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公开(公告)号：US5108996A
公开(公告)日：1992-04-28
申请号：US497562
申请日：1990-03-21
CPC分类号： C07J1/0048 , C07J1/0044 , C07J43/003
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.17 is ##STR2## is hydrogen or --OH or acyloxy of 1 to 18 carbon atoms, Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms and P is selected from the group consisting of pyrimidinyl and pyridyl optionally substituted with 1 or 2 individual members of the group consisting of amino, alkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and (B aminated 5- or 6-membered heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms) and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidant activity.
摘要翻译： 选自下式的化合物的化合物其中R 2和R 12独立地是氢或甲基，R 11是具有1至18个碳原子的有机基团，任选地含有至少一个与原子相邻的原子的杂原子 11碳原子是碳，13位和17位的波浪线表示当13-甲基是α时，R'17基团是β，R17是α，当13-甲基是β时，R17是 β和R'17是α，R17是-OH或1至18个碳原子的酰氧基，R'17是氢或-OH或含1至18个碳原子的酰氧基，Z选自 由单键键合，1至5个碳原子的亚烷基和2至5个碳原子的亚烯基和亚炔基组成的组，P选自嘧啶基和吡啶基，任选被1或2个独立成员取代的氨基 ，烷基氨基和1至4个烷基碳原子的二烷基氨基和（B胺化的5或6元环 任选被1至3个碳原子的烷基取代的杂环）及其无毒的药学上可接受的具有抗炎和抗氧化活性的酸加成盐。
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公开(公告)号：US5302719A
公开(公告)日：1994-04-12
申请号：US990729
申请日：1992-12-15
IPC分类号： C07D213/74 , C07J43/00 , C07D401/00
CPC分类号： C07D213/74 , C07J43/003
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.A, R.sub.A.sup.1, R.sub.B R.sub.B.sup.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms or R.sub.A and R.sub.A.sup.1 or R.sub.B and R.sub.B.sup.1 together with the nitrogen atom to which they are attached form a 5- to 6-member heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms and Y is hydrogen or ##STR2## wherein R.sub.6 is selected from the group consisting of hydrogen, --CH.sub.3, --F and --Cl, R.sub.9 and R.sub.11 form a second bond at 9(11) or R.sub.9 is hydrogen or --F and R.sub.11 is hydrogen, --OH or .dbd.0, R.sub.16 is --CH.sub.3 or hydrogen, R.sub.17 is hydrogen, --OH or acyloxy, the dotted lines indicate the possible presence of a second bond at 1(2) and 6(7)-positions and the wavy line indicates the .alpha.- and .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and antioxidant activity.
摘要翻译： 选自下列化合物的化合物其中RA，RA1，RB RB1分别选自氢和1至4个碳原子的烷基或RA和RA1或RB和RB1在一起的化合物 与它们所连接的氮原子形成任选被1至3个碳原子的烷基取代的5至6元杂环，Y是氢或其中R 6选自氢，-CH 3， -F和-Cl，R 9和R 11在9（11）处形成第二个键，或者R 9是氢或-F，R 11是氢，-OH或= 0，R 16是-CH 3或氢，R 17是氢，-OH或 酰氧基，虚线表示在1（2）和6（7） - 位上可能存在第二个键，并且波浪线表示α和β-位及其无毒的药学上可接受的具有抗氧化剂的酸加成盐 炎症和抗氧化活性。
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公开(公告)号：US5202316A
公开(公告)日：1993-04-13
申请号：US774568
申请日：1991-10-09
IPC分类号： C07D213/74 , C07J43/00
CPC分类号： C07D213/74 , C07J43/003
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.A, R'.sub.A, R.sub.B and R'.sub.B are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms or R.sub.A and R'.sub.A or R.sub.B and R'.sub.B together with the nitrogen atom to which they are attached form a 5- to 6-member heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms and Y is hydrogen or ##STR2## wherein R.sub.6 is selected from the group consisting of hydrogen, --CH.sub.3, --F and --Cl, R.sub.9 and R.sub.11 form a second bond at 9(11) or R.sub.9 is hydrogen or --F is hydrogen, --OH or .dbd.O, R.sub.16 is --CH.sub.3 or hydrogen, R.sub.17 is hydrogen, --OH or acyloxy, the dotted lines indicate the possible presence of a second bond at 1(2) and 6(7)-positions and the wavy line indicates the .alpha.- and .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and antioxidant activity.
