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    Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
    35.
    发明授权
    Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia 失效
    苯氧基 - 乙酸可用于治疗胰岛素抵抗和高血糖症

    公开(公告)号：US06844358B2

    公开(公告)日：2005-01-18

    申请号：US10300997

    申请日：2002-11-21

    申请人： Michael S. Malamas ,  Jay E. Wrobel ,  Arlene J. Dietrich ,  Zenan Li ,  Iwan Gunawan

    发明人： Michael S. Malamas ,  Jay E. Wrobel ,  Arlene J. Dietrich ,  Zenan Li ,  Iwan Gunawan

    IPC分类号： C07D307/80 ,  C07D333/56 ,  C07D333/60 ,  A61K31/44 ,  A61K31/42 ,  A61K31/425 ,  C07D405/00 ,  C07D411/00

    CPC分类号： C07D333/60 ,  C07D307/80 ,  C07D333/56

    摘要： This invention provides compounds of Formula I having the structure wherein: A is O, S, or N; B is —(CH2)m—, —CH(OH)—, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, —CH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or —OR5; m=1-6; n=1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is —CO2R10, —CONHR10, tetrazole, or —PO3; R9 and R10 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

    摘要翻译： 本发明提供具有以下结构的式I化合物：其中A为O，S或N; B为 - （CH 2）m - ， - CH（OH） - 或羰基; R 1为氢，卤素， 1-6个碳原子的烷氧基或1-6个碳原子的烷氧基，或三氟甲基; R 2是1-18个碳原子的烷基，6-10个碳原子的芳基，7-15个碳原子的芳基烷基， 烷基部分为1-6个碳原子; Het为R 2a为1-3个碳原子的亚烷基; G为氧，硫或氮; R 3，R 4各自独立地为氢，卤素 ，1-3个碳原子的烷基，6-10个碳原子的芳基或含有1至3个选自氧，氮，硫的杂原子的5至7个环原子的杂环; R 5是氢，1- 6个碳原子，-CH（R 7）R 8，-C（CH 2）n CO 2 R 9，-C（CH 3）2 CO 2 R 9，-CH（R 7）（CH 2）n CO 2 R 9或CH（R 7）C 6 H 4 CO 2 R 9; R 6是氢，卤素，1-6个碳原子的烷基或-OR 5; m = 1-6; n = 1- 6; R 7是氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; R -CONR 10，四唑或-PO 3; R 9和R 10各自独立地为氢，1-6个碳原子的烷基，6- 10个碳原子或7-15个碳原子的芳烷基;或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

    Amino-thiazolidinediones useful in the treatment of insulin resistance and hyperglycemia
    37.
    发明授权
    Amino-thiazolidinediones useful in the treatment of insulin resistance and hyperglycemia 失效
    用于治疗胰岛素抵抗和高血糖症的氨基 - 噻唑烷二酮类

    公开(公告)号：US06214842B1

    公开(公告)日：2001-04-10

    申请号：US09568832

    申请日：2000-05-11

    申请人： Michael S. Malamas ,  Iwan Gunawan

    发明人： Michael S. Malamas ,  Iwan Gunawan

    IPC分类号： A61K3156

    CPC分类号： C07D413/12 ,  C07D277/42 ,  C07D417/12

    摘要： This invention provides compounds of Formula I having the structure wherein: R is hydrogen or alkyl of 1-6 carbon atoms; A is R1, R2, R3 are each, independently, hydrogen, alkoxy of 1-6 carbon atoms, thioalkyl of 1-6 carbon atoms, trifluoromethyl, R4 is hydrogen, alkyl of 1-6 carbon atoms, halogen, or alkoxy of 1-6 carbon atoms; R5 is phenyl, naphthyl, thienyl, furyl, wherein R5 may be optionally mono-, di-, or tri-substituted with a sustituent selected from the group consisting of alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, trifluoromethyl, halogen, alkoxycarbonyl of 2-7 carbon atoms, alkylamino of 1-6 carbon atoms, and dialkylamino in which each of the alkyl groups is of 1-6 carbon atoms, nitro, cyano, —CO2H, alkylcarbonyloxy of 2-7 carbon atoms, and alkylcarbonyl of 2-7 carbon atoms; m=1-4; n=1-4; and X=O, S, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

    摘要翻译： 本发明提供具有以下结构的式I化合物，其中R是氢或1-6个碳原子的烷基; A是R 1，R 2，R 3各自独立地是氢，1-6个碳原子的烷氧基，1-6个碳的硫代烷基 原子，三氟甲基，R 4是氢，1-6个碳原子的烷基，卤素或1-6个碳原子的烷氧基; R 5是苯基，萘基，噻吩基，呋喃基，其中R 5可以是任选的单 - ，二 - 或三 被选自1-6个碳原子的烷基，1-6个碳原子的烷氧基，三氟甲基，卤素，2-7个碳原子的烷氧基羰基，1-6个碳原子的烷基氨基和二烷基氨基取代的取代基 其中每个烷基具有1-6个碳原子，硝基，氰基，-CO 2 H，2-7个碳原子的烷基羰基氧基和2-7个碳原子的烷基羰基; m = 1-4; n = 1-4; 和X = O，S或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

