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1. 发明申请

WO2005121084A1 A METHOD OF PREPARATION OF RAMIPRIL 审中-公开
标题翻译：一种制备RAMIPRIL的方法
公开(公告)号：WO2005121084A1
公开(公告)日：2005-12-22
申请号：PCT/CZ2005/000048
申请日：2005-06-08
申请人： ZENTIVA, a. s. , STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
发明人： STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： A method of preparation of ramipril of formula (I), during which the benzyl ester hydrochloride of formula (III) is converted to the benzyl ester of formula (II), which in turn affords, by reaction with the carboxyanhydride of formula (V), the benzyl ester of ramipril of formula (IV), which is subsequently converted to ramipril of formula (I).
摘要翻译：制备式（I）的雷米普利的方法，其中式（III）的苄酯盐酸盐转化成式（II）的苄基酯，其又通过与式（V）的羧酸酐反应，，式（IV）的雷米普里的苄基酯，其随后转化成式（I）的雷米普利。

2. 发明申请

WO2005068471A1 NEW CRYSTALLINE FORMS OF CLOPIDOGREL HYDROBROMIDE AND METHODS OF THEIR PREPARATION 审中-公开
标题翻译：氯碳酸氢盐的新型结晶形式及其制备方法
公开(公告)号：WO2005068471A1
公开(公告)日：2005-07-28
申请号：PCT/CZ2004/000089
申请日：2004-12-21
申请人： ZENTIVA, A.S. , HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
发明人： HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention concerns clopidogrel hydrobromide in the crystalline Form I characterized by an X-ray diffraction pattern with characteristic interplanar distances d of 4.01; 4.39 and 3.17 ú and which is further characterized by bands in the infrared spectra at 1743; 1421; 1237, 760 and 728 cm -1 . Clopidogrel hydrobromide in the crystalline Form II is characterized by an Xray diffraction pattern with characteristic interplanar distances d of 4.52; 3.83; 3.48 ú, as well as bands in the infrared spectra at 1754; 1436; 1317 and 1223 cm -1 . Crystalline form III is characterized by the following peaks ascertained by X-ray diffraction at 20 positions: 7.796 °; 15.380 °; 18.389 °; 19.369 ° and 23.895 °. The method of preparation of clopidogrel hydrobromide in the crystalline Form I consist in precipitating the clopidogrel base dissolved in toluene with a concentrated solution of hydrobromic acid. The method of preparation of clopidogrel hydrobromide in the crystalline Form II consist in dissolving the clopidogrel base in an organic solvent and precipitating it with a solution of hydrobromic acid in toluene or with gaseous hydrogen bromide. Form III can be used for the preparation of pharmaceutically applicable Form II.
摘要翻译：本发明涉及结晶形式I中的氯吡格雷氢溴酸盐，其特征在于具有4.01的特征性面间距离d的X射线衍射图谱; 4.39和3.17ú，其进一步特征在于1743年红外光谱中的谱带; 1421; 结晶形式II中的氯吡格雷氢溴酸盐的特征在于具有4.52的特征性面间距d的X射线衍射图; 3.83; 3.48ú，以及1754年的红外光谱带; 1436; 1317和1223厘米-1。结晶形式III的特征在于在20个位置通过X射线衍射确定的以下峰：7.796°; 15.380°; 18.389°; 19.369°和23.895°。结晶形式I中氯吡格雷氢溴酸盐的制备方法是用氢溴酸浓溶液沉淀溶解在甲苯中的氯吡格雷碱。在晶型II中制备氯吡格雷氢溴酸盐的方法包括将氯吡格雷碱溶解在有机溶剂中，并用氢溴酸在甲苯或与溴化氢气体的溶液中沉淀。 III型可用于制备药学上适用的II型。

3. 发明申请

WO2006042481A1 METHOD OF OBTAINING CLOPIDOGREL 审中-公开
标题翻译：获得胶质的方法
公开(公告)号：WO2006042481A1
公开(公告)日：2006-04-27
申请号：PCT/CZ2005/000077
申请日：2005-10-17
申请人： ZENTIVA A.S. , HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
发明人： HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Separation of the camphorsulfonic salts of the compounds of formula (I) and (II) by one or more crystallizations from a mixture of two solvents, both R(-)-10-camphorsulfonic acid and its salts with the compounds of formula (I) and (II) being well soluble in at least one of the components, the formula of which can be indicated as R a OH, wherein R a is a straight or branched C 1 to C 5 alkyl. In the other components, camphorsulfonic acid and its salts are less soluble; however, they dissolve compounds of formula (I) and (II) very well.
摘要翻译：通过一种或多种结晶从R（ - ） - 10-樟脑磺酸及其与式（I）化合物的盐的两种溶剂的混合物中分离式（I）和（II）化合物的樟脑磺酸盐，和（II）可溶于至少一种组分，其配方可以表示为R 1

4. 发明申请

WO2005105726A1 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型化合物，其制备和使用
公开(公告)号：WO2005105726A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/052014
申请日：2005-05-03
申请人： NOVO NORDISK A/S , HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid , PIHERA, Pavel , EBDRUP, Søren
发明人： HAVRANEK, Miroslav , SAUERBERG, Per , PETTERSSON, Ingrid , PIHERA, Pavel , EBDRUP, Søren
IPC分类号： C07C59/70
CPC分类号： C07C323/20 , C07C2602/08 , C07D207/333 , C07D213/30 , C07D213/70
摘要： Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hypertriglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
摘要翻译：通式（I）的新型化合物，其中变量如权利要求1所定义，这些化合物用作药物组合物，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARδ亚型，即1型糖尿病，2型糖尿病，血脂异常，综合征X（包括代谢综合征即葡萄糖耐量异常，胰岛素抵抗，高甘油三酯血症和/或肥胖），心血管疾病（包括动脉粥样硬化）和高胆固醇血症。

5. 发明申请

WO2007071766A2 NOVEL COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型化合物，其制备和使用
公开(公告)号：WO2007071766A2
公开(公告)日：2007-06-28
申请号：PCT/EP2006/070096
申请日：2006-12-21
申请人： NOVO NORDISK A/S , SAUERBERG, Per , PIHERA, Pavel , POLIVKA, Zdenék , HAVRANEK, Miroslav , PETTERSSON, Ingrid , MOGENSEN, John, Patrick
发明人： SAUERBERG, Per , PIHERA, Pavel , POLIVKA, Zdenék , HAVRANEK, Miroslav , PETTERSSON, Ingrid , MOGENSEN, John, Patrick
IPC分类号： C07C323/16 , A61K31/44 , A61P3/10 , C07D213/30 , C07D211/46 , C07D333/54 , C07D333/16 , C07D231/12 , C07D307/79 , C07C59/68 , C07D295/08
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as phar- maceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译：通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。本发明化合物是PPARd的活化剂，应用于治疗由其介导的病症。

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