公开(公告)号：EP1962849B1

公开(公告)日：2009-09-30

申请号：EP06831520.9

申请日：2006-12-19

申请人： Richter Gedeon Nyrt.

发明人： KESERÜ, György ,  WÉBER, Csaba ,  BIELIK, Attila ,  BOBOK, Amrita, Ágnes ,  GÁL, Krisztina ,  MESZLÉNYINÉ SIPOS, Márta ,  MOLNÁR, László ,  VASTAG, Mónika

IPC分类号： A61K31/4706 ,  A61K31/4709 ,  A61K31/4741 ,  C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  A61P25/00

CPC分类号： C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D405/12 ,  C07D491/04 ,  C07D491/10

摘要： Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation, to the intermediates of the preparation process, to the pharmaceutical formulations containing these compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.

公开(公告)号：EP2072041A1

公开(公告)日：2009-06-24

申请号：EP08462008.7

申请日：2008-10-06

申请人： Richter Gedeon Nyrt.

发明人： Bódis, Attila ,  Greiner, István ,  Nagy Kasza, Jonathán Mihály

IPC分类号： A61K9/16 ,  A61K9/28

CPC分类号： A61K9/2846 ,  A61K9/1694 ,  A61K9/2018 ,  A61K31/565

摘要： The invention relates to drospirenone containing film-coated tablet with improved resistance against the environmental influences, especially against atmospheric humidity. The invention further relates to a method for the preparation film-coated tablet cores whereby applying the active agent to the core may be accomplished with increased safety.

摘要翻译： 本发明涉及屈螺酮包含薄膜包衣片剂具有抗环境影响改善的耐，爱特别是抗大气湿度。 本发明还涉及到用于制备薄膜包衣片核心的方法，由此施加-活性剂的芯可以具有增加的安全性实现。

公开(公告)号：EP1915347B1

公开(公告)日：2009-01-28

申请号：EP06765404.6

申请日：2006-07-27

申请人： Richter Gedeon Nyrt.

发明人： FISCHER, János ,  KIS-VARGA, Istvánné ,  SZABO, György ,  LEIBINGER, János

IPC分类号： C07D231/12 ,  A61K31/4155

CPC分类号： C07D231/12

摘要： The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2- COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.

公开(公告)号：EP2013203A2

公开(公告)日：2009-01-14

申请号：EP07733855.6

申请日：2007-05-02

申请人： Richter Gedeon Nyrt.

发明人： NEU, József ,  TÖRLEY, József ,  GARADNAY, Sándor

IPC分类号： C07D417/12

CPC分类号： C07D417/12

摘要： The present invention provides a novel, industrially easily realisable and economically preferable process for production of pure 5-{2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one i.e., ziprasidone hydrochloride shown in the reaction scheme (II), (III), (IV), (V) and (VI). According to the invention the intermediate compound 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) is produced from 5-(2-bromoacethyl)-6-chloro-1,3-dihydro-2H-indole-2-one of Formula (IV). The highly pure ziprasidone base of Formula (II) is obtained in the reaction of 3-piperazinyl-1,2-benzisothiazol of Formula (VI) with 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) in an organic solvent or organic solvent mixture.

公开(公告)号：EP1711501B1

公开(公告)日：2009-01-14

申请号：EP05708499.8

申请日：2005-01-31

申请人： Richter Gedeon Nyrt.

发明人： CZIBULA, László ,  DOBAY, László ,  SZÖKE, Katalin ,  WERKNÉ PAPP, Éva ,  NAGYNÉ BAGDY, Judit ,  TÁRKÁNYI, Gábor

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  C07C233/43

摘要： The invention relates to N- [3- (3-cyanopyrazolo [1,5-a] pyrimidin-7-yl) - phenyl]-N-ethyl-acetamide of formula (IV) containing less than 0.2 % impurities, which is suitable for therapeutic application. Furthermore the invention relates to a process for the synthesis of therapeutically applicable compound of formula (IV) containing less than 0.2 % impurities by reacting the new intermediate N-{3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl­acetamide hydrochloride of formula (II) and 3-amino-4-pyrazol-carbonitrile base of formula (III) in an acid free medium. The invention also relates to the new N- {3- [3- (dimethylamino) -1- oxo -2- ­propenyl]phenyl } -N-ethyl-acetamide hydrochloride of formula (II). The invention also relates to a process for the synthesis of the new N- [3- [3, (dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl-acetamide hydrochloride of formula (II) having a purity of more than 99.5 %. Furthermore the invention relates to N-{3-[3-cyanopyrazolo (1,5-a) pyrimidin]­6 -yl-3- [ (3-N-ethyl-acetamido-phenyl) -3-oxo-propen-1-yl] - (pyrimidin-7-yl) -phenyl} - N-ethyl-acet-amide of formula (V), which is an isolated new impurity formed in 0.07 % yield during the synthesis of compound of formula (IV).

