公开(公告)号：US4530923A

公开(公告)日：1985-07-23

申请号：US435493

申请日：1982-10-20

申请人： Jozsef Rakoczi ,  Edit Berenyi nee Poldermann ,  Bela Fekete ,  Laszlo Szekeres ,  Gyula Papp ,  Eva Keszthelyi nee Udvary

发明人： Jozsef Rakoczi ,  Edit Berenyi nee Poldermann ,  Bela Fekete ,  Laszlo Szekeres ,  Gyula Papp ,  Eva Keszthelyi nee Udvary

IPC分类号： C07D295/08 ,  A61K31/395 ,  A61K31/55 ,  A61P9/06 ,  C07D295/088 ,  C07D295/092 ,  C07D295/10 ,  C07D295/13 ,  C07D295/15 ,  C07D223/02 ,  A61K31/33

CPC分类号： C07D295/088 ,  C07D295/13 ,  C07D295/15

摘要： The invention relates to new cyclic imines of the general formula (I), ##STR1## wherein A represents carbonyl or hydroxymethylene,B is oxygen or imino,R stands for hydrogen or lower alkyl,X.sub.1 and X.sub.2 may be the same or different and represent hydrogen, halogen, lower alkyl or alkoxy, amino or nitro,n is 6 or 7, andm is 0 or 1,and pharmaceutically acceptable acid addition salts and quaternary salts thereof. The invention relates further to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds as the active ingredient and to a process for the preparation of said pharmaceutical compositions.The cyclic imine derivatives of the invention possess valuable antiarrhythmic properties and can be used to advantage in the treatment of cardiovascular diseases.

摘要翻译： 本发明涉及通式（I）的新型环状亚胺，其中A代表羰基或羟基亚甲基，B是氧或亚氨基，R代表氢或低级烷基，X 1和X 2可以相同或不同， 代表氢，卤素，低级烷基或烷氧基，氨基或硝基，n为6或7，m为0或1，以及其药学上可接受的酸加成盐和季盐。 本发明进一步涉及制备所述化合物的方法，含有所述化合物作为活性成分的药物组合物和制备所述药物组合物的方法。 本发明的环状亚胺衍生物具有有价值的抗心律失常性质，可用于治疗心血管疾病。

公开(公告)号：US4511737A

公开(公告)日：1985-04-16

申请号：US551941

申请日：1983-11-15

申请人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay ,  Zoltan Vigh ,  Agnes Sokorai

发明人： Zoltan Budai ,  Attila Kis-Tamas ,  Tibor Mezei ,  Aranka Lay ,  Zoltan Vigh ,  Agnes Sokorai

IPC分类号： A01N33/24 ,  A01N33/04 ,  A01N35/10 ,  A01P21/00 ,  C07C251/44 ,  C07C251/50 ,  C07C131/02

CPC分类号： A01N35/10

摘要： The invention relates to new bicyclo(2.2.1)heptane derivatives of the general formula I ##STR1## wherein R represents a C.sub.1-12 alkyl group optionally substituted by a lower alkoxy group, a C.sub.2-4 alkenyl group or a phenyl-(lower alkyl) group optionally substituted on (I), phenyl ring by one or more lower alkoxy groups or halogen atoms.The invention relates further to plant growth regulating compositions comprising as active agent 0.001 to 95% by weight of a racemic and/or optically active compound of the general formula I, wherein R has the above defined meanings, along with a conventional organic or inorganic, solid and/or liquid carrier and/or filler and/or diluent and/or surfactant.The invention encompasses also the preparation of the compounds of the general formula (I) which comprises reacting a racemic or optically active compound of the general formula (II) ##STR2## wherein Y is an oxygen or sulfur atom or an oxim group, with a compound of the general formula (III)R--XwhereinR is as defined above, andX represents a leaving group, preferably a halogen atom, a sulfonyloxy or an aminooxy group, with the proviso that when using a compound of the general formula (II), in which Y is an oxim group, X is other than aminooxy group,in the presence of a basic condensing agent, and optionally resolving the racemic compound of the general formula (I) obtained into its optically active antipodes.

