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1. (WO2010076524) DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/076524 International Application No.: PCT/FR2009/052691
Publication Date: 08.07.2010 International Filing Date: 24.12.2009
IPC:
C07D 401/04 (2006.01) ,C07D 401/14 (2006.01) ,C07D 409/14 (2006.01) ,A61K 31/4439 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/4545 (2006.01) ,A61K 31/497 (2006.01) ,A61K 31/5375 (2006.01) ,A61P 7/00 (2006.01) ,A61P 9/00 (2006.01) ,A61P 25/00 (2006.01) ,A61P 27/00 (2006.01) ,G01N 33/53 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4545
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53
Immunoassay; Biospecific binding assay; Materials therefor
Applicants:
SANOFI [FR/FR]; 174, avenue de France F-75013 Paris, FR (AllExceptUS)
ALTENBURGER, Jean-Michel [FR/FR]; FR (UsOnly)
FOSSEY, Valérie [FR/FR]; FR (UsOnly)
ILLIANO, Stéphane [FR/FR]; FR (UsOnly)
MANETTE, Géraldine [FR/FR]; FR (UsOnly)
Inventors:
ALTENBURGER, Jean-Michel; FR
FOSSEY, Valérie; FR
ILLIANO, Stéphane; FR
MANETTE, Géraldine; FR
Agent:
ROMANOWSKI, Caroline; c/o Sanofi-Aventis Département Brevets 174, avenue de France F-75013 Paris, FR
Priority Data:
080747429.12.2008FR
090409228.08.2009FR
Title (EN) DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
(FR) DERIVES DE 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE COMME ACTIVATEURS DE HIF
Abstract:
(EN) The invention relates to compounds according to the formula (I): R is a -SO2-NR3R4 group, a hydrogen atom, a halogen atom, a -halogeno(C1-C5)alkyl group, a -CO2R5 group or a -SO2-R4 group; R1 is a heterocycloalkyl group containing no nitrogen atoms, a -W-(C3-C6)cycloalkyl group, a -W-aryl group, a -W-heteroaryl group, a -W-heterocycloalkyl group, a -W-COOR5 group, a -W-CONR5R6 group; R2 is a hydrogen atom, a -(C1-C5)alkyl group, a -(C1-C5)alkylene-0-(C1-C5)alkyl group, a -halogeno(C1-C5)alkyl group, a -W-COOR5 group, a -W-C(O)NHR5 group or a -W-C(O)-NR5R6 group; n is 0, 1 or 2; W is a -(C1-C5)alkylene- group- or a -(C3-C6)cycloalkylene- group; R3 and R4, identical or different, are, independently from one another, a hydrogen atom, a -(C1-C5)alkyl group, a -(C3-C6)cycloalkyl group, a -(C1-C5)alkylene-O-(C1-C5)alkyl group, an aryl, a -CH2-aryl group, a heteroaryl, a heterocycloalkyl, a -W-OH group, a -W-CHOH-CH2OH group, a -W-CO2R5 group, a -W-NR5R6 group or a -W-O-(CH2)n-aryl group; or else R3 and R4 jointly form a heterocycloalkyl group with the nitrogen atom that supports them; R5 and R6, identical or different, are, independently from one another, a hydrogen atom, a -(C1-C5)alkyl group or a (C1-C5)halogenoalkyl group, as well as to a method for preparing same and to the therapeutic applications thereof.
(FR) L'invention concerne des composés répondant à la formule (I) : R représente un groupe -SO2-NR3R4, un atome d'hydrogène, un atome d'halogène, un groupe -halogéno(C1 -C5)alkyle, un groupe -CO2R5 ou un groupe -SO2-R4; R1 représente un groupe hétérocycloalkyle ne contenant pas d'atome d'azote, un groupe -W-(C3-C6)cycloalkyle, un groupe -W-aryle, un groupe -W-hétéroaryle, un groupe -W-hétérocycloalkyle, un groupe -W-C00R5, un groupe -W-CONR5R6; R2 représente un atome d'hydrogène, un groupe -(C1 -C5)alkyle, un groupe -(C1 -C5)alkylène-0-(C1 - C5)alkyle, un groupe -halogéno(C1 -C5)alkyle, un groupe -W-C00R5, un groupe -W-C(O)NHR5 ou un groupe -W-C(O)-NR5R6; n représente 0, 1 ou 2; W est un groupe - (C1 -C5)alkylène- ou un groupe -(C3-C6)cycloalkylène-; R3 et R4, identiques ou différents, représentent, indépendamment l'un de l'autre, un atome d'hydrogène, un groupe -(C1 -C5)alkyle, un groupe -(C3-C6)cycloalkyle, un groupe -(C1 -C5)alkylène-O-(C1 -C5)alkyle, un aryle, un groupe -CH2-aryle, un hétéroaryle, un hétérocycloalkyle, un groupe -W-OH, un groupe -W-CHOH-CH2OH, un groupe -W-CO2R5,un groupe -W-NR5R6 ou un groupe -W-O-(CH2)n-aryle; ou bien R3 et R4 forment ensemble avec l'atome d'azote qui les porte un groupe hétérocycloalkyle; R5 et R6, identiques ou différents, représentent, indépendamment l'un de l'autre, un atome d'hydrogène, un groupe -(C1 -C5)alkyle ou un groupe (C1 -C5) halogénoalkyle, ainsi que leur procédé de préparation et leurs applications en thérapeutique.
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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, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, 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: French (FR)
Filing Language: French (FR)
Also published as:
DZDZP2011000452UAa201109445IL213789SG172803EP2382205JP2012513976
CN102333769CA2748411EA201170899KR1020110099786BRPI0924060TN2011000267
NZ593751DK2382205AU2009334569VN29030ID051.4537MYPI 2011003012
IN2541/KOLNP/2011