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21. 发明申请

WO2021071372A1 PROCESS OF VITAMIN K2 DERIVATIVES PREPARATION 审中-公开
公开(公告)号：WO2021071372A1
公开(公告)日：2021-04-15
申请号：PCT/PL2019/000086
申请日：2019-10-07
申请人： SIEĆ BADAWCZA ŁUKASIEWICZ - INSTYTUT FARMACEUTYCZNY
发明人： SIDORYK, Katarzyna , JATCZAK, Kamil , BURZYŃSKA-PRAJZNER, Agnieszka , CYBULSKI, Marcin , NAPIÓRKOWSKI, Marek , PIETRZKOWSKA, Dorota , JEDYNAK, Łukasz , KUBISZEWSKI, Marek
IPC分类号： C07C46/00 , C07C315/04 , C07C50/22 , C07C317/18 , C07C2602/10 , C07C2603/70 , C07C2603/86 , C07C317/24
摘要： The invention relates to an improved process of vitamin K2 derivatives preparation via the alkylation of the menadione-cyclopentadiene adduct.

22. 发明申请

WO2014191823A1 AMINE DERIVATIVES AS IL-15 ACTIVITY INHIBITORS 审中-公开
标题翻译：作为IL-15活性抑制剂的胺衍生物
公开(公告)号：WO2014191823A1
公开(公告)日：2014-12-04
申请号：PCT/IB2014/000896
申请日：2014-05-29
申请人： WARSZAWSKI UNIWERSYTET MEDYCZNY
发明人： KOZIAK, Katarzyna , ZYZYNSKA-GRANICA, Barbara , FILIPEK, Slawomir , NIEWIECZERZAL, Szymon , TRZASKOWSKI, Bartosz , ZEGROCKA-STENDEL, Oliwia , DUTKIEWICZ, Malgorzata , KRZECZYNSKI, Piotr , KACZMAREK, Elzbieta , WINIARSKA, Magdalena
IPC分类号： A61K31/00 , A61K31/155 , A61K31/16 , A61K31/417 , A61K31/4172 , A61P29/00
CPC分类号： A61K31/4172 , A61K31/155 , A61K31/16 , A61K31/417
摘要： The present invention relates to the benzoic acid derivatives of the formula (I), as described in the claims, their tautomers, isomers, pharmaceutically acceptable salts and solvates, for the use in the treatment of diseases related to interleukin 15 overproduction.
摘要翻译：本发明涉及如权利要求中所述的式（I）的苯甲酸衍生物，其互变异构体，异构体，药学上可接受的盐和溶剂合物，用于治疗与白细胞介素15过量产生有关的疾病。

23. 发明申请

WO2013133730A1 PROCESS FOR PREPARATION OF PROSTAGLANDIN F2α ANALOGUES 审中-公开
标题翻译：制备前列腺素F2α类似物的方法
公开(公告)号：WO2013133730A1
公开(公告)日：2013-09-12
申请号：PCT/PL2013/000028
申请日：2013-03-08
申请人： INSTYTUT FARMACEUTYCZNY
发明人： DAMS, Iwona , KUTNER, Andrzej , CHODYŃSKI, Michał , KRUPA, Małgorzata , PIETRASZEK, Anita , ZEZULA, Marta , CMOCH, Piotr , KOSIŃSKA, Monika
IPC分类号： C07C405/00 , C07F7/18
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0041 , C07C2601/08 , C07D493/08 , C07F7/0818 , C07F7/083 , C07F7/184
摘要： A convergent synthesis of the prostaglandin F 2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.
摘要翻译：利用结构上先进的苯基砜与对映异构体纯的醛ω-链合成子进行茱莉亚 - 柠檬酸的合成，开发了前列腺素F2alpha类似物，曲伏前列素和比马前列素的收敛合成。该新颖的收敛策略允许从普通和结构先进的前列腺素中间体合成高纯度的全系列前列腺素类似物。

