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1. WO2008039138 - NOVEL 5, 7-DISUBSTITUTED [1, 3 ] THIAZOLO [4, 5-D] PYRIMIDIN-2 (3H)-ONE DERIVATIVES AND THEIR USE IN THERAPY

Publication Number WO/2008/039138
Publication Date 03.04.2008
International Application No. PCT/SE2007/000857
International Filing Date 27.09.2007
IPC
C07D 513/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 11/06 2006.01
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 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 9/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
CPC
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 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
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 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 21/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
02Muscle relaxants, e.g. for tetanus or cramps
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • ASTRAZENECA AB [SE]/[SE] (AllExceptUS)
  • JOHANSSON, Rolf [SE]/[SE] (UsOnly)
  • KARLSTRÖM, Sofia [SE]/[SE] (UsOnly)
  • KERS, Annika [SE]/[SE] (UsOnly)
  • NORDVALL, Gunnar [SE]/[SE] (UsOnly)
  • REIN, Tobias [SE]/[SE] (UsOnly)
  • SLIVO, Can [SE]/[SE] (UsOnly)
Inventors
  • JOHANSSON, Rolf
  • KARLSTRÖM, Sofia
  • KERS, Annika
  • NORDVALL, Gunnar
  • REIN, Tobias
  • SLIVO, Can
Agents
  • ASTRAZENECA AB
Priority Data
60/827,46029.09.2006US
60/828,12504.10.2006US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL 5, 7-DISUBSTITUTED [1, 3 ] THIAZOLO [4, 5-D] PYRIMIDIN-2 (3H)-ONE DERIVATIVES AND THEIR USE IN THERAPY
(FR) NOUVEAUX DÉRIVÉS DE [1, 3 ]THIAZOLO[4, 5-D]PYRIMIDINE-2(3H)-ONE 5,7-DISUBSTITUTÉS ET LEUR UTILISATION EN THÉRAPIE
Abstract
(EN)
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
(FR)
L'invention concerne de nouveaux dérivés de [1,3]thiazolo[4,5-d]pyrimidine-2(3H)-one 5,7 disubstitués, représentés par la formule (I) dans laquelle R1, R2, R3, R4 et n ont les significations données dans le descriptif, des sels pharmaceutiquement acceptables de ces dérivés, des procédés de fabrication de ces composés, des compositions pharmaceutiques contenant ces composés et leur utilisation en thérapie. Les composés représentés par la formule (I) sont des antagonistes de récepteurs de CX3CR1 et sont par conséquent particulièrement utiles dans la traitement ou la prophylaxie de troubles neurodégénératifs, de maladies de démyélinisation, de troubles athérosclérotiques cardiovasculaires et cérébrovasculaires, de maladies artérielles périphériques, de l'arthrite rhumatoïde, de maladies pulmonaires telles que COPD, de l'asthme ou de la douleur.
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