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    PROCESS FOR PREPARING SULFONYL UREAS
    1.
    发明授权
    PROCESS FOR PREPARING SULFONYL UREAS 失效

    公开(公告)号：KR790001599B1

    公开(公告)日：1979-11-16

    申请号：KR790003342

    申请日：1979-09-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： KOCH W

    IPC: C07D223/16

    Abstract: Sulfonylureas (I; R1 =H C1-6 alkyl, OR C3-8 cycloalkyl; R2= C1-6 alkyl C3-8 cycloalkyl ,or R1 and R2are forming heterocyclic compd. with nitrogen which is attached in R1 or R2 ; R3 = e.g., C1-8 alkyl C3-8 alkenyl-alkyl, or C5-8 cycloalkyl, or c7-10 endoalkylene-cycloalkyl), useful as antidiabetics, were prepd. by treating sulfonyl isocyanate (II) or sulfonylcarbamic acid derivs. (III; Z = halogen, alkoxy, aryloxy, alkylthio, amino, arylamino, l-imidazolyl, or trichloromethyl) with R3NH2

    PROCESS FOR PREPARING SULFONYL UREAS
    2.
    发明授权
    PROCESS FOR PREPARING SULFONYL UREAS 失效

    公开(公告)号：KR790001598B1

    公开(公告)日：1979-11-16

    申请号：KR750000338

    申请日：1975-02-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： KOCH W

    IPC: C07D233/16

    Abstract: Title compds. (I;R1 =H or C1-6 alkyl or C3-8 cycloalkyl group R2 = C1-6 alkyl or C3-8 cycloalkyl group, R1 ,R2 can form hetero cyclic rings with N, R3 = C1-8 alkyl, C3-8 alkenyl-alkyl or C5-8 cycloalkyl group ,Z =halogen ,alkoxy, aryloxy, or trichloromethyl group), useful as antidiabetics, were prepd. treating the sulfonamide[II with azide as R3NCO (or R3CON3) or carbamic acid deriv. of R3NHCOZ. Thus I (R1 = R2 =me, R3 = cyclohexyl) at 1μmole/kg orally in dogs decreased the plasma glucose level to 69% of controls in2hr

    Retrosteroid a ring formation
    3.
    发明授权
    Retrosteroid a ring formation 失效
    回归环形成

    公开(公告)号：US3766213A

    公开(公告)日：1973-10-16

    申请号：US3766213D

    申请日：1971-01-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： USKOKOVIC M ,  FURST A ,  KOCH W

    IPC: C07C59/205 ,  C07C59/215 ,  C07D7/26

    CPC classification number: C07C59/205 ,  C07C59/215 ,  C07C2603/16 ,  C07J15/005 ,  C07J75/005

    Abstract: A PROCESS FOR PRODUCING KNOWN RETROSTEROIDS OF THE FORMULA:

    1-R1,2-R2,3-(O=),4-R4,6-R6,7-R7,11-R11,16-R16-ANDROST-4-

    ENE WHERE C17 IS Z

    WHEREIN: R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R2 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER AKLANOYLTHIO, AND HALO; R7 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R11 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY AND LOWER ALKANOYLOXY; R16 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKOXY, LOWER ALKANOYLOXY, AND, WHEN THE 17B-SUBSTITUENT IS ACETYL OR SUBSTITUTED ACETYL, FLUORINE; Z IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF CARBONYL, (17B-HYDROXY-17-A-LOWER ALKANOIC ACID LACTONE), AND

    >C(-R17ALPHA)-R17BETA

    R17B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, LOWER ALKANOYLOXY, AND

    Y-CH2-CO-

    Y IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALO, AND HYDROXY; R17A, WHEN R17B IS HYDROXY AND LOWER ALKANOYLOXY, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALIPHATIC HYDROCARBYL, AND WHEN R17B IS

    Y-CH2-CO-

    IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN ALKYL, HYDROXY, LOWER ALKANOYLOXY, AND HALO; Q WHEN TAKEN ALONE, IS OXO; T1 WHEN TAKEN ALONE, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKALI METAL OXY AND LOWER ALKOXY; AND T1 AND Q, WHEN TAKEN TOGETHER ARE NITROLO.

    N-substituted phenylalanine derivatives
    6.
    发明授权
    N-substituted phenylalanine derivatives 失效
    N-取代的苯乙胺衍生物

    公开(公告)号：US3852338A

    公开(公告)日：1974-12-03

    申请号：US19148671

    申请日：1971-10-21

    Applicant: HOFFMANN LA ROCHE

    Inventor： KAISER A ,  KOCH W ,  SCHEER M ,  WOLCKE U

    IPC: C07C235/12 ,  C07C275/24 ,  C07F5/04 ,  C07C101/08

    CPC classification number: C07C275/24 ,  C07C235/12 ,  C07F5/04

    Abstract: Phenylalanine derivatives which are N-substituted with a carbonyl, thio, or sulfonyl substituent useful as hypotensive, anti-pyretic and anti-parkinson agents and processes for their preparation from phenylalanine including intermediates in these processes.

    Abstract translation: 用作低血压，抗热解和抗帕金森病药物的羰基，硫代或磺酰基取代基被N-取代的苯丙氨酸衍生物及其制备方法，包括这些方法中的中间体。

    Indoline derivatives
    10.
    发明授权
    Indoline derivatives 失效
    吲哚衍生物

    公开(公告)号：US3780062A

    公开(公告)日：1973-12-18

    申请号：US3780062D

    申请日：1971-10-21

    Applicant: HOFFMANN LA ROCHE

    Inventor： KAISER A ,  KOCH W ,  WOLCKE U

    IPC: C07D209/42 ,  C07D27/38

    CPC classification number: C07D209/42 ,  Y10S514/96 ,  Y10S514/962

    Abstract: INDOLINE DERIVATIVES SUBSTITUTED IN THE 1-POSITION WITH HYDROGEN, ALKANOYL, BENZOYL, ALKOXY-CARBONYL OR O-NITROPHENYLTHIO, IN THE 2-POSITION WITH A CARBOXY OR ESTER GROUP AND THE 5- AND 6-POSITIONS WITH AN ALKANOYLOXY OR ALKOXY GROUP, WHICH ARE USEFUL AS HYPOTENSIVE, ANTIPYRETIC AND ANTI-PARKINSON AGENTS.

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