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11. 发明授权

US4362875A Process for preparing (1-acylaminomethyl)-1,2,3,4-tetrahydroisoquinolines 失效
标题翻译：（1-酰氨基甲基）-1,2,3,4-四氢异喹啉的制备方法
公开(公告)号：US4362875A
公开(公告)日：1982-12-07
申请号：US967046
申请日：1978-12-06
申请人： Jurgen Seubert
发明人： Jurgen Seubert
IPC分类号： C07D217/06 , C07D217/14 , C07D217/16 , C07D405/12 , C07D471/04 , A61K31/47
CPC分类号： C07D471/04 , C07D217/14
摘要： Novel tetrahydroquinolines of the formula ##STR1## wherein R is cycloalkyl or cycloalkenyl each containing 4-7 ring carbon atoms and the cycloalkyl optionally being substituted by one of methyl, hydroxyl or oxo; phenyl substituted by 1-2 of amino, acylamino of up to 4 carbon atoms, Hal, hydroxyl, methoxy or nitro, wherein Hal is fluorine, chlorine, bromine or iodine; thienyl; pyridyl; tetrahydropyranyl; tetrahydrothiopyranyl; and when at least one of R.sup.2, R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is other than H, also phenyl; R.sup.2, R.sup.3 and R.sup.4 each are H or methyl; R.sup.5 and R.sup.6 each are H, methyl or methoxy; R.sup.7 is H or --CO--CH.sub.2 --X wherein X is chlorine, bromine or iodine; the acid addition salts thereof; which compounds are useful as antihelmintics and as intermediates for the production of 2-acyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives; and the corresponding compounds wherein R is alkyl of 1-6 carbon atoms, phenyl substituted by three of the substituents named above, and phenyl when all of R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H; are produced by acylating the corresponding 1-aminomethyl-1,2,3,4-tetrahydroisoquinoline wherein R.sup.7 is H, and optionally thereafter reducing the R group and/or reacting the ring nitrogen atom with an acylating group.
摘要翻译：其中R是环烷基或环烯基，其各自含有4-7个环碳原子，并且所述环烷基任选被甲基，羟基或氧代中的一个取代; 由1-2个氨基取代的苯基，至多4个碳原子的酰基氨基，Hal，羟基，甲氧基或硝基，其中Hal是氟，氯，溴或碘; 噻吩基吡啶基四氢吡喃基; 四氢噻喃基; 并且当R 2，R 3，R 4，R 5或R 6中的至少一个不是H时，也是苯基; R2，R3和R4各自为H或甲基; R5和R6各自为H，甲基或甲氧基; R7是H或-CO-CH2-X，其中X是氯，溴或碘; 其酸加成盐; 哪些化合物可用作抗肠上皮素，以及作为制备2-酰基-4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉衍生物的中间体; 以及当R2，R3，R4，R5和R6全部为H时，其中R为1-6个碳原子的烷基，被三个上述取代基取代的苯基和苯基的相应化合物; 通过酰化相应的其中R7是H的1-氨基甲基-1,2,3,4-四氢异喹啉，然后任选地还原R基团和/或使环氮原子与酰化基团反应来制备。

12. 发明授权

US4162314A 7[2(Substituted phenyl)2-(amino)acetamido]cephalosporin derivatives 失效
标题翻译： 7 {8 2（取代苯基）2-（氨基）乙酰氨基{9头孢菌素衍生物
公开(公告)号：US4162314A
公开(公告)日：1979-07-24
申请号：US806241
申请日：1977-06-13
申请人： Rudolf Gottschlich , Rolf Gericke , Horst Juraszyk , Jurgen Seubert , Wighard Strehlow , Helmut Wahlig , Rolf Bergmann , Elvira Dingeldein
发明人： Rudolf Gottschlich , Rolf Gericke , Horst Juraszyk , Jurgen Seubert , Wighard Strehlow , Helmut Wahlig , Rolf Bergmann , Elvira Dingeldein
IPC分类号： A61K20060101 , A61K31/165 , A61K31/395 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07B20060101 , C07D499/48 , C07D499/64 , C07D499/68 , C07D501/20 , C07D501/22 , C07D501/32 , C07D501/36 , C07D501/60
CPC分类号： C07D501/20 , C07D499/68
摘要： Novel .beta.-lactam antibiotics are compounds of the formula: ##STR1## wherein R is alkyl of up to 6 carbon atoms or, when A is oxygen, R is hydrogen; A is oxygen or --OCO--; Z is ##STR2## R.sup.1 is hydrogen, acetoxy or S-Het; Het is 1,2,3-triazol-5-yl, 1-methyltetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl; and n is an integer from 0 to 8; or a readily-cleavable ester or physiologically-acceptable salt thereof.
摘要翻译：新型β-内酰胺抗生素是下式的化合物：其中R是至多6个碳原子的烷基，或当A是氧时，R是氢; A是氧或-OCO-; Z是氢，乙酰氧基或S-Het; Het是1,2,3-三唑-5-基，1-甲基四唑-5-基，1,3,4-噻二唑-2-基或2-甲基-1,3,4-噻二唑-5-基; 且n为0至8的整数; 或易裂解的酯或其生理上可接受的盐。

13. 发明授权

US4141978A 2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the preparation thereof 失效
标题翻译： 2-酰基-4-氧代 - 吡嗪并 - 异喹啉衍生物及其制备方法
公开(公告)号：US4141978A
公开(公告)日：1979-02-27
申请号：US742133
申请日：1976-11-15
申请人： Jurgen Seubert , Herbert Thomas , Peter Andrews
发明人： Jurgen Seubert , Herbert Thomas , Peter Andrews
IPC分类号： C07D217/14 , C07D241/36 , A61K31/495
CPC分类号： C07D217/14
摘要： 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.

14. 发明授权

US4001411A 2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the preparation thereof 失效
标题翻译： 2-乙酰-4-氧代 - 吡咯并 - 异喹啉衍生物及其制备方法
公开(公告)号：US4001411A
公开(公告)日：1977-01-04
申请号：US533467
申请日：1974-12-16
申请人： Jurgen Seubert , Herbert Thomas , Peter Andrews
发明人： Jurgen Seubert , Herbert Thomas , Peter Andrews
IPC分类号： C07D471/14 , A23K1/16 , A61K31/4745 , A61K31/495 , A61P9/00 , A61P25/00 , A61P33/10 , C07D217/14 , C07D471/04 , C07D241/36
CPC分类号： C07D471/04 , C07D217/14
摘要： 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.

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