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1. 发明授权

US4167517A Gona-4,9(10)-dienes and process of producing the same 失效
标题翻译： Gona-4,9（10） - 衍生物及其制备方法
公开(公告)号：US4167517A
公开(公告)日：1979-09-11
申请号：US816871
申请日：1977-07-18
申请人： Kurt Ponsold , Michael Hubner , Michael Oettel
发明人： Kurt Ponsold , Michael Hubner , Michael Oettel
IPC分类号： C07J1/00 , C07J41/00
CPC分类号： C07J1/0081 , C07J41/0044 , C07J41/0094
摘要： New gona-4,9(10)-dienes of formula I ##STR1## where R is alkyl of 1 to 3 carbon atoms and X is Cl, Br, F, N.sub.3, SCN, CN, OH, OR'(R'=alkyl), NH.sub.2, a substituted amino group or a heterocyclic compound including nitrogen in the ring. The compounds have valuable biological properties, especially hormonal and antihormonal effects, and can be used to advantage in pharmaceutical preparations for the treatment of endocrinopathies and for reproduction control in human beings and livestock.The invention also embraces a process for making the compounds by converting 3-methyoxy-13.beta.-R-gona-2,5(10)-diene-17.beta.-spiro-1',2'-oxiranes first to 17.beta.-hydroxy-17.alpha.-CH.sub.2 X-13.beta.-R-gon-5(10)-en-3-one, then to the 17.beta.-hydroxy-17.alpha.-CH.sub.2 X-13.beta.-R-gona-4,9(10)-diene-3-ones of formula I.
摘要翻译：其中R是1至3个碳原子的烷基，X是Cl，Br，F，N 3，SCN，CN，OH，OR'（R' =烷基），NH 2，取代的氨基或在环中包含氮的杂环化合物。这些化合物具有宝贵的生物学特性，特别是激素和抗激素作用，可用于治疗内分泌病和用于人和牲畜繁殖控制的药物制剂中。

2. 发明授权

US4029648A Process of making gona-1,3,5(10),9(11)-tetraenes 失效
标题翻译：制备聚1,3,5（10），9（11） - 四烯的方法
公开(公告)号：US4029648A
公开(公告)日：1977-06-14
申请号：US649465
申请日：1976-01-15
申请人： Kurt Ponsold , Helmut Kasch
发明人： Kurt Ponsold , Helmut Kasch
IPC分类号： C07J1/00 , C25B3/02 , C07J17/00
CPC分类号： C07J1/0059 , C25B3/02
摘要： Gona-1,3,5(10),9(11)-tetraenes having the formula ##STR1## IN WHICH FORMULA N IS 1 OR 2,R.sup.1 is a hydrogen, hydroxy, alkoxy, or alkanoyl substituent,R.sup.2 is a hydrogen, alkoxy, acetoxy, alkyl, akenyl, or alkynyl substituent, or a substituent having the formula --CH.sub.2 X in which X is a halogen, pseudohalogen, or O-alkyl substituent, orR.sup.1 or R.sup.2 together are oxygen, or a methyleneoxy or ethylenedioxy substituent,R.sup.3 is a hydroxy, alkoxy, alkanoyl, or alkoxymethyleneoxy substituent, andR.sup.4 is a methyl or ethyl substituent,Are made from gona-1,3,5(10)trienes by electrolysis of a solution thereof in water and/or a primary or secondary alcohol in the presence of an electroconductive compound.The gona-1,3,5(10),9(11)-tetraenes are intermediates for the production of steroidal pharmaceuticals for fertility control in human and animal therapeutics.
摘要翻译：具有下式的Gona-1,3,5（10），9（11） - 四烯，其中N为1或2，R1为氢，羟基，烷氧基或烷酰基取代基，R2为氢，烷氧基，乙酰氧基，烷基，烯基或炔基取代基，或具有式-CH 2 X的取代基，其中X为卤素，假卤素或O-烷基取代基，或者R 1或R 2一起为氧或亚甲氧基或亚乙二氧基取代基， R3是羟基，烷氧基，烷酰基或烷氧基亚甲基氧基取代基，R4是甲基或乙基取代基，通过在水中和/或主要的电解电离从GONA-1,3,5（10）电解质化合物存在下的次要酒精。

