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19 条记录 (耗时 0.026 秒)

    Novel 3-keto-steroids
    4.
    发明授权
    Novel 3-keto-steroids 失效
    新的3-酮醇酯

    公开(公告)号：US5081113A

    公开(公告)日：1992-01-14

    申请号：US497564

    申请日：1990-03-21

    申请人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    发明人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    IPC分类号： A61K31/58 ,  A61P3/06 ,  A61P29/00 ,  A61P39/02 ,  C07J1/00 ,  C07J43/00

    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。

    19-nor-3-keto steroids
    5.
    发明授权
    19-nor-3-keto steroids 失效
    19-NOR-3-KETO STEROIDS

    公开(公告)号：US5108996A

    公开(公告)日：1992-04-28

    申请号：US497562

    申请日：1990-03-21

    申请人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    发明人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    IPC分类号： A61K31/58 ,  A61P3/06 ,  A61P39/02 ,  C07J1/00 ,  C07J43/00

    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。

    Novel 17-hetero substituted steroids
    6.
    发明授权
    Novel 17-hetero substituted steroids 失效
    新型17-取代类固醇

    公开(公告)号：US4921846A

    公开(公告)日：1990-05-01

    申请号：US245750

    申请日：1988-09-16

    申请人： Lucien Nedelec ,  Andre Claussner ,  Daniel Philibert ,  Martine Moguilewsky

    发明人： Lucien Nedelec ,  Andre Claussner ,  Daniel Philibert ,  Martine Moguilewsky

    IPC分类号： A61K31/58 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00

    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。

    N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines
    7.
    发明授权
    N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines 失效
    N，N，N'，N'-6-（1-哌嗪基）-2,5-吡啶基亚胺

    公开(公告)号：US5302719A

    公开(公告)日：1994-04-12

    申请号：US990729

    申请日：1992-12-15

    申请人： Andre Claussner ,  Jacques LeClaire ,  Lucien Nedelec ,  Daniel Philibert

    发明人： Andre Claussner ,  Jacques LeClaire ,  Lucien Nedelec ,  Daniel Philibert

    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。

    N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines
    8.
    发明授权
    N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines 失效
    N，N，N'，N'-6-（1-哌嗪基）-2,5-吡啶基亚胺

    公开(公告)号：US5202316A

    公开(公告)日：1993-04-13

    申请号：US774568

    申请日：1991-10-09

    申请人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    发明人： Andre Claussner ,  Jacques Leclaire ,  Lucien Nedelec ,  Daniel Philibert

    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。

    19-nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, and the intermediates of this process, their use as medicaments and compositions
    9.
    发明授权
    19-nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, and the intermediates of this process, their use as medicaments and compositions 失效
    19-还没有在位置11beta具有硫代碳链的类固醇，其制备方法和该方法的中间体，以及该方法的中间体，它们作为药物和组合物的用途

    公开(公告)号：US06281204B1

    公开(公告)日：2001-08-28

    申请号：US08244735

    申请日：1994-06-09

    申请人： Andre Claussner ,  Francois Nique ,  Jean-Georges Teutsch ,  Patrick Van De Velde

    发明人： Andre Claussner ,  Francois Nique ,  Jean-Georges Teutsch ,  Patrick Van De Velde

    IPC分类号： A61K3158

    CPC分类号： C07J31/006 ,  C07J41/0005 ,  C07J41/0016 ,  C07J41/0083 ,  C07J43/003

    摘要： Compounds of formula (I), wherein R17 and R′17 are such that: either R17 and R′17 together form ketone, hydrazono, oxime or methylene, or R17 is hydroxyl, hydroxymethyl or acyloxy and R′17 is hydrogen, alkyl or optionally substitued alkenyl or alkynyl; R3 is hydrogen or alkyl; R16 is hydrogen, halogen or alkyl; m is 0, 1 or 2; X, Y and Z are such that: X is methylene, arylene or arylenoxy bonded to the steroid by a carbon atom; Y is a saturated or unsaturated straight or branched aliphatic chain which is optionally interrupted by oxygen; and Z is aryl, arylalkyl or straight or branched alkyl; addition salts thereof, a preparation method therefor, medicinal uses thereof, compositions containing said compounds, and resulting novel intermediates.

    摘要翻译： 式（I）化合物，其中R 17和R 17如此：R 17和R 17一起形成酮，亚肼基，肟或亚甲基，或R 17为羟基，羟甲基或酰氧基，R 17为氢，烷基或 任选取代的烯基或炔基; R3是氢或烷基; R16是氢，卤素或烷基; m为0,1或2; X，Y和Z使得：X是亚甲基，亚芳基或亚芳基氧基通过碳原子键合到类固醇; Y是任选被氧中断的饱和或不饱和直链或支链脂族链; Z为芳基，芳烷基或直链或支链烷基; 其加成盐，其制备方法，其医药用途，含有所述化合物的组合物，以及所得的新型中间体。