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Last Updated: March 29, 2024

Details for Patent: 9,453,039


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Title:Crystal structures of SGLT2 inhibitors and processes for preparing same
Abstract: The present invention relates to physical crystal structures of a compound of the formula I: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.2a, R.sup.3 and R.sup.4 are as defined herein, especially ##STR00002## pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
Inventor(s): Gougoutas; Jack Z. (Princeton, NJ), Lobinger; Hildegard (Princeton, NJ), Ramakrishnan; Srividya (Princeton, NJ), Deshpande; Prashant P. (Princeton, NJ), Bien; Jeffrey T. (Princeton, NJ), Lai; Chiajen (Princeton, NJ), Wang; Chenchi (Princeton, NJ), Riebel; Peter (Princeton, NJ), Grosso; John Anthony (Princeton, NJ), Nirschl; Alexandra A. (Princeton, NJ), Singh; Janak (Princeton, NJ), DiMarco; John D. (Princeton, NJ)
Assignee: AstraZeneca AB (Sodertalje, SE)
Filing Date:Jul 10, 2013
Application Number:13/938,763
Claims:1. A crystalline structure of a compound of formula I ##STR00066## which is (R)-PG (form SD-3).

2. The crystalline structure according to claim 1, in substantially pure form.

3. The crystalline structure (R)-PG (form SD-3) according to claim 1 having the formula 1b ##STR00067##

4. The crystalline structure according to claim 3 characterized by one or more of the following: a) a powder x-ray diffraction pattern comprising 2.theta. values (CuK.alpha. .lamda.=1.5418 .ANG.) of 3.9.+-.0.1, 8.0.+-.0.1, 8.7.+-.0.1, 15.3.+-.0.1, 15.6.+-.0.1, 17.2.+-.0.1, 19.2.+-.0.1, 19.9.+-.0.1 and 20.3.+-.0.1, at room temperature; b) a solid state .sup.13C NMR spectrum having substantially similar peak positions at 15.8, 17.6, 39.0, 60.9, 63.2, 67.4, 69.7, 77.3, 79.2, 79.8, 113.3, 123.6, 129.0, 130.4, 132.0, 135.6, 139.2 and 157.9 ppm, as determined on a 400 MHz spectrometer relative to TMS at zero; c) a differential scanning calorimetry thermogram having an endotherm in the range of about 43.degree. C. to 60.degree. C. or as shown in FIG. 8; or d) thermal gravimetric analysis curve with about 18.7% weight loss from about room temperature up to about 235.degree. C. or as shown in FIG. 6.

5. A pharmaceutical composition comprising an effective amount of a crystal structure of a compound of formula I according to claim 1 and a pharmaceutically acceptable carrier or diluent.

6. The pharmaceutical composition according to claim 5 wherein the crystalline structure is in substantially pure form.

7. A pharmaceutical composition comprising an effective amount of the crystal structure according to claim 1 in combination with one or more therapeutic agents selected from the group consisting of an antidiabetic agent, a anti-hypertensive agent, an anti-atherosclerotic agent and a lipid-lowering agent.

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