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    Phenylimidazolidines containing nitrooxy or carbonyloxy groups
    4.
    发明授权
    Phenylimidazolidines containing nitrooxy or carbonyloxy groups 失效
    含有硝基氧基或羰基氧基的苯基咪唑烷

    公开(公告)号：US06242611B1

    公开(公告)日：2001-06-05

    申请号：US09101027

    申请日：1998-09-28

    申请人： Andre Claussner ,  Francois Goubet ,  Jean-Georges Teutsch

    发明人： Andre Claussner ,  Francois Goubet ,  Jean-Georges Teutsch

    IPC分类号： C07D23372

    CPC分类号： C07D233/78

    摘要： A subject of the invention is the products of formula (I): in which: R1 and R2 represent in particular cyano and trifluoromethyl, R3 represents in particular alkyl, alkenyl or alkynyl, substituted in particular by nitrooxy or carbonyloxy, R4 and R5 represent in particular methyl optionally substituted by fluorine, X and Y represent in particular oxygen, as well as their salts and isomers.

    摘要翻译： 本发明的主题是式（I）的产物：其中：R 1和R 2特别表示氰基和三氟甲基，R 3特别表示烷基，烯基或炔基，特别被硝基氧基或羰氧基取代，R 4和R 5表示 任选被氟取代的特定甲基，X和Y特别表示氧，以及它们的盐和异构体。

    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
    8.
    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。

    Phenylimidazolidines having antiandrogenic activity
    9.
    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。

    Steroids, their use as medicaments, their preparation process, the intermediates of this process and the compositions containing them
    10.
    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。