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29 条记录 (耗时 0.021 秒)

    Novel 4-alkylthio-steroids
    1.
    发明授权
    Novel 4-alkylthio-steroids 失效
    新型4-烷硫基类固醇

    公开(公告)号：US4988684A

    公开(公告)日：1991-01-29

    申请号：US454697

    申请日：1989-12-21

    申请人： Jean-Francois Gourvest ,  Dominique Lesuisse ,  Daniel Philibert ,  Jean P. Vevert

    发明人： Jean-Francois Gourvest ,  Dominique Lesuisse ,  Daniel Philibert ,  Jean P. Vevert

    IPC分类号： A61K31/565 ,  A61K31/00 ,  A61P5/00 ,  A61P5/32 ,  A61P35/00 ,  C07J1/00 ,  C07J31/00 ,  C07J41/00 ,  C07J71/00

    CPC分类号： C07J41/0038 ,  C07J31/003 ,  C07J41/0094 ,  C07J71/001

    摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 6 carbon atoms unsubstituted or substituted with at least one member of the group consisting of alkoxy and alkylthio of 1 to 4 carbon atoms, --NO.sub.2, --CN and halogen, X and Y together are .dbd.O or Y is hydrogen and X is --OH, etherified --OH or esterified --OH, the dotted lines in the 1(2), 6(7) and 9(11) positions indicate a possible double bond with the proviso that R.sub.1 is alkyl of 1 to 6 carbon atoms when X and Y are .dbd.O and there is a double bond in at least one of the 1(2), 6(7) and 9(11) positions having aromatase inhibiting activity.

    摘要翻译： 式（I）的化合物，其中R选自1至4个碳原子的烷基和2至4个碳原子的烯基和炔基，R 1是未取代或取代的1至6个碳原子的烷基 与至少一个由1-4个碳原子的烷氧基和烷硫基组成的组，-NO 2，-CN和卤素，X和Y一起为= O或Y为氢，X为-OH，醚化-OH或酯化 -OH，1（2），6（7）和9（11）位中的虚线表示可能的双键，条件是当X和Y为O时，R 1为1至6个碳原子的烷基， 在具有芳香酶抑制活性的1（2），6（7）和9（11）位中的至少一个中是双键。

    Steroids
    4.
    发明授权
    Steroids 失效
    STEROIDS

    公开(公告)号：US5081114A

    公开(公告)日：1992-01-14

    申请号：US633288

    申请日：1990-12-24

    申请人： Jean-Francois Gourvest ,  Dominique Lesuisse

    发明人： Jean-Francois Gourvest ,  Dominique Lesuisse

    IPC分类号： A61K31/565 ,  A61P35/00 ,  A61P43/00 ,  C07J1/00 ,  C07J41/00

    CPC分类号： C07J1/0011 ,  C07J41/0038

    摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, ##STR2## alkyl and alkoxy of 1 to 12 carbon atoms, aryl and aryloxy of 6 to 12 carbon atoms and aralkyl and aralkoxy of 7 to 12 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms or taken together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocycle optionally containing a second heteroatom of --S--, --O-- or --N--, R.sub.A is selected from the group consisting of hydrogen, halogen, --OH, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, --NH.sub.2, mono- and dialkylamino of 1 to 6 alkyl carbon atoms, carbamoyl and alkoxy carbamoyl of up to 7 carbon atoms, X is --O-- or ##STR3## R.sub.17 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms and the dotted lines at 1(2) and 6(7) indicates an optional double bond, with the proviso that R.sub.A is not hydrogen when R is alkoxy, aryloxy or aralkoxy having aromatic specific activity useful in treating cancers.

    摘要翻译： 式I的化合物，其中R选自氢，1〜12个碳原子的烷基和烷氧基，6-12个碳原子的芳基和芳氧基以及7-12个碳原子的芳烷基和芳烷氧基 碳原子，R 1和R 2分别是1至6个碳原子的烷基或与它们所连接的氮原子一起形成5或6元杂环，任选地含有-S + 13，-O-或 - N-，RA选自氢，卤素，-OH，烷基，烷硫基和1至6个碳原子的烷氧基，-NH 2，1至6个烷基碳原子的一烷基氨基和二烷基氨基，氨基甲酰基和烷氧基氨基甲酰基 最多7个碳原子，X是-O-或者R 17选自氢，1至12个碳原子的烷基和1至12个碳原子的有机羧酸的酰基，虚线在 1（2）和6（7）表示任选的双键，条件是当R是烷氧基时，RA不是氢，芳基 具有芳族比活性的氧或芳烷氧基可用于治疗癌症。

    Novel steroids
    5.
    发明授权
    Novel steroids 失效
    新的STEROIDS

    公开(公告)号：US5086047A

    公开(公告)日：1992-02-04

    申请号：US633291

    申请日：1990-12-24

    申请人： Jean-Francois Gourvest ,  Dominique Lesuisse

    发明人： Jean-Francois Gourvest ,  Dominique Lesuisse

    IPC分类号： A61K31/565 ,  A61P5/32 ,  A61P43/00 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00

