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1. 发明授权

US4490369A Benzazepine derivatives, their pharmaceutical compositions and method of use 失效
标题翻译：苯扎西平衍生物，其药物组合物和使用方法
公开(公告)号：US4490369A
公开(公告)日：1984-12-25
申请号：US547940
申请日：1983-11-02
申请人： Manfred Reiffen , Joachim Heider , Norbert Hauel , Volkhard Austel , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Klaus Noll , Helmut Pieper , Gerd Kruger , Johannes Keck
发明人： Manfred Reiffen , Joachim Heider , Norbert Hauel , Volkhard Austel , Wolfgang Eberlein , Walter Kobinger , Christian Lillie , Klaus Noll , Helmut Pieper , Gerd Kruger , Johannes Keck
IPC分类号： C07C59/64 , C07D205/04 , C07D223/16 , C07D243/02 , C07D243/04 , C07D491/04 , A61K31/55 , C07D521/00
CPC分类号： C07D223/16 , C07C59/64 , C07D205/04 , C07D243/02 , C07D243/04 , C07D491/04
摘要： Compounds of the formula ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO--, --CH.sub.2 --CO-- or ##STR2## where R.sub.7 is alkyl of 1 to 3 carbon atoms, andB is methylene, carbonyl or thiocarbonyl, orA is --CO--CO--, --N.dbd.CH--, ##STR3## where R.sub.8 is hydrogen or alkyl of 1 to 3 carbon atoms substituted by a phenyl, methoxyphenyl or dimethoxyphenyl, andB is methylene;E is n-alkylene of 2 to 4 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;G is n-alkylene of 1 to 5 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, wherein one methylene group of an n-alkylene of 2 to 5 carbon atoms can be replaced by a carbonyl group, with the proviso that B represents a methylene or carbonyl group, or methylene-n-hydroxy-alkylene of 1 to 4 carbon atoms, where the methylene group is attached to the nitrogen atom; andR.sub.1 to R.sub.5 are simple substituents of various types;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中A是-CH 2 -CH 2 - ， - CH = CH - ， - NH-CO-， - CH 2 -CO-或者其中R 7是1至3个碳原子的烷基，和B 是亚甲基，羰基或硫代羰基，或A是-CO-CO-，-N = CH-，其中R 8是氢或被苯基，甲氧基苯基或二甲氧基苯基取代的1至3个碳原子的烷基，和 B是亚甲基; E是任选被1至3个碳原子的烷基取代的2至4个碳原子的正亚烷基，2-羟基 - 正丙烯，2-羟基 - 正丁烯或3-羟基 - 正丁烯; G是任选被1至3个碳原子的烷基取代的1至5个碳原子的正亚烷基，其中2至5个碳原子的正亚烷基的一个亚甲基可被羰基取代，条件是 B表示亚甲基或羰基，或亚甲基与氮原子连接的1至4个碳原子的亚甲基 - 正 - 羟基 - 亚烷基; 而R1至R5是各种简单的取代基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

