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1. 发明公开

EP4454703A2 PHARMACEUTICAL COMPOSITIONS WITH LOW AMOUNTS OF NITROSAMINE IMPURITIES AND METHODS FOR PRODUCING THE SAME 审中-公开
公开(公告)号：EP4454703A2
公开(公告)日：2024-10-30
申请号：EP24200515.5
申请日：2021-10-15
申请人： Zentiva K.S.
发明人： RIHA, Jaroslav , RIDVAN, Ludek , DOUSA, Michal , KUBELKA, Tomas , GIBALA, Petr , BARTACEK, Frantisek , STASIAK, Pawel , KALASEK, Stanislav , KLUK, Anna , ZVONÍEK, Vít
IPC分类号： A61P3/10
CPC分类号： A61K9/2027 , A61K9/2054 , A61K9/2009 , A61K9/2077 , A61K31/155 , A61K31/4985 , A61K31/522 , A61K31/40 , A61K31/403 , A61K31/513 , A61K31/7048 , A61K31/381 , A61P3/10 , A61K9/2013 , A61K9/2059
摘要： The present invention relates to pharmaceutical compositions comprising metformin with low amounts of nitrosamine impurities and methods for producing the same. More specifically, the present invention relates to methods and compositions that reduce the amount of nitrosable compounds in the active pharmaceutical ingredient and/or reduce the conversion of nitrosable compounds into nitrosamines in the finished dosage form.

2. 发明公开

EP3618814A1 FILM-COATED TABLETS OF DEFERASIROX 审中-公开
公开(公告)号：EP3618814A1
公开(公告)日：2020-03-11
申请号：EP18726029.4
申请日：2018-05-03
申请人： Zentiva, K.S.
发明人： GAJDOSOVA, Michaela , SVOBODOVA, Jaroslava , PECEK, Daniel
IPC分类号： A61K9/20 , A61K9/28 , A61K31/4196

3. 发明公开

EP3572069A1 INCREASING SOLUBILITY AND BIOAVAILABILITY OF ENZALUTAMIDE 审中-公开
公开(公告)号：EP3572069A1
公开(公告)日：2019-11-27
申请号：EP19020336.4
申请日：2019-05-20
申请人： Zentiva K.S.
发明人： Obadalova, Iva , Schongut, Marek , Krejcik, Lukas , Zvatora, Pavel
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K31/4166 , A61K9/20
摘要： The submitted solution relates to the pharmaceutical mixture containing amorphous enzalutamide and at least one excipient from the group of C 5 to C 12 saccharides or their derivatives or their derivatives with possible another substance, wherein the mixture is in the form of solid premix.

4. 发明公开

EP3501609A1 PHARMACEUTICAL COMPOSITIONS COMPRISING IBRUTINIB 审中-公开
公开(公告)号：EP3501609A1
公开(公告)日：2019-06-26
申请号：EP18020631.0
申请日：2018-12-07
申请人： Zentiva K.S.
发明人： Zvatora, Pavel , Beranek, Josef , Cernova, Miroslava , Tieger, Ester , Zvonicek, Vit
IPC分类号： A61Q90/00 , A61K8/99 , A61K45/06 , A61K33/44 , A61P43/00 , A61K31/519
摘要： The solution relates to a pharmaceutical composition without surfactants comprising ibrutinib form C of formula and at least one acceptable excipient selected from the group consisting of a filler, binder, disintegrants and lubricants. The composition comprising ibrutinib of form C while this form has higher solubility, and thus comprises no surfactant fraction. The composition may take the form of tablets or capsules.

