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    Treatment of rumen acidosis with α-amylase inhibitors
    3.
    发明授权
    Treatment of rumen acidosis with α-amylase inhibitors 失效
    用α-淀粉酶抑制剂治疗瘤胃酸中毒

    公开(公告)号：US07271158B2

    公开(公告)日：2007-09-18

    申请号：US10774139

    申请日：2004-02-06

    申请人： Bernard Joseph Banks ,  Mark Andrew Haxell ,  Graham Lunn ,  Michael Stephen Pacey ,  Lee Richard Roberts

    发明人： Bernard Joseph Banks ,  Mark Andrew Haxell ,  Graham Lunn ,  Michael Stephen Pacey ,  Lee Richard Roberts

    IPC分类号： A01N43/04 ,  A61K31/715 ,  C07H1/00

    CPC分类号： A61K31/715 ,  A23K10/12 ,  A23K20/163 ,  A23K50/10 ,  A61K31/7016 ,  A61K31/702

    摘要： 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.

    摘要翻译： 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。

    Treatment of rumen acidosis with α-amylase inhibitors
    4.
    发明授权
    Treatment of rumen acidosis with α-amylase inhibitors 失效
    用α-淀粉酶抑制剂治疗瘤胃酸中毒

    公开(公告)号：US07022684B2

    公开(公告)日：2006-04-04

    申请号：US10059667

    申请日：2002-01-29

    申请人： Bernard Joseph Banks ,  Mark Andrew Haxell ,  Graham Lunn ,  Michael Stephen Pacey ,  Lee Richard Roberts

    发明人： Bernard Joseph Banks ,  Mark Andrew Haxell ,  Graham Lunn ,  Michael Stephen Pacey ,  Lee Richard Roberts

    IPC分类号： A01N43/04 ,  A61K31/715

    CPC分类号： A61K31/715 ,  A23K10/12 ,  A23K20/163 ,  A23K50/10 ,  A61K31/7016 ,  A61K31/702

    摘要： 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 rumen 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 rumen 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.

    摘要翻译： 本文描述的发明涉及：在制备用于治疗瘤胃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; 适用于在动物中治疗瘤胃酸中毒的制剂，其包含与适当的赋形剂，稀释剂或载体混合的细菌α-淀粉酶和/或α-葡糖苷酶的有效抑制剂，所述合适的赋形剂，稀释剂或载体根据预期给药途径和标准 制药/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。

    Tetrahydronaphthyridine derivatives
    5.
    发明授权
    Tetrahydronaphthyridine derivatives 失效
    四氢萘并吡啶衍生物

    公开(公告)号：US07557121B2

    公开(公告)日：2009-07-07

    申请号：US11128804

    申请日：2005-05-12

    申请人： Graham Lunn ,  John Paul Mathias ,  Ross Sinclair Strang

    发明人： Graham Lunn ,  John Paul Mathias ,  Ross Sinclair Strang

    IPC分类号： A61K31/44 ,  C07D515/02

    CPC分类号： C07D471/04

    摘要： The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I′) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

    摘要翻译： 本发明涉及通式（I）的四氢萘并吡啶衍生物：或其中A和R 1如上所定义的通式（I'）的化合物，以及制备用于制备组合物的中间体的方法 包括由H3配体介导的治疗疾病，特别是炎性，过敏性和呼吸道疾病，病症和病症的用途。

    Tetrahydronaphthyridine Derivatives
    7.
    发明申请
    Tetrahydronaphthyridine Derivatives 审中-公开
    四氢萘并吡啶衍生物

    公开(公告)号：US20090258861A1

    公开(公告)日：2009-10-15

    申请号：US12491370

    申请日：2009-06-25

    申请人： Graham Lunn ,  John Paul Mathias ,  Ross Sinclair Strang

    发明人： Graham Lunn ,  John Paul Mathias ,  Ross Sinclair Strang

    IPC分类号： A61K31/55 ,  A61K31/506 ,  A61K31/497 ,  A61K31/4436 ,  A61P35/00

    CPC分类号： C07D471/04

    摘要： The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I′) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

    摘要翻译： 本发明涉及通式（I）的四氢萘并吡啶衍生物：或其中A和R 1如上所定义的通式（I'）的化合物，以及制备用于制备组合物的中间体的方法 包括由H3配体介导的治疗疾病，特别是炎性，过敏性和呼吸道疾病，病症和病症的用途。

    Tetrahydronaphthyridine derivatives
    8.
    发明申请
    Tetrahydronaphthyridine derivatives 失效
    四氢萘并吡啶衍生物

    公开(公告)号：US20050256135A1

    公开(公告)日：2005-11-17

    申请号：US11128804

    申请日：2005-05-12

    申请人： Graham Lunn ,  John Mathias ,  Ross Strang

    发明人： Graham Lunn ,  John Mathias ,  Ross Strang

    IPC分类号： A61K31/4745 ,  A61K31/497 ,  A61K31/506 ,  C07D471/02 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I′) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

    摘要翻译： 本发明涉及通式（I）的四氢萘啶衍生物或其中A和R 1如本文所定义的通式（I'），或其制备方法， 用于制备含有H3配体介导的治疗疾病，特别是炎性，过敏性和呼吸系统疾病，疾病和病症的治疗疾病的组合物和含有的组合物的中间体。

    Antiparasitic terpene alkaloids
    10.
    发明授权
    Antiparasitic terpene alkaloids 失效
    抗寄生虫萜生物碱

    公开(公告)号：US07494992B2

    公开(公告)日：2009-02-24

    申请号：US10777713

    申请日：2004-02-12

    申请人： Nathan A. Chubb ,  Douglas J. Critcher ,  James J. Eshelby ,  Graham Lunn ,  Andrew J. Rudge ,  Nigel D. Walshe ,  Paul H Wiedenau ,  David H. Williams

    发明人： Nathan A. Chubb ,  Douglas J. Critcher ,  James J. Eshelby ,  Graham Lunn ,  Andrew J. Rudge ,  Nigel D. Walshe ,  Paul H Wiedenau ,  David H. Williams

    IPC分类号： C07D491/04 ,  A61K31/5365

    CPC分类号： C07D498/04

    摘要： The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation.More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.

    摘要翻译： 本发明涉及新颖的萜烯生物碱及其作为抗寄生虫剂的用途。 本发明还涉及一种抗寄生虫剂，其包含本发明的萜烯生物碱化合物作为抗寄生虫制剂中的有效成分。 更具体地说，本发明涉及萜烯生物碱（1S，2R，4aS，5R，8R，8aR）-2-（乙酰氧基）-8a-羟基-3,8-二甲基-5-（1-甲基乙烯基） -1,2,4a，5,6,7,8,8a-八氢萘-1-基（2S，3aR，9bR）-6-氯-9β-羟基-5-甲基-1,2,3,3a， 5,9b-六氢吡咯并[2,3-c] [2,1]苯并恶嗪-2-羧酸乙酯。 还公开了包含其的药物组合物。