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1. 发明申请

WO1995001357A1 OPTICALLY ACTIVE 1-(4-NITROPHENYL)-4-METHYL-7,8-METHYLENEDIOXY-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：光活性1-（4-硝基苯基）-4-甲基-7,8-甲基二氧代-3,4-二氢-5H- 2,3-苯并二氮杂及其制备方法
公开(公告)号：WO1995001357A1
公开(公告)日：1995-01-12
申请号：PCT/HU1994000024
申请日：1994-06-30
申请人： GYOGYSZERKUTATO INTÉZET KFT. , LING, István , HAMORI, Tamás , BOTKA, Péter , SOLYOM, Sándor , SIMAY, Antal , MORAVCSIK, Imre
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07D491/056
CPC分类号： C07D491/04
摘要： The invention relates to the (+)- and (-)-enantiomers of the compounds of formula (I) as well as a process for the preparation of these enantiomers. This process comprises reducing 1-(4-nitrophenyl)-4-methyl-7,8-methylenedioxy-5H &cir& _-2,3-benzodiazepine of formula (II) by using an adduct formed from an (R)- or (S)-, respectively, 2-amino-1,1-diphenyl-alkan-1-ol derivative of general formula (III), wherein R1 and R2, which are different, stand for a straight or branched chain C1-4 alkyl group or an unsubstituted phenyl or benzyl group, with one molar equivalent of borane or a borane complex. The enantiomers of the compound of formula (I) are valuable intermediates in the synthesis of therapeutically active compounds.
摘要翻译：本发明涉及式（I）化合物的（+） - 和（ - ） - 对映异构体以及制备这些对映异构体的方法。该方法包括通过使用由（R） - 或（S（R））形成的加合物来还原式（II）的1-（4-硝基苯基）-4-甲基-7,8-亚甲基二氧基-5H和） - 分别为通式（III）的2-氨基-1,1-二苯基 - 烷-1-醇衍生物，其中不同的R 1和R 2表示直链或支链C 1-4烷基或未取代的苯基或苄基，与一摩尔当量的硼烷或硼烷络合物。式（I）化合物的对映异构体是合成治疗活性化合物的有价值的中间体。

2. 发明申请

WO1996038441A1 3(2H)-PYRIDAZINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： 3（2H） - 吡啶酮衍生物和含有这些化合物的药物组合物
公开(公告)号：WO1996038441A1
公开(公告)日：1996-12-05
申请号：PCT/HU1996000030
申请日：1996-05-28
申请人： GYOGYSZERKUTATO INTÉZET KFT , MATYUS, Péter , HARSING, László , KARIM, Mariann , KOSARY, Judit , PAPP, Agnes , SIMAY, Antal , TILAHUN, Yemane , TOMORI, Éva , HORVATH, Edit , HORVATH, Katalin , VARGA, Ildikó , ZARA, Erzsébet , BIDLO, Margit , DRUGA, Alice , RABLOCZKY, György , VARGA, Márta , KARPATI, Egon , KASZTREINER, Endre , KIRALY, István , MATHÉ, Ildikó , MATHÉ, György , SEBESTYÉN, László , MAKK, Nándor
发明人： GYOGYSZERKUTATO INTÉZET KFT
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D319/20
摘要： The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (1), and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess alpha 1- and alpha 2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.
摘要翻译：本发明涉及式（1）的R-2- [3 - （[1,4]苯并二恶烷-2-基甲基氨基）-1-丙基] -3（2H） - 哒嗪酮，以及S-2- [3- （2）的（[1,4]苯并二恶烷-2-基甲基氨基）-1-丙基] -3（2H） - 哒嗪酮及其酸加成盐以及含有这些化合物的药物组合物。此外，本发明涉及制备上述化合物的方法。式（4）和（5）的新起始化合物也参与本发明的范围。根据本发明的化合物具有α1-和α2-肾上腺素受体拮抗作用和泌尿生殖选择性。因此，它们可用于治疗良性前列腺增生。

3. 发明申请

WO1988002254A1 NEW PSYCHOSTIMULANT AGENT 审中-公开
标题翻译：新的PSYCHOSTIMULANT代理
公开(公告)号：WO1988002254A1
公开(公告)日：1988-04-07
申请号：PCT/HU1987000040
申请日：1987-09-25
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , KNOLL, József , SIMAY, Antal , SZINNYEI, Éva , SOMFAI, Éva , TÖRÖK, Zoltán , MOZSOLITS, Károly , BERGMANN, János
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： A61K31/135
CPC分类号： A61K31/135
摘要： Pharmaceutical composition comprising as active ingredient a compound of general Formula (I), wherein R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms; R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms, alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms, with the proviso that groups R and R together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the general Formula (I) by methods known per se. The compounds of the general Formula (I) are psychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficites of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.
摘要翻译：药物组合物，其包含作为活性成分的通式（I）的化合物，其中R 1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R 2代表包含1至8个碳原子的直链或支链烷基，由卤素，羟基，具有1至4个碳原子的烷氧基或1或2个苯基取代的1至8个碳原子的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少三个碳原子。本发明还涉及通过本身已知的方法制备通式（I）的化合物的方法。通式（I）的化合物是具有新的效应谱系的精神兴奋剂，其可用于治疗增加心理活动（学习和保留）和用于治疗抑郁症的学习和保留的临床模式，如阿尔茨海默病，并且没有已知的兴奋剂的副作用（例如由于儿茶酚胺释放）。

