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.

公开(公告)号：US4599327A

公开(公告)日：1986-07-08

申请号：US557629

申请日：1983-12-02

申请人： Mihaly Nogradi ,  Dezso Korbonits ,  Agnes Gottsegen ,  Sandor Antus ,  Zsuzsa Furst ,  Jozsef Knoll ,  Jozsef Szejtli ,  Agnes Stadler ,  Gabor Kovacs ,  Katalin Marmarosi

发明人： Mihaly Nogradi ,  Dezso Korbonits ,  Agnes Gottsegen ,  Sandor Antus ,  Zsuzsa Furst ,  Jozsef Knoll ,  Jozsef Szejtli ,  Agnes Stadler ,  Gabor Kovacs ,  Katalin Marmarosi

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/715 ,  A61P1/08 ,  A61P23/00 ,  A61P23/02 ,  A61P25/02 ,  A61P25/04 ,  C07C43/178 ,  C07C43/205 ,  C07C43/23 ,  C07C59/68 ,  C07D221/12 ,  C07D311/78 ,  C07D311/80 ,  C07D311/92 ,  C07D493/10 ,  C08B37/00 ,  C08B37/16 ,  A61K31/70

CPC分类号： C07D493/10 ,  C07C309/00 ,  C07C43/1782 ,  C07C43/1785 ,  C07C43/2055 ,  C07C43/23 ,  C07C59/68 ,  C07D221/12 ,  C07D311/78 ,  C07D311/80 ,  C08B37/0015

摘要： 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.

摘要翻译： 式（1a）化合物的2,6-二-O-甲基-β-环糊精复合物其中R 2'代表C 1至C 12烷基或其中R 11为C 1至C 4的式 烷基; R 12是氢或C 1至C 4烷基; n为0或1; p为1〜4; r为1〜4; 和R 3'和R 4'各自为C1至C4烷基，或其药学上可接受的盐，具有止痛活性。

公开(公告)号：US4524068A

公开(公告)日：1985-06-18

申请号：US550478

申请日：1983-11-09

申请人： Jozsef Szejtli ,  Zsuzsanna Budai ,  Erzsebet Radvany nee Hegedus ,  Laszlo Papp ,  Gyorgy Kormoczy ,  Gabriella Pap nee Imrenyi

发明人： Jozsef Szejtli ,  Zsuzsanna Budai ,  Erzsebet Radvany nee Hegedus ,  Laszlo Papp ,  Gyorgy Kormoczy ,  Gabriella Pap nee Imrenyi

IPC分类号： A01N43/30 ,  A61K47/48 ,  C07D317/54 ,  A61K31/73

CPC分类号： B82Y5/00 ,  A01N43/30 ,  A61K47/48969 ,  C07D317/54

摘要： The invention relates to new inclusion complexes of piperonyl butoxide formed with cyclodextrin.The new complex of the invention can be prepared by reacting cyclodextrin or a solution thereof formed with water and/or an organic solvent having 1-4 carbon atoms, preferably ethanol with piperonyl butoxide or a solution thereof formed with an organic solvent having 1-4 carbon atoms, preferably ethanol at a temperature between 20.degree. C. and 90.degree. C., whereby the piperonyl butoxide is used in an amount of 0.6-1.5 moles related to 1 mole of cyclodextrin.The complexes of the present invention synergize the pesticidal effect of known insecticides and fungicides to a much higher extent of known insecticides and fungicides to a much higher extent than piperonyl butoxide used per se.

摘要翻译： 本发明涉及与环糊精形成的胡椒基丁醚的新的包合络合物。 本发明的新配合物可以通过使环糊精或其与水和/或具有1-4个碳原子的有机溶剂，优选乙醇与胡椒基丁醚形成的溶液或其形成有有机溶剂的溶液， 碳原子，优选乙醇，温度在20℃至90℃之间，其中胡椒基丁醚的用量为与1摩尔环糊精有关的0.6-1.5摩尔。 本发明的配合物与已知的杀虫剂和杀真菌剂的杀虫作用相比，已知的杀虫剂和杀真菌剂的杀虫效果比本身使用的胡椒基丁醚的效果高得多。

