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1. 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。

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

US4214001A 1-(4-Acylamino-phenyl)-2-amino-ethanols and salts thereof 失效
标题翻译： 1-（4-酰基氨基 - 苯基）-2-氨基 - 乙醇及其盐
公开(公告)号：US4214001A
公开(公告)日：1980-07-22
申请号：US883814
申请日：1978-03-06
申请人： Gunther Engelhardt , Johannes Keck , Kruger , Klaus Noll , Helmut Pieper
发明人： Gunther Engelhardt , Johannes Keck , Kruger , Klaus Noll , Helmut Pieper
IPC分类号： A61K31/17 , A61K31/167 , A61K31/27 , A61P25/04 , A61P25/08 , C07C67/00 , C07C215/52 , C07C239/00 , C07C269/00 , C07C271/28 , C07C271/58 , C07C275/28 , C07C275/40 , A61K31/275 , C07C121/80 , C07C125/06
CPC分类号： C07C275/40
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or cyano;R.sub.2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms;R.sub.3 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 --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are each hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; andR.sub.4 is cycloalkyl of 3 to 5 carbon atoms or alkyl of 3 to 5 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds as well as the salts are useful as analgesics, uterospasmolytics and antiasthmatics.
摘要翻译：其中R1是氢，卤素或氰基的式“IMAGE”的化合物; R2是氟，氰基，三氟甲基，硝基或1-4个碳原子的烷基; R3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个碳原子的芳烷氧基或-NR5R6，其中R5和R6分别为氢， 2至5个碳原子的烯基，6至10个碳原子的芳基或7至11个碳原子的芳烷基; R4为3〜5个碳原子的环烷基或3〜5个碳原子的烷基; 和无毒的，药学上可接受的酸加成盐。化合物以及盐可用作镇痛药，子宫内膜溶解药和止喘药。

4. 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.

5. 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。

6. 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.

7. 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。

8. 发明授权

US4876302A Polyurethane dispersions and the use thereof as finishing agents 失效
标题翻译：聚氨酯分散体及其作为整理剂的用途
公开(公告)号：US4876302A
公开(公告)日：1989-10-24
申请号：US284970
申请日：1988-12-15
申请人： Klaus Noll , Wilhelm Thoma , Klaus Nachtkamp , Walter Schroer , Josef Pedain
发明人： Klaus Noll , Wilhelm Thoma , Klaus Nachtkamp , Walter Schroer , Josef Pedain
IPC分类号： C08L75/04 , C08G18/00 , C08G18/08 , C08G18/12 , C08G18/66 , C08G18/72 , C08G18/73 , C08G18/75 , C08J7/04 , C08L75/00 , C09D175/00 , C09D175/04 , C09D175/06 , C09D175/12
CPC分类号： C09D175/06 , C08G18/0819 , C08G18/12 , C08G18/6644 , C08G18/6659 , C08G18/722 , C08J7/047 , C08J2475/00
摘要： The present invention is directed to aqueous coating compositions suitable for use as coating and finishing agents for surface coatings, preferably PVC or polyurethane coatings, based on sedimentation-stable polyurethane dispersions having a solids content of about 10-70% by weight wherein the polyurethane-urea solids material is based on polyester diols, low molecular weight diols and optionally triols, chemically incorporated hydrophilic groups, specific mixtures of diisocyanates and polyamine chain extenders having an average functionality of greater than 2 and wherein the aqueous preparations additionally contain alkoxylated dimethyl-polysiloxanes and water-soluble polyethylene oxides. The present invention is also directed to a process for applying top coats and finishes to surface coatings, preferably PVC or polyurethane surface coatings, wherein the above-described aqueous coating and finishing agents are used as the top coat and the coatings are cured at about 70.degree.-170.degree. C.
摘要翻译：本发明涉及适用于基于沉积稳定的聚氨酯分散体的表面涂层（优选PVC或聚氨酯涂层）的涂层和整理剂的水性涂料组合物，其中固体含量为约10-70％（重量），其中聚氨酯 - 脲固体材料基于聚酯二醇，低分子量二醇和任选的三醇，化学引入的亲水基团，二异氰酸酯的特定混合物和平均官能度大于2的多胺扩链剂，其中所述水性制剂另外含有烷氧基化二甲基 - 聚硅氧烷，水溶性聚环氧乙烷。本发明还涉及一种将表面涂层和表面涂层施用于表面涂层，优选PVC或聚氨酯表面涂层的方法，其中上述水性涂料和整理剂用作顶涂层，并且涂层在约70℃下固化 DEG-170℃

