Vanilloid receptor modulators

• US 20060142333A1
• Filed: 02/13/2003
• Published: 06/29/2006
• Est. Priority Date: 02/15/2002
• Status: Active Grant

• Current Assignee: Darren Jason Mitchell, Gregor James MacDonald, Harshad Kantilal Rami, Mervyn Thompson, Susan Maric Westaway
• Original Assignee: Darren Jason Mitchell, Gregor James MacDonald, Harshad Kantilal Rami, Mervyn Thompson, Susan Maric Westaway
• Inventors: MacDonald, Gregor James, Westaway, Susan Maric, Thompson, Mervyn, Rami, Harshad Kantilal, Mitchell, Darren Jason
• Granted Patent: US 7,538,121 B2
• Time in Patent Office: Days
• US Class Current: 514/310
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 1/14 Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: C07D 215/38 Nitrogen atoms nitro radicals C07D215/18
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/14 containing three or more hetero rings

Abstract

Certain compounds of formula (I),
or a pharmaceutically acceptable salt or solvate thereof, wherein R¹, R², R³, P, X, Y, q, r ans s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.

Claims

1. A compound of formula (I),

2. A compound of formula (i), as claimed in claim 1, of formula (IA),

3. A compound of formula (I), as claimed in claim 1, of formula (IB),

4. A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, as claimed in claim 1, substantially as hereinbefore described with reference to any one of the Examples.

6. A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, as claimed in claim 1, for use as an active therapeutic substance.

7. A method for the treatment or prophylaxis of disorders in which antagonism of the Vanilloid (VR1) receptor is beneficial in mammals including humans, which method comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of formula (i) or a pharmaceutically acceptable salt or solvate thereof, as claimed in claim 1.

9. A pharmaceutical composition, which comprises a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, as claimed in claim 1, and a pharmaceutically acceptable carrier or excipient therefor.

5. A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, which process comprises:

(a) reacting a compound of formula (II);

wherein, R¹, R², q, r, X and Y are as defined in relation to formula (I), with a compound of formula (III);

wherein, P, R³ and s are as defined in relation to formula (I) and thereafter, as necessary, carrying out one or more of the following reactions;

(i) converting one compound of formula (I) into another compound of formula (I);

(ii) removing any protecting group;

(iii) preparing a salt or a solvate of the compound so formed.

8. (canceled)