Process for preparation of sulfone derivatives
    2.
    发明公开
    Process for preparation of sulfone derivatives 失效
    Verfahren zur Herstellung von Sulfon-Derivaten。

    公开(公告)号:EP0322800A1

    公开(公告)日:1989-07-05

    申请号:EP88121599.0

    申请日:1988-12-23

    IPC分类号: C07D249/08 C07D233/60

    摘要: A process for preparing sulfone derivatives of the formula:
    wherein R¹ and R² are each a hydrogen atom, a lower alkyl group or a substituted or unsubstituted cyclo(lower)alkyl, cyclo(lower)alkylmethyl, lower alkenyl, heterocyclic, aryl or ar(lower)alkyl group, R⁴, R⁵, R⁶ and R⁷ are each a hydrogen atom, a lower alkyl group, a lower alkenyl group or a substituted or unsubstituted aryl grcup and Az is a 1,2,4- or 1,3,4-triazole or imidazole ring, which comprises subjecting a sulfide or sulfoxide compound of the formula:
    wherein R¹, R², R⁴, R⁵, R⁶, R⁷ and Az are each as defined above and n is an integer of 0 or 1 to oxidation with an oxidizing agent in the presence of a metal catalyst.

    摘要翻译: 制备下式的砜衍生物的方法:其中R 1和R 2各自为氢原子,低级烷基或取代或未取代的环(低级)烷基,环(低级)烷基甲基, 低级烯基,杂环,芳基或芳(低级)烷基,R 4,R 5,R 6和R 7各自为氢原子,低级烷基,低级烯基或 取代或未取代的芳基基团,并且Az是1,2,4-或1,3,4-三唑或咪唑环,其包括使下式的硫化物或亚砜化合物:其中R 1, R 2,R 4,R 5,R 6,R 7和A 11各自如上所定义,n是0或1的整数,在金属存在下用氧化剂氧化 催化剂。

    Novel thiazole derivatives
    4.
    发明公开
    Novel thiazole derivatives 失效
    Thiazolderivate。

    公开(公告)号:EP0511021A1

    公开(公告)日:1992-10-28

    申请号:EP92303750.1

    申请日:1992-04-24

    摘要: A novel thiazole derivative of formula [1] or a pharmaceutically acceptable salt thereof:

    wherein A is a singe bond, straight-chained or branched-chained lower alkylene or straight-chained or branched lower alkenylene, B is a single bond or -CO-; R¹ is carboxy or -CON(R⁷)OR⁸ (R⁷ and R⁸ are the same or different and each is hydrogen or lower alkyl); R² is lower alkyl; R³ and R⁴ are the same or different and each is hydrogen, lower alkyl or lower alkoxycarbonyl; R⁵ is hydrogen or halogen; and R⁶ is hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, thiol, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, nitro, amino, substituted amino, cyano, carboxy or acyl.
    The compounds of the present invention are useful as therapeutic or preventive drugs for autoimmune diseases and inflammatory diseases.

    摘要翻译: 式[1]的新型噻唑衍生物或其药学上可接受的盐:其中A为单键,直链或支链低级亚烷基或直链或支链低级亚烯基,B为单键或 -CO-; R 1是羧基或-CON(R 7)OR 8(R 7和R 8相同或不同,各自为氢或低级烷基)。 R 2是低级烷基; R 3和R 4相同或不同,各自为氢,低级烷基或低级烷氧基羰基; R 5是氢或卤素; R 6为氢,卤素,低级烷基,羟基,低级烷氧基,硫醇,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,硝基,氨基,取代氨基,氰基,羧基或酰基。 本发明的化合物可用作自身免疫疾病和炎性疾病的治疗或预防药物。

    Imide derivatives, and their production and use
    10.
    发明公开
    Imide derivatives, and their production and use 失效
    Imidderivate,ihre Herstellung und Verwendung。

    公开(公告)号:EP0464846A1

    公开(公告)日:1992-01-08

    申请号:EP91111223.3

    申请日:1991-07-05

    摘要: An imide compound of the formula:

    wherein
       Z is a group of the formula:

    in which B is a carbonyl group or a sulfonyl group, R¹, R², R³ and R⁴ are each a hydrogen atom or a lower alkyl group, or R¹ and R² or R¹ and R³ may be combined together to make a non-aromatic hydrocarbon ring or R¹ and R³ may be combined together to make an aromatic ring, said non-aromatic hydrocarbon ring being optionally bridged with a lower alkylene group or an oxygen atom therein and said aromatic ring, said non-aromatic hydrocarbon ring and said lower alkylene group being each optionally substituted with at least one lower alkyl, and n is an integer of 0 or 1;
       D is a group of the formula:



            -(CH₂) p -A-(CH₂) q -



    in which A is a non-aromatic hydrocarbon ring optionally bridged with a lower alkylene group or an oxygen atom, said non-aromatic hydrocarbon ring and said lower alkylene group being each optionally substituted with at least one lower alkyl, and p and q are each an integer of 0, 1 or 2; and
       Ar is an aromatic group, a heterocyclic aromatic group, a benzoyl group, a phenoxy group or a phenylthio group and G is

    or Ar is a biphenylmethylidene group and G is

    all of the above groups being each optionally substituted with at least one of lower alkyl, lower alkoxy and halogen; and its acid addition salts, useful as an antipsycotic agent.

    摘要翻译: 下式的酰亚胺化合物:其中Z是下式的基团:其中B是羰基或磺酰基,R 1,R 2,R 3和R R 4各自为氢原子或低级烷基,或者R 1和R 2或R 1和R 3可以组合在一起形成非芳族烃环或R 1 >和R 3可以组合在一起形成芳环,所述非芳族烃环任选地与低级亚烷基或氧原子桥连,所述芳环,所述非芳族烃环和所述低级亚烷基 基团各自任选被至少一个低级烷基取代,n是0或1的整数; D是下列基团: - (CH 2)p -A(CH 2)q - ,其中A是任选与低级亚烷基或氧原子桥连的非芳族烃环,所述非芳族烃环和所述低级 亚烷基各自任选被至少一个低级烷基取代,p和q各自为0,1或2的整数; Ar是芳基,杂环芳基,苯甲酰基,苯氧基或苯硫基,G是或Ar是联苯亚甲基,G是,所有上述基团各自任意取代 与至少一种低级烷基,低级烷氧基和卤素; 和其酸加成盐,可用作抗精神病药。