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    4- or 5-Nitroimidazoles and processes for their manufacture
    1.
    发明授权
    4- or 5-Nitroimidazoles and processes for their manufacture 失效
    4-或5-硝基咪唑及其制备方法

    公开(公告)号：US3996238A

    公开(公告)日：1976-12-07

    申请号：US522567

    申请日：1974-11-11

    申请人： Atso Ilvespaa

    发明人： Atso Ilvespaa

    IPC分类号： C07D233/54 ,  C07D233/70 ,  C07D233/92 ,  C07D49/34

    CPC分类号： C07D233/92 ,  C07D233/70

    摘要： 4- or 5-nitro-imidazoles of the formula I ##SPC1##wherein one of the radicals R.sub.1 and R.sub.2 is hydrogen or lower alkyl and R.sub.2 is the nitro group or R.sub.1 is the nitro group and R.sub.2 is hydrogen or lower alkyl, R.sub.3 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkylsulphonyl-lower alkyl, dilower alkylamino-lower alkyl, lower alkylene-amino-lower alkyl, lower oxaalkyleneamino-lower alkyl, lower thiaalkyleneamino-lower alkyl or lower azaalkyleneamino lower alkyl, R.sub.4 is oxo or thioxo and R.sub.5 is a phenyl radical which optionally has one, two or more substituents, an optionally substituted furyl, thienyl, pyrrolyl, indolyl, oxazolyl, thiazolyl, thiadiazolyl, 4,5-dihydro-thiazolyl-(2), tetrahydro-thiazolyl-(2), pyrazolyl, indazolyl, imidazolyl-(5), imidazolyl-(4), pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, 1,3,5- or 1,2,4-triazinyl, pyrrolidinyl, pyrazolinyl, indolinyl, pyrazolidinyl, imidazolinyl, imidazolidinyl, piperidyl, morpholinyl, thiazinyl, thiomorpholinyl or piperazinyl radical, an optionally C-lower alkylated pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino, N'-lower alkyl-piperazino, N'-.beta.-hydroxyethyl-piperazino or pyridinium radical and R.sub.6 and R.sub.7 independently of one another denote hydrogen or lower alkyl or conjointly form the missing part of a fused benzene nucleus which is optionally substituted by lower alkyl, lower alkoxy, halogen, trifluoromethyl and/or nitro, as well as their S-oxides, sulphones N-oxides and/or acid addition salts thereof, which are useful as agents against schistosomes, filaria, trichomonades, bacteriae, and/or amoebae.

    摘要翻译： 其中基团R 1和R 2中的一个为氢或低级烷基且R 2为硝基或R 1为硝基且R 2为氢或低级烷基的式I的4-或5-硝基 - 咪唑，R 3为低级烷基， 低级烷氧基 - 低级烷基，低级烷基磺酰基 - 低级烷基，低级烷基氨基 - 低级烷基，低级亚烷基 - 氨基 - 低级烷基，低级亚烷基氨基 - 低级烷基，低级亚烷基氨基 - 低级烷基，低级亚烷基氨基 - 低级烷基， 氧代或硫代，R5是任选具有一个，两个或更多个取代基的苯基，任选取代的呋喃基，噻吩基，吡咯基，吲哚基，恶唑基，噻唑基，噻二唑基，4,5-二氢 - 噻唑基 - （2） 噻唑基 - （2），吡唑基，吲唑基，咪唑基 - （5），咪唑基 - （4），吡啶基，吡嗪基，嘧啶基，哒嗪基，1,3,5-或1,2,4-三嗪基，吡咯烷基，吡唑啉基， ，吡唑烷基，咪唑啉基，咪唑烷基，哌啶基，吗啉基，噻嗪基，硫代吗啉基或哌嗪基 1，任选的C低级烷基化吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代，哌嗪子基，N'-低级烷基 - 哌嗪基，N'-β-羟基乙基 - 哌嗪基或吡啶鎓基，R 6和R 7彼此独立地表示氢或低级烷基 或共同形成任选被低级烷基，低级烷氧基，卤素，三氟甲基和/或硝基取代的稠合苯核心的缺失部分，以及它们的S-氧化物，砜氧化物和/或其酸加成盐， 它们可用作抗血吸虫，丝丝虫，毛滴虫，细菌和/或变形虫的药剂。

