专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明申请

WO2010100512A8 NOVEL CRYSTALLINE HYDRATE, AMORPHOUS AND POLYMORPHIC FORMS OF DIHYDRO-BENZOXAZOLE-6-YL-ACETAMIDE DERIVATIVE AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：新型水晶，二羟基苯并噻唑-6-基乙酰胺衍生物的非晶态和多晶型及其制备方法
公开(公告)号：WO2010100512A8
公开(公告)日：2011-07-21
申请号：PCT/HU2010000023
申请日：2010-03-01
申请人： RICHTER GEDEON NYRT , DEMETER ADAM , NEMET ZOLTAN , NEMES ANDRAS , SEBOK FERENC , BARTANE SZALAI GIZELLA , CZIBULA LASZL
发明人： DEMETER ADAM , NEMET ZOLTAN , NEMES ANDRAS , SEBOK FERENC , BARTANE SZALAI GIZELLA , CZIBULA LASZL
IPC分类号： C07D413/12 , A61K31/423 , A61P25/00
CPC分类号： C07D413/12
摘要： The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro- benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.
摘要翻译：本发明涉及2- [4-（4-氟 - 苄基） - 哌啶-1-基] -2-氧代-N-（2-氧代-2,3-二氢化物）的新型结晶水合物，无定形和结晶多晶型物 - 苯并恶唑-6-基） - 乙酰胺（I）（radiprodil）。还描述了制备这些形式的方法，含有这些形式的组合物及其使用方法。

42. 发明申请

WO2011061554A8 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF BLADDER DISORDERS 审中-公开
公开(公告)号：WO2011061554A8
公开(公告)日：2011-05-26
申请号：PCT/HU2010/000125
申请日：2010-11-18
申请人： RICHTER GEDEON NYRT. , LOVÁSZ, Sándor , FURKA, Beáta , SZÉKELY, Ákosné , FORRAI, Gáborné , RODENNÉ JUHÁSZ, Maria , SÉNYI, Lajos
发明人： LOVÁSZ, Sándor , FURKA, Beáta , SZÉKELY, Ákosné , FORRAI, Gáborné , RODENNÉ JUHÁSZ, Maria , SÉNYI, Lajos
IPC分类号： A61K31/728 , A61K33/30
摘要： The invention relates to pharmaceutical compositions with activity against disorders of urogenital system of mammals which comprises a zinc-hyaluronan complex as active ingredient and a pharmaceutically acceptable carrier and/or additive. The process for the preparation of said pharmaceutical compositions as well as the therapeutic use thereof for the treatment and prevention of diseases associated with abnormalities and deficiencies of glucosaminoglycan (GAG) layer in the urogenital system in mammals and a kit comprising zinc hyaluronate solution, a catheter which is applicable to intravesical administration and optionally a balloon which is applicable to bladder dillatation are also within the scope of the invention.

43. 发明申请

WO2010106383A1 NOVEL CRYSTALLINE FORM OF ANTIPROGESTIN CDB-4124 审中-公开
标题翻译：抗肿瘤蛋白CDB-4124的新型结晶形式
公开(公告)号：WO2010106383A1
公开(公告)日：2010-09-23
申请号：PCT/HU2010/000030
申请日：2010-03-22
申请人： RICHTER GEDEON NYRT , SÁNTA, Csaba , DEMETER, Ádám , HAVASI, Balázs , MAHÓ, Sándor
发明人： SÁNTA, Csaba , DEMETER, Ádám , HAVASI, Balázs , MAHÓ, Sándor
IPC分类号： C07J41/00 , A61K31/573 , A61P5/36
CPC分类号： C07J41/0083
摘要： The present invention relates to novel crystalline Form A of 17α-acetoxy-21-methoxy- l lβ-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124) and methods for the preparation of it in excellent purity.
摘要翻译：本发明涉及17a-乙酰氧基-11-甲氧基-11β-[4-N，N-二甲基氨基苯基] -19-去甲基-4,9-二烯-3,20-二酮的新型结晶形式A（也称为作为CDB-4124）及其制备方法纯度高。

44. 发明申请

WO2010070370A8 PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
公开(公告)号：WO2010070370A8
公开(公告)日：2010-06-24
申请号：PCT/HU2009/000109
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT. , CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
发明人： CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
IPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving suspending trans 4-[2-[4-(2,3-dichlorophenyl)-piperazine1-il]-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain or C 1-2 fully halogenated alkyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R 1 and R 2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.

