Insulin receptor partial agonists

• US 10,017,556 B2
• Filed: 11/19/2015
• Issued: 07/10/2018
• Est. Priority Date: 11/21/2014
• 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, Zhu, Yuping, Kekec, Ahmet, Madsen-Duggan, Christina B., Shi, Zhi-Cai, Wu, Zhicai, Mu, Yingjun
• Primary Examiner(s): Audet, Maury A
• Application Number:
  US14/945,461
• Publication Number:
  US 20170107268A1
• Time in Patent Office: 964 Days
• Field of Search: None
• 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: A61K 47/55 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• 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. A compound selected from the group consisting of

2. A composition comprising one or more compounds of claim 1 and a pharmaceutically acceptable carrier.

3. A method for treating diabetes comprising administering to an individual with diabetes a therapeutically effective amount of the composition of claim 2.

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

5. A method for treating diabetes comprising administering to an individual with diabetes a therapeutically effective amount of the compound of claim 1.

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

7. A compound having the formula

8. A composition comprising the compound of claim 7 and a pharmaceutically acceptable carrier.

9. A method for treating diabetes comprising administering to an individual with diabetes a therapeutically effective amount of the composition of claim 8.

10. The method of claim 9, wherein the diabetes is Type 1 diabetes, Type 2 diabetes, or gestational diabetes.