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21. 发明授权

US06194565B1 Process for preparing 16 &agr;-methyl-steroids 失效
标题翻译：制备16种α-甲基类固醇的方法
公开(公告)号：US06194565B1
公开(公告)日：2001-02-27
申请号：US08442959
申请日：1995-05-17
申请人： Jean Buendia , Patrick Roussel , Michel Vivat
发明人： Jean Buendia , Patrick Roussel , Michel Vivat
IPC分类号： C07J7100
CPC分类号： C07J71/0015 , C07J5/0076
摘要： Intermediates for the compound of the formula
摘要翻译：化合物的中间体

22. 发明授权

US5399685A Process for the preparation of 20-keto-21 alpha-01-steroids 失效
标题翻译：制备20-keto-21α-01类固醇的方法
公开(公告)号：US5399685A
公开(公告)日：1995-03-21
申请号：US75822
申请日：1993-06-11
申请人： Jean Buendia , Veronique Crocq , Christian Masson , Denis Prat , Michel Vivat
发明人： Jean Buendia , Veronique Crocq , Christian Masson , Denis Prat , Michel Vivat
IPC分类号： C07J9/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J75/00 , C12P33/00 , C12R1/865
CPC分类号： C07J9/00 , C07J21/006 , C07J33/007 , C07J41/0094
摘要： A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, R.sub.3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R.sub.1 has the above definition with a magnesium organic compound reagent of the formulaHalMg--CH.sub.2 --R.sub.2 Awherein Hal is a halogen and R.sub.2 is defined as above to obtain a compound of the formula ##STR3## wherein R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula ##STR4## wherein R.sub.5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula ##STR5## wherein R.sub.1, R.sub.2, R.sub.3 and K are defined as above, subjecting the latter to autoxidation to obtain a compound of the formula ##STR6## wherein R.sub.1, R.sub.2, R.sub.3 and K are defined as above, reacting the latter with an acid to obtain a reconjugated 3-keto compound of the formula ##STR7## wherein R.sub.1, R.sub.2 and R.sub.3 are defined as above and reacting the latter with a regio- and enantioselective reducing agent to obtain a compound of formula I and intermediates formed therein.
摘要翻译：一种制备式I化合物的方法，其中R 1是1至3个碳原子的烷基，R 2是1至12个碳原子的烷基，R 3是1至4个碳原子的烷基，包括使其中R 4是易裂解醚的剩余部分，K是缩酮形式，缩醛缩醛或混合缩酮形式的被保护酮官能团，并且R 1具有上述定义与式HalMg- CH2-R2A其中Hal是卤素，R2如上定义，得到式III的化合物，其中R 1，R 2和K如上定义，使其与酰化剂反应，得到式其中R 5是1至6个碳原子的烷基或6至10个碳原子的芳基，并且R 1，R 2和K如上定义，使其与适当的烷基化剂反应，得到下式的化合物：IMAGE > V其中R1，R2，R3和K如上所定义，对其进行处理进行自氧化以获得式VI的化合物，其中R 1，R 2，R 3和K如上定义，使其与酸反应，得到下式的共轭3-酮化合物，其中R 1， R2和R3如上定义并使其与区域和对映选择性还原剂反应，得到式I化合物及其中形成的中间体。

23. 发明授权

US4927921A Novel 23-keto-steroids 失效
标题翻译：新型23-酮类固醇
公开(公告)号：US4927921A
公开(公告)日：1990-05-22
申请号：US128997
申请日：1987-12-04
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, and 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.
摘要翻译：式I的化合物，其中R 1是氢或甲基，R 2是甲基或乙基，A，B，C和D环任选地含有至少一个双键并且任选被至少一个成员所取代任选保护的-OH，= O，1-4个碳原子的烷基和烷氧基，2至4个碳原子的卤素和烯基和炔基，R选自卤素，-OH，烷硫基和烷氧基， 6个碳原子，7至15个碳原子的芳烷氧基，芳硫基和芳烷硫基，而R 3和R 4分别是氢或1至6个碳原子的烷基或7至15个碳原子的芳烷基或与氮一起形成任选地含有另外的氮或氧原子的杂环，除了其中R是甲氧基的产物，R1和R2各自表示甲基，A环带有3β-乙酰氧基官能团，并且B环在5（6）中含有双键，可用作中间体 20-酮 - 孕烷的制备。