2. 发明授权

US4244967A Antiphlogistic pharmaceutical compositions containing a phenylethanolamine and methods of use 失效
标题翻译：含有苯乙醇胺的消炎药物组合物及其使用方法
公开(公告)号：US4244967A
公开(公告)日：1981-01-13
申请号：US72553
申请日：1979-09-04
申请人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
发明人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
IPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325 , A61P29/00 , A61P43/00 , A61K31/27
CPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325
摘要： The method of using compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms,R.sub.3 is cycloalkyl or alkyl, each of 3 to 5 carbon atoms, andR.sub.4 is hydrogen or --CO--R.sub.5, whereR.sub.5 is alkoxy of 1 to 5 carbon atoms, alkenyloxy of 2 to 5 carbon atoms, aryloxy of 6 to 10 carbon atoms, aralkoxy of 7 to 11 carbon atoms, or amino which may be mono- or di-substituted by alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, aryl of 6 to 10 carbon atoms and/or aralkyl of 7 to 11 carbon atoms,and non-toxic, pharmacologically acceptable acid addition salts thereof as antirheumatics and antiphlogistics.
摘要翻译：使用下式化合物的方法其中R1是氢，氟，氯，溴，碘或氰基，R2是氟，氰基，三氟甲基，硝基或1-4个碳原子的烷基，R3是环烷基或烷基， 3〜5个碳原子，R4为氢或-CO-R5，R5为1〜5个碳原子的烷氧基，2〜5个碳原子的烯氧基，6〜10个碳原子的芳氧基，7〜11个芳氧基碳原子或可以被1至5个碳原子的烷基，2至5个碳原子的烯基，6至10个碳原子的芳基和/或7至11个碳原子的芳烷基单取代或二取代的氨基，以及无毒，药理学上可接受的酸加成盐作为抗风湿剂和消炎药。

3. 发明授权

US5084449A Anti-bacterial compositions comprising a substituted bis-(4-aminophenyl)-sulfone and a dihydro-folic acid reductase 失效
标题翻译：包含取代的双 - （4-氨基戊基）-SULFONE和二羟基酸降解酶的抗菌组合物
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.

4. 发明授权

US4362738A Esters and amides containing the 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetyl moiety 失效
标题翻译：含有1-（4-氯苯甲酰基）-5-甲氧基-2-甲基-1H-吲哚-3-乙酰基部分的酯和酰胺
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。

5. 发明授权

US4829058A Substituted bis-(4-aminophenyl)-sulfones 失效
标题翻译：取代的双 - （4-氨基苯基） - 砜
公开(公告)号：US4829058A
公开(公告)日：1989-05-09
申请号：US62291
申请日：1987-06-15
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.
摘要翻译：公开了通式为（I）的取代的双（4-氨基苯基） - 砜，其中R 1是氢，烷基或环烷基; 基团，R 2是氢或C 1 -C 3烷基，R 3是腈，C 1 -C 3烷基氨基羰基，C 2 -C 3烷基氨基羰基，C 3 -C 7 N-环烷基-C 1 -C 3烷基氨基羰基C 1 -C 3烷基氨基，C 1 -C 3，二烷基氨基羰基烷氧基，烷基氨基磺酰基，二C1-C3烷基氨基亚氨基，二C1-C3烷基氨基磺酰基，羟基C1-C3烷基，C1-C3烷基羰基，氨基C1-C3烷基或C1-C3烷氧基C1-C3烷基，或当R1和R2各自为氢时，R3 可以是羟基，羟基羰基C1-C3烷氧基或二C1-C3氨基羰基烷氧基; 或者当R1是C1-C3烷基或C1-C3环烷基，R2是氢或C1-C3烷基时，R3也可以是卤素，三氟甲基，硝基，氨基，氨基磺酰基，氨基羰基，C1-C3烷基，羧基或C1-C3 烷氧基羰基并且R 4是氢，或者当R 1和R 2各自为氢且R 3为卤素或羟基时，R 4也可以是卤素，羟基或C 1 -C 3烷氧基; 或其无毒的药学上可接受的盐。还公开了单独包含这些化合物并与二氢叶酸还原酶抑制剂组合的药物组合物。化合物和组合物可用于其对细菌，分枝杆菌和疟原虫的抑制作用。

6. 发明授权

US4992430A Anti-bacterial compositions comprising a substituted bis-(4-aminophenyl)-sulfone and a dihydro-folic acid reductase 失效
标题翻译：包含取代的双 - （4-氨基苯基） - 砜和二氢叶酸还原酶的抗菌组合物
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.

