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1. 发明授权

US5843948A Piperazinophenyl- and piperazinophenyloxycarboxylic acid derivatives, and processes and intermediates for their preparation and pharmaceutical compositions comprising them 失效
标题翻译：哌嗪基苯基和哌嗪苯氧基羧酸衍生物，以及其制备方法和中间体以及包含它们的药物组合物
公开(公告)号：US5843948A
公开(公告)日：1998-12-01
申请号：US994754
申请日：1997-12-19
申请人： Wolfgang Kehrbach , Uwe Schoen , Jack A. J. den Hartog , Jan H. van Maarseveen , Chris G. Kruse , Jochen Antel , Jan-Hendrik Reinders , Dieter Ziegler , Gerhard-Wilhelm Bielenberg
发明人： Wolfgang Kehrbach , Uwe Schoen , Jack A. J. den Hartog , Jan H. van Maarseveen , Chris G. Kruse , Jochen Antel , Jan-Hendrik Reinders , Dieter Ziegler , Gerhard-Wilhelm Bielenberg
IPC分类号： C07D295/08 , A61K31/495 , A61P7/02 , C07D213/74 , C07D213/78 , C07D295/14 , C07D295/155 , C07D295/135 , C07D401/04
CPC分类号： C07D213/74 , C07D295/155 , Y02P20/55
摘要： Compounds having fibrinogen receptor-antagonistic activity, of the general formula I ##STR1## in which Z is oxygen or a methylene group, B is a phenyl or pyridyl radical, R.sup.1 is hydrogen or a group forming a biolabile ester, and their physiologically acceptable acid addition salts and physiologically acceptable salts of acids of formula I.
摘要翻译：具有纤维蛋白原受体拮抗活性的化合物，其中Z为氧或亚甲基的通式I ，B为苯基或吡啶基，R 1为氢或形成不可生物酯的基团及其生理学上可接受的酸式I的酸的加成盐和生理上可接受的盐。

2. 发明授权

US4906640A 3-sulfonyl-3,7-diazabicyclo[3,3,1]nonane compounds and medicaments containing said compounds 失效
标题翻译： 3-磺酰基-3,7-二氮杂双环[3,3,1]壬烷化合物和含有所述化合物的药物
公开(公告)号：US4906640A
公开(公告)日：1990-03-06
申请号：US214032
申请日：1988-06-30
申请人： Uwe Schoen , Wolfgang Kehrbach , Klaus-Ullrich Wolf
发明人： Uwe Schoen , Wolfgang Kehrbach , Klaus-Ullrich Wolf
IPC分类号： A61K31/435 , A61P1/14 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10
摘要： 3-sulfonyl-3,7-diazabicyclo[3,3,1]nonane compounds corresponding to the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen or lower alkyl orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents lower alkyl, thienyl, halogen substituted thienyl or a --(CH.sub.2).sub.n --R.sup.5 group, wherein n=0-3 andR.sup.5 is an optionally substituted phenyl group.The compounds are pharmacologically active, particularly in influencing the motility of the stomach.
摘要翻译：对应于式（I）的3-磺酰基-3,7-二氮杂双环[3,3,1]壬烷化合物，其中R 1是烷基，环烷基烷基或苄基，R 2是氢或低级烷基，R 3是氢或更低烷基或R 2和R 3一起形成亚烷基链，并且R 4表示低级烷基，噻吩基，卤素取代的噻吩基或 - （CH 2）n -R 5基团，其中n = 0-3，R 5是任选取代的苯基。这些化合物具有药理活性，特别是影响胃的运动性。