24. 发明授权

US4847014A Novel steroids 失效
标题翻译：新型类固醇
公开(公告)号：US4847014A
公开(公告)日：1989-07-11
申请号：US129658
申请日：1987-12-07
申请人： Michel Vivat , Jean Buendia
发明人： Michel Vivat , Jean Buendia
IPC分类号： C07J7/00 , C07J9/00 , C07J31/00 , C07J41/00
CPC分类号： C07J31/006 , C07J41/0061 , C07J7/002 , C07J9/005
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 have one or more double bonds and are optionally substituted with one or more members of the group consisting of halogen protected hydroxy, 1/8O, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkoxy of 1 to 6 carbon atoms, aralkoxy of 7 to 15 carbon atoms, alkylthio of 1 to 6 carbon atoms, arylthio of 6 to 14 carbon atoms, aralkylthio of 7 to 15 carbon atoms and ##STR2## wherein R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and aralkyl of 7 to 15 carbon atoms or R.sub.3 and R.sub.4 together with the nitrogen atom form another heterocycle optionally containing a nitrogen atom or oxygen atom and their preparation and their use to form 20-keto-pregnanes.
摘要翻译：式Ⅰ化合物，其中R 1是氢或甲基，R 2是甲基或乙基，A，B，C和D环任选地具有一个或多个双键并且任选被一个或多个基团的成员取代由卤素保护的羟基，1/80，烷基和1至4个碳原子的烷氧基和2至4个碳原子的烯基和炔基组成，R选自卤素，-OH，1至6个碳原子的烷氧基具有7至15个碳原子的芳烷氧基，1至6个碳原子的烷硫基，6至14个碳原子的芳硫基，7至15个碳原子的芳烷硫基和其中R 3和R 4分别选自氢， 1至6个碳原子的烷基和7至15个碳原子的芳烷基或R3和R4与氮原子一起形成任选含有氮原子或氧原子的另一个杂环及其制备及其用于形成20-酮 - 孕烷的用途。

25. 发明授权

US4601854A Process for the production of prednisone 17.21-diacylates 失效
标题翻译：生产泼尼松17.21-二酰基化酶的方法
公开(公告)号：US4601854A
公开(公告)日：1986-07-22
申请号：US695485
申请日：1985-01-28
申请人： Jean Buendia , Michel Vivat
发明人： Jean Buendia , Michel Vivat
IPC分类号： C07J5/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J43/00 , C07J21/00
CPC分类号： C07J9/00 , C07J41/005 , C07J43/006 , C07J5/0053 , C07J7/0015 , C07J7/0085
摘要： A novel process for the preparation of prednisone derivatives of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 8 carbon atoms comprising reacting a compound of the formula ##STR2## with a reducing agent to obtain a compound of the formula ##STR3## reacting the latter with a strong base in the presence of copper ions and oxygen to obtain a compound of the formula ##STR4## reacting the latter with hydroxylamine to obtain a compound of the formula ##STR5## in its syn or anti isomeric form or a mixture thereof, reacting the latter with an acylating agent derived from a radical of the formula ##STR6## and with a reducing agent to obtain a compound of the formula ##STR7## in its Z or E isomeric form or a mixture thereof, subjecting the latter to treatment with an epoxidizing agent and then a dehydrating agent to obtain a compound of the formula ##STR8## reacting the latter with a halogenation agent and subjecting the resulting product to hydrolysis to obtain a compound of the formula ##STR9## wherein Hal is a halogen and reacting the latter with a derivative of an acyl of the formula R.sub.1 CO-- to obtain the compound of formula I which are known compounds.
摘要翻译：一种用于制备式I的泼尼松衍生物的新方法，其中R 1是1至4个碳原子的烷基，R 2选自氢和1至8个碳原子的烃，包括使式II的化合物与还原剂反应，得到下式的化合物，其中在后者与强碱在铜离子和氧的存在下反应，得到下式的化合物，其中IV与式羟胺以获得其顺式或反式异构体形式的式VIII化合物或其混合物，使其与衍生自下式基团的酰化剂和还原剂反应，得到化合物其Z或E异构体形式的式（VI）化合物或其混合物，将其用环氧化物处理，然后用脱水剂处理，得到式脱色剂并将所得产物水解，得到式VIII的化合物，其中Hal为卤素并使其与式R 1 CO-的酰基衍生物反应，得到已知的式I化合物化合物。

26. 发明授权

US4221809A .beta.-Lactones of 2-hydroxy-cyclopentanecarboxylic acid 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：US4221809A
公开(公告)日：1980-09-09
申请号：US36877
申请日：1979-05-08
申请人： Jean Buendia , Michel Vivat
发明人： Jean Buendia , Michel Vivat
IPC分类号： C07C62/32 , C07D305/14 , C07D309/12 , A61K31/365
CPC分类号： C07D309/12 , C07C62/32 , C07D305/14
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)m.sub.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)n.sub. 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 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-OR'A，R'A选自氢，四氢吡喃基，1至3个碳原子的烷基，并且R“A是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任选被羟基保护的羟基任选取代的苯基易于水解的基团，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 nA 是2,3,4或5，波浪线表示这些键处于一个或另一个可能的配置，当A是一个简单的波 nd，环戊烷环和氧之间的键位于具有低血压活性的α位和用于制备的新方法和中间体。

27. 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。

28. 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.

29. 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。

30. 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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