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1. (WO2011114148) 4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau   
Pub. No.: WO/2011/114148 International Application No.: PCT/GB2011/050515
Publication Date: 22.09.2011 International Filing Date: 16.03.2011
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 11/00 (2006.01) ,A61P 9/10 (2006.01) ,A61P 19/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
02
for joint disorders, e.g. arthritis, arthrosis
Applicants:
BENGTSSON, Boel, Ase [SE/SE]; SE (UsOnly)
BLACKABY, Wesley [GB/GB]; GB (UsOnly)
CUMMING, John [GB/GB]; GB (UsOnly)
FAULL, Alan, Wellington [GB/GB]; GB (UsOnly)
LARSSON, Joakim [SE/SE]; SE (UsOnly)
NASH, Ian, Alun [GB/GB]; GB (UsOnly)
OLDHAM, Keith [GB/GB]; GB (UsOnly)
PAPE, Andrew [GB/GB]; GB (UsOnly)
ASTRAZENECA AB [SE/SE]; SE-151 85 Södertälje, SE (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
ASTRAZENECA UK LIMITED [GB/GB]; 2 Kingdom Street London Greater London W2 6BD, GB (MG)
Inventors:
BENGTSSON, Boel, Ase; SE
BLACKABY, Wesley; GB
CUMMING, John; GB
FAULL, Alan, Wellington; GB
LARSSON, Joakim; SE
NASH, Ian, Alun; GB
OLDHAM, Keith; GB
PAPE, Andrew; GB
Agent:
ASTRAZENECA INTELLECTUAL PROPERTY; AstraZeneca AB SE-151 85 Södertälje, SE
Priority Data:
61/314,81817.03.2010US
Title (EN) 4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS
(FR) DÉRIVÉS DE 4H-[1,2,4]TRIAZOLO[5,1-B]PYRIMIDIN-7-ONE À TITRE D'ANTAGONISTES DES RÉCEPTEURS CCR2B
Abstract:
(EN) The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical compositions, which comprise compounds that act via antagonism of the CCR2b receptor for which MCP-1 is one of the known ligands and so may be used to treat inflammatory disease, atherosclerosis, diabetes, obesity, cancer, chronic obstructive pulmonary disease (COPD) rheumatoid arthritis and/or neuropathic pain, which is mediated by these receptors.
(FR) Cette invention concerne de nouveaux composés destinés à être utilisés dans les compositions, des procédés pour leur préparation, des intermédiaires utiles dans leur préparation et leur utilisation à titre d'agents thérapeutiques. Cette invention concerne également des compositions pharmaceutiques, qui comprennent des composés qui agissent par antagonisme du récepteur CCR2b pour lequel MCP-1 est un des ligands connus et peuvent, par conséquent, être utilisés pour traiter la maladie inflammatoire, l'athérosclérose, le diabète, l'obésité, le cancer, la pneumopathie obstructive chronique (COPD), la polyarthrite rhumatoïde et/ou la douleur neuropathique, qui est médié(e) par ces récepteurs.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)