    2-(Pyrrol-1-yl)amino-4,5-dihydro-1H-imidazole derivatives
    2.
    发明授权
    2-(Pyrrol-1-yl)amino-4,5-dihydro-1H-imidazole derivatives 失效
    2-（吡咯-1-基）氨基-4,5-二氢-1H-咪唑衍生物

    公开(公告)号：US3979408A

    公开(公告)日：1976-09-07

    申请号：US473038

    申请日：1974-05-24

    申请人： Aldo Trani

    发明人： Aldo Trani

    IPC分类号： C07D403/12 ,  C07D233/52 ,  C07D239/18 ,  C07D49/34

    CPC分类号： C07D233/52 ,  C07D239/18

    摘要： 2-(Pyrrol-1-yl)amino-4,5-dihydro-1H-imidazole derivatives of the following general formula I ##SPC1##wherein R, R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are independently selected from the class consisting of hydrogen, lower alkyl, carbo-lower alkoxy, phenyl, substituted phenyl, R.sub.4 represents hydrogen or lower alkyl, n is an integer and may be 2 or 3. The corresponding pharmaceutically acceptable acid addition salts of the substances of formula I above are considered as a part of the invention. The invention compounds display very interesting anthypertensive properties.

    摘要翻译： 2-（吡咯-1-基）氨基-4,5-二氢-1H-咪唑衍生物，其中R，R 1，R 2和R 3可以相同或不同，并且独立地选自 氢，低级烷基，碳 - 低级烷氧基，苯基，取代的苯基，R4代表氢或低级烷基，n是整数，可以是2或3.上述式Ⅰ的物质的相应药学上可接受的酸加成盐被认为是 本发明的一部分。 本发明化合物显示出非常有趣的沉默性质。

    2-Amino-1-(2-imidazolin-2-yl)-2-imidazolines
    6.
    发明授权
    2-Amino-1-(2-imidazolin-2-yl)-2-imidazolines 失效
    2-氨基-1-（2-咪唑啉-2-基）-2-咪唑啉

    公开(公告)号：US3927022A

    公开(公告)日：1975-12-16

    申请号：US41456173

    申请日：1973-11-07

    申请人： WARNER LAMBERT CO

    发明人： WITTEKIND RAYMOND R ,  SHAVEL JR JOHN

    IPC分类号： C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D233/50 ,  C07D49/34

    CPC分类号： C07D233/48 ,  C07D233/42 ,  C07D233/46 ,  C07D233/50

    摘要： The present invention relates to 2-amino-1-(2-imidazolin-2-yl)2-imidazolines, the free base of which has the following structural formulas:

    WHEREIN R1 is hydrogen, lower alkyl, cycloaklyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic or aryloxy; R2 is hydrogen, lower alkyl, aryl and substituted aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached form a heterocyclic ring; R3 and R4 are hydrogen, lower alkyl, aryl, or substituted aryl; R5 is hydrogen, lower alkyl, aryl or substituted aryl; N IS AN INTEGER FROM 0 TO 10. The compounds of this invention are useful as antiarrhythmic agents as well as antibacterial agents.

    摘要翻译： 本发明涉及2-氨基-1-（2-咪唑啉-2-基）-2-咪唑啉，其游离碱具有以下结构式：

    Organic polyisocyanates and method of making them
    7.
    发明授权
    Organic polyisocyanates and method of making them 失效
    有机多异氰酸酯及其制备方法

    公开(公告)号：US3912754A

    公开(公告)日：1975-10-14

    申请号：US47612174

    申请日：1974-06-03

    申请人： BAYER AG

    发明人： FINDEISEN KURT ,  WAGNER KUNO

    IPC分类号： C07D233/96 ,  C08G18/00 ,  C08G18/78 ,  C08G18/79 ,  C07D49/34

    CPC分类号： C07D233/96 ,  C08G18/7887

    摘要： Organic polyisocyanates which are a reaction product of an excess of an organic polyisocyanate and hydrocyanic acid have the formula

    in which R represents an aliphatic C2 to C12 cycloaliphatic C4 to C15, aromatic C6 to C15 or araliphatic C7 to C15 hydrocarbon radical, and X represents hydrogen or a group of the formula

    wherein R has the same meaning as above. The compounds are useful in the production of polyurethanes.

