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1. 发明公开

EP3545950A1 PHARMACEUTICAL COMPOSITION COMPRISING BREXPIPRAZOLE 审中-公开
公开(公告)号：EP3545950A1
公开(公告)日：2019-10-02
申请号：EP18461541.7
申请日：2018-03-26
申请人： Adamed sp. z o.o.
发明人： GARBERA, Kamil , WOS-LATOSI, Katarzyna
IPC分类号： A61K9/16 , A61K31/496 , A61K9/20
摘要： The present invention relates to a pharmaceutical composition comprising a granulate comprising brexpiprazole, wherein the granulate is obtained by wet-granulation of a carrier using a granulation liquid that is a solution of brexpiprazole in a solvent system. The present invention relates also to a granulate used in the pharmaceutical composition, and a unit dosage form comprising the pharmaceutical composition, and the method for manufacturing a pharmaceutical composition comprising brexpiprazole.

2. 发明公开

EP3388063A1 TREATMENT OF A BACTERIAL VAGINAL INFECTION 审中-公开
公开(公告)号：EP3388063A1
公开(公告)日：2018-10-17
申请号：EP17461524.5
申请日：2017-04-14
申请人： Adamed sp. z o.o.
发明人： Berdzik-Kalarus, Sylwia
IPC分类号： A61K31/4178 , A61K31/4164 , A61K31/7048 , A61K45/06 , A61K9/00 , A61K9/20 , A61K47/06 , A61P31/04
CPC分类号： A61K31/4178 , A61K9/0034 , A61K9/06 , A61K9/1617 , A61K9/2018 , A61K31/4164 , A61K31/7048 , A61K45/06 , A61K47/06 , A61P13/04 , A61P31/04 , A61K2300/00
摘要： The present invention relates to furazidin for vaginal use in the treatment of a bacterial vaginal infection. Preferably, the bacterial vaginal infection is caused by Gardnerella vaginalis and/or Atopobium vaginae bacteria.

3. 发明公开

EP2797950A2 ANTICANCER FUSION PROTEIN 有权
标题翻译： ANTIKREBS-FUSIONSPROTEIN
公开(公告)号：EP2797950A2
公开(公告)日：2014-11-05
申请号：EP12824731.9
申请日：2012-12-22
申请人： Adamed sp. z o.o.
发明人： PIECZYKOLAN, Jerzy Szczepan , PAWLAK, Sebastian Dominik , EREK, Bart omiej Maciej , RÓZGA, Piotr Kamil
IPC分类号： C07K14/705 , C12N15/62 , C12N15/12 , A61K38/17 , A61P35/00
CPC分类号： C07K14/525 , C07K7/08 , C07K7/086 , C07K14/005 , C07K14/195 , C07K14/32 , C07K14/43563 , C07K14/43572 , C07K14/461 , C07K14/463 , C07K14/47 , C07K14/70575 , C07K2319/00 , C12N7/00 , C12N9/16 , C12N2760/16033 , C12Y301/04003
摘要： A fusion protein comprising domain (a) which is a functional fragment of hTRAIL protein sequence, which fragment begins with an amino acid at a position not lower than hTRAIL95, or a homolog of said functional fragment having at least 70% sequence identity, preferably 85% identity and ending with the amino acid hTRAIL281; and at least one domain (b) which is a sequence of a cytolytic effector peptide forming pores in the cell membrane, wherein the sequence of domain (b) is attached at the C-terminus or N-terminus of domain (a).The fusion protein can be used for the treatment of cancer diseases.
摘要翻译：一种融合蛋白，其包含作为hTRAIL蛋白序列的功能片段的结构域（a），所述片段以不低于hTRAIL95的氨基酸开始，或所述功能片段的同源物具有至少70％的序列同一性，优选为85 ％同一性，以氨基酸hTRAIL281结尾; 和至少一个结构域（b），其是在细胞膜中形成孔的细胞溶解效应肽的序列，其中结构域（b）的序列连接在结构域（a）的C末端或N末端。融合蛋白可用于治疗癌症。

