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1. 发明申请

WO2005072776A2 LIPOSOMAL FORMULATIONS OF THE ANTINEOPLASTIC AGENTS 审中-公开
标题翻译：抗生素代谢物的制备
公开(公告)号：WO2005072776A2
公开(公告)日：2005-08-11
申请号：PCT/PL2005000007
申请日：2005-01-28
申请人： INST 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 , A61K47/00
CPC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 -NR2R3, a monosaccharide moiety or a bond; Z is H, -0-, -N-, -OR4, -NR4 or a monosaccharide moiety, R5 is H or COOH.
摘要翻译：本发明涉及包封在作为脂质组分的组合物的脂质体囊泡中的抗肿瘤剂的脂质体制剂，其中治疗活性剂与脂质组分的比例为约1:10至约1:30（w / W）。脂质成分的组成含有至少一种磷脂衍生物和由通式（I）表示的至少一种烷基酚衍生物，其中：n为1〜17的整数; m是整数0-15; X是-C = O，-O-或键; Y是式-NR2R3，单糖部分或键的基团; Z是H，-O-，-N-，-OR4，-NR4或单糖部分，R5是H或COOH。

2. 发明申请

WO0056267A3 METHODS AND COMPOSITIONS FOR THE MANUFACTURE OF C-3' AND C-4' ANTHRACYCLINE ANTIBIOTICS 审中-公开
标题翻译：制备C-3'和C-4'蒽环霉素抗生素的方法和组合物
公开(公告)号：WO0056267A3
公开(公告)日：2001-02-22
申请号：PCT/IB0000527
申请日：2000-03-15
申请人： PRIEBE WALDEMAR , FOKT IZABELA , PRZEWLOKA TERESA , KRAWCZYK MARTA , SKIBICKI PIOTR , GRYNKIEWICZ GRZEGORZ , PEREZ SOLER ROMAN
发明人： PRIEBE WALDEMAR , FOKT IZABELA , PRZEWLOKA TERESA , KRAWCZYK MARTA , SKIBICKI PIOTR , GRYNKIEWICZ GRZEGORZ , PEREZ-SOLER ROMAN
IPC分类号： C07H15/252 , C07H1/00 , C07H15/24
CPC分类号： C07H15/252 , A61K31/704
摘要： The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3' of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4' of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.
摘要翻译：本发明公开了在糖部分的C-3'上具有修饰的烷基 - 芳香环取代或在糖部分的C-4'处的修饰或未修饰的烷基 - 芳香环取代的新的和新的取代的蒽环类。它还公开了制备糖底物的新方法和制备蒽环类抗生素的方法。这些蒽环类似物在体外对几种肿瘤细胞系显示出高细胞毒性。

3. 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.

4. 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。

5. 发明申请

WO2010095964A1 A METHOD FOR AMPHIPHILIC DRUG LOADING IN LIPOSOMES BY ION GRADIENT 审中-公开
标题翻译：离子梯度法测定脂质体中两性药物的含量
公开(公告)号：WO2010095964A1
公开(公告)日：2010-08-26
申请号：PCT/PL2010000014
申请日：2010-02-16
申请人： INST FARMACEUTYCZNY , GUBERNATOR JERZY , KOZUBEK ARKADIUSZ , GRYNKIEWICZ GRZEGORZ , OBUKOWICZ JANUSZ
发明人： GUBERNATOR JERZY , KOZUBEK ARKADIUSZ , GRYNKIEWICZ GRZEGORZ , OBUKOWICZ JANUSZ
IPC分类号： A61K9/127 , A61K31/704
CPC分类号： A61K31/704 , A61K9/127 , A61K9/1278
摘要： An active loading of amphophilic drugs, especially anthracycline antibiotics, in liposomes using conventional lipid compositions, is achieved by applying salts of polycarboxylic acids with mono- or divalent cations, preferably selected from sodium, potassium, calcium, magnesium or ammonium salt of ethylenediaminotetraacetic acid (EDTA) or ethyleneglycol-O-O'-bis(2-aminoethyl)-N,N,N',N'-tetraacetic acid (EGTA). The liposomal formulations obtained by the method of active loading of drugs to liposomes by EDTA or EGTA salts gradient are characterized by high loading efficiency, feature microcrystalline deposits of anthracyclines inside liposomes, which renders them stable and not susceptible to leakage. The liposomes are unilamellar and their size is close to 100 nanometers after drug loading.
摘要翻译：使用常规脂质组合物在脂质体中活性负载两性药物，特别是蒽环类抗生素，是通过将多羧酸的盐与一价或二价阳离子，优选选自亚乙基二氨基四乙酸的钠盐，钾盐，钙盐，镁盐或铵盐（ EDTA）或乙二醇-O-O'-双（2-氨基乙基）-N，N，N'，N'-四乙酸（EGTA）。通过EDTA或EGTA盐梯度将药物主动加载到脂质体的方法获得的脂质体制剂的特征在于高负载效率，特征在于脂质体内蒽环类的微晶沉积，其使得它们稳定且不易泄漏。载药后脂质体是单层的，其大小接近100纳米。

