公开(公告)号：US20140107051A1

公开(公告)日：2014-04-17

申请号：US14107055

申请日：2013-12-16

Applicant: INSTYTUT FARMACEUTYCZNY

Inventor： Grzegorz GRYNKIEWICZ ,  Grzegorz WEGRZYN ,  Barbara SZECHNER ,  Wieslaw SZEJA ,  Anna TYLKI-SZYMANSKA ,  Alicja WEGRZYN ,  Joanna JAKOBKIEWICZ-BANECKA ,  Sylwia BARANSKA ,  Barbara CZARTORYSKA ,  Ewa PIOTROWSKA

IPC: A61K31/353 ,  C07H17/07 ,  C07D407/12 ,  C07D311/34

CPC classification number: A61K31/353 ,  A61K31/352 ,  C07D311/34 ,  C07D407/12 ,  C07H17/07

Abstract: A pharmaceutical composition including a pharmaceutically acceptable excipient; and a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof, the natural isoflavone, the derivative thereof, or the pharmaceutically acceptable salt thereof being in a therapeutically effective amount for the treatment of mucopolysaccharidosis. A method of treatment of mucopolysaccharidosis, the method including administering to a patient in the need of such treatment—a therapeutically effective amount of a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof.

Abstract translation: 包含药学上可接受的赋形剂的药物组合物; 和式（I）的天然异黄酮，其衍生物或其药学上可接受的盐，其用于治疗粘多糖贮积病的治疗有效量的天然异黄酮，其衍生物或其药学上可接受的盐。 一种治疗粘多糖贮积症的方法，所述方法包括对需要这种治疗的患者施用治疗有效量的式（I）的天然异黄酮，其衍生物或其药学上可接受的盐。

公开(公告)号：US20180244714A1

公开(公告)日：2018-08-30

申请号：US15553301

申请日：2016-02-26

Applicant: Katarzyna KOZIAK ,  Krzysztof BOJAKOWSKI ,  Magdalena KOWALEWSKA ,  Dorota MACIEJKO ,  Oliwia ZEGROCKA-STENDEL ,  Iwona GRABOWSKA ,  Grzegorz GRYNKIEWICZ ,  Mariusz Marek GRUZA ,  Kamil JATCZAK ,  Katarzyna FILIP ,  Piotr CMOCH ,  Marta LASZCZ ,  Instytut Farmaceutyczny

Inventor： Katarzyna Koziak ,  Krzysztof Bojakowski ,  Magdalena Kowalewska ,  Dorota Maciejko ,  Oliwia Zegrocka-Stendel ,  Iwona Grabowska ,  Grzegorz Grynkiewicz ,  Mariusz Marek Gruza ,  Kamil Jatczak ,  Katarzyna Filip ,  Piotr Cmoch ,  Marta Laszcz

IPC: C07J63/00 ,  A61K31/58

CPC classification number: C07J63/008 ,  A61K31/58

Abstract: Described herein is compound including a protoescigenin derivative having pharmacological properties. Also described are a process of its preparation, and the use of such a compound as a medicament, especially for treating vascular disorders. A pharmaceutical composition comprising such compound is further described.

公开(公告)号：US09073813B2

公开(公告)日：2015-07-07

申请号：US13733855

申请日：2013-01-03

Applicant: INSTYTUT FARMACEUTYCZNY ,  WARSZAWSKI UNIWERSYTET MEDYCZNY

Inventor： Mariusz Gruza ,  Oliwia Zegrocka-Stendel ,  Tomasz Giller ,  Grzegorz Grynkiewicz ,  Marta Laszcz ,  Kamil Jatczak

IPC: C07C29/09 ,  C07C35/44 ,  C07C29/74 ,  C07C29/78 ,  C07C29/10 ,  C07C31/27 ,  C07J63/00

CPC classification number: C07C29/095 ,  C07C29/74 ,  C07C29/78 ,  C07C31/278 ,  C07C35/44 ,  C07J63/00 ,  C07J63/008

Abstract: A process for the preparation of protoescigenin by hydrolysis of escin isolated from Aesculus hippocastanum. The process includes the following steps: a two-step hydrolysis first under acidic and then basic conditions, enrichment of the crude mixture of sapogenins with protoescigenin, an isolation of the mixture of sapogenins in a solid form, and a purification of the obtained solid and isolation of high purity protoescigenin. The invention also relates to protoescigenin monohydrate in a crystalline form and the preparation thereof. Protoescigenin is a polyhydroxy aglycone, which can be used as a synthon in the chemical modifications of naturally occurring saponins.

