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1. 发明申请

WO1995019963A1 NEW PHARMACOTHERAPEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：新药物活性化合物
公开(公告)号：WO1995019963A1
公开(公告)日：1995-07-27
申请号：PCT/NL1995000031
申请日：1995-01-23
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , KUTNER, Andrzej , ZHAO, Hong , FITAK, Hanna , CHODYN'SKI, Michael , HALKES, Sebastianus, J. , WILSON, Stephen, R. , VAN DEL VELDE, Jan-Paul
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： C07C403/08
CPC分类号： C07C403/08 , C07B2200/07 , C07C45/30 , C07C401/00 , C07C2601/14 , C07C2601/16 , C07F9/532 , C07C47/19
摘要： The invention relates to a compound of general formula (I), wherein R1, R2, R4, R5 and R6 are each individually hydrogen atoms or methyl groups; R3 represents a methyl group or a methylene group; R7 and R8 are each individually straight or branched alkyl groups having 1 to 4 carbon atoms or cycloalkyl groups having 3 to 6 carbon atoms; Z is a hydrogen atom or a hydroxy group; n is an integer from 0 to 3; and the (a) bonds represent single or double carbon - carbon bonds; with the provisos: (1) that no cumulated double bonds are present in the molecule; (2) that either R3-C10, C5-C6 and C7-C8 or C10-C5, C6-C7 and C8-C9 form double bonds, with which optionally present additional double bonds are conjugated; and (3) that R3 represents a methyl group if R3-C10 is a single bond, and a methylene group if R3-C10 is a double bond. The invention also relates to a method of preparing this compound and to its use for the treament and/or prevention of certain disorders and diseases.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2，R 4，R 5和R 6各自为氢原子或甲基; R3表示甲基或亚甲基; R 7和R 8各自为具有1至4个碳原子的直链或支链烷基或具有3至6个碳原子的环烷基; Z是氢原子或羟基; n为0〜3的整数。（a）债券代表单一或双重碳 - 碳键; 条件是：（1）分子中不存在累积双键; （2）R3-C10，C5-C6和C7-C8或C10-C5，C6-C7和C8-C9形成双键，任选地存在额外的双键被共轭; 和（3）如果R3-C10是单键，则R3表示甲基，如果R3-C10是双键，则表示亚甲基。本发明还涉及一种制备该化合物的方法及其用于治疗和/或预防某些疾病和疾病的用途。

2. 发明申请

WO2009008754A2 PROCESS FOR THE PREPARATION OF CALCIPOTRIOL 审中-公开
标题翻译：制备钙三醇的方法
公开(公告)号：WO2009008754A2
公开(公告)日：2009-01-15
申请号：PCT/PL2008/000051
申请日：2008-07-11
申请人： INSTYTUT FARMACEUTYCZNY , KUTNER, Andrzej , CHODYNSKI, Michal , LESZCZYNSKA, Kinga , SZELEJEWSKI, Wieslaw , FITAK, Hanna
发明人： KUTNER, Andrzej , CHODYNSKI, Michal , LESZCZYNSKA, Kinga , SZELEJEWSKI, Wieslaw , FITAK, Hanna
IPC分类号： C07C401/00 , C07C35/21
CPC分类号： C07C401/00 , C07C2601/02 , Y02P20/55
摘要： Process comprising the step of reacting a C-22 phenylsulphonyl derivative of cholecalciferol of Formula (2), wherein R 1 and R 2 are the same or different and represent hydroxyl protecting groups, with a silyl derivative of alfa-hydroxy aldehyde of Formula (3), wherein R 3 represents silyl group of formula Si(R 4 ) (R 5 )(R 6 ), where R 4 -R 6 are the same or different and represent C 1-6 alkyl or phenyl groups, in the presence of a strong organic base in aprotic solvent, followed by a reductive desulfonation of the diastereomeric mixture of alfa- hydroxysulfones with sodium amalgam, removing the hydroxyl protecting groups, and purification, leads to calcipotriol containing less than 0,3% of (22Z)-isomer and free of mercury traces.
摘要翻译：（2）的胆钙化醇的C-22苯基磺酰基衍生物（其中R 1和R 2是与式（3）的α-羟基醛的甲硅烷基衍生物反应，其中R 3表示式Si的甲硅烷基（R 4））（R 5 5）（R 6），其中R 4 -R 6是相同或不同的并且代表C 1-6烷基或苯基，在强有机碱的存在下，在非质子溶剂中，然后用钠汞齐将α-羟基砜的非对映异构体混合物还原脱磺化，除去羟基保护基组和纯化，导致含有小于0.3％（22Z） - 异构体并且没有汞痕迹的卡泊三醇。

