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21. 发明授权

US3988317A Heterocyclic-substituted nebularin compounds 失效
标题翻译：杂环取代的蓝莓蛋白化合物
公开(公告)号：US3988317A
公开(公告)日：1976-10-26
申请号：US303290
申请日：1972-11-02
申请人： Wolfgang Kampe , Klaus Koch , Kurt Stach , Harald Stork , Felix Helmut Schmidt
发明人： Wolfgang Kampe , Klaus Koch , Kurt Stach , Harald Stork , Felix Helmut Schmidt
IPC分类号： C07H19/167 , C07D473/00 , C07H19/16
CPC分类号： C07H19/16
摘要： New heterocyclic-substituted nebularin compounds of the formula: ##SPC1##WhereinR.sub.1 is hydrogen, halogen or amino;R.sub.2 and R.sub.3, which may be the same or different, are hydrogen, hydroxyl, lower alkyl, alkoxy or hydroxyalkyl; andn is 2 or 3 or, when R.sub.1 is a halogen atom or an amino group, n can also be 1; and the pharmacologically compatible salts thereof;Are outstandingly effective in reducing body fat levels in mammals, e.g., the concentration of free fatty acids, of triglycerides and of cholesterol in serum.
摘要翻译：新的具有下式的杂环取代的新型白蛋白化合物：

22. 发明授权

US4906666A Hydroxamic acids and pharmaceutical compositions containing them, and anti-allergic use thereof 失效
标题翻译：羟肟酸和含有它们的药物组合物及其抗过敏应用
公开(公告)号：US4906666A
公开(公告)日：1990-03-06
申请号：US11096
申请日：1987-02-05
申请人： Erhard Reinholz , Walter-Gunar Friebe , Wolfgang Kampe , Jurgen Mertin , Otto-Henning Wilhelms
发明人： Erhard Reinholz , Walter-Gunar Friebe , Wolfgang Kampe , Jurgen Mertin , Otto-Henning Wilhelms
IPC分类号： A61K31/10 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/235 , A61K31/26 , A61K31/275 , A61K31/41 , A61P11/00 , A61P29/00 , A61P37/08 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/18 , C07C317/44 , C07C323/12 , C07C323/14 , C07C323/20 , C07C323/52 , C07C323/54 , C07C323/60 , C07C325/00 , C07C331/04 , C07D257/04 , C07D257/06
CPC分类号： C07D257/04 , A61K31/10 , A61K31/26 , A61K31/275 , C07C323/12 , C07C323/52 , C07C323/60 , C07C331/04 , C07D257/06
摘要： The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## CN, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.1 is a hydrogen atom, an alkyl radical optionally substituted by cycloalkyl or an alkenyl, cycloalkyl, aralkyl or aryl radical, wherein the aromatic moiety can be substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen; and the pharmacologically acceptable salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them for combating allergic diseases.
摘要翻译：本发明提供以下通式的化合物：其中Ar是任选被烷基，烯基，烷氧基，烷硫基，烷酰基，羟基，羟基烷基，羧基，烷氧基羰基，氨基甲酰基，硝基，氨基或卤素取代的苯基 A是直链或支链，饱和或不饱和的C1-C8脂族烃基，其任选被羟基取代，n是0,1或2，B是直链或支链的饱和或不饱和的C1- C8-脂族烃基，R是5-（1H） - 四唑基，-CO-NH-四唑基，CN，SCN，OH，卤素，5-（1H） - 四唑基硫代， NH-R1，其中R1是氢原子，任选被环烷基或烯基，环烷基，芳烷基或芳基取代的烷基，其中芳族部分可以被烷基，烯基，烷氧基，烷硫基，烷酰基，羟基，羟烷基，羧基，烷氧基羰基，氨基甲酰基，硝基，氨基或卤素; 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和含有它们的用于防治过敏性疾病的药物组合物。

23. 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.

24. 发明授权

US4517183A N-Substituted aziridine-2-carboxylic acid derivatives 失效
公开(公告)号：US4517183A
公开(公告)日：1985-05-14
申请号：US495548
申请日：1983-05-17
申请人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
发明人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
IPC分类号： A61K31/395 , A61K31/396 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P35/00 , A61P37/00 , A61P37/06 , C07D203/22 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D203/22 , Y10S514/885
摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

25. 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。

26. 发明授权

US4229464A Aminopropanol substituted indole compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：氨基丙醇取代的吲哚化合物和用于治疗心脏和循环系统疾病的组合物
公开(公告)号：US4229464A
公开(公告)日：1980-10-21
申请号：US943512
申请日：1978-09-18
申请人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/43 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/02 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/18 , C07D209/20
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , Y10S514/927
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏和循环系统疾病方面非常有效。

