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    Amidino-hydrazone derivatives
    41.
    发明授权
    Amidino-hydrazone derivatives 失效
    脒基腙衍生物

    公开(公告)号：US4076726A

    公开(公告)日：1978-02-28

    申请号：US579633

    申请日：1975-05-21

    Applicant: Harm Jan Panneman ,  Antonius Hermanus Nicolaas Maria Bruins

    Inventor： Harm Jan Panneman ,  Antonius Hermanus Nicolaas Maria Bruins

    IPC: C07C67/00 ,  C07C281/18 ,  C07C313/00 ,  C07C323/44 ,  C07D233/52 ,  C07D239/18 ,  C07C123/00 ,  C07D317/44

    CPC classification number: C07C281/18 ,  C07D233/52

    Abstract: The invention relates to novel amidino-hydrazone derivatives of the general formula: ##STR1## in which the dotted lines mean one extra bond starting from the (guanidine-) carbon atom to one of the adjacent nitrogen atoms, andA stands for methylene, ethylene, propylene or butylene, which groups may optionally be substituted with alkyl (1-4 C),R stands for hydroxy, alkyl (1-4 C), alkylthio or alkoxy (1-4 C), halogen, trifluoromethyl, nitro, amino, hydroxymethyl, acyloxy or an alkylenedioxy group,N is the number 0, 1, 2, 3 or 4,R.sub.1, r.sub.4 and R.sub.5 represent hydrogen or alkyl (1-4 C), with the proviso that one of them is absent in view of the presence of the double bond,R.sub.2 and R.sub.3 stand for hydrogen, alkyl (1-4 C), aralkyl, aryl, hydroxy or amino, with the proviso thatR.sub.2 + r.sub.3 together may also represent a saturated or unsaturated alkylene group with 2 or 3 carbon atoms, orR.sub.3 + r.sub.4 together with the nitrogen atom may also stand for a heterocyclic five- or six-membered ring,As well as the pharmaceutically acceptable acid addition salts thereof, having valuable, antihypertensive and antithrombosis activities.

    Abstract translation: 本发明涉及以下通式的新颖的脒基腙衍生物：其中虚线表示从（胍） - 碳原子到相邻的氮原子之一起始的一个额外的键，A代表亚甲基， 乙烯，丙烯或丁烯，这些基团可以任选被烷基（1-4C）取代，R代表羟基，（1-4C）烷基，烷硫基或烷氧基（1-4C），卤素，三氟甲基，硝基， 氨基，羟甲基，酰氧基或亚烷基二氧基，N为0,1,2,3或4，R1，R4和R5代表氢或烷基（1-4C），条件是其中一个不存在于 双键存在的观点，R2和R3代表氢，烷基（1-4C），芳烷基，芳基，羟基或氨基，条件是R2 + R3一起也可以表示饱和或不饱和的亚烷基与 2或3个碳原子或R3 + R4与氮原子一起也可以代表杂环五元或六元环，就像P 具有良好的可接受的酸添加剂，具有有价值，抗生素和抗凝血活性。

    N,N'-disubstituted halophenylacetamidines
    43.
    发明授权
    N,N'-disubstituted halophenylacetamidines 失效
    N，N {40-二取代的卤代苯乙酰胺

    公开(公告)号：US4029703A

    公开(公告)日：1977-06-14

    申请号：US657335

    申请日：1976-02-11

    Applicant: James R. McCarthy, Jr.

    Inventor： James R. McCarthy, Jr.

    IPC: A61K31/155 ,  C07C123/00

    CPC classification number: A61K31/155

    Abstract: N,N'-Disubstituted halophenylacetamidine compounds such as N,N'-dimethyl-3,4-dichlorophenyl-acetamidine, and their pharmaceutically-acceptable salts are prepared by the reaction of a substituted phenylacetonitrile with an alkylamine and alkylammonium salt or alternatively, by reaction of the acetonitrile or corresponding N-alkylphenylacetamide with a trialkyloxonium fluoroborate followed by reaction with a primary alkylamine.The compounds have pharmacological activity as antidepressants and antianxiety or calming agents.

    Abstract translation: N，N'-二取代的卤代苯基脒化合物如N，N'-二甲基-3,4-二氯苯基 - 乙脒及其药学上可接受的盐是通过取代的苯基乙腈与烷基胺和烷基铵盐的反应或者由 乙腈或相应的N-烷基苯基乙酰胺与三烷基氧氟硼酸酯反应，然后与伯烷基胺反应。该化合物具有作为抗抑郁药和抗焦虑剂或镇定剂的药理活性。

    Acaricidal and lepidoptericidal active carbon-imidothioates
    45.
    发明授权
    Acaricidal and lepidoptericidal active carbon-imidothioates 失效
    杀螨和杀虫螨活性碳酰亚胺硫代磷酸酯

    公开(公告)号：US3992447A

    公开(公告)日：1976-11-16

    申请号：US623844

    申请日：1975-10-20

    Applicant: George B. Large

    Inventor： George B. Large

    IPC: C07C335/32 ,  C07C123/00

    CPC classification number: C07C335/32

    Abstract: Carbon-imidothioates having the formula ##SPC1##Wherein R.sub.1 is selected from the group consisting of alkyl containing from 1 to 4 carbon atoms, alkynyl containing from 1 to 4 carbon atoms, alkoxy alkylene containing from 2 to 4 carbon atoms and benzyl, and R.sub.2 is either --CH.sub.3 or --H, are active acaricides and lepidoptericides which can be applied to acarids or lepidoptera at any stage of development.

