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1. 发明授权

US4479962A Indazoloxypropanolamine derivatives and use in combating, and for the prophylaxis of, cardiac and circulatory diseases 失效
标题翻译： Indazoloxypropanolamine衍生物，用于对抗和预防心脏和循环系统疾病
公开(公告)号：US4479962A
公开(公告)日：1984-10-30
申请号：US403968
申请日：1982-08-02
申请人： Fritz Wiedemann , Helmut Michel , Wolfgang Weckerle , Egon Roesch , Klaus Strein
发明人： Fritz Wiedemann , Helmut Michel , Wolfgang Weckerle , Egon Roesch , Klaus Strein
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/433 , A61K31/495 , A61K31/496 , A61P9/04 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/43 , C07D209/44 , C07D209/88 , C07D231/56 , C07D235/04 , C07D235/06 , C07D235/08 , C07D235/26 , C07D241/40 , C07D241/42 , C07D249/18 , C07D285/14
CPC分类号： C07D285/14 , C07D209/08 , C07D209/88 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/26 , C07D241/42 , C07D249/18
摘要： The present invention provides heteroaryloxypropanolamines and pharmaceutical compositions containing them, for combating, and for the prophylaxis of, cardiac and circulatory diseases. The heteroaryloxypropanolamines of the present invention are of the general formula: ##STR1## wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straight-chained or branched alkylene chain containing 2 to 6 carbon atoms, R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulfur or oxygen and R.sub.6, R.sub.7 and R.sub.8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R.sub.6 and R.sub.7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.
摘要翻译：本发明提供含有它们的异丙氧基丙醇胺和含有它们的药物组合物，用于对抗和预防心脏和循环系统疾病。本发明的杂芳氧基丙酰胺具有以下通式：其中A是双环或三环杂芳族基，其任选地部分氢化，X是含有2-6个碳原子的直链或支链亚烷基链，R 1 和R 2可以相同或不同，为氢原子或低级烷基或苄基，R 3，R 4和R 5可相同或不同，为氢原子或低级烷基，苄基，甲酰基，低级烷酰基，氰基，羟甲基，低级烷氧基羰基或氨基甲酰基或二价取代基硫或氧，R 6，R 7和R 8可以相同或不同，为氢或卤原子，低级烷基，硝基，氨基，低级烷硫基或低级烷氧基或 R6和R7一起表示任选不饱和的三亚甲基链; 及其药理学上可接受的盐。本发明还提供了制备这些化合物的方法，以及含有它们的药物组合物。

2. 发明授权

US4835280A Indoline compounds for synthesis of pharmaceutically active pyrrolobenzimidazoles 失效
标题翻译：用于合成药物活性吡咯并苯并咪唑的二氢吲哚化合物
公开(公告)号：US4835280A
公开(公告)日：1989-05-30
申请号：US72917
申请日：1987-07-14
申请人： Alfred Martens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckman , Klaus Strein , Egon Roesch
发明人： Alfred Martens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckman , Klaus Strein , Egon Roesch
IPC分类号： C07D403/12 , C07D405/12 , C07D487/04
CPC分类号： C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要翻译：本发明提供下式的吲哚衍生物：下式的有用的药物活性吡咯并苯并咪唑或其互变异构体：（I）这些化合物可用于治疗心脏或循环系统疾病，特别是那些对血压变化作出反应，心输出量增加和/或微循环变化的疾病。

3. 发明授权

US4695567A Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases 失效
标题翻译：吡咯并苯并咪唑，含有它们的药物组合物和使用它们治疗某些心脏和循环系统疾病的方法
公开(公告)号：US4695567A
公开(公告)日：1987-09-22
申请号：US820259
申请日：1986-01-17
申请人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
发明人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/50 , A61K31/505 , A61P9/00 , A61P9/04 , C07D403/12 , C07D405/12 , C07D487/04 , C07D403/06
CPC分类号： C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要翻译：本发明提供了以下通式的吡咯并苯并咪唑或其互变异构体：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 7环烷基; R2是氢，氰基，C1-C6烷基，C2-C6烯基或被羟基，C1-C6烷基，C1-C6烷氧基，氨基，C1-C6烷基氨基，C2-C12二烷基氨基或肼基取代的羰基或R2 并且R 1与它们所连接的碳一起形成C 3 -C 8螺环烷基环，或者R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基，X是价键，C 1 -C 4亚烷基或亚乙烯基，T是氧或硫; 并且Het是呋喃基，噻吩基，吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基，噻二唑基，吡嗪基，嘧啶基或哒嗪基，其中杂环五元和六元环是未取代的或被一个或多个C 1 -C 6烷基 C 1 -C 6烷氧基，C 1 -C 6烷硫基，羟基，氧代，硝基，氨基，卤素，羧基，C 2 -C 7烷氧基羰基，氨基羰基或氰基; 或其生理上可接受的盐与无机或有机酸反应。这些化合物可用于治疗心脏或循环系统疾病，特别是那些响应血压变化，心输出量增加和/或微循环变化的化合物。

