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1. 发明授权

US4238611A Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine 失效
标题翻译： 10-哌嗪二苯并（b，f）thiepine的多取代衍生物
公开(公告)号：US4238611A
公开(公告)日：1980-12-09
申请号：US646755
申请日：1976-01-06
申请人： Miroslav Protiva , Karel Sindelar , Irena Cervena , Jirina Metysova
发明人： Miroslav Protiva , Karel Sindelar , Irena Cervena , Jirina Metysova
IPC分类号： A61K31/495 , C07C17/093 , C07C17/14 , C07C57/58 , C07D337/14 , C07D409/04
CPC分类号： C07D337/14 , C07C17/093 , C07C17/14 , C07C321/00 , C07C323/00 , C07C57/58
摘要： Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.
摘要翻译：描述了10-哌嗪二苯并（b，f）噻吩的多取代衍生物及其制备方法。该组合物表现出精神药物和抗微生物特征，毒性低。所述化合物具有通式“IMAGE”，其中R2，R3，R7和R8选自氢，氟和氯原子，氟甲基，甲氧基和羟基，R2，R3， R 7和R 8不是氢，R选自具有1-3个碳原子的氢，烷基或烷基羟基，在酰基部分具有8-10个碳原子的酰氧基烷基和烷基部分和乙氧基羰基，m和n表示0-1的整数，10和11个碳原子之间的键是单键或双键。

2. 发明授权

US3985750A Fatty acid esters of 8-substituted 10-[4-(hydroxyalkyl)piperazino]-10,11-dihydrodibenzo[b,f]thiepins 失效
标题翻译： 8-取代的10- {8 4-（羟基烷基）哌嗪基{9-10,11-二氢二苯并{8b，f {9 thiepins）的脂肪酸酯
公开(公告)号：US3985750A
公开(公告)日：1976-10-12
申请号：US490218
申请日：1974-07-19
申请人： Miroslav Protiva , Jiri Jilek , Karel Sindelar , Jirina Metysova
发明人： Miroslav Protiva , Jiri Jilek , Karel Sindelar , Jirina Metysova
IPC分类号： C07D313/12 , C07D337/14 , C07D409/04
CPC分类号： C07D337/14 , C07D313/12
摘要： Fatty acid esters of 8-substituted 10-[4-(hydroxyalkyl)piperazino]-10,11-dihydrodibenzo[b,f]thiepins and oxepins having the formula ##SPC1##In which X is a sulfur or oxygen atom, R.sup.1 is a hydrogen, chloro, or trifluoromethyl radical, a lower alkyl radical having at most 5 carbon atoms, or a cycloalkyl radical having at least 3 and at most 8 carbon atoms, or an alkoxy or alkylthio radical the alkyl moiety of which has at most 4 carbon atoms, R.sup.2 is an alkyl radical having at least 5 and at most 17 carbon atoms, and n is 2, 3, or 4, and their salts with pharmaceutically acceptable inorganic and organic acids. The compounds have a high degree of neuroleptic activity and retain this activity for long periods after administration.Related fatty acid esters of 8-substituted 10-[4-(hydroxyalkyl)-piperazino]dibenzo[b,f]thiepins and oxepins having the formula ##SPC2##And fatty acid esters of 8-substituted 4-[4-(hydroxyalkyl)piperazino]thieno[2,3-b]-1-benzothiepins and oxepins having the formula ##SPC3##In which formulae X, R.sup.1, R.sup.2 and n each have the foregoing significance, are also included herein.
摘要翻译： 8-取代的10- [4-（羟基烷基）哌嗪基] -10,11-二氢二苯并[b，f]硫蛋白和具有式IN的氧杂环丁烷的脂肪酸酯，其中X是硫或氧原子，R1是氢，氯或三氟甲基，具有至多5个碳原子的低级烷基或具有至少3个且至多8个碳原子的环烷基，或其烷基部分具有至多4个碳原子的烷氧基或烷硫基，R 2 是具有至少5个且至多17个碳原子，n为2,3或4的烷基，以及它们与药学上可接受的无机酸和有机酸的盐。这些化合物具有高度的精神安定性活性，并且在施用后长时间保留该活性。

3. 发明授权

US4431808A Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US4431808A
公开(公告)日：1984-02-14
申请号：US356474
申请日：1982-03-09
申请人： Miroslav Protiva , Karel Sindelar , Antonin Dlabac , Jirina Metysova
发明人： Miroslav Protiva , Karel Sindelar , Antonin Dlabac , Jirina Metysova
IPC分类号： A61K31/00 , A61K31/455 , A61K31/55 , A61P25/00 , A61P25/24 , A61P25/26 , C07C29/147 , C07C33/46 , C07C45/00 , C07C45/29 , C07C47/575 , C07D211/22 , C07D321/10 , C07D327/02 , C07D339/00 , C07D405/02 , C07D405/04 , C07D405/06 , C07D409/02 , C07D409/04 , C07D411/02 , C07D411/04 , C07D411/06 , C07D407/04
CPC分类号： C07D411/06 , C07C29/147 , C07C323/00 , C07C33/46 , C07C45/00 , C07C45/29 , C07C47/575 , C07D211/22 , C07D321/10 , C07D327/02 , C07D339/00
摘要： A technique is described for the preparation of a wide variety of basic derivatives of linearly condensed tricyclic systems formed by two external benzene nuclei and a 7-membered central ring having 2 chalcogen atoms as hetero atoms.Derivatives of 11H-dibenzo(b,e)-1,4-dioxepin are obtained when the chalcogens are both oxygen atoms; derivatives of 11H-dibenzo(b,f)-1,4-dithiepin are obtained when the chalcogens are both sulfur atoms; derivatives of 6H-dibenz(b,e)-1,4-oxathiepin and 11H-dibenz(b,f)-1,4-oxathiepin are obtained with combinations of sulfur and oxygen atoms as chalcogens.
摘要翻译：描述了一种用于制备由两个外部苯核和具有2个硫属原子作为杂原子的7元中心环形成的线性缩合三环系统的各种各样的碱性衍生物的技术。当硫属元素都是氧原子时，得到11H-二苯并（b，e）-1,4-二氧杂环庚二烯的衍生物; 当硫属原子都是硫原子时，得到11H-二苯并（b，f）-1,4-二硫杂的衍生物; 通过硫和氧原子的组合作为硫属元素获得6H-二苯并（b，e）-1,4-氧硫杂环十二环和11H-二苯并（b，f）-1,4-氧硫杂环庚三烯的衍生物。

