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    C-aryl glucoside SGLT2 inhibitors and method
    3.
    发明授权
    C-aryl glucoside SGLT2 inhibitors and method 有权
    C-芳基葡糖苷SGLT2抑制剂及方法

    公开(公告)号：US06414126B1

    公开(公告)日：2002-07-02

    申请号：US09679027

    申请日：2000-10-04

    申请人： Bruce Ellsworth ,  William N. Washburn ,  Philip M. Sher ,  Gang Wu ,  Wei Meng

    发明人： Bruce Ellsworth ,  William N. Washburn ,  Philip M. Sher ,  Gang Wu ,  Wei Meng

    IPC分类号： C07H1520

    CPC分类号： C07H15/203 ,  A61K31/70 ,  A61K31/7034 ,  A61K45/06 ,  C07C43/225 ,  C07C45/46 ,  C07C49/84 ,  A61K2300/00

    摘要： SGLT2 inhibiting compounds are provided having the formula where R1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CN, —CO2R5b, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5h)R6d, —CONR6R6a, —NHCOR5c, —NHSO2R5d, —NHSO2Aryl, Aryl, —SR5e, —SOR5f, —SO2R5g, —SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,aryl, alkylaryl or cycloalkyl, or R6 and R6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH2)n where n is 0-3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

    摘要翻译： 提供的SGLT2抑制化合物具有式R 1，R 2和R 2a独立地是氢，OH，OR 5，低级烷基，CF 3，OCHF 2，OCF 3，SR 5i或卤素，或者R 1，R 2和R 2a中的两个与它们相同的碳 R 3和R 4独立地是氢，OH，OR 5 a，OA基，OCH 2芳基，低级烷基，环烷基，CF 3，-OCHF 2，-OCF 3，卤素，-CN，-CO 2 R 5b ，-CO 2 H，-COR 6 b，-CH（OH）R 6c，-CH（OR 5h）R 6d，-CONR 6 R 6 a，-NHCOR 5 C，-NHSO 2 R 5d，-NHSO 2芳基，芳基，-SR 5e，-SOR 5 f，-SO 2 R 5，-SO 2芳基或五 ，六或七元杂环，或R 3和R 4与它们所连接的碳一起形成环状五，六或七元碳环或杂环; R5，R5a，R5b，R5c，R5d，R5e，R5f，R5g，R5h R5i独立地为低级烷基; R6，R6a，R6b，R6c和R6d独立地为氢，烷基，芳基，烷基芳基或环烷基，或R6和R6a与它们所连接的氮一起 形成五至六元或七元杂环; A为O，S，NH或（CH2）n，其中n为0-3。另外还提供了一种用于治疗糖尿病和相关疾病的方法，该方法采用上述的SGLT2抑制量 化合物单独或与另一种抗糖尿病剂或其它治疗剂组合。

    2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
    4.
    发明授权
    2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors 有权
    2-氨基-3-官能化的四氢化萘衍生物和相关的糖原磷酸化酶抑制剂

    公开(公告)号：US07365061B2

    公开(公告)日：2008-04-29

    申请号：US11273167

    申请日：2005-11-14

    申请人： Philip M. Sher ,  Gang Wu ,  Wei Meng ,  Alexandra A. Nirschl ,  William N. Washburn ,  Terry Stouch

    发明人： Philip M. Sher ,  Gang Wu ,  Wei Meng ,  Alexandra A. Nirschl ,  William N. Washburn ,  Terry Stouch

    IPC分类号： A61K31/404 ,  A61K31/454 ,  A61K31/397 ,  C07D209/04 ,  C07D205/04 ,  C07D401/08

    CPC分类号： C07D209/42 ,  C07D235/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/04 ,  C07D493/08 ,  C07D495/04

    摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X, Y and Z are defined herein.

