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    Sulfonamides and their use as a medicament
    1.
    发明授权
    Sulfonamides and their use as a medicament 失效
    磺酰胺及其作为药物的用途

    公开(公告)号：US08088772B2

    公开(公告)日：2012-01-03

    申请号：US12517691

    申请日：2007-12-11

    申请人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Frank Jaschinski ,  Guy Lemaillet ,  Cornelia Marty-Ernst ,  Elena Marzi ,  Leonardo Scapozza

    发明人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Frank Jaschinski ,  Guy Lemaillet ,  Cornelia Marty-Ernst ,  Elena Marzi ,  Leonardo Scapozza

    IPC分类号： A61K31/5375 ,  A61K31/44 ,  A61K31/415 ,  A61K31/18 ,  C07D295/00 ,  C07D231/10 ,  C07D213/00 ,  C07D309/00

    CPC分类号： C07C311/38 ,  C07C311/21 ,  C07D207/335 ,  C07D209/40 ,  C07D213/24 ,  C07D213/53 ,  C07D215/12 ,  C07D217/12 ,  C07D231/12 ,  C07D233/64 ,  C07D271/12 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D333/58

    摘要： The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of —NH—NH—, —NH—NH—CH2—, ethinyl, —NH—C(O)—CH2—, —NH—NH—SO2—, —C(O)—NH—CH2—, —NH—N═CH—, —NH—N═C(Me)-, a —NH—N═CH— motif being part of a heterocyclic system, preferably a substituted or unsubstituted pyrazole or pyridazine system, and pharmaceutically active salts thereof. Further, the invention relates to the use of these compounds as a medicament, especially for the treatment of cancer.

    摘要翻译： 本发明涉及式（I）的磺酰胺化合物的用途：其中R 1选自H，CN，卤素，三氟甲基，甲基，乙基，羟基，甲氧基，乙氧基，吗啉代，R2选自 其中R为苯基或吗啉代，-NC（O）Me，-NC（O）Et，-CH2C（O）OMe，CH2C（O）OEt，R3选自 由H，NO 2，NH 2，卤素，-COOMe，-COOEt，RC（O）N-，吗啉代，R 4选自H，支链或非支链的甲基，乙基，丙基，丁基，戊基 乙氧基，丙氧基，丁氧基，取代或未取代的苯基，炔基，Me2SO2-，COOR，其中R是支链或非支链的甲基，乙基，丙基，丁基，戊基，-MeOC（O） - ，取代或未取代的 具有一个，两个或三个杂原子的五或六元芳族或非芳族杂环体系，杂芳基系统，稠合苯并杂环系统，X是包含2或3个 选自-NH-NH-，-NH-NH-CH 2 - ，乙炔基，-NH-C（O）-CH 2 - ， - NH-NH-SO 2 - ， - C（O）-NH -CH 2 - ， - NH-N = CH - ， - NH-N = C（Me） - ，作为杂环系统的一部分的-NH-N = CH-基序，优选取代或未取代的吡唑或哒嗪系统， 其药学活性盐。 此外，本发明涉及这些化合物作为药物，特别是用于治疗癌症的用途。

    AROMATIC 1,4-DI-CARBOXYLAMIDES AND THEIR USE
    2.
    发明申请
    AROMATIC 1,4-DI-CARBOXYLAMIDES AND THEIR USE 审中-公开
    芳香1,4-二羧酸酯及其用途

    公开(公告)号：US20100204219A1

    公开(公告)日：2010-08-12

    申请号：US12517680

    申请日：2007-12-11

    申请人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Guy Lemaillet ,  Leonardo Scapozza

    发明人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Guy Lemaillet ,  Leonardo Scapozza

    IPC分类号： A61K31/5377 ,  C07D213/81 ,  A61K31/44 ,  C07D405/14 ,  A61K31/4709 ,  C07D409/14 ,  A61K31/4436 ,  C07D417/14 ,  A61K31/4439 ,  C07D413/14 ,  C07D239/26 ,  A61K31/505 ,  A61P35/00 ,  A61P19/02 ,  A61P37/06

