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1. 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。

2. 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。

3. 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。

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. 发明授权

US07538213B2 Methods for preparation of olanzapine polymorphic form I 失效
标题翻译：奥氮平多形态I的制备方法
公开(公告)号：US07538213B2
公开(公告)日：2009-05-26
申请号：US10514520
申请日：2003-05-16
申请人： Janina Piechaczek , Magdalena Glice , Urszula Fraczek , Jadwiga Serafin , Wieslaw Szelejewski , Krzysztof Soltysiak
发明人： Janina Piechaczek , Magdalena Glice , Urszula Fraczek , Jadwiga Serafin , Wieslaw Szelejewski , Krzysztof Soltysiak
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.
摘要翻译：本发明涉及奥氮平多晶型I的制备方法。本发明还提供了新的奥氮平混合溶剂化物，它们是用于制备纯奥氮平多晶型I的有价值的中间体。

6. 发明申请

US20050239772A1 METHODS FOR PREPARATION OF OLANZAPINE POLYMORPHIC FORM I 失效
标题翻译：制备OLANZAPINE多聚体形式的方法I
公开(公告)号：US20050239772A1
公开(公告)日：2005-10-27
申请号：US10514520
申请日：2003-05-16
申请人： Janina Piechaczek , Magdalena Glice , Urszala Fraczek , Jadwiga Serafin , Wieslaw Szelejewski , Krzysztof Soltysiak
发明人： Janina Piechaczek , Magdalena Glice , Urszala Fraczek , Jadwiga Serafin , Wieslaw Szelejewski , Krzysztof Soltysiak
IPC分类号： C07D495/04 , A61K31/551 , C07D498/02
CPC分类号： C07D495/04
摘要： The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.
摘要翻译：本发明涉及奥氮平多晶型I的制备方法。本发明还提供新的奥氮平混合溶剂化物，它们是用于制备纯奥氮平多晶型物质I的有价值的中间体。

7. 发明授权

US07928063B2 Analogs of human growth hormone-releasing hormone, their preparation and use 有权
标题翻译：人类生长激素释放激素的类似物，其制备和用途
公开(公告)号：US07928063B2
公开(公告)日：2011-04-19
申请号：US10494218
申请日：2002-10-30
申请人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
发明人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
IPC分类号： A61K38/25
CPC分类号： C07K14/60 , A61K38/00 , Y02P20/55
摘要： Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab or Gap; R21 is hArg, Orn, Gab or Gap; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino groups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.
摘要翻译：具有下式的氨基酸序列的生长激素释放激素类似物：Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser -Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2（I），其中R11为hArg，Gab或Gap; R12是hArg，Orn，Gab或Gap; R20是hArg，hArg，Gab或Gap; R21是hArg，Orn，Gab或Gap; R29是D-Arg，hArg，Gab或Gap; 及其药学上可接受的盐。所述肽是GH释放的有效和选择性刺激物，并且它们对酶降解具有高度抗性。所述肽通过使用固相合成方法，通过在连接于聚合物载体的肽链的适当位置引入赖氨酸，2,4-二氨基丁酸或2,3-二氨基丙酸的合适衍生物，将侧链氨基脱保护并使游离氨基与胍基化剂反应，除去所有剩余的叔丁氧基羰基保护基团，并从载体上切割合成的肽，然后纯化并任选地将肽转化为药学上可接受的盐。

