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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

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。

3. 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。

4. 发明授权

US4346093A Heterocyclic oxypropanolamine compounds and pharmaceutical compositions 失效
公开(公告)号：US4346093A
公开(公告)日：1982-08-24
申请号：US117190
申请日：1980-01-31
申请人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Wolfgang Bartsch , Karl Dietmann
发明人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D251/72 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P9/00 , A61P9/08 , A61P9/12 , A61P25/02 , C07D209/04 , C07D209/08 , C07D209/42 , C07D209/43 , C07D231/56 , C07D233/00 , C07D235/02 , C07D235/06 , C07D235/26 , C07D235/28 , C07D249/08 , C07D249/18 , C07D401/12 , C07D405/12 , A61K31/41
CPC分类号： C07D209/08 , C07D209/42 , C07D235/26 , C07D249/18 , Y10S514/929
摘要： The present invention provides heterocyclic oxypropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl, aralkyl or lower alkanoyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl, hydroxyalkyl, alkoxycarbonyl or alkanoyloxyalkyl radicals or together represent an alkylene radical, R.sub.4 is a hydrogen atom or a lower alkanoyl radical or an aroyl radical, R.sub.5 is a hydrogen atom or a lower alkyl radical or an aralkyl radical, R.sub.6 is a hydrogen atom or a lower alkyl radical, R.sub.7 is a hydrogen atom, a hydroxyl group or a lower alkyl radical, Z is a valency bond, a methylene radical or an oxygen or sulphur atom, Ar is a carbocyclic aryl radical or a pyridyl radical, R.sub.8, R.sub.9 and R.sub.10, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, lower alkyl radicals, lower alkenyl radicals, lower alkoxy radicals, aralkoxy radicals, allyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or lower alkanoylamino radicals or R.sub.8 and R.sub.9 together represent a lower alkylenedioxy radical or R.sub.7 and R.sub.8 together represent a --CH.sub.2 --O-- radical and A is --X.sub.1 --Y.sub.1, in which X.sub.1 is a methylene or --NR.sub.11 -- radical, R.sub.11 being a hydrogen atom or a lower alkyl radical, and Y.sub.1 is a methylene radical or .dbd.C.dbd.Q, Q being an oxygen or sulphur atom; or A is --X.sub.2 .dbd.Y.sub.2 --, in which X.sub.2 and Y.sub.2, which can be the same or different and signify nitrogen atoms or .dbd.C(R.sub.12)-- groups, R.sub.12 being a hydrogen atom or a lower alkyl or an alkoxycarbonyl radical, and when --X.sub.2 .dbd.Y.sub.2 -- represents a --CH.dbd.N-- group and R.sub.1 is an alkyl or aralkyl radical, because of the ability of indazole to tautomerise, this can also be localized on the nitrogen atom represented by Y.sub.2, with the proviso that Y.sub.1 or Y.sub.2 is joined to .dbd.N--R.sub.1 in general formula (I), and, when Q is an oxygen atom or --X.sub.2 .dbd.Y.sub.2 -- represents --CR.sub.12 .dbd.CR.sub.12 -- and Z is a valency bond or when --X.sub.1 --Y.sub.1 -- represents ##STR2## and Z is an oxygen atom or a valency bond, either the two symbols R.sub.2 and R.sub.3 do not simultaneously represent hydrogen atoms or R.sub.7 and R.sub.8 together must form a --CH.sub.2 --O-- radical; and the pharmacologically 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 of cardiac and circulatory diseases.

