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1. 发明授权

US5807851A 2,3-Benzodiazepine Derivatives as non-competitive AMPA 失效
标题翻译： 2,3-苯并二氮杂衍生物作为非竞争性AMPA
公开(公告)号：US5807851A
公开(公告)日：1998-09-15
申请号：US832777
申请日：1997-04-04
申请人： Istvan Ling , Gizella Abraham , Pal Berzsenyi , Istvan Tarnawa , Sandor Solyom , Ferenc Andrasi , Tamas Hamori , Emese Csuzdi , Katalin Horvath , Melinda Gal , Imre Moravcsik , Marta Szollosy
发明人： Istvan Ling , Gizella Abraham , Pal Berzsenyi , Istvan Tarnawa , Sandor Solyom , Ferenc Andrasi , Tamas Hamori , Emese Csuzdi , Katalin Horvath , Melinda Gal , Imre Moravcsik , Marta Szollosy
IPC分类号： A61K31/55 , A61K31/551 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D243/02 , C07D243/04 , A01N43/62 , C07D243/00
CPC分类号： C07D243/02
摘要： Derivatives of 2,3-benzodiazepine are substituted by one or two halogen atom(s) and have the general formula ##STR1## These derivatives are non-competitive AMPA antagonists and are used in pharmaceutical compositions. A process to make the 2,3-benzodiazepine derivatives includes converting starting compounds which are substituted by one or two halogen groups and have the general formula ##STR2##
摘要翻译： 2,3-苯并二氮杂的衍生物被一个或两个卤素原子取代并具有通式<这些衍生物是非竞争性的AMPA拮抗剂，并用于药物组合物中。制备2,3-苯并二氮杂衍生物的方法包括转化被一个或两个卤素基团取代的起始化合物，并具有通式

2. 发明授权

US06600036B2 Condensed 2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors 失效
标题翻译：缩合2,3-苯并二氮杂衍生物及其作为AMPA受体抑制剂的用途
公开(公告)号：US06600036B2
公开(公告)日：2003-07-29
申请号：US09993646
申请日：2001-11-27
申请人： Ernese Csuzdi , Tamas Hamori , Gizella Abraham , Sandor Solyom , Istvan Tarnawa , Pal Berzsenyi , Ferenc Andrasi , Istvan Ling , Antal Simay , Melinda Gal , Katalin Horvath , Eszter Szentkuti , Marta Szollosy , Istvan Pallagi
发明人： Ernese Csuzdi , Tamas Hamori , Gizella Abraham , Sandor Solyom , Istvan Tarnawa , Pal Berzsenyi , Ferenc Andrasi , Istvan Ling , Antal Simay , Melinda Gal , Katalin Horvath , Eszter Szentkuti , Marta Szollosy , Istvan Pallagi
IPC分类号： C07D24310
CPC分类号： C07D487/04 , C07D491/04 , C07D491/14
摘要： Compounds of formula I are described, their production and use in pharmaceutical agents.
摘要翻译：描述了式I化合物，其制备和在药剂中的用途。

3. 发明授权

US5756495A 3-substituted 3H-2, 3-benzodiazepine derivatives, the production and use as pharmaceutical agents 失效
标题翻译： 3-取代的3H-2,3-苯并二氮杂衍生物，生产和用作药剂
公开(公告)号：US5756495A
公开(公告)日：1998-05-26
申请号：US776536
申请日：1997-01-31
申请人： Tamas Hamori , Istvan Tarnawa , Sandor Solyom , Pal Berzsenyi , Erzsebet Birkas , Ferenc Andrasi , Istvan Ling , Tibor Hasko , Gabor Kapus , Emese Csuzdl , Marta Szollosy , Franciska Erdo , Antal Simay , Gabor Zolyomi
发明人： Tamas Hamori , Istvan Tarnawa , Sandor Solyom , Pal Berzsenyi , Erzsebet Birkas , Ferenc Andrasi , Istvan Ling , Tibor Hasko , Gabor Kapus , Emese Csuzdl , Marta Szollosy , Franciska Erdo , Antal Simay , Gabor Zolyomi
IPC分类号： A61K31/4162 , A61K31/55 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P39/02 , C07D491/04 , C07D491/056 , C07D491/00
CPC分类号： C07D491/04
摘要： New 3-substituted 3H-2,3-benzodiazepine derivatives of general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and n have the meanings indicated in the description, their production as well as their use as pharmaceutical agents are described.
摘要翻译： PCT No.PCT / DE95 / 01029 Sec。 371日期1997年4月23日 102（e）日期1997年4月23日PCT提交1995年7月28日PCT公布。出版物WO96 / 04283 日期1996年2月15日通式Ⅰ的新的3-取代的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具有描述，他们的生产以及它们作为药剂的用途被描述。

