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    • 1. 发明授权
      US06451794B1 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，其制备及其作为环氧合酶2（COX-2）抑制剂的用途
    • US06451794B1
    • 2002-09-17
    • US09508029
    • 2000-06-13
    • Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
    • Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
    • A61K314985
    • 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 4 R 5; R 1和R 2独立地选自被一个或多个氟原子取代的H，C 1-6烷基，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 4 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（CH 2）n CO 2 C 1-6烷基，O（CH 2） ）nSC1-6烷基，（CH2）nNR4R5或（CH2）nSC1-6烷基，C（O）NR4R5; R3是C1-6烷基或NH2; 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; n为1-4。 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。
    • 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
    • 2. 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
    • 9. 发明授权
      US07196107B2 Thia-and oxazoles and their use as ppars activators 失效
    • Thia-and oxazoles and their use as ppars activators
    • Thia和恶唑及其作为ppars激活剂的用途
    • US07196107B2
    • 2007-03-27
    • US10451307
    • 2001-12-18
    • Paul John Beswick , Vipulkumar Patel , Michael Lawrence Sierra
    • Paul John Beswick , Vipulkumar Patel , Michael Lawrence Sierra
    • A61K31/426 , A61K31/421 , C07D277/20 , C07D263/30
    • C07D277/24
    • A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5. Use of a compound of formula (I) for the manufacture of a medicament for the prevention or treatment of a hPPAR mediated disease or condition, such as dyslipidemia, syndrome X, heart failure, hypercholesteremia, cardiovascular disease, type II diabetes mellitus, type 1 diabetes, insulin resistance hyperlipidemia, obesity, anorexia bulimia, inflammation and anorexia nervosa
    • 式（I）化合物或其药学上可接受的盐和溶剂化物。 R 1和R 2独立地为H或C 1-3烷基，m为0-3; X 1是NH，NCH 3，O，S; R 3，R 4和R 5独立地为H，CH 3，CF 3， OCH 3，OCH 3，烯丙基或卤素; 其中n为1或2;（3）其中n为1或2; R 10和R 11独立地代表H，氟或C 1-16烷基; R 26和R 27独立地是H，C 1-3烷基或R 26和R 26， 27与它们所键合的碳原子一起形成3-5元环烯基环。 R 6和R 7独立地表示H，氟或C 1-16烷基; R 9是C 1-6烷基或CF 3 N; Y和Z之一是N，另一个是S或O; 每个R 8独立地表示CF 3，OCH 3，CH 3或卤素; y是O，1,2,3,4,5。式（I）化合物在制备用于预防或治疗hPPAR介导的疾病或病症如血脂异常，综合征X，心脏的药物中的用途 失败，高胆固醇血症，心血管疾病，II型糖尿病，1型糖尿病，胰岛素抵抗性高脂血症，肥胖，厌食症，炎症和神经性厌食
    • 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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