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31. 发明授权

US5892028A 17, 20-epoxy steroids 失效
标题翻译： 17，20-环氧类固醇
公开(公告)号：US5892028A
公开(公告)日：1999-04-06
申请号：US946970
申请日：1997-10-08
申请人： Jean Buendia , Remi Chauvin , Michel Vivat
发明人： Jean Buendia , Remi Chauvin , Michel Vivat
IPC分类号： A61K31/58 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J75/00
CPC分类号： C07J21/006 , C07J21/00 , C07J41/0061 , C07J41/0094 , C07J5/0053 , Y02P20/55
摘要： A compound of the formula ##STR1## wherein R is .dbd.O or ##STR2## and the rings A and B are selected from the group consisting of ##STR3## K is oxo or a protector group of oxo of the formula ##STR4## n is 2 or 3 and R.sub.1 is an ether or ester remainder, K' is oxo or a protector oxime, hydrazone or semicarbazone group and the wavy lines symbolize an isomer mixture, a process for their preparation and their use as intermediates.
摘要翻译：式（Ⅰ）化合物其中R为= O或，环A和B选自和，K为氧代或保护基式中的酮基为2或3，R 1为醚或酯残基，K'为氧代或保护基肟，腙或缩氨基脲基，波浪线表示异构体混合物，其制备方法并将其用作中间体。

32. 发明授权

US5502182A Process for the preparation of hydrocortisone 失效
标题翻译：制备氢化可的松的方法
公开(公告)号：US5502182A
公开(公告)日：1996-03-26
申请号：US362120
申请日：1994-12-22
申请人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
发明人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
IPC分类号： C07J5/00 , C07J13/00 , C07J21/00 , C07J33/00
CPC分类号： C07J21/00 , C07J13/007 , C07J33/007 , C07J5/0053 , Y02P20/55
摘要： A compound of the formula ##STR1## wherein K represents a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3, and M is chlorine, bromine, or ##STR3## wherein R.sub.a and R.sub.b are individually selected from the group consisting of hydrogen, --OH, and alkyl and alkoxy of 1 to 4 carbon atoms and R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms, trialkyl silyl triphenyl silyl and diphenyl alkyl silyl.
摘要翻译：其中K代表下式的氧代保护基，其中n是2或3，M是氯，溴或者其中R a和R b分别选自由氢，-OH和1-4个碳原子的烷基和烷氧基组成的组，R选自1至6个碳原子的烷基，7至15个碳原子的芳烷基，三烷基甲硅烷基三苯基甲硅烷基和二苯基烷基甲硅烷基。

33. 发明授权

US5391732A Process for the preparation of biphenyl-imidazole derivatives 失效
标题翻译：联苯咪唑衍生物的制备方法
公开(公告)号：US5391732A
公开(公告)日：1995-02-21
申请号：US177158
申请日：1994-01-04
申请人： Neerja Bhatnagar , Jean Buendia , Christine Griffoul
发明人： Neerja Bhatnagar , Jean Buendia , Christine Griffoul
IPC分类号： C07C311/16 , A61K31/00 , C07C311/19 , C07C317/14 , C07D233/66 , C07D233/84 , C07D233/90 , C07D233/92 , C07D403/10 , C07F5/02 , C07F9/6506 , C07D403/04 , C07D211/08 , C07D233/58 , C07F9/28
CPC分类号： C07D233/92 , C07D403/10
摘要： A novel process for the preparation of a compound of the formula ##STR1##
摘要翻译：一种制备式（Ⅰ）化合物的新方法

34. 发明授权

US5294704A 4,9(11),17(20)-pregnatriene-3-ones 失效
标题翻译： 4,9（11），17（20） - 三孕烯-3-酮
公开(公告)号：US5294704A
公开(公告)日：1994-03-15
申请号：US971189
申请日：1992-11-04
申请人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
发明人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
IPC分类号： C07J7/00 , C07J13/00 , C07J21/00 , C07J33/00 , C07J75/00
CPC分类号： C07J13/005 , C07J13/007 , C07J21/006 , C07J33/007 , Y02P20/55 , Y02P20/582
摘要： A process for the production of a compound of the formula ##STR1## wherein R is an acyl group of 1 to 8 carbon atoms. The compound is formed through an intermediate compound of the formula ##STR2## wherein R.sub.1 is selected from the group consisting of methyl, phenyl, tolyl, and xylyl and wherein K is a protective group selected from the group consisting of ##STR3## in which n is 2 or 3 and the wavy line means that the group SO.sub.2 --R.sub.1 may have either isomeric form or are mixtures thereof.
摘要翻译：制备式“化合物”的化合物的方法，其中R是1至8个碳原子的酰基。该化合物通过下式的中间体化合物形成：其中R 1选自甲基，苯基，甲苯基和二甲苯基，其中K是保护基团，其选自下组，其中n 是2或3，波浪线表示SO2-R1基团可以具有异构形式或其混合物。

