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grantDate 2016-01-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2016-01-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2556752-T3
titleOfInvention Cannabinoid receptor ligands
abstract A compound according to formula (I), or a pharmaceutically acceptable salt or solvate thereof X4 is O or N (Rbx); wherein Rbx is hydrogen, alkyl, haloalkyl, alkoxyalkyl, -C (O) O (alkyl), monocyclic cycloalkyl, - (CR1cR1d) q3- (monocyclic cycloalkyl), or haloalkoxyalkyl; and A1 is -N (Rb) C (O) Ra, -N (Rb) C (O) ORd, -N (Rb) C (O) N (Rb), -N (Rb) (Rc), or - N> = C (Rp) (Rq); or X4 and A1 together are N> = N (Rcx); A3 is C (O) Rh, -S (O) 2Rc, -C (O) N (Rh) 2, -C (S) N (Rh) 2, -S (O) 2N (Rh) 2, -C (> = NORh) Rh, -N (Rh) C (O) Rh, -N (Rh) C (O) ORe, -N (Rh) S (O) 2Rc, -N (Rh) C (O) N (Rh) 2, -N (Rh) S (O) 2N (Rh) 2, -CN, -ORh, or -N (Rh) 2; Ra and Rc are each, at each occurrence independently hydrogen, alkyl, haloalkyl, - (CR1aR1b) q3-A3, G1d, or - (CR1aR1b) q3-G1d; Rb is each, at each occurrence independently hydrogen, alkyl, haloalkyl, alkoxyalkyl, monocyclic cycloalkyl, - (CR1cCR1d) q3- (monocyclic cycloalkyl), or haloalkoxyalkyl; Rd, at each occurrence is independently alkyl, haloalkyl, - (CR1aR1b) q3-A3, G1d, or - (CR1aR1b) q3-G1d; Rcx is alkyl, haloalkyl, - (CR1aR1b) q3-A3, G1d, or - (CR1aR1b) q3-G1d; Rp is hydrogen, alkyl, haloalkyl, - (CR1aR1b) q3-A3, -C (O) ORd, -C (O) Rd, G1d, or - (CR1aR1b) q3-G1d; Rq is hydrogen, alkyl, haloalkyl, -N (Rb) Rc), - (CR1aR1b) q3-A3, G1d, or - (CR1aR1b) q3-G1d; or Rp and Rq, together with the carbon atom to which they are attached, form a monocyclic 5, 6, 7, or 8-membered ring, optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting in oxo, alkyl, haloalkyl, and halogen; A5 represents the formula (a), (b) or (c) G1d, at each occurrence, it is independently a monocyclic heterocycle, a monocyclic heteroaryl, a phenyl, a monocyclic cycloalkyl, or a monocyclic cycloalkenyl; wherein G1d is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of -N (Rh) 2, -CN, oxo, alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, and OH; Re, at each occurrence, is independently C1-C4 alkyl, C1-C4 haloalkyl, monocyclic cycloalkyl, monocyclic heterocycle, or - (CR1cCR1d) q3- (monocyclic cycloalkyl); Rf, at each occurrence, is independently hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, - (CR1cR1d) q3-ORh, monocyclic heterocycle, monocyclic cycloalkyl, or - (CR1cR1d) q3- (monocyclic cycloalkyl); Rh, at each occurrence, is independently hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, monocyclic cycloalkyl, or - (CR1cR1d) q3- (monocyclic cycloalkyl); R21, R22 and R23 are each independently alkyl, alkenyl, alkynyl, haloalkyl, - (CR2aR2b) q4-OH, - (CR2aR2b) q4-O-alkyl, - (CR2aR2b) q4-O-haloalkyl, - (CR2aR2b) q4 -CO-G2a, - (CR2aR2b) q4-O- (CR2cR2d) q3-G2a, - (CR2aR2b) q5- C (O) -Ra, - (CR2aR2b) q5-C (> = N-ORf) Ra, - (CR2aR2b) q5-SO2-Rd, (CR2aR2b) q5-G2b, - (CR2aR2b) q5-C (O) N (Rb) (Rc), or - (CR2aR2b) q5-CN; G2a is independently at each occurrence cycloalkyl, heterocycle, aryl, or heteroaryl; G1b is a monocyclic ring selected from the group consisting of cycloalkyl, cycloalkenyl, thienyl, phenyl, furanyl, oxazolyl, isoxazolyl, oxadiazolyl, and heterocycle; wherein the heterocycle contains zero or a double bond, one or two oxygen, and zero or a nitrogen as ring atoms; two non-adjacent atoms of said heterocyclic ring may optionally be connected by an alkenylene bridge of 2, 3, or 4 carbon atoms, or optionally connected by an alkylene bridge of 1, 2, 3, or 4 carbon atoms; each G2b ring is optionally fused with a monocyclic ring selected from the group consisting of benzo, cycloalkyl, cycloalkenyl, heterocycle and heteroaryl; G2a and G2b are each independently unsubstituted or substituted at each occurrence with 1, 2, 3, 4, 5, or 6 substituents independently selected from the group consisting of oxo, alkyl, halogen, -OH, alkoxy, haloalkoxy, and haloalkyl; X1 is O or S; X2 is N (R10) wherein R10 is alkyl, alkoxyalkyl, haloalkoxyalkyl, or haloalkyl; R3, R4, R5, R6, R7, R8 and R9 are each independently G3, hydrogen, alkyl, alkenyl, alkynyl, -NO2, -CN, halogen, -ORh, -N (Rh) 2, -C (O) Rh, -C (O) O (Rh), haloalkyl, - (CR3aR3b) q6-ORh, - (CR3aR3b) q6-N (Rh) 2, - (CR3aR3b) q6- C (O) Rh, or - (CR3aR3b ) q6-C (O) O (Rh); G3, at each occurrence, is independently cycloalkyl, cycloalkenyl, aryl, heterocycle, or heteroaryl wherein each G3 is independently unsubstituted or substituted with 1, 2, 3 or 4 substituents selected from the group consisting of C1-C4 alkyl, C2 alkenyl -C4, C2-C4 alkynyl, halogen, C1-C4 haloalkyl,> = N-CN,> = N-ORh, -CN, oxo, -ORh, -OC (O) Rh, -OC (O) N (Rh ) 2, -S (O) 2Re, -S (O) 2N (Rh) 2, -C (O) Rh, -C (O) ORh, -C (O) N (Rh) 2, -N (Rh ) 2, -N (Rh) C (O) Rh, -N (Rh) S (O) 2Re, -N (Rh) C (O) O (Re), and -N (Rh) C (O) N (Rh) 2; R1a, at each occurrence, is independently hydrogen, halogen, C1-C4 alkyl or C1-C4 haloalkyl; R1b, at each occurrence, is independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 haloalkyl, -ORh, -N (Rh) 2, -N (Rh) C (O) Rh, -N (Rh) C (O) ORe; or -N (Rh) S (O) 2Re; R1c, R1d, R2a, R2b, R2c, R2d, R3a and R3b, at each occurrence, are each independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 haloalkyl; Rx at each occurrence is independently C1-C4 alkyl, halogen, C1-C4 haloalkyl or -CN; q4, at each occurrence, is independently 2, 3, 4, or 5; q3, at each occurrence, is 1, 2 or, 3; q5 and q6, at each occurrence, are each independently 1, 2, 3, 4, 5, or 6; z is 0, 1, 2, 3, or 4; and the monocyclic cycloalkyl and the monocyclic heterocycle, as a substituent or as part of a substituent, of Rb, Rb, Re, Rf, and Rh, are each independently unsubstituted or substituted at each occurrence with 1, 2, 3, or 4 substituents independently selected from the group consisting of oxo, C1-C4 alkyl, halogen, OH, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 haloalkyl,
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Total number of triples: 826.