24. 发明申请

WO2010107329A2 ARIPIPRAZOLE SALTS 审中-公开
标题翻译：阿维菌唑
公开(公告)号：WO2010107329A2
公开(公告)日：2010-09-23
申请号：PCT/PL2010/000031
申请日：2010-04-23
申请人： KOZLUK, Tomasz , WOZNIAK, Robert
发明人： KOZLUK, Tomasz , WOZNIAK, Robert
IPC分类号： C07D215/227
CPC分类号： C07D215/227
摘要： Aripiprazole salts, consisting of aripiprazole and tricarboxylic acid derivative, wherein one carboxyl group of an acid forms ester with C 1 -C 4 -aliphatic alcohol, represented by formula (1), wherein is double bond and R is H, or is single bond and R is -O (C=O) R 2 , R2 is Ci-C4-aliphatic group or phenyl, optionally substituted by -CH 3 or - OCH3 group in position 4 of the phenyl ring, n = 1 - 2, are new derivatives of antipsychotic effect. Aripiprazole salts are prepared in the reaction of aripiprazole free base and bicarboxylic acid anhydride in C 1 -C 4 aliphatic alcohol as a solvent.
摘要翻译：由阿立哌唑和三羧酸衍生物组成的阿立哌唑盐，其中一个羧基与C1-C4脂族醇形成酯，由式（1）表示，其中双键和R为H，或为单键，R 是-O（C = O）R 2，R 2是C 1 -C 4脂族基团或苯基，任选地被苯环的4位的-CH 3或-OCH 3基团取代，n = 1-2，是抗精神病效应的新衍生物。阿立哌唑盐是在阿立哌唑游离碱和双羧酸酐作为溶剂的C1-C4脂族醇反应中制备的。

25. 发明申请

WO2009123483A1 PROCESS FOR PREPARATION OF TELMISARTAN 审中-公开
标题翻译： TELMISARTAN的制备方法
公开(公告)号：WO2009123483A1
公开(公告)日：2009-10-08
申请号：PCT/PL2009/000027
申请日：2009-03-30
申请人： ZAKLADY FARMACEUTYCZNE POLPHARMA SA , GRUZA, Mariusz, Marek , ZAGRODZKA, Joanna , KRZECZYNSKI, Piotr , FILIP, Katarzyna
发明人： GRUZA, Mariusz, Marek , ZAGRODZKA, Joanna , KRZECZYNSKI, Piotr , FILIP, Katarzyna
IPC分类号： C07D235/08 , C07D403/04
CPC分类号： C07D403/04 , C07D235/08 , Y02P20/55
摘要： A process for preparation of telmisartan comprises: (i) oxidation of compound of formula (a), wherein R 2 is a hydrogen atom or a substituent of formula (b), in which R 1 is a protecting group for the carboxyl function, to an aldehyde of formula (c), in which R 2 is defined as in the formula (a), and, optionally, (ii) in case R 2 in the compound (c) thus obtained is a hydrogen atom, iV-alkylation of the compound (c) with a biphenyl derivative, (iii) treatment of the compound (c) thus obtained with N- methyl- o -nitroaniline in a cyclocondensation reaction, and (iv) cleavage of the protecting group R 1 .
摘要翻译：制备替米沙坦的方法包括：（ⅰ）将式（ⅰ）化合物氧化成醛，其中R 2为氢原子或式（ⅱ）的取代基，其中R 1为羧基官能团的保护基，其中R 2如式（a）中所定义，并且任选地，（ⅱ）在如此获得的化合物（c）中的R 2为氢原子时，化合物（c）的N-烷基化），（iii）在环化缩合反应中用N-甲基 - 邻硝基苯胺处理由此获得的化合物（c），和（iv）裂解保护基团R1。

26. 发明申请

WO2007075095A1 PROCESS FOR THE PREPARATION OF PRAMIPEXOLE BASE AND/OR ITS SALTS 审中-公开
标题翻译：制备原料和/或其盐的方法
公开(公告)号：WO2007075095A1
公开(公告)日：2007-07-05
申请号：PCT/PL2006/000093
申请日：2006-12-29
申请人： INSTYTUT FARMACEUTYCZNY , BALICKI, Roman , SYPNIEWSKI, Michal , CIESIELSKA, Agnieszka , SZELEJEWSKI, Wieslaw , ZAGRODZKA, Joanna , CIEPLUCHA, Grazyna
发明人： BALICKI, Roman , SYPNIEWSKI, Michal , CIESIELSKA, Agnieszka , SZELEJEWSKI, Wieslaw , ZAGRODZKA, Joanna , CIEPLUCHA, Grazyna
IPC分类号： C07D277/82 , A61K31/428 , A61P25/16
CPC分类号： C07D277/82
摘要： The process for the preparation of pramipexole base and/or its pharmaceutically accepted salts, especially hydrochloride salt, is based on the reaction of (S)-(-)2,6-diamino-4,5,6,7-tetrahydrobenzothiazole with an alkylating agent, wherein the reaction is carried out with the absence of a base, in a solvent from which the resulting N-monoalkylated product selectively precipitates out as a salt, which, after isolation from the reaction mixture: a) upon the treatment of inorganic base is converted into free pramipexole base, and then into another pharmaceutically accepted pramipexole salt, or b) is converted directly into another pharmaceutically accepted pramipexole salt or the hydrate thereof.
摘要翻译：制备普拉克索碱和/或其药学上可接受的盐，特别是盐酸盐的方法是基于（S） - （ - ） - 2,6-二氨基-4,5,6,7-四氢苯并噻唑与烷基化剂，其中反应在不存在碱的情况下在溶剂中进行，所得的N-单烷基化产物从其中选择性地沉淀出盐，其在从反应混合物中分离后：a）在处理无机碱被转化为游离的普拉克索碱，然后转化成另一种药学上可接受的普拉克索盐，或者b）直接转化成另一种药学上可接受的普拉克索盐或其水合物。