4. 发明授权

US4863949A Aminopropanol derivatives, processes for the preparation thereof, the use thereof and pharmaceutical compositions containing them 失效
标题翻译：氨基丙醇衍生物，其制备方法，其用途和含有它们的药物组合物
公开(公告)号：US4863949A
公开(公告)日：1989-09-05
申请号：US98719
申请日：1987-09-21
申请人： Herbert Simon , Helmut Michel , Wolfgang Bartsch , Klaus Strein
发明人： Herbert Simon , Helmut Michel , Wolfgang Bartsch , Klaus Strein
IPC分类号： C07D521/00 , A61K31/13 , A61K31/165 , A61K31/17 , A61K31/215 , A61K31/27 , A61K31/33 , A61K31/445 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/02 , C07C67/00 , C07C203/02 , C07C231/00 , C07C233/00 , C07C233/12 , C07C233/34 , C07C235/10 , C07C313/00 , C07C315/04 , C07C317/18 , C07C317/20 , C07C317/28 , C07C317/30 , C07C317/46 , C07C319/20 , C07C323/20 , C07D209/04 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/82 , C07D215/22 , C07D215/227 , C07D235/06 , C07D311/18
CPC分类号： C07D209/08 , C07C255/00 , C07D209/34 , C07D209/42 , C07D215/227 , C07D311/18
摘要： The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.1 -- group and a --CH.sub.2 -- group of the chain B, can form a heteroaliphatic ring containing 4 to 6 carbon atoms and n is 1, 2 or 3; and the physiologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the treatment and/or prophylaxis of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的化合物：其中Ar是取代或未取代的芳族或杂芳族基团，A是含有至多8个碳原子的直链或支链亚烷基链，-CH 2 - 基团其中可以被含有3至7个碳原子的亚环烷基代替，B是含有至多12个碳原子的直链单环或双环，任选支链，饱和或不饱和的亚烷基链，其中-CH 2 - 基团可以可以被含有3至7个碳原子的亚环烷基和/或最多两个-CH 2 - 基团取代，其中可以被氧或硫原子或-S（= O）或-S（= O）取代） 2基团，X是价键，氧原子或-NR 1基团，其中R 1是氢原子或含有至多6个碳原子的直链或支链，饱和或不饱和的烷基或硝基烷基或R 1，一起与-NR 1基团的氮原子和链B的-CH 2 - 基团可以相同 rm是含有4至6个碳原子的杂脂族环，n为1,2或3; 及其生理上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。此外，本发明涉及这些化合物用于治疗和/或预防心脏和循环系统疾病的用途。

5. 发明授权

US4826847A Beta-blocking oxindole derivatives 失效
标题翻译： β-阻断羟吲哚衍生物
公开(公告)号：US4826847A
公开(公告)日：1989-05-02
申请号：US948422
申请日：1986-12-30
申请人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
发明人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/02 , C07D209/34 , C07D209/96 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , A61K31/505
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06
摘要： The present invention provides oxindole derivatives of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The above compounds display nitrate-like as well as .beta.-blocking actions.
摘要翻译：本发明提供下式的羟吲哚衍生物：其中各种取代基在下文定义。上述化合物显示硝酸盐样和β-阻断作用。

6. 再颁专利

USRE40707E1 Use of carbazole compounds for the treatment of congestive heart failure 有权
标题翻译：使用咔唑化合物治疗充血性心力衰竭
公开(公告)号：USRE40707E1
公开(公告)日：2009-05-05
申请号：US10721022
申请日：1996-02-07
申请人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Howard Shusterman , Gisbert Spooner , Klaus Strein
发明人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Howard Shusterman , Gisbert Spooner , Klaus Strein
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , A61K31/7048 , A61K2300/00
摘要： A method of treatment using carvedilol is disclosed, wherein the carvedilol decreases the risk of mortality caused by congestive heart failure in patients. The patients are titrated with low amounts of carvedilol, with the initial titration dosage being only 10 to 30% of the daily maintenance dose.
摘要翻译：公开了使用卡维地洛的治疗方法，其中卡维地洛降低患者充血性心力衰竭引起的死亡风险。患者用少量卡维地洛滴定，初始滴定剂量仅为日常维持剂量的10至30％。