6. 发明申请

WO2007003236A1 PROCESS FOR SYNTHESIS OF COMPLEX 2-DEOXY-2-IODO PYRANOSIDES OF HIGH PURITY, PARTICULARLY SUITABLE FOR MANUFACTURING PHARMACEUTICALLY PURE ANNAMYCIN 审中-公开
标题翻译：用于合成高纯度的复合2-脱氧-2-碘代吡喃糖苷的方法，特别适用于制备药物稳定的抗体
公开(公告)号：WO2007003236A1
公开(公告)日：2007-01-11
申请号：PCT/EP2006/002541
申请日：2006-03-14
申请人： ZACLAD BADAWCZO-PRODUKCYJNY "SYNTEX" , SZEJA, Wieslaw , GRYNKIEWICZ, Grzegorz , FOKT, Izabela
发明人： SZEJA, Wieslaw , GRYNKIEWICZ, Grzegorz , FOKT, Izabela
IPC分类号： C07H15/04 , C07H15/252
CPC分类号： C07H15/252 , C07H15/04
摘要： The method according to the invention comprises using as glycosyl donors high purity 2- deoxy-2-iodo derivatives of sugars of a defined configuration of C-2 carbon with O-alkyl, S- alkyl, O-aryl, S-aryl, O-heteroaryl, S-heteroaryl, O-acyl, O-silyl, O-N-imido, O-P- (phosphino, phosphono, thiophosphono, selenophosphono) groups at the anomeric position, and subjecting them to a condensation reaction with a compound containing a hydroxyl group or a protected hydroxyl group in the presence of electrophilic reagents, followed by deprotection and isolation of a pharmaceutically pure product. The objective of the present invention is to provide a method for preparing complex glycosides by coupling cyclic multifunctional compounds containing hydroxyl functional groups (glycosyl acceptors, including aglycones of natural origin which are known as constituents of active pharmaceutical ingredients) with diastereoisomerically pure 2-deoxy-2-halopyranosyl derivatives containing anomeric substituent capable of exchange under glycosidating conditions, for example by virtue of activation with electrophilic agents. This method substantially simplifies the synthesis of Annamycin. The present invention relies on a regio- and stereoselective reaction of cohalogenating 1,2- unsaturated sugars in the presence of hydroxyl group containing compounds, such as: water, alcohols, phenols, carboxylic acids, silanols, phosphinic acids, phosphoric acids, thiophosphoric acids, selenophosphoric acids, followed by separation of the product with proper C-2 carbon configuration required for the synthesis. As the separation of stereoisomers is carried out at the stage of obtaining a relatively inexpensive intermediate in the form of glycosyl donor, the method of the invention substantially reduces the cost of Annamycin manufacture. Other advantages of the synthesis process of the invention consist in the reduction of the number of stages of the antibiotic manufacture process and in yield increase of the final product.
摘要翻译：根据本发明的方法包括作为糖基供体使用具有O-烷基，S-烷基，O-芳基，S-芳基，O - 烷基，C 2- - 杂芳基，S-杂芳基，O-酰基，O-甲硅烷基，ON-亚氨基，OP-（膦基，膦酰基，硫代膦酰基，硒膦酰基）基团，并使其与含有羟基的化合物缩合反应或在亲电试剂存在下保护的羟基，然后脱保护和分离药学上纯的产物。本发明的目的是提供一种通过将含有羟基官能团（糖基受体，包括天然来源的糖苷配基，已知为活性药物成分的成分）的环状多官能化合物与非对映体纯的2-脱氧-4- 含有能够在糖苷化条件下交换的异头取代基的2-卤吡喃糖基衍生物，例如通过用亲电子试剂活化。该方法基本上简化了安环素的合成。本发明依赖于在含羟基的化合物如水，醇，酚，羧酸，硅烷醇，次膦酸，磷酸，硫代磷酸的存在下共卤化1,2-不饱和糖的区域和立体选择性反应，硒磷酸，然后用合成所需的合适的C-2碳配置分离产物。由于立体异构体的分离在获得糖基供体形式的相对便宜的中间体的阶段进行，本发明的方法显着降低了安环素制造的成本。本发明合成方法的其它优点在于减少抗生素制造过程的阶段数量和最终产品的产率增加。

