公开(公告)号：US4701449A

公开(公告)日：1987-10-20

申请号：US768867

申请日：1985-08-23

申请人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

发明人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

IPC分类号： A61K31/58 ,  A61P9/04 ,  A61P9/10 ,  C07J1/00 ,  C07J5/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J53/00 ,  A61K31/585 ,  A61K31/56

CPC分类号： C07J1/0011 ,  C07J1/0022 ,  C07J1/0033 ,  C07J1/0037 ,  C07J1/0044 ,  C07J21/00 ,  C07J21/003 ,  C07J21/006 ,  C07J31/003 ,  C07J31/006 ,  C07J33/005 ,  C07J41/0038 ,  C07J41/0094 ,  C07J43/006 ,  C07J51/00 ,  C07J53/007

摘要： Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.2 --CH.sub.2 OH, M is hydrogen, alkali metal or --NH.sub.4 or X and Y together form a member of the group consisting of ##STR2## or X is --OH and Y is ##STR3## R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, Alk is alkyl of 1 to 8 carbon atoms, the dotted lines in the 1(2) and 6(7) indicate the optional presence of a second carbon-carbon bond with the proviso that when R.sub.6 and R.sub.7 form cyclopropyl, there is no 6(7) second bond, the dotted line in 10-substituent indicates the optional presence of a third carbon-carbon bond, the wavy lines at R.sub.6 and R.sub.7 indicate the possible .alpha.- or .beta.-position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen R.sub.2 is methyl, X is hydroxy or acetoxy and Y is hydrogen, the dotted lines at 1(2) and 6(7) do not represent a second bond and the dotted line in the 10-substituent is a third carbon-carbon bond useful as aldosterone antagonists and for increasing hydrosodium diuresis while preserving organic potassium with reduced hormonal side effects.

公开(公告)号：US4464302A

公开(公告)日：1984-08-07

申请号：US173172

申请日：1980-07-28

申请人： Lucien Nedelec ,  Vesperto Torelli

发明人： Lucien Nedelec ,  Vesperto Torelli

IPC分类号： C07J13/00 ,  C07J5/00 ,  C07J41/00 ,  C07J43/00 ,  C07J3/00

CPC分类号： C07J5/0015 ,  C07J41/005 ,  C07J41/0072

摘要： Novel 17-[(hydroxymethyl)formamido methylene]-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with halogen or an oxygen or nitrogen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A,B,C and D rings may contain one or more double bonds and are optionally substituted with at least one member of the group consisting of hydroxy, keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and a process for their preparation which are intermediates for the preparation of the corresponding 17-hydroxyacetyl steroids.

摘要翻译： 式17的[17] - [（羟甲基）甲酰氨基亚甲基] - 类固醇，其中R 1选自氢，任选被卤素或氧或氮官能团取代的1至4个碳原子的烷基和烯基，和 2至4个碳原子的炔基，R2是1至4个碳原子的烷基，A，B，C和D环可以含有一个或多个双键，并且任选被至少一个羟基， 酮，卤素，具有1至4个碳原子的烷基和烷氧基以及2至4个碳原子的烯基和炔基及其制备方法，其是制备相应的17-羟基乙酰基类固醇的中间体。

公开(公告)号：US4396614A

公开(公告)日：1983-08-02

申请号：US332842

申请日：1981-12-21

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Daniel Philibert

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Daniel Philibert

IPC分类号： C07J5/00 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61K31/585 ,  A61P7/10 ,  A61P9/00 ,  A61P9/12 ,  C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J51/00

CPC分类号： C07J41/0088 ,  C07J1/0033 ,  C07J1/0081 ,  C07J21/003 ,  C07J51/00

摘要： Novel steroids of the formula ##STR1## wherein R is selected from the group consisting of R.sub.1 and R.sub.2, R.sub.1 is selected from the group consisting of alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms R.sub.2 is --(CH.sub.2).sub.n --R.sub.3, n is an integer from 1 to 8 and R.sub.3 is selected from the group consisting of free or protected --OH, free or protected --NH.sub.2, monoalkyl and dialkylamino with 1 to 6 carbon atoms, a free, esterified or salified --COOH and halogen X and Y together form ##STR2## or X is OH and Y is --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, an alkali metal and --NH.sub.4, Ra is selected from the group consisting of hydrogen and methyl, the dotted line in the I(2)-position indicates the optional presence of a double bond and the wavy line indicates that R may be in the .alpha.- or .beta.-position, with the proviso that R is not R.sub.1 or R.sub.2 when n is 1 and R.sub.3 is halogen, when the 1(2) bond is a simple bond and when Ra is --CH.sub.3, R.sub.3 is not a free carboxyl when Y is --CH.sub.2 --CH.sub.2 --COOM in which M is an alkali metal or --NH.sub.4 and R.sub.3 is not a salified carboxyl when Y is --CH.sub.2 --CH.sub.2 --COOH having aldosterone antagonistic properties and increases aqueous sodium diuresis while conserving organic potassium without secondary hormonal effects and their preparation.