7. 发明授权

US4113777A 2- OR 4-Hydroxy-3,5-dihalo-benzylamines and salts thereof 失效
标题翻译： 2-或4-羟基-3,5-二卤代苄胺及其盐
公开(公告)号：US4113777A
公开(公告)日：1978-09-12
申请号：US812325
申请日：1977-07-01
申请人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
发明人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
IPC分类号： A61K31/135 , C07C87/28
CPC分类号： A61K31/135 , Y10S514/849 , Y10S514/925
摘要： Compounds of the formula ##STR1## wherein X and R.sub.1 are each chlorine or bromine;R.sub.2 is isopropyl; tert.butyl; tert.pentyl; mono-, di- or tri-hydroxy-substituted branched alkyl of 3 to 5 carbon atoms; cyclohexyl; or hydroxycyclohexyl; andR.sub.3 is alkyl of 1 to 4 carbon atoms or, when R.sub.2 is other than cyclohexyl, also hydrogen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as secretolytics, antitussives, anti-ulcerogenics and stimulants for the production of the surfactant or antiatelectasis factor of the alveoli.
摘要翻译：其中X和R 1各自为氯或溴的式“IMAGE”的化合物; R2是异丙基; 叔丁基叔戊基 3至5个碳原子的单，二或三羟基取代的支链烷基; 环己基或羟基环己基; 并且R 3是1至4个碳原子的烷基，或者当R 2不是环己基时，也是氢; 和非毒性，药理学上可接受的酸添加量; 化合物作为其生物利用作为秘密，抗生素，抗生素和抗生素用于生产ALVEOLI的表面活性剂或抗原决定因子。

8. 发明授权

US4006246A Pharmaceutical compositions containing an aminobenzyl-amine and method of use 失效
标题翻译：含氨基苄基胺的药物组合物及其使用方法
公开(公告)号：US4006246A
公开(公告)日：1977-02-01
申请号：US649481
申请日：1976-01-15
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 , A61K31/24
CPC分类号： A61K31/19 , A61K31/135
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl, benzoyl or halobenzoyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is carboxyl or lower carbalkoxy, 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 or 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy-(cycloalkyl of 5 to 7 carbon atoms) or benzyl,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as anti-ulcerogenics, secretolytics, antitussives, and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.
摘要翻译：含有下式化合物作为活性成分的药物剂量单位组合物，其中R 1是氢，低级烷酰基，苯甲酰基或卤代苯甲酰基，R 2是氢，氯或溴，R 3是羧基或低级烷氧羰基，R 4和R 5各自是氢，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），烯基或2至4个碳原子，5至7个碳原子的环烷基，一或二羟基 - （5至7个碳原子的环烷基）或苄基，或非毒性，药理学上可接受的酸添加盐; 以及使用它们作为抗生素，秘密，抗生素和生物活性物质的抗生素或抗原决定因子的方法。