摘要翻译： 本发明涉及通式I（I）的新型双环（2.2.1）庚烷衍生物，其中R表示任选被低级烷氧基取代的C 1-12烷基，C 2-4链烯基或苯基 - （低级烷基）基团，其任选地在（I）上取代，苯基环由一个或多个低级烷氧基或卤素原子取代。 本发明进一步涉及植物生长调节组合物，其包含作为活性剂0.001至95重量％的通式I的外消旋和/或旋光活性化合物，其中R具有上述定义的含义，以及常规的有机或无机， 固体和/或液体载体和/或填料和/或稀释剂和/或表面活性剂。 本发明还包括通式（I）的化合物的制备，其包括使通式（II）的外消旋或光学活性化合物其中Y是氧或硫原子或肟基的（II） 与通式（III）RX的化合物，其中R如上定义，X​​表示离去基团，优选卤素原子，磺酰氧基或氨基氧基，条件是当使用通式 （II），其中Y是肟基，X不是氨基氧基，在碱性缩合剂的存在下，并且任选地将通式（I）的外消旋化合物拆分成其光学活性对映体。

公开(公告)号：US4342766A

公开(公告)日：1982-08-03

申请号：US254763

申请日：1981-04-16

申请人： Edit Berenyi nee Poldermann ,  Peter Gorog ,  Katalin Grasser ,  Ibolya Kosoczky ,  Agnes Koracs nee Palotay ,  Lujza Petocz

发明人： Edit Berenyi nee Poldermann ,  Peter Gorog ,  Katalin Grasser ,  Ibolya Kosoczky ,  Agnes Koracs nee Palotay ,  Lujza Petocz

IPC分类号： A61K31/4745 ,  A61K31/53 ,  A61P23/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/20 ,  A61P29/00 ,  C07D471/04 ,  A61K31/395

CPC分类号： C07D471/04

摘要： New compounds are disclosed of the formulae ##STR1## or pharmaceutically effective salts thereof, wherein R is hydrogen, C.sub.1-12 alkyl, or R is phenyl or phenyl-C.sub.1 to C.sub.4 alkyl wherein the phenyl can be substituted with 1 to 3 halogen, C.sub.1 to C.sub.4 alkyl, or C.sub.1 to C.sub.4 alkoxy substituents; andX.sub.1, X.sub.2 and X.sub.3 are hydrogen, C.sub.1 to C.sub.6 alkanoyl, or C.sub.1 to C.sub.6 haloalkanoyl; and where X.sub.1 is hydrogen, X.sub.2 and X.sub.3 are not simultaneously hydrogen. The compounds possess antiphlogistic, analgesic, anticonvulsive, or tranquilizing properties.

摘要翻译： 公开了新的化合物或其药学有效盐，其中R是氢，C 1-12烷基或R是苯基或苯基-C 1至C 4烷基，其中苯基可被1至3个卤素取代，C 1 至C 4烷基或C 1至C 4烷氧基取代基; 且X 1，X 2和X 3为氢，C 1至C 6烷酰基或C 1至C 6卤代烷酰基; 并且其中X1为氢，X2和X3不同时为氢。 该化合物具有消炎，镇痛，抗惊厥或镇静作用。

公开(公告)号：US4316022A

公开(公告)日：1982-02-16

申请号：US135143

申请日：1980-03-28

申请人： Gyorgy Hajos ,  Andras Messmer ,  Pal Benko ,  Lujza Petocz ,  Peter Gorog ,  Ibolya Kasoczky

发明人： Gyorgy Hajos ,  Andras Messmer ,  Pal Benko ,  Lujza Petocz ,  Peter Gorog ,  Ibolya Kasoczky

IPC分类号： A61K31/53 ,  A61K31/5513 ,  A61P23/00 ,  A61P29/00 ,  C07D249/08 ,  C07D253/10 ,  C07D487/04 ,  C07D487/14 ,  C07D401/14 ,  C07D403/14