27. 发明申请

WO2005108366A1 A PROCESS FOR THE PREPARATION OF 2-[N- [(S)-1-ETHOXYCARBONYL-3-PHENYLPROPYL]-(S)-ALANYL]-(1S, 3S, 5S) -2-AZABICYCLO [3.3.0] OCTANE-3-CARBOXYLIC ACID 审中-公开
标题翻译：制备2- [N - [（S）-1-乙氧基羰基-3-苯基丙基] - （S） - 醇] - （1S，3S，5S）-2-氮杂双环[3.3.0] 3-羧酸
公开(公告)号：WO2005108366A1
公开(公告)日：2005-11-17
申请号：PCT/PL2005/000029
申请日：2005-05-12
申请人： INSTYTUT FARMACEUTYCZNY , BANKOWSKI, Krzysztof , WACHAL, Teresa , SIDORYK, Katarzyna , SZELEJEWSKI, Wieslaw
发明人： BANKOWSKI, Krzysztof , WACHAL, Teresa , SIDORYK, Katarzyna , SZELEJEWSKI, Wieslaw
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： A process for preparation of 2-[N-[(S)-l-ethoxycarbonyl-3-phenylpropyl] - (S) -alanyl]-(1S, 3S, 5S)-2- azabicyclo [3.3.0 ] octane-3-carboxylic acid, ie. Ramipril, involves condensation of an activated derivative of 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-(S)-alanine with racemic (1R * , 3R * , 5R * ) -2-azabicyclo [3.3.0] octane-3-carboxylic acid, and then the desired diastereoisomer (la) is separated from the obtained diastereoisomeric mixture of 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl](S) -alanyl] - (1S, 3S, 5S ) -2-azabicyclo [3.3.0] octane-3-carboxylic acid (1a) and 2- [N-[(S)-1-ethoxycarbonyl-3-phenylpropyl ] - (S) -alanyl ] - (1R, 3R, 5R) -2- azabicyclo[3.3.0]octane-3-carboxyl ic acid (lb) by treating it with a solvent that selectively dissolves the undesired diastereoisomer (1b) while the diastereoisomer (1a) remains undissolved.
摘要翻译：制备2- [N - [（S）-1-乙氧基羰基-3-苯基丙基] - （S） - 丙氨酰] - （1S，3S，5S）-2-氮杂双环[3.3.0]辛烷-3 - 羧酸，即雷米普利涉及2- [N - [（S）-1-乙氧基羰基-3-苯基丙基] - （S） - 丙氨酸的活化衍生物与外消旋（1R，3R，5R * ）-2-氮杂双环[3.3.0]辛烷-3-羧酸，然后将所需的非对映异构体（Ia）从得到的2- [N - [（S）-1-乙氧基羰基-3-苯基丙基（S） - 丙氨酰] - （1S，3S，5S）-2-氮杂双环[3.3.0]辛烷-3-羧酸（1a）和2- [N - [（S）-1-乙氧基羰基-3- 苯基丙基] - （S） - 丙氨酰] - （1R，3R，5R）-2-氮杂双环[3.3.0]辛烷-3-羧酸（1b），通过用选择性溶解不需要的非对映异构体），而非对映异构体（1a）保持未溶解。