公开(公告)号：US4404189A

公开(公告)日：1983-09-13

申请号：US226615

申请日：1981-01-21

申请人： Gabor Kulcsar ,  Gyula Sebestyen ,  Agoston David ,  Tibor Zilahi

发明人： Gabor Kulcsar ,  Gyula Sebestyen ,  Agoston David ,  Tibor Zilahi

IPC分类号： A61K31/65 ,  A61K35/00

CPC分类号： A61K31/70 ,  A61K31/65

摘要： A synergistic antimicrobial active ingredient for a pharmaceutical or veterinary composition comprises 5 to 50 percent by weight of a primycin component which consists of a primycin fermentation product of Thermonospora galeriensis and 95 to 50 percent by weight of at least one other component selected from the group which consists of doxycyline compounds and sisomicin compounds. The doxycycline compounds are selected from the group which consists of doxycycline, salts thereof with mineral acids, and doxycycline tryclate. The sisomicin compounds are selected from the group which consists of sisomicin, substituted sisomicins with substitution at the N atom by lower alkyl, hydroxyl lower alkyl, lower aminoalkyl and lower alkanoyl, and sisomicin acid salts.

摘要翻译： 用于药物或兽医组合物的协同抗微生物活性成分包含5-50重量％的伯霉素组分，所述伯霉素组分由热霉菌属（Thermomonospora galeriensis）的伯霉素发酵产物和95至50重量％的至少一种选自以下的组中 由多西环素化合物和西索米星化合物组成。 多西环素化合物选自由多西环素，其与无机酸的盐和多西环素三环酸组成的组。 西索米星化合物选自西索霉素，在N原子被低级烷基取代的取代的西索米星，羟基低级烷基，低级氨基烷基和低级烷酰基以及西索米星酸盐组成的组。

公开(公告)号：US4357468A

公开(公告)日：1982-11-02

申请号：US288764

申请日：1981-07-31

申请人： Jozsef Szejtli ,  Bela Zsadon ,  Eva Fenyvesi ,  nee Otta; Klara Horvath ,  Ferenc Tudos

发明人： Jozsef Szejtli ,  Bela Zsadon ,  Eva Fenyvesi ,  nee Otta; Klara Horvath ,  Ferenc Tudos

IPC分类号： C08L1/00 ,  C08B11/08 ,  C08B15/00 ,  C08B37/16

CPC分类号： C08B37/0012 ,  C08B11/08

摘要： The invention relates to new sorbents of cellulose basis capable of forming inclusion complexes, as well as to a process for the preparation thereof. The new sorbents according to the invention are cellulose derivatives containing structural units of the general formula (I), ##STR1## wherein Cell is a group derived by removing m hydroxy groups from the glucose unit of the cellulose chain,m is an integer of 1 to 3,CD is a group derived by removing one hydroxy group from the .alpha., .beta. or .gamma.-cyclodextrin molecule,n is an integer of 1 to 5, andp stands for 0 or 1, which may optionally vary even within a single chain.The cellulose derivatives according to the invention are substances of loose structure, with large specific surface area and good swelling properties, which can be applied for solving the most diverse adsorption tasks. Thus e.g. the substances can be applied for the preparation of smoke filters in cigarettes, waste water purification (de-poisoning) filters, inserts for removing solvent vapors, etc., furthermore for solving specific tasks of fractionation according to molecular dimensions.

摘要翻译： 本发明涉及能够形成包合络合物的新型纤维素基质吸附剂，以及其制备方法。 根据本发明的新吸附剂是含有通式（I），Cell {[OCH 2（CHOH）pCH 2] nOCD} m（I）的结构单元的纤维素衍生物，其中Cell是从葡萄糖中除去m个羟基衍生的基团 纤维素链的单位，m为1〜3的整数，CD为从α，β或γ-环糊精分子除去一个羟基衍生的基团，n为1〜5的整数，p为0 或1，其可以任选地在单链内变化。 根据本发明的纤维素衍生物是松散结构的物质，具有大的比表面积和良好的溶胀性能，可用于解决最多样化的吸附任务。 因此，例如 该物质可用于制备香烟中的烟雾过滤器，废水净化（去中毒）过滤器，用于除去溶剂蒸气的插入物等，此外用于根据分子尺寸解决特定的分馏任务。

公开(公告)号：US4324743A

公开(公告)日：1982-04-13

申请号：US814726

申请日：1977-07-11

申请人： Laszlo Feuer ,  Arpad Furka ,  Ferenc Sebestyen ,  Jolan Hercsel nee Szepespataky ,  Erzsebet Bendefy nee Dobay

发明人： Laszlo Feuer ,  Arpad Furka ,  Ferenc Sebestyen ,  Jolan Hercsel nee Szepespataky ,  Erzsebet Bendefy nee Dobay

IPC分类号： A61K8/64 ,  A61K31/195 ,  A61K35/55 ,  A61K38/00 ,  A61Q19/00 ,  C07C237/10 ,  C07F9/09 ,  C07K14/00 ,  C07C143/02

