CRYSTALLINE SOLVATES AND COMPLEXES OF (1S)-1,5-ANHYDRO-1-C-(3-((PHENYL)METHYL)PHENYL)-D-GLUCITOL DERIVATIVES HAVING AMINO ACIDS AS SGLT2 INHIBITORS FOR TREATING DIABETES

Title:

CRYSTALLINE SOLVATES AND COMPLEXES OF (1S)-1,5-ANHYDRO-1-C-(3-((PHENYL)METHYL)PHENYL)-D-GLUCITOL DERIVATIVES HAVING AMINO ACIDS AS SGLT2 INHIBITORS FOR TREATING DIABETES

Document Type and Number:

Japanese Patent JP2019059779

Kind Code:

A

Abstract:

To provide novel free acid polymorphic crystals of SGLT2 inhibitors, production methods of the crystals, and pharmaceutical compositions containing the crystals, which possess an effect of inhibiting the sodium dependent glucose transporters (SGLT2) in the intestine and kidney of mammals and are useful in treatment of diabetes, diabetic complications, and the like.SOLUTION: The invention provides a crystal of a compound I represented by the formula in the figure, which is selected from the group consisting of ethylene glycol (EG) crystal (form SB-1), ethylene glycol (EG) crystal (form SB-2), 1:2 L-proline crystal (form 3), 1:1 L-proline crystal (form 6), and 1:1 L-proline hemihydrate crystal (form H.5-2).SELECTED DRAWING: None

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Inventors:

GOUGOUTAS JACK Z
LOBINGER HILDEGARD
RAMAKRISHNAN SRIVIDYA
PRASHANT P DESHPANDE
BIEN JEFFREY T
LAI CHIAJEN
WANG CHENCHI
LIEBEL PETER
GROSSO JOHN ANTHONY
ALEXANDRA A NIRSCHL
SINGH JANAK
JOHN D DIMARCO

Application Number:

JP2018236514A

Publication Date:

April 18, 2019

Filing Date:

December 18, 2018

Export Citation:

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Assignee:

ASTRAZENECA AB

International Classes:

C07D309/10; A61K31/351; A61P3/04; A61P3/06; A61P3/10; A61P9/10; A61P13/12; A61P25/00; A61P27/12; A61P43/00

Foreign References:

WO2004063209A2	2004-07-29
WO2005121142A1	2005-12-22

Other References:

化学実験操作法　上巻, JPN6010029432, 1963, pages 371 - 399, ISSN: 0004291148

Attorney, Agent or Firm:

Michiko Matsutani
Yasushi Morimoto
Nobuhiko Akiyama

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