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    • 3. 发明授权
    • Aminoalkyl-substituted benzimidazolidin-2-ones
    • 氨基烷基取代的苯并咪唑烷-2-酮
    • US4215119A
    • 1980-07-29
    • US26608
    • 1979-04-03
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • C07D215/02A61K31/404A61K31/415A61K31/4166A61K31/4184A61K31/42A61K31/423A61K31/4245A61K31/536A61P9/08A61P9/12A61P11/00A61P25/24A61P25/26C07D215/22C07D215/227C07D223/04C07D233/32C07D233/36C07D235/04C07D235/22C07D235/26C07D263/54C07D263/58C07D265/22C07D265/36C07D405/04C07D405/12C07D413/12A61K31/535
    • C07D215/227C07D233/36C07D235/26C07D263/58C07D265/36Y10S514/929
    • 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.
    • 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。
    • 4. 发明授权
    • Aminoalkyl-substituted benzoxazine derivatives
    • 氨基烷基取代的苯并恶嗪衍生物
    • US4154829A
    • 1979-05-15
    • US773394
    • 1977-03-02
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • C07D215/02A61K31/404A61K31/415A61K31/4166A61K31/4184A61K31/42A61K31/423A61K31/4245A61K31/536A61P9/08A61P9/12A61P11/00A61P25/24A61P25/26C07D215/22C07D215/227C07D223/04C07D233/32C07D233/36C07D235/04C07D235/22C07D235/26C07D263/54C07D263/58C07D265/22C07D265/36C07D405/04C07D405/12C07D413/12C07D265/30A61K31/535
    • C07D215/227C07D233/36C07D235/26C07D263/58C07D265/36Y10S514/929
    • 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.
    • 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。
    • 7. 发明授权
    • N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines
and salts thereof
    • N,N {40-双 - {8({62-羟基 - {62-苯基) - 乙基{9-聚亚甲基二胺及其盐
    • US4021485A
    • 1977-05-03
    • US628819
    • 1975-11-04
    • Kurt SchrommAnton MentrupErnst-Otto RenthWerner Traunecker
    • Kurt SchrommAnton MentrupErnst-Otto RenthWerner Traunecker
    • C07C229/38C07C275/24C07D215/26C07D215/32C07C91/16
    • C07D215/26C07C229/38C07C275/24C07D215/32Y02P20/55
    • 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.
    • 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。