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21. 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。

22. 发明授权

US4072755A Novel cyclopentanoic acid derivatives 失效
标题翻译：新型环戊酸衍生物
公开(公告)号：US4072755A
公开(公告)日：1978-02-07
申请号：US717049
申请日：1976-08-24
申请人： Jean Buendia , Michel Vivat , Jeanine Schalbar
发明人： Jean Buendia , Michel Vivat , Jeanine Schalbar
IPC分类号： A61K31/045 , A61K31/19 , A61P43/00 , C07C35/06 , C07C67/00 , C07C401/00 , C07C405/00 , A01N9/24 , C09F5/00
CPC分类号： C07C35/06 , Y10S514/906
摘要： Novel cyclopentanoic acid derivatives of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and --CH.sub.2 OH, R' is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and a non toxic, pharmaceutically acceptable cation and R.sub.1 is selected from the group consisting of hydrogen, 2-tetrahydropyranyl, branched or straight chain, saturated or unsaturated alkyl of 1 to 4 carbon atoms and ##STR3## and R.sub.2 is selected from the group consisting of straight or branched chain alkyl of 1 to 12 carbon atoms and phenyl with the alkyl and phenyl being optionally substituted with --COOA wherein A is selected from the group consisting of hydrogen, alkali metal, ammonium ion, ion of an organic amine, alkyl and haloalkyl of 1 to 7 alkyl carbon atoms with the proviso that R.sub.1 is not hydrogen or 2-tetrahydropyranyl when R is a carboxylic group, and the OH and R groups on the ring and OR.sub.1 group on the chain may be in either of the two possible positions about the carbon atom to which they are attached having analgesic, anti-inflammatory and smooth muscle relaxant activity.
摘要翻译：新的式（I）的环戊酸衍生物其中R选自由下列组成的组：IMA和CH 2 OH，R'选自氢，1至4个碳原子的烷基和无毒的，药学上可接受的阳离子，R 1选自氢，2-四氢吡喃基，支链或直链，饱和或不饱和的1至4个碳原子的烷基，且R 2选自直链或支链具有1至12个碳原子的烷基和苯基，其中烷基和苯基任选被-COOA取代，其中A选自氢，碱金属，铵离子，有机胺的离子，1至7的烷基和卤代烷基烷基碳原子，条件是当R是羧基时，R 1不是氢或2-四氢吡喃基，环上的OH和R基团和链上的OR1基团可以在关于它们所连接的碳原子具有镇痛，抗炎和平滑肌松弛剂活性。

23. 发明授权

US3984442A Process for the preparation of trans-epoxy cis-alkenes 失效
标题翻译：反式环氧顺式烯烃的制备方法
公开(公告)号：US3984442A
公开(公告)日：1976-10-05
申请号：US605159
申请日：1975-08-15
申请人： Jean Buendia , Michel Vivat
发明人： Jean Buendia , Michel Vivat
IPC分类号： C07D303/32 , B01J21/00 , B01J27/00 , B01J31/00 , C07B61/00 , C07D301/26 , C07D303/40 , C07D303/42 , C07D303/14
CPC分类号： C07D303/42
摘要： A novel process for the preparation of substituted trans-epoxy cis-alkenes of the formula ##EQU1## wherein Alk is straight or branched alkyl of 1 to 6 carbon atoms and m is 3,4 or 5 which are intermediates for prostaglandin compounds.
摘要翻译：一种用于制备式OO的取代的反式环氧顺式 - 烯烃的新方法PARALELL PARALLEL CH 3 - （CH 2）m -CH-CH-CH = CH-CH 2 -CH 2 -C-CH 2 COCO 2，其中Alk是 1至6个碳原子的直链或支链烷基，m是3,4或5，它们是前列腺素化合物的中间体。

24. 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

25. 发明授权

US5756722A Intermediates for the preparation of .DELTA..sup.4,9(11),17(20) -pregnatriene-3-ones 失效
标题翻译：制备DELTA 4,9（11），17（20） - 三烯-3-酮的中间体
公开(公告)号：US5756722A
公开(公告)日：1998-05-26
申请号：US708931
申请日：1996-09-06
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： The novel intermediates of the formula ##STR1## wherein L, K and M are as defined in the specification which are useful intermediates for the preparation of .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.
摘要翻译：式（Ⅰ）的新型中间体，其中L，K和M如本说明书中所定义，它们是制备DELTA 4,9（11），16-孕三烯-3-酮的有用中间体。

26. 发明授权

US5556962A 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：US5556962A
公开(公告)日：1996-09-17
申请号：US538027
申请日：1995-10-02
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 is a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3 and L is a 11.beta.-hydroxy, the dotted line in the 11-position is not a bond and X is chlorine, bromine or iodine which avoids an 11-hydroxylation step in the preparation of hydrocortisone.
摘要翻译：式中的化合物其中K为式IMA的保护基，其中n为2或3，L为11β-羟基，11位的虚线不是键，X是氯，溴或碘，其避免了在制备氢化可的松中的11-羟基化步骤。

27. 发明授权

US5502223A Process for preparation of .DELTA..sup.4,9(11),16 pregnatriene-3,20-diones 失效
标题翻译：制备DELTA 4,9（11），16孕三烯-3,20-二酮的方法
公开(公告)号：US5502223A
公开(公告)日：1996-03-26
申请号：US343050
申请日：1995-02-21
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 preparation of a compound of the formula ##STR1## wherein R.sub.1 is acyl of an organic carboxylic acid of 1 to 8 carbon atoms useful as intermediates for synthesis of therapeutically active steroids.
摘要翻译：一种制备下式化合物的方法，其中R 1是可用作合成治疗活性类固醇的中间体的1至8个碳原子的有机羧酸的酰基。

28. 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。

29. 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。

30. 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。

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