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    Cyclopropylmethyl piperazines, the process for preparing the same and their use in therapeutics
    44.
    发明授权
    Cyclopropylmethyl piperazines, the process for preparing the same and their use in therapeutics 失效
    环丙基甲基哌嗪，其制备方法及其在治疗中的应用

    公开(公告)号：US4474783A

    公开(公告)日：1984-10-02

    申请号：US305752

    申请日：1981-09-25

    申请人： Max F. Robba ,  Michel E. Aurousseau

    发明人： Max F. Robba ,  Michel E. Aurousseau

    IPC分类号： C07D295/02 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D241/04 ,  C07D295/03 ,  C07D295/06 ,  C07D295/073 ,  C07D295/08 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/12 ,  C07D295/14 ,  C07D295/15 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D317/68 ,  C07D409/06 ,  C07D295/00

    CPC分类号： C07D295/185 ,  C07D295/03 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/15 ,  C07D295/192 ,  C07D295/205 ,  C07D317/68

    摘要： A compound having the formula ##STR1## in which R is hydrogen or alkyl having 1 to 4 carbon atoms; R.sub.1 is hydrogen, alkyl having 1 to 5 carbon atoms, cycloalkylmethyl in which the cycloalkyl group has from 3 to 6 carbon atoms, 2-hydroxyethyl, alkoxycarbonyl in which the alkoxy group has 1 or 2 carbon atoms, 2-carboxypropyl, N-benzyl-2-carbamoyl propyl, phenyl, phenyl substituted by methoxy, trifluoromethyl or acetyl, benzyl, benzyl substituted by halogen, benzoyl, benzoyl substituted by three methoxy groups, 3,5-dimethoxy-4-acetoxy or 3,5-dimethoxy-4-ethoxycarbonyloxy, cinnamoyl, cinnamoyl in which the phenyl ring is substituted with trifluoromethyl or by one or more methoxy groups, phenoxyacetyl, phenoxyacetyl in which the phenyl ring is substituted with halogen or methoxy, and ##STR2## in which m is 2 or 3 and R.sub.2 and R.sub.3 are identical and are alkyls having 1 to 3 carbon atoms; A is a pharmaceutically acceptable compound selected from the group consisting of inorganic acids, organic acids, alkyl halides and aryl halides; and n is 0, 1, 2 or 3;The compounds are useful in the treatment of cardiac disease symptomized by low cardiac flow.

    摘要翻译： 具有式“IMAGE”的化合物，其中R是氢或具有1至4个碳原子的烷基; R 1是氢，具有1至5个碳原子的烷基，环烷基具有3至6个碳原子的环烷基甲基，2-羟乙基，烷氧基具有1或2个碳原子的烷氧基羰基，2-羧丙基，N-苄基 -2-氨基甲酰基丙基，苯基，被甲氧基，三氟甲基或乙酰基取代的苯基，苄基，被卤素取代的苄基，苯甲酰基，被三个甲氧基取代的苯甲酰基，3,5-二甲氧基-4-乙酰氧基或3,5-二甲氧基-4 乙氧基羰基氧基，肉桂酰基，肉桂酰基，其中苯环被三氟甲基取代或被一个或多个甲氧基取代，苯氧基乙酰基，其中苯基环被卤素或甲氧基取代的苯氧基乙酰基，和其中m是2或3的“ R2和R3是相同的并且是具有1至3个碳原子的烷基; A是选自无机酸，有机酸，烷基卤和芳基卤的药学上可接受的化合物; 并且n为0,1,2或3; 该化合物可用于治疗低心脏流量症状的心脏病。

    Process for the preparation of morpholine and piperidine derivatives
    46.
    发明授权
    Process for the preparation of morpholine and piperidine derivatives 失效
    吗啉和哌啶衍生物的制备方法

    公开(公告)号：US4384116A

    公开(公告)日：1983-05-17

    申请号：US230196

    申请日：1981-02-02

    申请人： Albert Pfiffner

    发明人： Albert Pfiffner

    IPC分类号： C07D295/02 ,  A01N43/40 ,  A01N43/84 ,  C07D211/14 ,  C07D265/30 ,  C07D295/023 ,  C07D295/03 ,  C07D295/06

    CPC分类号： C07D295/03 ,  C07D295/023

    摘要： The invention relates to an improved process for the preparation of fungicidally active compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 individually are lower alkyl of from 1 to 4 carbons or halo-(lower alkyl) of from 1 to 4 carbons or R.sub.1 and R.sub.2 together with the carbon to which they are attached form a 3 to 7 membered cycloalkyl ring or lower alkyl-substituted cycloalkyl of from 4 to 9 carbons, R.sub.3, R.sub.4 and R.sub.5 individually are hydrogen or lower alkyl of from 1 to 4 carbons and X is methylene or oxygen, and salts of those compounds which are basic.The improved process comprises the reaction of a compound of the formula, ##STR2## wherein R.sub.3, R.sub.4, R.sub.5 and X have the significance given hereinabove, with a compound which forms a carbonium ion of the formula ##STR3## wherein R.sub.1 and R.sub.2 have the significance as given hereinabove.