6. 发明公开

EP3386945A1 SOLID FORMS OF (2R,4S)-5-(BIPHENYL-4-YL)-4-[(3-CARBOXYPROPIONYL)AMINO]-2- -METHYLPENTANOIC ACID ETHYL ESTER, ITS SALTS AND A PREPARATION METHOD 审中-公开
公开(公告)号：EP3386945A1
公开(公告)日：2018-10-17
申请号：EP16818971.0
申请日：2016-12-12
申请人： Zentiva, K.S.
发明人： HALAMA, Ales , ZVATORA, Pavel , VOSLAR, Michal , STACH, Jan , ZAPADLO, Michal , DAMMER, Ondrej , KREJCIK, Lukas , DVORAKOVA, Lenka , REZANKOVA, Marketa , VYSLOUZIL, Rostislav
IPC分类号： C07C233/47 , A61K31/216
CPC分类号： C07C233/47 , A61K31/216 , C07B2200/13
摘要： The invention relates to solid forms of the free acid of sacubitril of formula 1, especially a crystalline form, incl. a method of removing chemical impurities from the crude free acid of sacubitril that is characterized in the use of well crystallizing salts of sacubitril with the amines of formula 9, where R1, R2, R3 independently stand for hydrogen or a C1-C7 alkyl, preferably the salt with cyclohexylamine, tert-butylamine or iso-propylamine. The invention further relates to a novel solid, crystalline form of sacubitril (8) - hemisolvate of the potassium salt of sacubitril, incl. a direct and highly efficient and industrially usable preparation methods of a solid form of sacubitril free acid and its pharmaceutically applicable salts, especially the crystalline sodium salt of formula 5, calcium salt of sacubitril of formula 6 and hemisolvate of the potassium salt of sacubitril of formula 8.

7. 发明授权

EP3131910B1 USE OF A 1,3,5-TRIAZIN-2-YL PHOSPHORAMIDATE COMPOUND IN THE SYNTHESIS OF SOFOSBUVIR 有权
公开(公告)号：EP3131910B1
公开(公告)日：2018-08-15
申请号：EP15720254.0
申请日：2015-04-15
申请人： Zentiva K.S.
发明人： STEFKO, Martin , MAN, Stanislav , RADL, Stanislav
IPC分类号： C07F9/6521 , C07F9/6558
CPC分类号： C07F9/65586 , C07F9/6521
摘要： The present invention relates to a new type of 1,3.5-triazin-2-yl phosphoramidates of general formula I with the absolute configuration (S) at the phosphorus atom, an Sp diastereoisomer, wherein R1 and R2 can independently be H, a C1-C6 (un)branched alkyl, a C1-C6 (un)branched alkoxy group, a C1-C6 (un)branched alkylsulfanyl group, C1-C6 (un)branched monoalkylamino or dialkylamino group, including cyclic amino groups, e.g. pyrrolidino, piperidino or morpholino group; and to their use for the production of biologically active phosphoramidate prodrugs, especially sofosbuvir of formula II. Sofosbuvir II is a nucleotide inhibitor of the RNA polymerase, used for the treatment of hepatitis C in the form of a prodrug, releasing the active antiviral agent 2'-deoxy-2'-a-fluoro- P-C-methyluridine-5'-triphosphate in the organism.

