Decahydro-8H-isoquino(2,1-g)(1,6)naphthyridine derivatives and related
compounds
    1.
    发明授权
    Decahydro-8H-isoquino(2,1-g)(1,6)naphthyridine derivatives and related compounds 失效
    十氢-8H-异喹啉(2,1-g)(1,6)萘啶衍生物和相关化合物

    公开(公告)号:US4956365A

    公开(公告)日:1990-09-11

    申请号:US257372

    申请日:1988-10-12

    IPC分类号: C07D471/14 C07D491/22

    CPC分类号: C07D471/14

    摘要: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;W is oxygen or sulfur; andZ is --R.sup.1, --OR.sup.2 or --NR.sup.3 R.sup.4, whereinR.sup.1 is lower alkyl, lower haloalkyl, cycloalkyl, optionally substituted phenyl or phenyl lower alkyl, or heteroaryl;R.sup.2 is lower alkyl, optionally substituted phenyl or phenyl lower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --(CH.sub.2).sub.m, --N(R.sup.5)-- or oxygen, in which m is an integer of 0-2 and R.sup.5 is hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers.

    摘要翻译: (1)和(2)的化合物:其中:X和Y独立地是氢,羟基,低级烷基,低级烷氧基或卤素,或X和Y一起是 亚甲二氧基或亚乙基-1,2-二氧基; W是氧或硫; 且Z为-R1,-OR2或-NR3R4,其中R1为低级烷基,低级卤代烷基,环烷基,任选取代的苯基或苯基低级烷基或杂芳基; R2是低级烷基,任意取代的苯基或苯基低级烷基; R3和R4独立地是氢,烷基,任选取代的苯基或苯基低级烷基; 或者R 3和R 4与它们所连接的氮一起代表下式的杂环:其中A是 - (CH 2)m,-N(R 5) - 或氧,其中m是整数0 -2和R5是氢或低级烷基; 或其药学上可接受的盐可用作α2-受体阻滞剂。

    Isoindolinyl derivatives
    2.
    发明授权
    Isoindolinyl derivatives 失效
    异吲哚啉衍生物

    公开(公告)号:US5726197A

    公开(公告)日:1998-03-10

    申请号:US971015

    申请日:1992-11-02

    摘要: Compounds of the Formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halo, optionally substituted phenyl, amino, nitro or trifluoromethyl; and X is --NH--, --O-- or --S--; and the pharmaceutically acceptable salts thereof exhibit high affinity and selectivity for imidazoline receptors, and are are particularly useful for modification of the female reproductive cycle.

    摘要翻译: 下式的化合物:其中:R 1和R 2独立地是氢或低级烷基; R3是氢,低级烷基,低级烷氧基,羟基,卤素,任意取代的苯基,氨基,硝基或三氟甲基; X为-NH-,-O-或-S-; 并且其药学上可接受的盐对咪唑啉受体表现出高亲和力和选择性,并且对于雌性生殖循环的改变特别有用。

    1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines
    5.
    发明授权
    1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
    1,9-链烷基-2,3,4,5-四氢-1H-3-苯并氮杂

    公开(公告)号:US4957914A

    公开(公告)日:1990-09-18

    申请号:US231818

    申请日:1988-08-12

    IPC分类号: C07D223/14 C07D223/32

    CPC分类号: C07D223/32 C07D223/14

    摘要: 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.

    摘要翻译: 1,9-烷基桥-2,3,4,5-四氢-1H-3-苯并吖庚因及其衍生物,即式I化合物:其中:R选自 由氢,氰基,低级烷基,低级烯基和芳烷基组成的基团; R 1,R 2和R 3各自独立地选自:氢,羟基,卤素,三氟甲基,硝基,酰氨基,低级烷氧基,低级烷基和低级烷硫基; Y是具有2至4个碳原子的低级亚烷基; 和其药学上可接受的盐可用作CNS剂,例如作为抗抑郁药,抗焦虑药和抗高血压药,和/或作为其前体。

    Laidlomycin phenylcarbamate
    6.
    发明授权
    Laidlomycin phenylcarbamate 失效
    苯基氨基甲酸铵

    公开(公告)号:US4542027A

    公开(公告)日:1985-09-17

    申请号:US582691

    申请日:1984-02-23

    申请人: Robin D. Clark

    发明人: Robin D. Clark

    CPC分类号: C07H19/01 A23K20/195

    摘要: A compound represented by the formula ##STR1## wherein R.sup.1 is an alkali metal cation or hydrogen and which useful for increasing the feed efficiency of ruminants and for treating coccidiosis in domestic animals, especially chickens.

    摘要翻译: 由式 + TR 表示的化合物,其中R1是碱金属阳离子或氢,并且其可用于提高反刍动物的饲料效率和用于在家畜,特别是鸡中治疗球虫病。

    9-(1,4-Benzodioxan-2-ylalkyl and
hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones
    7.
    发明授权
    9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones 失效
    9-(1,4-苯并二恶烷-2-基烷基和羟烷基)-1-氧杂-4,9-二氮杂螺[5.5]十一烷-3-酮

    公开(公告)号:US4353901A

    公开(公告)日:1982-10-12

    申请号:US312447

    申请日:1981-10-19

    申请人: Robin D. Clark

    发明人: Robin D. Clark

    IPC分类号: C07D498/10 A61K31/535

    摘要: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula: ##STR1## wherein:R.sup.1 is ##STR2##R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms;X is hydrogen, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms or halo;m is 1 or 2; andn is 1, 2 or 3; andthe pharmaceutically acceptable acid addition salts thereof.

    摘要翻译: 用于预防和/或治疗高血压,充血性心力衰竭,心律失常,偏头痛,血管痉挛症和哮喘的化合物由下式表示:(I)

    9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones
    8.
    发明授权
    9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones 失效
    9- [2-(3-吲哚基)乙基] -1-氧杂-4,9-二氮杂螺[5.5]十一烷-3-酮

    公开(公告)号:US4332804A

    公开(公告)日:1982-06-01

    申请号:US246459

    申请日:1981-03-23

    申请人: Robin D. Clark

    发明人: Robin D. Clark

    摘要: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl of one to four carbon atoms or lower alkoxy of one to four carbon atoms; andthe pharmaceutically acceptable acid addition salts thereof.

    摘要翻译: 用于预防和/或治疗高血压,充血性心力衰竭,心律失常,偏头痛,血管痉挛症和哮喘的化合物由式(I)表示,其中:R,R 1,R 2,R 3和R 4独立地为 氢或1-4个碳原子的低级烷基; R5和R6独立地是氢,1-4个碳原子的低级烷基或1-4个碳原子的低级烷氧基; 及其药学上可接受的酸加成盐。