3. 发明申请

WO2003087048A3 PREPARATION OF 24 ALKYL ANALOGS OF CHOLECALCIFEROL AND NON-RACEMIC COMPOUNDS 审中-公开
公开(公告)号：WO2003087048A3
公开(公告)日：2003-10-23
申请号：PCT/PL2003/000037
申请日：2003-04-10
申请人： INSTYTUT FARMACEUTYCZNY , KUTNER, Andrzej , MARTYNOW, Jacek , CHODYNSKI, Michal , SZELEJEWSKI, Wieslaw , FITAK, Hanna , KRUPA, Malgorzata
发明人： KUTNER, Andrzej , MARTYNOW, Jacek , CHODYNSKI, Michal , SZELEJEWSKI, Wieslaw , FITAK, Hanna , KRUPA, Malgorzata
IPC分类号： C07C401/00
摘要： Disclosed is a process for the preparation of 24-alkyl analogs of cholecalcyferol of Formula (1) having a (5E) or (5Z) configuration, wherein X represents a hydrogen atom, a hydroxy group or an OR 1 group, wherein R 1 , R 2 and R 3 may be the same or different and represent groups suitable for hydroxyl protection, and R 4 is a C 1-6 alkyl chain or a C 1-6 alkyl groups, especially for calcipotriol. The invention also provides new non-racemic compounds being valuable synthones for the synthesis of pharmacologically active substances.

4. 发明申请

WO2006071129A1 PROCESS FOR PREPARATION OF A PHARMACEUTICAL GRADE CALCIPOTRIOL ANHYDROUS 审中-公开
标题翻译：制备药物级别的非卡那霉素的方法
公开(公告)号：WO2006071129A1
公开(公告)日：2006-07-06
申请号：PCT/PL2005/000087
申请日：2005-12-29
申请人： INSTYTUT FARMACEUTYCZNY , KUTNER, Andrzej , CHODYNSKI, Michal , RYZNAR, Teresa , FITAK, Hanna , WINIARSKI, Jerzy , GORECKI, Bartlomiej , BURZYNSKA, Agnieszka , SZELEJEWSKI, Wieslaw
发明人： KUTNER, Andrzej , CHODYNSKI, Michal , RYZNAR, Teresa , FITAK, Hanna , WINIARSKI, Jerzy , GORECKI, Bartlomiej , BURZYNSKA, Agnieszka , SZELEJEWSKI, Wieslaw
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： A process for the preparation of a pharmaceutical grade calcipotriol anhydrous, wherein a crude calcipotriol is dissolved in one or more solvents, of which at least one forms azeotropic system with water, and then: a) in the case the water and impurities content in the substance exceeds the admissible level, solvents are azeotropically evaporated under reduced pressure, resulting in a clear anhydrous oil , or (b) in the case the water content in the substance does not exceed the admissible level, the solution is allowed to crystallize the product, (c) product obtained in step (a) or (b) is crystallized at least once from anhydrous solvent or mixture of anhydrous solvents.
摘要翻译：一种制备药物级卡泊三醇无水物的方法，其中将粗卡西醇三醇溶解在一种或多种溶剂中，其中至少一种与水形成共沸系统，然后：a）在水和杂质含量在物质超过允许的水平，溶剂在减压下共沸蒸发，导致澄清的无水油，或（b）在物质中的水含量不超过允许水平的情况下，溶液使产物结晶，（c）步骤（a）或（b）中获得的产物至少一次由无水溶剂或无水溶剂的混合物结晶。