8. 发明公开

EP3281941A1 PROCESS FOR PREPARING 2-(5-BROMO-4-(1-CYCLOPROPYLNAPHTHALEN-4-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO)ACETIC ACID 审中-公开
标题翻译：制备2-（5-溴-4-（1-环丙基酞嗪-4-基）-4H-1,2,4-三唑-3-基硫基）乙酸的方法
公开(公告)号：EP3281941A1
公开(公告)日：2018-02-14
申请号：EP17020330.1
申请日：2017-08-02
申请人： Zentiva K.S.
发明人： Stach, Jan , Radl, Stanislav , Zvatora, Pavel , Pisa, Ondrej , Benediktova, Kristyna , Halama, Ales
IPC分类号： C07D249/10 , C07F7/18
CPC分类号： C07D249/10 , Y02P20/55
摘要： The object of the invention is a novel and efficient production method of 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4 H -1,2,4-triazol-3-ylthio)acetic acid of formula 1 known under the generic name lesinurad. The novel method is based on bromination of 2-(4-(1-cyclopropylnaphthalen-4-yl)-4 H -1,2,4-triazol-3-ylthio)acetic acid of formula 17, whose carboxyl function is protected by a trialkylsilyl group. When the novel method is used, the bromination reaction runs selectively and with a high conversion rate of the input compound. The introduction and deprotection of the used protecting group run very easily, so there is no need to isolate the produced intermediates of formula 18 and 19, which reduces the number of handling steps. The isolation of the product from the reaction mixture is advantageously based on the good crystallizing properties of the newly found salts of lesinurad of formula 21 and 22.
摘要翻译：本发明的目的在于提供一种新颖且有效的式（I）化合物的2-（5-溴-4-（1-环丙基萘-4-基）-4H-1,2,4-三唑-3-基硫基）乙酸的制备方法， 1通用名称为lesinurad。该新方法基于溴化式17的2-（4-（1-环丙基萘-4-基）-4H-1,2,4-三唑-3-基硫代）乙酸，其羧基官能团被保护三烷基甲硅烷基。当使用新方法时，溴化反应选择性地进行并且输入化合物的转化率高。所用保护基团的引入和脱保护非常容易进行，因此不需要分离生成的式18和19中间体，这减少了处理步骤的次数。产物从反应混合物中的分离有利地基于新发现的式21和22的稀盐的良好结晶性质。

9. 发明公开

EP3280701A1 A METHOD OF CHIRAL RESOLUTION OF THE KEY INTERMEDIATE OF THE SYNTHESIS OF APREMILAST AND ITS USE FOR THE PREPARATION OF PURE APREMILAST 有权
标题翻译：一种合成APREMILAST中间体的手性拆分方法及其用于纯APREMILAST的制备
公开(公告)号：EP3280701A1
公开(公告)日：2018-02-14
申请号：EP16718846.5
申请日：2016-04-11
申请人： Zentiva K.S.
发明人： FAIGL, Ferenc , DOUBSKY, Jan , KLVANA, Robert , RICHTER, Jindrich , FOGASSY, Elemer , MATRAVOLGYI, Bela , MIZSAK, Agnes
IPC分类号： C07D209/40 , C07C315/06 , C07C317/28 , C07C233/15
摘要： The present invention provides a method of chiral resolution of racemic amines of the benzyl type by means of salts formed with tartaric acid of formula (3) and intermediate of formula (2), and their use in the synthesis of Apremilast of formula 1.

10. 发明公开

EP3263552A1 METHODS FOR PREPARING INTERMEDIATES FOR THE SYNTHESIS OF OBETICHOLIC ACID 审中-公开
标题翻译：制备中间体用于合成代谢酸的方法
公开(公告)号：EP3263552A1
公开(公告)日：2018-01-03
申请号：EP17020257.6
申请日：2017-06-19
申请人： Zentiva K.S.
发明人： Kubelka, Tomas , Slavikova, Marketa , Zezula, Josef , Cerny, Josef
IPC分类号： C07C305/12 , A61K31/567 , A61K31/575
CPC分类号： C07J9/005 , C07J17/00 , C07J51/00
摘要： The present invention discloses a method for preparing the key intermediates of formula 2 (disilylated derivative) and enones of formula 3 (mixture of E/Z isomers) for synthesis of the active pharmaceutical ingredient - obeticholic acid of formula 1. The principle of the method is that it comprises a reaction of the compound of formula 8 , wherein R 1 is a C1 to C4 linear or branched alkyl, with trimethylsilyl iodide in the presence of a base and a mixture of a polar aprotic and non-polar solvent under an inert atmosphere at a temperature in the range of from 40°C to 70°C.
摘要翻译：本发明公开了制备式2的关键中间体（二甲硅烷基化衍生物）和式3的烯酮（E / Z异构体的混合物）用于合成式1的活性药物成分 - 氧化乙烯酸的方法。该方法的原理在于它包括式8化合物（其中R1是C1-C4直链或支链烷基）与三甲基甲硅烷基碘在惰性气氛下在碱和极性非质子传递溶剂和非极性溶剂的混合物存在下的反应在40℃至70℃范围内的温度下进行。

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