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1. 发明授权

US4668786A P-fluorobenzoyl-piperidino alkyl theophylline derivatives 失效
标题翻译：对氟苯甲酰 - 哌啶子基烷基茶碱衍生物
公开(公告)号：US4668786A
公开(公告)日：1987-05-26
申请号：US813439
申请日：1985-12-26
申请人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
发明人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
IPC分类号： A61K31/52 , A61K31/522 , A61P25/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D295/22 , C07D307/02 , C07D473/08
CPC分类号： C07D473/08
摘要： New derivatives of theophylline having the formula ##STR1## wherein R is hydrogen or a hydroxy group, and n is an integer of 0.ltoreq.n.ltoreq.3 and/or the pharmaceutically acceptable, acid addition salts thereof, exhibit in addition to other properties, histamine-serotinine- bradykynine- antagonistic, anti-anaphylactic and .beta.-adrenergic stimulating effects.

2. 发明授权

US4503237A Method for the production of acemetacin 失效
标题翻译：生产acemetacin的方法
公开(公告)号：US4503237A
公开(公告)日：1985-03-05
申请号：US450507
申请日：1982-12-16
申请人： Ren/e/ Gnehm , Rolf Weber
发明人： Ren/e/ Gnehm , Rolf Weber
IPC分类号： C07D209/28 , C07D309/10
CPC分类号： C07D209/28
摘要： 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-3-indole acetic acid as known per se is obtainable by means of a novel and more simple method. This method comprises hydrolizing 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indole acetic acid tetrahydropyranyl ester, which ester is a novel compound. The final product obtained is a valuable drug having antiinflammatory activity.
摘要翻译： 1-（4-氯苯甲酰基）-5-甲氧基-2-甲基-3-吲哚乙酸本身就是通过一种新颖而简单的方法获得的。该方法包括使1-（4-氯苯甲酰基）-5-甲氧基-2-甲基-3-吲哚乙酸四氢吡喃酯水解，该酯是新化合物。获得的最终产品是具有抗炎活性的有价值的药物。

3. 发明授权

US4483999A Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood 失效
标题翻译：具有降低血液中脂肪物质水平的能力的苯氧基链烷酸衍生物
公开(公告)号：US4483999A
公开(公告)日：1984-11-20
申请号：US773148
申请日：1977-03-01
申请人： Kurt Thiele , Quazi Ahmed , Rudolf Adrian , Ulrich Jahn
发明人： Kurt Thiele , Quazi Ahmed , Rudolf Adrian , Ulrich Jahn
IPC分类号： C07C59/68 , C07C59/70 , C07C69/712 , C07D211/46 , C07D473/08 , C07C69/76
CPC分类号： C07C321/00 , C07C59/68 , C07C59/70 , C07D211/46 , C07D473/08
摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.
摘要翻译：式中，R 1为氢，卤素，含有1至4个碳原子的烷基或烷氧基，R2为氢，卤素，羟基或含有1至4个碳原子的烷氧基烷基，n和m的新型化合物整数，使得和（n + m）在3〜10的范围内，n与m不同，x是含有1〜4个碳原子的烷基，氢或作为主体1的金属阳离子的阳离子，元素周期系统的2和3，有机碱性离子或铵离子。这些化合物由于其相当的降低血液中脂肪物质含量的能力而具有药用效用。

4. 发明授权

US4440561A Defoliant composition and method 失效
标题翻译：脱叶成分和方法
公开(公告)号：US4440561A
公开(公告)日：1984-04-03
申请号：US345490
申请日：1982-02-03
申请人： Jacques Meyer , Walter E. Scharen
发明人： Jacques Meyer , Walter E. Scharen
IPC分类号： A01N47/30 , A01N61/02 , A01N37/40
CPC分类号： A01N47/30 , A01N61/02
摘要： Compositions containing Bifenox and Linuron in combination with a mineral oil, such as white oil, show a remarkable synergism of the constituents and are of use as pre-harvest defoliants for crop plants, e.g. for desiccation of potato plants.
摘要翻译：含有Bifenox和Linuron与矿物油（例如白油）组合的组合物显示了组分的显着协同作用，并且用作作物植物的收获前脱叶剂。用于马铃薯植物的干燥。