3. 发明授权

US4861715A Process for the production of nourseothricine and its adsorbate 失效
标题翻译：过氧化氢和其吸附物的生产过程
公开(公告)号：US4861715A
公开(公告)日：1989-08-29
申请号：US572928
申请日：1984-01-20
申请人： Friedrich Bergter , Harald Bocker , Ernst-Joachim Bormann , Wolfgang Forberg , Heinz Fricke , Udo Grafe , Hans-Helmut Grosse , Ingeborg Heller , Matthias Hilliger , Wolf Junne , Hellmut Linde , Michael Menner , Klaus-Dieter Menzel , Peter-Jurger Muller , Gunter Plonka , Hans D. Pohl , Jorg Schneider , Heinz Thrum
发明人： Friedrich Bergter , Harald Bocker , Ernst-Joachim Bormann , Wolfgang Forberg , Heinz Fricke , Udo Grafe , Hans-Helmut Grosse , Ingeborg Heller , Matthias Hilliger , Wolf Junne , Hellmut Linde , Michael Menner , Klaus-Dieter Menzel , Peter-Jurger Muller , Gunter Plonka , Hans D. Pohl , Jorg Schneider , Heinz Thrum
IPC分类号： A61K35/74 , C12P1/06
CPC分类号： C12P1/06
摘要： A process is disclosed for the fermentative production of the ergotropically effective antibiotic nourseothricin, with which, using different carbohydrate sources and suitable inorganic and organic nitrogen sources as well as different mineral salts, with or without addition of stock substances of the respiratory chain or the intracellular amino acid transport, and through influencing the phosphate substance exchange and avoidance of further limitations with regulated acidity conditions, high concentrations of this antibiotic are cultivated in the culture solution. The recovery of the active substance in the culture solution follows either by chromatographic techniques in the form of salts or through addition of a physiologically compatible adsorbent as mycelium-containing nourseothricin-adsorbate, which preferably can be added to the dosaging of mixed feed agents.
摘要翻译：公开了一种用于发挥生产有效的抗生素药物的方法，使用不同的碳水化合物来源和合适的无机和有机氮源以及不同的矿物盐，伴有或不添加呼吸链或细胞内的物质氨基酸转运，通过影响磷酸盐物质的交换，避免受规定酸度条件的进一步限制，培养液中培养出高浓度的抗生素。培养液中的活性物质的回收率可以通过盐形式的色谱技术或通过添加生理上相容的吸附剂作为含菌丝体的次氯酸盐吸附物，其优选可加入混合饲料的剂量。

4. 发明授权

US4474701A Process for the separation of 4-androsten-3,17-dione and 1,4-androstadien-3,17-dione 失效
标题翻译：分离4-雄甾-3,17-二酮和1,4-雄甾烯-3,17-二酮的方法
公开(公告)号：US4474701A
公开(公告)日：1984-10-02
申请号：US474314
申请日：1983-03-10
申请人： Gerhard Teichmuller , Joachim Rabe , Harry Henkel
发明人： Gerhard Teichmuller , Joachim Rabe , Harry Henkel
IPC分类号： C07J1/00 , C07J41/00
CPC分类号： C07J1/0011 , C07J41/0094
摘要： A process is disclosed for the separation of 4-androsten-3,17-dione/1,4-androstadien-3,17-dione mixtures, which are produced, e.g., upon microbiological sterol-side chain decomposition, through conversion of said mixture into a mixture of 17.beta.-cyano-17.alpha.-hydroxy-4-androsten-3-one/17.beta.-cyano-17.alpha.-hydroxy-1,4-androstadien-3-one, from which the difficultly soluble 17.beta.-cyano-17.alpha.-hydroxy-4-androsten-3-one is separated in crystalline form through filtration, and the 17.beta.-cyano-17.alpha.-hydroxy-1,4-androstadiene remaining in the mother liquor is re-split, directly or after extraction with organic solvent, by treatment in alkaline medium, into 1,4-androstadien-3,17-dione, and isolated as such. The separation of the products follows in high yields, and in sufficient purity for further working-up in the synthesis of androstane and pregnane derivatives, as well as estratrienes.
摘要翻译：公开了用于分离4-雄甾-3,17-二酮/ 1,4-雄甾烯-3,17-二酮混合物的方法，其通过例如微生物甾醇侧链分解产生，通过所述混合物的转化转化为17β-氰基-17α-羟基-4-雄甾-3-酮/17β-氰基-17α-羟基-1,4-雄甾烯-3-酮的混合物，难溶于17β- 通过过滤将氰基-17α-羟基-4-雄甾-3-酮以结晶形式分离，并将残留在母液中的17β-氰基-17α-羟基-1,4-雄甾二烯直接再分裂或者用有机溶剂萃取后，通过在碱性介质中处理，形成1,4-雄甾二烯-3,17-二酮，并将其分离。产物的分离遵循高产率，并且具有足够的纯度用于进一步处理雄甾烷和孕烷衍生物以及雌三烯的合成。