5. 发明申请

WO2004031204A2 PROCESS AND INTERMEDIATES TO PREPARE l7ß-hydroxy-7alpha-methyl-19-nor-17alpha-pregn-5(10)-en-20-yn-3-one 审中-公开
标题翻译：制备17β-羟基-7α-甲基-19-去甲-17α-孕-5（10）-en-20-炔-3-酮的方法和中间体
公开(公告)号：WO2004031204A2
公开(公告)日：2004-04-15
申请号：PCT/PL0300099
申请日：2003-10-01
申请人： PRZED FARMACEUTYCZNE ANPHARM S , MARTYNOW JACEK , KUTNER ANDRZEJ , SZELEJEWSKI WIESLAW , WOJCIECHOWSKA WANDA , FITAK HANNA
发明人： MARTYNOW JACEK , KUTNER ANDRZEJ , SZELEJEWSKI WIESLAW , WOJCIECHOWSKA WANDA , FITAK HANNA
IPC分类号： C07J21/00 , C07J75/00 , C07J
CPC分类号： C07J75/00 , C07J21/00
摘要： The present invention is a process for the preparation of l7ß-hydroxy-7alpha-methyl-19-nor-17alpha-pregn-5(10)-en-20-yn-3-one (17alpha-ethynyl-l7ß-hydroxy-7alpha-methyl-5(10)-estren-3-one, tibolone) of formula 1, which comprises hydrolysis of 17alpha-ethynyl-l7ß-hydroxy-7alpha-methyl-5(10)-estrene 3,3-cyclic ketals of formula 2, where groups R1, R2, R3 and R4 are hydrogen atoms or alkyl groups, or R1 and R3, taken together with the carbon atoms within the dioxolane ring to which they are attached, form an alicyclic ring fused to the dioxolane ring, with R2 and R4 being hydrogen atoms, or R1 and R3 together with the carbon atoms to which they are attached form an aromatic ring fused to the dioxolane ring, where R2 and R4, taken together, form a chemical bond within said aromatic ring. In addition, the present invention includes an intermediate, compound of formula 2 and two processes to prepare 17alpha-ethynyl-17(3-hydroxy-7alpha-methyl-5(10)-estrene 3,3-cyclic ketals of formula 2: (a) by contacting 17alpha-ethynyl-l7ßhydroxy-7alpha-methyl-4-estren-3-one with vicinal diols in the presence of a protic acid, and (b) by contacting 7alpha-methyl-5(10)-estrene-17-one 3,3-cyclic ketals of formula 4, where R1-R4 are defined as above, with metal acetylides, in inert solvents.
摘要翻译：本发明是制备17β-羟基-7α-甲基-19-去甲-17α-孕-5（10）-en-20-炔-3-酮（17α-乙炔基-17β-羟基-7α - 甲基-5（10） - 雌酚-3-酮，替勃龙酮），其包括水解17α-乙炔基-17β-羟基-7α-甲基-5（10） - 雌甾3,3-环缩酮的式 2，其中基团R 1，R 2，R 3和R 4是氢原子或烷基，或者R 1和R 3与它们所连接的二氧戊环内的碳原子一起形成稠合到二氧戊环的脂环， R2和R4是氢原子，或R1和R3与它们所连接的碳原子一起形成稠合到二氧戊环的芳香环，其中R 2和R 4一起在所述芳环中形成化学键。此外，本发明包括中间体式2的化合物和两种制备式2的17α-乙炔基-17（3-羟基-7α-甲基-5（10） - 雌甾3,3-环缩酮的方法：（ a）通过在质子酸存在下将17α-乙炔基-17β-羟基-7α-甲基-4-雌酮-3-酮与邻立二醇接触，和（b）通过使7α-甲基-5（10） - 雌二醇-17 在惰性溶剂中，使用式4的3,3-环缩酮，其中R1-R4如上定义，与金属乙炔化物反应。