45. 发明申请

WO2010070370A1 PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
标题翻译：哌嗪化合物的制备方法及其盐酸盐的制备方法
公开(公告)号：WO2010070370A1
公开(公告)日：2010-06-24
申请号：PCT/HU2009000109
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT , CZIBULA LASZL , JUHASZ BALINT , AGAINE CSONGOR EVA , SEBOEK FERENC , GALAMBOS JANOS , N GRADI KATALIN
发明人： CZIBULA LASZL , JUHASZ BALINT , AGAINE CSONGOR EVA , SEBOEK FERENC , GALAMBOS JANOS , N GRADI KATALIN
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving suspending trans 4-[2-[4-(2,3-dichlorophenyl)-piperazine1-il]-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C1-6 straight or branched chain or C1-2 fully halogenated alkyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R1 and R2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及一种通过将反式4- [2- [4-（2,3-二氯苯基）） - 哌嗪-1-基] - 环己胺或其盐或其水合物或溶剂化物，然后在惰性溶剂中在存在碱存在下加入通式（VI）的碳酸衍生物，其中R是烷基， 6个直链或支链或C1-2完全卤代烷基，Z是-OR或-X，其中R如上所述，X是卤素，并使得到的通式（Ⅳ）化合物（其中R如上所述）原位或任选地在分离状态下与通式（Ⅴ）的胺反应，其中R 1和R 2如上所述，得到通式（I）的化合物，然后任选地形成盐酸盐和/或水合物和/或溶剂合物它们。

46. 发明申请

WO2008062244A8 POLYMORPHS OF 5-{2-[4-(1,2-BENZISOTHIAZOL-3-YL)-1-PIPERAZINYL]-ETHYL}-6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE HYDROBROMIDE AND PROCESSES FOR PREPARATION THEREOF 审中-公开
标题翻译： 5- {2- [4-（1,2-苯基联苯-3-基）-1-哌嗪基] - 乙基} -6-氯-1,3-二氢-2H-吲哚-2-酮氢溴酸盐和方法的多异构体为其准备
公开(公告)号：WO2008062244A8
公开(公告)日：2009-06-11
申请号：PCT/HU2007000112
申请日：2007-11-23
申请人： RICHTER GEDEON NYRT , NEU JOZSEF , DEMETER ADAM , VARGA ZOLTAN , HAVASI BALAZS , GARADNAY SANDOR , HEGEDUES BELA
发明人： NEU JOZSEF , DEMETER ADAM , VARGA ZOLTAN , HAVASI BALAZS , GARADNAY SANDOR , HEGEDUES BELA
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The present invention provides pharmaceutically applicable compounds and polymorphs belonging to the ziprasidone hydrobromide compound group with antipsychotic effect. The present invention provides hydrobromide polymorphs of 5-{2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one, ziprasidone of Formula (I) having neuroleptic activity.
摘要翻译：本发明提供具有抗精神病作用的属于齐拉西酮氢溴酸盐化合物组的药学上适用的化合物和多晶型物。本发明提供了5- {2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基] - 乙基} -6-氯-1,3-二氢-2H-吲哚-2-酮的氢溴酸盐多晶型物 - 一种具有神经安定药活性的式（I）的齐拉西酮。