    Aryl-oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
    38.
    发明授权
    Aryl-oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia 失效
    可用于治疗胰岛素抵抗和高血糖症的芳基 - 氧代 - 乙酸

    公开(公告)号：US6110963A

    公开(公告)日：2000-08-29

    申请号：US307918

    申请日：1999-05-10

    申请人： Michael S. Malamas

    发明人： Michael S. Malamas

    IPC分类号： C07C59/90 ,  C07D257/04 ,  C07D307/80 ,  C07D333/56 ,  C07D405/12 ,  C07D413/06 ,  C07D417/12 ,  A61K31/38 ,  A61K31/35 ,  A61K31/415 ,  C07D417/00

    CPC分类号： C07D257/04 ,  C07C59/90 ,  C07D307/80 ,  C07D333/56 ,  C07D405/12 ,  C07D413/06 ,  C07D417/12

    摘要： This invention provides compounds of Formula I having the structure ##STR1## wherein A is C or N;B is O, S, N, or CH.dbd.CH;E is ##STR2## or --X--D; D is ##STR3## or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole;Y is hydrogen, alkyl of 1-6 carbon atoms, or halogen;Z is O, S, or N;R is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, or trifluoromethyl;R.sup.1 is alkyl of 1-12 carbon atoms, aryl of 6-10 carbon atoms, aralkyl of 7-15 carbon atoms, halogen, Het-alkyl wherein the alkyl moiety contains 1-6 carbon atoms, or aryl mono-, di- or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, trifluoromethyl, and alkoxy of 1-6 carbon atoms;Het is ##STR4## G is O, S, or N; and the remaining variables are as defined in claim 1, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin or hyperglycemia.

    摘要翻译： 本发明提供具有其中A为C或N的结构的式I化合物; B是O，S，N或CH = CH; E为或-X-D; D是1-12个碳原子的烷基; X是CO，CH（OH），CH 2或-CH-S-2-苯并噻唑; Y为氢，1-6个碳原子的烷基或卤素; Z是O，S或N; R为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素或三氟甲基; R1为1-12个碳原子的烷基，6-10个碳原子的芳基，7-15个碳原子的芳烷基，卤素，其中烷基部分含有1-6个碳原子的Het-烷基，或芳基一，二或二 被选自卤素，1-6个碳原子的烷基，三氟甲基和1-6个碳原子的烷氧基的取代基取代三取代; Het是G是O，S或N; 并且其余变量如权利要求1所定义，或其药学上可接受的盐，其可用于治疗与胰岛素或高血糖相关的代谢紊乱。

    Benzyl and naphthalenylmethyl thiophenones and cyclopentenones as antihyperglycemic agents
    39.
    发明授权
    Benzyl and naphthalenylmethyl thiophenones and cyclopentenones as antihyperglycemic agents 失效
    苄基和萘甲基噻吩酮和环戊烯酮作为抗高血糖药

    公开(公告)号：US5610197A

    公开(公告)日：1997-03-11

    申请号：US423624

    申请日：1995-04-17

    申请人： Michael S. Malamas

    发明人： Michael S. Malamas

    IPC分类号： C07C45/51 ,  C07C45/68 ,  C07C45/71 ,  C07C49/747 ,  C07C49/753 ,  C07D333/32 ,  A61K31/12 ,  C07C49/213

    CPC分类号： C07D333/32 ,  C07C45/512 ,  C07C45/68 ,  C07C45/71 ,  C07C49/747 ,  C07C49/753

    摘要： This invention relates to benzyl and naphthalenylmethyl thiophenones and cyclopentenones, some of which are novel, which have oral antihyperglycemic activity in diabetic mice, a genetic animal model of non-insulin dependent diabetes mellitus. These compounds are represented by the formula ##STR1## wherein: R.sup.2 and R.sup.3 are independently selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl or R.sup.2 together with R.sup.3 forms a benzo ring fused to the phenyl ring and optionally substituted with one or two substituents independently selected from C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl;R.sup.1 is selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl; andR.sup.4 is selected from the group consisting of: ##STR2## wherein R.sup.5 is H or C.sub.1-6 alkyl or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及苄基和萘甲基噻吩酮和环戊烯酮，其中一些是新型的，其在糖尿病小鼠中具有口服抗高血糖活性，这是非胰岛素依赖性糖尿病的遗传动物模型。 这些化合物由下式表示：其中：R 2和R 3独立地选自氢，C 1-6烷基，卤素，C 1-6烷氧基，硫代C 1-6烷基或三氟甲基或R 2与R 3一起形成苯并 任选地被一个或两个独立地选自C 1-6烷基，卤素，C 1-6烷氧基，硫代C 1-6烷基或三氟甲基的取代基取代; R 1选自氢，C 1-6烷基，卤素，C 1-6烷氧基，硫代C 1-6烷基或三氟甲基; 并且R 4选自：其中R 5是H或C 1-6烷基或其药学上可接受的盐。