7. 发明申请

WO2016135553A1 PROTOESCIGENIN DERIVATIVE, PROCESS OF ITS PREPARATION, USE OF SAID COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THAT COMPOUND 审中-公开
标题翻译：孕激素衍生物，其制备方法，化合物的使用和包含该化合物的药物组合物
公开(公告)号：WO2016135553A1
公开(公告)日：2016-09-01
申请号：PCT/IB2016/000187
申请日：2016-02-26
申请人： WARSZAWSKI UNIWERSYTET MEDYCZNY , INSTYTUT FARMACEUTYCZNY , KOZIAK, Katarzyna , BOJAKOWSKI, Krzysztof , KOWALEWSKA, Magdalena , MACIEJKO, Dorota , ZEGROCKA-STENDEL, Oliwia , GRABOWSKA, Iwona , GRYNKIEWICZ, Grzegorz , GRUZA, Mariusz Marek , JATCZAK, Kamil , FILIP, Katarzyna , CMOCH, Piotr , ŁASZCZ, Marta
发明人： KOZIAK, Katarzyna , BOJAKOWSKI, Krzysztof , KOWALEWSKA, Magdalena , MACIEJKO, Dorota , ZEGROCKA-STENDEL, Oliwia , GRABOWSKA, Iwona , GRYNKIEWICZ, Grzegorz , GRUZA, Mariusz Marek , JATCZAK, Kamil , FILIP, Katarzyna , CMOCH, Piotr , ŁASZCZ, Marta
IPC分类号： C07J63/00 , A61K31/58 , A61P9/14
CPC分类号： C07J63/008
摘要： The present invention relates to a protoescigenin derivative of formula (I) having pharmacological properties, process of its preparation, use of such compound as medicament especially for treating vascular disorders, as well as to a pharmaceutical composition comprising such compound.
摘要翻译：本发明涉及具有药理学性质的式（I）的原丝酵母衍生物，其制备方法，这种化合物，特别是用于治疗血管疾病的药物的用途，以及包含该化合物的药物组合物。