4. 发明授权

US4243805A 3 Fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(bf) thiepins and method for the preparation thereof 失效
标题翻译： 3氟-10-哌嗪基-8-取代的10,11-二氢二苯并 - （bf）硫蛋白及其制备方法
公开(公告)号：US4243805A
公开(公告)日：1981-01-06
申请号：US972323
申请日：1978-12-22
申请人： Miroslav Protiva , Miroslav Rajsner , Karel Sindelar , Jiri Jilek , Vaclav Bartl , Jirina Metysova , Antonin Dlabac , Leon Langsadl , Josef Pomykacek , Frantisek Miksik
发明人： Miroslav Protiva , Miroslav Rajsner , Karel Sindelar , Jiri Jilek , Vaclav Bartl , Jirina Metysova , Antonin Dlabac , Leon Langsadl , Josef Pomykacek , Frantisek Miksik
IPC分类号： A61K31/38 , A61K31/495 , A61K31/55 , A61P25/00 , A61P25/26 , A61P31/04 , C07C17/093 , C07C17/14 , C07C51/08 , C07D295/073 , C07D295/088 , C07D295/092 , C07D295/205 , C07D337/14 , C07D409/04 , C07D409/12 , C07D409/14
CPC分类号： C07D295/073 , C07C17/093 , C07C17/14 , C07C323/00 , C07C51/08 , C07D295/088 , C07D295/205 , C07D337/14
摘要： Techniques for the preparation of 3-fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(b,f) thiepins and their addition salts with organic and inorganic acids are disclosed. The described compositions evidence psychotropic activity and low toxicity and are characterized as neuroliptics with a high degree of cataleptic, anti-apomorphine and central depressant action.
摘要翻译：公开了制备3-氟-10-哌嗪基-8-取代的10,11-二氢二苯并 - （b，f）硫蛋白及其与有机和无机酸的加成盐的技术。所描述的组合物表现出精神活性和低毒性，并且被表征为具有高程度的抗痴呆，抗阿扑吗啡和中枢抑制作用的神经元。

5. 发明授权

US4678788A N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo (B,F) thiepins and acid addition salts thereof 失效
标题翻译： N-取代的2-氯-7-氟-10-哌嗪基-10,11-二氢二苯并（B，F）硫蛋白及其酸加成盐
公开(公告)号：US4678788A
公开(公告)日：1987-07-07
申请号：US821992
申请日：1986-01-24
申请人： Miroslav Protiva , Jiri Jilek , Irena Cervena , Antonin Dlabac , Martin Valchar , Josef Pomykacek
发明人： Miroslav Protiva , Jiri Jilek , Irena Cervena , Antonin Dlabac , Martin Valchar , Josef Pomykacek
IPC分类号： A61K31/495 , A61P25/20 , C07D337/14 , C07D409/12 , C07D409/04
CPC分类号： C07D409/12 , C07D337/14
摘要： N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepins are disclosed of the general formula I, ##STR1## in which R represents an aminocarbonyl, amino-oximinomethyl, 1,3-dioxolan-2-yl or 1,3-dioxan-2-yl, group and their addition salts with convenient organic and inorganic acids. These compounds are highly potent antidopaminergic, non-cataleptic neuroleptics of use in the treatment of schizophrenia. According to recent pharmacological assay results, the subject compounds are expected to be substantially free of the usual undesired extrapyramidal side effects. They can be obtained by common preparative methods from the respective starting compounds of formula III, IV or V, or also by appropriate interconversion reactions of other compounds of formula I. If required, the resulting bases are neutralized with suitable acids, preferably methanesulfonic, maleic or hydrochloric acid, to yield the corresponding addition salts that can be used in formulating proper dosage forms for pharmacological evaluation and therapeutical application.
摘要翻译： N-取代的2-氯-7-氟-10-哌嗪基-10,11-二氢二苯并（b，f）thiepins公开了通式I，其中R表示氨基羰基，氨基 - 肟基甲基，1,3-二氧戊环-2-基或1,3-二恶烷-2-基，它们与方便的有机和无机酸的加成盐。这些化合物是用于治疗精神分裂症的高效抗癌剂，非抗抑郁药治疗精神分裂症。根据最近的药理学测定结果，本发明化合物预期基本上不含常见的不希望的锥体束外副作用。它们可以通过相应的式III，IV或V的起始化合物的常规制备方法获得，或者也可以通过其它式I化合物的适当相互转化反应获得。如果需要，所得碱用合适的酸中和，优选甲磺酸，马来酸或盐酸，以产生相应的加成盐，其可用于配制用于药理学评价和治疗应用的适当剂型。

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