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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。

    Mandelic hydrazides
    6.
    发明授权
    Mandelic hydrazides 失效
    扁豆酰肼

    公开(公告)号：US07776920B2

    公开(公告)日：2010-08-17

    申请号：US12279227

    申请日：2007-01-18

    申请人： Rolf Gericke ,  Markus Klein ,  Werner Mederski ,  Norbert Beier ,  Florian Lang

    发明人： Rolf Gericke ,  Markus Klein ,  Werner Mederski ,  Norbert Beier ,  Florian Lang

    IPC分类号： C07C243/38 ,  A61K31/166

    CPC分类号： C07C243/38

    摘要： Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.

    摘要翻译： 式（I）的新型扁桃酸酰肼，其中R 1 -R 11具有权利要求1所述的含义，是SGK抑制剂，可用于治疗SGK诱发的疾病和投诉，例如糖尿病，肥胖症，代谢综合征 血脂异常），全身和肺高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维和炎症过程中。

    3-Oxoindazolesquaric Acid Derivatives
    8.
    发明申请
    3-Oxoindazolesquaric Acid Derivatives 审中-公开
    3-氧代吲唑啉酸衍生物

    公开(公告)号：US20080234348A1

    公开(公告)日：2008-09-25

    申请号：US12064395

    申请日：2006-08-02

    申请人： Werner Mederski ,  Rolf Gericke ,  Markus Klein ,  Norbert Beier ,  Florian Lang

    发明人： Werner Mederski ,  Rolf Gericke ,  Markus Klein ,  Norbert Beier ,  Florian Lang

    IPC分类号： A61K31/416 ,  C07D231/54 ,  A61P3/10 ,  A61P3/04 ,  A61P35/00

    CPC分类号： C07D231/56

    摘要： Novel squaric acid compounds of the formula (I), in which R1, R2, R2′, R2″ and X have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be used for the treatment of diseases and complaints such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.

    摘要翻译： 式（I）的新型方酸化合物，其中R 1，R 2，R 2，R 2， / SUP>“，X具有权利要求1所述的含义，是CHK1 CHK2和SGK激酶的抑制剂，可用于治疗疾病和投诉，例如癌症，糖尿病，肥胖症，代谢综合征（血脂异常），全身和 肺高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维和炎症过程中。

    ACYLHYDRAZONE DERIVATIVES AND THE USE THEREOF IN THE INHIBITION, REGULATION AND/OR MODULATION OF KINASE SIGNAL TRANSDUCTION
    10.
    发明申请
    ACYLHYDRAZONE DERIVATIVES AND THE USE THEREOF IN THE INHIBITION, REGULATION AND/OR MODULATION OF KINASE SIGNAL TRANSDUCTION 审中-公开
    ACYLHYDRAZONE衍生物及其在抑制，调节和/或调节激酶信号转导中的用途

    公开(公告)号：US20080214674A1

    公开(公告)日：2008-09-04

    申请号：US12100987

    申请日：2008-04-10

    申请人： Rolf Gericke ,  Norbert Beier ,  Oliver Poeschke ,  Lars Burgdorf ,  Helga Drosdat ,  Florian Lang

    发明人： Rolf Gericke ,  Norbert Beier ,  Oliver Poeschke ,  Lars Burgdorf ,  Helga Drosdat ,  Florian Lang

    IPC分类号： A61K31/165 ,  C07C251/86 ,  A61P3/10 ,  A61P3/04 ,  A61P9/00 ,  A61P35/00

    CPC分类号： C07C251/86

    摘要： Acylhydrazone derivatives of the formula (I) are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in any type of fibrosis and inflammatory process. In which R1, R5 each, independently of one another, H, OH, OA, OAc or methyl, R2, R3, R4, R6, R7, R8, R9, R10 each, independently of one another, H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2 or COOH, R11H or CH3, A alkyl having 1, 2, 3 or 4 C atoms, X CH2, CH2CH2, OCH2 or —CH(OH)—, Hal F, Cl, Br or I.

    摘要翻译： 式（I）的酰腙衍生物是SGK抑制剂，可用于治疗SGK诱发的疾病和病症，例如糖尿病，肥胖，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 在任何类型的纤维化和炎症过程。 其中R 1，R 5各自独立地为H，OH，OA，OAc或甲基，R 2，R 2， R 4，R 4，R 6，R 7，R 8，R 8， 各自独立地为H，OH，OA，OAc，OCF 3，Hal，NO 2， / SUB>，CF 3，A，CN，OSO 2，CH 3，SO 2，CH 2， 3，NH 2或COOH，R 11 H或CH 3，具有1,2,3或4个碳原子的烷基 原子，X CH 2，CH 2 CH 2，OCH 2或-CH（OH） - ，Hal F，Cl，Br或I.