4. 发明公开

EP2374809A1 A process for the preparation of 6-O-acetyl-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose 审中-公开
标题翻译： Verfahren zur Herstellung von 6-O-乙酰基-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖
公开(公告)号：EP2374809A1
公开(公告)日：2011-10-12
申请号：EP10461509.1
申请日：2010-03-16
申请人： Adamed sp. z o.o. , Zaklad Doswiadczalny CHEMIPAN Instytutu Chemii Fizyczneh i Instytutu Chemii Organicznej Polskiej Akademii Nauk
发明人： Majka, Zbigniew , Raczko, Jerzy , Bartoszewski, Zbigniew, , Powala, Sylwester , Radwanski, Bogdan
IPC分类号： C07H1/00 , C07H5/06
CPC分类号： C07H1/00 , C07H5/06
摘要： The invention relates to a process for the preparation of 6-O-acetyl-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose, which process comprises reaction of 1,6-anhydro-2-azido-2-deoxy-D-glucopyranose with benzyl bromide in acetonitrile in the presence of solid sodium hydroxide to form 1,6-anhydro-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose; subsequent reaction of 1,6-anhydro-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose with acetic anhydride in the presence of trifluoroacetic acid to form 1,6-di-O-acetyl-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose; and treatment of 1,6-di-O-acetyl-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose with piperidine in THF.
6-0-Acetyl-2-azido-3,4-di-O-benzyl-2-deoxy-D-glucopyranose is useful as a building block for synthesis of glucosamine oligosaccharides.
摘要翻译：本发明涉及制备6-O-乙酰基-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖的方法，该方法包括将1,6-脱水-2 - 叠氮基-2-脱氧-D-吡喃葡萄糖与苄基溴在乙腈中在固体氢氧化钠存在下反应，形成1,6-脱水-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖吡喃葡萄糖; 在三氟乙酸存在下，1,6-脱水-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖与乙酸酐的反应形成1,6-二-O-乙酰基 -2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖; 并用哌啶在THF中处理1,6-二-O-乙酰基-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖。 6-0-乙酰基-2-叠氮基-3,4-二-O-苄基-2-脱氧-D-吡喃葡萄糖可用作合成葡糖胺寡糖的结构单元。

5. 发明授权

EP1513845B2 A PROCESS FOR THE PREPARATION OF OLANZAPINE AND AN INTERMEDIATE THEREFOR 有权
标题翻译：用于生产中间THEREFOR奥氮平和
公开(公告)号：EP1513845B2
公开(公告)日：2010-11-03
申请号：EP03732782.2
申请日：2003-06-10
申请人： Adamed SP. Z O.O.
发明人： MAJKA, Zbigniew , STAWINSKI, Tomasz , RECHNIO, Justyna , WIECZOREK, Maciej
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of olanzapine which process consists in N-methylation of 2-methyl-4-piperazin-1-yl-10H-thieno[2,3-b][1,5]benzodiazepine. The invention relates also to a new intermediate compound, 2-methyl-4-(4-formyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]-benzodiazepine of formula III and a process for the preparation thereof.

6. 发明授权

EP1874745B1 NEW 3-PHENYLPROPIONIC ACID DERIVATIVES AND THEIR USE AS PPAR- GAMMA RECEPTOR LIGANDS 有权
标题翻译： NEW 3-苯基丙酸衍生物及其作为PPAR-γ受体配体的用途
公开(公告)号：EP1874745B1
公开(公告)日：2009-11-11
申请号：EP06703590.7
申请日：2006-01-17
申请人： Adamed SP. Z O.O.
发明人： MAJKA, Zbigniew , RUSIN, Katarzyna , KLUDKIEWICZ, Dominik , SULIKOWSKI, Daniel , KUROWSKI, Krzysztof , MATUSIEWICZ, Katarzyna , STAWINSKI, Tomasz , KOWALCZYK, Piotr
IPC分类号： C07D277/42 , A61K31/426 , A61K31/421 , A61K31/4164 , C07D263/38 , C07D233/84 , C07D417/12
CPC分类号： C07D417/12 , C07D233/84 , C07D263/38 , C07D277/42
摘要： The invention relates to new compounds, being 3-phenylpropionic acid derivatives of formula I wherein W represents COOH group or its bioisosters, or -COO-C1-C4-alkyl group; Y represents NH, N-C1-C10-alkyl, O, or S; Z represents NH, N-C1-C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N-C1-C10-alkyl, N-aryl, NSO2-C1-C10-alkyl, N-SO2-aryl, or N-SO2-heteroaryl; R1 to R6 each independently represent hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof. The compounds are the ligands of PPAR- gamma receptor and are useful as medicaments.

7. 发明公开

EP1513845A1 A PROCESS FOR THE PREPARATION OF OLANZAPINE AND AN INTERMEDIATE THEREFOR 有权
标题翻译：用于生产中间THEREFOR奥氮平和
公开(公告)号：EP1513845A1
公开(公告)日：2005-03-16
申请号：EP03732782.2
申请日：2003-06-10
申请人： Adamed SP. Z O.O.
发明人： MAJKA, Zbigniew , STAWINSKI, Tomasz , RECHNIO, Justyna , WIECZOREK, Maciej
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of olanzapine which process consists in N-methylation of 2-methyl-4-piperazin-1-yl-10H-thieno[2,3-b][1,5]benzodiazepine. The invention relates also to a new intermediate compound, 2-methyl-4-(4-formyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]-benzodiazepine of formula III and a process for the preparation thereof.