4. 发明申请

US20080269202A1 Novel 2,3-benzodiazepine derivatives and their use as antipsychotic agents 审中-公开
标题翻译：新型2,3-苯并二氮杂衍生物及其作为抗精神病药的用途
公开(公告)号：US20080269202A1
公开(公告)日：2008-10-30
申请号：US12080418
申请日：2008-04-02
申请人： Emese Csuzdi , Sandor Solyom , Pal Berzsenyi , Ferenc Andrasi , Istvan Sziraki , Katalin Horvath , Zoltan Nagy
发明人： Emese Csuzdi , Sandor Solyom , Pal Berzsenyi , Ferenc Andrasi , Istvan Sziraki , Katalin Horvath , Zoltan Nagy
IPC分类号： A61K31/551 , C07D243/00 , A61P25/00
CPC分类号： C07D243/02 , C07D401/06 , C07D403/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D419/04
摘要： Disclosed are novel 2,3-benzodiazepine derivatives and methods of making the same.
摘要翻译：公开了2,3-苯并二氮杂衍生物及其制备方法。

5. 发明申请

US20070027143A1 Novel substituted 2,3-benzodiazepine derivatives 审中-公开
标题翻译：新型取代的2,3-苯并二氮杂衍生物
公开(公告)号：US20070027143A1
公开(公告)日：2007-02-01
申请号：US10771847
申请日：2004-02-03
申请人： Sandor Solyom , Gizella Abraham , Tamas Hamori , Pal Berzsenyl , Fenrec Andrasi , Istvan Kurucz
发明人： Sandor Solyom , Gizella Abraham , Tamas Hamori , Pal Berzsenyl , Fenrec Andrasi , Istvan Kurucz
IPC分类号： A61K31/5513 , A61K31/551 , C07D491/02
CPC分类号： C07D417/04 , C07D243/02 , C07D491/04
摘要： The invention relates to new 2,3-benzodiazepine derivatives of formula (I), isomers and acid addition salts thereof and to pharmaceutical compositions containing the same, as well as to pharmaceutical compositions and methods of using the same suitable for treating conditions associated with muscle spasms, epilepsy, acute and chronic forms of neurodegenerative diseases as well as preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders.
摘要翻译：本发明涉及式（I）的新的2,3-苯并二氮杂衍生物，其异构体及其酸加成盐以及含有它们的药物组合物，以及适用于治疗与肌肉相关的病症的药物组合物和方法痉挛，癫痫，急性和慢性形式的神经变性疾病以及预防，治疗或缓解急性和慢性炎症性疾病的症状。