    CPC分类号： C07D401/14 ,  C07D233/96 ,  C07D407/12

    摘要： The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R1, R2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C1-C3 alkyl group and a C1-C3 alkoxy group, R3 represents, independently from one another if p is not 0, hydrogen, halogen, a C1-C5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C1-C4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C1-C3 alkyl, a hydroxyl or a benzyl group, a C1-C6 alkylsulfonyl, a mono or disubstituted C1-C5 alkyl group, a branched or a cyclic amine, R6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF3 or a branched or unbranched C1-C4 alkyl group, if m=1 then C represents —CH2—O—, —CH2—, —CH2CH2—, —CH2CH2CH2—, —CH2(CH2)CH2— or denotes a chemical bond between N—C or C—C, the CONR6 group may be linked to C either via its carbon or via its nitrogen atom, CYC stands for a by R3 substituted or unsubstituted phenyl, pyridinyl, naphthyl, quinolinyl, isoquinolinyl, isoxaxolinyl, thiophenyl, 1,3,4-thiadiazazolidinyl, furanyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, morpholinyl, furanyl, cyclohexenyl, and chromen-2-on-yl and its use as a medicament for the treatment of cancer.

    摘要翻译： 本发明涉及新的式（I）化合物，其中X，Y，Z彼此独立地表示C或N，n表示1,2,3，m为0或1，p表示0或1的整数 至6，R 1，R 2彼此独立地表示氢，卤素原子，羟基，C 1 -C 3烷基和C 1 -C 3烷氧基，如果p不为0，则R 3彼此独立地表示氢， 卤素，C1-C5直链或支链烷基，羧基，甲酯基，碳乙氧基，苄基，酰基，羟基，C1-C4直链或支链烷氧基，三氟甲基，氰基，吗啉代，1,3 N-乙酰氨基或酰胺基，饱和5-8元环，任选被C 1 -C 3烷基，羟基或苄基取代的杂环，C 1 -C 6烷基磺酰基，单取代或双取代 C1-C5烷基，支链或环状胺，R6是H或脂环族杂脂环系的一部分，如果m为0，则C代表CF 3或支链或非支链C 1-C4烷基，如果m = 1，则C代表-CH 2 -O - ， - CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - ， - CH 2（CH 2）CH 2 - 或表示N-C或C- C，CONR 6基团可以通过其碳或通过其氮原子与C连接，CYC代表R3取代或未取代的苯基，吡啶基，萘基，喹啉基，异喹啉基，异恶唑啉基，噻吩基，1,3,4-噻二唑烷基 ，呋喃基，四氢喹啉基，四氢异喹啉基，吗啉基，呋喃基，环己烯基和色烯-2-酮及其作为治疗癌症的药物的用途。

    SULFONAMIDES AND THEIR USE AS A MEDICAMENT
    3.
    发明申请
    SULFONAMIDES AND THEIR USE AS A MEDICAMENT 失效
    磺酰胺及其作为药物使用

    公开(公告)号：US20100249135A1

    公开(公告)日：2010-09-30

    申请号：US12517691

    申请日：2007-12-11

    申请人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Jaschinskin Frank ,  Guy Lemaillet ,  Cornelia Marty-Ernest ,  Elena Marzi ,  Leonardo Scapozza

    发明人： Gabriel Garcia ,  Pierre Daram ,  Barbara Froesch ,  Jaschinskin Frank ,  Guy Lemaillet ,  Cornelia Marty-Ernest ,  Elena Marzi ,  Leonardo Scapozza

    IPC分类号： A61K31/5375 ,  A61P35/00 ,  C07C311/21 ,  A61K31/18 ,  C07D231/12 ,  A61K31/415 ,  C07D213/32 ,  A61K31/4406 ,  C07D265/30 ,  A61K31/44

    CPC分类号： C07C311/38 ,  C07C311/21 ,  C07D207/335 ,  C07D209/40 ,  C07D213/24 ,  C07D213/53 ,  C07D215/12 ,  C07D217/12 ,  C07D231/12 ,  C07D233/64 ,  C07D271/12 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D333/58

    摘要： The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of —NH—NH—, —NH—NH—CH2-, ethinyl, —NH—C(O)—CH2—, —NH—NH—SO2—, —C(O)—NH—CH2—, —NH—N═CH—, —NH—N═C(Me)-, a —NH—N═CH— motif being part of a heterocyclic system, preferably a substituted or unsubstituted pyrazole or pyridazine system, and pharmaceutically active salts thereof. Further, the invention relates to the use of these compounds as a medicament, especially for the treatment of cancer.

