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1. 发明申请

WO0053166A3 USE OF CONDENSED 2,3-BENZODIAZEPINE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF DISEASES RELATED TO THE INHIBITION OF LIPID PEROXIDATION 审中-公开
标题翻译：使用稠合的2,3-苯二酮衍生物进行与抑制脂肪过氧相关的疾病的治疗和预防
公开(公告)号：WO0053166A3
公开(公告)日：2000-12-21
申请号：PCT/HU0000011
申请日：2000-02-15
申请人： EGYT GYOGYSZERVEGYESZETI GYAR , RACZNE BAJNOGEL JUDIT , SZENASI GABOR , GIGLER GABOR , LEVAY GYOERGY , SZABO GEZA , TIHANYI KAROLY , EGYED ANDRAS , BARKOCZY JOZSEF , RATKAI ZOLTAN , GREFF ZOLTAN , SCHNEIDER GEZA , SIMIG GYULA , BALAZS LASZLO , DOMAN IMRE , KOTAY NAGY PETER , SERES PETER
发明人： RACZNE BAJNOGEL JUDIT , SZENASI GABOR , GIGLER GABOR , LEVAY GYOERGY , SZABO GEZA , TIHANYI KAROLY , EGYED ANDRAS , BARKOCZY JOZSEF , RATKAI ZOLTAN , GREFF ZOLTAN , SCHNEIDER GEZA , SIMIG GYULA , BALAZS LASZLO , DOMAN IMRE , KOTAY NAGY PETER , SERES PETER
IPC分类号： A61K31/551
CPC分类号： A61K31/551
摘要： The invention relates to the use of 8-substituted-9H-1,3-dioxolo(4,5-h)(2,3)benzodiazepine derivatives of general formula (I) and pharmaceutically acceptable acid addition salts and quaternary ammonium derivatives thereof for the preparation of pharmaceutical compositions suitable for the treatment or prophylaxis of diseases and states related to increased (pathological) lipid peroxidation and diseases caused by increased production of free radicals, e.g. atherosclerosis, pancreatitis, rheumatoid arthritis, cataract, Parkinson's disease, inflammatory diseases (e.g. hepatitis), ischemic heart disease, cerebral ischemia and renal failure.
摘要翻译：本发明涉及通式（I）的8-取代-9,9-1,3-二氧杂环戊烯（4,5-h）（2,3）苯并二氮杂衍生物及其药学上可接受的酸加成盐及其季铵衍生物适用于治疗或预防与增加的（病理性）脂质过氧化作用有关的疾病和状态的药物组合物的制备以及由增加的自由基产生引起的疾病，例如动脉粥样硬化，胰腺炎，类风湿性关节炎，白内障，帕金森病，炎性疾病（例如肝炎），缺血性心脏病，脑缺血和肾衰竭。

