# US 7,741,491 B2 · Diphenylamine-substituted salicylthiazole derivatives and related compounds as phosphotyrosine phosphatase 1B (PTB1B) inhibitors for using as blood-sugar decreasing active ingredients for treating diabetes

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- Number: US 7,741,491 B2
- Document ID: US7741491B2
- Status: Granted
- Kind: B2
- Application number: 11/609,463
- Filed: 2006-12-12
- Published: 2007-08-16
- Granted: 2010-06-22
- Earliest claimed: 2004-07-17
- Assignees: Sanofi-Aventis Deutschland GmbH
- Inventors: Stefan Petry; Karl-Heinz Baringhaus; Norbert Tennangels; Guenter Mueller; Reinhard Kirsch
- Web page: https://patentgrep.com/patent/US7741491B2

## CPC

- C07D 277/42: Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 277/46: by carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood glucose levels.

## Claims

### Claim 1

A compound of formula I
, wherein:
R1, and R2 are each H;
R3, R4, and R5 are, independently of one another, selected from H, F, NH—SO2—CH3, COOH, and CO—NH(C1-C6)-alkyl;
R6 is H;
A is a bond;
B is NH; and
D is phenyl;
or a physiologically tolerated salt thereof.

### Claim 2 (depends on 1)

A medicament comprising a compound of claim 1.

### Claim 3 (depends on 2)

The medicament of claim 2 which comprises at least one other active ingredient.

### Claim 4 (depends on 3)

A medicament as claimed in claim 3, wherein the other active ingredient comprises one or more of the following:
antidiabetics, hypoglycemic active ingredients, HMGCoA reductase inhibitors, cholesterol absorption inhibitors, PPAR gamma agonists, PPAR alpha agonists, PPAR alpha/gamma agonists, fibrates, MTP inhibitors, bile acid absorption inhibitors, CETP inhibitors, polymeric bile acid adsorbents, LDL receptor inducers, ACAT inhibitors, antioxidants, lipoprotein lipase inhibitors, ATP-citrate lyase inhibitors, squalene synthetase inhibitors, lipoprotein(a) antagonists, lipase inhibitors, insulins, sulfonylureas, biguanides, meglitinides, thiazolidinediones, α-glucosidase inhibitors, active ingredients which act on the ATP-dependent potassium channel of the beta cells, CART agonists, NPY agonists, MC4 agonists, orexin agonists, H3 agonists, TNF agonists, CRF agonists, CRF BP antagonists, urocortin agonists, β3 agonists, MSH (melanocyte-stimulating hormone) agonists, CCK agonists, serotonin reuptake inhibitors, mixed serotoninergic and noradrenergic compounds, 5HT agonists, bombesin agonists, galanin antagonists, growth hormones, growth hormone-releasing compounds, TRH agonists, uncoupling protein 2 or 3 modulators, leptin agonists, DA agonists (bromocriptine, Doprexin), lipase/amylase inhibitors, PPAR modulators, RXR modulators, TR-β agonists and amphetamines.

### Claim 5 (depends on 2)

A method for reducing blood glucose which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 6 (depends on 2)

A method for the treatment of type II diabetes which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 7 (depends on 2)

A method for the treatment of disturbances of glucose metabolism which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 8 (depends on 2)

A method for weight reduction in mammals which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 9 (depends on 2)

A method for the treatment of obesity in mammals which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 10 (depends on 2)

A method for the treatment of insulin resistance which comprises administering to a patient in need thereof an effective amount of a medicament of claim 2.

### Claim 11 (depends on 2)

A process for producing a medicament as claimed in claim 2, which comprises mixing the active ingredient with a pharmaceutically suitable carrier and converting this mixture into a form suitable for administration.