Title:
AMINO ACID COMPLEXES OF C-ARYL GLUCOSIDES FOR TREATMENT OF DIABETES AND METHOD
Document Type and Number:
WIPO Patent Application WO2002083066
Kind Code:
A3
Abstract:
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 (I) wherein R1, R2 and R2a are independently hydrogen, OH, OR5, alkyl, -OCHF<2>, -OCF<3>, -SR5a or halogen; R3 and R4 are independently hydrogen, OH, OR5b, alkyl, cycloalkyl, CF<3>, -OCHF<2>, -OCF<3>, halogen, -CONR6R6a, -CO<2>R5c, -CO<2>H, -COR6b, -CH(OH)R6c, -CH(OR5d)R6d, -CN, -NHCOR5e, -NHSO<2>R5f, -NHSO<2>Aryl, -SR5g, -SOR5h, -SO<2>R5i, 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 R3 and R4 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>; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently 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 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.
Inventors:
GOUGOUTAS JACK Z (US)
Application Number:
PCT/US2002/011066
Publication Date:
March 06, 2003
Filing Date:
April 08, 2002
Export Citation:
Assignee:
BRISTOL MYERS SQUIBB CO (US)
GOUGOUTAS JACK Z (US)
GOUGOUTAS JACK Z (US)
International Classes:
C07H7/04; A61K31/351; A61K31/7004; A61K45/06; A61P3/04; A61P3/06; A61P3/10; A61P9/10; A61P9/12; A61P13/12; A61P17/02; A61P27/02; C07D309/10; C07H15/203; (IPC1-7): C07H7/04; A61K31/70
Domestic Patent References:
| WO1998031697A1 | 1998-07-23 | |||
| WO2001016147A1 | 2001-03-08 |
Foreign References:
| US5663377A | 1997-09-02 | |||
| US5444050A | 1995-08-22 |
Other References:
See also references of EP 1385856A4
Download PDF: