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1. 发明授权

US5235097A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，制备该化合物的中间体及其制备方法
公开(公告)号：US5235097A
公开(公告)日：1993-08-10
申请号：US890781
申请日：1992-06-01
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： C07C51/09 , C07C69/63 , C07C69/712
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. ##STR4## Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的（2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸（I）的改进方法，其包括使通式（（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选地被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

2. 发明授权

US5155260A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，用于制备该化合物的中间体和制备中间体的方法
公开(公告)号：US5155260A
公开(公告)日：1992-10-13
申请号：US698081
申请日：1991-05-10
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： B01J27/08 , A61K31/19 , A61K31/235 , C07B61/00 , C07C51/09 , C07C59/48 , C07C59/64 , C07C59/68 , C07C65/21 , C07C67/31 , C07C69/63 , C07C69/712 , C07C229/24 , C07D211/34
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸的改进方法，其包括使通式（X）的酯与（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（IMAGE）（ II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

3. 发明授权

US5288863A Process for the preparation of high-purity 1-(3-chloro-phenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine 失效
标题翻译：制备高纯度1-（3-氯 - 苯基）-4-甲基-7,8-二甲氧基-5H-2,3-苯并二氮杂的方法
公开(公告)号：US5288863A
公开(公告)日：1994-02-22
申请号：US878379
申请日：1992-05-04
申请人： Gyorgy Somogyi , Peter Botka , Gyula Horvath , Antal Simay , Roozsa Gyenge , Imre Moravcsik , Erno Orban , Tamas Hamori , Jeno Korosi , Csilla Kiss , Tibor Balogh , Maria Bidlo nee Igloi , nee Dievald; Emilia Uskert
发明人： Gyorgy Somogyi , Peter Botka , Gyula Horvath , Antal Simay , Roozsa Gyenge , Imre Moravcsik , Erno Orban , Tamas Hamori , Jeno Korosi , Csilla Kiss , Tibor Balogh , Maria Bidlo nee Igloi , nee Dievald; Emilia Uskert
IPC分类号： A61K31/55 , A61P25/00 , C07D243/02 , C07D243/04 , C07D243/12
CPC分类号： C07D243/02
摘要： The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).
摘要翻译：本发明涉及制备式（I）的1-（3-氯苯基）-4-甲基-7,8-二甲氧基-5H（OVS）-2,3-苯并二氮杂的方法（*化学结构*）（I）在高纯度和适合制药目的的质量。根据本发明，将1摩尔式（II）的2-丙酰基-3'-氯-4,5-二甲氧基二苯甲酮（*化学结构*）（II）与3-7摩尔水合肼在有机溶剂中的反应或在有机溶剂的混合物中，在15摄氏度至85摄氏度之间的温度下，在无空气氧气的情况下，任选地在水的存在下进行。然后将粗产物从含有1至5个碳原子的脂族醇中重结晶。

4. 发明授权

US06602865B1 Pyridazino(4,5-b)(1,5)oxazepinone, -thiazepinone and -diazepinone compounds 失效
标题翻译：哒嗪（4,5-b）（1,5）恶唑嗪酮，噻替酮和二氮杂酮化合物
公开(公告)号：US06602865B1
公开(公告)日：2003-08-05
申请号：US09439847
申请日：1999-11-15
申请人： Ferenc Andrasi , Agnes Angyal nee Pataky , Pal Berzsenyi , Sandor Boros , Laszlo Harsing , Katalin Horvath , Peter Matyus , Imre Moravcsik , Agnes Papp nee Behr , Antal Simay , Erzsebet Szabo nee Bagdy , Katalin Szabo nee Pusztai , Istvan Tarnawa , Ildiko Varga
发明人： Ferenc Andrasi , Agnes Angyal nee Pataky , Pal Berzsenyi , Sandor Boros , Laszlo Harsing , Katalin Horvath , Peter Matyus , Imre Moravcsik , Agnes Papp nee Behr , Antal Simay , Erzsebet Szabo nee Bagdy , Katalin Szabo nee Pusztai , Istvan Tarnawa , Ildiko Varga
IPC分类号： A61K3155
CPC分类号： C07D513/04 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554
摘要： Pyridazino(4,5-b)(1,5)oxazepinone, thiazepinone and diazepinone compounds of formula(I) and their tautomers and the acid-addition salts of all these compounds show memory-enhancing and neuroprotective properties.
摘要翻译：式（I）的哒嗪（4,5-b）（1,5）恶唑酮，噻替酮和二氮杂酮化合物及其互变异构体和所有这些化合物的酸加成盐显示记忆增强和神经保护性质。

