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公开(公告)号：US3947404A
公开(公告)日：1976-03-30
申请号：US367312
申请日：1973-06-05
IPC分类号： C07J19/00 , A61K20060101 , C07D20060101
摘要： New dihydrodigoxin derivatives of the formula ##SPC1##Wherein one of R.sub.1 and R.sub.2 represents a methyl or ethyl radical and the other represents hydrogen, methyl, ethyl or acetyl (i.e. alkanoyl; and R.sub.3 is hydrogen or an acetyl group; are outstandingly effective for therapy of cardiac insufficiencies, particularly via peroral administration.
摘要翻译： 式R 1和R 2的新的二氢二磷杂衍生物代表甲基或乙基，另一个表示氢，甲基，乙基或乙酰基（即烷酰基; R 3是氢或乙酰基）;对治疗心脏功能不全有显着的效果 ，特别是通过口腔管理。
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公开(公告)号：US3981862A
公开(公告)日：1976-09-21
申请号：US558381
申请日：1975-03-14
IPC分类号： C07J19/00
CPC分类号： C07J19/005
摘要： A process for the preparation of a C22-alkyl-derivative of digoxin of the formula ##SPC1##In whichR.sub.1 is an alkyl radical containing up to 4 carbon atoms,R.sub.2 and R.sub.3 are selected from the group consisting of hydrogen, acyl, benzyl, carbobenzoxy, trimethylsilyl, tetrahydropyranyl or phosphonoacyl radicals or together form an alkylidene radical,Comprising reacting a compound of the formula ##SPC2##With an alkyl iodide of the formula R.sub.1 I in the presence of a strongly polar aprotic solvent and an alkali metal hydride. If R.sub.2 and R.sub.3 are other than hydrogen they can subsequently be replaced by hydrogen by hydrolysis or hydrogenation. The product can be .alpha.- or .beta.-methylated to produce compounds of high resorption and low toxicity.
摘要翻译： 制备式IN的地高辛的C22-烷基衍生物的方法，其中R1是含有至多4个碳原子的烷基，R2和R3选自氢，酰基，苄基，苄氧羰基，三甲基甲硅烷基 ，四氢吡喃基或膦酰基基团或一起形成亚烷基，在强极性非质子溶剂和碱金属氢化物的存在下，将式I化合物与式Ia化合物反应。 如果R2和R3不是氢，那么它们随后可以通过水解或氢化被氢代替。 该产物可以是α-甲基化或β-甲基化以产生高吸收和低毒性的化合物。
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公开(公告)号：US4436735A
公开(公告)日：1984-03-13
申请号：US439653
申请日：1982-11-05
IPC分类号： A61K31/704 , A61P9/00 , C07J19/00 , A61K31/585
CPC分类号： C07J19/005
摘要： The present invention provides ketals of 3'"-dehydrocardenolide tridigitoxosides of the general formula: ##STR1## in which R.sub.1 and R.sub.2 are identical alkyl radicals containing up to 3 carbon atoms or together represent a cyclic ketal containing 2 to 6 carbon atoms, R.sub.3 represents two hydrogen atoms, the group ##STR2## or the radical ##STR3## wherein R.sub.1 and R.sub.2 have the above-given meaning, and R.sub.4 is a hydrogen atom or a lower acyl or alkyl radical.The present invention also provides processes for the preparation of these ketals, as well as pharmaceutical compositions containing them, which are useful for the treatment of cardiac insufficiency.
