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    • 7. 发明申请
    • 2-AMINONAPHTHALENE DERIVATIVES AND RELATED GLYCOGEN PHOSPHORYLASE INHIBITORS
    • 2-氨基萘基衍生物和相关的GLYCOGEN磷酸酶抑制剂
    • WO2006055435A1
    • 2006-05-26
    • PCT/US2005/040985
    • 2005-11-14
    • BRISTOL-MYERS SQUIBB COMPANYMENG, WeiSHER, Philip, M.ELLSWORTH, Bruce, A.WASHBURN, William, N.
    • MENG, WeiSHER, Philip, M.ELLSWORTH, Bruce, A.WASHBURN, William, N.
    • C07D209/42A61K31/404A61P3/10
    • 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 [PLEASE INSERT CHEMICAL STRUCTURE HERE] I 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。 这些新型化合物具有本文所定义的结构,即其中W,R 1和R 2的定义如下。
    • 8. 发明申请
    • CATECHOLAMINE SURROGATES USEFUL AS 'beta'3 AGONISTS
    • CATECHOLAMINE SURROGATES有用作β3激动剂
    • WO1997037646A1
    • 1997-10-16
    • PCT/US1997005324
    • 1997-04-01
    • BRISTOL-MYERS SQUIBB COMPANY
    • BRISTOL-MYERS SQUIBB COMPANYCHENG, Peter, T., W.BISACCHI, Gregory, S.GAVAI, Ashvinikumar, V.POSS, Kathleen, M.RYONO, Denis, E.SHER, Philip, M.SUN, Chong-QingWASHBURN, William, N.
    • A61K31/18
    • C07C311/46C07C311/08C07C311/39C07D263/32C07D277/28C07F9/4056
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof. As used in formula (I), and throughout the specification, the symbols have the following meanings: R is lower alkyl, aryl or arylalkyl; R is hydrogen, hydroxyl, hydroxymethyl or halogen; R is hydrogen or alkyl; R and R are independently hydrogen, alkoxy, alkoxymethyl, hydroxyl, -CN, -CON(R )R 2 , -N(R )R , -NR COR , -NR SO2R ; or R and R may together with the carbon atoms to which they are bonded form a heterocycle; R , R and R are independently A or B, wherein A is hydrogen, alkyl, cylcoalkyl, halogen, hydroxyl, aryl, alkoxy, cyano, -SR , -SOR , -SO2R , -N(R )R , -NR COR , -OCH2CON(R )R , -OCH2CO2R , CON(R )R , -CO2R ; and B is -(CH2)nN(R )R , -(CH2)mPO(OR )OR , -(CH2)nNR COR , -O-aryl, -OCH2CH2N(R )R , -COR , -SO2N(R )R , -NR CO2R , -NR CO(N(R )R ), heterocycle or -R and R may together with the carbon atoms to which they are bonded form a heterocycle, provided that at least one of R , R and R is B; R and R are independently hydrogen or lower alkyl; R is lower alkyl; R is hydrogen, lower alkyl, aryl or arylalkyl; m is an integer of 0 to 6; and n is an integer of 1 to 6. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
    • 式(I)化合物及其药学上可接受的盐。 在式(I)中使用,并且在整个说明书中,符号具有以下含义:R 1是低级烷基,芳基或芳基烷基; R 2是氢,羟基,羟甲基或卤素; R 3是氢或烷基; R 4和R 4独立地是氢,烷氧基,烷氧基甲基,羟基,-CN,-CON(R 6)R 6',-CO 2,R 6, R 6)R 6,-NR 6 COR 8,-NR 6 SO 2 R 1; 或R 4和R 4'可以与它们所键合的碳原子一起形成杂环; R 5,R 5和R 5独立地是A或B,其中A是氢,烷基,环烷基,卤素,羟基,芳基,烷氧基,氰基,-SR 7,-SOR -SO 2 R 7,-N(R 6)R 6',-NR 6 COR 8,-OCH 2 CON(R 6)R 6,-OCH 2 CO 2 R CON(R 6)R 6,-CO 2 R 6; 并且B是 - (CH 2)n N(R 6)R 6', - (CH 2)m PO(OR 6)OR 6, - (CH 2)n NR 6 COR 8, -O-芳基,-OCH 2 CH 2 N(R 6)R 6',-COR 7,-SO 2 N(R 6)R 6',-NR 6 CO 2 R 7, NR 6 CO(N(R 6)R 6'),杂环或-R 5和R 5可以与它们所键合的碳原子一起形成杂环,条件是 R 5,R 5'和R 5“中的至少一个是B; R 6和R 6独立地是氢或低级烷基; R 7是低级烷基; R 8是氢,低级烷基,芳基或芳基烷基; m为0〜6的整数。 并且n是1至6的整数。这些化合物是β三肾上腺素能受体激动剂,因此可用于例如糖尿病,肥胖症和胃肠道疾病的治疗。