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Glucose sensitive insulins and uses thereof

A glucose and insulin technology, applied in the direction of insulin, hormone peptides, sugar derivatives, etc., can solve problems such as difficulties

Pending Publication Date: 2021-07-23
诺和诺德牛津研究中心有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, binding glucose with reasonable affinity and selectivity in water is a very difficult task due to the very subtle structural differences with other carbohydrates

Method used

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  • Glucose sensitive insulins and uses thereof
  • Glucose sensitive insulins and uses thereof
  • Glucose sensitive insulins and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0153] The invention is further described by the following non-limiting examples.

[0154] 1. Insulin derivatives comprising human insulin or a human insulin analogue, a glucose mimetic and a macrocycle M of formula M1:

[0155]

[0156] where R 1 and R 2 independently selected from -OH,

[0157]

[0158] where R 4 , R 5 , R 6 , R 7 , R 8 and R 9 independently selected from hydrogen, halogen, (1-4C)alkyl and (1-4C)alkoxy; and

[0159] where R 3 represents the junction point of the macrocycle of formula M1.

[0160] 2. The insulin derivative according to embodiment 1, wherein said insulin derivative comprises two glucose mimetics and two macrocycles M of formula M1.

[0161] 3. The insulin derivative according to any one of embodiments 1-2, wherein R 1 and R 2 for

[0162]

[0163] 4. The insulin derivative according to any one of embodiments 1-3, wherein R 4 , R 5 , R 6 , R 7 , R 8 and R 9 Each is an ethyl group.

[0164] 5. The insulin derivative...

Embodiment 1

[0182] The B1-macrocyclic B29-glycoside desB30 human insulin 8 of Example 1;

Embodiment 2

[0183] The B1-macrocyclic A1-glycoside desB30 human insulin 12 of Example 2;

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Abstract

The present invention provides glucose sensitive insulin derivatives comprising a macrocycle, a glucose mimetic and human insulin or an analogue thereof, and their pharmaceutical use. Furthermore, the invention relates to pharmaceutical compositions comprising such glucose sensitive insulin derivatives, and to the use of such compounds for the treatment or prevention of medical conditions relating to diabetes.

Description

Background technique [0001] Glucose is the most important component of energy homeostasis in humans, and uncontrolled blood sugar is a hallmark of diabetes. The main purpose of diabetes treatment is to regulate blood sugar levels towards normal values, and insulin is the most effective drug for this purpose. However, using insulin to regulate blood sugar makes it difficult to strike a balance between hyperglycemia and hypoglycemia. Hypoglycemia often occurs even with modern glucose monitors, and various glucose-sensitive insulin delivery systems have been devised in an attempt to ameliorate this situation, either in the form of mechanical systems (pump / sensor) or molecular delivery systems. Therefore, it would be advantageous to confer glucose-regulating bioactivity on diabetes-related peptide and protein drugs, eg insulin's hypoglycemic activity is weak at low blood glucose values. [0002] Glucose-sensitive insulin bioactivity can be achieved by equipping insulin with a gl...

Claims

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Application Information

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IPC IPC(8): A61P5/50A61K38/28C07H15/26C07K14/62A61K47/55
CPCA61K47/55A61P5/50C07K14/62A61K38/00A61K47/549
Inventor T·霍格-詹森A·R·马德森T·克鲁瑟P·索尔伯格A·默里A·P·戴维斯A·M·查普曼
Owner 诺和诺德牛津研究中心有限公司
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