5. 发明授权

US4223143A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US4223143A
公开(公告)日：1980-09-16
申请号：US968577
申请日：1978-12-11
申请人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler
发明人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler
IPC分类号： C07D231/56 , C07D239/88 , C07D487/04
CPC分类号： C07D487/04 , C07D231/56 , C07D239/88
摘要： Novel quinazoline derivatives of the formula (1) ##STR1## wherein ring C is a pyrazole ring fused to ring B in two vicinal positions thereof that are not fused with ring A. The novel formula (1) compounds or pyrazolo-quinazoline-ones are structurally related to allopurinol, a well known drug useful in the treatment of gout and are expected to replace or complement allopurinol in the therapeutic use thereof. The generic name Benzoallopurinol is suggested for the novel formula (1) compounds; formula (1) includes angular and linear structures of the interfused rings A, B and C.Two methods for producing the novel formula (1) compounds are disclosed. The first method starts from the indazole structure that includes the interfused rings B and C, and ring A is formed on the indazole moiety. The second method starts from the quinazoline structure that includes interfused rings A and B, and the pyrazole ring C is formed on the benzo moiety (ring B) of the quinazoline structure. Either method may lead to angular or linear benzoallopurinols depending upon the substituents introduced into the starting structure for forming the complemental ring thereon.
摘要翻译：新的式（1）化合物或吡唑并喹唑啉衍生物（1）其中环C是与环B的两个相邻位置稠合的环B的吡唑环。 - 酮在结构上与别嘌呤醇有关，别嘌呤醇是用于治疗痛风的众所周知的药物，并且预期在其治疗用途中替代或补充别嘌呤醇。对于新型配方（1）化合物，建议通用名称苯并嘌呤; 公式（1）包括界面环A，B和C的角度和线性结构。公开了制备新式（1）化合物的两种方法。第一种方法是从包含界面环B和C的吲唑结构开始，在吲唑部分上形成环A。第二种方法从包括嵌段环A和B的喹唑啉结构开始，吡唑环C形成在喹唑啉结构的苯并部分（环B）上。根据引入到起始结构中的取代基来形成其上的互补环，任一方法都可能导致角或线性的苯并嘌呤醇。

6. 发明授权

US4210656A Imidazolyl vinyl ethers and process for preparing same 失效
标题翻译：咪唑基乙烯基醚及其制备方法
公开(公告)号：US4210656A
公开(公告)日：1980-07-01
申请号：US970312
申请日：1978-12-18
申请人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
发明人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
IPC分类号： A01N43/50 , A61K31/415 , A61P31/04 , C07D233/60 , C07D233/92 , C07D521/00
CPC分类号： C07D231/12 , A01N43/50 , C07D233/56 , C07D249/08
摘要： .alpha.-Aryl-.beta.-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar represents a substituted or unsubstituted aryl group, R an alkyl, aryl or aralkyl group, X an oxygen atom, a sulfur atom, a sulfinyl or a sulfonyl group and R1 a lower alkyl group or a nitro group. These compounds are effective wide spectrum fungicides and bactericides. To prepare these vinyl ethers, a corresponding 1-arylacylimidazole is o-alkylated in presence of NaH with a corresponding .alpha.-halogen ether, .alpha.-halogen thioether, .alpha.-halogen sulfinyl compound or a corresponding .alpha.-halogen sulfonyl compound.
摘要翻译：公开了α-氨基-β-咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：Ar表示取代或未取代的芳基，R是烷基，芳基或芳烷基 X为氧原子，硫原子，亚磺酰基或磺酰基，R 1为低级烷基或硝基。这些化合物是有效的广谱杀菌剂和杀菌剂。为了制备这些乙烯基醚，相应的1-芳基酰基咪唑在NaH存在下与相应的α-卤代醚，α-卤代硫醚，α-卤代亚磺酰基化合物或相应的α-卤代磺酰化合物进行邻烷基化。

7. 发明授权

US4153803A Cholesterol-lowering phenoxyalkanoic acid esters 失效
公开(公告)号：US4153803A
公开(公告)日：1979-05-08
申请号：US773144
申请日：1977-03-01
申请人： Kurt Thiele , Quazi Ahmed , Rudolf Adrian , Ulrich Jahn
发明人： Kurt Thiele , Quazi Ahmed , Rudolf Adrian , Ulrich Jahn
IPC分类号： A61K31/22 , C07C59/68 , C07C59/70 , C07C69/712 , C07C69/736 , C07D211/46 , C07D213/30 , C07D473/08 , C07C69/76
CPC分类号： C07C321/00 , C07C59/68 , C07C59/70 , C07D211/46 , C07D473/08
摘要： Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.2 contain together not more than 10 carbon atoms,Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, orY is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O.sup.- M.sup.+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A.sup.1 and A.sup.2 being the same and being as aforesaid or being different with one of A.sup.1 and A.sup.2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula,Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms,Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O.sup.- M.sup.+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A.sup.1 and A.sup.2 are different.