3. 发明授权

US4879299A Treatment of heart conditions with spartein compounds 失效
标题翻译：用撒丁酮化合物治疗心脏病
公开(公告)号：US4879299A
公开(公告)日：1989-11-07
申请号：US135109
申请日：1987-12-18
申请人： Uwe Schoen , Wolfgang Kehrbach , Bernd Hachmeister , Gerd Buschmann , Ulrich G. Kuehl
发明人： Uwe Schoen , Wolfgang Kehrbach , Bernd Hachmeister , Gerd Buschmann , Ulrich G. Kuehl
IPC分类号： A61K31/445 , C07D471/22
CPC分类号： C07D471/22 , A61K31/445
摘要： Compounds of Formula (I)S--(CH2)n--Atm (I)in whichS is a 17-spartein nucleus,n is 0 or 1, andA is 2-furyl, 2-thienyl or 2-(N-loweralkyl)pyrrylwhen n=0, or3-furyl or 3-thienyl when n=1, or pyridyl, or a phenyl group of Formula (II) ##STR1## in which at least one of R.sub.1, R.sub.2 and R.sub.3 is a defined substituent other than hydrogen. Such compounds and corresponding compounds in which A is an unsubstituted phenyl group are useful in pharmaceutical compositions as heart affecting agents. Methods of preparing such compounds and pharmaceutical compositions are disclosed. Also described is the use of such compounds or compositions, particularly compounds or compositions with positive inotropic activity, to treat various heart conditions.
摘要翻译：式（I）的化合物其中S为17-阿尔膦酸核的S-（CH 2）n-Atm（I），n为0或1，A为2-呋喃基，2-噻吩基或2-（N-低级烷基）当n = 0时为吡咯，或当n = 1时为3-呋喃基或3-噻吩基，或吡啶基或式（II）的苯基（II），其中R 1，R 2和R 3中的至少一个为除氢以外的定义的取代基。这些化合物和其中A是未取代的苯基的相应化合物可用作药物组合物作为心脏影响剂。公开了制备这些化合物和药物组合物的方法。还描述了使用这些化合物或组合物，特别是具有正性肌力活性的化合物或组合物来治疗各种心脏病症。

4. 发明授权

US4771044A Tetraoxo compounds and pharmaceutical compositions 失效
标题翻译：四氧化合物和药物组合物
公开(公告)号：US4771044A
公开(公告)日：1988-09-13
申请号：US898043
申请日：1986-08-19
申请人： Uwe Schoen , Wolfgang Kehrbach , Werner Benson , Andreas Fuchs , Michael Ruhland
发明人： Uwe Schoen , Wolfgang Kehrbach , Werner Benson , Andreas Fuchs , Michael Ruhland
IPC分类号： A61K31/435 , A61K31/44 , A61K31/495 , A61K31/505 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D471/08 , C07D471/10 , A61K31/395 , A61K31/445
CPC分类号： C07D471/08 , C07D471/10
摘要： Tetraoxo compounds of the Formula (I) ##STR1## wherein R.sup.1 is an alkyl, alkenyl, phenylalkyl or cycloalkylalkyl group,R.sup.2 and R.sup.3 are each independently an alkyl or phenyl group or together denote an alkylene group,W is a (CH.sub.2).sub.n --Q group, in which n is 2 to 10 and Q is(a) a displaceable leaving group X, or(b) Z-R.sup.4, where Z is a 1-piperazinyl group, and R.sup.4 is in position 4, and is hydrogen or a phenyl, substituted phenyl, N-heteroaryl or substituted N-heteroaryl group;and salts and acid addition salts of said compound, and a method for their preparation. Selected compounds of Formula (I) have been found to have central nervous system affecting activity.
摘要翻译：式（I）的四氢化合物其中R 1是烷基，烯基，苯基烷基或环烷基烷基，R 2和R 3各自独立地是烷基或苯基或一起表示亚烷基，W是（CH 2 ）nQ基团，其中n为2至10，Q为（a）可置换离去基团X或（b）Z-R4，其中Z为1-哌嗪基，R4为4位，为氢或苯基，取代的苯基，N-杂芳基或取代的N-杂芳基; 所述化合物的盐和酸加成盐及其制备方法。选定的式（I）化合物已被发现具有中枢神经系统影响活性。

5. 发明授权

US4742172A Intermediates for synthesizing pharmaceutically active 3,7-diazabicyclo-(3,3,1)-nonane compounds 失效
标题翻译：用于合成药学活性3,7-二氮杂双环（3,3,1） - 壬烷化合物的中间体
公开(公告)号：US4742172A
公开(公告)日：1988-05-03
申请号：US54868
申请日：1987-05-27
申请人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
发明人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
IPC分类号： A61K31/435 , A61P9/06 , A61P9/10 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10
摘要： 3,7-diaza bicyclo-(3,3,1)-nonane compounds of the formula ##STR1## in which substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4, Z.sub.1, and Z.sub.2 indicate the substituents as they are given in the description of the invention, can be employed to produce certain pharmaceutically useful compounds.
摘要翻译：其中取代基R 1，R 2，R 3，R 4，Z 1和Z 2的3,7-二氮杂双环 - （3,3,1） - 壬烷化合物表示取代基，如在其描述本发明可用于生产某些药学上有用的化合物。