6. 发明授权

US4668437A Novel 20 benzcylamino pregnene derivatives and process for preparing same 失效
标题翻译：新型20苄基氨基孕烯衍生物及其制备方法
公开(公告)号：US4668437A
公开(公告)日：1987-05-26
申请号：US775347
申请日：1985-09-11
申请人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago
发明人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago
IPC分类号： C07J5/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J
CPC分类号： C07J33/007 , C07J41/005 , C07J43/003 , C07J5/0015
摘要： The invention relates to new pregnene derivatives of the general formula (I), ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for a hydrogen atom or a C.sub.2-4 alkanoyl group;R.sup.3 stands for a hydrogen atom, a hydroxyl group or a C.sub.2-4 alkanoyloxy group;A represents a ring of the general formula (1) ##STR2## or a ring of the general formula (2), ##STR3## wherein R.sup.4 means a hydrogen atom or a methyl group;R.sup.5 stands for a hydroxyl group, a C.sub.2-4 alkanoyloxy group or a C.sub.1-3 alkoxy group;R.sup.6 means a hydroxyl group, a C.sub.2-4 alkanoyloxy group, a C.sub.1-3 alkoxy group, an oxo group or a C.sub.2-3 alkylenedithio group; the dotted line optionally represents one or more additional valence bonds, with the proviso that, when the dotted line between C.sub.9 and C.sub.11 represents an additional valence bond, then R.sup.3 stands for a hydrogen atom; and the wavy line shows that the given substituent can be bound to the carbon atom in two alternative spatial arrangements,as well as to their stereoisomers and the mixture of these stereoisomers.The compounds of the general formula (I) are valuable intermediates for the synthesis of known biologically active 21-hydroxyprogesterone derivatives.
摘要翻译：本发明涉及通式（I）的新孕烯衍生物，其中R1代表C1-4烷基; R2代表氢原子或C2-4烷酰基; R3代表氢原子，羟基或C2-4烷酰氧基; A表示通式（1）的环，（1）或通式（2）的环，其中R 4表示氢原子或甲基; R5代表羟基，C2-4烷酰氧基或C1-3烷氧基; R6表示羟基，C2-4烷酰氧基，C1-3烷氧基，氧代基或C2-3亚烷基二硫基; 虚线可选地表示一个或多个另外的价键，条件是当C9和C11之间的虚线表示另外的价键时，则R3代表氢原子; 并且波浪线表示给定的取代基可以以两种可选的空间排列结合于碳原子，以及它们的立体异构体和这些立体异构体的混合物。通式（I）的化合物是合成已知生物活性的21-羟孕酮衍生物的有价值的中间体。

7. 发明授权

US4328221A Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof 失效
标题翻译：取代的类固醇 - 螺恶唑烷酮衍生物及其制备方法
公开(公告)号：US4328221A
公开(公告)日：1982-05-04
申请号：US220139
申请日：1980-12-24
申请人： Katalin Szilagyi nee Farago , Sandor Solyom , Lajos Toldy , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Katalin Szilagyi nee Farago , Sandor Solyom , Lajos Toldy , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： A61K31/58 , A61P7/10 , A61P9/12 , C07J43/00
CPC分类号： C07J43/006
摘要： Compounds of the formula (I) having aldosterone-antagonizing activity are disclosed ##STR1## wherein R.sub.3 and R.sub.4 are each C.sub.1 to C.sub.3 alkyl; andZ is one of the following groups ##STR2## wherein R.sub.1 is hydrogen or methyl;R.sub.6 is hydrogen, C.sub.1 to C.sub.3 alkylthio or C.sub.2 to C.sub.4 acylthio; andX is oxo, hydroximino, C.sub.1 to C.sub.3 alkoxyimino, carboxy-alkoxyimino wherein the alkoxy has 2 to 4 carbon atoms or a salt-converted carboxy-alkoxy-imino wherein the alkoxy has 2 to 4 carbon atoms.
摘要翻译：公开了具有醛固酮拮抗活性的式（I）化合物，其中R 3和R 4各自为C 1至C 3烷基; （a）其中R1是氢或甲基;（e）其中R1是氢或甲基;和（c） R6是氢，C1-C3烷硫基或C2-C4酰硫基; 并且X是氧代，肟基，C 1至C 3烷氧基亚氨基，其中烷氧基具有2至4个碳原子的羧基 - 烷氧基亚氨基或其中烷氧基具有2至4个碳原子的盐转化的羧基 - 烷氧基亚氨基。