Abstract translation: 一种通过水解从七叶树七叶皂苷中分离的七叶皂苷制备原丝酵母素的方法。 该方法包括以下步骤：首先在酸性和碱性条件下进行两步水解，将粗皂苷元粗制混合物与原丝酵母素进行富集，分离固体形式的皂角蛋白的混合物，以及所得固体和 隔离高纯度原丝酵母。 本发明还涉及结晶形式的原生精皮质素一水合物及其制备。 原花青素是多羟基苷元，可用作天然皂苷的化学修饰中的合成子。

公开(公告)号：US20210317060A1

公开(公告)日：2021-10-14

申请号：US17045477

申请日：2019-04-06

Applicant: INSTYTUT FARMACEUTYCZNY

Inventor： Katarzyna SIDORYK ,  Marek NAPIORKOWSKI ,  Agnieszka BURZYNSKA-PRAJZNER ,  Marcin CYBULSKI ,  Marek KUBISZEWSKI ,  Kamil JATCZAK ,  Lukasz JEDYNAK ,  Jerzy WINIARSKI ,  Dorota PIETRZKOWSKA ,  Konrad ZIELINSKI

IPC: C07C46/04

Abstract: Provided is an improved process of vitamin K2 derivatives preparation, represented by formula (I) wherein n is an integer from 3 to 13.

公开(公告)号：US20150031898A1

公开(公告)日：2015-01-29

申请号：US14383543

申请日：2013-03-08

Applicant: INSTYTUT FARMACEUTYCZNY

Inventor： Iwona Dams ,  Andrzej Kutner ,  Michal Chodynski ,  Malgorzata Krupa ,  Anita Pietraszek ,  Marta Zezula ,  Piotr Cmoch ,  Monika Kosinska

IPC: C07C405/00 ,  C07F7/08

CPC classification number: C07C405/0016 ,  C07C405/00 ,  C07C405/0041 ,  C07C2601/08 ,  C07D493/08 ,  C07F7/081 ,  C07F7/083 ,  C07F7/1804

Abstract: A convergent synthesis of the prostaglandin F2α 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.

Abstract translation: 使用具有对映异构体纯的醛ω-链合成子的结构先进的苯基砜的朱莉娅 - 柠檬精油来开发前列腺素F2α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。

公开(公告)号：US20130190538A1

公开(公告)日：2013-07-25

申请号：US13733855

申请日：2013-01-03

Applicant: INSTYTUT FARMACEUTYCZNY ,  WARSZAWSKI UNIWERSYTET MEDYCZNY

Inventor： Mariusz GRUZA ,  Oliwia ZEGROCKA-STENDEL ,  Tomasz GILLER ,  Grzegorz GRYNKIEWICZ ,  Marta LASZCZ ,  Kamil JATCZAK

IPC: C07C29/09 ,  C07C35/44

CPC classification number: C07C29/095 ,  C07C29/74 ,  C07C29/78 ,  C07C31/278 ,  C07C35/44 ,  C07J63/00 ,  C07J63/008

Abstract: A process for the preparation of protoescigenin by hydrolysis of escin isolated from Aesculus hippocastanum. The process includes the following steps: a two-step hydrolysis first under acidic and then basic conditions, enrichment of the crude mixture of sapogenins with protoescigenin, an isolation of the mixture of sapogenins in a solid form, and a purification of the obtained solid and isolation of high purity protoescigenin. The invention also relates to protoescigenin monohydrate in a crystalline form and the preparation thereof. Protoescigenin is a polyhydroxy aglycone, which can be used as a synthon in the chemical modifications of naturally occurring saponins.

Abstract translation: 一种通过水解从七叶树七叶皂苷中分离的七叶皂苷制备原丝酵母素的方法。 该方法包括以下步骤：首先在酸性和碱性条件下进行两步水解，将粗皂苷元粗制混合物与原丝酵母素进行富集，分离固体形式的皂角蛋白的混合物，以及所得固体和 隔离高纯度原丝酵母。 本发明还涉及结晶形式的原生精皮质素一水合物及其制备方法。 原花青素是多羟基苷元，可用作天然皂苷的化学修饰中的合成子。