Ergoline derivatives
    2.
    发明授权
    Ergoline derivatives 失效
    二元醇衍生物

    公开(公告)号:US07666877B2

    公开(公告)日:2010-02-23

    申请号:US11914570

    申请日:2006-05-29

    IPC分类号: A61K31/48 C07D457/08

    CPC分类号: C07D457/06 C07D457/08

    摘要: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.

    摘要翻译: 公开了麦角灵衍生物,式(I),其中R 1和R 2各自独立地为H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基或 - 杂芳基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8烯基,任选的R 10取代的C 2 -C 8炔基; 任选的R 10取代的C 3 -C 8环烷基,或任选的R 10取代的C 4 -C 8环烯基; 或R 1和R 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环,除了氮原子以外,还含有独立地选自N,O和S的2个杂原子; R3为H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; 或CO-CH 2 R 1 R 2; R4是F; Cl; Br; 一世; OR1; NR1R2或具有R1的意义之一; R5具有以游离形式或盐形式用于预防或治疗由趋化因子受体及其配体之间相互作用介导的疾病或疾病的R1的意义。

    N-substituted piperazides of lysergic acid
    5.
    发明授权
    N-substituted piperazides of lysergic acid 失效
    N取代的柠檬酸管

    公开(公告)号:US3592816A

    公开(公告)日:1971-07-13

    申请号:US3592816D

    申请日:1967-11-01

    申请人: SANDOZ LTD

    CPC分类号: A61K31/48 C07D457/08

    摘要: THE PRESENT INVENTION RELATES TO COMPOUNDS OF GENERAL FORMULA I,

    4-R1,7-CH3,9-((4-R2-PIPERAZIN-1-YL)-CO-)-6A,7,8,9,10,10A-

    6H-INDOLO(4,3-FG)QUINOLINE WHERE THE 10,10A POSITION IS

    X--Y

    IN WHICH R1 IS HYDROGEN OR METHYL, AND R2 IS ARALKYL OF 7 TO 9 CARBON ATOMS, ARYL OR ARYL SUBSTITUTED BY ONE OR MORE OF THE FOLLOWING RADICALS: METHYL, ALKOXY OF 1 TO 4 CARBON ATOMS, CHLORINE OR BROMINE, AND

    X--Y IS -CH=C
    AND THEIR ACID ADDITION SALTS. THE COMPOUNDS IN WHICH R1 IS HYDROGEN AND

    X--Y IS -CH=C
    HAVE ANTIDEPRESSIVE PROPERTIES. THE REMAINING COMPOUNDS HAVE SEDATIVE PROPERTIES. THE PREPARATION OF THE COMPOUNDS IS ALSO DESCRIBED.

    Ergoline Derivatives
    8.
    发明申请
    Ergoline Derivatives 失效
    二元醇衍生物

    公开(公告)号:US20090018127A1

    公开(公告)日:2009-01-15

    申请号:US11914570

    申请日:2006-05-29

    CPC分类号: C07D457/06 C07D457/08

    摘要: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.

    摘要翻译: 公开了麦角灵衍生物,式(I),其中R 1和R 2各自独立地为H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基或 - 杂芳基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8烯基,任选的R 10取代的C 2 -C 8炔基; 任选的R 10取代的C 3 -C 8环烷基,或任选的R 10取代的C 4 -C 8环烯基; 或R 1和R 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环,除了氮原子以外,还含有独立地选自N,O和S的2个杂原子; R3为H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; 或CO-CH 2 R 1 R 2; R4是F; Cl; Br; 一世; OR1; NR1R2或具有R1的意义之一; R5具有以游离形式或盐形式用于预防或治疗由趋化因子受体及其配体之间相互作用介导的疾病或疾病的R1的意义。

    Lysergic acid n nicotinoyl piperazide
    10.
    发明授权
    Lysergic acid n nicotinoyl piperazide 失效
    LYSERGIC ACID N NICOTINOYL PIPERAZIDE

    公开(公告)号:US3752815A

    公开(公告)日:1973-08-14

    申请号:US3752815D

    申请日:1970-09-04

    申请人: SANDOZ LTD

    发明人: STUTZ P

    摘要: THE PRESENT INVENTION CONCERNS THE NOVEL HETEROCYCLIC COMPOUND OF THE FORMULA:

    1-((PYRID-3-YL)-CO-),4-((7-CH3-4,6,6A,7,8,9-HEXAHYDRO-

    INDOLO(4,3-FG)QUINOLIN-9-YL)-CO-)PIPERAZINE

    AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. THE COMPOUNDS ARE USEFUL IN THE TREATMENT OF CONDITIONS OF ORTHOSTASIS AND HYPERTONIA, AND ARE ALSO SALIDIURETICS, ANTI-PHLOGISTICS AND EDEMA-INHIBITORS.