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1. WO1999026909 - ALPHA-HYDROXY, -AMINO AND -FLUORO DERIVATIVES OF BETA-SULPHONYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASES INHIBITORS

Publication Number WO/1999/026909
Publication Date 03.06.1999
International Application No. PCT/IB1998/002154
International Filing Date 18.11.1998
Chapter 2 Demand Filed 18.06.1999
IPC
C07C 317/46 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
44having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
46the carbon skeleton being further substituted by singly-bound oxygen atoms
C07C 317/50 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
44having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
48the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
50at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
CPC
A61P 1/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 13/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
10of the bladder
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
Applicants
  • PHARMACIA & UPJOHN COMPANY [US]/[US] (AllExceptUS)
  • WARPEHOSKI, Martha, A. [US]/[US] (UsOnly)
  • MITCHELL, Mark, Allen [US]/[US] (UsOnly)
  • HARPER, Donald, E. [US]/[US] (UsOnly)
  • MAGGIORA, Linda, Louise [US]/[US] (UsOnly)
Inventors
  • WARPEHOSKI, Martha, A.
  • MITCHELL, Mark, Allen
  • HARPER, Donald, E.
  • MAGGIORA, Linda, Louise
Agents
  • BEAUMONT, William, E.
Priority Data
60/072,65521.11.1997US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) ALPHA-HYDROXY, -AMINO AND -FLUORO DERIVATIVES OF BETA-SULPHONYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASES INHIBITORS
(FR) DERIVES $g(a)-HYDROXY, AMINO ET HALO D'ACIDES HYDROXAMIQUES $g(b)-SULFONYLE UTILISES COMME INHIBITEURS DE METALLOPROTEINASES MATRICIELLES
Abstract
(EN) The present invention provides a compound of formula (I), or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, -(CH2)h-C3-8 cycloalkyl, substituted and unsubstituted -(CH2)h-aryl, substituted and unsubstituted-(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted -(CH2)h-C3-8 cycloalkenyl, substituted and unsubstituted -(CH2)h-aryl, substituted and unsubstituted -(CH2)h-heterocyclic ring, substituted and unsubstituted -(CH2)i-X-R4 (X is -O-, -S(=O)j-, -NR7-, -S(=O)2NR8-, or -C(=O)-), and -(CH2)iCHR5R6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.
(FR) La présente invention concerne un composé de formule (I), ou des sels pharmaceutiquement acceptables de ce composé, formule dans laquelle R1 représente C4-12 alkyle, C4-12 alkényle, C4-12 alkynyle, -(CH2)h-C3-8 cycloalkyle, (CH2)h- aryle substitué ou non substitué, -(CH2)h-het substitué ou non substitué, R2 représente C1-12 alkyle substitué ou non substitué, C2-12 alkényle substitué ou non substitué, C2-12 alkynyle substitué ou non substitué, -(CH2)h-C3-8 cycloalkyle substitué ou non substitué, -(CH2)h-C3-8 cycloalkyle substitué ou non substitué, -(CH2)h aryle substitué ou non substitué, -(CH2)h- noyau hétérocyclique substitué ou non substitué, -(CH2)i-X-R4 substitué ou non substitué (X représentant -O-, -S(=O)j-, -NR7-, -S(=O)2NR8-, ou -C(=O)-), et (CH2)jCHR5R6. Ces composés sont des inhibiteurs des métalloprotéinases matricielles impliquées dans la dégradation tissulaire.
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