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1. 发明申请

WO2011049474A1 SALTS OF IMATINIB WITH TARTARIC ACIDS 审中-公开
标题翻译：。OF。。。。。。。。
公开(公告)号：WO2011049474A1
公开(公告)日：2011-04-28
申请号：PCT/PL2010/000105
申请日：2010-10-21
申请人： KOZLUK, Tomasz , WOŹNIAK, Robert
发明人： KOZLUK, Tomasz , WOŹNIAK, Robert
IPC分类号： C07D401/04 , A61K31/506 , A61P35/00
CPC分类号： C07D401/04
摘要： New imatinib acid addition salts are represented by general formula (I), wherein R represents O-acyl group of L- or D-tartaric acid, n represents any number in the range from 1 to 2, and their solvates and hydrates. Salts are preferably selected from a group comprising imatinib salts of dibenzoyl-L-tartaric, dibenzoyl-D- tartaric, di-p-anizoyl-L-tartaric, di-p-anizoyl-D-tartaric, di-p-tolyl-L- tartaric, dipivaloyl-L-tartaric or diacetyl-L-tartaric acids, which may be used in the treatment and/ or prevention of diseases mediated by tyrosine kinases.
摘要翻译：新的伊马替尼加成盐由通式（I）表示，其中R表示L-或D-酒石酸的O-酰基，n表示1至2的任何数字，以及它们的溶剂合物和水合物。盐优选选自二苯甲酰基-L-酒石酸，二苯甲酰基-D-酒石酸，二对茴香酰-L-酒石酸，二对茴香酰-D-酒石酸，二对甲苯基-L - 酒石酸，二新戊酰-L-酒石酸或二乙酰基-L-酒石酸，其可用于治疗和/或预防由酪氨酸激酶介导的疾病。

2. 发明申请

WO2009148341A1 PROCESS FOR PREPARATION OF TADALAFIL 审中-公开
标题翻译：制备方法
公开(公告)号：WO2009148341A1
公开(公告)日：2009-12-10
申请号：PCT/PL2009/000060
申请日：2009-06-03
申请人： ZAKLADY FARMACEUTYCZNE POLPHARMA SA , KACZMAREK, Lukasz , PYC, Pawel , BADOWSKA-ROSLONEK, Katarzyna
发明人： KACZMAREK, Lukasz , PYC, Pawel , BADOWSKA-ROSLONEK, Katarzyna
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： Process for the preparation of tadalafil of high pharmaceutical purity is characterized in that the sequence of reactions comprising acetylation of methyl (1 R ,3 R )-1-(1,3-benzodioxol-5-yl)-2,3,4,9- tetrahydro- 1H-pyrido[3,4-b]indole-3-carboxylate with acetyl chloride and cyclisation of the formed intermediate with methyl amine, is performed as a 'one-pot' process, without isolating the intermediate methyl (1 R ,3 R )-1-(1,3-benzodioxol-5-yl)-2-(chloroacetyl)-2,3,4,9- tetrahydro- 1H-pyrido[3,4-b]indole-3-carboxylate.
摘要翻译：用于制备高药物纯度的他达拉非的方法的特征在于包含（1R，3R）-1-（1,3-苯并间二氧杂环戊烯-5-基）-2,3,4,9- 四氢-1H-吡啶并[3,4-b]吲哚-3-羧酸乙酯与乙酰氯反应，并将形成的中间体与甲胺环化，进行“一锅”方法，而不分离中间体（1R，3R ）-1-（1,3-苯并间二氧杂环戊烯-5-基）-2-（氯乙酰基）-2,3,4,9-四氢-1H-吡啶并[3,4-b]吲哚-3-羧酸乙酯。