27. 发明授权

US4904666A Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use 失效
标题翻译：吡唑并（3,4-d）嘧啶化合物，组合物和使用方法
公开(公告)号：US4904666A
公开(公告)日：1990-02-27
申请号：US181729
申请日：1988-04-14
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Otto-Henning Wilhelms
IPC分类号： A61K31/505 , A61K31/519 , A61P11/08 , A61P11/16 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供通式如下的吡唑并[3,4-d] - 嘧啶：其中R 1为C 1至C 6 - 烷基，C 2至C 6链烯基，C 3至C 7环烷基基团或芳基，R 2是C 2至C 6 - 烯基，C 3至C 7 - 环烷基或在烷基部分具有1至6个碳原子的芳烷基或杂烷基，如果需要，卤素，C1至C6烷基，羟基，C1至C6烷氧基，C1至C3-卤代烷基，C3至C7-烷氧基羰基，氨基羰基，C2至C7-烷基氨基羰基，C3至C13-二烷基氨基羰基，氰基或C1至C6-烷硫基并且R 3是氢原子或C 2至C 6烷基如果需要，被羟基取代一次或多次，或者是四氢呋喃基或四氢吡喃基，条件是当R 1是甲基时，R 2不能是未被取代的苄基，以及其与无机和有机酸的生理上可接受的盐。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。

28. 发明授权

US4321194A N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation 失效
标题翻译： N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激
公开(公告)号：US4321194A
公开(公告)日：1982-03-23
申请号：US59863
申请日：1979-07-23
申请人： Elmar Bosies , Herbert Berger , Wolfgang Kampe , Uwe Bicker , Alfred Grafe
发明人： Elmar Bosies , Herbert Berger , Wolfgang Kampe , Uwe Bicker , Alfred Grafe
IPC分类号： C07D203/08 , A61K31/395 , A61K31/396 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P37/04 , C07D203/06 , C07D401/04 , C07D403/06 , C07D405/04 , C07D409/04 , C07D203/10 , C07D203/12 , C07D203/14
CPC分类号： C07D203/06 , Y10S514/885
摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.
摘要翻译：其中X是羧基，腈，烷氧基羰基或氨基甲酰基的氮杂环丁烷-2-羧酸衍生物，R和R 1是各种有机基团或其药理学上可接受的盐，具有显着的免疫刺激活性，特别是与添加化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素。那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。

29. 发明授权

US4224438A Adenosine-5'-carboxylic acid amides 失效
标题翻译：腺苷-5'-羧酸酰胺
公开(公告)号：US4224438A
公开(公告)日：1980-09-23
申请号：US161338
申请日：1971-07-09
申请人： Erich Fauland , Wolfgang Kampe , Max Thiel , Karl Dietmann , Wolfgang Juhran
发明人： Erich Fauland , Wolfgang Kampe , Max Thiel , Karl Dietmann , Wolfgang Juhran
IPC分类号： C07H19/16 , A61K31/70 , C07H19/18
CPC分类号： C07H19/16
摘要： Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.
摘要翻译：具有以下通式的腺苷-5'-羧酸衍生物：其中Z为两个氢原子或二价低级亚烷基，其中R 1和R 2独立为氢，羟基，氨基，低级烷基，低级烯基，任选N-烷基化的低级氨基烷基，环烷基，羟基烷基或哌啶基，或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基或亚氨基，亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。虽然酯具有一些活性，但它们可用于制备以标记的冠状动脉为特征的酰胺。

30. 发明授权

US4171446A Indazole compounds 失效
标题翻译：吲唑化合物
公开(公告)号：US4171446A
公开(公告)日：1979-10-16
申请号：US790646
申请日：1977-04-25
申请人： Fritz Wiedemann , Wolfgang Kampe
发明人： Fritz Wiedemann , Wolfgang Kampe
IPC分类号： C07D231/56 , C07D301/00 , C07D405/12
CPC分类号： C07D231/56
摘要： Indazole compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R' is hydrogen or acyl, e.g., alkanoyl, andR.sub.2 is benzyl or a radical of the general formula ##STR2## in which X is a reactive residue and Y is hydroxyl or X and Y together represent oxygen and, when R' is an acyl radical, R.sub.2 can also be hydrogen:Are valuable intermediates for the preparation of pharmacologically active compounds, e.g., adrenergic .beta.-receptor active 3-indazolyl-(4)-oxy-propan-2-ol-amines.
摘要翻译：式（I）的吲唑化合物，其中R 1是氢或低级烷基，R'是氢或酰基，例如烷酰基，R 2是苄基或通式为“IMAGE”的基团，其中X是反应性残基，Y是羟基或X和Y一起代表氧，当R'是酰基时，R 2也可以是氢：

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