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公开(公告)号:US4921861A
公开(公告)日:1990-05-01
申请号:US185049
申请日:1988-04-22
申请人: Jozsef Knoll , ne Simonyi; Katalin Budai , Edit Berenyi ne Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
发明人: Jozsef Knoll , ne Simonyi; Katalin Budai , Edit Berenyi ne Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
CPC分类号: A61K31/47
摘要: The 3-amino-4-ethylthio-quinoline of the Formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof possess useful therapeutical properties. They exhibit a potent and highly selective anxiolytic and narcosis potentiating effect and are devoid of sedative and anti-convulsive effect. Consequently, the invention relates to pharmaceutical compositions comprising the compound of Formula I or a salt thereof as active agent.The invention also relates to a new and improved process for the preparation of the compound of Formula I.
摘要翻译: 式I的3-氨基-4-乙硫基 - 喹啉(I)及其药学上可接受的酸加成盐具有有用的治疗性质。 它们具有强效和高选择性的抗焦虑和麻醉增效作用,没有镇静和抗惊厥作用。 因此,本发明涉及包含式I化合物或其盐作为活性剂的药物组合物。 本发明还涉及制备式I化合物的新的和改进的方法。
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公开(公告)号:US4921960A
公开(公告)日:1990-05-01
申请号:US184796
申请日:1988-04-22
申请人: Jozsef Knoll , Katalin Budai nee Simonyi , Edit Berenyi nee Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
发明人: Jozsef Knoll , Katalin Budai nee Simonyi , Edit Berenyi nee Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
IPC分类号: A61K31/47 , A61P25/20 , A61P25/22 , C07D215/38
CPC分类号: C07D215/38
摘要: The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.2-5 alkinyl, C.sub.3-7 cycloalkyl or optionally substituted phenyl-(C.sub.1-4 alkyl);R.sub.2 represents hydrogen or C.sub.1-5 alkanoyl;X.sub.1 and X.sub.2 can be identical or different and each stands for hydrogen, halogen, trifluoromethyl or C.sub.1-4 alkoxy;(with the proviso that if R.sub.1 stands for ethyl, at least one of R.sub.2, X.sub.1 and X.sub.2 is different from hydrogen) and pharmaceutically acceptable acid additions salts possess valuable anxiolytic properties devoid of sedative effect and can be used in therapy.The compounds of the general Formula I can be prepared by methods known per se.
摘要翻译: 通式Ⅰ的新化合物(Ⅰ)(其中R1代表C1-5烷基,C2-5链烯基,C2-5炔基,C3-7环烷基或任意取代的苯基 - (C 1-4烷基); R 2表示氢或C 1-5烷酰基; X 1和X 2可以相同或不同,各自表示氢,卤素,三氟甲基或C 1-4烷氧基;(条件是如果R1代表乙基,则R2,X1中的至少一个 和X2不同于氢)和药学上可接受的酸加成盐具有不具有镇静作用的有价值的抗焦虑性质,并且可用于治疗。通式I的化合物可以通过本身已知的方法制备。
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