3. 发明申请

WO2006016829A1 CONTROLLED-RELEASE FORMULATION COMPRISING TAMSULOSIN HYDROCHLORIDE 审中-公开
标题翻译：包含TAMSULOSIN HYDROCHLORIDE的控制释放配方
公开(公告)号：WO2006016829A1
公开(公告)日：2006-02-16
申请号：PCT/PL2005/000052
申请日：2005-08-12
申请人： INSTYTUT FARMACEUTYCZNY , WIACKOWSKI, Lech , SZELEJEWSKI, Wieslaw , ZAREMBA, Andrzej , PESTA-DYNDA, Edyta , MARCHLEWSKA-CELA, Zofia
发明人： WIACKOWSKI, Lech , SZELEJEWSKI, Wieslaw , ZAREMBA, Andrzej , PESTA-DYNDA, Edyta , MARCHLEWSKA-CELA, Zofia
IPC分类号： A61K9/00
CPC分类号： A61K9/2027 , A61K9/2013 , A61K9/2846 , A61K31/18
摘要： A solid oral controlled-release formulation of tamsulosin hydrochloride in the form of an enteric coated tablet, wherein tamsulosin hydrochloride is ho-mogenously dispersed within a matrix consisting of a mixture of fatty component and hydrophilic component, together with at least one diluent and optionally other pharmaceutically acceptable excipients, exhibiting ex- hibiting a dissolution profile of tamsulosin hydrochloride, as measured in a Type II paddle apparatus in accordance with the dissolution testing method specified in the European Pharmacopoeia at 37±0.5°C and 100 rpm in a 0.1 N HC1 buffer for 2 hours, followed by pH 7.2 buffer for the rest of test: 10-40% during first 2 hours (in HC1), 35-70% after 3 h (in pH 7.2 buffer system), not less than 70% of the declared content after 5 h (in pH 7.2 buffer system).
摘要翻译：一种肠溶包衣片形式的盐酸坦索罗辛的固体口服缓释制剂，其中盐酸坦索罗辛与由至少一种稀释剂和任选的其它稀释剂组成的基质中共同分散在由脂肪组分和亲水组分的混合物组成的基质内药学上可接受的赋形剂，显示了在II型桨式装置中按照欧洲药典在37±0.5℃和100rpm下在0.1N HCl缓冲液中规定的溶出试验方法测量的盐酸坦洛新的溶出曲线， 2小时，其次为pH7.2缓冲液，第2小时（HC1）为10-40％，3小时后为35-70％（pH 7.2缓冲液），不少于70％ 5 h后声称含量（pH 7.2缓冲系统）。

4. 发明申请

WO2005095379A2 CRYSTALLINE METHANESULFONIC ACID ADDITION SALTS OF IMATINIB 审中-公开
标题翻译： IMATINIB的结晶甲磺酸添加剂
公开(公告)号：WO2005095379A2
公开(公告)日：2005-10-13
申请号：PCT/PL2005/000024
申请日：2005-04-02
申请人： INSTYTUT FARMACEUTYCZNY , SZCZEPEK, Wojciech , SAMSON-LAZINSKA, Dorota , ZAGRODZKI, Bogdan , GLICE, Magdalena , MARUSZAK, Wioleta , KORCZAK, Kataryzna , MODZELEWSKI, Ryszard , LAWECKA, Marta , KACZMAREK, Lukasz , SZELEJEWSKI, Wieslaw , FRACZEK, Urszula , CMOCH, Piotr
发明人： SZCZEPEK, Wojciech , SAMSON-LAZINSKA, Dorota , ZAGRODZKI, Bogdan , GLICE, Magdalena , MARUSZAK, Wioleta , KORCZAK, Kataryzna , MODZELEWSKI, Ryszard , LAWECKA, Marta , KACZMAREK, Lukasz , SZELEJEWSKI, Wieslaw , FRACZEK, Urszula , CMOCH, Piotr
IPC分类号： C07D401/00
CPC分类号： C07D401/04
摘要： The invention relates to the methanesulfonic acid addition salts of Imatinib and to the processes for their preparation. In particular, the invention relates to the process for the preparation of Imatinib methanesulfonate a-crystal form. 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 the polymorphic forms thereof as well as 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制备方法。特别地，本发明涉及制备甲磺酸伊马替尼α-晶型的方法。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及其药物组合物。

5. 发明申请

WO2008054233A2 PROCESS FOR THE PREPARATION OF DOCETAXEL 审中-公开
标题翻译：制备DOCETAXEL的方法
公开(公告)号：WO2008054233A2
公开(公告)日：2008-05-08
申请号：PCT/PL2007/000073
申请日：2007-10-31
申请人： INSTYTUT FARMACEUTYCZNY , ACHMATOWICZ, Osman , BANKOWSKI, Krzysztof , SZELEJEWSKI, Wieslaw , MICHALAK, Olga , SZECHNER, Barbara
发明人： ACHMATOWICZ, Osman , BANKOWSKI, Krzysztof , SZELEJEWSKI, Wieslaw , MICHALAK, Olga , SZECHNER, Barbara
CPC分类号： C07D305/14 , C07C271/22 , C07D263/06 , C07D413/12
摘要： The process for preparation of docetaxel consists in that the hydroxy! groups at C-7 and C-10 position of 10- deacetolobaccatin III and amino group of (4S,5R)-2- methoxephenyl-4-phenyl-l,3-oxazolidine-5-carboxylic acid are simultaneously protected with allyloxycarbonyl to give 7,10- diallyloxycarbonyl-10-deacetylbaccatin III (VI) and (4S,5R)-N- allyloxycarbonyl-2-(4-metoxyphenyl)-4-phenyloxazolidine-5- carboxylic acid (IV), respectively, said groups after esterification are removed upon one technological operation, whereas the synthesis is finalized by the introduction of tert-butyloxycarbonyl group onto amino group of (2R,3S)-3-phenylisoserine.
摘要翻译：多西紫杉醇的制备方法在于羟基！ 10-脱乙酰壳多糖III的C-7和C-10位的基团和（4S，5R）-2-甲氧基苯基-4-苯基-1,3-恶唑烷-5-羧酸的氨基同时用烯丙氧基羰基保护，得到 7,10-二烯丙氧基羰基-10-脱乙酰基浆果赤霉素III（VI）和（4S，5R）-N-烯丙氧基羰基-2-（4-甲氧基苯基）-4-苯基恶唑烷-5-羧酸（IV）在一个技术操作中被除去，而通过在（2R，3S）-3-苯基异丝氨酸的氨基上引入叔丁氧基羰基来最终确定合成。

