Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
    14.
    发明授权
    Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 失效
    趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂

    公开(公告)号:US07557124B2

    公开(公告)日:2009-07-07

    申请号:US11587288

    申请日:2005-04-22

    CPC分类号: C07D309/14 C07D405/12

    摘要: Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

    摘要翻译: 式I化合物(其中n,R 1,R 3,R 4,R 5,R 6,R 7,R 8,R 9,R 10,R 15,R 16,Y和Z如本文所定义),其是趋化因子受体活性的调节剂, 预防或治疗某些炎性和免疫调节性疾病和疾病,过敏性疾病,特应性病症,包括过敏性鼻炎,皮炎,结膜炎和哮喘,以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

    Efficient production of heterologous proteins using mannosyl transferase inhibitors
    15.
    发明授权
    Efficient production of heterologous proteins using mannosyl transferase inhibitors 有权
    使用甘露糖基转移酶抑制剂有效生产异源蛋白

    公开(公告)号:US08765409B2

    公开(公告)日:2014-07-01

    申请号:US13588022

    申请日:2012-08-17

    IPC分类号: C12P21/00 C07D277/36

    摘要: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.

    摘要翻译: 描述了用于生产具有降低量的O-连接糖基化的蛋白质组合物的化合物和方法。 该方法包括在某些亚苄基噻唑烷二酮类Pmt介导的O-连接糖基化抑制剂存在下培养的细胞中产生蛋白质。

    Substituted spirochromanone derivatives
    17.
    发明授权
    Substituted spirochromanone derivatives 有权
    取代的螺二氢茚酮衍生物

    公开(公告)号:US08093389B2

    公开(公告)日:2012-01-10

    申请号:US12007000

    申请日:2008-01-08

    CPC分类号: C07D519/00 C07D491/10

    摘要: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of —N(Re)Rf; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1表示由选自吲哚,1H-吲唑,2H-吲唑,1H-噻吩并[2,3-c]所示的芳环形成的基团, 吡唑,1H-吡唑并[3,4-b]吡啶,苯并[b]呋喃,苯并咪唑,苯并恶唑,1,2-苯并异恶唑和咪唑并[1,2-a] R 1和R 2各自表示氢原子,卤素原子,氰基,C 2 -C 6烯基,C 1 -C 6烷氧基,卤代-C 1 -C 6烷氧基,环-C 3 -C 6烷氧基, C2-C7烷酰基,卤代-C2-C7烷酰基,C2-C7烷氧基羰基,卤代-C2-C7烷氧基羰基,环-C3-C6烷氧基羰基,芳烷氧基羰基,氨基甲酰基-C1-C6 烷氧基,羧基-C2-C6烯基或-Q1-N(Ra)-Q2-Rb的基团; 任选取代的C 1 -C 6烷基,芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; R 3和R 4各自表示氢原子,卤素原子,硝基,环-C 3 -C 6烷基,任选被C 1 -C 6烷基或环-C 3 -C 6烷基取代的氨基甲酰基,或者 -N(R f)R f; 任选取代的C 2 -C 7烷酰基,C 1 -C 6烷氧基,C 2 -C 7烷氧基羰基,环C 3 -C 6烷氧基羰基,C 1 -C 6烷基磺酰基,C 1 -C 6烷硫基,环C 3 -C 6烷氧基,环C 3 -C 6烷基 - C 1 -C 6烷氧基,环-C 3 -C 6烷基磺酰基,环-C 3 -C 6烷硫基或环-C 3 -C 6烷基-C 1 -C 6烷硫基; 或任选取代的C 1 -C 6烷基; T和U各自表示氮原子或次甲基; V表示氧原子或硫原子。 本发明的化合物可用作各种ACC相关疾病的治疗剂。