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1. 发明授权

US4309429A Xanthene and thioxanthene derivatives, compositions thereof, and treatment therewith 失效
标题翻译：呫吨和噻吨衍生物，其组合物及其处理
公开(公告)号：US4309429A
公开(公告)日：1982-01-05
申请号：US105985
申请日：1979-12-21
申请人： Niels Lassen , Klaus P. Bogeso , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
发明人： Niels Lassen , Klaus P. Bogeso , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
IPC分类号： C07D409/04 , A01N43/40 , A61K31/435 , A61P25/18 , C07D335/16 , C07D335/18 , C07D405/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/04 , A61K31/54 , A61K31/445
CPC分类号： C07D335/18 , C07C309/00 , C07C323/00
摘要： The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention correspond to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twenty-two carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts.

2. 发明授权

US4275209A Xanthene and thioxanthene derivatives 失效
标题翻译：呫吨和噻吨衍生物
公开(公告)号：US4275209A
公开(公告)日：1981-06-23
申请号：US106353
申请日：1979-12-21
申请人： Niels Lassen , Klaus P. Bogeso , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
发明人： Niels Lassen , Klaus P. Bogeso , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
IPC分类号： C07D409/04 , A01N43/40 , A61K31/435 , A61P25/18 , C07D335/16 , C07D335/18 , C07D405/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/04
CPC分类号： C07D335/18 , C07C309/00 , C07C323/00
摘要： The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention corresponds to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts.
摘要翻译：本发明涉及具有有用的药效学活性的新型噻吨酮和呫吨衍生物，例如精神安定药活性和止吐活性，制备所述衍生物的方法，含有该衍生物的药物组合物，以及通过施用治疗性的方法治疗精神疾病的方法将一种所述衍生物的活性量提供给包括人在内的活体动物体。本发明的新化合物对应于式I：其中X为卤素原子，含1-4个碳原子的烷基，含1-4个碳原子的烷氧基，甲硫基基团，甲基磺酰基，二甲基氨磺酰基，三氟甲基或乙酰基; Y是氢，氟或甲基; Z是氧或硫; n为0〜3的整数，R为在1〜4个选自任意酯化的羟基或羟甲基的取代基取代的环中具有4〜6个碳原子的环烷基，甲基，氨基，乙酰胺基，甲磺酰氨基或氧代基，具有一个或两个选自氧和氮原子并且任选被任选酯化的羟基或氧代基取代的五或六元饱和杂环，任何酯化的羟基是具有10至22个碳原子的脂族羧酸的酯，以及它们的无毒的药学上可接受的酸加成盐。

3. 发明授权

US4285956A Xanthene and thioxanthene derivatives, compositions thereof and treatment therewith 失效
标题翻译：呫吨和噻吨衍生物，其组合物和其处理
公开(公告)号：US4285956A
公开(公告)日：1981-08-25
申请号：US35735
申请日：1979-05-03
申请人： Niels Lassen , Klaus P. Boges , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
发明人： Niels Lassen , Klaus P. Boges , Peter B. Hansen , Jorn L. M. Buus , Allan J. Bigler
IPC分类号： C07D409/04 , A01N43/40 , A61K31/435 , A61P25/18 , C07D335/16 , C07D335/18 , C07D405/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/04 , A61K31/445 , C07D279/00
CPC分类号： C07D335/18 , C07C309/00 , C07C323/00
摘要： The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention correspond to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-: membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts with the proviso that methyl is present only when one of the other named substituents is also present.

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