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1. 发明授权

US4384140A 2-Chloroethyl urea derivatives 失效
标题翻译： 2-氯乙基脲衍生物
公开(公告)号：US4384140A
公开(公告)日：1983-05-17
申请号：US348724
申请日：1982-02-16
申请人： Peter Bregnedal , Jorn L. M. Buus
发明人： Peter Bregnedal , Jorn L. M. Buus
IPC分类号： A61K31/17 , A61K31/275 , A61K31/40 , A61P35/00 , C07C67/00 , C07C239/00 , C07C275/68 , C07C127/17
CPC分类号： C07C275/68
摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。本发明的新化合物可以由下式表示：其中X和Y相同或不同，并且选自苯基和环己基，所述苯基和环己基任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代，一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

2. 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.

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.

4. 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。

5. 发明授权

US4153694A Behenic acid esters, compositions thereof and a method of preparation thereof 失效
标题翻译：山萮酸酯，其组合物及其制备方法
公开(公告)号：US4153694A
公开(公告)日：1979-05-08
申请号：US826049
申请日：1977-08-19
申请人： Jorn L. M. Buus , Niels Lassen
发明人： Jorn L. M. Buus , Niels Lassen
IPC分类号： C07D279/28 , A61K31/54 , A61K31/5415 , A61P25/00 , C07D417/06 , A61K31/38
CPC分类号： C07D417/06 , A61K31/54
摘要： The present invention relates to novel behenic acid esters of the following general formula: ##STR1## wherein X is "N" or "CH," the non-toxic acid addition salts thereof, a method for the preparation of said esters and therapeutic compositions thereof having prolonged effect.It is an object of the present invention to provide behenic acid esters of Formula I, a method of making the same, a method for the alleviation, palliation, mitigation or inhibition of the manifestations of certain physiological-psychological abnormalities of animals therewith, and pharmaceutical compositions comprising such compounds as active ingredient.Other objects will be apparent to one skilled in the art and still other objects will become apparent hereinafter.BACKGROUND OF THE INVENTIONIn recent years esters of neuroleptic active phenothiazines have been suggested and found useful in preparations having prolonged effect when administered parenterally, The esters which have been found most useful are enanthic, decanoic and palmitic acid esters of fluphenazine which are mostly administered as sterile solutions in vegetable oils which solutions are injected intramuscularly. The neuroleptic effect of such solutions may last for as long as 15 days.Also aliphatic carboxylic acid esters of some very strong neuroleptic phenothiazines having a fluorine atom in the 7-position have been suggested and include esters of aliphatic carboxylic acids having up to and including 17 carbon atoms, especially the decanoic and palmitic acid esters.During continued work with such esters in pharmacological experiments it was found that the decanoic and palmitic acid esters of the very strongly neuroleptic 2-trifluoromethyl-7-fluoro-10-(3'-(4-(2-hydroxyethyl)-1-piperidyl)propyl)phenothiazine and 2-trifluoromethyl-7-fluoro-10-(3'-(4-2-hydroxyethyl)-1-piperazinyl)propyl)phenothiazine when administered in ordinary doses as oily solutions by injection tended to give too high concentrations at the start causing a pronounced sedation in the first week.SUMMARY OF THE INVENTIONIt has now surprisingly been found that the behenic acid esters of formula I not only have a more prolonged effect but also cause less sedation in the test animals when injected in the form of oily solutions. It also seems that other side effects such as extrapyrimidal symptoms mostly are avoided.The compounds of formula I may be prepared - according to the method of the invention - by reacting a compound of the following general formula: ##STR2## wherein X is as defined before, with a reactive derivative of behenic acid, such as an acid halide or the anhydride, whereupon the compound of formula I formed by the reaction is isolated as the free base or as a non-toxic acid addition salt thereof.The esterification process according to the invention is preferably carried out in the presence of an inert organic solvent such as a ketone, preferably acetone, or an ether such as diethylether.The reactive derivative of behenic acid is preferably an acid halide, especially the acid chloride, or the acid anhydride.The non-toxic acid addition salts of the compounds of formula I are preferably salts of pharmaceutically acceptable acids such as mineral acids, for example hydrochloric acid, hydrobromic acid, phosphoric acid, sulphuric acid, and the like, and organic acids such as acetic acid, tartaric acid, maleic acid, citric acid, methane sulphonic acid, and the like.
摘要翻译：本发明涉及以下通式的新颖的山嵛酸酯：其中X是“N”或“CH”，其无毒的酸加成盐，制备所述酯和治疗组合物的方法具有延长的效果。

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