Amino acid complexes of C-aryl glucosides for treatment of diabetes and method

阅读量:

23

申请(专利)号:

10/117914

申请日期:

04/08/2002

公开/公告号:

US6774112

公开/公告日期:

08/10/2004

申请(专利权)人:

Bristol-Myers Squibb Company (Princeton, NJ)

发明人:

JZ Gougoutas

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被引量:

225

摘要:

Crystalline complexes are obtained from a 1:1 or 2:1 mixtures of either the (D) or (L) enantiomer of natural amino acids and compounds of formula wherein R 1 , R 2 and R 2a are independently hydrogen, OH, OR 5 , alkyl, —OCHF 2 , —OCF 3 , —SR 5a or halogen; R 3 and R 4 are independently hydrogen, OH, OR 5b , alkyl, cycloalkyl, CF 3 , —OCHF 2 , —OCF 3 , halogen, —CONR 6 R 6a , —CO 2 R 5c , —CO 2 H, —COR 6b , —CH(OH)R 6c , —CH(OR 5d )R 6d , —CN, —NHCOR 5e , —NHSO 2 R 5f , —NHSO 2 Aryl, —SR 5g , —SOR 5h , —SO 2 R 5i , or a five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO 2 , or R 3 and R 4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO 2 ; R 5 , R 5a , R 5b , R 5c , R 5d , R 5e , R 5f , R 5g , R 5h and R 5i are independently alkyl; R 6 , R 6a , R 6b , R 6c and R 6d are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R 6 and R 6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO 2 . A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above complex alone or in combination with another antidiabetic agent or other therapeutic agent.

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