CNS active substituted azetidinone compounds
    6.
    发明授权
    CNS active substituted azetidinone compounds 失效
    CNS活性取代的氮杂环丁酮化合物

    公开(公告)号:US4719207A

    公开(公告)日:1988-01-12

    申请号:US747018

    申请日:1985-06-20

    摘要: Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.

    摘要翻译: 提供具有下式的取代的氮杂环丁酮化合物:其中R 1和R 2之一表示取代的低级烷基,叠氮基,氨基,低级酰氨基,巯基或低级烷硫基 另一个表示氢基团,或者都表示氢原子或低级烷基; R3表示氢原子或由下式表示的基团:其中X表示(其中R5表示氢原子或低级烷基),Y表示羟基,低级烷氧基,氨基 ,一或二低级烷基氨基); R 4表示氢原子,取代或未取代的低级烷基或由式-CH 2 CO-A(其中A表示氨基或由下式表示的基团:其中X和Y如上所定义) ),条件是当R 1和R 2均为氢原子时,至少R 4表示氢原子以外的基团,只要R 3或R 4表示除氢原子以外的基团,则该化合物具有强CNS作用。

    Thiophene derivative and pharmaceutical composition thereof
    8.
    发明授权
    Thiophene derivative and pharmaceutical composition thereof 失效
    噻吩衍生物及其药物组合物

    公开(公告)号:US6090804A

    公开(公告)日:2000-07-18

    申请号:US214228

    申请日:1998-12-30

    摘要: Thiophene derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof. Said compounds act as an anti-PCP agonist and therefore are useful as psychotropic or antischizophrenic agents and so on. ##STR1## (In the above formula, R.sub.1 is a formula --A.sub.1 --X.sub.1 --R.sub.3 ; R.sub.2 is a formula --A.sub.2 --X.sub.2 --R.sub.4 or does not exist; B ring is a 7- to 10-membered nitrogen-containing cycloalkyl ring; Ar ring is an aryl or heteroaryl ring; A.sub.1, A.sub.2 and A.sub.3 may be the same or different from one another and each represents a bond or a lower alkylene group; X.sub.1 and X.sub.2 may be the same or different from each other and each represents a bond or a formula --O--, --S--or the like; R.sub.3 and R.sub.4 may be the same or different from each other and each represents a hydrogen atom, a cyclic imido group or a lower alkyl group, a cycloalkyl group, an aryl group or an aralkyl group; with the proviso that, when Ar ring is thiazole ring, either one of A.sub.1 and A.sub.2 is a lower alkylene group. Also, when Ar ring is a benzene ring, a case in which one of R.sub.1 and R.sub.2 is methyl group or a halogen group and the other is a hydrogen atom is excluded.)

    摘要翻译: PCT No.PCT / JP97 / 02255 Sec。 371日期1998年12月30日第 102(e)1998年12月30日日期PCT 1997年6月30日PCT公布。 公开号WO98 / 00420 日期1998年1月8日由以下通式(I)表示的噻吩衍生物或其药学上可接受的盐。 所述化合物作为抗PCP激动剂,因此可用作精神药物或抗精神分裂药物等。 (在上式中,R 1为式-A 1 -X 1 -R 3; R 2为式-A 2 -X 2 -R 4或不存在; B环为7至10元含氮环烷基环; Ar环 是芳基或杂芳基环; A 1,A 2和A 3可以彼此相同或不同,并且各自表示键或低级亚烷基; X 1和X 2可以彼此相同或不同,并且各自表示键或 式-O-,-S-等; R 3和R 4可以相同或不同,表示氢原子,环状亚氨基或低级烷基,环烷基,芳基或 芳烷基;条件是当Ar环是噻唑环时,A1和A2中的任一个是低级亚烷基,当Ar环是苯环时,其中R1和R2之一是甲基 或卤素基团,另一个为氢原子。)