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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US06187770B1 N-substituted azaheterocyclic compounds 失效
标题翻译： N-取代的氮杂环化合物
公开(公告)号：US06187770B1
公开(公告)日：2001-02-13
申请号：US09267302
申请日：1999-03-15
申请人： Tine Krogh Jørgensen , Rolf Hohlweg , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
发明人： Tine Krogh Jørgensen , Rolf Hohlweg , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
IPC分类号： A61K31395
CPC分类号： C07D513/04
摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Z, R1, R2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
摘要翻译：本发明涉及通式为X，Z，R 1，R 2和r的新的N-取代的氮杂杂环化合物，如本说明书的详细部分所定义，或其盐，其制备方法，含有它们的组合物，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症，其中C纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由分泌物引起或与分泌有关的适应症和胰岛素拮抗肽的循环，例如非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

6. 发明授权

US6017915A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US6017915A
公开(公告)日：2000-01-25
申请号：US79599
申请日：1998-05-15
申请人： Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
发明人： Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
IPC分类号： C07D321/12 , A61K31/335 , A61K31/357 , A61K31/4406 , A61K31/55 , A61P3/08 , A61P25/00 , A61P29/00 , C07D273/00 , C07D273/01 , C07D405/06 , C07D405/12 , C07D413/06 , A61K31/535 , C07D413/12
CPC分类号： C07D405/06 , C07D405/12 , C07D413/06
摘要： The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
摘要翻译：本发明涉及新型N-取代氨基醇，氨基酸及其酸衍生物，其中取代的烷基链形成N-取代基或其盐的一部分，其制备方法，含有它们的组合物及其用途用于临床治疗C型纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用的疼痛，痛觉过敏和/或炎性疾病。

7. 发明授权

US6066632A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US6066632A
公开(公告)日：2000-05-23
申请号：US376735
申请日：1999-08-17
申请人： Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Rolf Hohlweg , Erik Fischer , Uffe Bang Olsen , Zdenek Polivka , Karel Sindelar , Vladimir Valenta
发明人： Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Rolf Hohlweg , Erik Fischer , Uffe Bang Olsen , Zdenek Polivka , Karel Sindelar , Vladimir Valenta
IPC分类号： C07D211/34 , C07D401/06 , C07D405/06 , C07D409/06 , A01N43/46 , A61K31/44 , C07D219/00 , C07D487/00 , C07D513/00
CPC分类号： C07D401/06 , C07D211/34 , C07D405/06 , C07D409/06
摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
摘要翻译：本发明涉及以下通式的新的N-取代的氮杂杂环化合物：其中X，Y，Z，R 1，R 2和r如在本说明书的详细部分中所定义，或其盐，其制备方法，含有它们的组合物，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症的用途，其中C纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由或由胰岛素拮抗肽的分泌和循环，例如非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

8. 发明授权

US6040318A Tricycle substituted with azaheterocyclic carboxylic acids 失效
标题翻译：用氮杂环羧酸取代三环
公开(公告)号：US6040318A
公开(公告)日：2000-03-21
申请号：US98579
申请日：1998-06-17
申请人： Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Rolf Hohlweg , Erik Fischer , Uffe Bang Olsen , Zdenek Polivka , Karel Sindelar , Vladimir Valenta
发明人： Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Rolf Hohlweg , Erik Fischer , Uffe Bang Olsen , Zdenek Polivka , Karel Sindelar , Vladimir Valenta
IPC分类号： C07D211/34 , C07D401/06 , C07D405/06 , C07D409/06 , A01N43/40 , A01N43/36 , C07D211/06
CPC分类号： C07D401/06 , C07D211/34 , C07D405/06 , C07D409/06
摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
摘要翻译：本发明涉及以下通式的新的N-取代的氮杂杂环化合物：其中X，Y，Z，R 1，R 2和r如在本说明书的详细部分中所定义，或其盐，其制备方法，含有它们的组合物，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症的用途，其中C纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由或由胰岛素拮抗肽的分泌和循环，例如非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

9. 发明授权

US5912262A Heterocyclic compounds 失效
公开(公告)号：US5912262A
公开(公告)日：1999-06-15
申请号：US957163
申请日：1997-10-24
申请人： Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
发明人： Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
IPC分类号： C07D321/12 , A61K31/335 , A61K31/357 , A61K31/4406 , A61K31/55 , A61P3/08 , A61P25/00 , A61P29/00 , C07D273/00 , C07D273/01 , C07D405/06 , C07D405/12 , C07D413/06 , A61K31/40
CPC分类号： C07D405/06 , C07D405/12 , C07D413/06
摘要： The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

10. 发明授权

US06214816B1 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US06214816B1
公开(公告)日：2001-04-10
申请号：US09266236
申请日：1999-03-10
申请人： Rolf Hohlweg , Tine Krogh Jørgensen , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
发明人： Rolf Hohlweg , Tine Krogh Jørgensen , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
IPC分类号： C07D40106
CPC分类号： C07D403/06 , C07D413/06
摘要： The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt thereof. These compounds are useful for treating painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation. They are also useful for treating indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g., non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
摘要翻译：化合物是式I的N-取代的氮杂环化合物，其中R1和R2独立地是氢，卤素，三氟甲基，羟基，C1-6烷基或C1-6-烷氧基; 并且Y是> N-CH 2 - ，其中只有下划线原子参与环系; 并且X是-C（R 6 R 7） - ， - CH 2 CH 2 - ， - CH = CH-CH 2 - ， - CH 2 -CH = CH-， - CH 2 - （C = O） - ， - （C = O） -CH 2 CH 2 CH 2 - ， - CH = CH-，CH（R 10）CH 2 - ， - CH 2 CH（R 10）或 - （C = O） - 其中R 6和R 7独立地是氢或C 1-6 - 烷基，其中R 10是C 1-6 - 烷基或苯基; 和r为0,1或2; 并且Z选自其中A是-CH 2 - ， - O - ， - S-或-N（R 5） - ，其中R 5是H或C 1-6 - 烷基; 并且R 3是 - （CH 2）p COR 4，其中p是1,2,3或4，并且R 4是OH，NH 2，NHOH或C 1-6 - 烷氧基; 或其药学上可接受的盐。这些化合物可用于治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理学作用的疼痛，痛觉过敏和/或炎性病症。它们还可用于治疗由胰岛素拮抗肽（例如非胰岛素依赖性糖尿病（NIDDM））和老龄化相关性肥胖症分泌和循环引起或与之相关的适应症。

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