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11. 发明授权

US4190671A Chalcone derivatives 失效
标题翻译：查耳酮衍生物
公开(公告)号：US4190671A
公开(公告)日：1980-02-26
申请号：US883252
申请日：1978-03-03
申请人： Anthony E. Vanstone , Graham K. Maile
发明人： Anthony E. Vanstone , Graham K. Maile
IPC分类号： A61K31/12 , A61K31/19 , A61K31/22 , A61K31/235 , A61K31/255 , A61K31/365 , A61P1/04 , C07C45/00 , C07C45/29 , C07C45/67 , C07C45/68 , C07C47/56 , C07C49/835 , C07C49/84 , C07C51/00 , C07C59/125 , C07C59/74 , C07C59/90 , C07C65/32 , C07C65/38 , C07C65/40 , C07C67/00 , C07C69/025 , C07C69/347 , C07C69/76 , C07C69/95 , C07C309/44 , C07C309/72 , C07C317/44 , C07D307/88 , C07C65/22 , C07C65/20
CPC分类号： C07D307/88 , C07C317/44 , C07C45/29 , C07C45/673 , C07C47/56 , C07C59/74 , C07C59/90 , C07C65/38 , C07C65/40 , Y02P20/582 , Y10S514/826 , Y10S514/926 , Y10S514/927
摘要： The present invention provides new chalcone derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydroxyl, carboxylic acid or sulphonic acid group or a carboxyalkoxy or sulphoalkoxy radical, R.sub.2 and R.sub.3, which may be the same or different, are hydrogen or halogen atoms, hydroxyl groups or alkoxy radicals and R.sub.4 is an alkyl, hydroxyalkyl, alkoxy, carboxyalkoxy, sulphoalkoxy or carboxyalkylcarbonyloxyalkyl radical or a carboxylic acid or sulphonic acid group, with the proviso that compounds of general formula (Ia) always contain at least one carboxylic acid or sulphonic acid group; and the non-toxic inorganic and organic salts of those compounds containing at least one carboxylic acid or sulphonic acid group, the compounds of the invention are useful for treating inflammatory and allergic conditions and for treating ulcerous conditions of the gastro-intestinal tract in humans.
摘要翻译：本发明提供了以下通式的新的查耳酮衍生物：其中R 1是羟基，羧酸或磺酸基或羧基烷氧基或磺基烷氧基，R 2和R 3，其可以是氢或卤素原子，羟基或烷氧基，R4是烷基，羟基烷基，烷氧基，羧基烷氧基，磺基烷氧基或羧基烷基羰基氧基烷基或羧酸或磺酸基团，条件是通式（Ia）总是含有至少一个羧酸或磺酸基团; 和含有至少一个羧酸或磺酸基团的那些化合物的无毒无机和有机盐，本发明的化合物可用于治疗炎性和变态反应病症以及治疗人类胃肠道溃疡病症。

12. 发明授权

US4161538A Substituted phenylacetic acid derivatives and process for the preparation thereof 失效
标题翻译：取代苯乙酸衍生物及其制备方法
公开(公告)号：US4161538A
公开(公告)日：1979-07-17
申请号：US885527
申请日：1978-03-10
申请人： Atsusuke Terada , Kazuyuki Wachi , Eiichi Misaka
发明人： Atsusuke Terada , Kazuyuki Wachi , Eiichi Misaka
IPC分类号： C07C279/14 , A61K31/19 , C07C65/20
CPC分类号： C07C279/14 , C07C2101/08
摘要： 4-(2-Oxo- or hydroxyimino-cycloalkan-1-ylmethyl)phenylacetic acid derivative and nontoxic pharmaceutically acceptable salt thereof are useful as an anti-inflammatory agent. The above 2-oxo-compound may be prepared by (a) hydrolyzing and decarboxylating 4-(1-alkoxycarbonyl-2-oxocycloalkan-1-ylmethyl)phenylacetic acid ester derivative or (b) reacting p-halomethylphenylacetic acid ester derivative with an enamine of cycloalkanone and hydrolyzing the resulting product. And further, the above 2-hydroxyimino-compound may be prepared by (c) reacting 4-(2-oxocycloalkan-1-ylmethyl)phenylacetic acid derivative (the product of process (a) or (b)) with hydroxylamine or (d) reacting a dilithium salt of cycloalkanone oxime with p-halomethyl- or p-sulfonyloxymethyl-phenylacetic acid ester derivative and hydrolyzing the resulting product.
摘要翻译： 4-（2-氧代 - 或肟基 - 环烷基-1-基甲基）苯乙酸衍生物及其无毒的药学上可接受的盐可用作抗炎剂。上述2-氧代化合物可以通过（a）水解和脱羧4-（1-烷氧基羰基-2-氧代环烷烃-1-基甲基）苯乙酸酯衍生物或（b）使对卤甲基苯乙酸酯衍生物与烯胺的环烷酮并水解所得产物。此外，上述2-羟基亚氨基化合物可以通过（c）使4-（2-氧代环烷烃-1-基甲基）苯乙酸衍生物（方法（a）或（b）的产物）与羟胺或（d ）使环烷酮肟的二锂盐与对卤甲基 - 或对 - 磺酰氧基甲基 - 苯基乙酸酯衍生物反应并水解所得产物。