    CPC分类号： C07J41/0038 ,  C07J21/00 ,  C07J31/006 ,  C07J41/0016

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.2 and ##STR6## q is an integer from 1 to 3, Rc is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, R" is hydrogen or acyl W is selected from the group consisting of hydrogen, optionally substituted alkyl and alkylthio of 1 to 6 carbon atoms and optionally substituted arylthio of 6 to 10 carbon atoms, Z is hydrogen or alkyl of 1 to 10 carbon atoms, n is an integer from 0 to 2, the dotted lines in 1(2)-, 4(5)- and 6(7)-position indicate an optional double bond between the carbon atoms and their non-toxic, pharmaceutically acceptable salts having aromatase specific activity.

    摘要翻译： 选自下列化合物的化合物：其中R选自氢，烷基，烷硫基和1至6个碳原子的卤代烷基，其中R 2为2至6个碳的链烯基和炔基 6至10个碳原子的任选取代的芳硫基，6至12个碳原子的芳基，1至12个碳原子的有机羧酸的酰基，-CN，3至6个碳原子的环烷基和 - （CH 2）m - Re，m是1至3的整数，Re是-OH或-SH或-Salk，Alk是1至6个碳原子的烷基，X选自氧，NO-R1，或 = X是H 2或RA，RB分别选自氢，卤素和1至6个碳原子的烷基，R 1是氢或1至6个碳的烷基，R'是氢或酰基， 波浪线表示 - 或 - 位，Y选自氧，NOR，或= Y为 H2， q为1至3的整数，Rc选自t 由氢，碳原子数为1〜6的烷基，碳原子数为2〜6的烯基和炔基组成的基团，R“为氢或酰基W选自氢，任意取代的烷基和1〜6的烷硫基 碳原子和任选取代的6至10个碳原子的芳硫基，Z是氢或1-10个碳原子的烷基，n是0-2的整数，1（2） - ，4（5） - 和 6（7） - 表示碳原子与其具有芳香族化合物比活性的无毒的药学上可接受的盐之间的任选双键。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    7.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
    氨基吲唑衍生物作为药物和药物组合物，包括它们

    公开(公告)号：US07166629B2

    公开(公告)日：2007-01-23

    申请号：US10654703

    申请日：2003-09-04

    申请人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    发明人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    摘要： The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C)cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译： 本发明涉及通式（I）的新型衍生物，其中R3是（1-6C）烷基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，芳基或杂芳基 （1-10C）环烷基，杂环，杂环烷基，环烷基，金刚烷基，多环烷基，烯基，炔基，CONR1R2，COOR1，SO2R1，C（-NH）R1或C（-NH）NR1 激进; R 5和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8， -OC（O）R8，NR8R9，NHC（O）R8，C（O）NR8R9，NHC（S）R8，C（S）NR8R9，SR8，S（O） R 8，NHSO 2 R 8，SO 2 NR 8 R 9，-O-SO 2 R 8，-SO 2 -O （1-6C）烷氧基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，杂环，环烷基，链烯基，炔基，金刚烷基 或多环烷基。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    10.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 失效
    氨基吲唑衍生物作为药物和药物组合物，包括它们

    公开(公告)号：US07407981B2

    公开(公告)日：2008-08-05

    申请号：US11683452

    申请日：2007-03-08

    申请人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney ,  Gilles Tiraboschi

    发明人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney ,  Gilles Tiraboschi

    IPC分类号： A61K31/415 ,  C07D231/00

    CPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D403/12 ,  C07D405/12

    摘要： The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.

    摘要翻译： 本发明涉及通式（I）的新型衍生物，其中R3是（1-6C）烷基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，芳基或 与（1-10C）环烷基，杂环，杂环烷基，环烷基，金刚烷基，多环烷基，烯基，炔基，CONR1R2，COOR1，SO2R1，C（-NH）R1或C（ - NH）NR1基; R 5，R 6和R 7彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，OR 8，COOH，C（ O）OR 8，-OC（O）R 8，NR 8 R 9，NHC（O）R 8，C（O）NR 8 R 9，NHC（S）R 8，C（S）NR 8 R 9，SR 8，S（O）R 8，SO 2 R 8，NHSO 2 R 8，SO 2 NR 8 R 9，-O-SO 2 R 8，-SO 2， （1-6C）烷氧基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，杂环，环烷基，烯基 ，炔基，金刚烷基或多环烷基，以治疗选自以下的疾病：神经变性疾病，中风，颅脑和脊髓创伤和周围神经病变，肥胖症，代谢疾病，II型糖尿病，原发性高血压，动脉粥样硬化心血管疾病，多囊卵巢综合征 ，综合征X，免疫缺陷和癌症。