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1. 发明申请

WO2020008320A8 ANTI-XYLAN SULFATE POLYCLONAL ANTISERUM AND USE THEREOF IN ELISA METHODS 审中-公开
公开(公告)号：WO2020008320A8
公开(公告)日：2020-01-09
申请号：PCT/IB2019/055557
申请日：2019-07-01
申请人： CHEMI SPA
发明人： LEONI, Flavio , PORRO, Giuliana
IPC分类号： G01N33/53
摘要： The object of the present invention is an anti-xylan sulfate antiserum having an antibody titre of between 1/10000 and 1/15000, and obtainable using a specific immunization method, and use thereof in one or more ELISA methods for determining xylan sulfate levels in biological fluids.

2. 发明申请

WO2020008320A1 TIANTI-XYLAN SULFATE POLYCLONAL ANTISERUM AND USE THEREOF IN ELISA METHODS 审中-公开
公开(公告)号：WO2020008320A1
公开(公告)日：2020-01-09
申请号：PCT/IB2019/055557
申请日：2019-07-01
申请人： CHEMI SPA
发明人： LEONI, Flavio , PORRO, Giuliana
IPC分类号： G01N33/53
摘要： The object of the present invention is an anti-xylan sulfate antiserum having an antibody titre of between 1/10000 and 1/15000, and obtainable using a specific immunization method, and use thereof in one or more ELISA methods for determining xylan sulfate levels in biological fluids.

3. 发明申请

WO2011154854A9 PROCESS FOR THE PREPARATION OF 2 -HYDROXY- 4 -PHENYL -3, 4 -DIHYDRO-2H-CHROMEN- 6 -YL -METHANOL AND (R) - FESO - DEACYL 审中-公开
标题翻译：制备2-羟基-4-苯基-3,4-二氢-2H-吡喃-6-基 - 乙醇和（R） - FESO-DEACYL的方法
公开(公告)号：WO2011154854A9
公开(公告)日：2013-01-31
申请号：PCT/IB2011051896
申请日：2011-04-29
申请人： CHEMI SPA , CIAMBECCHINI UMBERTO , TURCHETTA STEFANO , DE FERRA LORENZO , ZENONI MAURIZIO
发明人： CIAMBECCHINI UMBERTO , TURCHETTA STEFANO , DE FERRA LORENZO , ZENONI MAURIZIO
IPC分类号： C07D311/20 , C07C215/54 , C07C219/28
CPC分类号： C07D311/20 , C07C213/00 , C07C213/02 , C07C213/10 , C07C215/54
摘要： The present invention regards an improved and industrially advantageous process for the preparation of the 2-hyaroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called "feso chromenyl" and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called "(R)-feso deacyl", which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine furnarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate "(R)-feso deacyl", called form B.
摘要翻译：本发明涉及一种改进和工业上有利的制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇中间体的方法，也称为“feso chromenyl”和（R） -2- [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚，也称为“（R） - 非索酰基”，它们又用于合成西索罗定，特别是西索罗定。该方法利用在工业水平上无毒且易于管理的试剂，能够获得称为B型关键中间体“（R） - feso deacyl”的新型稳定和非吸湿结晶形式。

4. 发明申请

WO2010004597A1 ROCESS FOR THE PRODUCTION OF N-ACYL-PHOSPHATIDYL-ETANOLAMINE 审中-公开
标题翻译：用于生产N-乙酰基 - 苯胺基胺的方法
公开(公告)号：WO2010004597A1
公开(公告)日：2010-01-14
申请号：PCT/IT2008000460
申请日：2008-07-08
申请人： CHEMI SPA , DE FERRA LORENZO , ANIBALDI MAURO , AMMIRATI ETTORE
发明人： DE FERRA LORENZO , ANIBALDI MAURO , AMMIRATI ETTORE
IPC分类号： C07F9/10
CPC分类号： C07F9/106 , C07F9/10
摘要： The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C1O-C30, pure or mixed together, and X=OH or OM, where M= alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.
摘要翻译：该文献描述了以工业规模制备式（I）的N-酰基 - 磷酰基 - 乙醇胺的方法，其中R 1，R 2和R 3彼此独立地为饱和的单不饱和或多不饱和酰基C 1 -C 30，纯或混合在一起，X = OH或OM，其中M =碱金属或碱土金属，铵或烷基铵。所讨论的方法允许使用有限摩尔过量的试剂N-酰基 - 乙醇胺将合成或天然来源的卵磷脂转化为高纯度的式（I）的N-酰基 - 磷酰基 - 乙醇胺，其中酰基如通过在磷脂酶D存在下的磷脂酰化反应和适合于工业规模生产的条件下，通式（I）所定义。