CPC分类号： C07K14/001 ,  A61K31/195 ,  A61K35/55 ,  A61K8/44 ,  A61K8/64 ,  A61Q19/00 ,  C07C237/10 ,  C07F9/091 ,  A61K38/00 ,  A61Q11/00 ,  A61Q17/00

摘要： A process for preparing gamma-L-glutamyl-taurine, which has been found to be effective therapeutically through the control of vitamin A metabolism, which comprises reacting carbobenzyloxy-L-glutaminic acid-.alpha.-benzyl ester with triethylamine and isobutylchloroformate and then treating the reaction mixture with cystamine dihydrochloride to recover N,N'-bis-(N-carbobenzyloxy-gamma-[.alpha.-benzyl]-L-glutamyl)-cystamine. The latter is reacted with hydrogen peroxide in glacial acetic acid to produce carbobenzyloxy-gamma-(.alpha.-benzyl)-L-glutamyl taurine. The latter compound is treated with hydrogen bromide in glacial acetic acid to recover the gamma-(.alpha.-benzyl)-L-glutamyl taurine and this compound is treated with potassium hydroxide solution to yield the gamma-L-glutamyl taurine.

摘要翻译： 已经发现通过控制维生素A代谢来治疗有效的γ-谷氨酰 - 牛磺酸的制备方法，其包括使苄氧羰基-L-谷氨酸-α-苄基酯与三乙胺和氯甲酸异丁酯反应，然后将 反应混合物与胱胺二盐酸盐回收N，N'-双 - （N-苄酯基-γ-[α-苄基] -L-谷氨酰基） - 胱胺。 后者与冰醋酸中的过氧化氢反应生成苄酯基-γ-（α-苄基）-L-谷氨酰基牛磺酸。 将后一种化合物用溴化氢在冰醋酸中处理以回收γ-（α-苄基）-L-谷氨酰基牛磺酸，该化合物用氢氧化钾溶液处理，得到γ-谷氨酰基牛磺酸。

公开(公告)号：US4317920A

公开(公告)日：1982-03-02

申请号：US041106

申请日：1979-05-21

申请人： Endre Palosi ,  Dezso Korbonits ,  Pal Kiss ,  Csaba Gonczy ,  Gergely Heja ,  Judit Cser nee Kun ,  Rudolf Szebeni ,  Maria Szomor nee Wundele ,  Ida Szvoboda nee Kanzel

发明人： Endre Palosi ,  Dezso Korbonits ,  Pal Kiss ,  Csaba Gonczy ,  Gergely Heja ,  Judit Cser nee Kun ,  Rudolf Szebeni ,  Maria Szomor nee Wundele ,  Ida Szvoboda nee Kanzel

IPC分类号： C07D333/24 ,  C07B31/00 ,  C07B35/06 ,  C07C37/055 ,  C07C41/32 ,  C07C43/215 ,  C07C43/295 ,  C07C45/67 ,  C07C45/71 ,  C07C51/00 ,  C07C51/377 ,  C07C57/30 ,  C07C57/58 ,  C07C59/64 ,  C07C59/76 ,  C07C67/00 ,  C07C239/00 ,  C07C271/58 ,  C07C275/70 ,  C07C301/00 ,  C07C303/06 ,  C07C303/22 ,  C07C303/32 ,  C07C305/22 ,  C07C309/63 ,  C07C309/66 ,  C07C309/73 ,  C07C381/00 ,  C07D257/04 ,  C07D263/56 ,  C07D333/22 ,  C07C131/00 ,  C07C125/06

CPC分类号： C07C309/73 ,  C07C309/66 ,  C07C37/055 ,  C07C41/16 ,  C07C41/32 ,  C07C45/67 ,  C07C45/71 ,  C07C51/377

摘要： Arylacetic acid derivatives of the formula ##STR1## with R.sup.1, R.sup.2 and R.sup.3 specifically defined and which are useful as antirheumatic and antiinflammatory pharmaceuticals are practiced by catalytic hydrogenation of new compounds of the formula ##STR2## in which R and R.sup.10 are also specifically defined. The method of making the latter compound is also set forth.

