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公开(公告)号：US10981884B2
公开(公告)日：2021-04-20
申请号：US16087388
申请日：2017-03-21
发明人： Irén Hortobágyi , István Lászlófi , Zsuzsanna Kardos , József Molnár , László Takács , Róbertné Tormási
IPC分类号： C07D307/937 , A61K9/19
摘要： The invention provides a stable epoprostenol sodium and a process for the preparation this pharmaceutically active ingredient.
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公开(公告)号：US11958798B2
公开(公告)日：2024-04-16
申请号：US17973129
申请日：2022-10-25
发明人： Imre Rozsumberszki , Zsuzsanna Kardos , Irén Hortobágyi , Tibor Szabó , Csaba Váradi , Tamás Bán
IPC分类号： C07C51/09 , C07C67/31 , C07C59/46 , C07C69/608
CPC分类号： C07C51/09 , C07C67/31 , C07B2200/13 , C07C59/46 , C07C69/608 , C07C2602/22
摘要： The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
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公开(公告)号：US11724979B2
公开(公告)日：2023-08-15
申请号：US17377125
申请日：2021-07-15
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
CPC分类号： C07C51/347 , C07C13/547 , C07C35/37 , C07C41/26 , C07C41/30 , C07C41/48 , C07C43/315 , C07C45/30 , C07C45/305 , C07C45/65 , C07C51/09 , C07C51/412 , C07C59/72 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C2603/14 , C07C45/305 , C07C49/84 , C07C45/30 , C07C49/84 , C07C45/65 , C07C49/755 , C07C51/09 , C07C59/70 , C07C41/48 , C07C43/315 , C07C67/14 , C07C69/76 , C07C67/29 , C07C69/76 , C07C67/293 , C07C69/76 , C07C51/412 , C07C59/70
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US11535580B2
公开(公告)日：2022-12-27
申请号：US17048053
申请日：2019-04-16
发明人： Imre Rozsumberszki , Zsuzsanna Kardos , Irén Hortobágyi , Tibor Szabó , Csaba Váradi , Tamás Bán
IPC分类号： C07C51/09 , C07C67/31 , C07C59/46 , C07C69/608
摘要： The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
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公开(公告)号：US10322990B2
公开(公告)日：2019-06-18
申请号：US15518096
申请日：2015-09-28
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US11008594B2
公开(公告)日：2021-05-18
申请号：US16087402
申请日：2017-03-21
发明人： Irén Hortobágyi , István Lászlófi , Zsuzsanna Kardos , József Molnár , László Takács , Tamás Bán
摘要： The invention provides a new enzimatic process for the preparation of chiral carboxylic acids, their salts and acid derivatives of the general formula (I) by enzymatic hydrolysis of racemic carboxylic acid ester of the general formula (II) and optionally subsequent esterification or acylation.
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公开(公告)号：US10421737B2
公开(公告)日：2019-09-24
申请号：US16091019
申请日：2017-03-30
发明人： Irén Hortobágyi , István Lászlófi , Zsuzsanna Kardos , József Molnár , László Takács , Tamás Bán
IPC分类号： C07D307/93
摘要： The invention provides a new process for the preparation of optically active Beraprost of formula (I) starting from racemic Beraprost alkyl ester through hydrolysis, enantiomer esterification, preparation of diacyl-Beraprost ester diastereomers and their separation and hydrolysis.
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公开(公告)号：US09212125B2
公开(公告)日：2015-12-15
申请号：US14367317
申请日：2012-12-10
发明人： Zsuzsanna Kardos , Tibor Kiss , István Lászlofi , Irén Hortobágyi , Zoltán Bischof , Ádám Bódis , Gábor Havasi
IPC分类号： C07D407/00 , C07C67/333 , C07D307/935 , C07C405/00 , C07D307/937
CPC分类号： C07D307/935 , C07C67/333 , C07C405/00 , C07C2601/08 , C07D307/937 , Y02P20/55
摘要： The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereoselectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
摘要翻译： 本发明涉及一种制备式（I）的曲伏前列素的方法，其包括立体选择性地还原式（II）化合物，如果需要结晶，所得到的式（III）化合物，所述内酯基团 将式（Ⅳ）化合物还原，由此得到的式（Ⅳ）化合物的对 - 苯基 - 苯甲酰基保护基被除去，如果结晶后所需的式（Ⅴ）三元醇是 维t希反应成式（Ⅵ）的酸，然后酯化。
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公开(公告)号：US20140343299A1
公开(公告)日：2014-11-20
申请号：US14367317
申请日：2012-12-10
发明人： Zsuzsanna Kardos , Tibor Kiss , István Lászlofi , Irén Hortobágyi , Zoltán Bischof , Ádám Bódis , Gábor Havasi
IPC分类号： C07C67/333 , C07D307/937
CPC分类号： C07D307/935 , C07C67/333 , C07C405/00 , C07C2601/08 , C07D307/937 , Y02P20/55
摘要： The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereo selectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
摘要翻译： 本发明涉及一种制备式（I）的曲伏前列素的方法，其包括式（II）化合物立体选择性还原，所得式（III）化合物如果需要结晶，则内酯基 的式（Ⅳ）化合物被还原，得到如此得到的式（Ⅳ）化合物的对 - 苯基 - 苯甲酰基保护基，如果需要，结晶后所得到的式（Ⅴ）三醇被转化 通过Wittig反应进入式（VI）的酸，然后将其酯化。
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公开(公告)号：US11319274B2
公开(公告)日：2022-05-03
申请号：US16978391
申请日：2019-03-07
发明人： Irén Hortobágyi , István Lászlófi , Zoltán Varga , Imre Juhász , Imola Ritz , Zsuzsanna Kardos
IPC分类号： C07C51/43 , C07C59/72 , C07C215/10
摘要： The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
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