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention relates to new benzo-as-triazine derivatives of the formulae (I) and (Ia) and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 and R.sub.2 each represent hydrogen, a C.sub.1-20 alkylcarbonyl group, a phenylcarbonyl or phenyl-(C.sub.1-4 alkyl)-carbonyl group having optionally one or more halogen, hydroxy or C.sub.1-3 alkoxy substituents which may be the same or different, furthermore a pyridylcarbonyl, a pyrazinylcarbonyl, a furylcarbonyl, a chloroacetyl or a C.sub.1-4 alkoxycarbonyl group, orR.sub.1 and R.sub.2 may form, together with the adjacent nitrogen atoms, a pyrazole ring having optionally a C.sub.1-6 alkyl substituent in position 4,with the proviso that one of R.sub.1 and R.sub.2 is always different from hydrogen,R.sub.3 stands for hydrogen, mercapto group, a C.sub.1-4 alkylmercapto group, amino group, a C.sub.1-4 alkylamino group, a piperazino group having optionally an N-alkyl or 2-pyridyl substituent, a morpholino group or a piperidino group, andR.sub.4 stands for hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy group.The compounds of the formulae (I) and (Ia) are prepared by acylating the respective 2,4,5-unsubstituted 4,5-dihydro-benzo-as-triazine derivatives.The new compounds of the formulae (I) and (Ia) possess analgesic, antiphlogistic and narcosis-potentiating effects.

摘要翻译： 本发明涉及式（I）和（Ia）的新的苯并三嗪衍生物及其药学上可接受的酸加成盐，其中R 1和R 2各自代表氢， C1-20烷基羰基，具有任选一个或多个卤素的苯基羰基或苯基 - （C 1-4烷基） - 羰基，可以相同或不同的羟基或C 1-3烷氧基取代基，此外，吡啶基羰基，吡嗪基羰基， 呋喃基羰基，氯乙酰基或C 1-4烷氧基羰基，或者R 1和R 2可以与相邻的氮原子一起形成在4位具有任选的C 1-6烷基取代基的吡唑环，条件是R1和R2之一 总是不同于氢，R3代表氢，巯基，C1-4烷基巯基，氨基，C1-4烷基氨基，任选具有N-烷基或2-吡啶基取代基的哌嗪基，吗啉代基或 哌啶子基，R4代表氢，卤素， C 1-4烷基或C 1-4烷氧基。 式（I）和（Ia）的化合物通过酰化各自的2,4,5-未取代的4,5-二氢 - 苯并 - 三嗪衍生物来制备。 式（I）和（Ia）的新化合物具有镇痛，消炎和麻醉增效作用。

公开(公告)号：US4303660A

公开(公告)日：1981-12-01

申请号：US150349

申请日：1980-05-16

申请人： Edit Berenyi nee Poldermann ,  Eniko Szirt nee Kiszelly ,  Peter Gorog ,  Lujza Petocz ,  Ibolya Kosoczky ,  Agnes Kovacs nee Palotai ,  Gabriella rmos nee Lassu

发明人： Edit Berenyi nee Poldermann ,  Eniko Szirt nee Kiszelly ,  Peter Gorog ,  Lujza Petocz ,  Ibolya Kosoczky ,  Agnes Kovacs nee Palotai ,  Gabriella rmos nee Lassu

IPC分类号： A61K31/4162 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/519 ,  A61P1/00 ,  A61P1/04 ,  A61P25/04 ,  A61P29/00 ,  C07D231/16 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D231/16