7. 发明授权

US5902821A Use of carbazole compounds for the treatment of congestive heart failure 失效
标题翻译：使用咔唑化合物治疗充血性心力衰竭
公开(公告)号：US5902821A
公开(公告)日：1999-05-11
申请号：US875603
申请日：1997-12-29
申请人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Shusterman , Gisbert Sponer , Klaus Strein
发明人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Shusterman , Gisbert Sponer , Klaus Strein
IPC分类号： C07D207/16 , A61K31/196 , A61K31/34 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/54 , A61K31/549 , A61K31/662 , A61K31/70 , A61K31/702 , A61K38/00 , A61K45/00 , A61K45/06 , A61P9/00 , A61P9/04 , C07D209/88
CPC分类号： A61K31/403 , A61K31/7048
摘要： A method of treatment using carvedilol is disclosed, wherein the carvedilol decreases the mortality caused by congestive heart failure in patients. The patients are titrated with low amounts of carvedilol, with the initial titration dosage being only 10 to 30% of the daily maintenance dose.
摘要翻译： PCT No.PCT / EP96 / 00498 Sec。 371 1997年12月29日第 102（e）1997年12月29日PCT PCT 1996年2月7日PCT公布。公开号WO96 / 24348 日本1996年8月15日公开了使用卡维地洛的治疗方法，其中卡维地洛降低患者充血性心力衰竭引起的死亡率。患者用少量卡维地洛滴定，初始滴定剂量仅为日常维持剂量的10至30％。

8. 发明授权

US5783558A Parathormone fragments, their preparation and medicaments containing these 失效
标题翻译： parathormone片段，它们的制备和含有这些的药物
公开(公告)号：US5783558A
公开(公告)日：1998-07-21
申请号：US256363
申请日：1994-07-20
申请人： Christian Duvos , Hubert Mayer , Bernd Mueller-Beckmann , Klaus Strein , Edgar Wingender
发明人： Christian Duvos , Hubert Mayer , Bernd Mueller-Beckmann , Klaus Strein , Edgar Wingender
IPC分类号： A61K38/22 , A61K38/00 , A61P3/00 , A61P19/10 , A61P43/00 , C07K14/575 , C07K14/635 , A61K38/29
CPC分类号： C07K14/635 , A61K38/00
摘要： The invention concerns parathormone (PTH) fragments including the amino acid range of the natural parathormone of +3 to +35 and their physiologically compatible derivatives, a process for the preparation of the fragments according to the solid phase and liquid phase synthesis from partly blocked amino acids contained in the fragments which are coupled with one another in the sequence which corresponds to the amino acid sequence in the fragments to be prepared and medicaments containing at least one of the fragments, especially with calcium-regulating action in the body.
摘要翻译： PCT No.PCT / EP93 / 00259 Sec。 371日期：1994年7月20日 102（e）日期1994年7月20日PCT提交1993年2月4日PCT公布。公开号WO93 / 15109 日期：1993年8月5日本发明涉及包含+3至+35的天然parathormone的氨基酸范围及其生理上相容的衍生物的parathormone（PTH）片段，根据固相和液相制备片段的方法从与待制备的片段中的氨基酸序列相对应的序列中彼此偶联的片段中包含的部分封闭的氨基酸合成，以及含有至少一个片段的药物，特别是在身体。

9. 发明授权

US4963686A Certain pyridinoylamino-indolin-2-one derivatives 失效
标题翻译：某些吡啶基氨基 - 二氢吲哚-2-酮衍生物
公开(公告)号：US4963686A
公开(公告)日：1990-10-16
申请号：US217143
申请日：1988-07-05
申请人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
发明人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/12 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D403/14 , C07D487/04 , C07D487/10 , C07D487/14
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D487/10
摘要： The new pyrrolobenzimidazoles according to the present invention are compounds of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom, an alkyl or alkenyl radical or a cyano group or a carbonyl group substituted by a hydroxyl or hydrazino group or by an alkyl, alkoxy, amino, alkylamino or dialkylamino group or together with R.sub.1 represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical, X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinylene radical, T is an oxygen or sulphur atom and Py is a 2-, 3- or 4-pyridyl radical which optionally carries an oxygen atom on the ring heteroatom and/or can be substituted one or more times by alkyl, alkoxy, hydroxyl, cyano or nitro, as well as by halogen; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.

10. 发明授权

US4831032A Cardiotonic benzimidazoles 失效
标题翻译：强心苯并咪唑
公开(公告)号：US4831032A
公开(公告)日：1989-05-16
申请号：US881983
申请日：1986-07-03
申请人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
发明人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P9/04 , A61P9/12 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/58 , C07D277/62 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D487/04 , C07D513/04
摘要： The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
摘要翻译：本发明提供以下通式的苯并咪唑：其中R1，X，A和R2如说明书中所定义。本发明还提供制备这些新的苯并咪唑和含有它们的药物组合物的方法，以及制备它们的中间体。新的苯并咪唑可用于治疗对降低血压，正性肌力作用和/或微循环改善作出反应的心脏或循环系统疾病。

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