摘要翻译： 选自下列化合物的化合物其中RA，R'A，RB和R'B分别选自氢和1至4个碳原子的烷基或RA和R A或RB和R'B与它们所连接的氮原子一起形成任选被1至3个碳原子的烷基取代的5至6元杂环，Y是氢或其中R 6选自 由氢，-CH 3，-F和-Cl，R 9和R 11组成的基团在9（11）处形成第二个键，或者R 9是氢或-F是氢，-OH或= O，R 16是-CH 3或氢， R17是氢，-OH或酰氧基，虚线表示在1（2）和6（7） - 位上可能存在第二个键，波浪线表示α和β位，它们的无毒， 具有抗炎和抗氧化活性的药学上可接受的酸加成盐。
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公开(公告)号：US5081113A
公开(公告)日：1992-01-14
申请号：US497564
申请日：1990-03-21
CPC分类号： C07J1/0048 , C07J1/0044 , C07J43/003
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of halogen, --CH.sub.3, fluorine and chlorine, R.sub.9 and R.sub.11 together form a second bond at 9(11) or R.sub.9 is hydrogen or fluorine and R.sub.11 is selected from the group consisnting of hydrogen, --OH and .dbd.O, the dotted lines in rings A and B indicate a possible additonal bond at 1(2) and 6(7), R.sub.17 is hydrogen or acyl or an organic carboxylic acid of 1 to 18 carbon atoms, R'.sub.17 is ##STR2## Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms, P is pyrimidinyl or pyridyl optionally substituted with one or two individual members of the group consisting of --NH.sub.2, alkylamino, dialkylamino and aminated 5- or 6- membered heterocycles optionally substituted with alkyl of 1 to 3 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidation activity.
摘要翻译： 选自下列化合物的化合物其中R 6选自卤素，-CH 3，氟和氯，R 9和R 11一起在9（11）或R9上形成第二个键 是氢或氟并且R 11选自氢，-OH和= O的基团，环A和B中的虚线表示在1（2）和6（7）处可能的附加键，R 17是氢或酰基 或具有1至18个碳原子的有机羧酸，R'17是选自单键，1至5个碳原子的亚烷基和2至5个碳原子的亚烯基和亚炔基，P 是任选被一个或两个独立的由-NH 2，烷基氨基，二烷基氨基和胺化的5-或6-元杂环取代的嘧啶基或吡啶基，任选被1至3个碳原子的烷基取代，其无毒的药学上可接受的 具有抗炎和抗氧化的酸加成盐 dation活动。
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公开(公告)号：US5707982A
公开(公告)日：1998-01-13
申请号：US68735
申请日：1993-05-28
申请人： Andre Claussner , Daniel Philibert , Lucien Nedelec , Patrick Van De Velde , Francois Nique , Jean-Georges Teutsch
发明人： Andre Claussner , Daniel Philibert , Lucien Nedelec , Patrick Van De Velde , Francois Nique , Jean-Georges Teutsch
CPC分类号： C07J41/0077 , C07J41/0083 , C07J43/003 , C07J63/008
摘要： A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##
摘要翻译： 具有选自由下列组成的组的19-去甲甾醇类型：其中A和B环具有选自下组的结构：
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公开(公告)号：US5149696A
公开(公告)日：1992-09-22
申请号：US484424
申请日：1990-02-23
CPC分类号： C07J41/0083 , C07J41/0077 , C07J43/003
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.
摘要翻译： 具有下式的新型19-去甲类固醇：其中A和B环具有选自具有激素性质的组合和其制备和中间体的结构的结构。
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公开(公告)号：US5290771A
公开(公告)日：1994-03-01
申请号：US875460
申请日：1992-04-29
CPC分类号： C07J41/0083 , C07J41/0077 , C07J43/003
摘要： The novel compounds of the invention are 19 nor-steroids of the formula: ##STR1## Where A, B, C, D, X, Y, Z, R.sub.17, and R.sup.1 are as defined in the specification, having hormonal properties and their preparation and intermediates.