2. 发明专利

NZ503300A 8-substituted-9H-1,3-dioxolo[4,5-H],[2,3]benzodiazepine derivatives, as AMPA/kainate receptor inhibitors 未知
公开(公告)号：NZ503300A
公开(公告)日：2001-06-29
申请号：NZ50330098
申请日：1998-08-07
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： TIHANYI KAROLY , VEGH MIKLOS , SIMIG GYULA , BALAZS LASZLO , DOMAN IMRE , GREFF ZOLTAN , KOTAY NAGY PETER , SERES PETER , SZABO GEZA , GACSALYI ISTVAN , GIGLER GABOR , GYERTYAN ISTVAN , LEVAY GYORGY , KOVACS ATTILA , SIMO ANNAMARIA , SZABADOS TAMAS , EGYED ANDRAS , CSELENYAK JUDIT , RATKAI ZOLTAN , BARKOCY JOZEF , SCHNEIDER GEZA
IPC分类号： A61K31/551 , A61P1/08 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/28 , C07D491/04 , C07D491/056 , A61K31/55
摘要： A 8-substituted-9H-1,3-dioxolo-[4,5-H][2,3]-benzodiazepine derivative of the formula I wherein: X is a carbonyl group or a methylene group; R1 is a hydrogen atom, a hydroxy group, an alkoxy group, an alkanoyloxy group, a alkylsulfonyloxy group or a group of the formula -NR4R5; or X forms together with R1 a cyano group, a tetrazolyl group, -CHNOH, -COR6 R4 and R5 are independently, a hydrogen atom or an alkoxy group, an alkanoyl group or an alkyl group optionally substituted by a saturated or unsaturated heterocyclic group having 5 or 6 members and comprising one or two nitrogen atom(s) or a nitrogen atom and an oxygen atom as the heteroatom, or by an N-[phenyl-alky]-N-alkylamino group, wherein the phenyl group is optionally substituted by 1 to 3 alkoxy groups; or R4 and R5 form with the adjacent nitrogen atom and optionally with a further nitrogen atom or an oxygen atom, a saturated or unsaturated heterocyclic group having 5 to 10 members; R6 is a hydroxy group or an alkoxy group, a phenoxy group, a naphthyloxy group, or an amino group optionally substituted by an alkyl group; R2 is a nitro group, an amino group or a alkanoylamino group; R3 is a hydrogen atom, an alkyl group, or a group of the formula -COR7; R7 is a hydrogen atom, an alkyl group optionally substituted by 1 to 3 halo atoms, an alkoxy group, a phenoxy group, a pyridyl group, a phenyl group or a naphthyl group which two latter groups are optionally substituted by 1 to 3 substituents, or a group of the formula -(CH2)n-NR8R9; R8 and R9 are independently a hydrogen atom, an alkyl group optionally substituted by a phenyl group or a saturated heterocyclic group having 5 or 6 members and containing a nitrogen group or a nitrogen and an oxygen group, and said phenyl group is optionally substituted by 1 to 3 alkoxy groups; or R8 and R9 form, together with the adjacent nitrogen atom and optionally a further nitrogen or oxygen atom, a saturated or unsaturated heterocyclic group having 5 or 6 members optionally substituted by a phenyl group that is optionally substituted by 1 to 3 substituents selected from a halo atom or an alkoxy group; n is 0, 1 or 2; Y is a hydrogen atom, or a methyl group; or Y forms together with R3 a valence bond between the carbon atom in position 8 and the nitrogen atom in position 7; and pharmaceutically suitable acid addition salts and quaternary ammonium derivatives thereof. The compounds are useful for treating epilepsy, a neurodegenerative disease or post-stroke conditions.

3. 发明专利

NO20000655L 未知
公开(公告)号：NO20000655L
公开(公告)日：2000-04-10
申请号：NO20000655
申请日：2000-02-09
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： RSTKAI ZOLTSN , BARKOCZY JOZSEF , SCHNEIDER GEZA , CSELENYOK JUDIT , SIMIG GYULA , BALSZS LSSZLO , DOMSN IMRE , GREFF ZOLTSN , NAGY PETER KOTAY , SERES PETER , SZABO GEZA , GACSSLYI ISTVSN , GIGLER GSBOR , GYERTYSN ISTVSN , LEVAY GYOERGY , KOVSCS ATTILA , SIMO ANNAMSRIA , SZABADOS TAMSS , EGYED ANDRSS , VEGH MIKLOS , TIHANYI KSROLY
IPC分类号： A61K31/551 , A61P1/08 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/28 , C07D491/04 , C07D491/056 , A61K31/55
摘要： The disclosure relates to a novel 8-substituted-9H-1,3-dioxolo-[4,5-h][2,3]benzodiazepine compound of formula I and pharmaceutically acceptable quaternary ammonium salts thereof, a process for preparing the same, a pharmaceutical composition containing a 8-substituted-9H-1,3-dioxolo-[4,5-h][2,3]benzodiazepine compound, and a method of treatment using the pharmaceutical composition. A complete description of the compound of formula I is found in the specification. The compounds of the general formula I possess unique competitive AMPA/kainite antagonist properties making them useful in the treatment of diseases where inhibition of the AMPA/kainite receptors may a favorable effect.

5. 发明专利

HUT69165A PROCESS TO PREPARARE 2,2-DIMETHYL-5-(2,5-DIMETHYL PHENOXI)-PENTANE ACID 未知
公开(公告)号：HUT69165A
公开(公告)日：1995-08-28
申请号：HU9300959
申请日：1993-04-02
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： SCHNEIDER GEZA , LADANYI LASZLO , SOHAR PAL , KOTAY NAGY PETER , BLASKO GABOR , BALOGH GYULA , KOEVESDI ISTVAN
IPC分类号： C07C59/68

6. 发明专利

HUT67085A PROCESS FOR PREPARING 1-[/2S/-METHYL-3-MERCAPTO-PROPIONYL]-PYRROLIDINE-/2S/-CARBOXYLIC ACID 未知
公开(公告)号：HUT67085A
公开(公告)日：1995-01-30
申请号：HU9200837
申请日：1992-03-13
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： BECK IVAN , JAKFALVI ELEMER , DIETZ ANDRAS , DINNYES ISTVANNE , SCHNEIDER GEZA , KOVACS JOZSEFNE , BLASKO GABOR , UERMOES LASZLONE
IPC分类号： A61K31/40 , A61K31/401 , A61P9/12 , C07D207/16