摘要： The invention relates to novel pyrazolo[1,5-c]quinazoline derivatives of the general formula I ##STR1## wherein R represents a hydrogen atom, a C.sub.1-4 alkyl group or an acyl group,R.sub.1 represents a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.2-4 alkenyl group, an aralkyl group, wherein the alkyl group has 1 to 4 carbon atoms, a phenylalkenyl group, wherein the alkenyl group has 2 to 4 carbon atoms, furthermore a carboxy group or a phenyl group optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy, nitro or di(C.sub.1-4 alkyl)amino groups, orR and R.sub.1 may form together a valence bond,R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl or a phenyl group, orR.sub.1 and R.sub.2 may form together a C.sub.2-7 alkylene group,R.sub.3 represents a nitro group, an amino group, an alkylamino group, a dialkylamino group, wherein the alkyl groups have 1 to 4 carbon atoms, an alkylideneimino group, wherein the alkylidene group has 1 to 4 carbon atoms, a benzylideneimino group or an acylamino group,and pharmaceutically acceptable acid addition salts thereof.The novel compounds of the general formula I can be employed primarily as analgesic agents.

摘要翻译： 本发明涉及通式I（XIX）的新颖的吡唑并[1,5-c]喹唑啉衍生物，其中R表示氢原子，C1-4烷基或酰基，R1表示氢原子， C1-12烷基，C3-8环烷基，C2-4烯基，其中烷基具有1至4个碳原子的芳烷基，苯基烯基，其中烯基具有2至4个碳原子 此外，羧基或任选被一个或多个选自卤素，羟基，C 1-4烷氧基，硝基或二（C 1-4烷基）氨基的取代基取代的苯基，或R和R 1可以一起形成 价键，R2表示氢原子，C1-4烷基或苯基，或R1和R2可以一起形成C2-7亚烷基，R3表示硝基，氨基，烷基氨基，二烷基氨基 基团，其中烷基具有1至4个碳原子，亚烷基亚氨基，其中亚烷基具有1至4个碳 n原子，亚苄基亚氨基或酰氨基，及其药学上可接受的酸加成盐。 通式I的新化合物可以主要用作止痛剂。

公开(公告)号：US4243660A

公开(公告)日：1981-01-06

申请号：US31583

申请日：1979-04-19

申请人： Csaba Szantay ,  Lajos Novak ,  Miklos Toth ,  Jozsef Balla ,  Bela Stefko ,  Attila Kis-Tamas

发明人： Csaba Szantay ,  Lajos Novak ,  Miklos Toth ,  Jozsef Balla ,  Bela Stefko ,  Attila Kis-Tamas

IPC分类号： A01N37/02 ,  A01N49/00 ,  C07C29/10 ,  C07C41/30 ,  C07C43/15 ,  C07C43/17 ,  C07C69/145 ,  C07D309/12 ,  C07F9/54 ,  A01N25/00 ,  A01N37/06

CPC分类号： C07D309/12 ,  A01N37/02 ,  C07C29/10 ,  C07C41/30 ,  C07C43/15 ,  C07C43/17 ,  C07C67/08 ,  C07C67/293 ,  C07C69/145 ,  C07F9/5407

摘要： The invention relates to a composite insect attractant for male cabbage moths (Mamestra brassicae) containing (Z)-11-hexadecenyl acetate and (Z)-11-heptadecenyl acetate as active agents in a weight ratio of 70 to 90:80 to 1, optionally along with a liquid or solid adjuvant. An insect trap can contain the composition which is used for attracting and trapping cabbage moth. Their mating is disrupted by air permeation techniques. (Z)-11-heptadecenyl acetate is a synergistically active new compound. The composition according to the invention produces a significantly stronger stimulating reaction on male cabbage moths than the known sex lure compositions.