6. 发明授权

US4550112A 3,7-Diazabicyclo(3,3,1)nonane compounds and their use in treating heart disease 失效
标题翻译： 3,7-二氮杂双环（3,3,1）壬烷化合物及其在治疗心脏病中的应用
公开(公告)号：US4550112A
公开(公告)日：1985-10-29
申请号：US532762
申请日：1983-09-16
申请人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
发明人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
IPC分类号： A61K31/435 , A61P9/06 , A61P9/10 , C07D471/08 , C07D471/10 , A61K31/445
CPC分类号： C07D471/08 , C07D471/10
摘要： Novel 3,7-diaza bicyclo-(3,3,1)-nonane compounds are described which are represented by the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 each denotes hydrogen,R.sub.1 and R.sub.2 each denotes (A) a substituent which contains up to 12 carbon atoms and which is selected from the group consisting of alkyl, alkenyl, and alkinyl, or (B) a cycloalkyl group containing 3 to 6 carbon atoms which is attached to the nitrogen atom directly or by an alkylene group containing 1 to 3 carbon atoms, andR.sub.3 and R.sub.4 each denotes an alkyl group with up to 7 carbon atoms, or both together form an alkylene chain represented by the formula --(CH.sub.2).sub.n --, wherein n is an integer ranging between about 3 and 6, such that the substituents R.sub.1, R.sub.2, R.sub.3, and R.sub.4 together contain at least 5 carbon atoms. Also described are processes of producing said compounds, pharmaceutical compositions containing compounds of Formula I, and methods of preparing and using said compositions.
摘要翻译：描述了由下式表示的新颖的3,7-二氮杂双环（3,3,1） - 壬烷化合物：其中Z1和Z2各自表示氢，R1和R2各自表示（A）含有至多12个碳原子，并且其选自烷基，烯基和炔基，或（B）含有3至6个碳原子的环烷基，其直接连接到氮原子上或通过含有1至 3个碳原子，并且R 3和R 4各自表示具有至多7个碳原子的烷基，或两者一起形成由式 - （CH 2）n - 表示的亚烷基链，其中n为约3至6的整数，使得取代基R 1，R 2，R 3和R 4一起含有至少5个碳原子。还描述了生产所述化合物的方法，含有式I化合物的药物组合物，以及制备和使用所述组合物的方法。

7. 发明授权

US4695566A 3-aminocarbonylmethoxy-5-phenylpyrazole compounds, antiarrythmic compositions containing them, and intermediates in their preparation 失效
标题翻译： 3-氨基羰基甲氧基-5-苯基吡唑化合物，含有它们的抗焦虑组合物及其制备中间体
公开(公告)号：US4695566A
公开(公告)日：1987-09-22
申请号：US751045
申请日：1985-07-02
申请人： Henning Heinemann , Wolfgang Kehrbach , Uwe Schoen , Gerd Buschmann , Ulrich Kuhl
发明人： Henning Heinemann , Wolfgang Kehrbach , Uwe Schoen , Gerd Buschmann , Ulrich Kuhl
IPC分类号： C07D401/12 , A61K31/415 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/535 , A61P9/06 , C07D231/20 , C07D317/00 , C07D405/04 , C07D405/12 , C07D498/04
CPC分类号： C07D405/04 , C07D231/20
摘要： 3-(aminoalkylaminocarbonylmethoxy)-5-phenylpyrazole compounds corresponding to the formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 and R.sub.9 may be hydrogen or lower alkyl groups, or R.sub.5 with R.sub.6 and/or R.sub.8 with R.sub.9 may also form specified cyclic groups, R.sub.3 and R.sub.4 may be hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro, hydroxy or alkylene dioxy, and Z represents an alkylene chain or the 2-hydroxypropylene chain. The compounds possess pharmacological, in particular antiarrhythmic, properties.
摘要翻译：对应于下式的其中R 1，R 2，R 5，R 6，R 7和R 8和R 9可以是氢或低级烷基，或者R 5和R 6和/或R 8的3-（氨基烷基氨基羰基甲氧基）-5-苯基吡唑化合物其中R 9还可以形成指定的环状基团，R 3和R 4可以是氢，卤素，低级烷基，低级烷氧基，三氟甲基，硝基，羟基或亚烷基二氧基，Z表示亚烷基链或2-羟基丙烯链。该化合物具有药理学，特别是抗心律不齐的特性。