5. 发明授权

US4315909A Process for the preparation of solid drug formulations 失效
标题翻译：制备固体药物制剂的方法
公开(公告)号：US4315909A
公开(公告)日：1982-02-16
申请号：US81449
申请日：1979-10-03
申请人： Reinhard Huttenrauch
发明人： Reinhard Huttenrauch
IPC分类号： A61K9/20 , A61K9/34 , A61K47/38
CPC分类号： A61K47/38 , A61K9/2054
摘要： In order to allow for the greatest possible range of variation in the rate of liberation of active agents within an organism and to allow for the use of a wide variety of active agents in solid drug formulations, cellulose graft copolymers are employed as adjuvant. The excellent flow properties and compacting behavior of these cellulose graft copolymers allow for formulation without the need for additional process steps, while variations in the type and proportion of the grafted components allows for the synthesis of adjuvants ideally suited for a specific intended use.
摘要翻译：为了允许生物体内活性剂释放速率的最大可能变化范围，并且允许在固体药物制剂中使用多种活性剂，使用纤维素接枝共聚物作为佐剂。这些纤维素接枝共聚物的优异的流动性能和压实行为允许配制而不需要额外的工艺步骤，而接枝组分的类型和比例的变化允许合成适合于特定预期用途的佐剂。

6. 发明授权

US4248790A Gona-4,9(10)-dienes and process of producing the same 失效
标题翻译： Gona-4,9（10） - 衍生物及其制备方法
公开(公告)号：US4248790A
公开(公告)日：1981-02-03
申请号：US11951
申请日：1979-02-13
申请人： Kurt Ponsold , Michael Hubner , Michael Oettell
发明人： Kurt Ponsold , Michael Hubner , Michael Oettell
IPC分类号： A61K31/565 , A61P5/00 , C07J1/00 , C07J41/00 , C07C117/00 , C07J17/00
CPC分类号： C07J1/0081 , C07J41/0044 , C07J41/0094
摘要： New gona-4,9(10)-dienes of formula I ##STR1## where R is alkyl of 1 to 3 carbon atoms and X is Cl, Br, F, N.sub.3, SCN, CN, OH, OR'(R'-alkyl), NH.sub.2, a substituted amino group or a heterocyclic compound including nitrogen in the ring. The compounds have valuable biological properties, especially hormonal and antihormonal effects, and can be used to advantage in pharmaceutical preparation, for the treatment of endocrinopathies and for reproduction control in human beings and livestock.The invention also embraces a process for making the compounds by converting 3-methoxy-13.beta.-R-gona-2,5(10)-diene-17.beta.-spiro-1,`2`-oxiranes to 17.beta.-hydroxy-17.alpha.-CH.sub.2 -13.beta.-R-gona-4,9(10)-diene-3-ones to the 17.alpha.-CH.sub.2 X-14.beta.-ols which are hydrolyzed to the 17.beta.-OH which latter are then converted to the compounds of formula I.
摘要翻译：其中R是1至3个碳原子的烷基，X是Cl，Br，F，N 3，SCN，CN，OH，OR'（R' - 烷基），NH 2，取代的氨基或在环中包含氮的杂环化合物。这些化合物具有宝贵的生物学特性，特别是激素和抗激素作用，可用于药物制剂中的优势，用于治疗人类和家畜的内分泌病和繁殖控制。本发明还包括通过将3-甲氧基-13β-R-gona-2,5（10） - 二烯-17β-螺-1“2'-环氧乙烷转化为17β-羟基 - 17α-CH2Bβ-R-Gona-4,9（10） - 二烯-3-酮与17α-CH2-14β-醇反应，其被水解成17β-OH，后者转化为式I的化合物。

