： C07D403/10 , A61K31/4184
CPC分类号： C07D403/10
摘要： New crystalline forms of candesartan cilexetil is prepared from the solution in a chlorinated solvent by addition of an alkane while new amorphous is prepared from above solution by precipitating by addition of cycloalkane. The form depends on the concentration of a solute in a chlorinated solvent.
摘要翻译：通过加入烷烃由氯化溶剂中的溶液制备新的结晶形式，同时通过加入环烷烃沉淀从上述溶液制备新的无定形物。形式取决于溶剂在氯化溶剂中的浓度。

17. 发明申请

WO2005063702A1 PREPARATION OF R-5-(2-(2-ETHOXYPHENOXYETYLAMINO)PROPYL)-2- METHOXYBENZENESULPHONAMIDE HYDROCHLORIDE OF HIGH CHEMICAL 审中-公开
标题翻译： -2-羟基苯甲酰胺氢氯化物的制备R-5-（2-（2-乙氧基甲酰氨基）丙基）-2-甲氧基苯磺酰氯
公开(公告)号：WO2005063702A1
公开(公告)日：2005-07-14
申请号：PCT/SI2004/000047
申请日：2004-12-27
申请人： LEK PHARMACEUTICALS D.D. , FURLAN, Borut , COPAR, Anton
发明人： FURLAN, Borut , COPAR, Anton
IPC分类号： C07C303/40
CPC分类号： C07C311/37 , C07C303/40 , C07C303/44
摘要： In the present invention, the process for the preparation of tamsulosin hydrochloride and subsequent purification with thermal crystallisation to provide essentially pure tamsulosin hydrochloride is disclosed.
摘要翻译：在本发明中，公开了制备盐酸坦洛新并随后用热结晶纯化以提供基本上纯的坦索罗辛盐酸盐的方法。

18. 发明申请

WO2004066997A2 PREPARATION OF NEW PHARMACEUTICALLY SUITABLE SALT OF LOSARTAN AND FORMS THEREOF WITH NEW PURIFICATION AND ISOLATION METHODS 审中-公开
标题翻译：利用新的纯化和分离方法制备新型药物合成盐的洛沙坦及其形态
公开(公告)号：WO2004066997A2
公开(公告)日：2004-08-12
申请号：PCT/SI2004/000001
申请日：2004-01-29
申请人： LEK PHARMACEUTICALS D.D. , ANTONCIC, Ljubomir , COPAR, Anton , SVETE, Peter , HUSU-KOVACECIC, Breda , HAM, Zoran , MAROLT, Boris
发明人： ANTONCIC, Ljubomir , COPAR, Anton , SVETE, Peter , HUSU-KOVACECIC, Breda , HAM, Zoran , MAROLT, Boris
IPC分类号： A61K31/4178
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-h idroxymethyl-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-4-chloro-5hidroxymethyl-1-[[2'-(1 H-tetrazole-5-yl)[1.1'-biphenyl]-4-yl]-1 H-imidazole have been prepared.
摘要翻译： 2-正丁基-4-氯-5-羟甲基-1 - [[2' - （1H-四唑-5-基）甲基] - 氨基甲酸酯的药学上合适的晶体和无定形碱金属盐和碱土金属盐，已经制备了[1,1'-联苯] -4-基] -1H-苯并咪唑，并且已经描述了用于所述高纯度盐的新制造，纯化和分离方法。含有新的2-正丁基-4-氯-5,5-间苯二甲酸钾结晶钾盐的稳定的药物组合物;羟甲基-1 - [[2' - （1H-四唑-5-基）[1,1'-联苯] -4-基 ] -1H-咪唑已被制备。

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