Claims for Patent: 10,392,357

Summary for Patent: 10,392,357

Title:	Glucagon-like peptide 1 modulator and uses thereof
Abstract:	Disclosed herein are novel glucagon-like peptide-1 (GLP-1) modulators and their uses in manufacturing medicaments for the treatment and/or prophylaxis of diseases and/or disorders associated with hyperglycemia.
Inventor(s):	Chein; Rong-Jie (Taipei, TW), King; Klim (Taipei, TW), Lin; Nai-Pin (Taipei, TW), Cheng; Yu-Hong (Taipei, TW)
Assignee:	Acaemia Sinica (Taipei, TW)
Application Number:	15/576,307
Patent Claims:	1. A compound of formula (I), ##STR00041## wherein, X is O or S; R.sub.1 is ##STR00042## R.sub.2 is H or a nitrogen protecting group; R.sub.3 and R.sub.4 are independently H, halogen, optionally substituted alkyl, or alkenyl; or R.sub.3 and R.sub.4 are taken together to form an optionally substituted 6-membered carbocycle or heterocycle; R' is H or optionally substituted alkyl; and n and m are independently an integral between 1 to 10, provided that when X is O, then R.sub.3 and R.sub.4 are not H; when X is S, then m is not for 4. 2. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00043## ##STR00044## ##STR00045## 3. The compound of claim 1, wherein the compound is ##STR00046## 4. A method for treating diseases and/or disorders associated with hyperglycemia in a subject comprising administering to the subject a therapeutically effective amount of the compound of claim 1, so as to reduce the blood sugar level of the subject; wherein the diseases and/or disorders associated with hyperglycemia is diabetes, obesity, impaired glucose tolerance, impaired fasting glycemia (IFG) hyperinsulinemia, hyperlipidemia, hyper-cholesterolemia, hypertriglyceridemia, lipid metabolism disorder, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia, gout or diabetic complication. 5. The method of claim 4, wherein the compound is ##STR00047## 6. The method of claim 4, further comprising administering to the subject a blood sugar reducing agent before, together with, or after the administration of the compound of claim 1. 7. The method of claim 6, wherein the blood sugar reducing agent is selected from the group consisting of, alpha-glucosidase inhibitor, biguanide, dopamine agonist, dipeptidyl peptidase-4 (DPP-4) inhibitor, glucagon-like peptide-1 (GLP-1), meglitinide, sodium glucose transporter (SGLT) 2 inhibitor, sulfonylurea, and thiazolidinedione. 8. The method of claim 7, wherein the alpha-glucosidase inhibitor is acarbose or miglitol. 9. The method of claim 7, wherein the biguanide is metformin. 10. The method of claim 7, wherein the dopamine agonist is bromocriptine. 11. The method of claim 7, wherein the DPP-4 inhibitor is alogliptin, linagliptin, saxagliptin, sitagliptin, or simvastatin. 12. The method of claim 7, wherein the GLP-1 is lixisenatide, albiglutide, dulaglutide, exenatide, or liraglutide. 13. The method of claim 7, wherein the SGLT 2 inhibitor is dapagliflozin, canagliflozin, or empagliflozin. 14. The method of claim 7, wherein the sulfonylurea is glimepiride, gliclazide, glipizide, glyburide, chlorpropamide, tolazamide, or tolbutamide. 15. The method of claim 7, wherein the thiazolidinedione is pioglitazone or rosiglitazone. 16. The method of claim 4, wherein the diabetic complication is retinopathy, neuropathy, nephropathy, ulcer, or macroangiopathy.

Details for Patent 10,392,357

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Glaxosmithkline Llc	TANZEUM	albiglutide	For Injection	125431	04/15/2014		2035-06-30
Eli Lilly And Company	TRULICITY	dulaglutide	Injection	125469	09/18/2014		2035-06-30
Eli Lilly And Company	TRULICITY	dulaglutide	Injection	125469	09/04/2020		2035-06-30
Sanofi-aventis U.s. Llc	ADLYXIN	lixisenatide	Injection	208471	07/27/2016		2035-06-30