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1. 发明授权

US07078533B2 Method for the racemization of etodolic acid 失效
标题翻译：雌二醇酸外消旋化的方法
公开(公告)号：US07078533B2
公开(公告)日：2006-07-18
申请号：US10800404
申请日：2004-03-12
申请人： Lorenzo De Ferra , Elio Ullucci
发明人： Lorenzo De Ferra , Elio Ullucci
IPC分类号： C07D491/52
CPC分类号： C07D491/04
摘要： A method for the resolution of etodolic acid by crystallization of its salt with optically active 1-phenylethylamine and subsequent recovery of the (R,S) etodolic acid from the mother liquors of crystallization by racemization and crystallization is described.
摘要翻译：描述了通过用光学活性1-苯基乙胺使其盐结晶并随后通过外消旋和结晶从母液中回收（R，S）二十二烷酸来分离乙内酯酸的方法。

2. 发明授权

US08518988B2 Polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphthalenyl) ester 有权
标题翻译：（4-羟基氨基甲酰基 - 苯基） - 氨基甲酸（6-二甲基氨基甲基-2-萘基）酯的盐酸盐的多晶型物
公开(公告)号：US08518988B2
公开(公告)日：2013-08-27
申请号：US13575641
申请日：2010-12-03
申请人： Stefano Turchetta , Maurizio Zenoni
发明人： Stefano Turchetta , Maurizio Zenoni
IPC分类号： A01N37/00 , A61K31/21 , A61K9/20
CPC分类号： C07C271/28 , A61K31/27
摘要： Herein described is a novel crystalline form of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester. In particular, herein described is a polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester, characterized by a Powder X Ray Diffraction spectrum as indicated in FIG. 1, and/or by a DSC profile as indicated in FIG. 2, and/or by a TGA profile as indicated in FIG. 3 and/or by an IR spectrum as indicated in FIG. 4.
摘要翻译：本文描述了（4-羟基氨基甲酰基 - 苯基） - 氨基甲酸（6-二乙基氨基甲基-2-萘基）酯的盐酸盐的新结晶形式。特别地，本文描述的是（4-羟基氨基甲酰基 - 苯基） - 氨基甲酸（6-二乙基氨基甲基-2-萘基）酯的盐酸盐的多晶型物，其特征在于如图1所示的粉末X射线衍射光谱。 1，和/或通过如图1所示的DSC轮廓。 2，和/或如图1所示的TGA轮廓。 3和/或通过如图1所示的IR光谱。 4。

3. 发明申请

US20120196988A1 PROCESS FOR THE PREPARATION OF CROSS-LINKED POLYALLYLAMINES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制备交联聚乙烯胺或其药学上可接受的盐的方法
公开(公告)号：US20120196988A1
公开(公告)日：2012-08-02
申请号：US13362495
申请日：2012-01-31
申请人： Mauro GABOARDI , Erminio OLDANI
发明人： Mauro GABOARDI , Erminio OLDANI
IPC分类号： C08J3/24 , C08G73/02
CPC分类号： C08F20/52 , A61K31/785 , C08F26/02 , C08K5/0025 , C08K5/42 , C08L39/00
摘要： The present invention relates to a process for the preparation of cross-linked polyallylamines or pharmaceutically acceptable salts thereof.The invention further relates to a process for the preparation of Sevelamer or pharmaceutically acceptable salts thereof, preferably hydrochloride or carbonate salts, used in the treatment of hyperphosphatemia, and having good flowability, low porosity and/or a swelling index of between 7 and 9.
摘要翻译：本发明涉及制备交联聚烯丙胺或其药学上可接受的盐的方法。本发明进一步涉及用于治疗高磷酸盐血症，具有良好流动性，低孔隙率和/或膨胀指数在7至9之间的塞维拉姆或其药学上可接受的盐，优选盐酸盐或碳酸盐的制备方法。

4. 发明申请

US20050215793A1 Amorphous 3-pyridil-1-hydroxyethyliden-1, 1-biphosphonic acid monosodium salt and process for the preparation thereof 有权
标题翻译：无定形3-吡啶-1-羟基乙烯-1,1-二膦酸单钠盐及其制备方法
公开(公告)号：US20050215793A1
公开(公告)日：2005-09-29
申请号：US11068484
申请日：2005-02-28
申请人： Stefano Turchetta , Pietro Massardo , Umberto Ciambecchini
发明人： Stefano Turchetta , Pietro Massardo , Umberto Ciambecchini
IPC分类号： A61K31/675 , C07F9/58
CPC分类号： C07F9/3873 , C07F9/58
摘要： A process for the preparation of 3-pyridil-1-hydroxyethyliden-1,1-biphosphonic acid monosodium salt of formula in an amorphous form, preferably lyophilized, and its pharmaceutical compositions are described. Said amorphous form, characterized by stability and simplicity of preparation and formulation, can be obtained by an industrially applicable lyophilization process, which comprises the steps of: a) dissolving or suspending 3-pyridyl-1-hydroxyethyliden-1,1-biphosphonic acid in an aqueous solvent, b) adding one equivalent of a base having sodium as cation c) subjecting the solution to lyophilization
摘要翻译：描述了一种制备无定形形式的3-吡啶-1-羟基乙烯基-1,1-二膦酸单钠盐，优选冻干的方法及其药物组合物。所述非晶形式，其特征在于制备和配制的稳定性和简单性，可通过工业上可应用的冻干方法获得，其包括以下步骤：a）将3-吡啶基-1-羟乙基-1,1-二膦酸溶解或悬浮在水性溶剂，b）加入1当量的具有钠的碱作为阳离子c）使溶液冷冻干燥

