N-Aryl-N'-(phenyl- or phenoxy-alkyl)-piperazines and salts thereof
    2.
    发明授权
    N-Aryl-N'-(phenyl- or phenoxy-alkyl)-piperazines and salts thereof 失效
    N-芳基-N {40-(苯基 - 或苯氧基 - 烷基) - 哌嗪及其盐

    公开(公告)号:US4100282A

    公开(公告)日:1978-07-11

    申请号:US793736

    申请日:1977-05-04

    CPC分类号: C07D207/27 A61K31/495

    摘要: Compounds of the formula ##STR1## wherein R is phenyl; phenyl having one or two substituents attached thereto, said substituents being selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, chlorine and trifluoromethyl; naphthyl; tetrahydronaphthyl; indanyl; pyridyl; isoquinolyl; or thiazolyl;R.sub.1 is ##STR2## where R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms,R.sub.4 and R.sub.5 are each hydrogen or alkyl of 1 to 4 carbon atoms, andQ is oxygen or two hydrogens,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halogen,A is a single carbon-to-carbon bond or --OCH.sub.2 --,R.sub.6 is hydrogen, hydroxyl, alkoxy of 1 to 4 carbon atoms or alkanoyloxy of 1 to 4 carbon atoms, andm is 0, 1, 2, 3, 4 or 5, but other than 0 when R.sub.6 is hydroxyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as CNS-depressants, adrenolytics, antiphlogistics, analgesics, antihistaminics and anticholesteremics.

    摘要翻译: 其中R是苯基的式“IMAGE”的化合物; 所述取代基选自1至4个碳原子的烷基,1至4个碳原子的烷氧基,1至4个碳原子的烷硫基,氯和三氟甲基; 萘基; 四氢萘基; 茚满基 吡啶基 异喹啉基 或噻唑基; R1是,其中R3是氢,1-4个碳原子的烷基,R4和R5分别是氢或1-4个碳原子的烷基,Q是氧或两个氢,R2是氢,1-4个 碳原子数为1〜4的烷氧基或卤素,A为单碳 - 碳键或-OCH2-,R6为氢,羟基,1〜4个碳原子的烷氧基或1〜4个碳原子的烷酰氧基, 并且M IS为0,1,2,3,4或5,但当R6为羟基时为0以及非毒性,药理学上可接受的酸添加量; 化合物作为它们的有效作为CNS抑制剂,肾上腺素,消炎药,镇痛药,抗组胺药和抗胆碱血症有用。

    Pharmaceutical compositions containing an N-phenyl-imidazolidine-2-one
and method of use
    3.
    发明授权
    Pharmaceutical compositions containing an N-phenyl-imidazolidine-2-one and method of use 失效
    含有N-苯基 - 咪唑烷-2-酮的药物组合物及其使用方法

    公开(公告)号:US3992537A

    公开(公告)日:1976-11-16

    申请号:US636738

    申请日:1975-12-01

    摘要: Pharmaceutical compositions containing as an active ingredient a compound of the formula ##SPC1##Wherein R' is in the m- or p-position and is selected from the group consisting of--CH.sub.2 --A, --CHR.sub.1 --CH.sub.2 --Aand ##EQU1## where R.sub.1 is hydrogen or hydroxyl, andA is ##SPC2##WhereR.sub.3 is hydrogen, chlorine, methyl, ethyl, trifluoromethyl or lower alkoxy, andR.sub.4 is hydrogen or methyl, orR.sub.3 and R.sub.4, together with each other and neighboring carbon atoms of the phenyl ring to which they are attached, are naphthyl,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as CNS-depressants, neuroleptics and anticholesteremics.