摘要翻译： 式（I）的新型类固醇，其中R选自R1和R2，R1选自1至8个碳原子的烷基和2至8个碳原子的烯基和炔基R2是 - （CH 2）n -R 3，n是1至8的整数，并且R 3选自游离或保护的-OH，游离或保护的-NH 2，具有1至6个碳原子的单烷基和二烷基氨基， 酯化或成盐的-COOH和卤素X和Y一起形成或者X是OH，Y是-CH 2 -CH 2 -COOM，M选自氢，碱金属和-NH 4，Ra选自 由氢和甲基组成的组，I（2） - 位中的虚线表示任选存在双键，波浪线表示R可以是α或β-位，条件是R 当n为1且R 3为卤素时，不是R 1或R 2，当1（2）键为单键并且当R a为-CH 3时，当Y为 当Y是具有醛固酮拮抗性的-CH 2 -CH 2 -COOH时，其中M是碱金属或-NH 4，并且R3不是盐化的羧基，并且在保留没有次级激素作用的有机钾的同时增加水溶性钠的利尿，-CH 2 -CH 2 -COOM 他们的准备。

公开(公告)号：US4395408A

公开(公告)日：1983-07-26

申请号：US292794

申请日：1981-08-14

申请人： Vesperto Torelli ,  Roger Deraedt ,  Lucien Nedelec

发明人： Vesperto Torelli ,  Roger Deraedt ,  Lucien Nedelec

IPC分类号： A61K31/56 ,  A61K31/57 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  C07J13/00 ,  C07J41/00 ,  C07J5/00 ,  A01N45/00 ,  C07C117/00

CPC分类号： C07J41/0027 ,  C07J13/007 ,  C07J41/0005 ,  Y10S514/885

摘要： Novel 3-amino-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, W is selected from the group consisting of hydrogen and --OH and taken together with x forms ethylidene, X is selected from the group consisting of ethyl, ##STR2## and taken together with W forms ethylidene and the wavy lines signify that the substituents are in the .alpha. or .beta.-position with the proviso that when R.sub.1 is methyl and X is ethyl, ##STR3## W is --OH and their non-toxic, pharmaceutically acceptable acid addition salts and their preparation and intermediates therefore capable of stimulating immunitary activity.

摘要翻译： 式（Ⅰ）的新型3-氨基类固醇，其中R 1选自氢和甲基，W选自氢和-OH，并与x一起形成亚乙基，X选自 由乙基组成的基团与W一起形成亚乙基，波浪线表示取代基在α或β-位，条件是当R 1是甲基且X是乙基时，W是 -OH及其无毒的药学上可接受的酸加成盐及其制备和中间体因此能够刺激免疫活性。

公开(公告)号：US4376734A

公开(公告)日：1983-03-15

申请号：US319912

申请日：1981-11-10

申请人： Vesperto Torelli ,  Lucien Nedelec

发明人： Vesperto Torelli ,  Lucien Nedelec

IPC分类号： C07J41/00 ,  C07J5/00 ,  C07J7/00

CPC分类号： C07J41/0027 ,  C07J41/0011

摘要： A novel process for the preparation of 3-amino-steroids of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## and the wavy lines indicate that the substituents may be in the .alpha.- or .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts in good yields and novel intermediates.

摘要翻译： 用于制备式（I）的3-氨基 - 类固醇的新方法，其中X选自和波浪线表示取代基可以是α或β-位， 其无毒的，药学上可接受的酸加成盐和良好的产率和新的中间体。

公开(公告)号：US4263290A

公开(公告)日：1981-04-21

申请号：US98766

申请日：1979-11-30

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

IPC分类号： C07D317/14 ,  A61K31/57 ,  A61P5/38 ,  A61P9/12 ,  C07D317/72 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  C07J43/00 ,  C07J51/00 ,  C07J53/00 ,  A61K31/56

CPC分类号： C07J7/002 ,  C07D317/72 ,  C07J17/00 ,  C07J43/006 ,  C07J5/0015 ,  C07J7/007

摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 taken together form a cycloalkyl of 3 to 8 carbon atoms or are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms with the proviso that both cannot be hydrogen, R.sub.3 is alkyl of 2 to 4 carbon atoms, R.sub.4 ' is selected from the group consisting of hydrogen, hydroxyl, acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and ##STR2## and M is selected from the group consisting of hydrogen and alkali metal, having antagonistic properties to aldosterone and increasing sodium-water diuresis with conservation of organic potassium and a novel process and novel intermediates for their preparation.