9. 发明授权

US4871735A Naphthyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：萘衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US4871735A
公开(公告)日：1989-10-03
申请号：US96097
申请日：1987-09-11
申请人： Joachim Heider , Manfred Psiorz , Andreas Bomhard , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Jurgen Dammgen
发明人： Joachim Heider , Manfred Psiorz , Andreas Bomhard , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Jurgen Dammgen
IPC分类号： C07D209/48 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/55 , A61P9/00 , A61P9/12 , C07D209/44 , C07D209/46 , C07D217/04 , C07D217/22 , C07D217/24 , C07D223/16 , C07D491/04 , C07D491/056
CPC分类号： C07D223/16 , C07D209/44 , C07D209/46 , C07D217/04 , C07D217/24 , C07D491/04
摘要： The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen atoms, alkyl or alkoxy groups, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, particularly a heart rate lowering activity.The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的萘基衍生物，其中N表示数1或2，A表示-CH 2 - ， - CO - ， - CH 2 CH 2 - ， - CH = CH-，而标记有x的原子与苯基连接，E表示任选被烷基取代的直链亚烷基，G表示任选被烷基取代的直链亚烷基，L表示键或氧原子如果G表示任选被烷基取代的具有2至5个碳原子的直链亚烷基，则可以相同或不同的R 1和R 2表示烷基或烷氧基，或者R 1和R 2一起表示亚烷基二氧基，R 3表示氢原子或烷基或烯丙基，可以相同或不同的R 4，R 5和R 6表示氢原子，烷基或烷氧基，其对映体和酸加成盐，具有有价值的药理学性质，特别是一个心率下降活动。新化合物可以使用本身已知的方法制备。

10. 发明授权

US4576989A Aqueous solutions or dispersions of cationic oligo-urethanes, a process for the production thereof and the use thereof to produce coatings 失效
标题翻译：阳离子低聚氨酯的水溶液或分散体，其制备方法及其用于生产涂料的方法
公开(公告)号：US4576989A
公开(公告)日：1986-03-18
申请号：US701710
申请日：1985-02-14
申请人： Klaus Noll , Terry Potter , Josef Pedain , Jurgen Schwindt
发明人： Klaus Noll , Terry Potter , Josef Pedain , Jurgen Schwindt
IPC分类号： C08G18/00 , C08G18/08 , C08G18/10 , C08G18/38 , C09D5/44 , C09D5/46 , C09D175/00 , F23N3/04 , F23N5/14 , F23N5/18 , C08L75/04
CPC分类号： F23N3/042 , C08G18/0814 , C08G18/10 , C08G18/3821 , C08G18/3825 , C08G18/3838 , C09D5/4465 , F23N2025/04 , F23N2035/04 , F23N2035/06 , F23N2035/10 , F23N5/14 , F23N5/18
摘要： The present invention is directed to aqueous solutions or dispersions which may contain blocked polyisocyanates of cationic oligourethanes which are crosslinkable at elevated temperature and contain(a) about 0.1 to 3% by weight of ternary or quaternary ammonium ions introduced through Michael adducts of secondary amines having at least one hydroxyl group and specific acrylic acid derivatives,(b) up to about 2.8% by weight of tert. amino nitrogen atoms incorporated through Michael adducts of secondary amines having at least one hydroxyl group and specific acrylic acid derivatives and(c) about 0 to 15% by weight of blocked isocyanate groups, provided that the ternary ammonium groups of (a), the tert. nitrogen atoms of (b) and the blocked isocyanate groups are present in an equivalent ratio of (a+b):blocked isocyanate groups of about 1:1 to 1:1.5. The present invention is additionally directed to a process for the preparation of these solutions or dispersions of oligourethanes and to their use for coating heat resistant substrates, particularly by coating metallic substrates by cathodic electrodeposition and subsequently cross-linking these coatings at elevated temperature.
摘要翻译：本发明涉及水溶液或分散体，其可以含有阳离子低聚氨酯的封端多异氰酸酯，其可在升高的温度下可交联，并含有（a）约0.1至3重量％的通过仲胺的迈克尔加成物引入的三元或季铵离子，所述仲胺具有至少一个羟基和特定的丙烯酸衍生物，（b）至多约2.8重量％的叔丁醇。氨基氮原子通过具有至少一个羟基的仲胺的迈克尔加成物和特定的丙烯酸衍生物加入，（c）约0至15重量％的封端异氰酸酯基团，条件是（a）的三元铵基团，叔。（b）的氮原子和封端的异氰酸酯基团以（a + b）：约1：1至1：1.5的封端异氰酸酯基团的当量比存在。本发明另外涉及制备这些低聚氨酯的这些溶液或分散体的方法，以及它们用于涂覆耐热基材的用途，特别是通过阴极电沉积涂覆金属基材并随后在升高的温度下交联这些涂层。

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