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    • 7. 发明申请
      US20050032821A1 Pyrimidine derivatives useful as selective cox-2 inhibitors 失效
    • Pyrimidine derivatives useful as selective cox-2 inhibitors
    • 可用作选择性cox-2抑制剂的嘧啶衍生物
    • US20050032821A1
    • 2005-02-10
    • US10477547
    • 2002-05-23
    • Alan Naylor , Jeremy Payne , Neil Pegg
    • Alan Naylor , Jeremy Payne , Neil Pegg
    • A61K31/505 , A61K31/513 , A61P29/00 , A61P43/00 , C07D239/34 , C07D401/12 , C07D45/02
    • C07D239/34 , A61K31/505 , C07D401/12
    • The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and b(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of Formula (i) and (ii) and where (iv) defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2C1-6alkyl, C1-4alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in treatment of the pain, fever and inflammation of variety of conditions and diseases.
    • 本发明提供式（I）化合物，其中：R 1选自H，C 1-6烷基，被1至5个氟原子取代的C 1-2烷基，C 3-6烯基，C 3-10环烷基C 1-6烷基 ，C 4-12桥环烷基，A（CR 4 R 5）n和b（CR 4 R 5）n; R 2是被1至5个氟原子取代的C 1-2烷基; R 3选自C 1-6烷基，NH 2和R 7 CONH; R 4和R 5独立地选自H或C 1-6烷基; A是未取代的5-或6-元杂芳基或未取代的6-元芳基，或被一个或多个R 6取代的5-或6-元杂芳基或6-元芳基; R 6选自卤素，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，被一个或多个F，NH 2 SO 2和C 1-6烷基SO 2取代的C 1-6烷氧基; B选自式（i）和（ii），其中（iv）定义环的连接点; R 7选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 C 1-6烷基，C 1-6烷基COOC 1-6烷基，C 1-6烷基COO，H 2 C 1-6烷基，C 1-4烷基OCONHC 1 -6-烷基和C 1-6烷基CONHC 1-6烷基; 并且n为0至4.式（I）化合物是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发热和炎症。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明授权
      US06831097B2 2,3-diaryl-pyrazolo[1,5-B]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors 失效
    • 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 Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
    • Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
    • A61K315025
    • C07D487/04 , A61K31/50 , Y02P20/55
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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