摘要翻译： 式Ⅰ'的新型19-去甲甾类化合物，其中R 1和R 2一起形成3至8个碳原子的环烷基或分别选自氢，1至4个碳原子的烷基和烯基，和 2至6个碳原子的炔基，条件是两者不能是氢，R3是2至4个碳原子的烷基，R4'选自氢，羟基，1至18碳的有机羧酸的酰氧基 原子和M选自氢和碱金属，对醛固酮具有拮抗作用，并增加钠 - 水利尿与保护有机钾的新方法和新的制备中间体。

公开(公告)号：US4136179A

公开(公告)日：1979-01-23

申请号：US831254

申请日：1977-09-07

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

IPC分类号： A61K31/57 ,  A61P5/38 ,  A61P9/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J17/00 ,  C07J43/00 ,  A61K31/56

CPC分类号： C07J17/00 ,  C07J43/003 ,  C07J5/0015 ,  C07J7/002 ,  C07J9/00

摘要： 2,2-DIMETHYL-19-NOR-STEROIDS OF THE FORMULA ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, ##STR2## and R.sub.2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 17 carbon atoms and the dotted lines indicate the optional presence of a double bond in 9(10) and 11(12) positions having antialdosteronic activity and an increased sodium diuresis with conservation of organic potassium and their preparation and novel intermediates.

公开(公告)号：US4078059A

公开(公告)日：1978-03-07

申请号：US719138

申请日：1976-08-31

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex

IPC分类号： A61K31/57 ,  A61P9/00 ,  A61P9/12 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  C07J31/00 ,  A61K31/56

CPC分类号： C07J5/0015 ,  C07J17/00 ,  C07J31/003 ,  C07J7/002

摘要： Novel 2,2-dimethyl steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, --OH and ##STR2## R.sub.1 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 17 carbon atoms Z is selected from the group consisting of hydrogen and ##STR3## in the .alpha.-position, R.sub.2 is alkyl of 1 to 4 carbon atoms and the dotted line in the B ring indicates the optional presence of a double bond in the 6(7) position having antialdosterone activity and increasing sodium diuresis while conserving organic potassium.

摘要翻译： 式（Ⅰ）所示的新型2,2-二甲基类固醇，其中R选自氢，-OH和R 1选自氢和1至17个碳原子的烃基Z是 选自α位中的氢和，R2是1至4个碳原子的烷基，B环中的虚线表示在6（7）位任选存在双键， 抗肿瘤活性和增加钠利尿，同时保护有机钾。

公开(公告)号：US4565656A

公开(公告)日：1986-01-21

申请号：US343357

申请日：1982-01-27

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Michel Hardy

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Michel Hardy

IPC分类号： C07J5/00 ,  C07J13/00 ,  C07J41/00 ,  C07J3/00

CPC分类号： C07J41/005 ,  C07J5/0053

摘要： A novel process for the preparation of 17.beta.-hydroxyacetyl-17.alpha.-ol-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with halogen or an oxygen or nitrogen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A,B,C and D rings may contain one or more double bonds and are optionally substituted with at least one member of the group consisting of hydroxy, keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms which compounds are generally known of the cortisonic type with known properties.

摘要翻译： 制备式Ia的17β-羟基乙酰基-17α-醇类的新方法，其中R1选自氢，任选被卤素或氧取代的1至4个碳原子的烷基 或氮官能团和2至4个碳原子的烯基和炔基，R2是1至4个碳原子的烷基，A，B，C和D环可以含有一个或多个双键，并且任选被至少一个成员 由1-4个碳原子的羟基，酮基，卤素，烷基和烷氧基以及2至4个碳原子的烯基和炔基组成的组通常已知具有已知性质的皮质类型。

公开(公告)号：US4258039A

公开(公告)日：1981-03-24

申请号：US125891

申请日：1980-02-29

申请人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex ,  Colette Tournemine

发明人： Lucien Nedelec ,  Vesperto Torelli ,  Robert Fournex ,  Colette Tournemine

IPC分类号： A61K31/565 ,  A61K31/575 ,  A61K31/585 ,  A61P5/38 ,  A61P9/00 ,  A61P9/12 ,  C07J1/00 ,  C07J9/00 ,  C07J21/00 ,  C07J51/00 ,  A61K31/58

CPC分类号： C07J21/003 ,  C07J1/0033 ,  C07J51/00

摘要： Novel 7-alkyl-.DELTA..sup.4 -17.alpha.-pregnene-3-ones of the formula ##STR1## wherein R is selected from the group consisting of saturated and unsaturated alkyl of 2 to 8 carbon atoms, cycloalkyl alkyl of 4 to 8 carbon atoms and arylalkyl of 7 to 12 carbon atoms and X and Y form the group ##STR2## or X is OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, alkali metal and NH.sub.4 and the wavy line indicates the .alpha.- or .beta.-position or mixtures thereof having aldosterone antagonistic activity and increased hydrosodium diuresis with organic potassium conservation while devoid of secondary hormonal effects and their preparation.

摘要翻译： 新型7-烷基-TATA4-17α-孕烯-3-酮，其中R选自2-8个碳原子的饱和和不饱和烷基，4-8个碳原子的环烷基烷基 7至12个碳原子的原子和芳基烷基，X和Y形成基团，或X是OH，Y是，M选自氢，碱金属和NH 4，波浪线表示 α-或β-位或其混合物具有醛固酮拮抗活性和增加的氢化钠利尿与有机钾保护，而没有次级激素作用及其制备。