47. 发明申请

WO2007102037A3 A PROCESS FOR THE PREPARATION OF POLYMORPH FORM I OF (S)-(+)-METHYL-a-(2-CHLOROPHENYL)-6,7-DYHIDRO-THIENO-[3,2-c]PYRIDINE-5(4H)-ACETATE HYDROGEN SULFATE 审中-公开
标题翻译：制备（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二氢 - 噻吩并[3,2-c]吡啶-5（4H） - 酮的多晶型I的方法乙酸氢硫酸盐
公开(公告)号：WO2007102037A3
公开(公告)日：2008-11-13
申请号：PCT/HU2007000021
申请日：2007-03-08
申请人： RICHTER GEDEON NYRT , GARADNAY SANDOR , GREINER ISTVAN , NEU JOZSEF
发明人： GARADNAY SANDOR , GREINER ISTVAN , NEU JOZSEF
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of the pharmaceutically applicable polymorph Form I of (S)-(+)-methyl-a-(2-clorophenyl)-6,7-dyhidro-thieno[3,2-c]-pyridine-5(4H)-acetate hydrogen sulfate of formula I; by reacting (S)-(+)-methyl-a-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate and sulfuric acid in the presence of solvents which comprises dissolving (S)-(+)-methyl-a-(2-chloropnenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate in an ether; mixing this solution with a solution of a C 6 -C 11 alcohol and sulfuric acid; and recovering the so obtained compound of formula I from the mother liquor.
摘要翻译：本发明涉及制备（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二苯并噻吩并[3,2-c] - 式I的吡啶-5（4H） - 乙酸盐硫酸氢盐; 通过使（S） - （+） - 甲基-α-（2-氯苯基）-6,7-二氯 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯和硫酸在溶剂存在下反应其包括在醚中溶解（S） - （+） - 甲基-α-（2-氯代烯基）-6,7-二氯 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯; 将该溶液与C 6 -C 11 - 醇和硫酸的溶液混合; 并从母液中回收如此得到的式I化合物。

48. 发明申请

WO2008035128A1 PHARMACEUTICAL COMPOSITIONS CONTAINING ROSUVASTATIN CALCIUM 审中-公开
标题翻译：含有ROSUVASTATIN钙的药物组合物
公开(公告)号：WO2008035128A1
公开(公告)日：2008-03-27
申请号：PCT/HU2007/000082
申请日：2007-09-11
申请人： RICHTER GEDEON NYRT. , VIRÁGH, Mária , MONOSTORI, Iidikó
发明人： VIRÁGH, Mária , MONOSTORI, Iidikó
IPC分类号： A61K9/20 , A61K47/02 , A61K31/505 , A61K31/22 , A61K47/12
CPC分类号： A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K31/22 , A61K31/505
摘要： The subject of the present invention is a novel pharmaceutical composition containing amorphous rosuvastatin calcium, and magnesium hydroxide and/or calcium acetate or calcium gluconate or calcium glycerophosphate or aluminum hydroxide as stabilizing additive and one or more pharmaceutically acceptable excipients.
摘要翻译：本发明的主题是含有无定形罗苏伐他汀钙和氢氧化镁和/或乙酸钙或葡萄糖酸钙或甘油磷酸钙或氢氧化铝作为稳定添加剂和一种或多种药学上可接受的赋形剂的新型药物组合物。

