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    • 6. 发明授权
    • 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
    • 2-氨基萘衍生物和相关的糖原磷酸化酶抑制剂
    • US07223786B2
    • 2007-05-29
    • US11273479
    • 2005-11-14
    • Wei MengPhilip M. SherBruce A. EllsworthWilliam N. Washburn
    • Wei MengPhilip M. SherBruce A. EllsworthWilliam N. Washburn
    • A61K31/405C07D209/12C07D209/14
    • C07D235/24C07D209/42C07D491/04C07D495/04
    • 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.
    • 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。
    • 10. 发明授权
    • Sulfonic, phosphonic or phosphiniic acid .beta..sub.3 agonist derivatives
    • 磺酸,膦酸或次膦酸β3激动剂衍生物
    • US5491134A
    • 1996-02-13
    • US307217
    • 1994-09-16
    • Philip M. SherArvind Mathur
    • Philip M. SherArvind Mathur
    • C07C309/11C07F9/38C07F9/40A61K31/66A61K31/185C07F9/30
    • C07F9/3808C07C309/11C07F9/4006
    • Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: A is a bond or --OCH.sub.2 --, where the oxygen is linked to R.sup.1 ;B is --CH.sub.2 -- or when R.sup.3 is hydrogen, B may be --CH.sub.2 O-- where the oxygen is linked to the phenyl ring;R.sup.1 is an aryl group;R.sup.2 is hydrogen or lower alkyl;R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 together form the group --CH.sub.2 CH.sub.2 --; andR.sup.4 is --SO.sub.3 H, --P(O.sub.2 H)R.sup.5, --P(O.sub.2 R.sup.5')R.sup.5, --PO.sub.3 H.sub.2, --PO.sub.3 HR.sup.5' or --PO.sub.3 (R.sup.5').sub.2 where R.sup.5 and R.sup.5' are independently lower alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, for example, in the treatment of diabetes, obesity, achalasia, and gastrointestinal diseases.
    • 式Ⅰ化合物及其药学上可接受的盐,其中:A是一个键或-OCH 2 - ,其中氧连接到R 1; B是-CH 2 - 或当R 3是氢时,B可以是-CH 2 O-,其中氧连接到苯环上; R1是芳基; R2是氢或低级烷基; R3是氢; 或R 2和R 3一起形成基团-CH 2 CH 2 - ; R4是-SO3H,-P(O2H)R5,-P(O2R5')R5,-PO3H2,-PO3HR5'或-PO3(R5')2,其中R5和R5'独立地是低级烷基。 这些化合物是β3肾上腺素能受体激动剂,并且可用于例如治疗糖尿病,肥胖症,贲门失弛缓症和胃肠道疾病。