4. 发明申请

WO1997028135A1 2,3-BENZODIAZEPINE DERIVATIVES AND THEIR USE AS AMPA-RECEPTOR INHIBITORS 审中-公开
标题翻译： 2,3-苯并二氮杂衍生物及其作为AMPA受体抑制剂
公开(公告)号：WO1997028135A1
公开(公告)日：1997-08-07
申请号：PCT/DE1997000225
申请日：1997-01-29
申请人： SCHERING AKTIENGESELLSCHAFT , LING, István , ABRAHAM, Gizella , SOLYOM, Sándor , HAMORI, Tamás , TARNAWA, István , BERZSENYI, Pál , ANDRASI, Ferenc , CSUZDI, Emese , SZÖLLOSY, Márta , SIMAY, Antal , PALLAGI, István , HORVATH, Katalin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D243/02
CPC分类号： C07D243/02
摘要： The invention concerns compounds of formula (I), in which: X designates hydrogen or halogen; Y designates -NR - or -N=; R , R and R designate hydrogen or different substituents; R designates optionally substituted C1-C6 alkyl; R designates hydrogen; or R and R together designate oxygen; R designates C1-C4 alkyl; and (a) designates a double bond or single bonds. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.
摘要翻译：式（I）其中X是氢或卤素的化合物中，Y是-NR <3> - 或-N =，R <1>，R <2>和R <3>为氢或各种取代基，R <4>是任选取代的 C1-C6烷基，R <5>是氢或R <4>和R <5>一起是氧，R <6> C 1-4烷基和（a）表示双键或单键，由于它们的AMPA的非竞争性抑制受体作为用于中枢神经系统疾病的治疗药是有用的。

5. 发明申请

WO1997028163A1 CONDENSED 2,3-BENZODIAZEPINE DERIVATIVES AND THEIR USE AS AMPA-RECEPTOR INHIBITORS 审中-公开
标题翻译：简明2,3-苯二氮类衍生物及其作为AMPA受体抑制剂
公开(公告)号：WO1997028163A1
公开(公告)日：1997-08-07
申请号：PCT/DE1997000234
申请日：1997-01-29
申请人： SCHERING AKTIENGESELLSCHAFT , CSUZDI, Ernese , HAMORI, Tamás , ABRAHAM, Gizella , SOLYOM, Sándor , TARNAWA, István , BERZSENYI, Pál , ANDRASI, Ferenc , LING, István , SIMAY, Antal , GAL, Melinda , HORVATH, Katalin , SZENTKUTI, Eszter , SZÖLLOSY, Márta , PALLAGI, István
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D491/14
CPC分类号： C07D487/04 , C07D491/04 , C07D491/14
摘要： The invention concerns compounds of formula (I), in which R , R , R and R mean hydrogen or different substituents; X means hydrogen or halogen; Y means C1-6 alkoxy or X and Y together mean -O-(CH2)n-O-; n means 1, 2 or 3; and A together with nitrogen forms a saturated or unsaturated five-member heterocycle which can contain between 1 and 3 nitrogen atoms and/or an oxygen atom and/or one or two carbonyl groups. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.
摘要翻译：式（I）其中，R <1>，R <2>，R <3>和R <4>是氢或不同的取代基，X为氢或卤素的化合物中，Y是C 1-6 - 烷氧基或X和Y一起是-O - （CH 2）N O-，n为1，2或3，A是饱和或与氮其可以1-3个氮原子和/或氧原子和/或含有一个或两个羰基，是由于不饱和的五元杂环一起他们对AMPA受体的非竞争性抑制可以用作药物用于治疗中枢神经系统的疾病。

6. 发明申请

WO1996004283A1 NEW 3-SUBSTITUTED 3H-2,3-BENZODIAZEPINE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS 审中-公开
标题翻译： NEW 3-取代3H-2,3-苯并二氮杂衍生物，它们的生产和用作药物
公开(公告)号：WO1996004283A1
公开(公告)日：1996-02-15
申请号：PCT/DE1995001029
申请日：1995-07-28
申请人： SCHERING AKTIENGESELLSCHAFT , HAMORI, Tamás , TARNAWA, István , SOLYOM, Sándor , BERZSENYI, Pál , BIRKAS FALGLNÉ, Erzsébet , ANDRASI, Ferenc , LING, István , HASKO, Tibor , KAPUS, Gábor , CSUZDL, Emese , SZO"e;LLO"e;SY, Márta , ERDO"e; VLDANÉ, Franciska , SIMAY, Antal , ZOLYOMI, Gábor
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D491/056
CPC分类号： C07D491/04
摘要： New 3-substituted 3H-2,3-benzodiazepine derivatives are disclosed having the general formula (I), in which R , R , R , R , R , R , R and n have the meanings given in the description, as well as their preparation and use as medicaments.
摘要翻译：有新的3-取代的通式（I）的3H-2,3-苯并二氮杂衍生物，其中R <1>，R <2>，R <3>，R <4>，R <5> - [R <6 >，R <7>和n具有在说明书中给出的含义，它们的制备和它们作为药物的用途。

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