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    SGK1 INHIBITORS FOR THE PROPHYLAXIS AND/OR THERAPY OF VIRAL DISEASES AND/OR CARCINOMAS
    2.
    发明申请
    SGK1 INHIBITORS FOR THE PROPHYLAXIS AND/OR THERAPY OF VIRAL DISEASES AND/OR CARCINOMAS 有权

    公开(公告)号：US20110060050A1

    公开(公告)日：2011-03-10

    申请号：US12867963

    申请日：2009-02-17

    申请人： Thomas Fuchss ,  Rolf Gericke ,  Norbert Beier ,  Florian Lang ,  Phillipp Lang ,  Karl Lang

    发明人： Thomas Fuchss ,  Rolf Gericke ,  Norbert Beier ,  Florian Lang ,  Phillipp Lang ,  Karl Lang

    IPC分类号： A61K31/166 ,  C07C243/38 ,  A61P31/12 ,  A61P35/00

    CPC分类号： C07C243/38

    摘要： The present invention relates to a compound of the formula I, Ia and Ib, and its pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios. The present invention furthermore also relates to compounds of the formula II for the prophylaxis and/or treatment of viral diseases and/or carcinomas, in which R1, R2 each, independently of one another, denote H, CHO or acetyl, R3, R4, R5, R6, R7, R8, R9, R10, R11 each, independently of one another, denote H, A, OSO2A, Hal, NO2, OR12, N(R12)2, CN, O—COA, —[C(R12)2]nCOOR12, O—[C(R12)2]oCOOR12, SO3H, —[C(R12)2]nAr, —CO—Ar, O—[C(R12)2]nAr, —[C(R12)2]nHet, —[C(R12)2]nC≡CH, O—[C(R12)2]nC≡CH, —[C(R12)2]nCON(R12)2, —[C(R12)2]nCONR12N(R12)2, O—[C(R12)2]nCON(R12)2, O—[C(R12)2]oCONR12N(R12)2, NR12COA, NR12CON(R12)2, NR12SO2A, N(SO2A)2, COR12, S(O)mAr, SO2NR12 or S(O)mA, R3 and R4 together also denote CH═CH—CH═CH, R3 and R4, R7 and R8 or R8 and R9 together also denote alkylene having 3, 4 or 5 C atoms, in which one or two CH2 groups may be replaced by oxygen, A denotes unbranched or branched alkyl having 1-6 C atoms, in which 1-7 H atoms may be replaced by F, or cyclic alkyl having 3-7 C atoms, Ar denotes phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR12, N(R12)2, NO2, CN, phenyl, CON(R12)2, NR12COA, NR12CON(R12)2, NR12SO2A, COR12, SO2N(R12)2, S(O)mA, —[C(R12)2]n—COOR12 and/or —O[C(R12)2]o—COOR12, Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be mono-, di- or trisubstituted by Hal, A; OR12, N(R12)2, NO2, CN, COOR12, CON(R12)2, NR12COA, NR12SO2A, COR12, SO2NR12, S(O)mA, ═S, ═NR12 and/or ═O (carbonyl oxygen), R12 denotes H or A, Ha1 denotes F, Cl, Br or I, m denotes O, 1 or 2, n denotes O, 1, 2 or 3, o denotes 1, 2 or 3, for the prophylaxis and/or treatment of viral diseases and/or carcinomas, and their pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios.

    Difluorophenyldiacylhydrazide derivatives
    4.
    发明授权
    Difluorophenyldiacylhydrazide derivatives 有权
    二氟苯基二酰肼衍生物

    公开(公告)号：US08492440B2

    公开(公告)日：2013-07-23

    申请号：US13131233

    申请日：2009-11-02

    申请人： Thomas Fuchss ,  Ulrich Graedler ,  Norbert Beier ,  Rolf Gericke ,  Florian Lang

    发明人： Thomas Fuchss ,  Ulrich Graedler ,  Norbert Beier ,  Rolf Gericke ,  Florian Lang

    IPC分类号： A61K31/16 ,  C07C241/00

    CPC分类号： C07C243/38 ,  A61K31/15 ,  A61K45/06 ,  A61K2300/00

    摘要： Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseases.

    摘要翻译： 式Ⅰ的新型二氟苯基二酰肼衍生物，其中R1，R2，R3，R4，R5，R6和R7具有权利要求1所述的含义，是激酶抑制剂，可用于治疗诸如糖尿病，肥胖症 ，代谢综合征（血脂异常），全身和肺性高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维，炎症过程，肿瘤和肿瘤疾病中。

    Aminopyridine-derivatives as inductible no-synthase inhibitors
    7.
    发明申请
    Aminopyridine-derivatives as inductible no-synthase inhibitors 失效
    氨基吡啶衍生物作为可诱导的无合酶抑制剂

    公开(公告)号：US20070043072A1

    公开(公告)日：2007-02-22

    申请号：US10573204

    申请日：2004-09-30

    申请人： Thomas Fuchss

    发明人： Thomas Fuchss

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： The compounds of Formula (I) in which R1, R2, R3 and R4 have the meanings as given in the description are novel effective iNOS inhibitors.

    摘要翻译： 其中R1，R2，R3和R4具有本说明书中给出的含义的式（I）化合物是新的有效的iNOS抑制剂。

    Imidazo[4,5-c]quinolines as DNA-PK inhibitors
    8.
    发明授权
    Imidazo[4,5-c]quinolines as DNA-PK inhibitors 有权
    咪唑并[4,5-c]喹啉作为DNA-PK抑制剂

    公开(公告)号：US09000153B2

    公开(公告)日：2015-04-07

    申请号：US13819488

    申请日：2011-07-26

    申请人： Thomas Fuchss ,  Werner Mederski ,  Frank Zenke

    发明人： Thomas Fuchss ,  Werner Mederski ,  Frank Zenke

    IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/4745 ,  A61K45/06 ,  C07D215/42 ,  C07D215/46

    CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C12N9/12 ,  C12Y207/11001 ,  A61K2300/00

    摘要： The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).

    摘要翻译： 本发明涉及式（I）和（II）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 8，X和m具有权利要求中所示的含义，和/或生理上可接受的盐，互变异构体和立体异构体 包括其所有比例的混合物。 式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。 本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。 本发明还涉及制备式（I）化合物的方法。

    Pyrazoloquinolines
    9.
    发明授权
    Pyrazoloquinolines 有权
    吡唑并喹啉

    公开(公告)号：US08802712B2

    公开(公告)日：2014-08-12

    申请号：US13807954

    申请日：2011-06-24

    申请人： Thomas Fuchss ,  Werner Mederski ,  Frank Zenke

    发明人： Thomas Fuchss ,  Werner Mederski ,  Frank Zenke

    IPC分类号： A01N43/56 ,  A61K31/415 ,  A01N43/42 ,  A61K31/44 ,  A61K31/535 ,  A61K31/497 ,  C07D401/00 ,  C07D471/00 ,  C07D491/00 ,  C07D498/00 ,  C07D513/00 ,  C07D515/00

    CPC分类号： C07D471/04 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/18 ,  C07D215/38 ,  C07D519/00 ,  C12N9/99 ,  A61K2300/00

    摘要： The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts

    摘要翻译： 本发明涉及式（I），（II）和（III）的化合物，和/或其生理上可接受的盐，互变异构体和立体异构体，包括其所有比例的混合物。 式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。 本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。 本发明还涉及通过式（II）或（III）化合物与式（I）化合物的碱或酸的任意转化来制备式（I）化合物的方法， 成为其中一种盐