GIP/GLP1 co-agonist compounds

Patent metadata

Field	Value
Publication number	US-11084861-B2
Application number	US-201916518468-A
Country	US
Kind code	B2
Filing date	Jul 22, 2019
Priority date	Jul 23, 2018
Publication date	Aug 10, 2021
Grant date	Aug 10, 2021

Abstract

The present invention relates to compounds having activity at both the human glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. The present invention also relates to compounds having an extended duration of action at each of these receptors. Furthermore, the present invention relates to compounds that may be administered orally. Compounds may be useful in the treatment of type 2 diabetes mellitus (“T2DM”). Also, the compounds may be useful in the treatment of obesity.

First claim

We claim:

1. A compound wherein the compound is any one of the amino acid sequences selected from the group consisting of SEQ ID NO:10, SEQ ID NO:11, SEQ ID NO:12, SEQ ID NO:13, and SEQ ID NO:14, or a pharmaceutically acceptable salt thereof.

2. A compound as claimed by claim 1 wherein the compound is SEQ ID NO:13, or a pharmaceutically acceptable salt thereof.

3. A compound as claimed by claim 1 wherein the compound is SEQ ID NO:10, or a pharmaceutically acceptable salt thereof.

4. A compound as claimed by claim 1 wherein the compound is SEQ ID NO:11, or a pharmaceutically acceptable salt thereof.

5. A compound as claimed by claim 1 wherein the compound is SEQ ID NO:12, or a pharmaceutically acceptable salt thereof.

6. A compound as claimed by claim 1 wherein the compound is SEQ ID NO:14, or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising any one of the compounds as claimed by claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, diluent, or excipient.

8. A method of treating type 2 diabetes mellitus or obesity comprising; administering an effective amount of any one of the compounds as claimed by claim 1 , or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

9. A method of treating type 2 diabetes or obesity comprising administering an effective amount of a compound of the amino acid sequence SEQ ID NO:13, or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

10. A method of providing therapeutic weight loss, comprising administering an effective amount of any one of the compounds as claimed by claim 1 , or a pharmaceutically acceptable salt thereof, to a subject in need thereof.

Assignees

• Lilly Co Eli

Inventors

• Abraham Milata Mary
• Alsina-Fernandez Jorge
• Brown Robert Andrew
• Cabrera Over
• Coskun Tamer
• Cummins Robert Chadwick
• Elsayed Mohamed Elsayed Hamed
• Qu Hongchang
• Wallis James Lincoln
• Datta-Mannan Amita
• Lai Xianyin

Classifications

• A61K38/00

  Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title