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    Thiadiazole compounds useful as inhibitors of H.sup.+ /K.sup.+ atpase
    3.
    发明授权
    Thiadiazole compounds useful as inhibitors of H.sup.+ /K.sup.+ atpase 失效
    可用作H + / K + atpase抑制剂的噻二唑化合物

    公开(公告)号：US6060472A

    公开(公告)日：2000-05-09

    申请号：US55209

    申请日：1998-04-06

    申请人： Khashayar Karimian ,  Tim Fat Tam ,  Regis C. S. H. Leung-Toung ,  Wanren Li

    发明人： Khashayar Karimian ,  Tim Fat Tam ,  Regis C. S. H. Leung-Toung ,  Wanren Li

    IPC分类号： C07D285/08 ,  C07D417/12 ,  C07D417/14 ,  A61K31/496 ,  C07D417/04

    CPC分类号： C07D285/08 ,  C07D417/12 ,  C07D417/14

    摘要： Novel 3,5-disubstituted 1,2,4-thiadiazole compounds are provided, which are effective in treating peptic ulcers by the inhibition of H.sup.+ /K.sup.+ -ATPase. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadiazole corresponding to the general formula (I): ##STR1## where R.sup.1 is a group with cell penetration properties for the inhibition of the enzyme in-vitro and in-vivo, and Y is a substituent that tunes the reactivity of the inhibitor towards the cysteine residue of H.sup.+ /K.sup.+ -ATPase. The Y group may also serve in recognition.

    摘要翻译： 提供了新的3,5-二取代的1,2,4-噻二唑化合物，其通过抑制H + / K + -ATP酶而有效治疗消化性溃疡。 本发明的化合物是相应于通式（I）的3,5-二取代的1,2,4-噻二唑：其中R1是在体外和体内抑制酶的细胞穿透性的基团 ，Y是调节抑制剂对H + / K + -ATPase的半胱氨酸残基的反应性的取代基。 Y团队也可以承认。

    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones
    5.
    发明授权
    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones 失效
    3-羟基-4-吡啶酮的环烷基衍生物

    公开(公告)号：US08097624B2

    公开(公告)日：2012-01-17

    申请号：US12149853

    申请日：2008-05-09

    申请人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    发明人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    IPC分类号： A61K31/5377 ,  A61K31/44 ,  A61K31/497 ,  C07D213/78 ,  C07D401/06 ,  C07D413/06

    CPC分类号： C07D213/81

    摘要： The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups. X is C3-C6 cycloalkyl; Y is selected from the group consisting of C1 to C6 cycloalkyl; C1 to C6 alkyl, and C1 to C6 alkyl monosubstituted with a C3-C6 cycloalkyl; T is C1 to C6 alkyl; W is C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R4 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R5 is selected from the group consisting of hydrogen and C1 to C6 alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.

    摘要翻译： 本发明提供3-羟基-4-吡啶酮的环烷基衍生物，其可用于螯合金属离子如铁。 描述其准备和使用。 特别地，本发明涉及在化学和生物系统中除铁，包括具有式I的螯合剂，其中R1是X，条件是R2是Y; 或R1为T，条件是R2为W; 或R1为X，条件是R2R5N一起形成选自哌啶基，吗啉基，吡咯烷基或哌嗪基的杂环，其中哌啶基，吗啉基，吡咯烷基或哌嗪基是未取代的或被一至三个C1至C6烷基取代 。 X是C 3 -C 6环烷基; Y选自C1-C6环烷基; C 1 -C 6烷基和被C 3 -C 6环烷基单取代的C 1至C 6烷基; T是C1-C6烷基; W是C3-C6环烷基; R 3选自氢和C 1至C 6烷基; R 4选自氢和C 1至C 6烷基; R5选自氢和C1至C6烷基; 及其药学上可接受的盐。 这些化合物的药物组合物可用于从具有铁超负荷疾病的患者中去除过量的身体铁。

    Process for the manufacture of 3-hydroxy-N-alkyl-1-cycloalky1-6-alkyl-4-oxo-1,4-dihydropyridine-2-carboxamide and its related analogues
    6.
    发明授权
    Process for the manufacture of 3-hydroxy-N-alkyl-1-cycloalky1-6-alkyl-4-oxo-1,4-dihydropyridine-2-carboxamide and its related analogues 有权
    制备3-羟基-N-烷基-1-环烷基-1-6-烷基-4-氧代-1,4-二氢吡啶-2-甲酰胺及其相关类似物的方法

    公开(公告)号：US07893269B2

    公开(公告)日：2011-02-22

    申请号：US11667751

    申请日：2005-11-17

    申请人： Tim Fat Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Vittoria Agostino ,  Birenkumar Hasmukhbhai Shah