摘要翻译： 本发明提供了通式为：其中R 1和R 2是含有至多3个碳原子的相同烷基或一起代表含有2至6个碳原子的环状缩酮的3“ - 脱氢伐尼洛德三唑一硫酮的缩酮 原子，R 3表示两个氢原子，基团
或基团 ，其中R 1和R 2具有上述含义，并且R 4是氢原子或低级酰基或烷基。 本发明还提供了制备这些缩酮的方法以及含有它们的药物组合物，其可用于治疗心功能不全。 -
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公开(公告)号：US4461763A
公开(公告)日：1984-07-24
申请号：US439654
申请日：1982-11-05
IPC分类号： C07J19/00 , A61K31/704 , A61P9/00 , C07J41/00
CPC分类号： C07J41/0016
摘要： The present invention provides 3'"-dehydrocardenolide tridigitoxoside oximes of the general formula: ##STR1## in which R.sub.1 is a hydrogen atom or an alkyl radical containing up to 3 carbon atoms, R.sub.2 is a hydrogen atom or a lower acyl or alkyl radical and R.sub.3 represents two hydrogen atoms, the group ##STR2## or the oximino group .dbd.NOR.sub.1, wherein R.sub.1 has the above-given meaning.The present invention also provides a process for the preparation of these oximes, as well as pharmaceutical compostions containing them which are useful for the treatment of cardiac insufficiency.
摘要翻译： 本发明提供具有以下通式的3' - 脱氢伐尼德定三叠氮酮肟：其中R 1是氢原子或含有至多3个碳原子的烷基，R 2是氢原子或低级酰基 或烷基，R 3表示两个氢原子，基团肟基或肟基= NOR1，其中R 1具有上述含义。 本发明还提供了制备这些肟的方法，以及含有它们的药物组合物，其可用于治疗心功能不全。
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5.发明授权Cardenolide-bis-digitoxoside alkyl compounds, pharmaceutical compositions and method of use 失效卡多内酯 - 二 - 二氧杂锇烷基化合物，药物组合物和使用方法
公开(公告)号：US4353895A
公开(公告)日：1982-10-12
申请号：US288442
申请日：1981-07-30
IPC分类号： A61K31/58 , A61P9/00 , C07J19/00 , A61K31/705
CPC分类号： C07J19/005
摘要： Cardioactive cardenolide-bis-digitoxosides of the formula ##STR1## in which R.sub.1 is a hydrogen atom, a hydroxyl group or an acyloxy radical containing up to 3 carbon atoms, andR.sub.2, R.sub.3 and R.sub.4 each independently is a hydrogen atom, an acyl radical containing up to 3 carbon atoms,with the proviso that the compound contains at least one alkyl radical. The compounds exhibit desirable rates of excretion, primarily extrarenally.
摘要翻译： 其中R 1为氢原子，羟基或含有至多3个碳原子的酰氧基的式“IMAGE”的心脏活性的心灵内酯 - 二 - 二氧杂硅氧烷，R2，R3和R4各自独立地为氢原子，酰基 含有至多3个碳原子，条件是该化合物含有至少一个烷基。 化合物显示出所需的排泄速率，主要是外消旋的。
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公开(公告)号：US4292314A
公开(公告)日：1981-09-29
申请号：US151481
申请日：1980-05-19
CPC分类号： C07J41/0016
摘要： The present invention provides 12-dehydrodigoxin oximes of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms, lower acyl radicals or lower alkyl radicals or R.sub.1 and R.sub.2 together can represent an alkylidene radical containing 2 to 6 carbon atoms and R.sub.3 is a hydrogen atom or a lower alkyl or aralkyl radical. The present invention also provides a process for the preparation of these oximes and pharmaceutical compositions containing them and is also concerned with the use of these oximes for the preparation of pharmaceuticals for the treatment of cardiac insufficiency.
摘要翻译： 本发明提供了以下通式的12-脱氢二氧in肟：其中R 1和R 2可以相同或不同，为氢原子，低级酰基或低级烷基，或者R 1和R 2一起可代表亚烷基 含有2至6个碳原子，且R 3是氢原子或低级烷基或芳烷基。 本发明还提供了制备这些肟和含有它们的药物组合物的方法，并且还涉及这些肟用于制备用于治疗心功能不全的药物的用途。
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公开(公告)号：US4107299A
公开(公告)日：1978-08-15
申请号：US738808
申请日：1976-11-04
申请人： Fritz Kaiser , Wolfgang Schaumann , Kurt Stach, deceased , by Werner Plattner, administrator , Wolfgang Voightlander
发明人： Fritz Kaiser , Wolfgang Schaumann , Kurt Stach, deceased , by Werner Plattner, administrator , Wolfgang Voightlander
IPC分类号： A61K31/704 , A61P9/04 , C07J19/00 , A61K31/705
CPC分类号： C07J19/005
摘要： 12-Epi-digoxins of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen or a lower alkanoyl or alkyl radical,R.sub.3 is hydrogen or a lower alkanoyl radical, andR.sub.4 is hydrogen or a lower alkyl, alkenyl or alkynyl radical,Are characterized by marked cardioactivity and therapeutic spectrum. They are produced by reduction of the corresponding 12-dehydrodigoxin.