5. 发明授权

US06482819B1 2,3-benzodiazepine derivatives 失效
标题翻译： 2,3-苯并二氮杂衍生物
公开(公告)号：US06482819B1
公开(公告)日：2002-11-19
申请号：US09463440
申请日：2000-04-10
申请人： Gizella Ábrahám , Emese Csuzdi , Sándor Sólyom , Pál Berzsenyi , István Tarnawa , Ferenc Andrási , István Ling , Tamás Hámori , Katalin Horváth , Imre Moravcsik , István Pallagi , Antal Simay
发明人： Gizella Ábrahám , Emese Csuzdi , Sándor Sólyom , Pál Berzsenyi , István Tarnawa , Ferenc Andrási , István Ling , Tamás Hámori , Katalin Horváth , Imre Moravcsik , István Pallagi , Antal Simay
IPC分类号： A61K31551
CPC分类号： C07D487/04
摘要： 2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.
摘要翻译：式（I）的2,3-苯并二氮杂，其立体异构体和酸加成盐，其中变量具有本说明书中给出的含义，以及含有它们的药物组合物，其适用于治疗与肌肉痉挛，癫痫以及急性并且公开了慢性形式的神经变性疾病。

6. 发明授权

US06265445B1 Antiarrhythmic compounds 失效
标题翻译：抗心律不齐的化合物
公开(公告)号：US06265445B1
公开(公告)日：2001-07-24
申请号：US09555602
申请日：2000-07-28
申请人： Gyula Papp , András Varró , Péter Mátyus , Ildikó Varga , Tivadar Rettegi , Alice Druga , Antal Simay , Imre Moravcsik , Pál Berzsenyi , Daniella Barlocco , Giorgio Cignarella , Márta Pátfalusi
发明人： Gyula Papp , András Varró , Péter Mátyus , Ildikó Varga , Tivadar Rettegi , Alice Druga , Antal Simay , Imre Moravcsik , Pál Berzsenyi , Daniella Barlocco , Giorgio Cignarella , Márta Pátfalusi
IPC分类号： A61K3117
CPC分类号： C07C233/36 , C07C217/18 , C07C233/78 , C07C275/40 , C07C311/08 , C07C335/20 , Y10S514/821
摘要： The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.
摘要翻译：本发明涉及具有双重攻击点的新型抗心律失活的苯氧基烷基胺衍生物。更具体地说，本发明涉及式（1）的新的苯氧基烷基胺衍生物，其中R 1和R 2彼此独立地表示氢，卤素或C 1-4烷基; R 3，R 4和R 5彼此独立地代表氢或C 1-4烷基; R 6表示氢，C 1-4烷基或苄基; R 7表示硝基或任选被C 1-4烷基，苯甲酰基，C 1-4烷基羰基，C 1-4烷基磺酰基，C 1-4的单取代的氨基烷基氨基甲酰基或C 1-4烷基硫代氨基甲酰基; n和m均为0或1，条件是当R 1为氢时，R 2不同于氢，以及立体异构体或其立体异构体的混合物，其酸加成盐和水合物，前药和所有这些化合物的代谢物。