8. 发明授权

US4133903A Process for preparing bitter beverages 失效
标题翻译：苦味饮料的制备方法
公开(公告)号：US4133903A
公开(公告)日：1979-01-09
申请号：US747986
申请日：1976-12-06
申请人： Kurt Thiele , Heinz O. Bernhard
发明人： Kurt Thiele , Heinz O. Bernhard
IPC分类号： C12G3/04 , A23L2/00 , A23L2/56 , A23L27/20 , C12G3/06
CPC分类号： A23L2/56 , A23L27/2052 , C12G3/06
摘要： A bitter beverage and process for forming the same, which comprises an aqueous solution containing cynaropicrin as such in a concentration of at least 2.5 mg/liter, the solution having a pH-value of not more than 7.0.
摘要翻译：一种苦味饮料及其形成方法，其含有浓度为至少2.5mg /升的含有赤霉素的水溶液，该溶液的pH值不大于7.0。

9. 发明授权

US3947584A Novel indolyl alkyl amines, method of producing same, and their use as anorectic agents 失效
标题翻译：新型吲哚基烷基胺，其制备方法及其作为厌食剂的用途
公开(公告)号：US3947584A
公开(公告)日：1976-03-30
申请号：US397779
申请日：1973-09-17
申请人： Ludwig Zirngibl , Rudolf Adrian , Ulrich Jahn
发明人： Ludwig Zirngibl , Rudolf Adrian , Ulrich Jahn
IPC分类号： C07D209/14 , C07D209/16 , A61K31/40
CPC分类号： C07D209/16 , Y10S514/91
摘要： Indolyl alkyl amines of the following formula: ##SPC1##And their salts with organic or inorganic acids. In this formula I, A and A.sup.1 denote identical or different alkyl radicals which both together have a total of 3-8 C-atoms. R.sup.1 denotes hydrogen, a lower alkyl radical having up to 4 C-atoms or a possibly substituted benzyl or benzoyl radical. R.sup.2 and R.sup.3 may be the same or different and denote hydrogen, a halogen (more particularly chlorine, bromine or fluorine) or (possibly halogenated) lower alkyl radicals or (possibly etherified) hydroxy radicals. R.sup.4 denotes hydrogen, a lower alkyl radical, an acyl group or a (possibly substituted) benzyl radical or the cyano-ethyl group. The compounds are useful as anoretics (appetite inhibitors) and can be made by various disclosed methods.
摘要翻译：下式的吲哚基烷基胺：

10. 发明授权

US4554356A Method for production of imidazolyl vinyl ethers 失效
标题翻译：咪唑基乙烯基醚的制备方法
公开(公告)号：US4554356A
公开(公告)日：1985-11-19
申请号：US692324
申请日：1985-01-16
申请人： Ludwig Zirngibl , Kurt Thiele
发明人： Ludwig Zirngibl , Kurt Thiele
IPC分类号： C07D233/00 , B01J31/02 , C07B61/00 , C07D233/60 , C07D233/68 , C07D233/70 , C07D233/91 , C07D333/00 , C07D401/00 , C07D409/00 , C07D521/00
CPC分类号： C07D231/12 , C07D249/08
摘要： A process for the manufacture of imidazolylvinyl ethers of the formula ##STR1## wherein Im represents the substituted or unsubstituted 1-H-imidazol-1-yl group and An, R and Y are defined hereinbelow by condensation of a corresponding ketone of the formulaAr--CO--CHR--Im (II)with the splitting-off of a Z group, with a condensable substance of the formulaZ--Y (III)in the aqueous solution of a strong inorganic base, preferably in concentrated aqueous soda lye. The reaction may also be carried out in the presence of a second liquid organic phase, preferably benzene or toluene, especially in the presence of a phase transfer catalyst in this case. Through careful crystallization of the product manufactured according to this method, it is possible to manufacture approximately pure E-isomers of the imidazolylvinyl ether of formula (I), without the requirement of chromatographic separation.
摘要翻译： PCT No.PCT / EP82 / 00010 Sec。 371日期1982年5月24日 102（e）日期1982年5月24日PCT提交1982年1月21日PCT公布。出版物WO82 / 02552 日本1982年8月5日。一种制备式（I）的咪唑基乙烯基醚的方法，其中Im表示取代或未取代的1-H-咪唑-1-基，An，R和Y定义如下通过将式Ar-CO-CHR-Im（II）的相应的酮与Z基团的分离与式ZY（III）的可冷凝物质在强无机碱的水溶液中缩合，优选在浓缩的苏打碱液中。反应也可以在第二液体有机相存在下进行，优选苯或甲苯，特别是在这种情况下在相转移催化剂存在下。通过根据该方法制造的产品的仔细结晶，可以制备式（I）的咪唑基乙烯基醚的近似纯的E-异构体，而不需要色谱分离。

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