摘要翻译： 本发明的新化合物是下式的19种类固醇：其中A，B，C，D，X，Y，Z，R 17和R 1如说明书中所定义，具有激素性质及其 制剂和中间体。
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公开(公告)号：US4921846A
公开(公告)日：1990-05-01
申请号：US245750
申请日：1988-09-16
CPC分类号： C07J41/0083 , C07J21/00 , C07J21/006 , C07J31/006 , C07J71/001
摘要： Steroids with a 17-spiro substituent of 3,4 or 6 ring members of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of carbocyclic aryl, heterocyclic aryl and aralkyl, R.sub.2 is a hydrocarbon of 1 to 18 carbon atoms in the .alpha.-or .beta.-position, the wavy line of the spiro ether indicates the oxygen is .alpha.-or .beta.-, X is selected from the group consisting of --CH.dbd.CH--CH.sub.2 --CH.sub.2 -- and --(CH.sub.2).sub.n --, n is 1, 2 or 4, the A and B rings have a structure selected from the group consisting of ##STR2## R' and R" are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.e is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, substituted alkyl of 1 to 6 carbon atoms and acyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiprogestomimetic activity.
摘要翻译： 具有3,4或6个具有式I的环成员的17-螺环取代基的类固醇，其中R 1选自碳环芳基，杂环芳基和芳烷基，R 2是1至18个碳原子的烃， α - 或β-位，螺醚的波浪线表示氧是α-或β-，X选自-CH = CH-CH 2 -CH 2 - 和 - （CH 2）n - （a）和（b）中，A和B环具有选自下列的结构：（a）
（b） （c） 和 R' R“分别为氢或1至4个碳原子的烷基，Re选自氢，1至6个碳原子的烷基，1至6个碳原子的取代烷基和酰基及其无毒的药学上 可接受的酸加成盐具有显着的抗切割模拟活性。 -
公开(公告)号：US5166146A
公开(公告)日：1992-11-24
申请号：US568597
申请日：1990-08-16
CPC分类号： C07J41/0083 , C07J63/008
摘要： A compound of the formula ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon of 1 to 8 carbon atoms, R.sub.a and R.sub.b are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is hydrogen or optionally substituted alkyl of 1 to 12 carbon atoms, n is an integer from 1 to 6, Z is free carboxy or salified with an alkali metal, alkaline earth metal or NH.sub.4 and X is the remainder of an optionally substituted and optionally unsaturated 5 or 6-member ring and the wavy line indicates the .alpha.- or .beta.-position for R.sub.1 having anti-glucocorticoid activity.
摘要翻译： 式（I）的化合物其中R 1是1至8个碳原子的脂族烃，R a和R b分别是氢或1至4个碳原子的烷基，R 2是氢或任选取代的1至12的烷基 碳原子，n为1至6的整数，Z为游离羧基或用碱金属，碱土金属或NH 4盐化，X为任选取代的和任选不饱和的5或6元环的其余部分，波浪线 表示具有抗糖皮质激素活性的R1的α或β位。
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公开(公告)号：US4943566A
公开(公告)日：1990-07-24
申请号：US225305
申请日：1988-07-28
申请人： Lucien Nedelec , Francois Nique , Daniel Philibert , Martine Moguilewsky , Marie-Madeleine Bouton
发明人： Lucien Nedelec , Francois Nique , Daniel Philibert , Martine Moguilewsky , Marie-Madeleine Bouton
IPC分类号： A61K31/56 , A61K31/565 , A61K31/58 , A61P35/00 , C07J1/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J21/006 , C07J1/0081 , C07J31/006 , C07J41/0083
摘要： A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom connected to the C ring by a carbon atom, R.sub.2 is methyl or ethyl, the A and B rings being selected from the group consisting of ##STR2## Re is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl and the D ring is selected from the group consisting of ##STR3## one of R.sub.3 and R.sub.4 is selected from the group consisting of hydroxy, protected hydroxy, acyl and alkoxy and the other is an optionally substituted aryl, R.sub.5 is an optionally substituted aryl and their non-toxic, pharmaceutically acceptable salts with acids and bases with the proviso that when the A and B rings are ##STR4## R.sub.1 is ##STR5## R.sub.2 is methyl, R.sub.3 is --OH, R.sub.4 is phenyl having anti proliferative properties.
摘要翻译： 选自下列化合物的化合物：其中R 1是具有1至18个碳原子的有机物，其任选地含有至少一个与碳原子连接在C环上的杂原子，R2是甲基或乙基， A和B环选自
+ TR Re选自氢，任选取代的1至6个碳原子的烷基和酰基，D环选自 的R 3和R 4中的一个选自羟基，保护的羟基，酰基和烷氧基，另一个是任选取代的芳基，R 5是任选取代的芳基及其与酸的无毒的药学上可接受的盐 碱基，条件是当A和B环为R 1时，R 2为甲基，R 3为-OH，R 4为具有抗增殖性质的苯基。
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