    摘要翻译： 提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管 与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件 包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。 这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，X，Y和Z在本文中定义。

    O-aryl glucoside SGLT2 inhibitors and method
    5.
    发明授权
    O-aryl glucoside SGLT2 inhibitors and method 有权
    O-芳基葡糖苷SGLT2抑制剂及方法

    公开(公告)号：US06683056B2

    公开(公告)日：2004-01-27

    申请号：US09791512

    申请日：2001-02-23

    申请人： William N. Washburn ,  Philip M. Sher ,  Gang Wu

    发明人： William N. Washburn ,  Philip M. Sher ,  Gang Wu

    IPC分类号： A61K3170

    CPC分类号： C07H15/203 ,  C40B40/00

    摘要： wherein when Y is  or heteroaryl; A is —O(CH2)m, S, —NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.

    摘要翻译： 其中当Y是 - 杂芳基时，A是-O（CH2）m，S，-NH（CH2）m或（CH2）n，其中n是0-3，m是0-2; R 1至R 6 本发明还提供了一种用于治疗糖尿病和相关疾病的方法，其使用单独的SGLT2抑制量的上述化合物或与一种，两种或更多种其它抗糖尿病药物组合，和/或一种，两种或更多种降血脂剂 。

    2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
    6.
    发明授权
    2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors 有权
    2-氨基萘衍生物和相关的糖原磷酸化酶抑制剂

    公开(公告)号：US07223786B2

    公开(公告)日：2007-05-29

    申请号：US11273479

    申请日：2005-11-14

    申请人： Wei Meng ,  Philip M. Sher ,  Bruce A. Ellsworth ,  William N. Washburn

    发明人： Wei Meng ,  Philip M. Sher ,  Bruce A. Ellsworth ,  William N. Washburn

    IPC分类号： A61K31/405 ,  C07D209/12 ,  C07D209/14

    CPC分类号： C07D235/24 ,  C07D209/42 ,  C07D491/04 ,  C07D495/04

    摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1 and R2 are defined herein.

    摘要翻译： 提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管 与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件 包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。 这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1和R 2 2定义在本文中。

    2-hydroxy-3—(4-hydroxy-3-sulfonamidophenyl)—propylamines useful as beta 3 adrenergic agonists
    7.
    发明授权
    2-hydroxy-3—(4-hydroxy-3-sulfonamidophenyl)—propylamines useful as beta 3 adrenergic agonists 有权
    可用作β3肾上腺素能激动剂的2-羟基-3-（4-羟基-3-磺酰胺基苯基） - 丙胺

    公开(公告)号：US06436914B1

    公开(公告)日：2002-08-20

    申请号：US09912778

    申请日：2001-07-25

    申请人： Philip M. Sher ,  William N. Washburn ,  Jollie D. Godfrey, Jr.

    发明人： Philip M. Sher ,  William N. Washburn ,  Jollie D. Godfrey, Jr.

    IPC分类号： A61K3166

    CPC分类号： C07D323/00 ,  C07C311/08 ,  C07C2601/14 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18 ,  C07F9/4021

    摘要： Compounds are provided having the formula including pharmaceutically acceptable salts thereof, wherein R1 is lower alkyl, aryl or arylalkyl; A is hydrogen or B is hydrogen, alkyl, alkenyl, or but when A is hydrogen, B may only be R2, R2′, R2″, R3 R3′ and R3″ are as defined herein; m is 0−3. These compounds possess activity at the beta 3 adrenergic receptor in mammals and are useful in the treatment of diabetes, obesity, depression, achalasia and intestinal hypermotility disorders.

    摘要翻译： 提供具有包括其药学上可接受的盐的化合物，其中R 1是低级烷基，芳基或芳烷基; A是氢或B是氢，烷基，烯基，或者当A是氢时，B可以仅是R 2，R 2'，R 2“，R 3 R3'和R3“如本文所定义; m是0-3。 这些化合物在哺乳动物的β3肾上腺素能受体中具有活性，可用于治疗糖尿病，肥胖症，抑郁症，贲门失弛缓症和肠过度运动障碍。