5. 发明申请

US20030236221A1 Process for the preparation of esters of heparin 审中-公开
标题翻译：制备肝素酯的方法
公开(公告)号：US20030236221A1
公开(公告)日：2003-12-25
申请号：US10402330
申请日：2003-03-28
申请人： CHEMI SPA
发明人： Lorenzo De Ferra , Mauro Montorsi
IPC分类号： A61K031/727 , C08B037/10
CPC分类号： C08B37/0075
摘要： The description relates to a process for the production of esters of heparin, wherein from 0.1 to 2 g of a halogenated reagent having the formula RnullCH2nullX, where R is a phenyl group which is non-substituted or substituted by a halogen atom or by a nitro group, and X is a halogen atom, preferably chlorine, are reacted with from 2 to 20 g of one of the quaternary ammonium salts of heparin in from 30 to 250 ml of N,N-dimethylformamide and/or N,N-dimethylacetamide. The process in question allows esters of heparin to be obtained at lower cost and within shorter times than the methods known in the art, minimising among other things the use of lachrymatory reagents, such as, for example, benzyl chloride.
摘要翻译：该描述涉及生产肝素酯的方法，其中0.1至2g具有式R-CH 2 -X的卤化试剂，其中R是未被取代或被卤素原子取代的苯基或硝基，X为卤素原子，优选氯，与2-20g一种30％至250ml N，N-二甲基甲酰胺和/或N，N-二甲基甲酰胺的肝素季铵盐反应， N-二甲基乙酰胺。所讨论的方法允许以比本领域已知的方法更低的成本和更短的时间内获得肝素酯，其中最小化使用氯甲烷试剂，例如苄基氯。

6. 发明申请

US20070049637A1 Process for the synthesis of cationic lipids 审中-公开
标题翻译：阳离子脂质合成方法
公开(公告)号：US20070049637A1
公开(公告)日：2007-03-01
申请号：US10579223
申请日：2004-11-03
申请人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
发明人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
IPC分类号： A61K31/22 , C07C229/02
CPC分类号： C07C213/00 , C07C213/08 , C07C215/10 , C07C219/08 , Y02P20/55
摘要： A process for the synthesis of lipid cations having general formula (6): in which: R1 represents a lipophilic chain; R2, R3, R4, which are identical or different from one another, represent C1-C10 alkyl, C1-C10 alkenyl, or C1-C10 alkynyl radicals, optionally containing hydroxyl, ether, halogen and acyloxy functions, and X− is an oxy-anion or a halide; in which a compound of formula (2), in which R5 and R6, which are identical or different from one another, represent a C1-C5 acyl, a benzyl group or a diol-protective group, is reacted in an alcoholic solvent with from 1 to 6 equivalents of NR2R3R4.
摘要翻译：用于合成具有通式（6）的脂质阳离子的方法：其中：R 1表示亲脂链; R 2，R 3，R 4，它们彼此相同或不同，表示C 1〜 C 1 -C 10烷基，C 1 -C 10链烯基或C 1 -C 10烷基，C 1 -C 10 - 任选地含有羟基，醚，卤素和酰氧基官能团的炔基，X - 是氧阴离子或卤化物; 其中式（2）的化合物（其中R 5和R 6）彼此相同或不同，表示C 1〜 C 1 -C 5酰基，苄基或二醇保护基在醇溶剂中与1至6当量的NR 2 R 2 - 3 R 4。

7. 发明授权

US07105681B2 Process for the preparation of sulphinyl derivatives by oxidation of the corresponding sulfides 失效
标题翻译：通过氧化相应硫化物制备亚磺酰基衍生物的方法
公开(公告)号：US07105681B2
公开(公告)日：2006-09-12
申请号：US11149544
申请日：2005-06-10
申请人： Stefano Tur{overscore (c)}hetta , Pietro Massardo , Angela Tuozzi
发明人： Stefano Tur{overscore (c)}hetta , Pietro Massardo , Angela Tuozzi
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Process for preparing sulfinyl derivatives of Formula 2, useful as inhibitors of gastric acid secretion, comprising the selective oxidation of the corresponding sulfides of formula 1, as represented in the following scheme The oxidation is performed with hydrogen peroxide in the presence of low amounts of a rhenium compound as catalyst, at a temperature from 0° C. to room temperature.
摘要翻译：用于制备式2的亚磺酰基衍生物的方法，其可用作胃酸分泌的抑制剂，包括选择性氧化式1的相应硫化物，如以下方案所示。氧化是在少量的铼化合物作为催化剂，在0℃至室温的温度下进行。