摘要翻译： 本发明涉及含有（Z）-11-十六碳烯基乙酸酯和（Z）-11-十七碳烯酸乙酯作为活性剂的重量比为70至90:80至1的男性白菜蛾（Mamestra brassicae）的复合昆虫引诱剂， 任选地与液体或固体佐剂一起。 昆虫陷阱可以包含用于吸引和捕获白菜蛾的组合物。 它们的交配被空气渗透技术所破坏。 （Z）-11-十七碳烯酸乙酯是协同活性的新化合物。 根据本发明的组合物比已知的性诱剂组合物对雄性白菜蛾产生显着更强的刺激反应。

公开(公告)号：US4160035A

公开(公告)日：1979-07-03

申请号：US848351

申请日：1977-11-03

申请人： Laszlo Levai ,  Gyula Mikite ,  Attila Kis-Tamas

发明人： Laszlo Levai ,  Gyula Mikite ,  Attila Kis-Tamas

IPC分类号： C07C205/42 ,  A01N9/24

CPC分类号： C07C205/42

摘要： A plant protecting composition with pesticidal effects contains an effective amount of at least one compound of the formula ##STR1## wherein R is a C.sub.1-20 alkyl group or a phenyl or phenyl-C.sub.1-3 alkylene group having optionally one or more C.sub.1-3 alkyl or halogen substituents on the phenyl ring, and a diluent in an amount necessary to make up the final weight of the composition. To kill plant pests, the composition is applied to growing plants either prior to or after emergence.

摘要翻译： 具有杀虫作用的植物保护组合物含有有效量的至少一种式（I）的化合物，其中R是C 1-20烷基或具有任选一个或多个的苯基或苯基-C 1-3亚烷基 苯基环上的C 1-3烷基或卤素取代基，以及构成组合物最终重量所需量的稀释剂。 为了杀死植物害虫，组合物在出苗之前或之后施用于生长的植物。

公开(公告)号：US4123615A

公开(公告)日：1978-10-31

申请号：US771369

申请日：1977-02-23

申请人： Laszlo Levai ,  Gyula Mikite

发明人： Laszlo Levai ,  Gyula Mikite

IPC分类号： C07B61/00 ,  B01J23/00 ,  C07C67/00 ,  C07C201/00 ,  C07C201/16 ,  C07C205/14 ,  C07C205/16 ,  C07C76/02

CPC分类号： C07C201/12 ,  C07C201/16

摘要： The invention relates to a novel process for producing the threo- and erythro-isomers of 1-phenyl-2-nitro-1,3-propanediol through the aldol-type alkaline condensation of benzaldehyde and nitroethanol, wherein the reaction mixture is acidified and, if desired, the isomers are separated from the obtained isomer mixture and the obtained isomers are transformed into each other through epimerization, characterized in that the condensation and, if desired, also the epimerization are carried out in the presence of catalytical amounts of an alkaline hydroxide.The process according to the invention makes it possible to produce 1-phenyl-2-nitro-1,3-propanediol, an intermediate of the antibiotic chloramphenicol, in high yields, and in an extremely advantageous way which can be carried out simply and economically even on an industrial scale.

摘要翻译： 本发明涉及一种通过苯甲醛和硝基乙醇的醛醇型碱性缩合生产1-苯基-2-硝基-1,3-丙二醇的苏 - 和红 - 异构体的新方法，其中反应混合物被酸化， 如果需要，将异构体与获得的异构体混合物分离，所得异构体通过差向异构体彼此转化，其特征在于缩合反应，如果需要，还可以在催化量的碱性氢氧化物存在下进行差向异构化 。

公开(公告)号：US3882177A

公开(公告)日：1975-05-06

申请号：US35771873

申请日：1973-05-07

申请人： EGYT GYOGYSZERVEGYESZETI GYAR

发明人： UJHIDY AUREL ,  SZOTYORI LASZLO ,  SZEPVOLGYI JANOS ,  HORVATH KAROLY ,  NAGY FERENC ,  ORBAN ISTVAN ,  SIMONYI ISTVAN