摘要翻译： 具有R1，R2和R3特异性定义并且可用作抗风湿和抗炎药物的式“IMAGE”的芳基乙酸衍生物通过催化氢化式（IMAGE）的新化合物来进行，其中R和R 10也被具体定义。 还阐述了制备后一种化合物的方法。

公开(公告)号：US4305953A

公开(公告)日：1981-12-15

申请号：US143611

申请日：1980-04-25

申请人： Todor Pfliegel ,  Erzsebet Radvanyi nee Hegedus ,  Gizella Hamar nee Nemes ,  Andras Franko ,  Lajos Ferenczy

发明人： Todor Pfliegel ,  Erzsebet Radvanyi nee Hegedus ,  Gizella Hamar nee Nemes ,  Andras Franko ,  Lajos Ferenczy

IPC分类号： A01N47/18 ,  A01N47/34 ,  A01N47/38 ,  A61K31/415

CPC分类号： A61K31/415 ,  A01N47/18 ,  A01N47/34 ,  A01N47/38

摘要： The invention relates to new synergistic fungicidal compositions comprising a mixture of (a) methyl 2-benzimidazolecarbamate or a precursor thereof, such as methyl 1-(butylcarbamoyl)-2-benzimidazolecarbamate and 1,2-bis(3-methoxy-carbonyl-2-thioureido)benzene and (b) 1H-.alpha.-butyl-.alpha.-phenylimidazol-1-yl-propanenitrile.

摘要翻译： 本发明涉及新的协同杀真菌组合物，其包含（a）2-苯并咪唑亚氨基甲酸甲酯或其前体的混合物，例如1-（丁基氨基甲酰基）-2-苯并咪唑亚甲基氨基甲酸甲酯和1,2-双（3-甲氧基 - 羰基-2 - 硫脲基）苯和（b）1 H-α-丁基-α-苯基咪唑-1-基 - 丙腈。

公开(公告)号：US4304930A

公开(公告)日：1981-12-08

申请号：US105988

申请日：1979-12-21

申请人： Endre Palosi ,  Gergely Heja ,  Dezso Korbonits ,  Pal Kiss ,  Csaba Gonczi ,  Judit Cser nee Kun ,  Ida Szvoboda nee Kanzel ,  Gabor Szabo ,  Tamas Kallay ,  Laszlo Ledniczky ,  Maria Szomor nee Wundele

发明人： Endre Palosi ,  Gergely Heja ,  Dezso Korbonits ,  Pal Kiss ,  Csaba Gonczi ,  Judit Cser nee Kun ,  Ida Szvoboda nee Kanzel ,  Gabor Szabo ,  Tamas Kallay ,  Laszlo Ledniczky ,  Maria Szomor nee Wundele

IPC分类号： C07C63/33 ,  C07C51/00 ,  C07C51/06 ,  C07C51/09 ,  C07C59/11 ,  C07C59/68 ,  C07C255/32 ,  C07C255/53 ,  C07C51/08 ,  C07C121/78

CPC分类号： C07C255/00 ,  C07C59/68

摘要： 2-(3-Phenoxy-phenyl)-propionic acid or its pharmaceutical treatments, are prepared by hydrolyzing and partially decarboxylating ##STR1## wherein R=C.sub.1 -C.sub.6 alkyl or amino, the latter compounds being themselves new and, where R=C.sub.1 -C.sub.6 alkyl, have antiinflammatory pharmaceutical properties.

摘要翻译： 2-（3-苯氧基 - 苯基） - 丙酸或其药物处理通过水解和部分脱羧制备，其中R = C 1 -C 6烷基或氨基，后者化合物本身是新的，并且其中R = C1- C6烷基，具有抗炎药物性质。

公开(公告)号：US4226884A

公开(公告)日：1980-10-07

申请号：US756409

申请日：1977-01-03

申请人： Laszlo Feuer

发明人： Laszlo Feuer

IPC分类号： A61K8/44 ,  A61K8/64 ,  A61K31/195 ,  A61K35/55 ,  A61K38/22 ,  A61Q11/00 ,  A61K31/255 ,  C07C143/12

CPC分类号： A61K8/64 ,  A61K31/195 ,  A61K8/447 ,  A61Q11/00

摘要： A deproteinized, defatted aqueous extract of the parathyroid gland insoluble in benzene, chloroform and carbon tetrachloride is found to be L-gamma-glutamyl-taurine which has vitamin-A type activity and is generally effective for the treatment of a wide range of mammalian disorders which are directly or indirectly connected with pathological alterations of the aerobiospherical genetical adaptational system (AGAS).

摘要翻译： 发现不溶于苯，氯仿和四氯化碳的甲状旁腺脱蛋白脱脂含水提取物是具有维生素A型活性的L-谷氨酰基牛磺酸，对于治疗广泛的哺乳动物疾病通常是有效的 它们直接或间接地与空气微球基因适应系统（AGAS）的病理改变相关。