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1. 发明申请

WO0076994A2 PROCESS FOR THE PREPARATION OF FUMAGILLIN 审中-公开
标题翻译：制备FUMAGILLIN的方法
公开(公告)号：WO0076994A2
公开(公告)日：2000-12-21
申请号：PCT/HU0000054
申请日：2000-06-06
申请人： SANOFI SYNTHELABO , FARKAS GYULA , GYOERBIRO ANDREA , HERMECZ ISTVAN , SIMON KALMAN , SZABO ANNA , VASVARI ARPADNE
发明人： FARKAS GYULA , GYOERBIRO ANDREA , HERMECZ ISTVAN , SIMON KALMAN , SZABO ANNA , VASVARI ARPADNE
IPC分类号： C07D303/22 , C07D407/00
CPC分类号： C07D303/22
摘要： The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium. According to the process Fumagillin can be produced in high yield and pure condition and with higher stability than products obtained by other preparation methods.
摘要翻译：本发明涉及一种通过从其盐中释放制备烟曲霉素的方法，其特征在于使富马青霉素二环己胺盐与醇介质中的有机酸反应。根据该方法，富马林可以以高产率和纯度的条件生产，并且具有比通过其它制备方法获得的产品更高的稳定性。

2. 发明申请

WO2005100320A3 CRYSTALLINE 2-AMINO-3-CYANOQUINOLINE DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：晶体2-氨基-3-氰基喹啉衍生物及其制备方法及含有它们的药物组合物
公开(公告)号：WO2005100320A3
公开(公告)日：2006-01-12
申请号：PCT/HU2005000036
申请日：2005-04-14
申请人： SANOFI AVENTIS , FINTA ZOLTAN , HERMECZ ISTVAN , HEJA GERGELY , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIPOS JUDIT , SZABO ANNA , VASVARI ARPADNE , VARKONYINE SCHLOVICSKO ERIKA
发明人： FINTA ZOLTAN , HERMECZ ISTVAN , HEJA GERGELY , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIPOS JUDIT , SZABO ANNA , VASVARI ARPADNE , VARKONYINE SCHLOVICSKO ERIKA
IPC分类号： C07D215/54 , C07D405/12 , C07D405/14 , C07D409/12 , A61K31/4706
CPC分类号： C07D405/12 , C07D215/54 , C07D405/14 , C07D409/12
摘要： The invention relates to the crystalline and amorphous forms of the desmotrop of general formula (IB) and its salts and solvates. - where in the formula R represents benzyl-, 2-(thienyl)methyl- or 2-(furyl)methyl group and R 1 represents phenyl or furyl group substituted with C 1-4 alkoxy group or halogen atom, to pharmaceutical compositions containing as for active ingredient the desmotrop of general formula (IB), and to preparation of the crystalline and amorphous forms of desmotrops (IA) and (IB).
摘要翻译：本发明涉及通式（IB）及其盐和溶剂合物的结晶和无定形形式。 - 其中式R表示苄基 - ，2-（噻吩基）甲基 - 或2-（呋喃基）甲基，R 1表示被C 1-4取代的苯基或呋喃基，对于含有活性成分的通式（IB）的去结构的药物组合物，以及制备无色形态的去结构（IA）和（IB）的药物组合物。