28. 发明申请

WO2005072776A3 LIPOSOMAL FORMULATIONS OF THE ANTINEOPLASTIC AGENTS 审中-公开
公开(公告)号：WO2005072776A3
公开(公告)日：2005-08-11
申请号：PCT/PL2005/000007
申请日：2005-01-28
申请人： INSTYTUT FARMACEUTYCZNY , KOZUBEK, Arkadiusz , GRYNKIEWICZ, Grzegorz , SZELEJEWSKI, Wieslaw , SLIFIRSKI, Piotr , GUBERNATOR, Jerzy , STASIUK, Maria , WISNIEWSKI, Krzysztof
发明人： KOZUBEK, Arkadiusz , GRYNKIEWICZ, Grzegorz , SZELEJEWSKI, Wieslaw , SLIFIRSKI, Piotr , GUBERNATOR, Jerzy , STASIUK, Maria , WISNIEWSKI, Krzysztof
IPC分类号： A61K9/127
摘要： The invention relates to the liposomal formulation of an antineoplastic agent encapsulated in the liposomal vesicles which are the composition of lipid components, wherein the ratio of a therapeutically active agent to the lipid components is between about 1:10 and about 1:30 (w/w). The composition of lipid components contains at least one phospholipid derivative and at least one alkylphenol derivative presented by a general formula (I) , wherein: n is an integer 1 - 17; m is an integer 0-15; X is -C=O, -0- or a bond; Y is a group of formula -NR 2 R 3 , a monosaccharide moiety or a bond; Z is H, -0-, -N-, -OR 4 , -NR 4 or a monosaccharide moiety, R 5 is H or COOH.

29. 发明申请

WO2002081491A2 NEW GENISTEIN DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM 审中-公开
标题翻译：新一代衍生物和含有它们的药物制剂
公开(公告)号：WO2002081491A2
公开(公告)日：2002-10-17
申请号：PCT/PL2002/000029
申请日：2002-04-08
申请人： INSTYTUT FARMACEUTYCZNY , INSTYTUT LEKÓW , ACHMATOWICZ, Osman , GRYNKIEWICZ, Grzegorz , PUCKO, Wieslaw , MAZUREK, Aleksander, P. , POLKOWSKI, Krzysztof , BORYSKI, Jerzy , SZEJA, Wieslaw , SZELEJEWSKI, Wieslaw , OPOLSKI, Adam , PASTUCH-GAWOLEK, Gabriella , RADZIKOWSKI, Czeslaw , SZECHNER, Barbara , WIETRZYK, Joanna , SKIERSKI, Janusz , WANDZIK, Ilona , KRZECZYNSKI, Piotr
发明人： ACHMATOWICZ, Osman , GRYNKIEWICZ, Grzegorz , PUCKO, Wieslaw , MAZUREK, Aleksander, P. , POLKOWSKI, Krzysztof , BORYSKI, Jerzy , SZEJA, Wieslaw , SZELEJEWSKI, Wieslaw , OPOLSKI, Adam , PASTUCH-GAWOLEK, Gabriella , RADZIKOWSKI, Czeslaw , SZECHNER, Barbara , WIETRZYK, Joanna , SKIERSKI, Janusz , WANDZIK, Ilona , KRZECZYNSKI, Piotr
IPC分类号： C07H15/00
CPC分类号： C07F7/1856 , C07D311/36 , C07D405/12 , C07H15/26
摘要： Genistein derivatives of Formula (1), wherein R 1 and R 2 are the same or different and independently represent hydrogen atom, alkyl, aryl, alkyloaryl, alkylcarbonyl, arylcarbonyl, while each of the above mentioned groups may be substituted in a chain or ring by amino, nitro or nitrile groups, R 5 (R 6 )R 7 -Si- group wherein R 5 , R 6 and R 7 are the same or different and denote C 1-6 alkyl or aryl, mono-, di- or oligosaccharide group while at least one hydroxyl group of saccharide group may be substituted by the same or different acyl, alkyl, acyloxyalkyl or aryl groups;R 3 represents hydrogen atom or -COCH 3 group; and R 4 represents hydrogen atom, -SO 3 H, SO 3 - or -NH 2 or -NO 2 group; and their pharmaceutically acceptable salts exhibit antyproliferative and antitumour activity. New derivatives and pharmaceutical preparations containing them may be suitable in clinical oncology and/or chemoprevention of neoplasms.
摘要翻译：式（1）的染料木黄酮衍生物，其中R 1和R 2相同或不同并且独立地表示氢原子，烷基，芳基，烷芳基，烷基羰基，芳基羰基，而上述各基团可以被链或环中的氨基，硝基或腈基，R5（R6）R7-Si-基团，其中R5，R6和R7相同或不同，表示C1-6烷基或芳基，单糖，二糖或寡糖基团，而至少一个糖基的羟基基团可以被相同或不同的酰基，烷基，酰氧基烷基或芳基取代; R3代表氢原子或-COCH3基团; 并且R 4表示氢原子，-SO 3 H，SO 3 - 或-NH 2或-NO 2基团; 其药学上可接受的盐显示出非增殖性和抗肿瘤活性。含有它们的新衍生物和药物制剂可能适用于肿瘤的临床肿瘤学和/或化学预防。

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