7. 发明授权

US4425349A Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
标题翻译：含硫异喹啉衍生物在药物组合物和使用方法中的应用
公开(公告)号：US4425349A
公开(公告)日：1984-01-10
申请号：US381775
申请日：1982-05-25
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/14 , C07D513/04 , A61K31/47
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/826 , Y10S514/869
摘要： The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,and salts and cyclic amides thereof.The new compounds possess valuable pharmaceutical activities, more particularly, are potent diuretic, antiasthmatic, hypotensive and antiinflammatory agents. Thus another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a pharmaceutically effective amount of at least one compound of the general formula (I) with at least one pharmaceutically inert carrier or diluent. The invention also relates to a process for preparing these compounds.
摘要翻译：本发明涉及新的含硫异喹啉衍生物。更具体地说，本发明涉及通式（I）的异喹啉衍生物，其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基和任选地被苯基取代，任选被一个或多个卤素或烷氧基取代的苯基，氰基或氨基甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，具有1至4个碳原子的直链或支链烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基，在烷基部分含有1至6个碳原子的氨基甲酰基，咔唑基或二烷基氨基，或者是具有1至6个碳原子的直链或支链的亚烷基，虚线代表进一步c 环的3-和4-位的碳 - 碳键或氢原子，及其盐和环状酰胺。新化合物具有有价值的药物活性，特别是有效的利尿，止喘，降压和抗炎药。因此，本发明的另一方面是药物组合物，其包含作为活性成分的药学有效量的至少一种通式（I）的化合物与至少一种药学上惰性的载体或稀释剂。本发明还涉及制备这些化合物的方法。

8. 发明授权

US4373104A Sulfur-containing isoquinoline derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：含硫异喹啉衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4373104A
公开(公告)日：1983-02-08
申请号：US164939
申请日：1980-07-01
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/00 , A61K31/47 , A61K31/472 , A61P7/08 , A61P7/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P29/00 , A61P43/00 , C07D217/14 , C07D217/16 , C07D513/04
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/869
摘要： Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,or salts thereof. The new compounds are potent diuretic agents.
摘要翻译：公开了式（I）的异喹啉（I）其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基，任选被苯基取代，苯基任选地被一个或多个卤素或烷氧基取代，氰基或甲酰甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，直链或支链具有1至4个碳原子的烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基碳原子，氨基甲酰基，咔唑基或在烷基部分含有1至6个碳原子的二烷基氨基，或者R2是具有1至6个碳原子的直链或支链链烯基，虚线代表另外的碳 - 碳键或氢原子在3-和环的4-位，或其盐。新化合物是有效的利尿剂。

9. 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。

10. 发明授权

US06194411B1 3(2H)-pyridazinone derivatives and pharmaceutical compositions containing these compounds 失效
标题翻译： 3（2H） - 哒嗪酮衍生物和含有这些化合物的药物组合物
公开(公告)号：US06194411B1
公开(公告)日：2001-02-27
申请号：US08973584
申请日：1998-07-20
申请人： Péter Mátyus , László Hársing , Mariann née Tapfer Karim , Judit Kosáry , Ágnes née Behr Papp , Antal Simay , Yemane Tilahun , Éva née Joszt Tomori , Edit Horváth , Katalin Horváth , Ildikó Varga , Erzsébet née Kaczián Zára , Margit née Iglóy Bidló , Alice Druga , György Rabloczky , Márta Varga , Egon Kárpáti , Endre Kasztreiner , István Király , Ildikó née Gyóry Máthé , György Máthé , László Sebestyén , Nándor Makk
发明人： Péter Mátyus , László Hársing , Mariann née Tapfer Karim , Judit Kosáry , Ágnes née Behr Papp , Antal Simay , Yemane Tilahun , Éva née Joszt Tomori , Edit Horváth , Katalin Horváth , Ildikó Varga , Erzsébet née Kaczián Zára , Margit née Iglóy Bidló , Alice Druga , György Rabloczky , Márta Varga , Egon Kárpáti , Endre Kasztreiner , István Király , Ildikó née Gyóry Máthé , György Máthé , László Sebestyén , Nándor Makk
IPC分类号： A61K31501
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)-pyridazionone of formula (1) and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazionone 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 formula (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;1- and &agr;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） - 哒嗪酮和S-2- [3- 具有式（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。

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