13. 发明授权

US4139717A 1,3-Dicarbonyl compounds 失效
标题翻译： 1,3-二羰基化合物
公开(公告)号：US4139717A
公开(公告)日：1979-02-13
申请号：US756739
申请日：1977-01-04
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
IPC分类号： C07C45/45 , C07C49/12 , C07C49/76 , C07C405/00 , C07F1/00 , C07F7/18 , C07C65/20 , C07C69/95
CPC分类号： C07F7/1804 , C07C405/00 , C07F1/00
摘要： 1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific .alpha.,.beta.-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.
摘要翻译：用作药物，农药，香料及其中间体的1,3-二羰基化合物通过在非质子惰性有机溶剂存在下使特定的α，β-不饱和羰基化合物与特定的有机铜锂化合物反应制备，然后使反应产物与有机羧酸卤化物或酸酐反应。特别地，提供了具有重要生理活性的新的2-酰基-3-取代的环戊烷-1-酮和2-酰基-3-取代的环己烷-1-酮。

14. 发明授权

US4097522A Synthesis of m-benzoyl-hydratropic acid 失效
标题翻译：间苯甲酰 - 水合酸的合成
公开(公告)号：US4097522A
公开(公告)日：1978-06-27
申请号：US690832
申请日：1976-05-28
申请人： Leandro Baiocchi
发明人： Leandro Baiocchi
IPC分类号： C07C59/84 , C07C51/00 , C07C51/09 , C07C67/00 , C07D307/83 , C07C65/20
CPC分类号： C07D307/83 , C07C51/09
摘要： A process is provided for the production of m-benzoyl-hydratropic acid which comprises heating the reaction mixture obtained from the condensation of 2-benzoyl-cyclohexanone and pyruvic acid, its esters or salts, at a temperature of 200.degree. to 230.degree. and in the presence of an acid catalyst.
摘要翻译：提供间苯甲酰基 - 水合酸的制备方法，该方法包括将从2-苯甲酰基 - 环己酮和丙酮酸，其酯或盐的缩合得到的反应混合物在200°至230℃的温度和酸催化剂的存在。

15. 发明授权

US3953500A Benzalicyclic carboxylic acid derivative 失效
标题翻译：苯环二羧酸衍生物
公开(公告)号：US3953500A
公开(公告)日：1976-04-27
申请号：US496855
申请日：1974-08-12
申请人： Shunsaku Noguchi , Tetsuya Aono , Yoshiaki Araki , Kiyohisa Kawai
发明人： Shunsaku Noguchi , Tetsuya Aono , Yoshiaki Araki , Kiyohisa Kawai
IPC分类号： C07C45/28 , C07C45/46 , C07C45/66 , C07C49/67 , C07C49/697 , C07C49/755 , C07C49/792 , C07C49/813 , C07C65/20
CPC分类号： C07C49/813 , C07C45/28 , C07C45/46 , C07C45/66 , C07C49/67 , C07C49/697 , C07C49/755 , C07C49/792
摘要： Compounds of the formula: ##SPC1##Wherein R.sup.1 is an aryl group which may be substituted, R.sup.2 is hydrogen or a lower alkyl group having 1 to 4 carbon atoms and n is 1 or 2, or derivatives at the carboxyl function thereof, are useful as medicines such as antipyretics, analgesics and anti-inflammatory agents.
摘要翻译：下式的化合物：

