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    • 16. 发明授权
    • Treatment of rumen acidosis with α-amylase inhibitors
    • 用α-淀粉酶抑制剂治疗瘤胃酸中毒
    • US07271158B2
    • 2007-09-18
    • US10774139
    • 2004-02-06
    • Bernard Joseph BanksMark Andrew HaxellGraham LunnMichael Stephen PaceyLee Richard Roberts
    • Bernard Joseph BanksMark Andrew HaxellGraham LunnMichael Stephen PaceyLee Richard Roberts
    • A01N43/04A61K31/715C07H1/00
    • A61K31/715A23K10/12A23K20/163A23K50/10A61K31/7016A61K31/702
    • The invention described herein relates to: the use of an effective inhibitor of a bacterial α-amylase and/or α-glucosidase in the manufacture of a composition for the treatment of acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial α-amylase and/or α-glucosidase to a ruminant; a formulation suitable for the treatment of acidosis in an animal which comprises an effective inhibitor of a bacterial α-amylase and/or α-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial α-amylase and/or α-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacterial α-amylase and/or α-glucosidase; a compound of the formula I: or veterinarily acceptable salt, solvate (including hydrate) or prodrug thereof; and processes to make an effective inhibitor of a bacterial α-amylase and/or α-glucosidase useful for the treatment of acidosis in a ruminant.
    • 本文描述的发明涉及:在制备用于治疗酸中毒的组合物中使用细菌α-淀粉酶和/或α-葡糖苷酶的有效抑制剂; 一种治疗瘤胃酸中毒的方法,包括向反刍动物施用有效量的有效的细菌α-淀粉酶和/或α-葡糖苷酶抑制剂; 适用于治疗动物中的酸中毒的制剂,其包含与适当的赋形剂,稀释剂或载体混合的有效抑制细菌α-淀粉酶和/或α-葡萄糖苷酶的方法,所述适合的赋形剂,稀释剂或载体相对于预期给药途径和标准药物 /兽医/农业实践; 用于鉴定用于治疗反刍动物酸中毒的细菌α-淀粉酶和/或α-葡糖苷酶的合适抑制剂的筛选方法; 一种改善反刍动物奶质量和/或量的方法,其包括用有效量的细菌α-淀粉酶和/或α-葡糖苷酶抑制剂处理反刍动物; 式I化合物或兽医学上可接受的盐,溶剂合物(包括水合物)或其前药; 并且制备用于治疗反刍动物酸中毒的细菌α-淀粉酶和/或α-葡糖苷酶的有效抑制剂的方法。
    • 18. 发明申请
    • Compounds Useful in Therapy
    • 化合物可用于治疗
    • US20080234252A1
    • 2008-09-25
    • US11914688
    • 2006-05-08
    • Justin Stephen BryansPatrick Stephen JohnsonLee Richard RobertsThomas Ryckmans
    • Justin Stephen BryansPatrick Stephen JohnsonLee Richard RobertsThomas Ryckmans
    • A61K31/55C07D249/08A61K31/4196C07D471/02C07D487/02A61P15/00A61K31/519A61K31/437C07D221/20C07D223/16
    • C07D471/04C07D401/04C07D403/04C07D403/14C07D471/10C07D487/04C07D491/10C07D498/04
    • Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2. R2 represents H, C1-6 alkyloxy or Het; n represents a number selected from 0 to 6; Het represents an unsaturated heterocycle of 5 or 6 atoms containing one or more heteroatoms selected from O, N, and S; R3 represents halo; Ring A represents a 4 to 7 membered, saturated, partially saturated, or unsaturated heterocycle containing one or more heteroatoms selected from O, N, and S; Ring B represents a saturated, partially saturated, or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, and S, or Ring B represents a saturated or unsaturated carbocyclic ring of from 3 to 8 atoms; Ring B is optionally fused to an aryl ring and is optionally substituted with one or more groups independently selected from R4; Ring A and Ring B share at least one atom; R4 represents oxo, [CH2]m—R5 or CH—R6R7; R5 represents H, OH, C1-6 alkyloxy, COOH, or CONR8R9; m represents a number selected from 0 or 1; and R6, R7, R8 and R9 independently represent H or C1-6 alkyl; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
    • 式(I)化合物或其药学上可接受的盐,溶剂合物,酯或酰胺,其中R 1表示[CH 2 N] -R <2> 。 R 2表示H,C 1-6烷氧基或Het; n表示选自0〜6的数; Het表示含有一个或多个选自O,N和S的杂原子的5或6个原子的不饱和杂环; R 3表示卤素; 环A表示含有一个或多个选自O,N和S的杂原子的4至7元饱和的,部分饱和的或不饱和的杂环; 环B表示含有一个或多个选自O,N和S的杂原子的3至8个原子的饱和,部分饱和或不饱和杂环,或环B表示3至8个原子的饱和或不饱和碳环; 环B任选地与芳环稠合并且任选地被一个或多个独立地选自R 4的基团取代; 环A和环B共享至少一个原子; R 4表示氧代,[CH 2 CH 2] m -R 5或CH-R 6, 7&lt; 7&gt;; R 5表示H,OH,C 1-6烷氧基,COOH或CONR 8 R 9; m表示选自0或1的数字; 且R 6,R 7,R 8和R 9独立地表示H或C 1〜 6烷基; 可用于治疗指示V1a拮抗剂的疾病,特别是痛经。