6. 发明申请

WO2006043846A1 SALT OF MONTELUKAST WITH TERT.-BUTYLAMINE 审中-公开
标题翻译：含叔丁基胺的蒙特利特盐
公开(公告)号：WO2006043846A1
公开(公告)日：2006-04-27
申请号：PCT/PL2005/000067
申请日：2005-10-21
申请人： INSTYTUT FARMACEUTYCZNY , Zaklady Farmaceutyczne POLPHARMA SA , ACHMATOWICZ, Osman , WISNIEWSKI, Krzysztof , RAMZA, Jan , SZELEJEWSKI, Wieslaw , SZECHNER, Barbara
发明人： ACHMATOWICZ, Osman , WISNIEWSKI, Krzysztof , RAMZA, Jan , SZELEJEWSKI, Wieslaw , SZECHNER, Barbara
IPC分类号： C07D215/18 , A61K31/4704 , A61P11/06
CPC分类号： C07D215/18
摘要： The invention relates to a novel salt of montelukast with tert-butylamine and its use in the process for the preparation of highly pure free montelukast acid and/or pharmaceutically acceptable salts thereof, in particular montelukast sodium.
摘要翻译：本发明涉及具有叔丁胺的孟鲁司特的新盐及其在制备高纯度游离孟鲁司特酸和/或其药学上可接受的盐，特别是孟鲁司特钠的方法中的用途。 / p>

7. 发明申请

WO2003037928A2 NEW PEPTIDES - ANALOGS OF HUMAN GROWTH HORMONE-RELEASING HORMONE 审中-公开
标题翻译：新肽 - 人类生长激素释放激素的模拟
公开(公告)号：WO2003037928A2
公开(公告)日：2003-05-08
申请号：PCT/PL2002/000080
申请日：2002-10-30
申请人： INSTYTUT FARMACEUTYCZNY , IZDEBSKI, Jan , KUNCE, Danuta , ORLOWSKA, Alicja , WITKOWSKA, Ewa , SZELEJEWSKI, Wieslaw , KUTNER, Andrzej , BANKOWSKI, Krzysztof , FRACKIEWICZ, Elzbieta
发明人： IZDEBSKI, Jan , KUNCE, Danuta , ORLOWSKA, Alicja , WITKOWSKA, Ewa , SZELEJEWSKI, Wieslaw , KUTNER, Andrzej , BANKOWSKI, Krzysztof , FRACKIEWICZ, Elzbieta
IPC分类号： C07K14/60
CPC分类号： C07K14/60 , A61K38/00 , Y02P20/55
摘要： New peptides - 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 (1), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or GAP; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. New peptitides 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, de protecting side-chain amino gorups and reacting free amino groups with a guanidinating agent, removing all remainingt-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新肽 - 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（1），其中R11为hArg，Gab或Gap; R12是hArg，Orn，Gab或GAP; R29是D-Arg，hArg，Gab或Gap; 其药学上可接受的盐是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。在固相合成方法中，通过在连接于聚合物载体的肽链中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来制备新的肽，脱保护侧链氨基将游离氨基与胍胍化剂反应，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，并任选地将肽转化成药学上可接受的盐。

