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19 条记录 (耗时 0.019 秒)

    Novel 3-keto-steroids
    1.
    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
    2.
    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。

    N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines
    3.
    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
    4.
    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。

    Novel 17-hetero substituted steroids
    8.
    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。

    Steroids, their use as medicaments, their preparation process, the intermediates of this process and the compositions containing them
    9.
    发明授权
    Steroids, their use as medicaments, their preparation process, the intermediates of this process and the compositions containing them 失效
    类固醇，它们作为药物的用途，其制备方法，该方法的中间体和含有它们的组合物

    公开(公告)号：US06492536B2

    公开(公告)日：2002-12-10

    申请号：US09891558

    申请日：2001-06-25

    申请人： Neerja Bhatnagar ,  Andre Claussner ,  Christian Marchandeau ,  Michele Resche Rigon ,  Jean-Georges Teutsch

    发明人： Neerja Bhatnagar ,  Andre Claussner ,  Christian Marchandeau ,  Michele Resche Rigon ,  Jean-Georges Teutsch

    IPC分类号： C07J300

    CPC分类号： C07J41/0094 ,  C07J7/0085 ,  C07J9/005 ,  C07J31/006

    摘要： The subject of the invention is the products of formula (I): in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.

    摘要翻译： 本发明的主题是式（I）的产物：其中R 1表示卤素，羟基，（C 1 -C 8）烷氧基或（C 1 -C 12）酰氧基，R 2表示卤素或氢，或R 1和R 2一起形成 Z选自任选取代的（C 1 -C 8）烷硫基，任选取代的芳硫基，（C 1 -C 8）烷氧基，卤素，氰基，巯基，氰硫基和（CH 2）0-1-CO 2 H，任选酯化，Y代表 氢或甲基，位置1-2或5-6中的虚线任选代表第二个键，以及它们的加成盐，其制备方法，该方法的中间体和含有它们的药物组合物。