9. 发明授权

US4093734A Amino-benzoic acid amides 失效
标题翻译：氨基 - 苯甲酸酰胺
公开(公告)号：US4093734A
公开(公告)日：1978-06-06
申请号：US734818
申请日：1976-10-22
申请人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
发明人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
IPC分类号： C07D295/12 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P1/04 , A61P1/08 , A61P25/24 , A61P25/26 , C07C237/30 , C07D207/09 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/40 , C07D213/75 , C07D233/30 , C07D295/13 , C07D453/02 , C07D207/44
CPC分类号： C07D213/40 , C07D207/09 , C07D211/26 , C07D211/56 , C07D233/30 , C07D295/13 , C07D453/02
摘要： Compounds of the formula ##STR1## wherein (A) WHEN THE AMINO-SUBSTITUENT IS IN THE P-POSITION WITH RESPECT TO THE CARBONYL GROUP,R.sub.1 is chlorine in the o-position with respect to the carbonyl group,R.sub.2 is hydrogen, andR.sub.3 is ethylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, N-methyl-cyclohexylamino, benzylamino or 1-ethyl-pyrrolidyl-(2)-aminomethyl, or(b) when the amino-substituent is in the o--, m-- or p-position with respect to the carbonyl group,R.sub.1 is hydrogen, chlorine or bromine,R.sub.2 is trifluoromethyl, nitro or, when R.sub.4 is 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl or 1-(alkyl of 1 to 3 carbon atoms)-piperidyl, also fluorine, chlorine, bromine or methyl,R.sub.3 is (alkyl of 1 to 5 carbon atoms)-amino, (cycloalkyl of 3 to 7 carbon atoms)-amino, benzylamino, quinuclidinyl-amino or --NH--(CH.sub.2).sub.n --R.sub.4where R.sub.4 is pyridyl, 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl, 1-(alkyl of 1 to 3 carbon atoms)-piperidyl or, when n is 2 or 3, also imidazolonyl, pyrrolidino, piperidino or morpholino, andn is 0, 1, 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anxiolytics, anticonvulsives, antiemetics and antiulcerogenics.
摘要翻译：式（A）的化合物其中（A）当氨基取代基位于与碳组相对位置时，R 1为相对于羰基的o位置的氯，R 2为氢，R 3为是乙基氨基，环戊基氨基，环己基氨基，环庚基氨基，N-甲基 - 环己基氨基，苄基氨基或1-乙基 - 吡咯烷基 - （2） - 氨基甲基，或（B）当氨基取代基位于O-，对于羰基，R1是氢，氯或溴，R2是三氟甲基，硝基，或当R4是1-（1至3个碳原子的烷基） - 吡咯烷基或1-（1至3个碳原子的烷基）时， - 哌啶基，氟，氯，溴或甲基，R3是（碳原子数1〜5的烷基） - 氨基，（3〜7个碳原子的环烷基） - 氨基，苄基氨基，奎宁环基 - 氨基或-NH-（CH2） n-R4，其中R4是吡啶基，1-（1至3个碳原子的烷基） - 吡咯烷基，1-（1至3个碳原子的烷基） - 哌啶基，或当n是2或3时，也是咪唑啉基，吡咯烷子基，哌啶子基或mor pholino和N IS 0,1,2或3，以及非毒性，药理学上可接受的酸添加量; 化合物作为它们的有效的有用的ANXIOLYTICS，ANTICONVULSIVES，抗原和抗生素。

10. 发明授权

US4073942A Halo-substituted hydroxybenzyl-amines as secretolytic agents 失效
标题翻译：卤代取代的羟基苄基胺作为分泌溶剂
公开(公告)号：US4073942A
公开(公告)日：1978-02-14
申请号：US635220
申请日：1975-11-25
申请人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
发明人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
IPC分类号： A61K31/135 , C07C87/29
CPC分类号： A61K31/135 , Y10S514/849 , Y10S514/925
摘要： Compounds of the formula ##STR1## wherein X is chlorine or bromine;R.sub.1 is hydrogen, chlorine or bromine;R.sub.2 is isopropyl; tert.butyl; tert.pentyl; mono-, di- or tri-hydroxy-substituted branched alkyl of 3 to 5 carbon atoms; cyclohexyl; or hydroxycyclohexyl; andR.sub.3 is alkyl of 1 to 4 carbon atoms or, when R.sub.2 is other than cyclohexyl, also hydrogen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as secretolytics, antitussives, anti-ulcerogenics and stimulants for the production of the surfactant or anti-atelectasis factor of the alveoli.
摘要翻译：其中X是氯或溴的式“IMAGE”的化合物; R1是氢，氯或溴; R2是异丙基; 叔丁基叔戊基 3至5个碳原子的单，二或三羟基取代的支链烷基; 环己基或羟基环己基; 并且R 3是1至4个碳原子的烷基，或者当R 2不是环己基时，也是氢; 和非毒性，药理学上可接受的酸添加量; 该化合物作为其生物利用作为秘密，抗生素，抗生素和抗生素用于生产ALVEOLI的表面活性剂或抗原决定因子。

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