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1. 发明申请

US20080194819A1 Process For Preparation of Imatinib Base 失效
标题翻译：伊马替尼碱的制备方法
公开(公告)号：US20080194819A1
公开(公告)日：2008-08-14
申请号：US11813212
申请日：2005-12-30
申请人： Wojciech Szczepek , Wojciech Luniewski , Lukasz Kaczmarek , Bogdan Zagrodzki , Dorota Samson-Lazinska , Wieslaw Szelejewski , Maciej Skarzynski
发明人： Wojciech Szczepek , Wojciech Luniewski , Lukasz Kaczmarek , Bogdan Zagrodzki , Dorota Samson-Lazinska , Wieslaw Szelejewski , Maciej Skarzynski
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The invention provides an improved process for preparation of imatinib base and its pharmaceutically acceptable acid addition salts. The process allows for using simple starting materials, while simultaneously avoiding a laborious isolation and purification of intermediates and the final product, thereby facilitating scale-up.
摘要翻译：本发明提供了制备伊马替尼碱及其药学上可接受的酸加成盐的改进方法。该方法允许使用简单的起始原料，同时避免中间体和最终产物的费力分离和纯化，从而有助于放大。

2. 发明申请

US20070197545A1 Crystalline Polymorphs Of Methanesulfonic Acid Addition Salts Of Imatinib 失效
标题翻译：伊马替尼甲磺酸加成盐的晶体多晶型物
公开(公告)号：US20070197545A1
公开(公告)日：2007-08-23
申请号：US10599461
申请日：2005-04-02
申请人： Wojciech Szczepek , Dorota Samson-Lazinska , Bogdan Zagrodzki , Magdalena Glice , Wioleta Maruszak , Kataryzna Korczak , Ryszard Modzelewski , Marta Lawecka , Lukasz Kaczmarek , Wieslaw Szelejewski , Urszula Fraczek , Piotr Cmoch
发明人： Wojciech Szczepek , Dorota Samson-Lazinska , Bogdan Zagrodzki , Magdalena Glice , Wioleta Maruszak , Kataryzna Korczak , Ryszard Modzelewski , Marta Lawecka , Lukasz Kaczmarek , Wieslaw Szelejewski , Urszula Fraczek , Piotr Cmoch
IPC分类号： A61K31/506 , C07D403/14
CPC分类号： C07D401/04
摘要： This invention relates to the methanesulfonic acid addition salts of Imatinib and to the synthesis thereof. In particular, this invention relates to the synthesis of crystalline α-form of Imatinib methanesulfonate. Furthermore, the invention is directed to a novel acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-[(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]benzamide with two molecules of methanesulfonic acid and to the polymorphic forms thereof, as well as to their pharmaceutical compositions.
摘要翻译：本发明涉及伊马替尼的甲磺酸加成盐及其合成。特别地，本发明涉及甲磺酸伊马替尼的结晶α-形式的合成。此外，本发明涉及4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3 - [（4-吡啶-3-基）嘧啶-2-基氨基）苯基]苯甲酰胺与两分子甲磺酸及其多晶型物，以及它们的药物组合物。

3. 发明授权

US07732601B2 Crystalline polymorphs of methanesulfonic acid addition salts of Imatinib 失效
标题翻译：伊马替尼甲磺酸加成盐的结晶多晶型物
公开(公告)号：US07732601B2
公开(公告)日：2010-06-08
申请号：US10599461
申请日：2005-04-02
申请人： Wojciech Szczepek , Dorota Samson-Lazinska , Bogdan Zagrodzki , Magdalena Glice , Wioleta Maruszak , Katarzyna Korczak , Ryszard Modzelewski , Marta Lawecka , Lukasz Kaczmarek , Wieslaw Szelejewski , Urszula Fraczek , Piotr Cmoch
发明人： Wojciech Szczepek , Dorota Samson-Lazinska , Bogdan Zagrodzki , Magdalena Glice , Wioleta Maruszak , Katarzyna Korczak , Ryszard Modzelewski , Marta Lawecka , Lukasz Kaczmarek , Wieslaw Szelejewski , Urszula Fraczek , Piotr Cmoch
IPC分类号： C07D401/14 , C07D403/14 , A61P35/00
CPC分类号： C07D401/04
摘要： This invention relates to the methanesulfonic acid addition salts of Imatinib and to the synthesis thereof. In particular, this invention relates to the synthesis of crystalline α-form of Imatinib methanesulfonate. Furthermore, the invention is directed to a novel acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-[(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]benzamide with two molecules of methanesulfonic acid and to the polymorphic forms thereof, as well as to their pharmaceutical compositions.
摘要翻译：本发明涉及伊马替尼的甲磺酸加成盐及其合成。特别地，本发明涉及甲磺酸伊马替尼的结晶α型的合成。此外，本发明涉及4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3 - [（4-吡啶-3-基）嘧啶-2-基氨基）苯基]苯甲酰胺与两分子甲磺酸及其多晶型物，以及它们的药物组合物。

