N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines
and salts thereof
    2.
    发明授权
    N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines and salts thereof 失效
    N,N {40-双 - {8({62-羟基 - {62-苯基) - 乙基{9-聚亚甲基二胺及其盐

    公开(公告)号:US4021485A

    公开(公告)日:1977-05-03

    申请号:US628819

    申请日:1975-11-04

    摘要: Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen or methyl, m is 0 or an integer from 1 to 8, inclusive, andAr is ##STR2## WHERE R is hydrogen or acyl, andR.sub.2 is hydrogen or --OR, as defined above, ##STR3## WHERE R has the meanings defined above, andR.sub.3 is hydroxy-lower alkyl, --NH--CO--R.sub.4, --NH--SO.sub.2 --R.sub.5, --CH.sub.2 --NH--CO--R.sub.4, --CH.sub.2 --NH--SO.sub.2 --R.sub.5 or --CH.sub.2 --NH--CO--NH--R.sub.4, whereR.sub.4 is hydrogen or lower alkyl, andR.sub.5 is lower alkyl or di-lower alkyl-amino, ##STR4## WHERE R.sub.6 is hydrogen, amino or hydroxyl,X is chlorine or bromine, andY is hydrogen, chlorine or bromine or ##STR5## WHERE R has the meanings defined above, andA is a saturated or unsaturated 5- to 6-membered ring,And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as bronchospasmolytics, uterine spasmolytics, antipruritics and antiallergics.

    摘要翻译: 式(Ⅰ)化合物其中R 1为氢或甲基,M为0或整数1至8,包含和Ar为(a)R为氢或酰基,R 2为氢 或-OR,如上所定义,(b)其中R具有上述定义,并且R 3是羟基 - 低级烷基,-NH-CO-R 4,-NH-SO 2 -R 5,-CH 2 -NH-CO -R4,-CH2-NH-SO2-R5或-CH2-NH-CO-NH-R4,其中R4是氢或低级烷基,R5是低级烷基或二 - 低级烷基 - 氨基,(c) 其中R6是氢,氨基或羟基,X是氯或溴,Y是氢,氯或溴。(d)其中R具有上述定义,A是饱和或不饱和的5-至6- 及其非毒性,药理学上可接受的酸添加剂; 化合物作为其作为BRONCHOSPASMOLYTICS,UTERINE SPASMOLYTICS,ANTIPRITICS和ANTIALLERGICS的有用的化合物。

    1-(6,7-Dimethoxyquinazol-4-yl)semicarbazides
    3.
    发明授权
    1-(6,7-Dimethoxyquinazol-4-yl)semicarbazides 失效
    1-(6,7-二甲氧基喹唑啉-4-基)氨基脲

    公开(公告)号:US4546102A

    公开(公告)日:1985-10-08

    申请号:US546864

    申请日:1983-10-31

    CPC分类号: C07D239/94

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms or trifluoromethyl;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, methyl or ethyl;R.sub.5 is hydrogen, alkyl of 1 to 8 carbon atoms, phenyl-(alkyl of 1 to 8 carbon atoms), cycloalkyl of 3 to 7 carbon atoms, (alkoxy of 1 to 4 carbon atoms) carbonyl-methyl, phenyl, substituted phenyl, naphthyl or substituted naphthyl; orR.sub.4 and R.sub.5, together with each other, are alkylene of 4 to 5 carbon atoms, optionally interrupted by --O-- or --NR.sub.6 --, where R.sub.6 is alkyl of 1 to 4 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics.

    摘要翻译: 其中R 1为氢,1至4个碳原子的烷基或三氟甲基的化合物< IMAGE> R2,R3和R4各自独立地为氢,甲基或乙基; R5是氢,1至8个碳原子的烷基,苯基(1至8个碳原子的烷基),3至7个碳原子的环烷基,(1至4个碳原子的烷氧基)羰基 - 甲基,苯基,取代的苯基, 萘基或取代的萘基; 或R 4和R 5彼此一起是4至5个碳原子的亚烷基,任选被-O-或-NR 6 - 间隔,其中R 6是具有1至4个碳原子的烷基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作强心剂。

    Hypertensive phenylalkylamines and salts thereof
    7.
    发明授权
    Hypertensive phenylalkylamines and salts thereof 失效
    高效苯丙氨酸及其盐

