Novel 2-propanol derivatives and preparation thereof
    31.
    发明授权
    Novel 2-propanol derivatives and preparation thereof 失效
    新型2-丙醇衍生物及其制备方法

    公开(公告)号:US3951986A

    公开(公告)日:1976-04-20

    申请号:US370693

    申请日:1973-06-18

    摘要: 2-Propanol derivatives of the formula: ##SPC1##And their pharmaceutically acceptable acid addition salts, which are useful as medicaments and can be produced by reacting a compound of the formula: A-CH.sub.2 -Z with a compound of the formula: A'-H [wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; W is oxygen, sulfur, sulfinyl or sulfonyl; Y is a group of either one of the formulae: ##SPC2##(wherein R.sub.2 is hydrogen, halogen, lower alkyl or lower alkoxy and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl); A and A' are each a group of either one of the formulae: ##SPC3##(wherein R.sub.1, W and Y are each as defined above), provided that A and A' are different each other; and Z is a group of either one of the formulae: ##EQU1## (wherein X is halogen, alkylsulfonyloxy or arylsulfonyloxy and R is as defined above)].

    摘要翻译: 下式的2-丙醇衍生物:

    Cyclopropylmethylamine derivatives
    33.
    发明授权
    Cyclopropylmethylamine derivatives 失效
    环丙基甲胺衍生物

    公开(公告)号:US4110376A

    公开(公告)日:1978-08-29

    申请号:US605012

    申请日:1975-08-15

    CPC分类号: C07D401/12

    摘要: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

    摘要翻译: 下式的新型环丙基甲胺化合物:其中R 1和R 2各自为氢或卤素,R 3为氢或甲基,及其无毒盐,其具有各种有用的药理活性,可通过还原相应化合物 其中R 1,R 2和R 3各自如上所定义,或其无毒盐,或通过下式的相应化合物的缩合:其中R 1和R 2各自如上所定义,X为 常规的可互换基团如卤素或磺酰氧基与甲胺或二甲胺。

    Novel n'-acylated phenyl-hydrazine and -hydrazone derivatives
    35.
    发明授权
    Novel n'-acylated phenyl-hydrazine and -hydrazone derivatives 失效
    新型n {40-酰基苯基 - 肼和腙衍生物

    公开(公告)号:US4060550A

    公开(公告)日:1977-11-29

    申请号:US651831

    申请日:1976-01-23

    摘要: Indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##STR1## wherein X.sub.1 and X.sub.2 are each methylene; A is an unsubstituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms; m is 0 or 1; n is 1 or 2; R.sub.3 is alkyl having up to 4 carbon atoms; cycloalkyl having 3 to 7 carbon atoms, unsubstituted or C.sub.1 -C.sub.4 alkyl-, nitro-, trifluoromethyl-, methylenedioxy-, ethylenedioxy- or halogen-substituted phenyl, or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.3 -C.sub.7 cycloalkyl, or unsubstituted or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.5 -C.sub.6 cycloalkenyl; and B is ##STR2## .

    摘要翻译: 吲哚乙酸衍生物,其具有优异的抗炎,解热和止痛活性,由下式表示,其中X1和X2各自为亚甲基; A是具有至多5个碳原子的未取代的烯属不饱和烃链; m为0或1; n为1或2; R3是具有至多4个碳原子的烷基; 具有3-7个碳原子的环烷基,未取代的或C 1 -C 4烷基 - ,硝基 - ,三氟甲基 - ,亚甲二氧基 - ,亚乙二氧基或卤素取代的苯基,或卤素 - ,C 1 -C 4烷基 - 或苯基取代的或苯环 - 或未取代的或卤素的,C 1 -C 4烷基或苯基取代的或苯环稠合的C 5 -C 6环烯基; 而B是

    Butyrophenone derivatives
    36.
    发明授权
    Butyrophenone derivatives 失效
    丁酰苯衍生物

    公开(公告)号:US4009173A

    公开(公告)日:1977-02-22

    申请号:US617730

    申请日:1975-09-29

    IPC分类号: C07D211/64 C07D403/04

    CPC分类号: C07D211/64

    摘要: Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.1 is ##STR4## R.sub.10 can not be a hydrogen atom, and their acid addition salts, which are useful as central and autonomic nervous system depressants.

    摘要翻译: 下式的新型丁基苯酚衍生物:其中R 1表示羟基或(其中R 6和R 7各自为氢原子或低级烷基,或者当与相邻的氮原子一起形成杂环时 基团),R 2表示任选取代的苯基或者其中R 8和R 9各自为氢原子或低级烷基,或者当与相邻的氮原子一起形成杂环基时,R 4表示 氢原子,低级烷基或任选取代的苯基,R 5表示氢原子,卤素原子,低级烷基,低级烷氧基或三氟甲基,R 10表示氢原子或R 3 CO 3表示的酰基 - (其中R 3是氢原子,低级烷基或任选取代的苯基),Z代表两个氢原子或氧原子,条件是当Z是氧原子且R 1不能是 氢原子, 和它们的酸加成盐,其可用作中枢神经系统抑制剂和自主神经系统抑制剂。

    Phenoxypropylamine derivatives
    40.
    发明授权
    Phenoxypropylamine derivatives 失效
    苯氧丙胺衍生物

    公开(公告)号:US4009275A

    公开(公告)日:1977-02-22

    申请号:US553932

    申请日:1975-02-28

    IPC分类号: A61K31/445 C07D401/04

    CPC分类号: C07D401/04 A61K31/445

    摘要: Phenoxypropylamine derivatives of the formula: ##STR1## (in which R.sub.2 is a halogen atom or a trifluoromethyl group) and R.sub.1 is a halogen atom or a C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl group, and their pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## wherein X is a halogen atom and R.sub.1 is as defined above with a compound of the formula:H-Ywherein Y is as defined above.

    摘要翻译: 下式的苯氧丙胺衍生物:其中R 2为卤原子或三氟甲基,R 1为卤素原子或C 1 -C 4烷基或C 2 -C 4烯基, 药学上可接受的盐,其可用作抗精神病药,并且可以通过使下式化合物与下式化合物反应来制备:其中X是卤素原子,R 1如上定义;