    发明人： Tim Fat Tam ,  Regis Leung-Toung ,  Yanqing Zhao ,  Wanren Li ,  Yingsheng Wang ,  Sandra Vittoria Agostino ,  Birenkumar Hasmukhbhai Shah

    IPC分类号： C07D403/02

    CPC分类号： C07D213/81 ,  Y02P20/55

    摘要： The present invention relates to a novel process for the preparation of 1-alkyl or 1-cycloalkyl derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine-2-carboxamide of formula (I). The process includes reacting an amine R2NH2 with a compound of formula (II) in a solution of metal hydroxide in water to give a compound of formula (III). Subsequent reaction of the compound of formula (III) with an acid chloride formation reagent in an inert solvent gives compounds of formula (I). The acid chloride formation reagent is selected from oxalyl chloride and dimethylformamide, dimethylchloromethylene-ammonium chloride and thionyl chloride and dimethylformamide. If desired, a compound of formula (I) where R5 is hydrogen may be formed when an intermediate substituent is used wherein R5 is an alcohol protective group removable by catalytic hydrogenation.

    摘要翻译： 本发明涉及制备式（I）的3-羟基-4-氧代-1,4-二氢吡啶-2-甲酰胺的1-烷基或1-环烷基衍生物的新方法。 该方法包括使胺R 2 NH 2与式（II）化合物在金属氢氧化物在水中的溶液中反应，得到式（III）化合物。 式（III）化合物与酰氯形成试剂在惰性溶剂中的随后反应得到式（I）化合物。 酰氯形成试剂选自草酰氯和二甲基甲酰胺，二甲基氯亚甲基氯化铵和亚硫酰氯和二甲基甲酰胺。 如果需要，当使用R5是可通过催化氢化除去的醇保护基团的中间取代基时，可以形成其中R 5为氢的式（I）化合物。

    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones
    7.
    发明申请
    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones 失效
    3-羟基-4-吡啶酮的环烷基衍生物

    公开(公告)号：US20090170850A1

    公开(公告)日：2009-07-02

    申请号：US12149853

    申请日：2008-05-09

    申请人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    发明人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    IPC分类号： A61K31/5377 ,  C07D213/78 ,  A61K31/44 ,  A61K31/497 ,  C07D401/06 ,  C07D413/06

    CPC分类号： C07D213/81

    摘要： The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups. X is C3-C6 cycloalkyl; Y is selected from the group consisting of C1 to C6 cycloalkyl; C1 to C6 alkyl, and C1 to C6 alkyl monosubstituted with a C3-C6 cycloalkyl; T is C1 to C6 alkyl; W is C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R4 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R5 is selected from the group consisting of hydrogen and C1 to C6 alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.

    摘要翻译： 本发明提供3-羟基-4-吡啶酮的环烷基衍生物，其可用于螯合金属离子如铁。 描述其准备和使用。 特别地，本发明涉及在化学和生物系统中除铁，包括具有式I的螯合剂，其中R1是X，条件是R2是Y; 或R1为T，条件是R2为W; 或R1为X，条件是R2R5N一起形成选自哌啶基，吗啉基，吡咯烷基或哌嗪基的杂环，其中哌啶基，吗啉基，吡咯烷基或哌嗪基是未取代的或被一至三个C1至C6烷基取代 。 X是C 3 -C 6环烷基; Y选自C1-C6环烷基; C 1 -C 6烷基和被C 3 -C 6环烷基单取代的C 1至C 6烷基; T是C1-C6烷基; W是C3-C6环烷基; R 3选自氢和C 1至C 6烷基; R 4选自氢和C 1至C 6烷基; R5选自氢和C1至C6烷基; 及其药学上可接受的盐。 这些化合物的药物组合物可用于从具有铁超负荷疾病的患者中去除过量的身体铁。

    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones
    8.
    发明授权
    Cycloalkyl derivatives of 3-hydroxy-4-pyridinones 失效

    公开(公告)号：US07410985B2

    公开(公告)日：2008-08-12

    申请号：US10580011

    申请日：2004-11-18

    申请人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    发明人： Tim Fat Tam ,  Michael Spino ,  Wanren Li ,  Yingsheng Wang ,  Yanqing Zhao ,  Birenkumar Hasmukhbhai Shah

    IPC分类号： A61K31/4412 ,  C07D213/81

    CPC分类号： C07D213/81

    摘要： The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2 R5 N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups. X is C3-C6 cycloalkyl; Y is selected from the group consisting of C1 to C6 cycloalkyl; C1 to C6 alkyl, and C1 to C6 alkyl monosubstituted with a C3-C6 cycloalkyl; T is C1 to C6 alkyl; W is C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R4 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R5 is selected from the group consisting of hydrogen and C1 to C6 alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.