# US 2014/0154263 A1 · Use of TAK1 Inhibitor to Achieve Glycemic Control in Mammals

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- Number: US 2014/0154263 A1
- Document ID: US20140154263A1
- Status: Published application
- Kind: A1
- Application number: 14/097,967
- Filed: 2013-12-05
- Published: 2014-06-05
- Earliest claimed: 2012-12-05
- Assignees: Connexios Life Sciences Pvt. Ltd.
- Applicants: Connexios Life Sciences Pvt. Ltd.
- Inventors: Anup Mammen Oommen; Mahesh Kumar Verma; Urvashi Bahadur; Swapnika Ramu
- Web page: https://patentgrep.com/patent/US20140154263A1

## CPC

- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/365: Lactones
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C12N 9/1205: {Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention relates to use of inhibitors of TAK-1 for the production of pharmaceutical agents to achieve glycemic control in mammals and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme.

## Claims

### Claim 1

A method of using inhibitors of TAK-1 in preparing a medicament for therapy of diseases which are based on loss of glycemic control in mammals.

### Claim 2 (depends on 1)

The method of use according to claim 1, wherein the medicament is used for the prevention or alleviation of pathological abnormalities of the metabolism of mammals such as hyperglycemia, low glucose tolerance, low insulin sensitivity, glucosuria, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipedemia, metabolic acidosis, obesity, diabetes mellitus and diabetes related secondary complications.

### Claim 3 (depends on 1)

The method of use according to claim 1, characterized in that inhibitors, pseudosubstrates, inhibitors of TAK-1 expression, binding proteins, or antibodies against the enzyme proteins or combination of the designated inhibitors of TAK-1 or TAK-1 like enzyme activity.

### Claim 4

A method for lowering elevated blood glucose levels in mammals comprising administering at least one oral administration of a therapeutically effective amount of at least one inhibitor of TAK-1 or of TAK-1 enzyme activity.

### Claim 5 (depends on 4)

The method according to claim 4, wherein the at least one inhibitor is administered in combination with at least one carrier substance.

### Claim 6 (depends on 4)

The method according to claim 4, wherein the at least one inhibitor is administered in multiple administrations

### Claim 7 (depends on 4)

The method according to claim 4, wherein the mammals demonstrate at least one of clinically appropriate basal, fasting and post-prandial hyperglycemia.

### Claim 8 (depends on 4)

The method according to claim 4, wherein the administration is for the prevention or alleviation of pathological abnormalities of metabolism of mammals such as diabetes, hyperglycemia, low glucose tolerance, glucosuria, metabolic acidosis, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, obesity and diabetic related secondary complications.

### Claim 9 (depends on 4)

The method according to claim 4, wherein the method comprises administering at least one oral administration of a therapeutically effective amount of at least one inhibitor of TAK-1 or of TAK-1 enzyme activity in combination with an adjuvant selected from and not limited to:
(a) dipeptidyl peptidase-IV (DP-IV) inhibitors;
(b) insulin sensitizing agents;
(c) insulin and insulin mimetics;
(d) sulfonylureas and other insulin secretagogues;
(e) alpha.-glucosidase inhibitors; and
(f) GLP-1, GLP-1 analogs, and GLP-1 receptor agonists.

### Claim 10 (depends on 9)

The method according to claim 9, wherein the adjuvant is a biguanide.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the biguanide is metformin.