8. 发明授权

US07087548B2 Preparation and use of a heterogeneous rhodium catalyst for the hydrogenation of a double bond of an α-β-unsaturated carbonyl compound 失效
标题翻译：用于氢化α-β-不饱和羰基化合物的双键的异相铑催化剂的制备和使用
公开(公告)号：US07087548B2
公开(公告)日：2006-08-08
申请号：US10493745
申请日：2002-10-24
申请人： Oreste Piccolo , Alessandra Verrazzani
发明人： Oreste Piccolo , Alessandra Verrazzani
IPC分类号： B01J31/00
CPC分类号： B01J31/1616 , B01J21/04 , B01J23/464 , B01J31/1805 , B01J37/18 , B01J2231/645 , B01J2531/822 , C07C45/62 , C07C49/255 , Y02P20/588
摘要： A process for preparing an Rh-based catalytic system heterogenized on an organic or mineral support, characterized in that: a) a rhodium derivative with a valency state>0 is reduced in an ether or aromatic solvent and in the presence of a compound chosen from the group consisting of lipophilic tertiary amines, lipophilic tertiary amides and lipophilic quaternary ammonium salts, and b) the mixture thus obtained is adsorbed onto a suitable organic or mineral support. Use of the abovementioned catalytic system to hydrogenate a C═C double bond of an α,β-unsaturated carbonyl compound.
摘要翻译：一种用于制备在有机或矿物载体上异质化的基于Rh的催化体系的方法，其特征在于：a）在醚或芳族溶剂中并且在选自以下的化合物存在下，化合价> 0的铑衍生物被还原由亲脂性叔胺，亲脂性叔酰胺和亲脂性季铵盐组成的组，和b）由此获得的混合物被吸附到合适的有机或矿物载体上。使用上述催化体系来氢化α，β-不饱和羰基化合物的C-C双键。

9. 发明申请

US20050267070A1 Process for the preparation of esters of heparin 审中-公开
标题翻译：制备肝素酯的方法
公开(公告)号：US20050267070A1
公开(公告)日：2005-12-01
申请号：US11195392
申请日：2005-08-01
申请人： Lorenzo De Ferra , Mauro Montorsi
发明人： Lorenzo De Ferra , Mauro Montorsi
IPC分类号： C08B37/00 , A61K31/727 , C08B37/10
CPC分类号： C08B37/0075
摘要： The description relates to a process for the production of esters of heparin, wherein from 0.1 to 2 g of a halogenated reagent having the formula R—CH2—X, where R is a phenyl group which is non-substituted or substituted by a halogen atom or by a nitro group, and X is a halogen atom, preferably chlorine, are reacted with from 2 to 20 g of one of the quaternary ammonium salts of heparin in from 30 to 250 ml of N,N-dimethylformamide and/or N,N-dimethylacetamide. The process in question allows esters of heparin to be obtained at lower cost and within shorter times than the methods known in the art, minimising among other things the use of lachrymatory reagents, such as, for example, benzyl chloride.
摘要翻译：该描述涉及生产肝素酯的方法，其中0.1至2g具有式R-CH 2 -X的卤代试剂，其中R是非 - 由卤素原子或硝基取代或取代，X为卤素原子，优选为氯，与2-20g的肝素季铵盐中的一种从30至250ml N反应， N-二甲基甲酰胺和/或N，N-二甲基乙酰胺。所讨论的方法允许以比本领域已知的方法更低的成本和更短的时间内获得肝素酯，其中最小化使用氯甲烷试剂，例如苄基氯。

10. 发明申请

US20050239695A1 Process for the formation of disulfide bonds in cyclic peptides 审中-公开
标题翻译：在环肽中形成二硫键的方法
公开(公告)号：US20050239695A1
公开(公告)日：2005-10-27
申请号：US11114021
申请日：2005-04-26
申请人： Silvana Cappelletti , Olivia Storace , Paola Annoni , Massimo Pinori
发明人： Silvana Cappelletti , Olivia Storace , Paola Annoni , Massimo Pinori
IPC分类号： C07K1/113 , C07K1/04 , C07K1/06 , A61K38/12 , C07K5/12 , C07K7/64
CPC分类号： C07K1/067 , C07K1/04 , Y02P20/55
摘要： A non-oxidative process is described for the formation of an intramolecular disulfide bond in precursors of the peptide or peptidomimetic type; said process comprises the preparation of a linear intermediate containing an —SH group in the S-sulfonate form and a second —SH group which is obtainable in the free form by means of acid treatment.
摘要翻译：描述了在肽或肽模拟型前体中形成分子内二硫键的非氧化方法; 所述方法包括制备含有S-磺酸盐形式的-SH基团的线性中间体和通过酸处理以游离形式获得的第二-SH基团。

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