    Abstract translation: 具有式+ q，10的碳酰亚氨基硫代酯，其中R 1选自含有1至4个碳原子的烷基，含有1至4个碳原子的炔基，含有2至4个碳原子的烷氧基亚烷基和苄基，以及 R2是-CH3或-H，是可以在任何发展阶段应用于螨虫或鳞翅目的活性杀螨剂和杀螨剂。

    Amidoxime derivatives and process for preparing the same
    46.
    发明授权
    Amidoxime derivatives and process for preparing the same 失效
    偕胺肟衍生物及其制备方法

    公开(公告)号：US3984470A

    公开(公告)日：1976-10-05

    申请号：US599355

    申请日：1975-07-28

    Applicant: Fernand Binon ,  Pierre Luc Eymard

    Inventor： Fernand Binon ,  Pierre Luc Eymard

    IPC: C07D307/79 ,  C07D307/86 ,  C07C123/00

    CPC classification number: C07D307/79 ,  C07D307/86

    Abstract: Amidoxime derivatives corresponding to the general formula: ##EQU1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 and R.sub.2, which are the same or different, represent hydrogen or a straight-chain lower alkyl radical containing from 1 to 3 carbon atoms, n is 0, 1 or 2 and R is selected from the groups consisting of: ##SPC1##Wherein X represents oxygen or sulphur, Y . . . Z represents HC--CH or C=C, R.sub.3 and R.sub.4, which are the same or different, represent hydrogen or a branched- or straight-chain lower alkyl radical containing from 1 to 3 carbon atoms with the provisos that:A. when n is 1, R.sub.1 and R.sub.2 are each hydrogen and R is selected from the groups A, B, C and D.b. when n is 2, R.sub.1 and R.sub.2 area each hydrogen and R is selected from the groups A, B, C and the group D when it represents .beta.-naphthyl.They are effective as antidepressive and antiaggressive agents.

    Abstract translation: 对应于通式为：NOHR1 PARALLEL | H2N-C-（CH2）nCOR | R2的偕胺肟衍生物及其药学上可接受的酸加成盐，其中相同或不同的R 1和R 2表示氢或直链低级烷基 含有1至3个碳原子的基团，n为0,1或2，R选自：

    Process for preparing new amidine compounds
    49.
    发明授权
    Process for preparing new amidine compounds 失效
    制备新的脒化合物的方法

    公开(公告)号：US3932492A

    公开(公告)日：1976-01-13

    申请号：US521855

    申请日：1974-11-07

    Applicant: Yoshiaki Inamoto ,  Koji Aigami

    Inventor： Yoshiaki Inamoto ,  Koji Aigami

    IPC: A01N37/52 ,  C07C67/00 ,  C07C239/00 ,  C07C257/16 ,  C07C123/00

    CPC classification number: C07C205/45

    Abstract: New amidine compounds of formula (I): ##EQU1## wherein R represents ##SPC1##(R' being H or CH.sub.3) and acid addition salts thereof, are prepared by reacting a nitrile of formula (II):R -- CN (II)wherein R represents ##SPC2##(R' being H or CH.sub.3) with a metal amide or with an alcohol and an acid under anhydrous conditions and the product thus obtained is reacted with ammonia.

    Abstract translation: 式（I）的新的脒化合物：其中R表示（R'为H或CH 3）的NH RC ANGLE（I）NH 2及其酸加成盐通过使式（II）的腈：R-CN（II ）其中R表示（R'为H或CH 3）与金属酰胺或与醇和酸在无水条件下反应，得到的产物与氨反应。

    Method of preparing O-methyl-isourea hydrogen sulfate and O-methyl-isourea sulfate from cyanamide
    50.
    发明授权
    Method of preparing O-methyl-isourea hydrogen sulfate and O-methyl-isourea sulfate from cyanamide 失效
    从氨腈制备O-甲基 - 异硫脲硫酸盐和O-甲基 - 异硫脲硫酸盐的方法

    公开(公告)号：US3931316A

    公开(公告)日：1976-01-06

    申请号：US533870

    申请日：1974-12-18

    Applicant: Stefan Weiss

    Inventor： Stefan Weiss

    IPC: C07C273/00 ,  C07C275/70 ,  C07C123/00

    CPC classification number: C07C273/00

    Abstract: O-Methyl-isourea hydrogen sulfate is prepared from cyanamide, methanol, and sulfuric acid in a yield of better than 90% when crystalline cyanamide is added to a mixture of sulfuric acid and methanol containing 50 - 150 parts by weight methanol per part sulfuric acid and holding the resulting composition at -10.degree. to 20.degree.C. The recovered O-methyl-isourea hydrogen sulfate is further converted to O-methyl-isourea sulfate with yields greatly exceeding 50%, and even 80%, by holding a mixture of approximately equimolar amounts of cyanamide and of the hydrogen sulfate in a liquid medium essentially consisting of methanol at 5.degree. to 40.degree.C until the O-methyl-isourea sulfate is formed and can be recovered.

    Abstract translation: 当将结晶氰胺加入含有50-150重量份甲醇/硫酸的硫酸和甲醇的混合物中时，由氰胺，甲醇和硫酸制备O-甲基异硫脲硫酸盐，收率高于90％ 并将所得组合物保持在-10℃至20℃。回收的O-甲基 - 异硫脲硫酸盐进一步转化为O-甲基 - 异硫脲硫酸盐，产率大大超过50％，甚至80％，通过保持 在基本上由5至40℃的甲醇组成的液体介质中，大约等摩尔量的氰胺和硫酸氢盐直到形成O-甲基 - 异硫脲硫酸盐并且可以回收。

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