7. 发明授权

US4124597A Process for making (DL) pantolactone 失效
标题翻译：制备（DL）泛酸内酯的方法
公开(公告)号：US4124597A
公开(公告)日：1978-11-07
申请号：US667410
申请日：1976-03-16
申请人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
发明人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
IPC分类号： C07D307/33 , C07D307/32
CPC分类号： C07D307/33
摘要： DL pantolactone is made by(a) introducing isobutyraldehyde, formalin and sodium cyanide solution continuously at a predetermined rate into a circulation reactor, continuously circulating the said mixture in said reactor while cooling the circulating mass in a heat exchanger, thus continuously causing the heat generated in the reaction between the components of said mixture to be discharged in said heat exchanger and by continuously re-mixing the formed reaction product with the reaction components;(b) continuously passing part of the reaction product into an after-treatment reactor where the said reaction is completed without re-mixing so as to form formisobutyraldolcyanohydrin;(c) passing the latter product into a first reaction chamber, reacting therein the product with a continuously introduced non-oxidizing strong acid at an elevated temperature and pressure so as to hydrolyze the product, thus forming a solution of .alpha.,.gamma.-dihydroxy-.beta.,.beta.-dimethylbutyric acid;(d) passing the said solution to a second reaction chamber and maintaining the solution therein at said elevated temperature and pressure until the .alpha.,.gamma.-dihydroxy-.beta.,.beta.-dimethylbutyric acid is lactonized to DL-.alpha.-hydroxy-.beta.,.beta.-dimethyl-.gamma.-butyrolactone and finally(e) recovering the latter product from the acid solution.The process permits obtaining DL-pantolactone in a continuous operation at a high yield.
摘要翻译： DL泛酸内酯由（A）将丙三醇，甲醛和氰化钠溶液以预定的速率连续循环到循环反应器中，连续循环在热交换器中冷凝循环质量的同时反应器中的混合物，连续地引起热生成在合格换热器中排放的混合物组分与反应组分连续重新混合形成的反应产物之间的反应中; （B）将反应产物的一部分连续通入反应器，在反应完成后，不再重新混合，从而形成甲基溴乙醇; （C）通过将产品输送到第一反应室，在产品的反应中连续引入非氧化强酸在高温和压力下进行水解，从而形成α，γ-二羟基 - β，β-二甲基丁酸; （D）将固体溶液通入第二反应室并维持其在高温和压力下的溶液，但α，γ-二羟基-β，β-二羟基丁酸被定义为DL-α-羟基-β，β- 二甲基γ-丁内酯，最后（E）从酸溶液中回收乳化剂产品。

8. 发明授权

US4095952A Apparatus for making (DL) pantolactone 失效
标题翻译：制备（DL）泛酸内酯的装置
公开(公告)号：US4095952A
公开(公告)日：1978-06-20
申请号：US733019
申请日：1976-10-15
申请人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
发明人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
IPC分类号： B01J19/24 , C07D307/33 , B01J1/00
CPC分类号： C07D307/33 , B01J19/2435
摘要： An apparatus for making DL-pantolactone in a continuous process comprises the following parts and setup:A circulation heater and a circulation reactor, means for introducing the components into the reactor, a heat-exchanger forming part of the circulation reactor, a longitudinal aftertreatment reactor and a final longitudinal reactor comprising dual reaction chambers with means for applying heat and pressure in the first chamber and maintaining the reaction product in the second chamber at such heat and pressure. The apparatus may also include a chamber for forming a premix of some of the components with a subsequent cooling device prior to the introduction into the circulation reactor. It may furthermore include a stripping column and pulsation column for recovering the final product from the solution.
摘要翻译：在连续过程中制备DL-泛酸内酯的装置包括以下部分和设置：