8. 发明授权

US4342754A Steroid-spiro-oxathiazolidine derivatives and a process for the preparation thereof 失效
标题翻译：类固醇 - 螺 - 恶噻唑烷衍生物及其制备方法
公开(公告)号：US4342754A
公开(公告)日：1982-08-03
申请号：US242711
申请日：1981-03-11
申请人： Sandor Solyom , Katalin Szilagyi nee Farago , Lajos Toldi , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Sandor Solyom , Katalin Szilagyi nee Farago , Lajos Toldi , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： A61K31/58 , A61P7/10 , C07J41/00 , C07J43/00
CPC分类号： C07J41/0088 , C07J43/006 , Y10S514/869
摘要： New steroid-spiro-oxathiazolidine derivatives pharmaceutical compositions containing the same, and to a process for the preparation thereof are disclosed.The new compounds have antimineral corticoide effects and have the following formula (I), ##STR1## wherein R.sub.1 is a C.sub.1-3 alkyl or a C.sub.2-4 alkenyl group, andZ is a group of the formulae (II) to (VI), ##STR2## wherein R.sub.2 is methyl or ethyl,R.sub.3 is hydrogen or methylR.sub.4 is hydrogen, a C.sub.1-3 alkyl group, a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group, a C.sub.2-4 alkylcarbonyl group, a C.sub.2-4 alkoxycarbonyl group or a C.sub.3-6 carboxyalkylcarbonyl group, andthe dotted lines may represent additional valence bonds, with the proviso that if Z is a group of the formula (VI), a double bond exists between the carbon atoms in positions 4 and 5 or 5 and 6, andif R.sub.4 is a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group or a C.sub.3-6 carboxyalkylcarbonyl group, the compounds may also be formed as their salts.
摘要翻译：公开了新的类固醇 - 螺 - 恶唑烷衍生物药物组合物及其制备方法。新化合物具有抗皮质素的作用，具有下式（I），其中R 1为C 1-3烷基或C 2-4链烯基，Z为式（II）〜（VI），其中R2是甲基或乙基，R3是氢或甲基R4是氢，（VI）其中R2是甲基或乙基， C 1-3烷基，二（C 1-4烷基） - 氨基-C 1-4烷基，C 2-4烷基羰基，C 2-4烷氧基羰基或C 3-6羧基烷基羰基，虚线可以代表额外的价键，条件是如果Z是式（VI）的基团，则在4位和5位或5位和6位之间的碳原子之间存在双键，如果R4是二 - （C1- 4烷基） - 氨基-C 1-4烷基或C 3-6羧基烷基羰基，化合物也可以形成为其盐。

9. 发明授权

US4218446A Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof 失效
标题翻译：取代的类固醇 - 螺恶唑烷酮衍生物及其制备方法
公开(公告)号：US4218446A
公开(公告)日：1980-08-19
申请号：US25080
申请日：1979-03-29
申请人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： C07J31/00 , A61K31/58 , A61P5/38 , C07J43/00
CPC分类号： C07J43/006 , Y10S514/869
摘要： Diuretic pharmaceutically active steroid-spiro-oxazolidinone compounds of the formula (I), ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is C.sub.1-4 alkyl,R.sup.3 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl,Z.sup.1 and Z.sup.2 each are hydrogen or together form a second valence bond, or Z.sup.1 is hydrogen and Z.sup.2 is R.sup.4 --S--,Z.sup.3 and Z.sup.4 each are hydrogen or together form a second valence bond, or Z.sup.3 is hydrogen and Z.sup.4 is R.sup.4 --S--, with at least one of the pairs Z.sup.1 -Z.sup.2 and Z.sup.3 -Z.sup.4 representing hydrogen and an R.sup.4 --S-- group, andR.sup.4 is hydrogen or alkyl, alkenyl, aralkyl or acyl with up to 7 carbon atoms, provided that when Z.sup.1 and Z.sup.2 together form a valence bond, or Z.sup.1 represents a hydrogen atom and Z.sup.2 and R.sup.4 --S-- group then R.sup.1 is methyl.
摘要翻译：式（I）的利尿药物活性类固醇 - 螺恶唑烷酮化合物，其中R 1是氢或甲基，R 2是C 1-4烷基，R 3是氢，C 1-4烷基或C 2-4链烯基， Z1和Z2各自为氢或一起形成第二价键，或Z1为氢，Z2为R4-S-，Z3和Z4各自为氢或一起形成第二价键，或Z3为氢，Z4为R4-S - ，其中至少一对Z1-Z2和Z3-Z4代表氢和R4-S-基团，R4是氢或具有至多7个碳原子的烷基，烯基，芳烷基或酰基，条件是当Z1和 Z2一起形成价键，或Z1表示氢原子，Z2和R4-S-基团，则R1为甲基。

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