    摘要翻译： 本发明涉及式（I）的磺酰胺化合物的用途：其中R 1选自H，CN，卤素，三氟甲基，甲基，乙基，羟基，甲氧基，乙氧基，吗啉代，R2选自 其中R为苯基或吗啉代，-NC（O）Me，-NC（O）Et，-CH2C（O）OMe，CH2C（O）OEt，R3选自 由H，NO 2，NH 2，卤素，-COOMe，-COOEt，RC（O）N-，吗啉代，R 4选自H，支链或非支链的甲基，乙基，丙基，丁基，戊基 乙氧基，丙氧基，丁氧基，取代或未取代的苯基，炔基，Me2SO2-，COOR，其中R是支链或非支链的甲基，乙基，丙基，丁基，戊基，-MeOC（O） - ，取代或未取代的 具有一个，两个或三个杂原子的五或六元芳族或非芳族杂环体系，杂芳基系统，稠合苯并杂环系统，X是包含2或3个 选自-NH-NH-，-NH-NH-CH 2 - ，乙炔基，-NH-C（O）-CH 2 - ， - NH-NH-SO 2 - ， - C（O）-NH -CH 2 - ， - NH-N = CH - ， - NH-N = C（Me） - ，作为杂环系统的一部分的-NH-N = CH-基序，优选取代或未取代的吡唑或哒嗪系统， 其药学活性盐。 此外，本发明涉及这些化合物作为药物，特别是用于治疗癌症的用途。

    Essential downstream component of the wingless signaling pathway and therapeutic and diagnostic applications based thereon
    7.
    发明授权
    Essential downstream component of the wingless signaling pathway and therapeutic and diagnostic applications based thereon 失效
    基于其的无翼信号传导途径的基本下游部分和治疗和诊断应用

    公开(公告)号：US07252951B2

    公开(公告)日：2007-08-07

    申请号：US10322579

    申请日：2002-12-19

    申请人： Konrad Basler ,  Erich Brunner ,  Barbara Froesch ,  Thomas Kramps ,  Oliver Peter

    发明人： Konrad Basler ,  Erich Brunner ,  Barbara Froesch ,  Thomas Kramps ,  Oliver Peter

    IPC分类号： G01N33/53 ,  G01N33/543

    CPC分类号： C12N15/113 ,  C07K14/43581 ,  C07K14/4702 ,  C12N2310/14 ,  C12N2310/53

    摘要： The present invention relates to a new essential downstream component of the Wnt/Wingless (Wnt/Wg) signaling pathway and therapeutic and diagnostic applications based thereon. The invention relates to nucleotide sequences of the Drosophila melanogaster legless (lgs) gene, of its encoded proteins, as well as derivatives (e.g., fragments) and analogues thereof. The invention further includes vertebrate and invertebrate homologues of the Lgs protein, comprising proteins that contain a contiguous stretch of amino acids with similarity to the Drosophila lgs gene. The invention further relates to the function of the Drosophila and the human Lgs proteins. Methods for producing the Lgs proteins, derivatives and analogs, e.g., by recombinant means and antibodies to Lgs are provided by the present invention. In addition, the invention also relates to the therapeutic and diagnostic methods and compositions based on Lgs proteins and nucleic acids or fragments thereof.

    摘要翻译： 本发明涉及Wnt / Wingless（Wnt / Wg）信号传导途径的新的基本下游组分以及其上的治疗和诊断应用。 本发明涉及黑腹果蝇无基因（lgs）基因，其编码的蛋白质以及衍生物（例如片段）及其类似物的核苷酸序列。 本发明还包括Lgs蛋白质的脊椎动物和无脊椎动物同系物，其包含与果蝇lgs基因具有相似性的氨基酸的连续片段的蛋白质。 本发明还涉及果蝇和人Lgs蛋白的功能。 通过本发明提供了通过重组方法和Lgs的抗体产生Lgs蛋白质，衍生物和类似物的方法。 此外，本发明还涉及基于Lgs蛋白质和核酸或其片段的治疗和诊断方法和组合物。