利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

40 条记录 (耗时 0.032 秒)

    Novel 11.beta.-substituted -19-nor-steriods
    1.
    发明授权
    Novel 11.beta.-substituted -19-nor-steriods 失效
    新型11β-取代-19-去甲基异亮氨酸

    公开(公告)号：US5043332A

    公开(公告)日：1991-08-27

    申请号：US421526

    申请日：1989-10-13

    申请人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert ,  Germain Costerousse

    发明人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert ,  Germain Costerousse

    IPC分类号： C07J1/00 ,  C07J7/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J63/00 ,  C07J71/00

    CPC分类号： C07J41/0094 ,  C07J1/0059 ,  C07J1/007 ,  C07J1/0088 ,  C07J21/006 ,  C07J41/0016 ,  C07J41/0077 ,  C07J41/0083 ,  C07J43/003 ,  C07J51/00 ,  C07J63/008 ,  C07J7/0005 ,  C07J71/001 ,  C07J71/0063

    摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R'.sub.a and R".sub.a are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom--with the proviso that when A and B are ##STR4## wherein R' and R" are both hydrogen, R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid activity, their preparation and novel intermediates.

    摘要翻译： 式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃 至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a） （c）图像（d）图像（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，R x选自 由氢和ORe组成，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，Ra可以在如波形线所示的E或Z位置，并且选自 的＆lt; IMAGE＆gt;和酰氧基，R'a和R'a是1〜4个碳原子的烷基或与n 氢原子形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为其中R'和R“均为氢时，R 1包含至少一个氮，磷或硅原子 当A和B是时，R1不是具有显着的抗糖皮质激素活性的直链烷基及其无毒的药学上可接受的酸加成盐，其制备和新的中间体。

    Novel 11.beta.-substituted-19-nor-steroids
    2.
    发明授权
    Novel 11.beta.-substituted-19-nor-steroids 失效
    新型11β-取代-19-去甲类固醇

    公开(公告)号：US4978657A

    公开(公告)日：1990-12-18

    申请号：US810316

    申请日：1985-12-17

    申请人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert ,  Germain Costerousse

    发明人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert ,  Germain Costerousse

    IPC分类号： C07J1/00 ,  C07J7/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J63/00 ,  C07J71/00

    CPC分类号： C07J41/0094 ,  C07J1/0059 ,  C07J1/007 ,  C07J1/0088 ,  C07J21/006 ,  C07J41/0016 ,  C07J41/0077 ,  C07J41/0083 ,  C07J43/003 ,  C07J51/00 ,  C07J63/008 ,  C07J7/0005 ,  C07J71/001 ,  C07J71/0063

    摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at leat one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## wherein R' and R" are both hydrogen, R.sub.1 contain at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid activity, their preparation and novel intermediates.

    摘要翻译： 式（Ⅰ）的新型19-去甲甾类化合物，其中R 1是1至18个碳原子的有机基团，其任选地含有一个杂原子与紧邻11个碳原子的原子是碳，R 2是1的烃 至8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组： + TR R'和R“分别选自氢，-CN和1至4个碳原子的烷基，Rx选自氢和ORe，Re选自由以下组成的组： 氢，任选取代的1至6个碳原子的烷基和酰基，Ra可以在如波形线所示的E或Z位置，并且选自由下列组成的组：酰氧基，Ra'和Ra“是 具有1至4个碳原子的烷基或与氮原子一起形成 任选地含有另一个杂原子的5至6个链成员的杂环，条件是当A和B是R 1和B均为氢时，R 1包含至少一个氮，磷或硅原子，当A和 B是不具有显着的抗糖皮质激素活性的线性烷基及其无毒的药学上可接受的酸加成盐，其制备方法和新的中间体。

    Novel 11 beta-substituted-19-nor-steroids
    3.
    发明授权
    Novel 11 beta-substituted-19-nor-steroids 失效
    新型11型β-取代-19-去甲甾类

    公开(公告)号：US4634696A

    公开(公告)日：1987-01-06

    申请号：US760703

    申请日：1985-07-30

    申请人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    发明人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    IPC分类号： A61K31/565 ,  A61P5/38 ,  C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  A61K31/56

    CPC分类号： C07J1/0088 ,  C07J1/0059 ,  C07J1/007 ,  C07J21/006 ,  C07J41/0077 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J71/0063

    摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.

    摘要翻译： 式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃 至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a） （c）＆lt; IMAGE＆gt;（d）和＆lt; IMAGE＆gt;（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，其中至少一个是其它 R x选自氢和ORe，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，R a可以在E或Z位置，如 波浪线，并且选自和酰氧基，Ra'和Ra“是烷基 1至4个碳原子或与氮原子一起形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时， A和B是，R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

    Novel 11.beta.-substituted-19-nor-steroids
    4.
    发明授权
    Novel 11.beta.-substituted-19-nor-steroids 失效
    新型11β-取代-19-去甲类固醇

    公开(公告)号：US4547493A

    公开(公告)日：1985-10-15

    申请号：US501373

    申请日：1983-06-06

    申请人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    发明人： Jean-Georges Teutsch ,  Vesperto Torelli ,  Roger Deraedt ,  Daniel Philibert

    IPC分类号： A61K31/565 ,  A61P5/38 ,  C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  A61K31/56

    CPC分类号： C07J1/0088 ,  C07J1/0059 ,  C07J1/007 ,  C07J21/006 ,  C07J41/0077 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J71/0063

    摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.