    摘要翻译： 本发明涉及制备式IMA的杀真菌活性化合物的改进方法，其中R 1和R 2分别是1至4个碳的低级烷基或1至4个碳的卤代（低级烷基）或R 1和 R2与它们所连接的碳一起形成3至7元环烷基环或4至9个碳的低级烷基取代的环烷基，R 3，R 4和R 5分别是氢或1至4个碳的低级烷基和X 是亚甲基或氧，以及那些是碱性化合物的盐。 改进的方法包括下式的化合物，其中R 3，R 4，R 5和X具有上述含义的化合物与形成下式的碳鎓离子的化合物反应：其中R 1和R 2具有 意义如上所述。

    Morpholino containing benzamides
    47.
    发明授权
    Morpholino containing benzamides 失效
    含吗啉代苯甲酰胺

    公开(公告)号：US4210754A

    公开(公告)日：1980-07-01

    申请号：US953721

    申请日：1978-10-20

    申请人： Willy Burkard ,  Pierre-Charles Wyss

    发明人： Willy Burkard ,  Pierre-Charles Wyss

    IPC分类号： C07D295/13 ,  C07D295/06 ,  C07D295/14

    CPC分类号： C07D295/13

    摘要： Benzamides of the formula ##STR1## wherein X is halogen, trifluoromethyl or C.sub.3-4 -alkyl and Y is hydrogen, halogen or nitro,and N-oxides thereof, prepared inter alia from N-(2-aminoethyl)-morpholine and an acid of the formula ##STR2## wherein X and Y are as hereinbefore set forth, are described. The end products are useful in the treatment of depressive conditions, that is, are useful as antidepressants.

    摘要翻译： 式I的苯甲酰胺其中X是卤素，三氟甲基或C 3-8 - 烷基，Y是氢，卤素或硝基，及其N-氧化物，其特别是由N-（2-氨基乙基） - 吗啉和 描述了其中X和Y如上所述的式II的酸。 最终产品可用于治疗抑郁症状，即可用作抗抑郁药。

    Process for the production of non-lachrymatory nitro amines
    49.
    发明授权
    Process for the production of non-lachrymatory nitro amines 失效
    生产无氯雷奈硝基胺的方法

    公开(公告)号：US4088817A

    公开(公告)日：1978-05-09

    申请号：US763272

    申请日：1977-01-27

    申请人： Jerry H. Hunsucker ,  Robert W. Shelton

    发明人： Jerry H. Hunsucker ,  Robert W. Shelton

    IPC分类号： C07D295/067 ,  C07D295/06

    CPC分类号： C07D295/067

    摘要： An improvement in the process for the production of P-1487 from the reaction of 1-nitropropane, 37% formaldehyde and morpholine, the improvement comprising mixing 1-nitropropane and 37% formaldehyde at a temperature of 40.degree.-42.degree. C., adding morpholine maintaining the temperature at 40.degree.-42.degree. C., holding the mixture for two hours at 40.degree.-42.degree. C., cooling to allow layer separation, separating the upper oil layer and concentrating the oil layer to P-1487 by removing excess water.

    摘要翻译： 由1-硝基丙烷，37％甲醛和吗啉的反应生产P-1487的方法有所改进，包括在40°-42℃的温度下混合1-硝基丙烷和37％甲醛，加入 保持温度在40〜-42℃，在40〜-4℃保持2小时，冷却，使层分离，分离上油层，通过除去油层将油层浓缩成P-1487 多余的水。

    Alkenyl and alkanylamines for treating depression
    50.
    发明授权
    Alkenyl and alkanylamines for treating depression 失效
    用于治疗抑郁症的烯基和烷基胺

    公开(公告)号：US4031245A

    公开(公告)日：1977-06-21

    申请号：US674706

    申请日：1976-04-07

    申请人： William John Welstead, Jr.

    发明人： William John Welstead, Jr.

    IPC分类号： C07D295/06 ,  C07D295/08 ,  A61K31/135

    CPC分类号： C07D295/08 ,  C07D295/06

    摘要： Novel alkenyl- and alkanylamines having the formula: ##STR1## wherein Am is lower-alkylamino, di-lower-alkylamino and piperidino; A is methylene and methylidyne; R is hydrogen, lower-alkyl, lower-alkoxy, halogen and trifluoromethyl; m is zero and one; n is one and two; X is halogen and the pharmaceutically acceptable acid addition salts thereof. The alkenylamines are prepared by contacting 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols with strong mineral acids. The alkanylamines are prepared by hydrogenation of the alkenylamines. Some of the compounds exhibit potent antagonism to the depressant effects of tetrabenazine.

    摘要翻译： 新的具有下式的烯基和烷基胺：其中Am是低级烷基氨基，二低级烷基氨基和哌啶子基; A是亚甲基和亚甲基; R为氢，低级烷基，低级烷氧基，卤素和三氟甲基; m是零和一; n是一和二; X是卤素及其药学上可接受的酸加成盐。 烯基胺通过使1-环丙基-1-苯基 - ω-氨基-1-链烷醇与强无机酸接触来制备。 链烷胺通过链烯基胺的氢化制备。 一些化合物表现出对丁苯那敏抑制作用的强烈拮抗作用。