N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines
and salts thereof
    11.
    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。

    HSV primase inhibitors
    12.
    发明授权
    HSV primase inhibitors 有权
    HSV启动子抑制剂

    公开(公告)号:US06323202B1

    公开(公告)日:2001-11-27

    申请号:US09534063

    申请日:2000-03-24

    IPC分类号: A61K31535

    摘要: The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or  wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.

    摘要翻译: 本发明提供对HSV起始酶具有活性的式1化合物:其中R 1是羟基或氨基; R 2是氢,卤素,(C 1-4)烷基或(C 1-4)烷氧基; R3是氢,卤素,(C1-4)烷基,(C1-4)烷氧基,氨基或叠氮基; R4与R2具有相同的意义; R5是氢或(C1-4)烷基; (C 1-7)烷基,(C 3-6)烷基},{苯基(C 1-7)烷氧基},{((单环杂环) - {(C 1-7) 烷氧基}},CH(W)C(O){O-(C1-4)烷基}其中W是氢或(C1-7)烷基,或其中Y是氢或(C1-7)烷基,Z是 (C 1-7)烷基,(C 3-6)环烷基,{(C 3-6)环烷基} - {(C 1-7)烷基},苯基(C 1-7)烷基或{{(单环杂环) -7)烷基}}或Y和Z与它们所连接的氮原子一起代表1-吡咯烷基,1-哌啶基,4-吗啉基或1-(4-甲基哌嗪基); 条件是(1)当R是本文定义的CH(W)C(O) - {O-(C 1-4)烷基}时,则R 5是氢; 和(2)R2,R3和R4中的至少一个不是氢。

    Pyridotriazoloquinazolines and triazolopyridoquinazolines useful as
antiallergics
    13.
    发明授权
    Pyridotriazoloquinazolines and triazolopyridoquinazolines useful as antiallergics 失效
    吡唑并三唑喹唑啉和三唑并吡啶喹唑啉可用作抗过敏药

    公开(公告)号:US4720496A

    公开(公告)日:1988-01-19

    申请号:US870365

    申请日:1986-06-04

    CPC分类号: C07D471/14

    摘要: Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.

    摘要翻译: 式(Ia)的化合物,其中(a)R 1是氢,低级烷基,低级烷氧基或8-卤素; R2是氢,低级烷基,低级烷氧基或稠合苯环; 并且R 3和R 4彼此一起是-N = N-NH-; 或(b)R 1和R 2彼此一起为-N = N-NH-; R3是氢,低级烷基,低级烷氧基,2-卤代,3-卤代或4-卤素; R4为氢,低级烷基,低级烷氧基或稠合苯环; 和与无机或有机碱形成的无毒的,药学上可接受的盐。 化合物及其盐可用作抗过敏药。

    1-(6,7-Dimethoxyquinazol-4-yl)semicarbazides
    15.
    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。

    Vasodilating or antidepressant phenalkanolaminoalkyl-substituted
imidazolidinones
    18.
    发明授权
    Vasodilating or antidepressant phenalkanolaminoalkyl-substituted imidazolidinones 失效
    血管舒张或抗抑郁药苯烷醇氨基烷基取代的咪唑啉酮

    公开(公告)号:US4271158A

    公开(公告)日:1981-06-02

    申请号:US102904

    申请日:1979-12-13

    摘要: Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--RwhereinQ 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 atomsor 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 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 or 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 - 或 - NR 3 - 其中R 3是氢或1至4个碳原子的烷基,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中的一个或两个不是卤素或三氟甲基时,还有-NR 3 R 9,其中R 3具有上述定义,R 8是氢, 1至20个碳原子的芳基,1至4个碳原子的烷基或芳烷基,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或5个碳原子的烷氧基羰基,以及R 5和R 6 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 -CONH-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。