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    Chroman derivatives
    13.
    发明授权
    Chroman derivatives 失效
    色原衍生物

    公开(公告)号：US5232944A

    公开(公告)日：1993-08-03

    申请号：US870749

    申请日：1992-04-20

    申请人： Rolf Gericke ,  Manfred Baumgarth ,  Ingeborg Lues ,  Jacques De Peyer ,  Rolf Bergmann

    发明人： Rolf Gericke ,  Manfred Baumgarth ,  Ingeborg Lues ,  Jacques De Peyer ,  Rolf Bergmann

    IPC分类号： C07D311/22 ,  C07D311/68 ,  C07D407/12 ,  C07D409/12

    CPC分类号： C07D407/12 ,  C07D311/22 ,  C07D311/68 ,  C07D409/12

    摘要： Novel chroman derivatives of the formula I ##STR1## in which X is O or NR.sup.11,Z is CH.sub.2, O, S or CHHal,R.sup.1 and R.sup.5 are each A,R.sup.2 is H or A,R.sup.1 and R.sup.2 together are also alkylene having 3-6 C atoms,R.sup.3 is OH or OAc,R.sup.4 is H,R.sup.3 and R.sup.4 together are also a bond,R.sup.6 and R.sup.7 are each H, A, HO, AO, CHO, ACO, ACS, HOOC, AOOC, AO--CS, ACOO, A--CS--O, hydroxyalkyl, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, ASO, ASO.sub.2, AO--SO, AO--SO.sub.2, AcNH, AO--CO--NH, H.sub.2 NSO, HANSO, A.sub.2 NSO, H.sub.2 NSO.sub.2, HANSO.sub.2, A.sub.2 NSO.sub.2, H.sub.2 NCO, HANCO, A.sub.2 NCO, H.sub.2 NCS, HANCS, A.sub.2 NCS, ASONH, ASO.sub.2 NH, AOSONH, AOSO.sub.2 NH, ACO-alkyl, nitro-alkyl, cyanoalkyl, A--C(.dbd.NOH) or A--C(.dbd.NNH.sub.2),R.sup.8 and R.sup.9 are each H or A or together are .dbd.O or .dbd.S,R.sup.10 is H, Hal, CHO or CH.sub.2 OH,R.sup.11 is H, A, Ac or CH.sub.2 OH,m is 1, 2 or 3,Hal is F, Cl, Br or I,A is alkyl having 1-6 C atoms,-alkyl is alkylene having 1-6 C atoms andAc is alkanoyl having 1-8 C atoms or aroyl having 7-11 C atoms,and their salts show effects on the cardiovascular system.

    摘要翻译： 式I 的新型色满衍生物，其中X为O或NR11，Z为CH2，O，S或CHHal，R1和R5各自为A，R2为H或A，R1和R2一起也为3 -6个C原子，R3是OH或OAc，R4是H，R3和R4同时也是键，R6和R7分别是H，A，HO，AO，CHO，ACO，ACS，HOOC，AOOC，AO-CS ，ACOO，A-CS-O，羟烷基，NO2，NH2，NHA，NA2，CN，F，Cl，Br，I，CF3，ASO，ASO2，AO-SO，AO-SO2，AcNH，AO-CO-NH ，H2NSO，HANSO2，A2NSO，H2NCO，HANCO，A2NCO，H2NCS，HANCO，A2NCS，H2NCS，HANCS，A2NCS，ASONH，ASO2NH，AOSONH，AOSO2NH，ACO-烷基，硝基 - 烷基，氰基烷基，AC（= NOH） （= NNH 2），R 8和R 9各自为H或A或一起为= O或= S，R 10为H，Hal，CHO或CH 2 OH，R 11为H，A，Ac或CH 2 OH，m为1,2或3， Hal是F，Cl，Br或I，A是具有1-6个C原子的烷基， - 烷基是具有1-6个C原子的亚烷基，Ac是具有1-8个C原子的烷酰基或具有7-11个C原子的芳酰基，以及 它们的盐显示对心血管系统的影响。

    Synthesis of chroman derivatives
    15.
    发明授权
    Synthesis of chroman derivatives 失效
    色氨酸衍生物的合成

    公开(公告)号：US5112972A

    公开(公告)日：1992-05-12

    申请号：US531490

    申请日：1990-05-31

    申请人： Rolf Gericke ,  Manfred Baumgarth ,  Ingeborg Lues ,  Rolf Bergmann ,  De Peyer