8. 发明授权

US07829746B2 Process for the preparation of calcipotriol 有权
标题翻译：卡泊三醇的制备方法
公开(公告)号：US07829746B2
公开(公告)日：2010-11-09
申请号：US12685256
申请日：2010-01-11
申请人： Andrzej Kutner , Michal Chodynski , Kinga Leszczynska , Wieslaw Szelejewski , Hanna Fitak
发明人： Andrzej Kutner , Michal Chodynski , Kinga Leszczynska , Wieslaw Szelejewski , Hanna Fitak
IPC分类号： C07C35/00
CPC分类号： C07C401/00 , C07C2601/02 , Y02P20/55
摘要： A process for the preparation of calcipotriol at least including: (a) reacting a C-22 phenylsulfonyl derivative of cholecalciferol of Formula 2, wherein R1 and R2 are the same or different and represent hydroxyl protecting groups, with a silyl derivative of alfa-hydroxy aldehyde of Formula 3, wherein R3 represents silyl group of formula Si(R4)(R5)(R6), where R4-R6 are the same or different and represent C1-6 alkyl or phenyl groups, in the presence of a strong organic base in an aprotic solvent, followed by reductive desulfonation of the obtained diastereomeric mixture of alfa-hydroxysulfones with sodium amalgam, removal of the hydroxyl protecting groups, and purification of the product. The process leads to the formation of calcipotriol containing less than 0.3% of the (22Z)-isomer. The obtained calcipotriol is free of mercury traces.
摘要翻译：一种制备卡泊三醇的方法，至少包括：（a）使式2的胆钙化甾醇的C-22苯基磺酰基衍生物与其中R 1和R 2相同或不同并代表羟基保护基，与α-羟基的甲硅烷基衍生物醛，其中R 3表示式Si（R 4）（R 5）（R 6）的甲硅烷基，其中R 4 -R 6相同或不同，表示C 1-6烷基或苯基，在强有机碱存在下在非质子溶剂中，然后将所得到的α-羟基磺酰胺与汞齐汞合物的非对映异构体混合物还原脱磺化，除去羟基保护基团并纯化产物。该方法导致含有小于0.3％的（22Z）异构体的卡泊三醇的形成。得到的卡泊三醇没有汞痕迹。

9. 发明授权

US4908464A Process for the production of 1,3,2-oxazaphosphorinanes 失效
标题翻译：生产1,3,2-oxazaphosphorinanes的方法
公开(公告)号：US4908464A
公开(公告)日：1990-03-13
申请号：US204582
申请日：1988-06-09
申请人： Wojciech J. Stec , Czeslaw Radzikowski , Wieslaw Szelejewski , Ryszard Kinas , Konrad Misiura , Grzegorz Grynkiewicz , Jacek Grodner , Halina Kusnierczyk , Andrzej Kutner , Slawomira Pilichowska
发明人： Wojciech J. Stec , Czeslaw Radzikowski , Wieslaw Szelejewski , Ryszard Kinas , Konrad Misiura , Grzegorz Grynkiewicz , Jacek Grodner , Halina Kusnierczyk , Andrzej Kutner , Slawomira Pilichowska
IPC分类号： C07F9/6584
CPC分类号： C07F9/65846
摘要： Process for production of derivatives of 1,3,2-oxazaphosphorinane of general formula 1, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atom or 2-halogenoalkyl group, and R.sub.1 and R.sub.2 are not at the same time hydrogen atoms, and X represents halogen atom is based, according to the invention, on the reduction of the respective 3-halogenoacyl derivatives of 1,3,2-oxazaphosphorinane of general formula 2, ##STR2## wherein the substituents have the above given meaning. The reduction is accomplished with the use of sodium borohydride in the presence of boron trifluoride etherate.Derivatives that are prepared by the procedure described here demonstrate antitumor activity.

10. 发明授权

US07897793B2 Process for preparation of 13,14-dihydro-PGF2 alpha derivatives 有权
标题翻译： 13,14-二氢-PGF2α衍生物的制备方法
公开(公告)号：US07897793B2
公开(公告)日：2011-03-01
申请号：US11874218
申请日：2007-10-18
申请人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wiśniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
发明人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wiśniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
IPC分类号： C07D307/93 , C07D493/00 , C07C69/74
CPC分类号： C07C309/73 , C07B2200/07 , C07C405/00 , C07C405/0016 , C07C405/0033 , C07C2601/08 , C07D303/04 , C07D307/935 , C07D317/12 , C07D317/26 , C07D327/10 , C07D493/08 , C07D493/18 , C07F7/1804
摘要： The invention relates to a process for the preparation of 13,14-dihydro-PGF2α derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2α, i.e., latanoprost.
摘要翻译：本发明涉及一种在通式（I）表示的碳15处制备R 1或R 2构型的13,14-二氢-PGF2α衍生物的方法，其中取代基的同一性在说明书中定义。式（I）的化合物在制备中是有价值的生物活性物质或中间体。本发明特别涉及制备13,14-二氢-15（R）-17-取代-18,19,20-三硝基-PGF2α（即拉坦前列素）的方法。

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