    摘要翻译: 含有式+ q,10的化合物作为活性成分的药物组合物在m-或p-位,并且选自-CH2-A,-CHR1-CH2-A和-CHR1 -CH-A,| CH3,其中R1是氢或羟基,A是+ q,12,其中R3是氢,氯,甲基,乙基,三氟甲基或低级烷氧基,R4是氢或甲基,或R3和R4一起 与它们所连接的苯环的彼此和相邻的碳原子是萘基,或非毒性,药理学上可接受的酸加成盐; 和使用它们作为CNS抑制剂,精神安定药和抗胆固醇药的方法。

    N-[1-(4-Amino-6,7-dialkoxy-2-quinazolinyl)-4-piperidy
l]-oxazolidine-2,4-diones
    6.
    发明授权
    N-[1-(4-Amino-6,7-dialkoxy-2-quinazolinyl)-4-piperidy l]-oxazolidine-2,4-diones 失效
    N- [1-(4-氨基-6,7-二烷氧基-2-喹唑啉基)-4-哌啶基] - 恶唑烷-2,4-二酮

    公开(公告)号:US4539323A

    公开(公告)日:1985-09-03

    申请号:US531842

    申请日:1983-09-14

    CPC分类号: C07D413/04 C07D413/14

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 8 carbon atoms or arylmethyl; orR.sub.1 and R.sub.2, together with each other, are --(CH.sub.2).sub.4 or --(CH.sub.2).sub.5 --; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or arylmethyl; orR.sub.3 and R.sub.4, together with each other, are --CH.sub.3 -- or --CH.sub.2 --CH.sub.2 --;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of cardiovascular diseases, especially hypertension.

    摘要翻译: 其中R 1和R 2可以相同或不同,各自独立地为氢,1至8个碳原子的直链或支链烷基或芳基甲基; 或R 1和R 2彼此一起为 - (CH 2)4或 - (CH 2)5 - ; 并且可以相同或不同的R 3和R 4各自独立地为氢,1至4个碳原子的直链或支链烷基或芳基甲基; 或R 3和R 4彼此一起为-CH 3 - 或-CH 2 -CH 2 - ; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用于治疗心血管疾病,特别是高血压。

    (1-Hydroxy-2-amino-alkyl)-substituted benzoxazinones and benzoxazolinones
    7.
    发明授权
    (1-Hydroxy-2-amino-alkyl)-substituted benzoxazinones and benzoxazolinones 失效
    (1-羟基-2-氨基 - 烷基)取代的苯并恶嗪酮和苯并恶唑啉酮

    公开(公告)号:US4460581A

    公开(公告)日:1984-07-17

    申请号:US433681

    申请日:1982-10-12

    摘要: Compounds of the formula ##STR1## wherein A is a single bond, ##STR2## R.sub.1 is --OH, --0--acyl, chlorine or hydrogen; R.sub.2 is hydrogen, methyl or ethyl;R.sub.3 is ##STR3## m is 2, 3 or 4; n is 1, 2 or 3;R.sub.4 is hydrogen or lower alkyl;R.sub.5 is hydrogen, lower alkyl or, when R.sub.4 is hydrogen, also phenyl;R.sub.6, R.sub.7 and R.sub.8 are each hydrogen or methyl;R.sub.9 is hydrogen, --Ar, --OAr or --NH--CO--Ar;Ar is ##STR4## R.sub.10, R.sub.11 and R.sub.12 which may be identical to or different from each other, are each hydrogen, hydroxyl, methyl, methoxy, halogen, methylenedioxy, --NH--R.sub.13 or --CONH.sub.2 ; andR.sub.13 is hydrogen, acyl or lower alkylsulfonyl;and non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as their salts are useful for the treatment of asthma, bronchitis, urticaria, conjunctivities, hay fever, colds and cardiovascular disorders, and for relaxation of the uterine musculature.

    摘要翻译: 其中A是单键的式“IMAGE”的化合物,R 1是-OH,-O-酰基,氯或氢; R2是氢,甲基或乙基; R3为 m为2,3或4; n为1,2或3; R4是氢或低级烷基; R5是氢,低级烷基,或当R4是氢时也是苯基; R6,R7和R8各自为氢或甲基; R9是氢,-Ar,-OAr或-NH-CO-Ar; Ar可以相同或不同,分别是氢,羟基,甲基,甲氧基,卤素,亚甲二氧基,-NH-R13或-CONH 2; R 1,R 2, 和R 13是氢,酰基或低级烷基磺酰基; 和无毒的药学上可接受的酸加成盐; 化合物及其盐可用于治疗哮喘,支气管炎,荨麻疹,结膜炎,花粉症,感冒和心血管疾病,以及用于放松子宫肌肉组织。