5. 发明授权

US4288442A Inhibiting adrenergic .beta.-receptors with piperidinopropyl derivatives 失效
标题翻译：用哌啶丙基衍生物抑制肾上腺素β受体
公开(公告)号：US4288442A
公开(公告)日：1981-09-08
申请号：US117172
申请日：1980-01-31
申请人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Gisbert Sponer , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Gisbert Sponer , Wolfgang Schaumann
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61K31/4523 , A61K31/505 , A61P9/08 , A61P9/12 , A61P25/02 , C07C205/56 , C07D209/04 , C07D209/08 , C07D209/82 , C07D211/14 , C07D211/22 , C07D235/04 , C07D401/14 , A61K31/445
CPC分类号： C07D211/22 , C07C205/56
摘要： A piperidinopropyl derivative of the formula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical, or together are an alkylene radical,R.sub.3 is hydrogen, hydroxy, or acyloxy,R.sub.4 is hydrogen or formyl,A together with the adjacent benzene ring and N-R.sub.4 forms a benzimidazolin-2-one, benzimidazoline-2-thione, oxindole, indazole carbazole, benztriazole, benzimidazole, indoline or indole moiety, andB is a heterocyclic radical or, under certain circumstances, a phenyl radical, either of which is optionally substituted by halogen, hydroxy, lower alkyl, hydroxy-lower alkyl, carboxamido-lower alkyl, lower alkoxy, amino, carboxamido, lower alkyl-carbonylamino, acyl or lower alkylsulphonylamino,or a pharmacologically acceptable salt thereof. The compounds inhibit adrenergic .beta.-receptors and lower blood pressure.
摘要翻译：其中R 1和R 2各自独立地是氢或低级烷基，或者一起是亚烷基，R 3是氢，羟基或酰氧基，R 4是氢或甲酰基，A和相邻的苯环和N-R4形成苯并咪唑啉-2-酮，苯并咪唑啉-2-硫酮，羟吲哚，吲唑咔唑，苯并三唑，苯并咪唑，二氢吲哚或吲哚部分，B为杂环基团，或在某些情况下为苯基羟基，低级烷基，羟基 - 低级烷基，甲酰胺基 - 低级烷基，低级烷氧基，氨基，甲酰氨基，低级烷基 - 羰基氨基，酰基或低级烷基磺酰基氨基，或其药理学上可接受的盐。这些化合物抑制肾上腺素能β受体和降低血压。

6. 发明授权

US5411989A Nitric acid esters of cyclohexanol derivatives 失效
标题翻译：环己醇衍生物的硝酸酯
公开(公告)号：US5411989A
公开(公告)日：1995-05-02
申请号：US168163
申请日：1993-12-17
申请人： Helmut Michel , Wolfgang Bartsch
发明人： Helmut Michel , Wolfgang Bartsch
IPC分类号： A61K31/16 , A61K31/04 , A61K31/18 , A61K31/19 , A61K31/21 , A61K31/215 , A61K31/265 , A61K31/275 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07C203/02 , C07C203/08 , C07C233/12 , C07C233/19 , C07C233/23 , C07C233/60 , C07C235/08 , C07C235/14 , C07C235/40 , C07C237/22 , C07C255/19 , C07C259/08 , C07C271/24 , C07C311/07 , C07C311/14 , C07D207/26 , C07D207/28 , C07D213/81 , C07D213/82 , C07D213/89 , C07D257/00 , C07D257/04 , C07D257/06 , C07D295/185 , C07C233/08 , C07C309/26
CPC分类号： C07D213/81 , C07C233/19 , C07C233/23 , C07C235/08 , C07C235/14 , C07C235/40 , C07C237/22 , C07C255/19 , C07C259/08 , C07C271/24 , C07C311/07 , C07D207/28 , C07D213/82 , C07D295/185 , C07C2101/14
摘要： The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.
摘要翻译：本发明涉及式I的环己醇的硝酸酯，其中A表示价键或C1-C6-亚烷基链，B表示基团-NR1-CO-Z，-NR1-SO2-Z或 -CO-NR 2 -Z，其中R 1表示氢或C 1 -C 6烷基烷基R 2氢，羟基，羟基-C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基或C 2 -C 6 - 炔基，Z表示氢，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基或C 2 -C 6 - 炔基，其可以任选地取代B为-NR 1 -CO-Z基团的情况 Z也可以表示C1-C6-烷氧基。