7. 发明专利

ZA917517B Process for preparing 1-((2s)-3-merkapto-methyl-1-oxopropyl)-l-proline 未知
公开(公告)号：ZA917517B
公开(公告)日：1994-08-26
申请号：ZA917517
申请日：1991-09-20
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： SCHNEIDER GEZA , BLASKO GABOR , KOVACS AGNES , UERMOES GABRIELLA , KUN JUDIT , DINNYES ILMA , BECK IVAN , JAKFALVI ELEMER , DIETZ ANDRAS
IPC分类号： C07D207/16 , C07D
摘要： The invention relates to a novel process for preparing 1-[(2S)-3-mercapto-2-methyl-1-oxopropyl]-L-proline (captopril) of formula (I). (I) which comprises hydrogenolysing 1-[(2S)-2-methyl-1-oxo-3-rhodanidopropyl]-L-proline of formula (II) (II) in an inert solvent, in the presence of a catalyst, at a temperature of 50 DEG to 120 DEG C. under a pressure of 105 to 107 Pa. The above compound of formula (II) is new and can be prepared by acylating L-proline with a reactive acylating derivative of (2S)-2-methyl-3-rhodanido-propionic acid of formula (III). (III)

8. 发明专利

ES2035798B1 未知
公开(公告)号：ES2035798B1
公开(公告)日：1994-02-16
申请号：ES9102086
申请日：1991-09-20
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： SCHNEIDER GEZA , BLASKO GABOR , KOVACS AGNES , URMOS GSABRIELLA , KUN JUDIT , DINNYES ILMA , BECK IVAN , JAKFALVI ELEMER , DIETZ ANDRAS
IPC分类号： C07D207/16
摘要： The invention relates to a novel process for preparing 1-[(2S)-3-mercapto-2-methyl-1-oxopropyl]-L-proline (captopril) of formula (I). (I) which comprises hydrogenolysing 1-[(2S)-2-methyl-1-oxo-3-rhodanidopropyl]-L-proline of formula (II) (II) in an inert solvent, in the presence of a catalyst, at a temperature of 50 DEG to 120 DEG C. under a pressure of 105 to 107 Pa. The above compound of formula (II) is new and can be prepared by acylating L-proline with a reactive acylating derivative of (2S)-2-methyl-3-rhodanido-propionic acid of formula (III). (III)

9. 发明专利

HU208419B PROCESS FOR SEPARATING 1-PROLIN 未知
公开(公告)号：HU208419B
公开(公告)日：1993-10-28
申请号：HU9204066
申请日：1992-12-21
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： BECK IVAN , BOCSIK LASZLO , DIETZ ANDRAS , DROZDIK GYOERGY , EGRI JANOS , JAKFALVI ELEMER , KOVACS JUDIT MARIA , SCHNEIDER GEZA , SZEMMELROTH JENOE , TELEKI JOZSEF
IPC分类号： C07D207/16

10. 发明专利

GB2264945A A PROCESS FOR PREPARING 1-[/2S/-METHYL-3-MERCAPTOPROPIONYL]-PYRROLIDINE-/2S /-CARBOXYLIC ACID 未知
公开(公告)号：GB2264945A
公开(公告)日：1993-09-15
申请号：GB9304757
申请日：1993-03-09
申请人： EGYT GYOGYSZERVEGYESZETI GYAR
发明人： SCHNEIDER GEZA , BLASKO GABOR , KOVACS AGNES , RMOES GABRIELLA , BECK IVAN , DINNYES ILMA , JAKFALVI ELEMER , DIETZ ANDRAS
IPC分类号： A61K31/40 , A61K31/401 , A61P9/12 , C07D207/16
摘要： The invention relates to a novel process for preparing 1-[/2S/-methyl-3-mercaptopropionyl]-pyrrolidine-/2S/-carboxylic acid of the formula I in which 1-[/2S/-methyl-3-thiocyanatopropionyl]-pyrrolidine-/2S/-carboxylic acid of the formula II is dissolved in an aqueous mineral acid, the solution obtained is diluted with water and the 1-[/2S/-methyl-3- carbamoylthio-propionyl]-pyrrolidine-/2S/-carboxylic acid of the formula III that forms is hydrolized with an aqueous solution of a base.t

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