16. 发明授权

US3824278A 1,6-disubstituted pyrocatechol derivatives 失效
标题翻译： 1,6-取代的吡咯烷醇衍生物
公开(公告)号：US3824278A
公开(公告)日：1974-07-16
申请号：US23749772
申请日：1972-03-23
申请人： SANDOZ AG
发明人： GALANTAY E
IPC分类号： C07C45/29 , C07C45/62 , C07C45/72 , C07C47/277 , C07C49/255 , C07F7/18 , C07C65/02 , C07C65/20
CPC分类号： C07F7/1852 , C07C45/29 , C07C45/62 , C07C45/72 , C07C47/277 , C07C49/255 , Y10S514/826 , Y10S514/958 , Y10S514/96
摘要： DISCLOSED ARE COMPOUNDS OF THE FORMULA

1,2-DI(RO-),4-(R0-(X)-(Z)-),5-(Q-(CH2)N-)-BENZENE

WHEREIN Z IS -CH2-CH2- OR -CH=CH-; X IS -CO- OR -COHR''-; R'' IS HYDROGEN OR LOWER ALKYL; Q IS -CH2OH, -COR'''' OR -CHO; R* IS ALKYL OF 4 TO 6 CARBON ATOMS; N IS 4, 5 OR 6; R IS HYDROGEN OR LOWER ALKYL; R'''' IS HYDROGEN OR A CATION FORMING A PHARMACEUTICALLLY ACCEPTABLE SALT; E,G., 1- 3'',4''-DIMETHOXY-6''-(5''''-CARBOXYPENTYL) PHENYL!-1-OCTAN-3-OL SODIUM SALT: SAID COMPONDS EXHIBITING PHARMACOLOGICAL ACTIVITY IN ANIMALS AND USEFUL, FOR EXAMPLE, AS BRONCHODILATOR AGENTS. THE COMPOUND IN WHICH X IS -CHOH- WITH Z BEING

-CH2-CH2-

AND Q BEING -COOR'' OR -CH2OH MAY BE PREPARED, FOR EXAMPLE, BY REDUCTION OF A CORRESPONDING COMPOUND IN WHICH X IS -CO-. SAID COMPOUNDS IN WHICH X IS -CO- MAY BE PRODUCED BY CATALYTIC HYDROGENATION OF A CORRESPONDING COMPOUND IN WHICH Z IS -CH=CHAND THE LATTER COMPOUNDS IN WHICH Q IS COOR'''' MAY BE PRODUCED BY COMPLETE TERMINAL OXIDATION OF A CORRESPONDING KEY COMPOUND IN WHICH Q IS -CH2OH, E.G. 1- 3'',4''DIMETHOXY-6''-(6''''-HYDROXYHEXYL) PHENYL 1 - 1 OCTEN - 3ONE. THE COMPOUNDS IN WHICH X IS -COH-ALKYL-MAY BE PRODUCED FRM COMPOUNDS IN WHICH X IS -CO-AND Z IS -CH2-CH2- BY GRIGNARD PROCEDURES AND THE FORMER IN WHICH Q IS -CH2OH ARE USED WHEN FORMING COMPOUNDS IN WHICH Q IS -CHO BY CONTROLLED TERMINAL OXIDATION AND THE LATTER MAY BE USED TO PREPARE COMPOUNDS IN WHICH Q IS -COOR'''' BY COMPLETE TERMINAL OXIDATION. THE KEY COMPOUNDS MAY BE PREPARED BY REACTING A TRIMETHYLCHLOROSILANE PROTECTED 3,4-DISUBSTITUTED6-(W-HYDROXYALKYL) - BENZALDEHYDE WITH A DIALKYL-2-OXOALKYL PHOSPHORANE IN THE PRESENCE OF A BASE.

