公开(公告)号：EP1891005A2

公开(公告)日：2008-02-27

申请号：EP06733186.8

申请日：2006-04-18

申请人： INSTYTUT FARMACEUTYCZNY

发明人： MARTYNOW, Jacek ,  JOZWIK, Julita ,  SZELEJEWSKI, Wieslaw ,  ACHMATOWICZ, Osman ,  KUTNER, Andrzej ,  WISNIEWSKI, Krzysztof ,  WINIARSKI, Jerzy ,  ZEGROCKA-STENDEL, Oliwia ,  GOLEBIEWSKI, Piotr

IPC分类号： C07C405/00 ,  C07C317/18 ,  C07D493/08 ,  C07F7/18 ,  C07D327/10 ,  C07C33/46 ,  C07D303/04

CPC分类号： C07C309/73 ,  C07B2200/07 ,  C07C405/00 ,  C07C405/0016 ,  C07C405/0033 ,  C07C2601/08 ,  C07D303/04 ,  C07D307/935 ,  C07D317/12 ,  C07D317/26 ,  C07D327/10 ,  C07D493/08 ,  C07D493/18 ,  C07F7/1856

摘要： Invention relates to the process for preparation of 13,14-dihydro-PGF2α derivatives of R or S configuration at carbon atom in omega chain substituted by hydroxyl, represented by formula (I), wherein the meaning of substituents is defined in the description. Compounds (I) are valuable biologically active substances or intermediates thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2α, ie. latanoprost.

摘要翻译： 本发明涉及在通式（I）表示的碳15处制备R 1或S 3构型的13,14-二氢-PGF2α衍生物的方法，其中取代基的同一性在说明书中定义。 式（I）的化合物在其制备中是有价值的生物活性物质或中间体。 本发明特别涉及制备13,14-二氢-15（R）-17-取代-18,19,20-三硝基-PGF2α（即拉坦前列素）的方法。

公开(公告)号：EP1756048A2

公开(公告)日：2007-02-28

申请号：EP05740619.1

申请日：2005-05-13

申请人： INSTYTUT FARMACEUTYCZNY

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 R1 is protective group, preferably t-butyl(dimethyl)silyl, where R2 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.

公开(公告)号：EP3774707A1

公开(公告)日：2021-02-17

申请号：EP19725426.1

申请日：2019-04-06

申请人： INSTYTUT FARMACEUTYCZNY

发明人： SIDORYK, Katarzyna ,  NAPIÓRKOWSKI, Marek ,  BURZY SKA-PRAJZNER, Agnieszka ,  CYBULSKI, Marcin ,  KUBISZEWSKI, Marek ,  JATCZAK, Kamil ,  JEDYNAK, ukasz ,  WINIARSKI, Jerzy ,  PIETRZKOWSKA, Dorota ,  ZIELI SKI, Konrad

IPC分类号： C07C41/18 ,  C07C315/04 ,  C07C317/14 ,  C07C317/18 ,  C07C45/27

公开(公告)号：EP1838666A1

公开(公告)日：2007-10-03

申请号：EP05821873.6

申请日：2005-12-29

申请人： INSTYTUT FARMACEUTYCZNY

发明人： KUNTER, 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.