# US 7,465,803 B2 · Nitroderivatives as drugs for diseases having an inflammatory basis

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- Number: US 7,465,803 B2
- Document ID: US7465803B2
- Status: Granted
- Kind: B2
- Application number: 10/398,289
- Filed: 2001-10-09
- Published: 2004-02-05
- Granted: 2008-12-16
- Earliest claimed: 2000-10-12
- Assignees: Nicox S.A.
- Inventors: Piero Del Soldato; Francesca Benedini; Patrizia Antognazza
- Web page: https://patentgrep.com/patent/US7465803B2

## CPC

- C07D 213/30: Oxygen atoms
- A61K 31/21: Esters, e.g. nitroglycerine, selenocyanates
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- C07C 203/04: having nitrate groups bound to acyclic carbon atoms
- C07C 233/25: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
- C07C 317/46: the carbon skeleton being further substituted by singly-bound oxygen atoms
- C07C 323/60: with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-X1-L-(W)p—NO2 wherein A contains the radical of a drug, X1 and W are bivalent radicals, p is an integer equal to 1 or 0, and L is a covalent bond, CO, oxygen, sulphur, or NR1C where R1C is H or a C1-C5 linear or branched alkyl.

## Claims

### Claim 1

A compound having the following general formula (I):
A-X1-L-(W)p—NO2 (I)
wherein:
p is an integer equal to 1 or 0;
A=R-T1-, wherein
R has the following formula:
T1=(CO)t or (X)t′, wherein X=O, S or NR1C, wherein R1C is H or a linear or branched alkyl, having from 1 to 5 carbon atoms, t and t′ are integers and equal to zero or 1, with the proviso that t=1 when t′=0; t=0 when t′=1;
X1=-TB-Y-TB1- wherein
TB and TB1 are equal or different;
TB=(CO) when t=0, TB-X when t′=0, X being as above;
TB1=(CO)tx, or (X)txx, wherein tx and txx have the value of 0 or 1; with the proviso that tx=1 when txx=0; and tx=0 when txx=1; X is as above;
Y is selected from the following:
wherein n3 is an integer from 0 to 3 and n3′ is an integer from 1 to 3;
wherein n3 and n3′ have the above meaning, or
wherein
R4 is hydroxy, hydrogen, or R5O— alkoxy wherein R5 is a C1-C10 linear, branched or cyclic alkyl group; and
R2 is a C2-C10 linear or branched alkenylene group which can contain one or more double bonds,
L=covalent bond, CO or X, X being as defined above;
W=YTO wherein YT has the same meanings of Y as defined above, and YT is equal to or different from Y.

### Claim 2 (depends on 1)

The compound of formula (I) according to claim 1, wherein Y is:
wherein n3 is an integer from 0 to 3 and n3′ is an integer from 1 to 3.

### Claim 3 (depends on 1)

A pharmaceutical formulation containing as active ingredient a compound of formula (I) according to claim 1 and a pharmaceutically acceptable excipient.