    摘要翻译： 作为过量的有机多异氰酸酯和氢氰酸的反应产物的有机多异氰酸酯具有下式：其中R代表脂族基团，其中R代表脂族基团 C 2 -C 12脂环族C 4至C 15，芳族C 6至C 15或芳脂族C 7至C 15烃基，X表示氢或式-C-NH-R-NCO PARALLEL O基团，其中R具有与上述相同的含义。

    1-Halophenyl-2-imino-imidazolidines
    8.
    发明授权
    1-Halophenyl-2-imino-imidazolidines 失效
    1-卤代苯基-2-亚氨基 - 咪唑烷

    公开(公告)号：US3894039A

    公开(公告)日：1975-07-08

    申请号：US27869972

    申请日：1972-08-07

    申请人： BAYER AG

    发明人： HILTMANN RUDOLF ,  WOLLWEBER HARTMUND ,  HERMANN GUNTHER

    IPC分类号： A01N43/50 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D49/30 ,  C07D49/34

    CPC分类号： C07D233/46 ,  C07D233/42 ,  C07D233/48

    摘要： 1-HALOPHENYL-2-IMINO-IMIDAZOLIDINES OF THE FORMULA

    IN WHICH Hal is halogen, R is hydrogen, halogen, lower alkyl, lower alkoxy or halo-lower alkyl, R'' and R'''' each independently is hydrogen or alkyl of one to six carbon atoms, and N IS 1, 2, 3 OR 4, AND THEIR SALTS, WHICH POSSESS BIRD REPELLENT PROPERTIES.

    摘要翻译： 其中Hal是卤素，R是氢，卤素，低级烷基，低级烷氧基或卤素 - 低级烷基，式中R'和R“各自独立地是氢或一个烷基的烷基， 六个碳原子和N个IS 1,2,3或4，以及它们的销售，具有良好的性能。

    2-Imidazolinyl-3-oxide-1-oxypropionic acid
    10.
    发明授权
    2-Imidazolinyl-3-oxide-1-oxypropionic acid 失效
    2-咪唑啉-3-氧化物-1-氧代丙酸

    公开(公告)号：US3873564A

    公开(公告)日：1975-03-25

    申请号：US28716872

    申请日：1972-09-07

    申请人： SYNVAR ASS

    发明人： SCHNEIDER RICHARD S ,  ULLMAN EDWIN F

    IPC分类号： C07C45/67 ,  C07C51/29 ,  C07C65/30 ,  C07D213/51 ,  C07D213/55 ,  C07F9/6506 ,  C08B33/00 ,  C12Q1/00 ,  C12Q1/34 ,  C12Q1/42 ,  G01R33/28 ,  C07D49/34

    CPC分类号： G01R33/281 ,  C07C45/673 ,  C07C51/29 ,  C07C65/30 ,  C07D213/51 ,  C07D213/55 ,  C07F9/6506 ,  C08B33/00 ,  C12Q1/00 ,  C12Q1/34 ,  C12Q1/42 ,  C12Q2334/00 ,  G01N2333/916 ,  Y10T436/24 ,  C07C49/747

    摘要： Compounds and method for assaying enzymes by adding to a medium containing an enzyme a stable free radical compound having a stable free radical functionality, bonded directly or indirectly to an enzyme labile functionality, which when subjected to an enzyme catalyzed reaction changes the environment of the free radical functionality. By following the change in the electron spin resonance (ESR) spectrum as affected by the change in environment, the type of enzyme and activity of enzyme may be determined. The compounds which find use in this invention are normally stable nitroxide radicals. Particularly, nitronyl nitroxides, with the nitrogens in an imidazoline ring are employed, having a methylene group joining the 2 position of the imidazoline ring with an asymmetric carbon atom. One of the groups bonded to the asymmetric carbon atoms has an enzyme labile functionality. Other compounds include two cyclic nitroxide containing rings joined by a chain having an enzyme labile functionality.

    摘要翻译： 通过向含有酶的培养基中添加具有稳定的自由基官能团的稳定的自由基化合物，直接或间接地结合于酶不稳定官能团的酶来测定酶的化合物和方法，其在进行酶催化反应时改变游离的环境 激进的功能。 通过遵循由环境变化影响的电子自旋共振（ESR）光谱的变化，可以确定酶的类型和酶的活性。