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1. WO2000039115 - PROTEASE INHIBITORS

Publication Number WO/2000/039115
Publication Date 06.07.2000
International Application No. PCT/US1999/030602
International Filing Date 21.12.1999
Chapter 2 Demand Filed 15.06.2000
IPC
C07D 225/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
225Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
02not condensed with other rings
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
04for non-specific disorders of the connective tissue
A61P 19/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
C07D 225/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
225Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
02not condensed with other rings
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • SMITHKLINE BEECHAM CORPORATION [US/US]; One Franklin Plaza Philadelphia, PA 19103, US (AllExceptUS)
  • MARQUIS, Robert, Wells, Jr. [US/US]; US (UsOnly)
  • VEBER, Daniel, Frank [US/US]; US (UsOnly)
Inventors
  • MARQUIS, Robert, Wells, Jr.; US
  • VEBER, Daniel, Frank; US
Agents
  • STERCHO, Yuriy, P. ; SmithKline Beecham Corporation Corporate Intellectual Property, UW2220 709 Swedeland Road P.O. Box 1539 King of Prussia, PA 19406-0939, US
Priority Data
60/114,14323.12.1998US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROTEASE INHIBITORS
(FR) INHIBITEURS DE PROTEASES
Abstract
(EN)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods of treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis, gingival disease including gingivitis and periodontitis; arthritis, more specifically osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
(FR)
L'invention concerne des composés représentés par la formule (I) ainsi que leurs solvates, hydrates et sels pharmaceutiquement acceptables, lesquels inhibent les protéases, y compris la cathepsine K. L'invention concerne également des compositions pharmaceutiques renfermant ces composés, de nouveaux intermédiaires de ces composés et des méthodes de traitement de la déperdition osseuse ou de la détérioration excessive du cartilage ou de la matrice osseuse, l'ostéoporose notamment, de pathologies gingivales, notamment la gingivite et la parodontite, de l'arthrite, plus précisément l'arthrose et la polyarthrite rhumatoïde, de la maladie osseuse de Paget, de l'hypercalcémie de type malin et de la maladie métabolique des os. Ces méthodes consistent à administrer un composé selon l'invention à un sujet, chez lequel il est nécessaire d'inhiber une déperdition osseuse ou une détérioration excessive du cartilage ou de la matrice osseuse.
Also published as
US09868800
Latest bibliographic data on file with the International Bureau