IP Library › Granted Patent US 12,473,339
Granted Patent B2
US 12,473,339 · App. 18/408,052 · Granted Nov 18, 2025

Acylated glucagon analogues

Inventors: Ditte Riber (Brønshøj, DK); Jakob Lind Tolborg (Herlev, DK); Dieter Wolfgang Hamprecht (Pozzolengo, IT); Wolfgang Rist (Ingelheim am Rhein, DE)
Assignee: Zealand Pharma A/S
C07K14/605A61K31/137A61K31/155A61K31/198A61K31/485A61K31/7048A61K38/26A61K38/28A61K45/06
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Quick Facts
Patent No.
US 12,473,339
App. No.
18/408,052
Granted
Nov 18, 2025
Kind
B2
Abstract

The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

Claims (20)

1 . A method of preventing weight gain or promoting weight loss in an individual in need thereof, said method comprising administering a therapeutically effective amount of a compound which is H—H-Aib-QGTFTSDYSKYLDERAAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 60), or a pharmaceutically acceptable salt thereof, to the individual.

2 . The method of claim 1 , wherein the individual has one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

3 . A method of treating a condition caused or characterized by excess body weight in an individual in need thereof, said method comprising administering to the individual a therapeutically effective amount of a compound which is H—H-Aib-QGTFTSDYSKYLDERAAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 60), or a pharmaceutically acceptable salt thereof.

4 . The method of claim 3 , wherein the condition is one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

5 . A method of preventing weight gain or promoting weight loss in an individual in need thereof, said method comprising administering a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERAAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 61), or a pharmaceutically acceptable salt thereof, to the individual.

6 . The method of claim 5 , wherein the individual has one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

7 . A method of treating a condition caused or characterized by excess body weight in an individual in need thereof, said method comprising administering to the individual a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERAAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 61), or a pharmaceutically acceptable salt thereof.

8 . The method of claim 7 , wherein the condition is one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

9 . A method of preventing weight gain or promoting weight loss in an individual in need thereof, said method comprising administering a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERRAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 62), or a pharmaceutically acceptable salt thereof, to the individual.

10 . The method of claim 9 , wherein the individual has one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

11 . A method of treating a condition caused or characterized by excess body weight in an individual in need thereof, said method comprising administering to the individual a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERRAKDFI-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-WLESA-NH 2 (SEQ ID NO: 62), or a pharmaceutically acceptable salt thereof.

12 . The method of claim 11 , wherein the condition is one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

13 . A method of preventing weight gain or promoting weight loss in an individual in need thereof, said method comprising administering a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERAAKDFIEWLE-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-A-NH 2 (SEQ ID NO: 63), or a pharmaceutically acceptable salt thereof, to the individual.

14 . The method of claim 13 , wherein the individual has one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

15 . A method of treating a condition caused or characterized by excess body weight in an individual in need thereof, said method comprising administering to the individual a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERAAKDFIEWLE-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-A-NH 2 (SEQ ID NO: 63), or a pharmaceutically acceptable salt thereof.

16 . The method of claim 15 , wherein the condition is one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

17 . A method of preventing weight gain or promoting weight loss in an individual in need thereof, said method comprising administering a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERRAKDFIEWLE-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-A-NH 2 (SEQ ID NO: 64), or a pharmaceutically acceptable salt thereof, to the individual.

18 . The method of claim 17 , wherein the individual has one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

19 . A method of treating a condition caused or characterized by excess body weight in an individual in need thereof, said method comprising administering to the individual a therapeutically effective amount of a compound which is H—H-Ac4c-QGTFTSDYSKYLDERRAKDFIEWLE-K([17-carboxy-heptadecanoyl]-isoGlu-GSGSGG)-A-NH 2 (SEQ ID NO: 64), or a pharmaceutically acceptable salt thereof.

20 . The method of claim 19 , wherein the condition is one or more of obesity, morbid obesity, morbid obesity prior to surgery, obesity linked inflammation, obesity linked gallbladder disease, obesity induced sleep apnea, diabetes, metabolic syndrome, hypertension, atherogenic dyslipidemia, atherosclerosis, arteriosclerosis, coronary heart disease, peripheral artery disease, or microvascular disease.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: RIBER, DITTE; TOLBORG, JAKOB LIND
To: ZEALAND PHARMA A/S
Reel/Frame 068766/0862 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: RIST, WOLFGANG
To: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG.
Reel/Frame 068766/0931 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: HAMPRECHT, DIETER WOLFGANG
To: BI RESEARCH ITALIA S.A.S. DI BI IT S.R.L.
Reel/Frame 068766/0971 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: BI RESEARCH ITALIA S.A.S. DI BI IT S.R.L.
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 068767/0073 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG.
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 068767/0125 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2024
From: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
To: ZEALAND PHARMA A/S
Reel/Frame 068767/0232 →
Continuity (6)
Continuation 17369061 · Jul 7, 2021
Continuation 16569381 · Sep 12, 2019
Continuation 15852458 · Dec 22, 2017
Continuation 14517497 · Oct 17, 2014
Provisional Application 61892256 · Oct 17, 2013
Related Publication 20240141010A1 · May 2, 2024
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