http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-082763-A1
Outgoing Links
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| filingDate | 2011-06-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
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| publicationDate | 2013-01-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-082763-A1 |
| titleOfInvention | PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR CANCER TREATMENT |
| abstract | Whose compounds are useful as therapeutic agents, particularly for the treatment of cancers. This also refers to pharmaceutical compositions containing an MDM2 inhibitor. Claim 1: A compound of the formula (1), or a pharmaceutically acceptable salt thereof, characterized in that: Q is a bond or optionally can be selected from O, NR7 or S (O) v, when n * is an integer from 1 to 6; Z is C = O or S (= O) 2; Each one presented is independently selected from H, C1-3 alkyl, (halo) C1-3 alkyl, (hydroxy) C1-3 alkyl, (alkoxy) C1-3 alkyl, or cyano; Rb is H, halo, C1-3 alkyl, (halo) C1-3 alkyl, (hydroxy) C1-3 alkyl, (alkoxy) C1-3 alkyl, or cyano; Rc and Rd are independently selected from H, halo, C1-3 alkyl, C1-3 alkoxy, (halo) C1-3 alkyl, (halo) C1-3 alkoxy, (alkoxy) C1-3 alkyl, or (hydroxy) alkyl C1-3, or Rc and Rd may optionally combine to form a spiro-cycloalkyl or heterocycle ring system; Re is (a) H or halo; or (b) C1-8 alkyl, C3-8 cycloalkyl, C3-8 heterocycle, cyano, halogen, hydroxyl, -OR5, NR7R8, or heterocycloalkyl, any of which may optionally be substituted with 1 or more Rx groups as allowed by valence, or Re and any of the R 'or R' 'groups may optionally combine to form a spiro-cycloalkyl or heterocycle ring system, or Rd and any of the R' or R '' groups may optionally combine to form a fused cycloalkyl or heterocycle ring system, or Rd and Re may optionally combine to form a fused cycloalkyl or heterocycle ring system; R 'and R' 'each presented, respectively, are independently H, halo, C1-3 alkyl, C1-3 alkoxy, (halo) C1-3 alkyl, (halo) C1-3 alkoxy, (alkoxy) C1 alkyl -3, (hydroxy) C1-3 alkyl, -S-C1-3 alkyl, C (O) C1-3 alkyl, -NR7R8, or hydroxyl, or R 'and R' 'bonded to the same carbon atom can optionally combine to form = O, or R 'and R' 'bonded to the same carbon atom can optionally combine to form a spiro or heterocycle fused cycloalkyl ring system; R1 is (a) -COOH, -C (O) OR10, -C (O) NHOH, -C (O) NH-NH2, -C (O) NHS (O) 2R10, -S (O) 2NHC (O ) R10, -S (O) 2NR7R8, -NR7C (O) R10, -NR7C (O) OR5, -C (O) NR7R8, -NR7S (O) 2R10, -NR7C (O) NR7R8, -S (O) vR10, hydroxylalkyl, -cyclopropyl-COOH, or CN; or (b) heteroaryl or heterocycle, any of which may optionally be substituted independently with one or more Rx groups as allowed by valence; R2 is (a) -NR7R8, NR7C (O) OR10, NR7C (O) NR7R10, or -C (Ra) R5R6; or (b) aryl, heteroaryl, cycloalkyl, or heterocycle, any of which may optionally be independently substituted with one or more Rx groups as allowed by valence; R3 and R4 are independently aryl or heteroaryl, any of which may optionally be independently substituted with one or more Rx groups as allowed by valence, or any R3 and Ra together with the ring carbon atom to which both bind. , or R4 and Rb together with the ring carbon atom to which both bind can optionally combine to form a spiro-fused bicyclic ring system selected from the group of formulas (2), where K is -O-, - NR7-, or -C (= O) NR7-; R5 and R6 each presented, respectively, are independently selected from (a) H or CN; (b) - (alkylene) t-OH, - (alkylene) t-OR9, - (alkylene) t-SR9, - (alkylene) t-NR10R11, - (alkylene) tC (O) R9, - (alkylene) tC (O) OR9, - (alkylene) t-OC (O) R9, - (alkylene) tS (O) vR9, - (alkylene) t-NHS (O) 2R10, - (alkylene) tN (R11) S (O ) 2R10, - (alkylene) tS (O) 2NR10R11, - (alkylene) tN (R11) S (O) 2NR10R11, -NR10C (O) R9, -C (O) NR10R11, -NR10S (O) 2R9, S ( O) 2NR10, or NR10C (O) NR10R11; or (c) haloalkyl, haloalkoxy, -C1-6 alkyl, C2-6 alkenyl, -C2-6 alkynyl, -C3-8 cycloalkyl, (-C3-8 cycloalkyl) (C1-3 