17. 发明授权

US3671579A Process for oxidizing a 1,1-bis(alkylphenyl) alkane 失效
标题翻译：氧化1,1-BIS（烷基苯基）烷烃的方法
公开(公告)号：US3671579A
公开(公告)日：1972-06-20
申请号：US3671579D
申请日：1970-03-04
申请人： GULF RESEARCH DEVELOPMENT CO
发明人： JOYCE THOMAS P JR , LAGALLY RALPH W , SCHULZ JOHANN G D
IPC分类号： C07C51/275 , C07C65/20
CPC分类号： C07C51/275 , C07C65/34
摘要： A process for converting a 1,1-bis(alkylphenyl)alkane to the corresponding benzophenone polycarboxylic acid which involves passing the 1,1-bis(alkylphenyl)alkane and aqueous nitric acid downwardly through a reactor maintained under oxidation conditions.
摘要翻译：将1,1-双（烷基苯基）烷烃转化为相应的二苯甲酮多元羧酸的方法，其涉及使1,1-双（烷基苯基）烷烃和硝酸水溶液向下通过保持在氧化条件下的反应器。

18. 发明授权

US3671570A Derivatives of 9-oxo-15-hydroxyprostanoic acid, homologs thereof and their preparation 失效
标题翻译： 9-OXO-15-羟基磷酸的衍生物，其同系物及其制备
公开(公告)号：US3671570A
公开(公告)日：1972-06-20
申请号：US3671570D
申请日：1970-07-30
申请人： AYERST MCKENNA & HARRISON
发明人： BAGLI JEHAN F , BOGRI TIBOR
IPC分类号： C07C405/00 , C07D309/12 , C07C61/36 , C07C65/20
CPC分类号： C07C405/00 , C07D309/12 , Y10S514/822 , Y10S514/826 , Y10S514/927
摘要： There are disclosed herein derivatives of 9-oxo-15-hydroxy prostanoic acid, lower alkyl esters thereof, and homologs thereof, as well as a process for preparing the above acids, lower alkyl esters thereof, and homologs thereof. The compounds possess hypotensive, antihypertensive, bronchospasmolytic and gastric acid secretion inhibiting properties, as well as inhibiting the aggregation of platelets and promoting the disaggregation of aggregated platelets. Methods for their use are also disclosed.
摘要翻译：本文公开了9-氧代-15-羟基前列腺烷酸的低级烷基酯及其同系物的衍生物，以及制备上述酸的方法，其低级烷基酯及其同系物。该化合物具有降血压，抗高血压，支气管痉挛和胃酸分泌抑制性质，以及抑制血小板聚集和促进聚集血小板的分解。还公开了它们的使用方法。

19. 发明授权

US3641136A Process for oxidizing a 1 1-bis(alkylphenyl) alkane 失效
公开(公告)号：US3641136A
公开(公告)日：1972-02-08
申请号：US3641136D
申请日：1970-05-08
申请人： GULF RESEARCH DEVELOPMENT CO
发明人： ONOPCHENKO ANATOLI , SCHULZ JOHANN G D , SEEKIRCHER RICHARD
IPC分类号： C07C51/265 , C07C63/02 , C07C65/20
CPC分类号： C07C51/265 , C07C63/331
摘要： A PROCESS OF OXIDIZING A 1,1-BIS(ALKYLPHENYL)ALKANE TO CONVERT ALKYL SUBSTITUENTS TO CARBOXYLIC ACID SUBSTIUENTS WHICH INVOLVES CONTACTING THE 1,1-BIS(ALKYLPHENYL)ALKANE WITH OXYGEN IN A LOWER CARBOXYLIC ACID CONTAINING COBALT AND A METHYLENIC KETONE.

20. 发明授权

US3641135A Process for oxidizing a 1 1-bis(alkylphenyl) alkane 失效
标题翻译：氧化1,1-二（烷基苯基）烷烃的方法
公开(公告)号：US3641135A
公开(公告)日：1972-02-08
申请号：US3641135D
申请日：1970-05-08
申请人： GULF RESEARCH DEVELOPMENT CO
发明人： ONOPCHENKO ANATOLI , SCHULZ JOHANN G D , SEEKIRCHER RICHARD
IPC分类号： C07C51/265 , C07C63/02 , C07C65/20
CPC分类号： C07C51/265 , C07C63/331
摘要： A PROCESS FOR OXIDIZING A 1,1-BIS(ALKYLPHENYL)ALKANE, WHEREIN THE ALKANE BRIDGE HAS AT LEAST TWO CARBON ATOMS, TO CONVERT ALKYL SUBSTITUENTS TO CARBOXYLIC ACID SUBSTITUENTS WHICH INVOLVES CONTACTING THE 1,1-BIS-(ALKYPHENYL) ALKANE WITH OXYGEN IN A LOWER CARBOXYLIC ACID CONTAINING COBALT AND AN ALIPHATIC HYDROCARBON HAVING FROM THREE TO SIX CARBON ATOMS.

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