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1. 发明授权

US4748175A Pyrimido[5,4-B][1,4]oxazine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US4748175A
公开(公告)日：1988-05-31
申请号：US947700
申请日：1986-12-30
申请人： Endre Kasztreiner , Gyorgy Rabloczky , Nandor Makk , Gyorgy Cseh , Maria Kuhar nee Kurthy , Eszter Diesler , Laszlo Jaszlits , Laszlo Sebestyen , Janos Wellmann , Aniko Tegdes , Judit Sarossy nee Kincsesy , Peter Matyus , Andras Varro , Laszlo Szam , Sarolta Vegvari nee Gyurki
发明人： Endre Kasztreiner , Gyorgy Rabloczky , Nandor Makk , Gyorgy Cseh , Maria Kuhar nee Kurthy , Eszter Diesler , Laszlo Jaszlits , Laszlo Sebestyen , Janos Wellmann , Aniko Tegdes , Judit Sarossy nee Kincsesy , Peter Matyus , Andras Varro , Laszlo Szam , Sarolta Vegvari nee Gyurki
IPC分类号： A61K31/535 , A61K31/5383 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D498/04
CPC分类号： C07D498/04
摘要： The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.1-4 alkyl or benzyl group; furtherNR.sup.5 R.sup.6 may also represents a 6-membered, saturated, nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.2-4 alkoxycarbonyl or C.sub.1-4 hydroxyalkyl group;R.sup.3 and R.sup.4 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group;R.sup.9 stands for hydrogen or a C.sub.1-4 alkyl group unsubstituted or monosubstituted by an oxo, cyano, aminocarbonyl, C.sub.2-5 alkoxycarbonyl, pyridiyl, morpholinocarbonyl, or phenyl group or mono- or polysubstituted by OH group(s), with the proviso that R.sup.2 is different from chlorine, 4-morpholinyl and piperidyl group when R.sup.9 stands for hydrogen; orR.sup.2 is different from chlorine and 4-morpholinyl group when R.sup.9 stands for a methyl or benzyl group.The compounds of the formula (I) are capable to increase the myocardial contractile force (the performance of the failing heart) and the coronary blood flow, thus they can therapeutically be used for the treatment of the chronic heart failure and coronary disturbances.

2. 发明授权

US06245921B1 Process for the isolation of pseudomonic acid A from pseudomonic acid complex-containing culture broth 失效
标题翻译：用于从含有假单胞菌酸的复合物的培养液中分离假单胞菌酸A的方法
公开(公告)号：US06245921B1
公开(公告)日：2001-06-12
申请号：US09497806
申请日：2000-02-03
申请人： Istvan Barta , Aniko Tegdes , Valeria Szell , Csaba Szabo , Edit Nagy Nee Arvai , Vilmos Keri , David Leonov , IIdiko Lang , Margit Bidlo Nee Igloy , Gyula Jerkovich , Janos Salat
发明人： Istvan Barta , Aniko Tegdes , Valeria Szell , Csaba Szabo , Edit Nagy Nee Arvai , Vilmos Keri , David Leonov , IIdiko Lang , Margit Bidlo Nee Igloy , Gyula Jerkovich , Janos Salat
IPC分类号： C07D31500
CPC分类号： C12P17/162
摘要： A process for the isolation of the pseudomonic acid A antibiotic of pharmaceutical quality from the culture broth of one of the pseudomonic acid A-producing species of the Pseudomonas bacterium genus comprising the extraction of the biosynthesized pseudomonic acid A from the culture broth at acidic pH with a chlorinated aliphatic hydrocarbon or isobutyl acetate, followed by purification, is disclosed. The invention includes processes for purification of the isolated pseudomonic acid A, including (a) by the distribution of the evaporated extract residue between the aqueous-alcohol and some aliphatic or aromatic hydrocarbon, and then the extraction of the increased water-containing aqueous-alcoholic phase with methylene chloride, ethyl acetate, or isobutyl acetate; (b) by the extraction of the extract with aqueous ammonium hydrogen carbonate, alkali metal hydroxide or ammonium hydroxide solution and the acidification of the resulting alkaline aqueous extract, then reextraction again with a chlorinated aliphatic hydrocarbon or isobutyl acetate; and (c) by the concentration of the extract and the recrystallization of the crystalline pseudomonic acid A in a mixture of isobutyl acetate and petroleum ether, or acetonitrile, or aqueous acetonitrile.
摘要翻译：从假单胞菌属的假单胞菌素A产生物种之一的培养液中分离出假单胞菌A抗生素药物质量的方法，包括在酸性pH下从培养液中提取生物合成的假单胞菌酸A，公开了氯化脂族烃或乙酸异丁酯，然后纯化。本发明包括纯化分离的假单胞菌酸A的方法，包括（a）通过在含水醇和某些脂族或芳族烃之间分配蒸发的提取物残渣，然后提取含水的含水醇与二氯甲烷，乙酸乙酯或乙酸异丁酯反应; （b）通过用碳酸氢铵水溶液，碱金属氢氧化物或氢氧化铵溶液萃取提取物，并将得到的碱性水提取物酸化，然后用氯化脂族烃或乙酸异丁酯再次萃取; 和（c）通过提取物的浓度和结晶假单胞菌酸A在乙酸异丁酯和石油醚或乙腈或乙腈水溶液的混合物中的重结晶。

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