公开(公告)号：US3956492A

公开(公告)日：1976-05-11

申请号：US532069

申请日：1974-12-12

申请人： Helmut Pieper ,  Gerd Kruger ,  Johannes Keck ,  Klaus-Reinhold Noll ,  Joachim Kaehling

发明人： Helmut Pieper ,  Gerd Kruger ,  Johannes Keck ,  Klaus-Reinhold Noll ,  Joachim Kaehling

IPC分类号： A61K31/33 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54

摘要： 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.

摘要翻译： 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。

公开(公告)号：US5084449A

公开(公告)日：1992-01-28

申请号：US623833

申请日：1990-12-07

申请人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

发明人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

IPC分类号： C12N9/99 ,  A61K31/135 ,  A61K31/165 ,  A61K31/24 ,  A61K31/275 ,  A61K31/505 ,  A61P31/04 ,  A61P33/00 ,  A61P43/00 ,  C07C67/00 ,  C07C205/26 ,  C07C205/34 ,  C07C313/00 ,  C07C315/04 ,  C07C317/36 ,  C07C317/48

CPC分类号： C07C205/34 ,  C07C205/26 ,  C07C317/00 ,  C07C323/00

摘要： Disclosed are substituted bis(4-aminophenyl-sulfonees of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.3 can also be halogen, trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, C.sub.1 -C.sub.3 alkylo, carboxy or C.sub.1 -C.sub.3 akoxycarbonyl; andR.sub.4 is hydrogen or, when R.sub.1 and R.sub.2 are each hydrogen and R.sub.3 is halogen or hydroxy, R.sub.4 can also be halogen, hydroxy or C.sub.1 -C.sub.3 alkoxy; or a nontoxic, pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising such compounds alone and in combination with dihydrofolic acid-reductage inhibitors. The compounds and compositions are useful for their inhibiting effect on bacteria, mycobacteria and plasmodia.

公开(公告)号：US4362738A

公开(公告)日：1982-12-07

申请号：US158587

申请日：1980-06-11

申请人： Johannes Keck ,  Gerd Kruger ,  Helmut Pieper ,  Klaus Noll ,  Gunther Engelhardt ,  Norbert Promberger ,  Rainer Zimmermann

发明人： Johannes Keck ,  Gerd Kruger ,  Helmut Pieper ,  Klaus Noll ,  Gunther Engelhardt ,  Norbert Promberger ,  Rainer Zimmermann

IPC分类号： C07D209/08 ,  A61K31/495 ,  A61P29/00 ,  C07C67/00 ,  C07C227/00 ,  C07C227/16 ,  C07C227/18 ,  C07C229/54 ,  C07C237/32 ,  C07C237/38 ,  C07C313/00 ,  C07C323/12 ,  C07C323/65 ,  C07D209/28 ,  C07D213/74 ,  C07D295/088 ,  C07D295/155 ,  C07D401/12 ,  C07H13/08 ,  C07D279/18 ,  A61K27/00

CPC分类号： C07D213/74 ,  C07D209/28 ,  C07D295/088 ,  C07D295/155

摘要： Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, are pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-aryl-piperazino or N-(alkyl of 1 to 3 carbon atoms)-piperazino;A is cycloalkylene of 5 to 7 carbon atoms; unsubstituted or substituted alkylene of 2 to 10 carbon atoms, where the substituents are one to two alkyls of 1 to 3 carbon atoms each, one to two carbalkoxys of 2 to 4 carbon atoms each, one to two phenyls, one to four hydroxyls, one halomethyl, one hydroxymethyl, one alkanoyloxy of 1 to 18 carbon atoms, one alkanoyloxymethyl of 1 to 18 carbon atoms in the alkanoyl moiety or one ##STR2## where R.sub.1, R.sub.2 and R.sub.3 have the meanings previously defined; or alkylene of 2 to 10 carbon atoms interrupted by oxygen, sulfur, sulfoxide, sulfonyl, phenyl, cyclohexyl, pyridyl, piperazino or unsubstituted or substituted imino, where the substituent on the imino group is alkyl of 1 to 6 carbon atoms, phenyl or phenylalkyl of 1 to 3 carbon atoms in the alkyl moiety;B is the acyl residue of an antiphlogistic carboxylic acid;and their non-toxic, pharmacologically acceptable acid addition salts. The compounds as well as their salts are useful as anti-inflammatories.