5. 发明申请

WO2010004597A8 PROCESS FOR THE PRODUCTION OF N-ACYL-PHOSPHATIDYL-ETHANOLAMINE 审中-公开
标题翻译：制备N-乙酰基 - 苯乙胺的方法
公开(公告)号：WO2010004597A8
公开(公告)日：2010-12-02
申请号：PCT/IT2008000460
申请日：2008-07-08
申请人： CHEMI SPA , DE FERRA LORENZO , ANIBALDI MAURO , AMMIRATI ETTORE
发明人： DE FERRA LORENZO , ANIBALDI MAURO , AMMIRATI ETTORE
IPC分类号： C07F9/10
CPC分类号： C07F9/106 , C07F9/10
摘要： The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C1O-C30, pure or mixed together, and X=OH or OM, where M= alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.
摘要翻译：该文献描述了以工业规模制备式（I）的N-酰基 - 磷酰基 - 乙醇胺的方法，其中R 1，R 2和R 3彼此独立地为饱和的单不饱和或多不饱和酰基C 1 -C 30，纯或混合在一起，X = OH或OM，其中M =碱金属或碱土金属，铵或烷基铵。所讨论的方法允许使用有限摩尔过量的试剂N-酰基 - 乙醇胺将合成或天然来源的卵磷脂转化为高纯度的式（I）的N-酰基 - 磷酰基 - 乙醇胺，其中酰基如通过在磷脂酶D存在下的磷脂酰化反应和适合于工业规模生产的条件下，通式（I）所定义。

6. 发明申请

WO2004076469A1 METHOD FOR THE SYNTHESIS OF METHYL-TRI-OXO-RHENIUM 审中-公开
标题翻译：甲基三氧化铱合成方法
公开(公告)号：WO2004076469A1
公开(公告)日：2004-09-10
申请号：PCT/IT2004/000060
申请日：2004-02-16
申请人： CHEMI SPA , TURCHETTA, Stefano , MASSARDO, Pietro , TUOZZI, Angela
发明人： TURCHETTA, Stefano , MASSARDO, Pietro , TUOZZI, Angela
IPC分类号： C07F13/00
CPC分类号： C07F13/00
摘要： A method for the synthesis of methyltrioxorhenium is described, wherein 0.5-1.5 moles of dirhenium heptaoxide are reacted with 1-3 moles of tetramethyl tin in the presence of 1-3 moles of chlorotrimethyl silane. The synthesis is carried out in the dark for approximately 24 hours in a polar aprotic organic solvent, preferably in acetonitrile.
摘要翻译：描述了合成甲基三氧铼的方法，其中在1-3摩尔氯代三甲基硅烷的存在下，使0.5-1.5摩尔的七氧化铼与1-3摩尔的四甲基锡反应。合成在黑暗中在极性非质子有机溶剂中，优选在乙腈中进行约24小时。

7. 发明申请

WO2020178776A1 PROCESS FOR PREPARING {6-[(DIETHYLAMINO)METHYL]NAPHTHALEN-2-YL}METHYL [4-(HYDROXYCARBAMOYL)PHENYL]CARBAMATE HAVING HIGH PURITY 审中-公开
公开(公告)号：WO2020178776A1
公开(公告)日：2020-09-10
申请号：PCT/IB2020/051907
申请日：2020-03-05
申请人： CHEMI SPA
发明人： TURCHETTA, Stefano , ZENONI, Maurizio , ULLUCCI, Elio , COCCIOLO, Stefania , BERARDI, Giorgio , MAULUCCI, Nakia
IPC分类号： C07C269/06 , C07C269/08 , C07C271/28
摘要： A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4- (hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%. An HPLC method for determining the purity of the product and possible impurities thereof is also described.