8. 发明申请

WO2009102226A1 MALONIC ACID SALT OF 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]- 2,4-THIAZOLIDINEDIONE 审中-公开
标题翻译： 5 - [[4- [2-（甲基-2-吡啶基]氨基]乙氧基]苯基]甲基] -2,4-噻唑烷二酮的马来酸盐
公开(公告)号：WO2009102226A1
公开(公告)日：2009-08-20
申请号：PCT/PL2009/000015
申请日：2009-02-11
申请人： ADAMED SP. Z O.O. , CHODYNSKI, Michal , KUTNER, Andrzej , LESZCZYNSKA, Kinga , PIETRASZEK, Anita , GLICE, Magdalena , KORCZAK, Kataryzna , MARUSZAK, Wioleta
发明人： CHODYNSKI, Michal , KUTNER, Andrzej , LESZCZYNSKA, Kinga , PIETRASZEK, Anita , GLICE, Magdalena , KORCZAK, Kataryzna , MARUSZAK, Wioleta
IPC分类号： C07D417/12 , A61K31/4439 , A61P3/10
CPC分类号： C07D417/12 , C07B2200/13
摘要： The invention discloses the malonic acid salt of 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione, encompassing its isomers, tautomers and/or solvates thereof, and their use for the treatment and/or prevention of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof.
摘要翻译：本发明公开了5 - [[4- [2-（甲基-2-吡啶基氨基）乙氧基]苯基]甲基] -2,4-噻唑烷二酮的丙二酸盐，包括其异构体，互变异构体和/或溶剂合物，用于治疗和/或预防糖尿病，与糖尿病有关的病症及其某些并发症。

9. 发明申请

WO2008118030A1 PROCESS FOR PREPARATION OF PURE POLYMORPHIC FORM 1 OF CLOPIDOGREL HYDROGENSULFATE 审中-公开
标题翻译：棕榈酸水合物的纯多晶型1的制备方法
公开(公告)号：WO2008118030A1
公开(公告)日：2008-10-02
申请号：PCT/PL2008/000023
申请日：2008-03-19
申请人： KOZLUK, Tomasz , WOZNIAK, Robert
发明人： KOZLUK, Tomasz , WOZNIAK, Robert
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Process for the preparation of substantially pure polymorphic Form 1 of clopidogrel hydrogensulfate, wherein the reaction of optically active clopidogrel base with sulfuric acid is carried out in the mixture of at least two solvents, chosen from group I, comprising aliphatic ethers, and from group II, comprising ketones, esters of C 1 -C 3 carboxylic acids and aliphatic alcohols C 1 -C 4 , primary, secondary and tertiary aliphatic alcohols C 1 -C 4 , then the resulting suspension is stirred until at least 70% of amorphous clopidogrel hydrogensulfate formed is transformed into polymorphic Form 1 of clopidogrel hydrogensulfate, and finally, the crystalline solid is isolated from the reaction mixture and subject to additional work-up procedure, aiming at the formation and stabilization of polymorphic Form 1.
摘要翻译：用于制备基本上纯的多晶型氯吡格雷硫酸氢盐形式1的方法，其中光学活性氯吡格雷碱与硫酸的反应在至少两种选自包含脂族醚的组I和II组的溶剂的混合物中进行，其包含酮，C 1 -C 3羧酸和脂族醇C 1 -C 4羧酸的酯，伯，仲和叔脂肪族醇C 1 -C 4，然后将所得悬浮液搅拌直到形成的至少70％的无定形氯吡格雷硫酸氢盐转化为多晶型形式1的氯吡格雷硫酸氢盐，最后，从反应混合物中分离出结晶固体，并进行额外的后处理，旨在形成和稳定多晶型物1。

10. 发明申请

WO2008091169A2 PROCESS FOR PREPARATION OF SUBSTANTIALLY PURE POLYMORPHIC FORM I OF OLANZAPINE 审中-公开
标题翻译：制备OLANZAPINE的大多数多晶型物质的方法
公开(公告)号：WO2008091169A2
公开(公告)日：2008-07-31
申请号：PCT/PL2008/000007
申请日：2008-01-22
申请人： TOMASZ KOZLUK NOBILUS ENT , KOZLUK, Tomasz
发明人： KOZLUK, Tomasz
CPC分类号： C07D495/04
摘要： A process for preparation of substantially pure polymorphic Form I of olazapine consists in that olanzapine starting material is subjected to: a) at least one digestion step in an acidic aqueous medium, with an optional addition of active charcoal, and then to neutralizing to pH within the range from about 6.0 to about 11.0, and b) at least one step of separation of impurities in a water - organic solvent system, followed by crystallization from the solution in methylene chloride, and wherein steps a) and b) are separated by steps of isolation of precipitate of olanzapine and can be accomplished in any order.
摘要翻译：制备基本上纯的奥氮平多晶型物I的方法在于将奥氮平起始物质经受：a）在酸性水性介质中至少一个消化步骤，任选加入活性炭，然后中和至pH值在约6.0至约11.0的范围内，和b）在水 - 有机溶剂体系中分离杂质的至少一个步骤，然后从溶液中在二氯甲烷中结晶，并且其中步骤a）和b）通过步骤的分离奥氮平的沉淀物并且可以以任何顺序完成。

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