9. 发明授权

US4532367A Antimicrobially effective derivatives of phenol and methods for their production 失效
标题翻译：苯酚的抗微生物有效衍生物及其生产方法
公开(公告)号：US4532367A
公开(公告)日：1985-07-30
申请号：US412851
申请日：1982-08-30
申请人： Herbert Teubner , Axel Kramer , Wolfgang Weuffen , Eberhard Schrotter , Gerhard Grubel
发明人： Herbert Teubner , Axel Kramer , Wolfgang Weuffen , Eberhard Schrotter , Gerhard Grubel
IPC分类号： A61K31/055 , A61K31/085 , C07C39/367 , C07C39/44 , C07C43/23 , C07C39/14
CPC分类号： C07C39/367 , A61K31/055 , A61K31/085 , C07C39/44 , C07C43/23
摘要： A method is provided for the production of antimicrobially effective phenol derivatives according to general Formula I in which R.sub.1 is bromine or chlorine, R.sub.2 is methyl or ethyl, R.sub.3 is hydrogen or sodium, potassium, ammonium or by alkyl with up to 10 C-atoms substituted ammonium, magnesium, calcium, barium, aluminum, tin, bismuth, copper, zinc, R.sub.4 and R.sub.5 are independently hydrogen, alkyl or alkoxy with up to 5 C-atoms, bromine or chlorine. The compounds are obtained by benzylation of 6-halogen- or 4-halogen-2-alkylphenol, halogenation of 2-alkyl-4-benzylphenol or -6-benzylphenol, or by alkylation of 6-halogen-4-benzylphenol or of 4-halogen-6-benzylphenol and if necessary through reaction of the product with hydroxide, alcoholate, carbonate or hydrogen carbonate of the above-mentioned metals. Water or lipid soluble effective substances are obtained which display a broad antimicrobial activity spectrum.
摘要翻译：提供了一种制备根据通式I的抗微生物酚衍生物的方法，其中R 1是溴或氯，R 2是甲基或乙基，R 3是氢或钠，钾，铵或具有至多10个C原子的烷基取代的铵，镁，钙，钡，铝，锡，铋，铜，锌，R4和R5独立地是氢，具有至多5个C原子的烷基或烷氧基，溴或氯。该化合物通过6-卤素或4-卤代-2-烷基苯酚苄化，2-烷基-4-苄基苯酚或-6-苄基苯酚的卤化，或通过6-卤素-4-苄基苯酚或4- 卤素-6-苄基苯酚，如果需要，通过产物与上述金属的氢氧化物，醇盐，碳酸盐或碳酸氢盐反应。获得显示广泛抗菌活性谱的水或脂溶性有效物质。

10. 发明授权

US4042502A Detoxification of cyanides and cyanide-containing solutions 失效
标题翻译：氰化物和含氰化物溶液的脱毒
公开(公告)号：US4042502A
公开(公告)日：1977-08-16
申请号：US560989
申请日：1975-03-21
申请人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
发明人： Joachim Schmidt , Wolfgang Bamberg , Hartmut Grunert , Erhard Schorm , Christian Weigelt
IPC分类号： A62D3/00 , A62D3/35 , A62D101/45 , C02F1/02 , C02F9/00 , C02C5/02
CPC分类号： A62D3/35 , C02F1/025 , A62D2101/45 , C02F2101/18
摘要： The method comprises preheating a cyanide solution to be detoxified by passing the cyanide solution through a heat exchanger and initiating a detoxifying hydrolysis of the cyanide solution by subjecting the cyanide solution to a temperature shock raising the temperature of the cyanide solution to between about 200.degree. and 250.degree. C and passing the cyanide solution through a tubular reactor at a pressure of between about 40 and 140 atm.
摘要翻译：该方法包括通过将氰化物溶液通过热交换器预热氰化物溶液以进行解毒，并通过使氰化物溶液温度升高使氰化物溶液的温度升高至约200℃和 250℃，并使氰化物溶液通过管式反应器，压力为约40至140atm。

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