8. 发明授权

US5679699A (Phenylalkylaminoalkyloxy) -heteroaryl-compounds, processes and intermediates for their production and pharmaceutical compositions containing them 失效
标题翻译：（苯基烷基氨基烷氧基） - 杂芳基化合物，其制备方法和中间体以及含有它们的药物组合物
公开(公告)号：US5679699A
公开(公告)日：1997-10-21
申请号：US576699
申请日：1995-12-21
申请人： Wolfgang Kehrbach , Michael Mlinaric , Dieter Ziegler , Reinhard Brueckner , Willi Bielenberg
发明人： Wolfgang Kehrbach , Michael Mlinaric , Dieter Ziegler , Reinhard Brueckner , Willi Bielenberg
IPC分类号： C07D231/20 , C07D261/12 , C07D271/06 , C07D271/07 , C07D285/08 , C07D401/12 , A61K31/415 , C07D403/12
CPC分类号： C07D271/07 , C07D231/20 , C07D261/12 , C07D285/08 , C07D401/12
摘要： 3-(Phenylalkylaminoalkyloxy)-heteroaryl compounds having heart rate lowering and/or anti-ischemic effects, methods for their preparation and pharmaceutical compositions containing them are described. The compounds correspond to the general formula I ##STR1## or to the general formula XXXI ##STR2## in which the substituents have the meanings given in the specification.
摘要翻译：描述了具有心率降低和/或抗缺血效果的3-（苯基烷基氨基烷氧基） - 杂芳基化合物，其制备方法和含有它们的药物组合物。所述化合物对应于通式I IMAGE> XXXI，其中取代基具有本说明书中给出的含义。

9. 发明授权

US5547967A (Phenylalkylaminoalkyloxy)-heteroaryl-compounds, processes and intermediates for their production and pharmaceutical compositions containing them 失效
标题翻译：（苯基烷基氨基烷氧基） - 杂芳基化合物，其制备方法和中间体以及含有它们的药物组合物
公开(公告)号：US5547967A
公开(公告)日：1996-08-20
申请号：US476118
申请日：1995-06-07
申请人： Wolfgang Kehrbach , Michael Mlinaric , Dieter Ziegler , Reinhard Brueckner , Willi Bielenberg
发明人： Wolfgang Kehrbach , Michael Mlinaric , Dieter Ziegler , Reinhard Brueckner , Willi Bielenberg
IPC分类号： C07D231/20 , C07D261/12 , C07D271/06 , C07D271/07 , C07D285/08 , C07D401/12 , A61K31/41 , A61K31/42 , C07D413/04 , C07D417/04
CPC分类号： C07D271/07 , C07D231/20 , C07D261/12 , C07D285/08 , C07D401/12
摘要： 3-(Phenylalkylaminoalkylozy)-heteroaryl compounds having heart rate lowering and/or anti-ischemic effects, methods for their preparation and pharmaceutical compositions containing them are described. The compounds correspond to the general formula I ##STR1## or to the general formula XXXI ##STR2## in which the substituents have the meanings given the specification.
摘要翻译：描述了具有心率降低和/或抗缺血效果的3-（苯基烷基氨基烷基） - 杂芳基化合物，其制备方法和含有它们的药物组合物。这些化合物对应于通式I IMAGE> XXXI，其中取代基具有给定的说明书的含义。

10. 发明授权

US4912113A 3,7-diazabicyclo(3,3,1)nonane compounds and pharmaceutical compositions containing such compounds 失效
标题翻译： 3,7-二氮杂双环（3,3,1）壬烷化合物和含有这些化合物的药物组合物
公开(公告)号：US4912113A
公开(公告)日：1990-03-27
申请号：US239766
申请日：1988-09-02
申请人： Uwe Schon , Wolfgang Kehrbach , Gerd Buschmann , Ulrich Kuhl , Dieter Ziegler
发明人： Uwe Schon , Wolfgang Kehrbach , Gerd Buschmann , Ulrich Kuhl , Dieter Ziegler
IPC分类号： A61K31/435 , A61P9/00 , A61P9/06 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10
摘要： 3,7-Diazabicyclo[3,3,1]nonane compounds having valuable heart rate-affecting pharmacological properties corresponding to the Formula I: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is lower alkyl,R.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents a benzhydryl group, optionally substituted by halogen, lower alkoxy, lower alkyl, hydroxy or trifluoromethyl, or a cinnamyl group optionally substituted by halogen, lower alkyl, lower alkoxy, hydroxy, nitro or trifluoromethyl.
摘要翻译：对应于式I的具有有价值的心率影响的药理学性质的3,7-二氮杂双环[3,3,1]壬烷化合物：其中R1是烷基，环烷基烷基或苄基，R2是低级烷基，R3是低级烷基，或R 2和R 3一起形成亚烷基链，并且R 4表示任选被卤素，低级烷氧基，低级烷基，羟基或三氟甲基取代的二苯甲基，或任选被卤素，低级烷基，低级烷氧基，羟基，硝基或三氟甲基。

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