公开(公告)号：EP1587814B1

公开(公告)日：2009-01-14

申请号：EP04705466.3

申请日：2004-01-27

申请人： Richter Gedeon Nyrt.

发明人： NEU, József ,  FISCHER, János ,  FODOR, Tamás ,  TÖRLEY, József ,  GIZUR, Tibor ,  LÉVAI, Sándor ,  DEMETER, Àdám ,  PERÉNYI, Éva

IPC分类号： C07F9/58 ,  C07F9/38

CPC分类号： C07F9/3873 ,  C07F9/582

摘要： Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof - wherein the meaning of R is 3'-pyridyl or 2'-amino-ethylidene group - from compounds of formula (II) - wherein the meaning of R is as described above - or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.

公开(公告)号：EP1971609A1

公开(公告)日：2008-09-24

申请号：EP06831518.3

申请日：2006-12-19

申请人： Richter Gedeon NYRT

发明人： NÓGRÁDI, Katalin ,  WÁGNER, Gábor ,  KESERÜ, György ,  BIELIK, Attila ,  GÁTI, Tamás ,  HÁDA, Viktor ,  KÓTI, János ,  GÁL, Krisztina ,  VASTAG, Mónika ,  BOBOK, Amrita, Ágnes

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P25/28

CPC分类号： C07D495/04

摘要： The present invention relates to new mGluRl and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH2)n, CH=CH, NH, N(CH3), NHCH2, N(CH3)CH2, O, OCH2, CH2COO, NHCH2COO; n is an integer of O to 2; Y represents a subtituent selected from H, CH3, F, Cl, Br; Z is H or CH3; R is alkyl, cycloalkyl, an optionally substituted phenyl or an optionally substituted heteroaryl, and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.

公开(公告)号：EP1966142A2

公开(公告)日：2008-09-10

申请号：EP06831519.1

申请日：2006-12-19

申请人： Richter Gedeon NYRT

发明人： BEKE, Gyula ,  BOZÓ, Éva ,  CZÍRA, Gábor ,  ÉLES, János ,  FARKAS, Sándor ,  HORNOK, Katalin ,  SCHMIDT, Éva ,  SZENTIRMAY, Éva ,  VÁGÓ, István ,  VASTAG, Mónika

IPC分类号： C07D213/74 ,  C07D221/12 ,  C07D295/12 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  A61K31/473 ,  A61P25/02

CPC分类号： C07D401/12 ,  C07D213/74 ,  C07D221/12 ,  C07D295/135 ,  C07D401/10 ,  C07D401/14

摘要： The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specificition, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.

公开(公告)号：EP1963354A2

公开(公告)日：2008-09-03

申请号：EP06808800.4

申请日：2006-10-11

申请人： Richter Gedeon NYRT

发明人： DANCSI, Lajosné ,  MAHÓ, Sándor ,  ARANYI, Antal ,  HORVÁTH, János

IPC分类号： C07J41/00

CPC分类号： C07J41/0094

摘要： The invention relates to a process for the synthesis of high purity 17α- cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I)

公开(公告)号：EP1963260A1

公开(公告)日：2008-09-03

申请号：EP06831516.7

申请日：2006-12-18

申请人： Richter Gedeon NYRT

发明人： BÓDI, József ,  ÉLES, János ,  SZÖKE, Katalin ,  VUKICS, Krisztina ,  GÁTI, Tamás ,  TEMESVÁRI, Krisztina ,  KISS-BARTOS, Dorottya

IPC分类号： C07D205/08 ,  C07D413/06 ,  C07D317/30 ,  C07D405/06 ,  C07F7/02

CPC分类号： C07D205/08 ,  C07D317/30 ,  C07D405/06 ,  C07D413/06 ,  C07F7/186 ,  C07F7/1892

摘要： This invention provides a novel, industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)- [3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) wherein, the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, Rl, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert.buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group.