Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1
申请人:Aicher Thomas Daniel
公开号:US20080275043A1
公开(公告)日:2008-11-06
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
本发明公开了具有11beta-HSD type 1拮抗活性的化合物的公式I:(I),以及制备这种化合物的方法。在另一实施例中,本发明公开了包含公式I化合物的制药组合物,以及将公式I和组合物用作药物治疗糖尿病,高血糖,肥胖症,高血压,高脂血症,综合征X和与高血糖有关的其他疾病的用途。
CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
申请人:AICHER Thomas Daniel
公开号:US20100184764A1
公开(公告)日:2010-07-22
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
本发明揭示了具有11beta-HSD type 1拮抗活性的I式化合物:(I),以及制备这种化合物的方法。在另一种实施方式中,本发明揭示了包括I式化合物的制药组合物,以及将I式和组合物用作药物治疗糖尿病,高血糖,肥胖症,高血压,高脂血症,X综合症和其他与高血糖有关的疾病的用途。
Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
申请人:Eli Lilly and Company
公开号:US07713979B2
公开(公告)日:2010-05-11
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
Synthesis of pyrrolidines and pyrrolidinones by the rhodium complex catalyzed cyclization of unsaturated amines
作者:Jian Qiang Zhou、Howard Alper
DOI:10.1021/jo00038a019
日期:1992.6
N-Allylic arylamines react with carbon monoxide, sodium borohydride, 2-propanol, and catalytic amounts of the zwitterionic complex eta-6-C6H6BPh3-Rh(COD)+ (1), to form pyrrolidines as the main products in most cases. Pyrrolidinones result from N-allylic alkylamines. An alternate route to the lactams from N-allylic alkylamines involves synthesis gas instead of CO/NaBH4, together with the dual catalytic system 1/[Ru(CO)3Cl2]2. Complementary to the N-allylic arylamine route to pyrrolidines with NaBH4 and 1 is the use of synthesis gas, 1, and 1,4-bis(diphenylphosphino)butane.