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    • 4. 发明授权
    • Aminobenzyl-amines and salts thereof
    • 氨基苄基胺及其盐
    • US4101671A
    • 1978-07-18
    • US780903
    • 1977-03-24
    • Johannes KeckKlaus-Reinhold NollHelmut PieperGerd KrugerSigfrid Puschmann
    • Johannes KeckKlaus-Reinhold NollHelmut PieperGerd KrugerSigfrid Puschmann
    • A61K31/135A61K31/19C07D221/24C07D295/135C07C87/28
    • C07D295/135A61K31/135A61K31/19C07D221/24
    • Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##STR2## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy (cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino,Provided, however, that when R.sub.3 is carboxyl or carbalkoxy, R.sub.4 and R.sub.5 are other than hydrogen, alkyl, mono- or di-hydroxyalkyl, alkenyl, cycloalkyl, mono- or di-hydroxy-cycloalkyl or benzyl; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
    • 其中R 1是氢或脂族或芳族羧酰基,R 2是氢,氯或溴,R 3是氟,1-4个碳原子的烷基,三氟甲基,氰基,氨基甲酰基,羧基,烷氧基,烷氧基, 乙酰基,1-羟乙基或者其中R 6和R 7各自为烷基,环烷基,羟基 - 环烷基,或彼此连接的氮原子,与它们相连的氮原子,吡咯烷子基,哌啶子基或吗啉代,R 4和R 5各自为 氢,1至5个碳原子的烷基,一或二羟基(1至5个碳原子的烷基),2至4个碳原子的烯基,5至7个碳原子的环烷基,一或二羟基(环烷基 5至7个碳原子),苄基,吗啉代羰基甲基或彼此连接的氮原子,吡咯烷基,哌啶子基,六亚甲基亚氨基,吗啉代,N-甲基 - 哌嗪子基或樟脑酸,提供,但是当R3 是羧基或烷氧基,R4和R5不同于氢 烷基,单 - 或二 - 羟基烷基,烯基,环烷基,单 - 或二 - 羟基 - 环烷基或苄基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作抗溃疡发生剂。
    • 6. 发明授权
    • Aminobenzyl-amides and salts thereof
    • 氨基苄基酰胺及其盐
    • US3950393A
    • 1976-04-13
    • US458099
    • 1974-04-05
    • Johannes KeckKlaus-Reinhold NollHelmut PieperGerd KrugerSigfrid Puschmann
    • Johannes KeckKlaus-Reinhold NollHelmut PieperGerd KrugerSigfrid Puschmann
    • C07C211/52A61K31/135A61K31/19C07C209/10C07C209/50C07C209/62C07C209/74C07C211/29C07C211/49C07C211/53C07C221/00C07C225/22C07C231/12C07C233/43C07C255/58C07D221/24C07D295/135C07C101/48C07C101/68
    • C07D295/135A61K31/135A61K31/19C07D221/24Y10S514/849
    • Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##EQU1## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy(cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anti-ulcergenics, secretolytics, antitussive, and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.
    • 式WHEREIN R 1的化合物是氢或脂族或芳族羧酸酰基,R 2是氢,氯或溴,R 3是氟,1至4个碳原子的烷基,三氟甲基,氰基,氨基甲酰基,羧基,烷氧基,烷氧基,乙酰基, 羟乙基或R6 -CH2-N ANGLE R7,其中R6和R7各自为烷基,环烷基,羟基 - 环烷基或彼此连接的氮原子,吡咯烷基,哌啶子基或吗啉代,R4和R5各自为 氢,1至5个碳原子的烷基,一或二羟基(1至5个碳原子的烷基),2至4个碳原子的烯基,5至7个碳原子的环烷基,一或二羟基(环烷基 5至7个碳原子),苄基,吗啉代羰基甲基或彼此连接的氮原子,吡咯烷基,哌啶子基,六亚甲基亚氨基,吗啉代,N-甲基哌嗪基或卡宾多,以及非毒性,药理学上可接受的 其添加量: 化合物作为其生物利用作为抗生素,秘密,抗生素和生物活性成分或抗生素因子的有效途径。
    • 10. 发明授权
    • Pharmaceutical compositions containing a
3-(amino-methylene)-5-phenyl-1,4-benzodiazepin-2-one and method of use
    • 含有3-(氨基 - 亚甲基)-5-苯基-1,4-苯并二氮杂-2-酮的药物组合物及其使用方法
    • US3956492A
    • 1976-05-11
    • US532069
    • 1974-12-12
    • Helmut PieperGerd KrugerJohannes KeckKlaus-Reinhold NollJoachim Kaehling
    • Helmut PieperGerd KrugerJohannes KeckKlaus-Reinhold NollJoachim Kaehling
    • A61K31/33A61K31/495A61K31/535A61K31/54
    • Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, cycloalkyl, phenyl, --A--YwhereinA is alkyl of 1 to 5 carbon atoms or alkenyl of 1 to 5 carbon atoms, andY is furyl, dialkylamino, hydroxyl, carbalkoxy or carbamido,Or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, thiomorpholino, thiomorpholino-S-oxide or N'-alkylpiperazino,R.sub.3 is halogen, nitro or trifluoromethyl,R.sub.4 is hydrogen, halogen or trifluoromethyl, andR.sub.5 is hydrogen, alkyl, cycloalkyl-methyl, alkylamino-alkyl, dialkylamino-alkyl or trifluoromethyl-alkyl;And a method of using the same as sedatives, tranquilizers, muscle-relaxants and anticonvulsives.
    • 含有作为活性成分的式WHEREIN R1和R2彼此相同或不同的化合物的药物剂量单位组合物各自为氢,环烷基,苯基,其中A为1至5个碳原子的烷基 或1至5个碳原子的链烯基,Y是呋喃基,二烷基氨基,羟基,烷氧羰基或氨基甲酰基,或者与其它任何其它的氮原子一起形成吡啶并吡咯烷酮,哌啶,异丙基苯胺,吗啉,噻唑啉, N-氧化物或N-烷基哌嗪基,R3是卤素,硝基或三氟甲基,R4是氢,卤素或三氟甲基,R5是氢,烷基,环烷基 - 甲基,烷基氨基 - 烷基,二烷基氨基 - 烷基或三氟甲基 - 烷基; 以及将其用作SEDATIVES,TRANQUILIZERS,MUSCLE-RELAXANTS和ANTICONVULSIVES的方法。