摘要翻译： 其中每个X可以相同或不同于另一个X的式“IMAGE”的化合物是氧或亚氨基; R1是氢，氟，氯或溴; R2和R3可以相同或不同，分别为氢; 未取代或单取代的1至6个碳原子的烷基，其中取代基为苯基或每个烷基部分具有1至3个碳原子的二烷基氨基; 吡啶基 或5至7个碳原子的环烷基; 吡咯烷基，哌啶子基，六亚甲基亚氨基，吗啉代，N-芳基 - 哌嗪子基或N-（1至3个碳原子的烷基） - 哌嗪基; R 2和R 3彼此连接并连接的氮原子。 A是5至7个碳原子的亚环烷基; 2至10个碳原子的未取代或取代的亚烷基，其中取代基为1至2个碳原子数为1至2个的烷基，每个为2至4个碳原子的1至2个碳烷氧基，1至2个苯基，1至4个羟基，1至2个 卤代甲基，一个羟甲基，一个1至18个碳原子的烷酰氧基，一个在烷酰基部分中具有1至18个碳原子的烷酰氧基甲基或一个，其中R1，R2和R3具有以前定义的含义; 或由氧，硫，亚砜，磺酰基，苯基，环己基，吡啶基，哌嗪子基或未取代或取代的亚氨基所取代的2至10个碳原子的亚烷基，其中亚氨基上的取代基是1至6个碳原子的烷基，苯基或苯基烷基 在烷基部分中具有1至3个碳原子; B是消炎性羧酸的酰基残基; 及其无毒，药理学上可接受的酸加成盐。 化合物及其盐可用作抗炎剂。

公开(公告)号：US4119710A

公开(公告)日：1978-10-10

申请号：US754981

申请日：1976-12-28

申请人： Gunther Engelhardt ,  Johannes Keck ,  Gerd Kruger ,  Klaus-Reinhold Noll ,  Helmut Pieper

发明人： Gunther Engelhardt ,  Johannes Keck ,  Gerd Kruger ,  Klaus-Reinhold Noll ,  Helmut Pieper

IPC分类号： C07D263/04 ,  C07D317/58 ,  A61K31/04 ,  A61K31/135 ,  A61K31/275 ,  A61K31/36

CPC分类号： C07D263/04 ,  C07D317/58

摘要： Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, trifluoromethyl, nitro or cyano, andR.sub.3 is alkyl of 3 to 5 carbon atoms, hydroxy(alkyl of 3 to 5 carbon atoms), cycloalkyl of 3 to 5 carbon atoms, 1-(3,4-methylenedioxy-phenyl)-2-propyl or 1-(p-hydroxy-phenyl)-2-propyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics, uterospasmolytics, bronchospasmolytics and antispastics for the skeletal musculature, and especially as .beta..sub.2 -receptor mimetics and .beta..sub.1 -receptor blockers.

摘要翻译： 其中R 1为氢，氟，氯，溴，碘或氰基的外消旋和旋光活性化合物，R 2为氟，三氟甲基，硝基或氰基，R 3为3至5个碳原子的烷基，羟基（烷基 3至5个碳原子的环烷基，3至5个碳原子的环烷基，1-（3,4-亚甲二氧基 - 苯基）-2-丙基或1-（对羟基 - 苯基）-2-丙基，和非毒性 其药理学可接受的酸添加剂; 这些化合物作为其作为骨质疏松症，骨质疏松症，骨质疏松症和骨质疏松症的抗生素有用的化合物，特别适用于β2受体的MIME和β受体阻断剂。

公开(公告)号：US5187977A

公开(公告)日：1993-02-23

申请号：US676892

申请日：1991-03-28

申请人： Ralf Koschorek ,  Gerd Kruger ,  Hartmut Rosendahl ,  Johann Rothen

发明人： Ralf Koschorek ,  Gerd Kruger ,  Hartmut Rosendahl ,  Johann Rothen

IPC分类号： B60G17/00 ,  G01C9/00 ,  G01C9/08 ,  G01P15/00

CPC分类号： G01C9/00

摘要： An apparatus for the recognition of a rising slope is provided in particular for commercial vehicles, such as trucks or busses. The device comprises at least one sensor (1) for the axle load of the rear axle and/or of the front axle, as well as a device (4) for measuring the vehicle acceleration relative to the road. The signals of the sensor (1) and of the device (4) are fed into an electronics (2). The electronics (2) recognizes from these fed-in data, whether the vehicle is disposed on an uphill grade or on a downhill grade or on level ground. The thus generated signal can be further employed in various electronic systems, for example, in an automatic drawbar force control system.

