Insulin receptor partial agonists

• US 10,689,430 B2
• Filed: 05/23/2017
• Issued: 06/23/2020
• Est. Priority Date: 05/25/2016
• Status: Active Grant

• Current Assignee: Merck Sharp & Dohme LLC (Merck & Co., Inc.)
• Original Assignee: Merck Sharp & Dohme Corporation (Merck & Co., Inc.)
• Inventors: Lin, Songnian, Yan, Lin, Huo, Pei, Pissarnitski, Dmitri, Feng, Danqing, Nargund, Ravi, Madsen-Duggan, Christina, Zhu, Yuping, Kekec, Ahmet, Wu, Zhicai
• Primary Examiner(s): Cordero Garcia, Marcela M
• Application Number:
  US16/301,010
• Publication Number:
  US 20190177393A1
• Time in Patent Office: 1,127 Days
• CPC Class Codes: A61K 38/00 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 Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07K 14/62 Insulins
• CPC Class Codes: C07K 2319/00 Fusion polypeptide

Abstract

Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

Claims

1. An insulin dimer selected from the group consisting of:

2. A composition comprising the insulin receptor partial agonist of claim 1 and a GLP-1 receptor agonist.

3. A method for treating diabetes comprising administering to an individual with diabetes a therapeutically effective amount of a composition comprising the insulin receptor partial agonist of claim 1.

4. The method of claim 3, wherein the diabetes is Type 1 diabetes, Type 2 diabetes, or gestational diabetes.

5. A composition for the treatment of diabetes comprising the insulin receptor partial agonist of claim 1.

6. The composition of claim 5, wherein the diabetes is Type 1 diabetes, Type 2 diabetes, or gestational diabetes.