3. 发明专利

HU0303062A2 NEW PROCESS AND NEW INTERMEDIATES FOR PREPARATION OF CARBOXAMIDO-THIAZOLE DERIVATIVES 未知
公开(公告)号：HU0303062A2
公开(公告)日：2003-12-29
申请号：HU0303062
申请日：2001-11-27
申请人： SANOFI SYNTHELABO
发明人： BOKOTEY SANDOR , GALAMBOS GEZANE , HAJDU FELIX , HERMECZ ISTVAN , HORVATH AGNES , IVANICS JOZSEFNE , KISS GYULANE , NAGY LAJOS , PODANYI BENJAMIN , SIMON ATTILA , SIPOS JUDIT , SMELKONE ESEK AGOTA , SZABO ANNA , VASVARI ARPADNE
IPC分类号： C07D209/42
摘要： Preparation of thiazol-2-yl amino carbonyl indole derivatives, their salts or solvates involves reacting N-(amino-thioxo-methyl)-1H-indole-2-carboxamide with an alpha -halogen-ketone. Preparation of thiazol-2-yl amino carbonyl indole derivative of formula (I), its salts or solvates involves reacting an N-(amino-thioxo-methyl)-1H-indole-2-carboxamide of formula (II) with an alpha -halogen-ketone of formula R8>-C(O)-CH(X)-R9>'> (III). (I) or its solvate is then transformed into its salt or liberated from its salt. [Image] R1>H or methyl; R2> - R5>R1>, T, OH, acetyloxy, methylthio, trifluoromethyl or amino; T : ethyl, methoxy, ethoxy or halo; R : H, -(CH2)nR6> or group of formula (a); R6>carboxyl or -COOR7>; R7>1-4C alkyl; n : 1 - 5; m : 0 or 1; R8>substituted phenyl of formula (b); R1>0>H or methoxy; R1>1>R1>, T or isopropyl; R1>2>R1>, ethyl, methoxy or halo; R1>1>+R1>2>methylenedioxy; R9>-CH2-R1>3>, -(CH2)2R1>3>, R'9> or 5-8C alkyl; R9>'>-S-CH2-R1>3> or -CH2-S-R1>3>; and R1>3>5-7C cycloalkyl; provided that R1>3> is 5-7C cycloalkyl when R1>0> - R1>2> is not H at the same time. Independent claims are also included for: (1) compounds of formulae (II) and (III); (2) preparation of (II) by transforming 1H-indole-2-carboxylic acid of formula (V) into 1H-indole-2-carboxylic acid halogenide of formula (VI), reacting (VI) with potassium-thiocyanate in the presence of a diprotic-aprotic solvent (preferably acetone or methyl-ethyl-ketone) and reacting the isothiocyanate of formula (VIII) with ammonia or ammonium hydroxide; and (3) preparation of (III) by acylating a methoxy benzene of formula (X) with an acid-chloride of formula Cl-C(O)-CH2-(CH2)o-S-(CH2)p-R1>4> (XI) in the presence of a Lewis acid (preferably titanium-tetrachloride or aluminum chloride), and halogenating R8>-C(O)-CH2-R'9> (IX). [Image] Hlg : halo. R1>4>5-7C cycloalkyl; o : 1 or 2; and p : 0 or 1. ACTIVITY : None given. MECHANISM OF ACTION : Cholecystokinin A (CCK-A) agonist.

4. 发明专利

BR0109890A 未知
公开(公告)号：BR0109890A
公开(公告)日：2003-06-03
申请号：BR0109890
申请日：2001-04-04
申请人： SANOFI SYNTHELABO
发明人： HERMECZ ISTVAN , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIMON KALMAN , SIPOS JUDIT , ESEK AGOTA SMELKONE , SZABO ANNA , VASVARI ARPADNE
IPC分类号： A61K31/427 , A61P1/00 , A61P25/00 , A61P43/00 , C07D20060101 , C07D417/12 , A61K31/425
摘要： Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid (I), their solvates, polymorphs and pseudo polymorphs are new. Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid of formula (I), their solvates, polymorphs and pseudo polymorphs are new. [Image] X : ethanolamine, diethanolamine or diethylamine. ACTIVITY : Gastrointestinal; Cerebroprotective. MECHANISM OF ACTION : Cholecystokinin A agonist. No biological data given.

5. 发明专利

CA2405004A1 THERAPEUTICALLY USEFUL NEW SALTS OF CCK INHIBITORS, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM 未知
公开(公告)号：CA2405004A1
公开(公告)日：2001-10-18
申请号：CA2405004
申请日：2001-04-04
申请人： SANOFI SYNTHELABO
发明人： SMELKONE ESEK AGOTA , SIMON KALMAN , SIPOS JUDIT , VASVARI ARPADNE , HORVATH AGNES , HERMECZ ISTVAN , SZABO ANNA , PODANYI BENJAMIN , KISS GYULANE , MORVAI MIKLOS
IPC分类号： A61K31/427 , A61P1/00 , A61P25/00 , A61P43/00 , C07D20060101 , C07D417/12 , A61K31/425
摘要： New salts of the general formula (I), their solvates, polymorphs and pseudo polymorphs wherein X stands for ethanolamine, diethanolamine or diethylamine .