35. 发明授权

US5260463A Process for the preparation of hydrocortisone 失效
标题翻译：制备氢化可的松的方法
公开(公告)号：US5260463A
公开(公告)日：1993-11-09
申请号：US935535
申请日：1992-08-25
申请人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
发明人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
IPC分类号： C07J5/00 , C07J13/00 , C07J21/00 , C07J33/00
CPC分类号： C07J21/00 , C07J13/007 , C07J33/007 , C07J5/0053 , Y02P20/55
摘要： An improved process for the preparation of hydrocortisone and novel intermediates which avoids an 11-hydroxylation step and results in improved yields.
摘要翻译：一种用于制备氢化可的松和新型中间体的改进方法，其避免了11-羟基化步骤并导致提高的产率。

36. 发明授权

US5187273A .DELTA..sup.4,9(11),17(20) -pregnatriene-3-ones 失效
标题翻译：（DELTA）4,9（11），17（20）-PREGNATRIENE-3-ONES
公开(公告)号：US5187273A
公开(公告)日：1993-02-16
申请号：US885150
申请日：1992-05-18
申请人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
发明人： Francis Brion , Jean Buendia , Christian Diolez , Michel Vivat
IPC分类号： C07J7/00 , C07J13/00 , C07J21/00 , C07J33/00 , C07J75/00
CPC分类号： C07J13/005 , C07J13/007 , C07J21/006 , C07J33/007 , Y02P20/55 , Y02P20/582
摘要： A compound of the formula ##STR1## wherein Hal is chlorine or bromine, R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms and a silylated group, K is a protective group selected from the group consisting of ##STR2## n is 2 or 3 and the wavy lines mean the groups may have either isomer form or are mixtures thereof which are intermediates for .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.
摘要翻译：式Ⅰ化合物其中Hal为氯或溴，R选自1至6个碳原子的烷基，7至15个碳原子的芳烷基和甲硅烷基基团，K为选自的保护基团由 n组成的组为2或3，波浪线表示基团可以具有异构体形式或其是DELTA 4,9（11），16-孕三烯-3-酮的中间体的混合物。

37. 发明授权

US5095130A Novel 23-keto-steroids 失效
标题翻译：新的23-KETO-STEROIDS
公开(公告)号：US5095130A
公开(公告)日：1992-03-10
申请号：US488674
申请日：1990-03-05
申请人： Michel Vivat , Jean Buendia
发明人： Michel Vivat , Jean Buendia
IPC分类号： C07J9/00 , C07J31/00 , C07J41/00 , C07J43/00
CPC分类号： C07J9/005 , C07J31/006 , C07J43/003
摘要： A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, the A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.

38. 发明授权

US4879392A Process for making perhydroindole-2-carbonxylic acid 失效
标题翻译：制备全氢吲哚-2-甲酸的方法
公开(公告)号：US4879392A
公开(公告)日：1989-11-07
申请号：US111982
申请日：1987-10-21
申请人： Francis Brion , Jean Buendia , Christian Marie
发明人： Francis Brion , Jean Buendia , Christian Marie
IPC分类号： C07C61/09 , C07C69/75 , C07C233/12 , C07D209/18 , C07D209/42 , C12P7/62
CPC分类号： C07C255/00 , C07C61/09 , C07D209/42
摘要： A process for the asymmetric preparation of a compound of the formula ##STR1## wherein the hydrogen at 3a and 7a are of cis or trans configuration and their non-toxic, pharmaceutically acceptable acid addition salts comprising submitting a compound of the formula ##STR2## to a Hoffman reaction and reacting the resulting product with formaldehyde in the presence of cyanide ions and acid halide of benzoic acid or an aliphatic carboxylic acid of 1 to 5 carbon atoms to obtain a compound of the formula ##STR3## wherein R is acyl of benzoic acid or aliphatic carboxylic acid of 1 to 5 carbon atoms, cyclizing the latter to form a compound of the formula ##STR4## selectively hydrolyzing the latter with a dilute aqueous mineral acid to obtain a compound of the formula ##STR5## subjecting the latter to hydrolysis with a concentrated aqueous mineral acid to form the acid addition salt of a compound of claim 1 and optionally forming the free base.
摘要翻译：用于不对称制备式Ia化合物的方法，其中3a和7a上的氢是顺式或反式构型及其无毒的药学上可接受的酸加成盐，包括将下式化合物 II化合物进行霍夫曼反应，并在氰化物离子和苯甲酸或1至5个碳原子的脂族羧酸的酰卤存在下，使所得产物与甲醛反应，得到式III化合物，其中R是酰基的苯甲酸或1至5个碳原子的脂族羧酸，使后者环化以形成式IV的化合物，用稀的无机酸水溶液选择性地水解后者，得到下式的化合物：使后者用浓缩的无机酸水溶液水解，形成权利要求1的化合物的酸加成盐，并任选地形成游离碱。

