Novel 2-propanol derivatives and preparation thereof
    23.
    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:

    Antihypertensive quinazoline compounds
    24.
    发明授权
    Antihypertensive quinazoline compounds 失效
    抗高血压喹唑啉化合物

    公开(公告)号:US4230706A

    公开(公告)日:1980-10-28

    申请号:US021776

    申请日:1979-03-19

    CPC分类号: C07D239/95

    摘要: Quinazoline compounds of the formula: ##STR1## wherein A is ##STR2## wherein n is an integer of 1 or 2, or ##STR3## wherein X is O or CH.sub.2, and n and m are independently an integer of 1 or 2, and its non-toxic pharmaceutically acceptable salts, having an excellent antihypertensive activity without causing adverse effects such as orthostatic hypotension.

    摘要翻译: 喹唑啉化合物,其结构式如下:其中A是其中n是1或2的整数,或者其中X是O或CH 2,n和m独立地是1或2的整数, 其无毒的药学上可接受的盐,具有优异的抗高血压活性而不引起诸如直立性低血压的不利影响。

    .gamma.-Piperidinobutyrophenones
    25.
    发明授权
    .gamma.-Piperidinobutyrophenones 失效
    {65-哌啶基丁酰苯

    公开(公告)号:US4148796A

    公开(公告)日:1979-04-10

    申请号:US388561

    申请日:1973-08-15

    CPC分类号: C07D401/06 C07D211/48

    摘要: Novel .gamma.-piperidinobutyrophenone derivatives of the formula, ##STR1## wherein R.sup.1 is halogen, amino, alkanoylamino, alkylamino or N-(alkanoyl)alkylamino;R.sup.2 is hydrogen or halogen, provided that when R.sup.1 is halogen, R.sup.2 must be halogen; andZ is a piperidino group having the formula (A), ##STR2## (wherein each of R.sub.a and R.sub.b is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sup.3 is hydrogen or hydroxyl; and n is 1 or 2), or a piperidino group having the formula (B), ##STR3## (wherein R.sub.c is hydrogen or lower alkyl; and each of R.sub.d and R.sub.e is hydrogen, halogen, lower alkyl or lower alkoxy), provided that when R.sup.1 is amino and R.sup.2 is hydrogen, Z cannot be represented by the formula (A), and their pharmaceutically acceptable acid addition salts, which are useful as psychotropic, neuroleptic or analgesic agents.

    摘要翻译: 其中R1是卤素,氨基,烷酰基氨基,烷基氨基或N-(烷酰基)烷基氨基的新颖的γ-哌啶基丁酰苯衍生物, R2是氢或卤素,条件是当R1是卤素时,R2必须是卤素; Z为具有式(A),(A)的哌啶子基,其中R a和R b各自为氢,卤素,低级烷基,低级烷氧基或三氟甲基; R 3为氢或羟基; n为1或 2)或具有式(B)的哌啶子基,其中R c是氢或低级烷基;并且R d和R e各自是氢,卤素,低级烷基或低级烷氧基),条件是当 R1是氨基,R2是氢,Z不能由式(A)表示,它们的药学上可接受的酸加成盐可用作精神药物,精神抑制剂或止痛剂。

    2-Morpholinyl tricyclic dibenzazepine compounds
    26.
    发明授权
    2-Morpholinyl tricyclic dibenzazepine compounds 失效
    2-吗啉基三环二苯并氮杂化合物

    公开(公告)号:US4017621A

    公开(公告)日:1977-04-12

    申请号:US635355

    申请日:1975-11-26

    摘要: Novel tricyclic compounds of the formula: ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH=CH-- or ##STR2## X is hydrogen, halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl (C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl, polyhalo(C.sub.1 -C.sub.2)alkyl, C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.3)alkyl or hydroxy(C.sub.1 -C.sub.3)alkyl, and non-toxic salts thereof which are useful as antidepressants and can be prepared by reduction of a compound of the formula: ##STR3## wherein A, X, R.sub.1, R.sub.2 and R.sub.3 are each as defined above.

    摘要翻译: 新颖的下式的三环化合物:其中A是-CH 2 -CH 2 - , - CH = CH-或X是氢,卤素,硝基,三氟甲基,C 1 -C 3烷基或C 1 -C 3烷氧基,R 1和 R 2各自为氢或C 1 -C 4烷基,R 3为氢,C 1 -C 4烷基,C 3 -C 5烯基,C 3 -C 5炔基,C 3 -C 6环烷基(C 1 -C 3)烷基,芳(C 1 -C 3)烷基,多卤代( C1-C2)烷基,C1-C4烷氧基(C1-C3)烷基或羟基(C1-C3)烷基,及其无毒盐,可用作抗抑郁剂,可通过还原下式化合物来制备: IMAGE>其中A,X,R 1,R 2和R 3各自如上所定义。

    Butyrophenone derivatives
    27.
    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。