Novel Acylated Insulin Analogues and Uses Thereof
AssigneeNovo Nordisk A/S
InventorsGrith Skytte Olsen, Bo Falck Hansen, Lauge Schaeffer, Ingrid Pettersson, Rita Slaaby, Jakob Brandt
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel insulin analogues and derivatives thereof, such as acylated insulin analogues, and their pharmaceutical use, in particular in the treatment or prevention of medical conditions relating to diabetes, obesity and cardiovascular diseases.
Claims20
An insulin derivative, comprising an insulin analogue comprising B5Y or B5F and a substituent comprising an acyl group, or a pharmaceutically acceptable salt, amide or ester thereof.
An insulin analogue comprising
- i. A14E, B5Y, B26A, B28K, desB29-30;
- ii. A14E, B5Y, B26G, B28K, desB29-30;
- iii. B5Y, B26A, B28K, desB29-30;
- iv. B5Y, B26G, B28K, desB29-30;
- v. B5Y, B28K, desB29-30;
- vi. A14E, B5F, B26G, B28K, desB29-30;
- vii. B5F, B28K, desB29-30;
- viii. B5Y, B26K, desB27-desB30;
- ix. BSY, desB30;
- x. BSY, B26G, desB30;
- xi. BSY, B26A, desB30;
- xii. BSF, B26A, B28K, desB29-30;
- xiii. BSY, B26A, B28K, desB29-30;
- xiv. BSY, B26G, B28K, desB29-30;
- xv. BSF, B26G, B28K, desB29-30;
- xvi. A14E, BSF, B26A, B28K, desB29-30;
- xvii. A14E, BSY, B26A, B28K, desB29-30;
- xviii. A14E, BSY, B26G, B28K, desB29-30;
- xix. A14E, BSY, B28K, desB29-30;
- xx. A14E, BSF, B28K, desB29-30;
- xxi. A14E, BSY, B26K, desB27-desB30;
- xxii. A14E, B5Y, desB30;
- xxiii. A14E, B5Y, B26G, desB30;
- or
- xxiv. A14E, B5Y, B26A, desB30.
- or a pharmaceutically acceptable salt, amide or ester thereof.
A method for determining selectivity of an insulin compound comprising the following steps:
- measuring the maximal AKT phosphorylation induced by said insulin compound relative to human insulin
- measuring the maximal ERK activation induced by said insulin compound relative to human insulin,
- wherein the ERK/AKT ratio is less than 1.
Dependencies are inferred from the claim text.