alkyl), -C4-8 cycloalkenyl , aryl, aryl (-C1-3alkyl), heteroaryl, heteroaryl (-C1-3alkyl), heterocycle or heterocycle (-C1-3alkyl), any of which may optionally be independently substituted with one or more Rx groups as was allowed by valence; R7 and R8 each presented, respectively, are independently selected from H, cyano, -O-C1-6 alkyl, -C 1-6 alkyl, halo-C 1-6 alkyl, cycloalkyl, -C2-6 alkenyl, -C2 alkynyl -6, aryl, heteroaryl, heterocycle, arylalkyl, heteroarylalkyl, heterocycle (C1-10 alkyl), or (-C3-8 alkylcycloalkyl) (C1-3 alkyl), any of which may optionally be substituted as allowed by valence with one or more Rx, or R7 and R8 can combine to form a C4-8 heterocycle ring optionally substituted with one or more Rx; R9 is haloalkyl, haloalkoxy, -C1-6 alkyl, C2-6 alkenyl, -C2-6 alkynyl, -C3-8 cycloalkyl, (-C3-8 cycloalkyl) (C1-3 alkyl), -C4-8 cycloalkenyl, aryl , heteroaryl, heterocycle, or heterocycloalkyl, any of which may optionally be substituted independently with one or more Rx groups as allowed by valence; R10 and R11 each presented, respectively, are independently selected from H, alkyl, haloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, arylalkyl, heteroarylalkyl, heterocycloalkyl, or cycloalkylalkyl, any of which may optionally be substituted as it was allowed by valence with one or more Rx, or R10 and R11 may combine to form a heterocycle ring optionally substituted with one or more Rx; Rx each presented is independently, deuterium, halo, cyano, nitro, oxo, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycle, aryl, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkyl, - (alkylene) t- OR *, - (alkylene) t S (O) vR *, - (alkylene) t-NR + R ++, - (alkylene) tC (= O) R *, - (alkylene) tC (= S) R *, - ( alkylene) tC (= O) OR *, - (alkylene) t-OC (= O) R *, - (alkylene) tC (= S) OR *, - (alkylene) tC (= O) NR + R ++, - (alkylene) tC (= S) NR + R ++, - (alkylene) tN (R +) C (= O) NR + R ++, - (alkylene) tN (R +) C (= S) NR + R ++, - (alkylene) tN (R +) C (= O) R *, - (alkylene) tN (R +) C (= S) R *, - (alkylene) t-OC (= O) NR + R ++, - (alkylene) t-OC (= S) NR + R ++, - (alkylene) t-SO2NR + R ++, - (alkylene) tN (R +) SO2R *, - (alkylene) tN (R +) SO2R + R ++, - (alkylene) tN (R +) C (= O) OR *, - (alkylene) tN (R +) C (= S) OR *, or - (alkylene) tN (R +) SO2R *, where the alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl groups , heterocycle, aryl, heteroaryl, arylalkyl, heteroarylalkyl, c icloalkylalkyl, and heterocycloalkyl can also be independently substituted with one or more halo, cyano, oxo, - (alkylene) t-OR *, - (alkylene) tS (O) vR *, - (alkylene) t-NR + R ++, - (alkylene) tC (= O) R *, - (alkylene) tC (= S) R *, - (alkylene) tC (= O) OR *, - (alkylene) t-OC (= O) R *, - (alkylene) tC (= S) OR *, - (alkylene) tC (= O) NR + R ++, - (alkylene) tC (= S) NR + R ++, - (alkylene) tN (R +) C (= O) NR + R ++, - (alkylene) tN (R +) C (= S) NR + R ++, - (alkylene) tN (R +) C (= O) R *, - (alkylene) tN (R +) C (= S) R *, - (alkylene) t-OC (= O) NR + R ++, - (alkylene) t-OC (= S) NR + R ++, - (alkylene) t-SO2NR + R ++, - (alkylene) tN (R + ) SO2R *, - (alkylene) tN (R +) SO2R + R ++, - (alkylene) tN (R +) C (= O) OR *, - (alkylene) tN (R +) C (= S) OR *, or - (alkylene) tN (R +) SO2R *; R * is H, haloalkyl, haloalkoxy, -C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-8 cycloalkyl, C 4-8 cycloalkenyl, aryl, heteroaryl, or heterocycle; R + and R ++ are independently H, alkyl, haloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, arylalkyl, heteroarylalkyl, heterocycloalkyl, or cycloalkylalkyl, or R + and R ++ linked to the same nitrogen atom can optionally combine to form a system of heterocycle ring; m is 1, 2 or 3; n and n * are each independently selected from 0 or an integer from 1 to 6; p is 0, 1, 2 or 3; t each presented is independently 0 or an integer from 1 to 6; and v each that is presented is independently 0, 1 or 2. |
| priorityDate | 2010-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 113.