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1. (WO2006133926) PYRAZOLE DERIVATES AS CANNABINOID RECEPTOR MODULATORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2006/133926 International Application No.: PCT/EP2006/005726
Publication Date: 21.12.2006 International Filing Date: 14.06.2006
IPC:
C07D 403/12 (2006.01) ,C07D 231/14 (2006.01) ,C07D 401/14 (2006.01) ,C07D 413/14 (2006.01) ,A61K 31/4155 (2006.01) ,A61K 31/4406 (2006.01) ,A61P 3/04 (2006.01) ,C07D 403/14 (2006.01) ,C07D 403/06 (2006.01) ,C07D 409/12 (2006.01) ,C07D 407/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4155
not condensed and 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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4406
only substituted in position 3, e.g. zimeldine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
407
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
CAREX SA [FR/FR]; Bioparc Parc d'Innovation BP 30442 67412 Boulevard Sébastien Brandt F-Illkirch, Cedex, FR (AllExceptUS)
AMENGUAL, Rémi [FR/FR]; FR (UsOnly)
MARSOL, Claire [FR/FR]; FR (UsOnly)
MAYEUX, Eric [FR/FR]; FR (UsOnly)
SIERRA, Michael [FR/DK]; DK (UsOnly)
WAGNER, Patrick [FR/FR]; FR (UsOnly)
Inventors:
AMENGUAL, Rémi; FR
MARSOL, Claire; FR
MAYEUX, Eric; FR
SIERRA, Michael; DK
WAGNER, Patrick; FR
Agent:
WALLS, Alan, James; PO Box 223 Tadworth Surrey KT20 5YF, GB
Priority Data:
05360022.717.06.2005EP
05360032.626.09.2005EP
05360047.424.11.2005EP
Title (EN) PYRAZOLE DERIVATES AS CANNABINOID RECEPTOR MODULATORS
(FR) DERIVES DE PYRAZOLE UTILISES COMME MODULATEURS DU RECEPTEUR CANNABINOIDE
Abstract:
(EN) Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter alia in the treatment of obesity: (I) wherein A1 is hydrogen, -COOH, or tetrazolyl, and A2 is hydrogen, -COOH, tetrazolyl, -CN, -CF3, -COR6, -SO2R6, -OR7, -NR7R8, -NHCOR6, and -NR7SO2R8 provided that one of A1 and A2 is either -COOH or tetrazolyl; p is O or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is O or 1 ; R1 is a bond, or - (CH2)aB1(CH2)b- wherein a and b are independently O, 1 , 2 or 3 provided that a+b is not greater than 4, and B1 is -CO-, -0-, -S-, -SO-, -SO2-, -CH2-, -CHOH- or -NR7-; R2 is a bond, -(CH2)aB1 (CH2)b- or -[(CH2)aB1 (CH2)b]n-A4-[(CH2)cB2(CH2)d]m- wherein a, b, and B1 are as defined for R1; B2 is as defined for B1, c and d are independently 0,1 , 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently O or 1 and A4 is a monocarbocyclic or monoheterocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF3, C1-C4 alkyl, cycloalkyl, -OR9, oxo or -NR7R8; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, -CF3, -OR9, -NR7R8, -(CH2)SCOR6, -(CH2)SSO2R6, -(CH2)SNR7COR6, -(CH2)SNR7COOR8, -(CH2)SNR7SO2R6, wherein s is 1 , 2, 3 or 4; R4 and R5 independently -R9, -CN, -F, -Cl, -Br, -OR9, -NR7R8, -NR7COR6, -NR7SO2R6, -COR6, -SR9, -SOR9, -SO2R6, (C1-C4 alkyl)OR9, -(C1-C4 alkyl)NR7R8, -(C1-C4 alkyl)NR7COR6, C1-C4 alkyl)NR7COOR8, -(C1-C4 alkyl)NR7SO2R6, -(C1-C4 alkyl)COR6, -(C1-C4 alkyl)SO2R6, -NR7COOR8, or [N-(C1-C4 alkyl)]- tetrazolyl; R6 is C1-C4 alkyl, cycloalkyl, -CF3 or -NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl and R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl.
(FR) L'invention concerne des composés représentés par la formule (I), qui sont de récepteurs cannabinoïdes CB1, utiles notamment pour le traitement de l'obésité: (I) A1 représente hydrogène, -COOH, ou tétrazolyle, et A2 représente hydrogène, -COOH, tétrazolyle, -CN, -CF3, -COR6, -SO2R6, -OR7, -NR7R8, -NHCOR6, et -NR7SO2R8 à condition que A1 ou A2 représente soit COOH, soit tétrazolyle; p représente O ou 1, et A3 représente phényle ou cycloalkyle, qui peuvent chacun être éventuellement substitués par R4 et/ou R5; q représente O ou 1; R1 représente une liaison, ou - (CH2)aB1(CH2)b-, a et b représentant séparément O, 1, 2 ou 3, à condition que a+b ne soit pas supérieur à 4, et B1 représente -CO-, -0-, -S-, -SO-, -SO2-, -CH2-, -CHOH- ou -NR7-; R2 représente une liaison, -(CH2)aB1 (CH2)b- ou -[(CH2)aB1 (CH2)b]n-A4-[(CH2)cB2(CH2)d]m-, dans laquelle a, b, et B1 ont les mêmes définitions que dans R1; B2 correspond à la définition de B1, c et d représentent séparément 0,1, 2 ou 3; à condition que a+b+c+d ne soient pas supérieurs à 6, n et m représentent séparément O ou 1, et A4 représente un cycle monocarbocyclique ou monohétérocyclique comprenant de 3 à 8 atomes, éventuellement substitué par un ou plusieurs des groupes suivants: -F, -Cl, -Br, -CN, -CF3, C1-C4 alkyle, cycloalkyle, -OR9, oxo ou -NR7R8; R3 représente hydrogène, C1-C4 alkyle, cycloalkyle, -CF3, -OR9, -NR7R8, -(CH2)SCOR6, -(CH2)SSO2R6, -(CH2)SNR7COR6, -(CH2)SNR7COOR8, -(CH2)SNR7SO2R6, dans lesquels s représente 1, 2, 3 ou 4; R4 et R5 représentent séparément -R9, -CN, -F, -Cl, -Br, -OR9, -NR7R8, -NR7COR6, -NR7SO2R6, -COR6, -SR9, -SOR9, -SO2R6, (C1-C4 alkyle)OR9, -(C1-C4 alkyle)NR7R8, -(C1-C4 alkyle)NR7COR6, C1-C4 alkyle)NR7COOR8, -(C1-C4 alkyl)NR7SO2R6, -(C1-C4 alkyl)COR6, -(C1-C4 alkyl)SO2R6, -NR7COOR8, ou [N-(C1-C4 alkyle)]- tétrazolyle; R6 représente C1-C4 alkyle, cycloalkyle, -CF3 ou -NR7R8; R7 et R8 représentent séparément hydrogène, C1-C4 alkyle ou cycloalkyle, et R9 représente hydrogène, C1-C4 alkyle, cycloalkyle, C1-C4 alkyle, entièrement ou partiellement fluoré.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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)
Also published as:
EP1928859US20080200527