49. 发明申请

WO2008032131A1 PROCESS FOR THE SELECTIVE ISOLATION, PURIFICATION AND SEPARATION OF MONOHYDROXYLATED 3,17-DIKETO-STEROID COMPOUNDS 审中-公开
标题翻译：选择性分离，纯化和分离单羟基氧化的3,17-二酮 - 甾体化合物的方法
公开(公告)号：WO2008032131A1
公开(公告)日：2008-03-20
申请号：PCT/HU2007/000084
申请日：2007-09-13
申请人： RICHTER GEDEON NYRT. , JAKSA, István , NÉMETH, Sándor , KÖNCZÖL, Kálmán , TERDY, László , KOZMA, István , BARTA, Ferenc
发明人： JAKSA, István , NÉMETH, Sándor , KÖNCZÖL, Kálmán , TERDY, László , KOZMA, István , BARTA, Ferenc
IPC分类号： C07J1/00
CPC分类号： C07J1/00 , C07J1/0011 , C07J1/0059
摘要： The subject of the present invention is a new process for the selective isolation, purification and separation of monohydroxylated 3,17-diketo-steroid compounds from a solution obtained preferably by microbiological way containing a mixture of steroid compounds via selective extraction, purification and selective crystallization of the steroid compounds by treatment of several solvents.
摘要翻译：本发明的主题是从通过选择性提取，纯化和选择性结晶的含有类固醇化合物的混合物的微生物学方法获得的溶液中选择性分离，纯化和分离单羟化3,17-二酮类固醇化合物的新方法的类固醇化合物通过处理几种溶剂。