    摘要翻译： 式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃 至8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：＆lt; IMAGE＆gt; + TR＆lt; IMAGE＆gt; R'和 R“分别选自氢，-CN和具有1至4个碳原子的烷基，其中至少一个不同于氢，Rx选自氢和ORe + L，Re选自 由氢，任选取代的1至6个碳原子的烷基和酰基组成的组Ra可以在如波形线所示的E或Z位置，并且选自由下列组成的组：酰基氧基，R a'和 R a“为1至4个碳原子的烷基或被取代 与氮原子一起形成任选含有另外杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时，当A和B为 R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

    Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids
    8.
    发明授权
    Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids 失效

    公开(公告)号：US5064822A

    公开(公告)日：1991-11-12

    申请号：US438359

    申请日：1989-11-16

    申请人： Daniel Philibert ,  Jean G. Teutsch ,  Germain Costerousse ,  Roger Deraedt

    发明人： Daniel Philibert ,  Jean G. Teutsch ,  Germain Costerousse ,  Roger Deraedt

    IPC分类号： C07J1/00 ,  C07J7/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

    CPC分类号： C07J7/003 ,  C07J1/0096 ,  C07J17/00 ,  C07J21/006 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0016 ,  C07J41/0077 ,  C07J41/0083 ,  C07J41/0094 ,  C07J51/00 ,  C07J7/0045 ,  C07J7/0075 ,  C07J71/001

    摘要： Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.3 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms, --OH, acetyl, hydroxyacetyl, carboxyalkoxy of 2 to 4 carbon atoms optionally esterified or salified and hydroxyalkyl of 1 to 6 carbon atoms optionally esterified, R.sub.4 is selected from the group consisting of hydrogen, alkylthio and alkoxy of 1 to 12 carbon atoms, trialkylsilyl of 1 to 6 carbon atoms, --CN, --OH and alkyl, alkenyl and alkynyl of up to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkylamino and dialkylamino of 1 to 6 alkyl carbon atoms, R.sub.5 is selected from the group consisting of hydrogen and methyl in the .alpha.- or .beta.-position, X is .dbd.0 or hydroxyimino or alkoxyimino of 1 to 4 carbon atoms in the syn or anti form and A and B are an epoxy or a second bond in the 9(10) position and their non-toxic, pharmaceutically acceptable acid addition salts where R.sub.4 is an amino group, with the proviso that A and B are not a second bond in the 9(10)-position when X is .dbd.0 and R.sub.5 is hydrogen and a) R.sub.2 is methyl and .alpha.) R.sub.3 is --OH and i) R.sub.1 is ethyl or phenyl and R.sub.4 is hydrogen or ii) R.sub.1 is ethyl, propyl, isopropyl, vinyl, allyl, isopropenyl, phenyl, 4-fluorophenyl, methoxyphenyl or thienyl and R.sub.4 is ethynyl or iii) R.sub.1 is propyl, isopropyl, vinyl, allyl, isopropenyl, 4-methoxyphenyl or thienyl and R.sub.4 is methyl and .beta.) R.sub.3 is acetyl and i) R.sub.1 is ethyl, vinyl or phenyl and R.sub.4 is --OH or ii) R.sub.1 is vinyl and R.sub.4 is methyl and b) R.sub.2 is ethyl and R.sub.1 is vinyl, R.sub.3 is --OH and R.sub.4 is hydrogen possessing a remarkable antiglucocorticoidal activity.

    Steroids
    10.
    发明授权
    Steroids 失效
    类固醇

    公开(公告)号：US4519946A

    公开(公告)日：1985-05-28

    申请号：US614440

    申请日：1984-05-25

    申请人： Jean G. Teutsch ,  Germain Costerousse ,  Daniel Philibert ,  Roger Deraedt

    发明人： Jean G. Teutsch ,  Germain Costerousse ,  Daniel Philibert ,  Roger Deraedt

    IPC分类号： C07J1/00 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P3/08 ,  A61P5/38 ,  A61P9/10 ,  A61P9/12 ,  A61P25/20 ,  A61P37/04 ,  A61P43/00 ,  C07J7/00 ,  C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J63/00 ,  C07J71/00 ,  C07J53/00

    CPC分类号： C07J41/0016 ,  C07J21/006 ,  C07J41/0077 ,  C07J41/0083 ,  C07J43/003 ,  C07J51/00 ,  C07J63/008 ,  C07J7/0005 ,  C07J71/001 ,  Y10S514/01

    摘要： Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbons atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C=A group at position 3 is selected from the group consisting of C-O, ketal, which may be open or closed ##STR2## --C.dbd.NOH,--C--NOAlK.sub.3 and C--CH.sub.2,AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocoritcoid activity and a process for their preparation.

    摘要翻译： 具有式“IMAGE”I的新型19-或类固醇和19-去甲基-D-同型甾族化合物，其中R 1是含有至少一个选自氮，磷和 具有与碳原子紧邻的原子的硅为碳，R2为碳原子数为1〜8的烃基，X选自五价环和任意含有双键的六角环， B和C一起形成双键或环氧基，第3位的C = A基团选自CO，缩酮，其可以是开或关的-C = NOH，-C-NOAlK3 和C-CH 2，AlK1，AlK 2和AlK 3选自由1至8个碳原子的烷基和7至15个碳原子的芳烷基组成的组及其无毒的药学上可接受的具有抗葡糖聚糖活性的酸加成盐和 他们的准备过程。