8. 发明公开

EP3243506A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：EP3243506A1
公开(公告)日：2017-11-15
申请号：EP16461520.5
申请日：2016-05-09
申请人： Adamed sp. z o.o.
发明人： Cieplucha, Agnieszka
IPC分类号： A61K9/16 , A61K9/20 , A61K31/00
CPC分类号： A61K9/1635 , A61K9/1694 , A61K9/2027 , A61K9/2077 , A61K31/397 , A61K31/505 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising rosuvastatin and ezetimibe for oral administration in the form of a blend of a first component comprising rosuvastatin or a pharmaceutically acceptable salt thereof, wherein the component is dry-granulated, a second component comprising ezetimibe or a pharmaceutically acceptable salt thereof, wherein the component is wet-granulated, and an optionally extragranular phase component, characterized in that the pharmaceutical composition is free from any rosuvastatin stabilizers, and d 90 value for granules of the first component is 800 µm or less. The invention relates also to an uncoated tablet comprising the composition, and a method of manufacturing the composition.
摘要翻译：本发明涉及包含瑞舒伐他汀和依泽替米贝的药物组合物，所述药物组合物以包含罗苏伐他汀或其药学上可接受的盐的第一组分的混合物的形式口服给药，其中所述组分是干式粒化的，第二组分包含依泽替米贝或其药学上可接受的盐其中所述组分是湿法制粒的颗粒和任选的颗粒外相组分，其特征在于所述药物组合物不含任何瑞舒伐他汀稳定剂，并且所述第一组分颗粒的d90值为800μm或更小。本发明还涉及包含该组合物的未包衣片剂，以及制备该组合物的方法。

9. 发明公开

EP3154982A1 COMPOUNDS COMPRISING 1,1',2,5'-TETRAHYDROSPIRO[INDOLE-3,2'-PYRROLE]-2,5'-DIONE SYSTEM AS INHIBITORS P53-MDM2 PROTEIN-PROTEIN INTERACTION 失效
标题翻译： VERBINDUNGEN MIT 1,1'，2,5'-TETRAHYDROSPIRO [INDOL-3,2'-PYRROL] -2,5'-二酮系统抑制剂P53-MDM2-蛋白质 - 蛋白质相互作用
公开(公告)号：EP3154982A1
公开(公告)日：2017-04-19
申请号：EP15733915.1
申请日：2015-06-11
申请人： Adamed sp. z o.o.
发明人： FEDER, Marcin , KALINOWSKA, Iwona , JASZCZEWSKA, Joanna Adriana , BURCHARD, Ewa , LEWANDOWSKI, Wojciech , BULKOWSKA, Urszula , MAZUR, Maria, , WOS-LATOSI, Katarzyna
IPC分类号： C07D487/10 , A61K31/407 , A61P35/00
CPC分类号： C07D487/20 , C07D487/10
摘要： A spirooxoindole compound represented by the formula selected from the group consisting of Formula (IA) and (IB), wherein all symbols are as defined in the description. The compound can find use in a method of prevention and/or treatment of diseases selected from the group consisting of cancer, immune diseases, inflammatory conditions, allergic skin diseases associated with excessive proliferation, and viral infections.
摘要翻译：由选自式（IA）和（IB）的式所表示的螺氧基吲哚化合物，其中所有符号如说明书中所定义。该化合物可用于预防和/或治疗选自癌症，免疫疾病，炎性病症，与过度增殖相关的过敏性皮肤疾病和病毒感染的疾病的方法中。

10. 发明公开

EP2934488A1 A PHARMACEUTICAL COMPOSITION CONTAINING CANDESARTAN CILEXETIL AND AMLODIPINE 有权转让
标题翻译：药用植物精油麻醉药物CANDESARTAN-CILEXETIL UND AMLODIPIN
公开(公告)号：EP2934488A1
公开(公告)日：2015-10-28
申请号：EP13826632.5
申请日：2013-12-19
申请人： Adamed sp. z o.o.
发明人： CIEPLUCHA, Agnieszka
IPC分类号： A61K9/16 , A61K9/20 , A61K31/4184 , A61K31/4422
CPC分类号： A61K31/4184 , A61K9/1641 , A61K9/2077 , A61K31/4422 , A61K2300/00
摘要： A combination pharmaceutical composition comprising candesartan cilexetil and amiodipine or a pharmaceutically acceptable salt thereof, a process for the preparation of such composition and unit dosage form comprising such a composition. The composition consists of a granulate containing candesartan cilexetil, polyethylene glycol and other excipients, wherein the weight ratio of candesartan cilexetil to polyethylene glycol is in the range from 5: 1 to 2: 1, and extragranular phase of powder blend comprising amiodipine or a pharmaceutically acceptable salt thereof and excipients. The composition is prepared by mixing the granulate prepared by wet granulation and extragranular phase.
摘要翻译：一种组合药物组合物，其包含坎地沙坦替卡西林和脒剂或其药学上可接受的盐，制备这种组合物的方法和包含这种组合物的单位剂型。组合物由含有坎地沙坦碳酸酯，聚乙二醇和其它赋形剂的颗粒组成，其中坎地沙坦酯与聚乙二醇的重量比在5:1至2:1的范围内，粉末混合物的颗粒外相包含氨喋呤或药物其可接受的盐和赋形剂。通过将通过湿法制粒制备的颗粒和颗粒外相混合制备组合物。

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