7. 发明授权

US5037849A Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof 失效
标题翻译：含有硝基烷基胺，新型硝基烷基胺的药物组合物及其制备方法
公开(公告)号：US5037849A
公开(公告)日：1991-08-06
申请号：US424452
申请日：1989-10-20
申请人： Herbert Simon , Helmut Michel , Michael Schultz , Wolfgang Bartsch
发明人： Herbert Simon , Helmut Michel , Michael Schultz , Wolfgang Bartsch
IPC分类号： A61K31/21 , A61K31/395 , A61K31/40 , A61K31/445 , A61P9/00 , A61P9/08 , A61P9/10 , C07C235/10 , C07C235/26 , C07C235/40 , C07C237/08 , C07C237/18 , C07C275/10 , C07C275/14 , C07C275/16 , C07C275/26 , C07D211/06 , C07D295/13 , C07D295/14 , C07D295/215
CPC分类号： C07D295/215 , A61K31/21 , C07C235/10 , C07C235/26 , C07C235/40 , C07C237/08 , C07C275/10 , C07C275/14 , C07C275/16 , C07C275/26 , C07D295/13 , C07C2101/14
摘要： The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.3 is a hydrogen atom or a lower-alkyl radical, when X is an --NR.sup.3 --CO-- radical, R.sup.3, together with the nitrogen atom and a carbon atom of the group A, bridge a heterocyclic ring containing 4 to 6 carbon atoms or R.sup.3, together with R.sup.2, A and the two nitrogen atoms, bridge a heterocyclic ring containing 3 to 5 carbon atoms; and the optically-active forms and physiologically acceptable salts thereof.
摘要翻译：本发明提供了有效抗心绞痛的心脏和循环系统疾病的药物组合物，其含有至少一种以下通式的硝基烷基胺衍生物：其中R 1是氢原子，低级烷基，C 3 -C 8 - 环烷基或C 3 -C 8 - 环烯基，氨基羰基，C 1 -C 6 - 单 - 或二 - 烷基氨基羰基，R 2是氢原子，低级烷基或C 3 -C 8 - 环烷基或环烯基或R 2，连同 R1和它们所连接的氮原子形成含有至多6个碳原子的杂脂族环，A是价键或直链或支链的低级亚烷基，其中-CH 2 - 基团可以被亚环烷基，B是低级亚烷基，其中-CH 2 - 基团可被亚环烷基代替，X是-NR 3 -CO-或-CO-NR 3 - 基，其中R 3是氢原子或低级烷基，当X是-NR 3 -CO-基时，R 3与硝基一起形成原子和A基团的碳原子，桥接含有4至6个碳原子的杂环或R3与R2，A和两个氮原子一起桥接含有3至5个碳原子的杂环; 和其光学活性形式和生理上可接受的盐。

8. 发明授权

US5030641A Cyclic azaaliphatic compounds with a nitroxy function, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：具有硝基官能团的环状氮杂脂族化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5030641A
公开(公告)日：1991-07-09
申请号：US424451
申请日：1989-10-20
申请人： Herbert Simon , Helmut Michel , Michael Schultz , Wolfgang Bartsch
发明人： Herbert Simon , Helmut Michel , Michael Schultz , Wolfgang Bartsch
IPC分类号： C07D211/56 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61P9/12 , C07D207/16 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/62
CPC分类号： C07D211/58 , C07D207/16 , C07D211/46 , C07D211/60 , C07D211/62
摘要： The present invention provides anti-angina pharmaceutical compositions containing at least one compound of the formula: ##STR1## wherein n is 1 or 2, R is a hydrogen atom or an H-(C.sub.1 -C.sub.8)-alkylene, hydroxy-(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N-(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N-(C.sub.1 -C.sub.8)-alkylene-CO--, R.sup.1 R.sup.2 N-CO-NR.sup.3 -(C.sub.1 -C.sub.8)-alkylene or R.sup.1 R.sup.2 N-CO-- radical, A is a valency bond or an --NR.sup.4 --CO-- or --CO--NR.sup.4 -- radical, R.sup.4 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated of cyclic alkyl radical containing up to 6 carbon atoms and B is a valency bond or a straight-chained or branched alkylene chain containing up to 8 carbon atoms, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms.
摘要翻译：本发明提供含有至少一种下式的化合物的抗心绞痛药物组合物：其中n为1或2，R为氢原子或H-（C1-C8） - 亚烷基，羟基 - （C1-C8） - 亚烷基，R1R2N-（C1-C8） - 亚烷基，R1R2N-（C1-C8） - 亚烷基-CO-，R1R2N-CO-NR3-（C1-C8） - 亚烷基或R1R2N-CO- A是价键或-NR4-CO-或-CO-NR4-基，R4是氢原子或直链或支链，饱和或不饱和的含有至多6个碳原子的环烷基，B是含有至多8个碳原子的价键或直链或支链亚烷基链，其中-CH 2 - 基团可被含有3至7个碳原子的亚环烷基代替。