    公开(公告)号:US4146645A

    公开(公告)日:1979-03-27

    申请号:US761476

    申请日:1977-01-24

    CPC分类号: C07C275/40

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, --(CH.sub.2).sub.n --R.sub.4 or --CO--R.sub.5,where n is 1 or 2,R.sub.4 is hydrogen, cyano or benzoyl, andR.sub.5 is hydrogen, lower alkoxy, benzyloxy, --CH.sub.2 --NH.sub.2, --CH(CH.sub.3)--NH.sub.2, --CH.sub.2 --NH--CH.sub.2 --C.sub.6 H.sub.5 or --CH(CH.sub.3)--NH--CH.sub.2 --C.sub.6 H.sub.5,R.sub.2 is hydrogen or methyl, andR.sub.3 is amino, nitro, --NH--CO--R.sub.6 or --NH--A--R.sub.7,where R.sub.6 is hydrogen, methyl, methoxy, ethoxy, methylthio or ethylthio,R.sub.7 is amino, methylamino or dimethylamino, andA is --CO-- or --SO.sub.2 --,provided, however, that R.sub.1 and R.sub.4 are other than hydrogen and R.sub.2 is other than hydrogen or methyl when R.sub.6 is hydrogen or methyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as hypertensives.

    Aminoalkyl-substituted benzimidazolidin-2-ones
    8.
    发明授权
    Aminoalkyl-substituted benzimidazolidin-2-ones 失效
    氨基烷基取代的苯并咪唑烷-2-酮

    公开(公告)号:US4215119A

    公开(公告)日:1980-07-29

    申请号:US26608

    申请日:1979-04-03

    摘要: Racemic and optically active compounds of the formulaQ-C.sub.n H.sub.2n -NH-Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl or 1 to 4 carbon atoms,n is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, R.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms, or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --COHN-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译: 其中Q为氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,三氟甲基或氨基,R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或三氟甲基,R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基,A是-O-,-CH 2 -CH 2 - 或 -NR 3 - ,其中R 3是氢或烷基或1至4个碳原子,n是2-6的整数,包括2和6,R是氢,苄基或者其中R 4是氢,甲基或乙基,R 5,R 6和 R 7可以相同或不同,分别为氢,卤素,羟甲基,三氟甲基,1至4个碳原子的烷基,1至4个碳原子的烷氧基,硝基,氰基,-CONHR 3,-CONHOH, - COOR 3,R8O-,甲基磺酰基甲基,或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时,也可以是-NR 3 R 9,其中R 3具有上述定义,R 8是氢, 1至20个碳原子的烷酰基,1至4个碳原子的烷酰基或芳烷基,R 9是氢,低级烷酰基,甲磺酰基,氨基甲酰基,二甲基氨磺酰基或2至5个碳原子的烷氧基羰基,以及R5和R6, 另一个是-O-CH 2 -O,-O-CH 2 -CH 2 -O - , - CH = CH-CH = CH-,-O-CH 2 -CONH-,-CH 2 -CH 2 -COOH-或-O-CO -NH-和无毒的药学上可接受的酸加成盐。 化合物及其盐可用作血管扩张剂和CNS刺激剂。

    Aminoalkyl-substituted benzoxazine derivatives
    9.
    发明授权
    Aminoalkyl-substituted benzoxazine derivatives 失效
    氨基烷基取代的苯并恶嗪衍生物

    公开(公告)号:US4154829A

    公开(公告)日:1979-05-15

    申请号:US773394

    申请日:1977-03-02

    摘要: Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 -- where the oxygen is bonded to the benzene ring, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,N is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, r.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --CONH-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译: 其中Q为氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,三氟甲基或氨基,R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或三氟甲基,R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基,A是-O-,-CH 2 -CH 2 - , - O-CH2-,其中氧与苯环结合,或-NR 3 - ,其中R 3是氢或1至4个碳原子的烷基,N是2至6,INCLUSIVE和R R的整数是氢,苄基或 其中R 4是氢,甲基或乙基,R 5,R 6和R 7可以彼此相同或不同,各自为氢,卤素,羟甲基,三氟甲基,1至4个碳原子的烷基,1至 4个碳原子,硝基,氰基,-CONHR 3,-CONHOH,-COOR 3,R 8 O - ,甲基磺酰基甲基,或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时,也可以是-NR 3 R 9, R 3具有上述定义,R 8为氢,1至20个碳原子的烷酰基,1至4个碳原子的烷基或芳烷基,R 9为氢,低级烷酰基,甲磺酰基,氨基甲酰基,二甲基氨磺酰基或烷氧基羰基2至5 碳原子和R 5和R 6彼此一起是-O-CH 2 -O,-O-CH 2 -CH 2 -O - , - CH = CH-CH = CH-,-O-CH 2 -CONH-, - CH2-CH2-CONH-或-O-CO-NH-,及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作血管扩张剂和CNS刺激剂。