50. 发明申请

WO2007144674A1 INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17α-ACETOXY-11β-[4-(N,N-DIMETHYL-AMINO)- PHENYL]-19-NORPREGNA-4,9-DIENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS 审中-公开
标题翻译：合成17a-乙酰基-11β-[4-（N，N-二甲基氨基） - 苯基] -19-壬基-4,9-二烯-3,20-二酮的工业方法和该方法的新中间体
公开(公告)号：WO2007144674A1
公开(公告)日：2007-12-21
申请号：PCT/HU2007/000045
申请日：2007-05-18
申请人： RICHTER GEDEON NYRT , DANCSI, Lajosné , VISKY, György , TUBA, Zoltán , CSÖRGEI, János , MOLNÁR, Csaba , MAGYARI, Endréné
发明人： DANCSI, Lajosné , VISKY, György , TUBA, Zoltán , CSÖRGEI, János , MOLNÁR, Csaba , MAGYARI, Endréné
IPC分类号： C07J21/00 , C07J31/00 , C07J41/00 , C07J71/00
CPC分类号： C07J21/006 , C07J31/006 , C07J41/0083 , C07J71/001
摘要： The present invention relates to a new industrial process for the synthesis of solvate- free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB -2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process. The process according to the invention is the following: i) 3-(ethylene-dioxy)-estra-5(10),9(11)-diene-17-one of formula (X) is reacted with potassium acetilyde formed in situ in dry tetrahydrofuran by known method, ii) the obtained 3-(ethylene-dioxy)-17α-ethynyl-17β-hydroxy-estra-5(10),9(11)-diene of formula (IX) is reacted with phenylsulfenyl chloride in dichloromethane in the presence of triethylamine and acetic acid, iii) the obtained isomeric mixture of 3-(ethylene-dioxy)-21-(phenyl-sulfinyl)-19-norpregna-5(10),9(11),17(20),20-tetraene of formula (VIII) is reacted first with sodium methoxide in methanol, then with trimethyl phosphite, iv) the obtained 3-(ethylene-dioxy)-17α-hydroxy-20-methoxy-19-norpregna-5(10),9(11),20-triene of formula (VII) is reacted with hydrogen chloride in methanol, then v) the obtained 3-(ethylene-dioxy)-17α-hydroxy-19-norpregna-5(10),9(11l)-diene-20- one of formula (VI) is reacted with ethylene glycol hi dichloromethane in the presence of trimethyl orthoformate and p-toluenesulfonic acid by known method, vi) the obtained 3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-19-norpregna- 5(10),9(11)-diene of formula (V) is reacted with hydrogen peroxide in a mixture of pyridine and dichloromethane in the presence of hexachloroacetone by known method, vii) the obtained 3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-5,10-epoxy-19-norpregn-9(11)-ene of formula (IV), containing approximately a 1:1 mixture of 5α,10α- and 5β,10β-epoxides, is isolated from the solution and reacted with a Grignard reagent obtained from 4-bromo-N,N-dimethyl-aniline in tetrahydrofuran in the presence of copper(I) chloride catalyst without separation of the isomers by known method, viii) the obtained 3,3,20,20-bis(ethylene-dioxy)-5α,17α-dihydroxy-11β-[4-(N,N-dimethylamino)-phenyl]-19-norpregn-9(11)-ene of formula (III) is reacted with potassium hydrogensulfate in water by known method, ix) the obtained 11β-[4-(N,N-dimethylamino)-phenyl]-17α-hydroxy-19-norpregn-4,9-diene-3,20-dione of formula (II) is acetylated with acetic anhydride in the presence of perchloric acid by known method, finally x) the solvate-free compound of formula (I) is liberated from the obtained solvate containing compound of formula (I) in a 1 : 1 mixture of ethanol and water at 70° C.
摘要翻译：本发明涉及合成无溶剂合物的17-乙酰氧基-11β-[4-（N，N-二甲基 - 氨基） - 苯基] -19-去甲基-4,9-二烯-3的新工业方法，（I）的20-二酮[CDB -2914]，其是强抗对虾和抗糖皮质激素剂。本发明还涉及在该方法中用作中间体的式（Ⅶ）和（Ⅷ）化合物。根据本发明的方法如下：i）式（X）的3-（亚乙基 - 二氧基） - 雌-5（10），9（11） - 二烯-17-与原位形成的乙酸乙酯反应在干燥的四氢呋喃中通过已知的方法，ii）将得到的式（IX）的3-（亚乙基 - 二氧基）-17a-乙炔基-17β-羟基 - 雌-5（10），9（11） - 二烯与苯基亚硫酰氯在三乙胺和乙酸的存在下在二氯甲烷中反应，iii）得到的3-（亚乙基 - 二氧基）-2-（苯基 - 亚磺酰基）-19-去甲基-5（10），9（11），17（ 20），式（VIII）的20-四烯首先与甲醇钠在甲醇中反应，然后与亚磷酸三甲酯反应，iv）得到的3-（亚乙基 - 二氧基）-17a-羟基-20-甲氧基-19-去甲基-5 （10），9（11），式（VII）的20-三烯与氯化氢在甲醇中反应，然后v）得到的3-（亚乙基 - 二氧基）-17a-羟基-19-去甲基-5（10），9（11l） - 二烯-20-酮（VI）与乙二醇二氯甲烷在三甲基邻位甲酸和对甲苯磺酸的方法，vi）得到的式（I）的3,3,20,20-双（亚乙基 - 二氧基）-17α-羟基-19-去甲酚-5（10），9（11） - 二烯（V）在六氯丙酮存在下，通过已知方法与吡啶和二氯甲烷的混合物中的过氧化氢反应，vii）获得的3,3,20,20-双（亚乙基 - 二氧基）-17a-羟基-5,10 从溶液中分离含有大约1：1的5a，10a-和5β，10β-环氧化物的1:1的式（IV）的1-环氧-19-降孕-9（11） - 烯，并与获得的格氏试剂反应在氯化铜（I）催化剂存在下，由4-溴-N，N-二甲基 - 苯胺在四氢呋喃中的溶液，而不用已知方法分离异构体，viii）得到的3,3,20,20-双（亚乙基 - 二氧基）-5α，17α-二羟基-11β-[4-（N，N-二甲基氨基） - 苯基] -19-去甲-9（11） - 烯与硫酸氢钾在水中的反应通过已知方法， ix）得到的11β-[4-（N，N-二甲基氨基） - 苯基] -17a-羟基-19-去甲基-4,9-二烯-3,20 （II）的二酮通过已知方法在高氯酸存在下用乙酸酐乙酰化，最后x）将无溶剂化物的式（I）化合物从所得到的含式（I）化合物的式 1：1乙醇和水的混合物在70℃

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式