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    • 5. 发明授权
    • 2,3-diaryl-pyrazolo[1,5-B]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors
    • 2,3-二芳基 - 吡唑并[1,5-B]哒嗪衍生物,它们的制备及其作为环加氧酶2(COX-2)抑制剂的用途
    • US06831097B2
    • 2004-12-14
    • US10212514
    • 2002-08-05
    • Paul John BeswickIan Baxter CampbellNeil MathewsAlan Naylor
    • Paul John BeswickIan Baxter CampbellNeil MathewsAlan Naylor
    • A61K315025
    • C07D487/04A61K31/50Y02P20/55
    • The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
    • 本发明提供式(I)化合物及其药学上可接受的衍生物,其中:R 0是卤素,C 1-6烷基,C 1-6烷氧基,被一个或多个氟原子取代的C 1-6烷氧基或O(CH 2)n NR R 5和R 2独立地选自H,C 1-6烷基,被一个或多个氟原子取代的C 1-6烷基,C 1-6烷氧基,C 1-6羟烷基,SC 1-6烷基, C(O)H,C(O)C 1-6烷基,C 1-6烷基磺酰基,被一个或多个氟原子取代的C 1-6烷氧基,O(CH 2)n CO 2 C 1-6烷基,O(CH 2)nSC 1-6烷基,(CH 2)n NR R 5,(CH 2)nSC 1-6烷基或C(O)NR 4 R 5; 条件是当R 0在4-位且是卤素时,R 1和R 2中的至少一个是C 1-6烷基磺酰基,被一个或多个氟原子取代的C 1-6烷氧基,O( O(CH 2)n C 1-6烷基,(CH 2)n NR 4 R 5或(CH 2)nSC 1-6烷基,C(O)NR 4 R 5; R 3, 是C 1-6烷基或NH 2; R 4和R 5独立地选自H或C 1-6烷基,或与它们所连接的氮原子一起形成4-8元饱和环; 而且是1-4.式(I)的化合物是COX-2的有效和选择性抑制剂,并且可用于治疗疼痛,发热,各种病症和疾病的炎症。
    • 9. 发明授权
    • Pyrazolopyridine derivatives as selective cox-2 inhibitors
    • 吡唑并吡啶衍生物作为选择性cox-2抑制剂
    • US07223772B1
    • 2007-05-29
    • US09830836
    • 1999-11-01
    • Ian Baxter CampbellAlan Naylor
    • Ian Baxter CampbellAlan Naylor
    • A61K31/415A61K31/44C07D231/56C07D471/02
    • C07D471/04
    • The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
    • 本发明提供式(I)化合物及其药学上可接受的衍生物,其中:R 0和R 1独立地选自H,卤素, C 1-6烷基,C 1-6烷氧基和被一个或多个氟原子取代的C 1-6烷氧基; R 2选自H,C 1-6烷基,被一个或多个氟原子取代的C 1-6烷基 ,C 1-6烷氧基,C 1-6 1-6烷基,C 1-6烷基,C(O)H,C(O) C 1-6烷基,C 1-6烷基磺酰基和被一个或多个氟原子取代的C 1-6烷氧基; R 3是C 1-6烷基或NH 2。 式(I)化合物是COX-2的有效和选择性抑制剂,可用于治疗疼痛,发热,各种病症和疾病的炎症。