6. 发明申请

WO03087048A2 PREPARATION OF 24 ALKYL ANALOGS OF CHOLECALCIFEROL AND NON-RACEMIC COMPOUNDS 审中-公开
标题翻译：选择性和不利于化合物的24种烷基胺类似物的制备
公开(公告)号：WO03087048A2
公开(公告)日：2003-10-23
申请号：PCT/PL0300037
申请日：2003-04-10
申请人： INST FARMACEUTYCZNY , KUTNER ANDRZEJ , MARTYNOW JACEK , CHODYNSKI MICHAL , SZELEJEWSKI WIESLAW , FITAK HANNA , KRUPA MALGORZATA
发明人： KUTNER ANDRZEJ , MARTYNOW JACEK , CHODYNSKI MICHAL , SZELEJEWSKI WIESLAW , FITAK HANNA , KRUPA MALGORZATA
IPC分类号： C07C31/133 , C07C309/73 , C07C401/00 , C07F7/18 , C07D277/74 , C07D277/76
CPC分类号： C07C31/1333 , C07C309/73 , C07C401/00 , C07C2601/02 , C07F7/1892
摘要： Disclosed is a process for the preparation of 24 -alkyl analogs of cholecalcyferol of Formula 1 having a (5E) or (5Z) configuration, wherein X represents a hydrogen atom, a hydroxy group or an OR1 group, wherein R1, R2 and R3 may be the same or different and represent groups suitable for hydroxyl protection, and R4 is a C1-6 alkyl chain or a C1-6 alkyl groups, especially for calcipotriol. The invention also provides new non-racemic compounds being valuable synthones for the synthesis of pharmacologically active substances.
摘要翻译：公开了制备具有（5E）或（5Z）构型的式1的胆碱酯的24-烷基类似物的方法，其中X表示氢原子，羟基或OR 1基团，其中R 1，R 2和R 3可以相同或不同，代表适用于羟基保护的基团，R4是C1-6烷基链或C1-6烷基，特别是卡泊三醇。本发明还提供了新的非外消旋化合物作为用于合成药理学活性物质的有价值的合成物。

7. 发明申请

WO2009008754A3 PROCESS FOR THE PREPARATION OF CALCIPOTRIOL 审中-公开
标题翻译：制备钙可乐的方法
公开(公告)号：WO2009008754A3
公开(公告)日：2009-02-26
申请号：PCT/PL2008000051
申请日：2008-07-11
申请人： INST FARMACEUTYCZNY , KUTNER ANDRZEJ , CHODYNSKI MICHAL , LESZCZYNSKA KINGA , SZELEJEWSKI WIESLAW , FITAK HANNA
发明人： KUTNER ANDRZEJ , CHODYNSKI MICHAL , LESZCZYNSKA KINGA , SZELEJEWSKI WIESLAW , FITAK HANNA
IPC分类号： C07C401/00 , C07C35/21
CPC分类号： C07C401/00 , C07C2601/02 , Y02P20/55
摘要： Process comprising the step of reacting a C-22 phenylsulphonyl derivative of cholecalciferol of Formula (2), wherein R1 and R2 are the same or different and represent hydroxyl protecting groups, with a silyl derivative of alfa-hydroxy aldehyde of Formula (3), wherein R3 represents silyl group of formula Si(R4) (R5)(R6), where R4-R6 are the same or different and represent C1-6 alkyl or phenyl groups, in the presence of a strong organic base in aprotic solvent, followed by a reductive desulfonation of the diastereomeric mixture of alfa- hydroxysulfones with sodium amalgam, removing the hydroxyl protecting groups, and purification, leads to calcipotriol containing less than 0,3% of (22Z)-isomer and free of mercury traces.
摘要翻译：方法包括使式（2）的胆钙化甾醇的C-22苯基磺酰基衍生物与式（3）的α-羟基醛的甲硅烷基衍生物反应，其中R 1和R 2相同或不同并代表羟基保护基，其中R 3表示在非质子传递溶剂中的强有机碱存在下，其中R 4 -R 6相同或不同并且表示C 1-6烷基或苯基的式Si（R 4）（R 5）（R 6）的甲硅烷基，随后通过将α-羟基砜与汞齐汞合物的非对映异构体混合物还原脱磺化，除去羟基保护基团并进行纯化，得到含有少于0.3％（22Z） - 异构体并且没有汞痕迹的卡泊三醇。