摘要翻译： 其中R 1和R 2各自独立地为氢或低级烷酰基或烷基，R 3为氢或低级烷酰基，R 4为氢或低级烷基， 烯基或炔基，由标记的亲和力和治疗谱表征。 它们通过还原相应的12-dehydrodigoxin产生。
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公开(公告)号：US3959261A
公开(公告)日：1976-05-25
申请号：US482956
申请日：1974-06-25
IPC分类号： C07D333/20 , A61K31/255 , A61K31/34 , A61K31/38 , A61K31/395 , A61K31/41 , A61K31/63 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/40 , C07C311/39 , C07D20060101 , C07D237/00 , C07D239/00 , C07D241/00 , C07D251/00 , C07D257/02 , C07D257/04 , C07D307/00 , C07D307/52 , C07D307/54 , C07D333/06 , C07D333/10 , C07D333/22 , C07D333/24 , C07D405/10 , C07D407/10
CPC分类号： A61K31/63 , C07C311/39 , C07D307/52 , C07D333/20
摘要： Novel biphenyl derivatives of the formula: ##SPC1##WhereinR.sub.1 is phenyl, furyl or thienyl; andR.sub.2 is carboxyl or tetrazolyl-(5);And the pharmacologically compatible salts thereof display outstanding diuretic and saluretic properties.
摘要翻译： 下式的新型联苯衍生物：
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9.发明授权Aminopropanol compounds and compositions for the treatment of cardiac and circulatory diseases 失效用于治疗心脏和循环系统疾病的氨基丙醇化合物和组合物
公开(公告)号：US4152446A
公开(公告)日：1979-05-01
申请号：US805558
申请日：1977-06-10
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/08 , C07D209/12 , C07D209/42 , A61K31/40 , C07D209/04
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12
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; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。
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10.发明授权Phenoxyalkylcarboxylic acid compounds and serum-lipid and triglyceride depressing therapeutic compositions 失效苯氧基烷基羧酸化合物和血清 - 脂质和甘油三酯抑制治疗组合物
公开(公告)号：US4151303A
公开(公告)日：1979-04-24
申请号：US719878
申请日：1976-09-01
申请人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
发明人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
IPC分类号： A61K31/22 , A61K31/19 , A61P3/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/19 , C07C233/22 , C07C235/20 , C07C101/42 , A01N9/20
CPC分类号： C07C233/12
摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein A is aryl, aryloxy, substituted aryl or substituted aryloxy, wherein the substituents are selected from lower alkyl, lower alkoxy, halogen and haloalkyl;B is a straight-chained or branched, saturated or unsaturated hydrocarbyl containing up to 5 carbon atoms;N is 1, 2 or 3 andR.sub.1, r.sub.2 and R.sub.3, which may be the same or different, are hydrogen or lower alkyl;And the pharmacologically compatible salts thereof; have been found to be outstandingly effective in depressing serum-lipid and triglycerides in the serum of mammals.
摘要翻译： 式（I）的新型苯氧基烷基羧酸化合物，其中A是芳基，芳氧基，取代的芳基或取代的芳氧基，其中取代基选自低级烷基，低级烷氧基，卤素和卤代烷基; B是含有至多5个碳原子的直链或支链饱和或不饱和烃基; N IS 1，2 OR 3，R 1，R 2和R 3可以相同或不同，为氢或低级烷基; 及其药理学兼容性; 已被认为是非常有效地抑制血清中的血清和血清中的血清脂蛋白。
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