6. 发明专利

CA2374639C PROCESS FOR THE PREPARATION OF FUMAGILLIN 未知
公开(公告)号：CA2374639C
公开(公告)日：2008-07-15
申请号：CA2374639
申请日：2000-06-06
申请人： SANOFI SYNTHELABO
发明人： GYORBIRO ANDREA , HERMECZ ISTVAN , SIMON KALMAN , FARKAS GYULA , SZABO ANNA , VASVARI ARPADNE
IPC分类号： C07D303/22 , C07D407/00
摘要： The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium. According to the process Fumagillin can be produced in high yield and pure condition and with higher stability than products obtained by other preparation methods.

7. 发明专利

SK15052002A3 Therapeutically useful new salts of CCK inhibitors, process for the preparation thereof and pharmaceutical preparations containing them 未知
公开(公告)号：SK15052002A3
公开(公告)日：2003-05-02
申请号：SK15052002
申请日：2001-04-04
申请人： SANOFI SYNTHELABO
发明人： HERMECZ ISTVAN , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIMON KALMAN , SIPOS JUDIT , SMELKONE ESEK AGOTA , SZABO ANNA , VASVARI ARPADNE
IPC分类号： A61K31/427 , A61P1/00 , A61P25/00 , A61P43/00 , C07D20060101 , C07D417/12 , A61K31/425
摘要： Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid (I), their solvates, polymorphs and pseudo polymorphs are new. Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid of formula (I), their solvates, polymorphs and pseudo polymorphs are new. [Image] X : ethanolamine, diethanolamine or diethylamine. ACTIVITY : Gastrointestinal; Cerebroprotective. MECHANISM OF ACTION : Cholecystokinin A agonist. No biological data given.

8. 发明专利

CA2374639A1 PROCESS FOR THE PREPARATION OF FUMAGILLIN 未知
公开(公告)号：CA2374639A1
公开(公告)日：2000-12-21
申请号：CA2374639
申请日：2000-06-06
申请人： SANOFI SYNTHELABO
发明人： SZABO ANNA , FARKAS GYULA , VASVARI ARPADNE , SIMON KALMAN , HERMECZ ISTVAN , GYORBIRO ANDREA
IPC分类号： C07D303/22 , C07D407/00
摘要： The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium. According t o the process Fumagillin can be produced in high yield and pure condition and with higher stability than products obtained by other preparation methods.

9. 发明专利

PL362650A1 THERAPEUTICALLY USEFUL NEW SALTS OF CCK INHIBITORS, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM 未知
公开(公告)号：PL362650A1
公开(公告)日：2004-11-02
申请号：PL36265001
申请日：2001-04-04
申请人： SANOFI SYNTHELABO
发明人： HERMECZ ISTVAN , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIMON KALMAN , SIPOS JUDIT , SMELKONE ESEK AGOTA , SZABO ANNA , VASVARI ARPADNE
IPC分类号： A61K31/427 , A61P1/00 , A61P25/00 , A61P43/00 , C07D20060101 , C07D417/12 , A61K31/425
摘要： Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid (I), their solvates, polymorphs and pseudo polymorphs are new. Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid of formula (I), their solvates, polymorphs and pseudo polymorphs are new. [Image] X : ethanolamine, diethanolamine or diethylamine. ACTIVITY : Gastrointestinal; Cerebroprotective. MECHANISM OF ACTION : Cholecystokinin A agonist. No biological data given.

10. 发明专利

EE200200582A 未知
公开(公告)号：EE200200582A
公开(公告)日：2004-04-15
申请号：EEP200200582
申请日：2001-04-04
申请人： SANOFI SYNTHELABO
发明人： HERMECZ ISTVAN , HORVATH AGNES , KISS GYULANE , MORVAI MIKLOS , PODANYI BENJAMIN , SIMON KALMAN , SIPOS JUDIT , ESEK AGOTA SMELKONE , SZABO ANNA , VASVARI ARPADNE
IPC分类号： A61K31/427 , A61P1/00 , A61P25/00 , A61P43/00 , C07D20060101 , C07D417/12 , A61K31/425
摘要： Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid (I), their solvates, polymorphs and pseudo polymorphs are new. Salts of 2-(((4-(4-chloro-2,5-dimethoxy-phenyl)-5-(2-cyclohexyl-ethyl)-2-thiazolyl)amino)carbonyl)-5,7-dimethyl-1H-indol-1-acetic acid of formula (I), their solvates, polymorphs and pseudo polymorphs are new. [Image] X : ethanolamine, diethanolamine or diethylamine. ACTIVITY : Gastrointestinal; Cerebroprotective. MECHANISM OF ACTION : Cholecystokinin A agonist. No biological data given.

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