8. 发明申请

WO2006071129B1 PROCESS FOR PREPARATION OF A PHARMACEUTICAL GRADE CALCIPOTRIOL ANHYDROUS 审中-公开
标题翻译：制备药物级无水三氯蔗糖的方法
公开(公告)号：WO2006071129B1
公开(公告)日：2006-08-31
申请号：PCT/PL2005000087
申请日：2005-12-29
申请人： INST FARMACEUTYCZNY , KUTNER ANDRZEJ , CHODYNSKI MICHAL , RYZNAR TERESA , FITAK HANNA , WINIARSKI JERZY , GORECKI BARTLOMIEJ , BURZYNSKA AGNIESZKA , SZELEJEWSKI WIESLAW
发明人： KUTNER ANDRZEJ , CHODYNSKI MICHAL , RYZNAR TERESA , FITAK HANNA , WINIARSKI JERZY , GORECKI BARTLOMIEJ , BURZYNSKA AGNIESZKA , SZELEJEWSKI WIESLAW
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： A process for the preparation of a pharmaceutical grade calcipotriol anhydrous, wherein a crude calcipotriol is dissolved in one or more solvents, of which at least one forms azeotropic system with water, and then: a) in the case the water and impurities content in the substance exceeds the admissible level, solvents are azeotropically evaporated under reduced pressure, resulting in a clear anhydrous oil , or (b) in the case the water content in the substance does not exceed the admissible level, the solution is allowed to crystallize the product, (c) product obtained in step (a) or (b) is crystallized at least once from anhydrous solvent or mixture of anhydrous solvents.
摘要翻译：一种制备无水药物级卡泊三醇的方法，其中将粗制卡泊三醇溶解在一种或多种溶剂中，其中至少一种溶剂与水形成共沸体系，然后：a）如果水和杂质含量在物质超过允许的水平，溶剂在减压下共沸蒸发，产生澄清的无水油，或（b）在物质中的水含量不超过允许水平的情况下，使溶液结晶产物，（c）步骤（a）或（b）中得到的产物从无水溶剂或无水溶剂混合物中结晶至少一次。

9. 发明申请

WO2005110979A3 PROCESS AND INTERMEDIATES TO PREPARE THE SULPHONYL DERIVATIVES OF CHOLECALCIFEROL 审中-公开
标题翻译：制备CHOLECALCIFEROL的磺酰衍生物的方法和中间体
公开(公告)号：WO2005110979A3
公开(公告)日：2006-03-16
申请号：PCT/PL2005000030
申请日：2005-05-13
申请人： INST FARMACEUTYCZNY , CHODYNSKI MICHAL , KRUPA MALGORZATA , FITAK HANNA , WINIARSKI JERZY , RYZNAR TERESA , GORECKI BARTLOMIEJ , SZELEJEWSKI WIESLAW , KUTNER ANDRZEJ
发明人： CHODYNSKI MICHAL , KRUPA MALGORZATA , FITAK HANNA , WINIARSKI JERZY , RYZNAR TERESA , GORECKI BARTLOMIEJ , SZELEJEWSKI WIESLAW , KUTNER ANDRZEJ
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Preparation of sulphonyl derivatives of cholecalciferol of Formula (I), wherein R 1 is protective group, preferably t-butyl(dimethyl)silyl, where R 2 is heterocyclic group, such as 2-thiazolyl, 2-benzothiazolyl, 1-phenyl-lH-tetrazo-5-yl, 2-pyridyl, 2-pyrimidynyl, 1-isochinolinyl, 1-methyl-2-imidazyl, 4-alkyl-1,2,4-triazo-3-yl, comprising the conversion of the hydroxyl derivative of cholecalciferol into the corresponding sulfide followed by its oxidation to the respective sulphone characterized by the use of hydroxyl derivative of cholecalciferol as a starting material, which triene system is protected as Diels-Alder adduct, and in particular as an adduct with sulfur dioxide of the formula 2a. Novel are derivatives of formula 3a and 4, isolated in the process provided in the invention.
摘要翻译：式（I）的胆钙化甾醇的磺酰基衍生物的制备，其中R 1是保护基，优选叔丁基（二甲基）甲硅烷基，其中R 2是杂环基， 2-噻唑基，2-苯并噻唑基，1-苯基-1H-双偶氮-5-基，2-吡啶基，2-嘧啶基，1-异链烷基，1-甲基-2-咪唑基，4-烷基-1,2,4- 包括将胆钙化甾醇的羟基衍生物转化为相应的硫化物，随后氧化为相应的砜，其特征在于使用胆钙化醇的羟基衍生物作为起始原料，该三烯体系被保护为Diels- Alder加合物，特别是与式2a的二氧化硫的加合物。新颖的是在本发明提供的方法中分离的式3a和4的衍生物。