摘要翻译： 提供用于识别上坡的装置特别用于商用车辆，例如卡车或公共汽车。 该装置包括至少一个用于后轴和/或前轴的轴负载的传感器（1），以及用于测量相对于道路的车辆加速度的装置（4）。 传感器（1）和设备（4）的信号被馈送到电子器件（2）中。 电子设备（2）从这些馈入数据中识别车辆是否处于上坡坡度，还是处于下坡坡度或水平地面。 这样产生的信号可以在各种电子系统中进一步使用，例如在自动牵引杆力控制系统中。

公开(公告)号：US4992430A

公开(公告)日：1991-02-12

申请号：US302158

申请日：1989-01-26

申请人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

发明人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

IPC分类号： C12N9/99 ,  A61K31/135 ,  A61K31/165 ,  A61K31/24 ,  A61K31/275 ,  A61K31/505 ,  A61P31/04 ,  A61P33/00 ,  A61P43/00 ,  C07C67/00 ,  C07C205/26 ,  C07C205/34 ,  C07C313/00 ,  C07C315/04 ,  C07C317/36 ,  C07C317/48

CPC分类号： C07C205/34 ,  C07C205/26 ,  C07C317/00 ,  C07C323/00

摘要： Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.3 can also be halogen, trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, C.sub.1 -C.sub.3 alkyl, carboxy or C.sub.1 -C.sub.3 alkoxycarbonyl; andR.sub.4 is hydrogen or, when R.sub.1 and R.sub.2 are each hydrogen and R.sub.3 is halogen or hydroxy, R.sub.4 can also be halogen, hydroxy or C.sub.1 -C.sub.3 alkoxy; or a nontoxic, pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising such compounds alone and in combination with dihydrofolic acid-reductase inhibitors. The compounds and compositions are useful for their inhibiting effect on bacteria, mycobacteria and plasmodia.

公开(公告)号：US4101671A

公开(公告)日：1978-07-18

申请号：US780903

申请日：1977-03-24

申请人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

发明人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

IPC分类号： A61K31/135 ,  A61K31/19 ,  C07D221/24 ,  C07D295/135 ,  C07C87/28

CPC分类号： C07D295/135 ,  A61K31/135 ,  A61K31/19 ,  C07D221/24

摘要： 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.

摘要翻译： 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。

公开(公告)号：USRE29628E

公开(公告)日：1978-05-09

申请号：US746954

申请日：1976-12-02

申请人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

发明人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

IPC分类号： A61K31/135 ,  A61K31/19 ,  C07D221/24

CPC分类号： A61K31/19 ,  A61K31/135 ,  C07D221/24

摘要： 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, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anti-ulcerogenics, secretolytics, .[.antitussive,.]. .Iadd.antitussives .Iaddend.and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.

公开(公告)号：US3950393A

公开(公告)日：1976-04-13

申请号：US458099

申请日：1974-04-05

申请人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

发明人： Johannes Keck ,  Klaus-Reinhold Noll ,  Helmut Pieper ,  Gerd Kruger ,  Sigfrid Puschmann

IPC分类号： C07C211/52 ,  A61K31/135 ,  A61K31/19 ,  C07C209/10 ,  C07C209/50 ,  C07C209/62 ,  C07C209/74 ,  C07C211/29 ,  C07C211/49 ,  C07C211/53 ,  C07C221/00 ,  C07C225/22 ,  C07C231/12 ,  C07C233/43 ,  C07C255/58 ,  C07D221/24 ,  C07D295/135 ,  C07C101/48 ,  C07C101/68

CPC分类号： C07D295/135 ,  A61K31/135 ,  A61K31/19 ,  C07D221/24 ,  Y10S514/849

摘要： 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.

摘要翻译： 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。