8. 发明申请

WO2016184887A1 PROCESS FOR THE PREPARATION OF POLYSACCHARIDES 审中-公开
标题翻译：制备多糖的方法
公开(公告)号：WO2016184887A1
公开(公告)日：2016-11-24
申请号：PCT/EP2016/061088
申请日：2016-05-18
申请人： CHEMI SPA
发明人： DE FERRA, Lorenzo , AMMIRATI, Ettore , ANDREASSI, Simona , ANNIBALDI, Mauro , MANDELLI, Luca , PINTO, Barbara , STRACQUALURSI, Felice
IPC分类号： C08B37/00 , A61K31/737
CPC分类号： C08B37/0057 , A61K31/737 , C07H11/00 , C08B37/0003
摘要： The present invention relates to a process for the preparation of a polysaccharide composed of D-xylose units of formula (III) linked together via beta 1,4 glycosidic bonds wherein R 1 is hydrogen or acetyl, R 2 is hydrogen, acetyl or a 4-O-methyl glucuronic acid unit, wherein, when R 2 is a 4-O-methyl glucuronic acid unit, the R 1 group on the same saccharide unit is defined as G, wherein G is hydrogen or acetyl, and wherein the sugar unit at the reducing end of such polysaccharide is xylose, lyxose or xylulose, said process comprising the following steps: selective deacetylation of xylan extracted from beech wood; and isomerization of the selectively deacetylated xylan achieved in step or the following steps: isomerization of xylan extracted from beech wood; and selective deacetylation of isomerized xylan achieved in step. The process is useful for the preparation of pentosan polysulfate or pharmaceutically acceptable salts thereof for pharmaceutical use.
摘要翻译：本发明涉及一种制备由式（III）的D-木糖单元组成的多糖的方法，其通过β1,4糖苷键连接在一起，其中R1是氢或乙酰基，R2是氢，乙酰基或4-O - 甲基葡糖醛酸单元，其中当R2是4-0-甲基葡萄糖醛酸单元时，同一糖单元上的R 1基团定义为G，其中G为氢或乙酰基，并且其中还原末端的糖单元所述方法包括以下步骤：从山毛榉木中提取的木聚糖的选择性脱乙酰化; 和在步骤或以下步骤中获得的选择性脱乙酰化木聚糖的异构化：从山毛榉木提取的木聚糖异构化; 并在步骤中实现异构化木聚糖的选择性脱乙酰化。该方法可用于制备用于药物用途的戊聚糖多硫酸酯或其药学上可接受的盐。

9. 发明申请

WO2015092669A1 PROCESS FOR THE PREPARATION OF COLESEVELAM 审中-公开
标题翻译：制备COLESEVELAM的方法
公开(公告)号：WO2015092669A1
公开(公告)日：2015-06-25
申请号：PCT/IB2014/066948
申请日：2014-12-16
申请人： CHEMI SPA
发明人： GABOARDI, Mauro , BARUTO, Alessandro , CASTALDI, Marta
IPC分类号： C08F8/00 , C08F8/30 , C08F8/44 , C08F226/02 , C08F8/02
CPC分类号： C08F8/44 , C08F8/00 , C08F8/02 , C08F8/30 , C08F226/02 , C08F2810/20 , C08J3/24 , C08J2339/00 , C08F126/02
摘要： The present invention relates to a new process for the synthesis of Colesevelam, which is used in therapy in cases of hypercholesterolemia due to low density lipoproteins. Said process comprises the reaction, in a basic environment, of polyallylamine with: i) at least one alkylating agent of formula X-(CH 2 ) 9 -CH 3 and at least one alkylating agent of formula Y-(CH 2 ) 6 -N + (CH 3 ) 3 Z - , wherein X and Y are each independently a leaving group, and Z is a halogen; and ii) at least one crosslinking agent. The present invention also relates to the Colesevelam obtainable by the above process.
摘要翻译：本发明涉及一种用于合成Colesevelam的新方法，其用于由于低密度脂蛋白引起的高胆固醇血症的治疗。所述方法包括在碱性环境中与聚烯丙胺反应：i）至少一种式X-（CH 2）9 -CH 3烷基化剂和至少一种式Y-（CH 2）6 -N +（CH 3））3Z-，其中X和Y各自独立地为离去基团，Z为卤素; 和ii）至少一种交联剂。本发明还涉及通过上述方法获得的Colesevelam。

10. 发明申请

WO2010004597A9 PROCESS FOR THE PRODUCTION OF N-ACYL-PHOSPHATIDYL-ETANOLAMINE 审中-公开
公开(公告)号：WO2010004597A9
公开(公告)日：2010-01-14
申请号：PCT/IT2008/000460
申请日：2008-07-08
申请人： CHEMI SPA , DE FERRA, Lorenzo , ANIBALDI, Mauro , AMMIRATI, Ettore
发明人： DE FERRA, Lorenzo , ANIBALDI, Mauro , AMMIRATI, Ettore
IPC分类号： C07F9/10
摘要： The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R 1 , R 2 and R 3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C 1O -C 30 , pure or mixed together, and X=OH or OM, where M= alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.

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