10. 发明申请

WO2005110979A2 PROCESS AND INTERMEDIATES TO PREPARE THE SULPHONYL DERIVATIVES OF CHOLECALCIFEROL 审中-公开
标题翻译：制备CHOLECALCIFEROL的磺酰衍生物的方法和中间体
公开(公告)号：WO2005110979A2
公开(公告)日：2005-11-24
申请号：PCT/PL2005/000030
申请日：2005-05-13
申请人： INSTYTUT FARMACEUTYCZNY , CHODYNSKI, Michal , KRUPA, Malgorzata , FITAK, Hanna , WINIARSKI, Jerzy , RYZNAR, Teresa , GORECKI, Bartlomiej , SZELEJEWSKI, Wieslaw , KUTNER, Andrzej
发明人： CHODYNSKI, Michal , KRUPA, Malgorzata , FITAK, Hanna , WINIARSKI, Jerzy , RYZNAR, Teresa , GORECKI, Bartlomiej , SZELEJEWSKI, Wieslaw , KUTNER, Andrzej
IPC分类号： C07C309/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Preparation of sulphonyl derivatives of cholecalciferol of Formula (I), wherein R 1 is protective group, preferably t-butyl(dimethyl)silyl, where R 2 is heterocyclic group, such as 2-thiazolyl, 2-benzothiazolyl, 1-phenyl-lH-tetrazo-5-yl, 2-pyridyl, 2-pyrimidynyl, 1-isochinolinyl, 1-methyl-2-imidazyl, 4-alkyl-1,2,4-triazo-3-yl, comprising the conversion of the hydroxyl derivative of cholecalciferol into the corresponding sulfide followed by its oxidation to the respective sulphone characterized by the use of hydroxyl derivative of cholecalciferol as a starting material, which triene system is protected as Diels-Alder adduct, and in particular as an adduct with sulfur dioxide of the formula 2a. Novel are derivatives of formula 3a and 4, isolated in the process provided in the invention.
摘要翻译：制备式（I）的胆钙化甾醇的磺酰基衍生物，其中R 1是保护基，优选叔丁基（二甲基）甲硅烷基，其中R 2是杂环基，例如2-噻唑基，2-苯并噻唑基，1-苯基-1H-双 5-吡啶基，2-嘧啶基，1-异辛基，1-甲基-2-咪唑基，4-烷基-1,2,4-三唑-3-基，其包括转化胆钙化醇的羟基衍生物进入相应的硫化物，然后氧化成相应的砜，其特征在于使用胆钙化醇的羟基衍生物作为起始原料，该三烯体系被保护为els-阿尔德加合物，特别是作为与式2a的二氧化硫的加合物。新颖的是在本发明提供的方法中分离的式3a和4的衍生物。

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