IPC分类号： C07C215/00 ,  C07C97/16

CPC分类号： C07C233/18

摘要： In a process for the preparation of DL-threo-1-(p-nitrophenyl)2-acetamino-1,3-propanediol from the isopropanol solution of DLthreo-1-(p-nitrophenyl)-2-acetamino-1,3-propanediol aluminiumalcoholate compounds formed in the Meerwein-PonndorfVerley reduction of p-nitro- Alpha -acetamino- Beta -hydroxypropiophenon via aqueous or aqueous-mineral acidic hydrolysis, evaporation and removal of the aluminium salt, the improvement that prior to or simultaneously with the separation of isopropanol the aluminium alcoholates formed in the reduction are hydrolyzed in the presence of the calculated amount or less, but not lower than 50 % of water, water vapour or of an equivalent amount of aqueous mineral acid solution, isopropanol is distilled out continuously, the powdery mixture of DL-threo-1-(pnitrophenyl)-2-acetamino-1,3-propanediol and aluminium oxide is treated to remove aluminium in the form of its double salt and optionally the hydrolysis is completed in this leaching step, and DL-threo-1-(p-nitrophenyl)-2-acetamino-1,3-propanediol is separated. This improved process can be carried out continuously with high yields and under optimum conditions, also making possible an almost complete recovery of isopropanol.

摘要翻译： 在DL-苏 - （对 - 硝基苯基）-2-乙酰氨基-1（对 - 硝基苯基）-2-异丙基苯胺的异丙醇溶液中制备DL-苏 - （对硝基苯基）-2-乙酰氨基-1,3-丙二醇的方法中 在Meerwein-Ponndorf-Verley中形成的3-丙二醇 - 醇铝化合物通过水或含水 - 无机酸性水解，蒸发和除去铝盐，还原对硝基-α-乙酰氨基-β-羟基 - 苯丙酮，改善了 在分离异丙醇之前或同时，还原中形成的醇铝化物在计算量或更少但不低于50％的水，水蒸气或等量的无机酸水溶液的存在下水解， 异丙醇被连续蒸馏出来，处理DL-苏 - （对 - 硝基苯基）-2-乙酰氨基-1,3-丙二醇和氧化铝的粉末混合物，以其双盐形式除去铝，任选的水解 在这个浸出步骤中完成，而DL-thre 分离出邻-1-（对硝基苯基）-2-乙酰氨基-1,3-丙二醇。

公开(公告)号：US3873542A

公开(公告)日：1975-03-25

申请号：US35617573

申请日：1973-05-01

申请人： EGYT GYOGYSZERVEGYESZETI GYAR

发明人： BERENYI NEE POLDERMANN EDIT ,  PALLOS LASZLO ,  PETOCZ LUJZA E ,  GOROG PETER ,  BUDAI ZOLTAN ,  KISZELLY ENIKO ,  BENKO PAL

IPC分类号： C07D215/18 ,  A61K31/53 ,  A61P29/00 ,  A61P31/04 ,  C07D215/42 ,  C07D471/04 ,  C07D57/34

CPC分类号： C07D471/04 ,  C07D215/42

摘要： 3-Amino-as-triazino(6,5-c)quinoline or its 1-oxide can be prepared as follows: 4-chloro-3-nitroquinoline is reacted with guanidine, the formed 4-guanidino-3-nitroquinoline is subjected to ring closure in an alkaline medium, and, if desired, the 1oxide group of the thus-obtained 3-amino-as-triazino(6,5-c)quinoline-1-oxide is split off under reductive conditions, the obtained 3-amino-1,2-dihydro-as-triazino(6,5-c)quinoline is oxidized into 3-amino-as-triazino(6,5-c)quinoline, and, if desired, any compound obtained by the above process is converted into its salt. The compounds of the invention are novel and possess valuable anti-inflammatory and antimicrobial activities.

摘要翻译： 3-氨基 - 三嗪并[6,5-c]喹啉或其1-氧化物可如下制备：将4-氯-3-硝基喹啉与胍反应，将形成的4-胍基-3-硝基喹啉 在碱性介质中闭环，如果需要，由此得到的3-氨基 - 三嗪[6,5-c] - 喹啉-1-氧化物的1-氧化物在还原条件下分离， 得到的3-氨基-1,2-二氢 - 三嗪并[6,5-c]喹啉被氧化为3-氨基 - 三嗪并[6,5-c]喹啉，如果需要， 将上述方法转化为其盐。