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Last Updated: October 23, 2020

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Claims for Patent: 10,406,172

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Summary for Patent: 10,406,172
Title:Pharmaceutical composition, methods for treating and uses thereof
Abstract: The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor, a DPPIV inhibitor and a third antidiabetic agent which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
Inventor(s): Eickelmann; Peter (Mittelbiberach, DE), Mark; Michael (Biberach an der Riss, DE), Seman; Leo John (Cheshire, CT), Thomas; Leo (Biberach an der Riss, DE), Broedl; Uli (Ingelheim am Rhein, DE), Grempler; Rolf (Birkenhard Warthausen, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:13/912,599
Patent Claims: 1. A pharmaceutical composition comprising in a single dosage form: (a) a sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor, wherein said SGLT2 inhibitor is 1-chloro-4-(.beta.-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy- )-benzyl]-benzene, wherein said pharmaceutical composition comprises 5, 10, 12.5 or 25 mg of said SGLT2 inhibitor, and (b) a dipeptidyl peptidase IV (DPPIV) inhibitor, wherein said DPPIV inhibitor is linagliptin or a pharmaceutically acceptable salt thereof, wherein said pharmaceutical composition comprises 2.5 or 5 mg of said DPPIV inhibitor, and (c) a third antidiabetic agent, wherein said third antidiabetic agent is metformin hydrochloride, wherein said pharmaceutical composition comprises 1000 mg of metformin hydrochloride, wherein said single dosage form is a tablet.

2. A pharmaceutical composition according to claim 1, said pharmaceutical composition comprising: (a) 10 mg of said SGLT-2 inhibitor, and (b) 5 mg of said DPPIV inhibitor, and (c) 1000 mg of metformin hydrochloride.

3. A pharmaceutical composition according to claim 1, said pharmaceutical composition comprising: (a) 25 mg of said SGLT-2 inhibitor, and (b) 5 mg of said DPPIV inhibitor, and (c) 1000 mg of metformin hydrochloride.

4. A pharmaceutical composition according to claim 1, said pharmaceutical composition comprising: (a) 5 mg of said SGLT-2 inhibitor, and (b) 2.5 mg of said DPPIV inhibitor, and (c) 1000 mg of metformin hydrochloride.

5. A pharmaceutical composition according to claim 1, said pharmaceutical composition comprising: (a) 12.5 mg of said SGLT-2 inhibitor, and (b) 2.5 mg of said DPPIV inhibitor, and (c) 1000 mg of metformin hydrochloride.

6. Method for improving glycemic control in a patient with type 2 diabetes mellitus comprising administering to the patient a pharmaceutical composition according to claim 2.

7. The method according to claim 6, wherein said pharmaceutical composition is administered once daily to the patient.

8. Method for improving glycemic control in a patient with type 2 diabetes mellitus comprising administering to the patient a pharmaceutical composition according to claim 3.

9. The method according to claim 8, wherein said pharmaceutical composition is administered once daily to the patient.

10. Method for improving glycemic control in a patient with type 2 diabetes mellitus comprising administering to the patient a pharmaceutical composition according to claim 4.

11. The method according to claim 10, wherein said pharmaceutical composition is administered twice daily to the patient.

12. Method for improving glycemic control in a patient with type 2 diabetes mellitus comprising administering to the patient a pharmaceutical composition according to claim 5.

13. The method according to claim 12, wherein said pharmaceutical composition is administered twice daily to the patient.

14. Method for slowing the progression of, delaying or treating a metabolic disorder selected from the group consisting of type 2 diabetes mellitus, impaired glucose tolerance, impaired fasting blood glucose, hyperglycemia, postprandial hyperglycemia, overweight, obesity, metabolic syndrome, gestational diabetes, new onset diabetes after transplantation (NODAT) and complications associated therewith, and post-transplant metabolic syndrome (PTMS) and complications associated therewith in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

15. Method according to claim 14 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

16. Method for improving glycemic control and/or for reducing of fasting plasma glucose, of postprandial plasma glucose and/or of glycosylated hemoglobin HbA1c in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

17. Method according to claim 16 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

18. Method for slowing, delaying or reversing progression from impaired glucose tolerance, impaired fasting blood glucose, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

19. Method according to claim 18 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

20. Method for preventing, slowing the progression of, delaying or treating of a condition or disorder selected from the group consisting of complications of diabetes mellitus such as cataracts and micro- and macrovascular diseases, such as nephropathy, retinopathy, neuropathy, tissue ischaemia, diabetic foot, arteriosclerosis, myocardial infarction, accute coronary syndrome, unstable angina pectoris, stable angina pectoris, stroke, peripheral arterial occlusive disease, cardiomyopathy, heart failure, heart rhythm disorders and vascular restenosis, in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

21. Method according to claim 20 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

22. Method for reducing body weight and/or body fat or preventing an increase in body weight and/or body fat or facilitating a reduction in body weight and/or body fat in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

23. Method according to claim 22 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

24. Method for preventing, slowing, delaying or treating the degeneration of pancreatic beta cells and/or the decline of the functionality of pancreatic beta cells and/or for improving and/or restoring the functionality of pancreatic beta cells and/or restoring the functionality of pancreatic insulin secretion in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

25. Method according to claim 24 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

26. Method for preventing, slowing, delaying or treating diseases or conditions attributed to an abnormal accumulation of ectopic fat in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

27. Method according to claim 26 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

28. Method for treating and preventing hyperuricemia and hyperuricemia associated conditions, kidney stones and hyponatremia in a patient in need thereof characterized in that an SGLT2 inhibitor, a DPP IV inhibitor and a third antidiabetic agent according to claim 1 are administered to the patient.

29. Method according to claim 28 wherein the patient: (1) is an individual diagnosed of one or more of the conditions selected from the group consisting of overweight, obesity, visceral obesity and abdominal obesity; or (2) is an individual who shows one, two or more of the following conditions: (a) a fasting blood glucose or serum glucose concentration greater than 110 mg/dL, in particular greater than 125 mg/dL; (b) a postprandial plasma glucose equal to or greater than 140 mg/dL; (c) an HbA1c value equal to or greater than 6.5%, in particular equal to or greater than 7.0%; or (3) is an individual wherein one, two, three or more of the following conditions are present: (a) obesity, visceral obesity and/or abdominal obesity, (b) triglyceride blood level .gtoreq.150 mg/dL, (c) HDL-cholesterol blood level <40 mg/dL in female patients and <50 mg/dL in male patients, (d) a systolic blood pressure .gtoreq.130 mm Hg and a diastolic blood pressure .gtoreq.85 mm Hg, (e) a fasting blood glucose level .gtoreq.100 mg/dL; or (4) has insufficient glycemic control despite diet and exercise or despite monotherapy with either the SGLT2 inhibitor, the DPPIV inhibitor or the third antidiabetic agent, or despite combination therapy with two agents selected from the group of the SGLT2 inhibitor, the DPPIV inhibitor and the third antidiabetic agent.

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