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    • 5. 发明申请
    • DITHIOLE COMPOUNDS AS COX INHIBITORS
    • 几何化合物作为COX抑制剂
    • WO2008052288A1
    • 2008-05-08
    • PCT/AU2007/001687
    • 2007-11-02
    • NEURO THERAPEUTICS LIMITEDJARROTT, BevynZANATTA, Shannon DeanWILLIAMS, Spencer John
    • JARROTT, BevynZANATTA, Shannon DeanWILLIAMS, Spencer John
    • C07D339/04A61K31/381A61P29/00
    • C07D339/04
    • A compound of formula (I) wherein: R 1 and R 2 are the same or different and are independently selected from H and a shielding group; X and Y are each independently selected from N and CH; R 3 is hydroxy, alkoxy, acyloxy or an ester group; R 4 is a direct bond to R 5 , -CH 2 - or -CH=; the broken line ----- represents an optional double bond between R 4 and R 5 ; and R 5 is a 5- or 6-membered substituted or unsubstituted unsaturated heterocyclic or heteroaromatic ring, or R 5 is a substituted heterocyclic ring containing the substituent = O or = S, wherein the heteroatom is selected from S, O or P, and wherein R 5 is optionally attached to R 4 through a substituent on the heterocyclic or heteroaromatic ring; or a pharmaceutically acceptable prodrug, metabolite, ester, salt, derivative, tautomer or isomer thereof. The compounds have utility as COX-inhibitors and for use in the treatment of pain, inflammation or a neurodegenerative disease.
    • 式(I)的化合物,其中:R 1和R 2相同或不同,独立地选自H和屏蔽基团; X和Y各自独立地选自N和CH; R 3是羟基,烷氧基,酰氧基或酯基; R 4是与R 5,-CH 2 - 或-CH =的直接键合。 虚线-----表示R 4和R 5之间的任选的双键; 并且R 5是5-或6-元取代或未取代的不饱和杂环或杂芳环,或者R 5是含有取代基= O或= S的取代杂环 其中所述杂原子选自S,O或P,并且其中R 5任选地通过杂环或杂芳环上的取代基连接到R 4上; 或其药学上可接受的前药,代谢物,酯,盐,衍生物,互变异构体或异构体。 这些化合物可用作COX抑制剂,并用于治疗疼痛,炎症或神经变性疾病。