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    Novel 11 beta-substituted-19-nor-steroids
    1.
    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-steriods
    2.
    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
    3.
    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
    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。

    Phenylimidazolidines having antiandrogenic activity
    10.
    发明授权
    Phenylimidazolidines having antiandrogenic activity 失效
    具有抗雄激素活性的苯基咪唑烷

    公开(公告)号：US5627201A

    公开(公告)日：1997-05-06

    申请号：US372648

    申请日：1995-01-13

    申请人： Martine Gaillard-Kelly ,  Francois Goubet ,  Daniel Philibert ,  Jean-Georges Teutsch

    发明人： Martine Gaillard-Kelly ,  Francois Goubet ,  Daniel Philibert ,  Jean-Georges Teutsch

    IPC分类号： C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  C07D233/84 ,  C07D233/86 ,  C07D233/88 ,  A61K31/415

    CPC分类号： C07D233/74 ,  C07D233/72 ,  C07D233/76 ,  C07D233/84 ,  C07D233/86 ,  C07D233/88

    摘要： A compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --NO.sub.2 and halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is selected from the group consisting of ##STR2## X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted with a member of the group consisting of halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted with at least one member of the group consisting of oxygen, nitrogen and sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A--B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.

    摘要翻译： 式Ⅰ化合物，其中R 1选自-CN，-NO 2和卤素，R 2为-CF 3或卤素，-AB-选自下组：X为-O - 或-S-，R 3选自氢，烷基，烯基和至多12个碳原子的炔基，最多12个碳原子的芳基和芳烷基，全部任选被至少一个成员组成的基团 的至多7个碳原子的-OH，卤素，-SH，-CN，酰基和酰氧基，至多12个碳原子的芳基，-O-芳基，-O-芳烷基-S-芳基，芳基和芳烷基任选地 被卤素，-CF 3，烷基，烷氧基，烯基，烯氧基，炔基和炔氧基取代，硫任选被氧化成砜或亚砜，游离，酯化，酰胺化或成盐的羧基，-NH 2，单和 3至6个环成员的二烷基氨基和杂环基并含有至少一个选自氧，硫的杂原子 ur和氮，烷基，烯基和炔基任选地被至少一个由氧，氮和硫组成的组中任意地被氧化成亚砜或砜，具有1-6个碳原子的烷基的三烷基甲硅烷基和酰基和酰氧基 1至7个碳原子的有机羧酸，Y是-O - ， - S-或-NH-，但其中-AB-是X的化合物是氧，R 3是氢，Y是氧或-NH - ，R 2是-CF 3或卤素，R 1是-NO 2或卤素及其无毒的药学上可接受的酸加成盐。