9. 发明授权

US4642309A Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效
公开(公告)号：US4642309A
公开(公告)日：1987-02-10
申请号：US780704
申请日：1985-09-26
申请人： Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
发明人： Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P25/02 , C07D209/34 , C07D401/06 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
摘要： The present invention provides indolin-2-one derivatives of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl radical or a radical of the general formula: ##STR2## in which A is a straight-chained or branched C.sub.2 -C.sub.4 alkylene radical and Z is an oxygen or sulphur atom, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, C.sub.2 -C.sub.6 alkanoyl radicals, C.sub.2 -C.sub.4 alkenyl radicals, C.sub.2 -C.sub.4 alkynyl radicals, C.sub.1 -C.sub.6 alkyl radicals, C.sub.1 -C.sub.6 alkoxy radicals, C.sub.2 -C.sub.4 alkenyloxy radicals, C.sub.2 -C.sub.4 alkynyloxy radicals, C.sub.1 -C.sub.6 alkylthio radicals, C.sub.2 -C.sub.6 alkanoylamido radicals or radicals of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 alkyl radicals or C.sub.3 -C.sub.10 cycloalkyl radicals or R.sub.4 and R.sub.5 together represent a C.sub.2 -C.sub.8 alkylene radical optionally interrupted by an oxygen or sulphur atom or by an >N-R.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical, X is a hydrogen atom, Y is a hydrogen atom or a group of the general formula ##STR4## in which Q is a hydrogen atom or, together with X, can also represent a bond and R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxyl or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by halogen, hydroxyl, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulphinyl, C.sub.1 14 C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, methylenedioxy, nitro, cyano or amino, with the proviso that R.sub.1 cannot be a C.sub.1 -C.sub.6 alkyl radical when X and Y are both hydrogen atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides intermediates of the general formula: ##STR5## in which R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxy or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by hydroxyl, halogen, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 14 C.sub.6 alkylsulphinyl, cyano C.sub.1 -C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, nitro amino or methylenedioxy.Furthermore, the invention provides processes for the preparation of the above indolin-2-one derivatives and the above intermediates, as well as pharmaceutical compositions containing the above indolin-2-one derivatives.

10. 发明授权

US4442295A 3-Cyano indoles as intermediates for cardioselective compounds 失效
标题翻译： 3-氰基吲哚作为心脏选择性化合物的中间体
公开(公告)号：US4442295A
公开(公告)日：1984-04-10
申请号：US288077
申请日：1981-07-29
申请人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch
发明人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , C07D209/12 , C07D209/14 , C07D209/42 , C07D209/43 , C07D405/12 , C07D209/04
CPC分类号： C07D405/12 , C07D209/12 , C07D209/14 , C07D209/42
摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: ##STR2## in which B is a reactive group or, together with R.sub.5, represents a valency bond, and R.sub.5 is a hydrogen atom or an aliphatic or aromatic acyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen atom, a methyl radical or a --CH.sub.2 --O--R.sub.5 radical, R.sub.5 having the same meaning as above, and R.sub.4 is an aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, with the proviso that R.sub.1 is not an aralkyl radical when R.sub.4 is a formyl radical. The present invention also provides processes for the preparation of these compounds. Furthermore, the present invention is concerned with the use of these compounds for the preparation of compounds with a heart and circulatory activity.
摘要翻译：本发明提供以下通式的吲哚衍生物：其中R 1是氢原子，芳烷基或具有以下通式的基团：其中B是反应性基团，或与R 5一起表示价键，R5表示氢原子或脂肪族或芳香族酰基，R2表示氢原子或低级烷基，R3表示氢原子，甲基或-CH2-O-R5基， R5具有与上述相同的含义，R4是氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基，条件是当R 4是甲酰基时，R 1不是芳烷基。本发明还提供了这些化合物的制备方法。此外，本发明涉及这些化合物用于制备具有心脏和循环活性的化合物的用途。

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