8. 发明申请

WO0056267A8 METHODS AND COMPOSITIONS FOR THE MANUFACTURE OF C-3' AND C-4' ANTHRACYCLINE ANTIBIOTICS 审中-公开
标题翻译：制备C-3'和C-4'蒽环类抗生素的方法和组合物
公开(公告)号：WO0056267A8
公开(公告)日：2001-05-17
申请号：PCT/IB0000527
申请日：2000-03-15
申请人： PRIEBE WALDEMAR , FOKT IZABELLA , PRZEWLOKA TERESA , KRAWCZYK MARTA , SKIBICKI PIOTR , GRYNKIEWICZ GRZEGORZ , PEREZ SOLER ROMAN
发明人： PRIEBE WALDEMAR , FOKT IZABELLA , PRZEWLOKA TERESA , KRAWCZYK MARTA , SKIBICKI PIOTR , GRYNKIEWICZ GRZEGORZ , PEREZ-SOLER ROMAN
IPC分类号： C07H15/252 , C07H1/00 , C07H15/24
CPC分类号： C07H15/252 , A61K31/704
摘要： The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3' of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4' of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.
摘要翻译：本发明公开了在糖部分的C-3'上具有改性的烷基 - 芳环取代的新的和新的取代的蒽环类，或在糖部分的C-4'被修饰或未修饰的烷基 - 芳环取代。它还公开了制备糖底物的新方法和制备蒽环类抗生素的方法。这些蒽环霉素类似物在体外对几种肿瘤细胞系显示高细胞毒性。

9. 发明申请

WO1994025478A1 16alpha,17alpha-ACETAL GLUCOCORTICOSTEROIDAL DERIVATIVES 审中-公开
标题翻译： 16α，17α-乙酰胆碱酯酶衍生物
公开(公告)号：WO1994025478A1
公开(公告)日：1994-11-10
申请号：PCT/PL1994000009
申请日：1994-04-28
申请人： INSTYTUT FARMACEUTYCZNY , INFARM SP. Z.O.O. , USZYCKA-HORAWA, Teresa , TRZPIL, Barbara , GRYNKIEWICZ, Grzegorz
发明人： INSTYTUT FARMACEUTYCZNY , INFARM SP. Z.O.O.
IPC分类号： C07J71/00
CPC分类号： C07J71/0031
摘要： New 16 alpha ,17 alpha -acetal glucocorticosteroid derivatives of general formula (I), wherein dotted line in the 1,2-position represents optional bond, R represents hydrogen atom or acetyl group and R1 and R2 represent independently hydrogen atom or fluorine atom, and their solvates with organic solvents, with antiinflammatory, antiallergic and immunosuppressive activities, the process for their preparation and pharmaceutical compositions containing them.
摘要翻译：新的16α，17α-通式（I）的α-丙醛糖皮质激素衍生物，其中1,2位上的虚线表示任选的键，R表示氢原子或乙酰基，R 1和R 2独立地表示氢原子或氟原子，和它们与有机溶剂的溶剂合物，具有抗炎，抗过敏和免疫抑制活性，其制备方法和含有它们的药物组合物。

10. 发明申请

WO2010095964A4 A METHOD FOR AMPHIPHILIC DRUG LOADING IN LIPOSOMES BY ION GRADIENT 审中-公开
公开(公告)号：WO2010095964A4
公开(公告)日：2010-08-26
申请号：PCT/PL2010/000014
申请日：2010-02-16
申请人： INSTYTUT FARMACEUTYCZNY , GUBERNATOR, Jerzy , KOZUBEK, Arkadiusz , GRYNKIEWICZ, Grzegorz , OBUKOWICZ, Janusz
发明人： GUBERNATOR, Jerzy , KOZUBEK, Arkadiusz , GRYNKIEWICZ, Grzegorz , OBUKOWICZ, Janusz
IPC分类号： A61K9/127 , A61K31/704
摘要： An active loading of amphophilic drugs, especially anthracycline antibiotics, in liposomes using conventional lipid compositions, is achieved by applying salts of polycarboxylic acids with mono- or divalent cations, preferably selected from sodium, potassium, calcium, magnesium or ammonium salt of ethylenediaminotetraacetic acid (EDTA) or ethyleneglycol-O-O'-bis(2-aminoethyl)-N,N,N',N'-tetraacetic acid (EGTA). The liposomal formulations obtained by the method of active loading of drugs to liposomes by EDTA or EGTA salts gradient are characterized by high loading efficiency, feature microcrystalline deposits of anthracyclines inside liposomes, which renders them stable and not susceptible to leakage. The liposomes are unilamellar and their size is close to 100 nanometers after drug loading.

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