39. 发明授权

US4279919A Novel lactones of cyclopentanols 失效
标题翻译：环戊醇的新型内酯
公开(公告)号：US4279919A
公开(公告)日：1981-07-21
申请号：US131053
申请日：1980-03-17
申请人： Jean Buendia , Michel Vivat
发明人： Jean Buendia , Michel Vivat
IPC分类号： C07C62/32 , C07D213/82 , C07D305/14 , C07D309/12 , C07D311/94 , A61K31/365
CPC分类号： C07D213/82 , C07C62/32 , C07D305/14 , C07D309/12 , C07D311/94
摘要： Novel lactones of the formula ##STR1## wherein the dotted line indicates the optional presence of a second bond, A is a single bond or --CH.sub.2 --CH.sub.2 --, R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.6 is --OR.sub.A ', R.sub.A ' is selected from the group consisting of hydrogen, tetrahydropyranyl, alkyl of 1 to 3 carbon atoms and ##STR2## R.sub.A " is selected from the group consisting of alkyl of 1 to 3 carbon atoms optionally substituted with carboxyl and phenyl optionally substituted with a member of the group consisting of carboxyl, free hydroxyl, hydroxyl protected with an acyl of 2 to 4 carbon atoms and hydroxyl protected with an easily hydrolyzable group and R and R.sub.6 together form a keto group, R.sub.7 is --CH.sub.2).sub.m.sbsb.A --CH.sub.3, m.sub.A is 3,4,5 or 6 and R.sub.6 and R.sub.7 taken together form .dbd.CH--(CH.sub.2).sub.n.sbsb.A --CH.sub.3, n.sub.A is 2,3,4 or 5 and the wavy lines indicate that the bonds are in one or the other of the possible configurations and when A is a simple bond, the bond between the cyclopentane ring and the oxygen is in the .alpha.-position having hypotensive activity and the wavy lines represent a paired configuration selected from the group consisting of .alpha.,.beta. and .beta.,.alpha. and mixtures thereof and novel processes and intermediates for their preparation.
摘要翻译：具有式“IMAGE”I的新型内酯，其中虚线表示任选存在第二键，A是单键或-CH 2 -CH 2 - ，R选自氢，1至4的烷基碳原子和2至4个碳原子的烯基和炔基，R6是-ORA'，RA'选自氢，四氢吡喃基，1至3个碳原子的烷基，并且“IMA”> RA“选自由任选被羧基取代的1至3个碳原子的烷基和任选被羧基，游离羟基，被2至4个碳原子的酰基保护的羟基和可容易水解的基团保护的羟基任选取代的基团并且R和R6一起形成酮基，R7是-CH2）mA-CH3，mA是3,4,5或6，R6和R7一起形成= CH-（CH 2）n -A-CH 3，n A是2,3 ，4或5，并且波浪线表示键处于一个或另一个可能的配置中，并且当A是简单的键时环戊烷环和氧之间的键位于具有低血压活性的α位，波浪线表示选自α，β和β，α及其混合物的配对构型，以及它们的新方法和中间体制备。

40. 发明授权

US4264623A .beta.-Lactones of 2-hydroxy-cyclopentane-carboxylic acids 失效
标题翻译： β-内酯2-羟基 - 环戊烷 - 羧酸的内酯
公开(公告)号：US4264623A
公开(公告)日：1981-04-28
申请号：US94771
申请日：1979-11-16
申请人： Jean Buendia , Michel Vivat , Laurent Taliani
发明人： Jean Buendia , Michel Vivat , Laurent Taliani
IPC分类号： A61K31/337 , A61K31/34 , A61K31/365 , A61K31/38 , A61P9/12 , C07D305/14 , C07D309/12 , C07D333/32 , C07D409/06 , C07D409/12 , C09B23/16 , C09B23/08
CPC分类号： C07D333/32 , C07D305/14 , C07D309/12
摘要： Novel .beta.-lactones of 2-hydroxy-cyclopentane-carboxylic acids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --O--CH.sub.2 --CH.sub.3 and --X--Ar, X is selected from the group consisting of --O-- and --CH.sub.2 --, Ar is an optionally substituted member selected from the group consisting of thienyl, thiazolyl, phenyl and thiadiazolyl, the optional substituents being at least one member selected from the group consisting of halogen and --CF.sub.3 and thw wavy lines indicate that the groups may be in the .alpha., .beta. or .beta., .alpha.-positions or mixtures thereof having hypotensive activity and their preparation.
摘要翻译：式（I）的2-羟基 - 环戊烷 - 羧酸的新型β-内酯，其中R 1选自氢和甲基，R 2选自-CH 2 -O-CH 2 -CH 3和 -X-Ar，X选自-O-和-CH 2 - ，Ar是选自噻吩基，噻唑基，苯基和噻二唑基的任选取代的成员，任选的取代基是至少一个选自由卤素和-CF 3和波浪线组成的组表示这些基团可以是具有降血压活性的α，β或β，α-位或其混合物及其制备。

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