    发明人： Rolf Gericke ,  Manfred Baumgarth ,  Ingeborg Lues ,  Rolf Bergmann ,  De Peyer

    IPC分类号： A61K31/44 ,  A61K31/50 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D405/12

    CPC分类号： C07D405/12

    摘要： The invention relates to new chroman derivatives of the formula I ##STR1## in which R.sup.1 is A,R.sup.2 and R.sup.8 are each H or A,R.sup.1 and R.sup.2 together are also alkylene with 3-6 C atoms,R.sup.3 is OH, OA or OAc,R.sup.4 is H,R.sup.3 and R.sup.4 together are also a bond,R.sup.5 is Ar or C.sub.n H.sub.2n -R.sup.9,R.sup.9 is alkenyl or alkynyl with 2-4 C atoms in each case, OH, OA, CHO, CO-A, CS-A, COOH, COOA, COO-alkyl-Ar, CS-OA, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, SA, SO-A, SO.sub.2 -A or Ar,Ar is a phenyl group which is unsubstituted or substituted once or twice by R.sup.10, R.sup.6, R.sup.7 and R.sup.10 are each H, A, HO, AO, CHO, ACO, CF.sub.3 CO, ACS, HOOC, AOOC, AO-CS, ACOO, A-CS-O, hydroxy-alkyl, mercapto-alkyl, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, AS, ASO, ASO.sub.2, AO-SO, AO-SO.sub.2, AcNH, AO-CO-NH, H.sub.2 NSO, HANSO, A.sub.2 NSO, H.sub.2 NSO.sub.2, HANSO.sub.2, A.sub.2 NSO.sub.2, H.sub.2 NCO, HANCO, A.sub.2 NCO, H.sub.2 NCS, HANCS, A.sub.2 NCS, ASONH, ASO.sub.2 NH, AOSONH, AOSO.sub.2 NH, ACO-alkyl, nitro-alkyl, cyano-alkyl, A-C(.dbd.NOH), A-C(.dbd.NNH.sub.2), H.sub.2 PO.sub.3 or A.sub.2 PO.sub.3,n is 1, 2 or 3,A is alkyl with 1-6 C atoms,-alkyl is alkylene with 1-6 C atoms andAC is alkanoyl with 1-8 C atoms or aroyl with 7-11 C atoms,and the salts thereof which display effects on the cardiovascular system and can be used for the treatment or prophylaxis of heart failure, angina pectoris, high blood pressure, incontinence and alopecia.

    摘要翻译： 本发明涉及式Ⅰ的新的苯并二氢吡喃衍生物，其中R 1是A，R 2和R 8各自是H或A，R 1和R 2一起也是具有3-6个C原子的亚烷基，R 3是OH，OA或OAc R 4是H，R 3和R 4一起也是键，R 5是Ar或C n H 2n-R 9，R 9是每种情况下具有2-4个C原子的链烯基或炔基，OH，OA，CHO，CO-A，CS-A ，COOH，COOA，COO-烷基-Ar，CS-OA，NO2，NH2，NHA，NA2，CN，F，Cl，Br，I，CF3，SA，SO-A，SO2-A或Ar，Ar是 R 10，R 6，R 7和R 10未取代或取代一次或两次的苯基分别为H，A，HO，AO，CHO，ACO，CF 3 CO，ACS，HOOC，AOOC，AO-CS，ACOO，A-CS- O，羟基烷基，巯基烷基，NO2，NH2，NHA，NA2，CN，F，Cl，Br，I，CF3，AS，ASO，ASO2，AO-SO，AO-SO2，AcNH， NH，H2NSO，HANSO，A2NSO，H2NCO，HANCO2，A2NCO，H2NCS，HANCO，A2NCO，H2NCS，HANCS，A2NCS，ASONH，ASO2NH，AOSONH，AOSO2NH，ACO-烷基，硝基 - 烷基，氰基 - 烷基，AC（= NOH ），AC（= NNH 2），H 2 PO 3或A 2 PO 3，n为1,2或3，A为具有1-6个C原子的烷基， - 烷基为亚烷基 1-6个C原子，AC是具有1-8个C原子的烷酰基或7-11个C原子的芳酰基及其对心血管系统有影响的盐，可用于治疗或预防心力衰竭，心绞痛 ，高血压，失禁和脱发。

    ACYLHYDRAZONE DERIVATIVES AND THE USE THEREOF IN THE INHIBITION, REGULATION AND/OR MODULATION OF KINASE SIGNAL TRANSDUCTION
    20.
    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.