IP Library Granted Patent US 7,906,523
Granted Patent B2
US 7,906,523 · App. 11/929,737 · Granted Mar 15, 2011

Dipeptidyl peptidase inhibitors

Assignee: Takeda Pharmaceutical Company Limited
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Quick Facts
Patent No.
US 7,906,523
App. No.
11/929,737
Granted
Mar 15, 2011
Kind
B2
Abstract

Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR 4 ; Q 1 and Q 2 are each independently selected from the group consisting of CO, SO, SO 2 , and C═NR 9 ; and each L, X, R 1 , R 2 , and R 3 are as defined herein.

Claims (32)

1. A compound having the formula

wherein the compound is in crystalline form.

2. A compound according to claim 1 , wherein the compound is in the same crystalline form as is formed when the compound is crystallized from methanol.

3. A method comprising:

crystallizing a compound having the formula

wherein the crystallization is performed in methanol.

4. A pharmaceutical composition comprising:

a compound having the formula

wherein the compound is in crystalline form; and

one or more pharmaceutical carriers,

wherein the pharmaceutical composition is in the form of a pill, capsule, tablet, wafer, powder or granule.

5. A pharmaceutical composition according to claim 4 , wherein the compound is in the same crystalline form as is formed when the compound is crystallized from methanol.

6. A pharmaceutical composition according to claim 4 , wherein the pharmaceutical composition is a pill or capsule adapted for oral administration.

7. A pharmaceutical composition according to claim 4 , wherein the pharmaceutical composition is in an oral dosage form selected from the group consisting of pills, tablets, capsules, wafers, powders, and granules.

8. A pharmaceutical composition according to claim 4 , wherein the pharmaceutical composition is adapted for topical or transdermal administration.

9. A pharmaceutical composition according to claim 4 , wherein the pharmaceutical composition is in a pulmonary dosage form.

10. A kit comprising:

a pharmaceutical composition comprising

a compound having the formula

wherein the compound is in crystalline form, and

one or more pharmaceutical carriers; and

instructions which comprise one or more forms of information selected from the group consisting of indicating a disease state for which the pharmaceutical composition is to be administered selected from the group consisting of diabetes, rheumatoid arthritis and breast cancer, storage information for the pharmaceutical composition, dosing information and instructions regarding how to administer the composition.

11. A kit according to claim 10 , wherein the kit comprises the pharmaceutical composition in a multiple dose form.

12. An article of manufacture comprising:

a pharmaceutical composition comprising

a compound having the formula

wherein the compound is in crystalline form, and

one or more pharmaceutical carriers; and

packaging materials.

13. An article of manufacture according to claim 12 , wherein the packaging material comprises a container for housing the pharmaceutical composition.

14. An article of manufacture according to claim 12 , wherein the container comprises a label indicating one or more members of the group consisting of a disease state for which the composition is to be administered selected from the group consisting of Type I diabetes, Type II diabetes, rheumatoid arthritis and breast cancer, storage information, dosing information and/or instructions regarding how to administer the composition.

15. An article of manufacture according to claim 12 , wherein the pharmaceutical composition is in a multiple dose form.

Continuity (4)
Continuation 11080992 · Mar 15, 2005
Provisional Application 60553571 · Mar 15, 2004
Provisional Application 60629524 · Nov 18, 2004
Related Publication 20080188501A1 · Aug 7, 2008