4. 发明授权

US07674901B2 Process for preparation of imatinib base 失效
标题翻译：伊马替尼碱的制备方法
公开(公告)号：US07674901B2
公开(公告)日：2010-03-09
申请号：US11813212
申请日：2005-12-30
申请人： Wojciech Szczepek , Wojciech Luniewski , Lukasz Kaczmarek , Bogdan Zagrodzki , Dorota Samson-Lazinska , Wieslaw Szelejewski , Maciej Skarzynski
发明人： Wojciech Szczepek , Wojciech Luniewski , Lukasz Kaczmarek , Bogdan Zagrodzki , Dorota Samson-Lazinska , Wieslaw Szelejewski , Maciej Skarzynski
IPC分类号： C07D419/00
CPC分类号： C07D401/04
摘要： An improved process for the preparation of imatinib base and its pharmaceutically acceptable acid addition salts by (a) reacting 2-methyl-5-nitroaniline with cyanamide in the presence of hydrochloric acid to obtain 1-(2-methyl-5-nitrophenyl)guanidine hydrochloride; (b) converting 1-(2-methyl-5-nitrophenyl)guanidine hydrochloride to 1-(2-methyl-5-nitrophenyl)guanidine nitrate; (c) condensing 3-acetylpyridine with N,N-dimethylformamide dimethyl acetal to obtain 3-(dimethylamino)-1-(3-pyridinyl)-prop-2-en-1-one; (d) reacting 3-(dimethylamino)-1-(3-pyridinyl)-prop-2-en-1-one with 1-(2-methyl-5-nitrophenyl)guanidine nitrate to obtain N-(5-nitro-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine; (e) reducing N-(5-nitro-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine using hydrazine in the presence of Raney nickel to obtain N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidine-amine; (f) condensing N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidine-amine with 4-chloromethylbenzoyl chloride in the presence of an inorganic base to obtain 4-(chloromethyl)-N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide; and (g) condensing 4-(chloromethyl)-N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide with an excess of N-methylpiperazine to obtain imatinib base; and adding water or a mixture of water and an organic solvent; and isolating said imatinib base. The process allows for using simple starting materials, while simultaneously avoiding a laborious isolation and purification of intermediates and the final product, thereby facilitating scale-up.
摘要翻译：（a）在盐酸存在下使2-甲基-5-硝基苯胺与氨基氰反应，制备伊马替尼碱及其药学上可接受的酸加成盐的改进方法，得到1-（2-甲基-5-硝基苯基）胍盐酸盐（b）将1-（2-甲基-5-硝基苯基）胍盐酸盐转化为1-（2-甲基-5-硝基苯基）硝酸胍; （c）将3-乙酰基吡啶与N，N-二甲基甲酰胺二甲基缩醛缩合，得到3-（二甲基氨基）-1-（3-吡啶基） - 丙-2-烯-1-酮; （d）使3-（二甲基氨基）-1-（3-吡啶基） - 丙-2-烯-1-酮与1-（2-甲基-5-硝基苯基）硝酸胍反应，得到N-（5-硝基 - -2-甲基苯基）-4-（3-吡啶基）-2-嘧啶胺; （e）在阮内镍存在下使用肼还原N-（5-硝基-2-甲基苯基）-4-（3-吡啶基）-2-嘧啶胺，得到N-（5-氨基-2-甲基苯基）-4 - （3-吡啶基）-2-嘧啶 - 胺; （f）在无机碱存在下，使N-（5-氨基-2-甲基苯基）-4-（3-吡啶基）-2-嘧啶胺与4-氯甲基苯甲酰氯缩合，得到4-（氯甲基）-N - （4-甲基-3-（4-（吡啶-3-基）嘧啶-2-基氨基）苯基）苯甲酰胺; 和（g）将4-（氯甲基）-N-（4-甲基-3-（4-（吡啶-3-基）嘧啶-2-基氨基）苯基）苯甲酰胺与过量的N-甲基哌嗪缩合得到伊马替尼碱 ; 并加入水或水和有机溶剂的混合物; 并分离所述伊马替尼碱基。该方法允许使用简单的起始原料，同时避免中间体和最终产物的费力分离和纯化，从而有助于放大。

5. 发明专利

IL178097D0 POLYMORPHS OF ACID ADDITION SALTS OF IAMATINIB WITH METHANESULFONIC ACID 未知
公开(公告)号：IL178097D0
公开(公告)日：2006-12-31
申请号：IL17809706
申请日：2006-09-14
申请人： INST FARMACEUTYCZNY , WOJCIECH SZCZEPEK , DOROTA SAMSON LAZINSKA , BOGDAN ZAGRODZKI , MAGDALENA GLICE , WIOLETA MARUSZAK , KATARYZNA KORCZAK , RYSZARD MODZELEWSKI , MARTA LAWECKA , LUKASZ KACZMAREK , WIESLAW SZELEJEWSKI , URSZULA FRACZEK , PIOTR CMOCH
IPC分类号： C07D20100101 , C07D401/04
摘要： This invention relates to the methanesulfonic acid addition salts of Imatinib and to the synthesis thereof. In particular, this invention relates to the synthesis of crystalline α-form of Imatinib methanesulfonate. Furthermore, the invention is directed to a novel acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-[(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]benzamide with two molecules of methanesulfonic acid and to the polymorphic forms thereof, as well as to their pharmaceutical compositions.

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