http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2353448-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c13193fe65025a46525ac2b48f75f12a http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bb75b0b19820e3833ebdcb31603b242b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-498 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D451-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-498 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D451-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-04 |
| filingDate | 2008-01-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2011-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_acf84ecdb16a917fd7052b5d0b1211dc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_658bdd959d2460830d25d21441acd5dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1603e57ee5898a892e5b56cbffff5cfc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_91676d5c533c762dfae0930f748327ab |
| publicationDate | 2011-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2353448-T3 |
| titleOfInvention | HETEROCYCLIC-SUBSTITUTED PIPERIDINS AS LIGANDOS OF ORL-1. |
| abstract | Compound of formula (I): ** (See formula) ** or a pharmaceutically acceptable derivative thereof, in which: each R2 is independently selected from: (a) -halo, -CN, -NO2, -OT3, - C (O) T3, -C (O) OT3, -C (O) N (T1) (T2), -S (O) 3H, -S (O) T3, -S (O) 2T3, -S ( O) 2N (T1) (T2), -N (T1) (T2), -N (T3) C (O) T3, -N (T3) C (O) N (T1) (T2), -N ( T3) S (O) 2T3, or -N (T3) S (O) 2N (T1) (T2); or (b) - (C1-C6) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl, - (C1-C6) alkoxy, - (C3-C7) cycloalkyl, - (C6-C14) bicycloalkyl, - (C8-C20) tricycloalkyl, - (C5-C10) cycloalkenyl, - (C7-C14) bicycloalkenyl, - (C5-C20) tricycloalkenyl, -hetero-cycle (5 or 6 member), or bicycloheterocycle (de 7 to 10 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R8 groups; or (c) -phenyl, -naphthalenyl, - (C14) aryl, or -heteroaryl (5 or 6 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R7 groups; a is an integer selected from 0, 1 or 2; R3 is selected from: (a) -H; or (b) - (C1-C6) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl, -O (C1-C6) alkyl, -O (C2-C6) alkenyl, -O (C2 -C6) alkynyl, - (C3-C7) cycloalkyl, - (C3-C7) cycloalkenyl, - (C3-C7) cycloalkoxy, - (C6-C14) bicycloalkyl, - (C8-C20) tricycloalkyl, - (C5-C10 ) cycloalkenyl, - (C7-C14) bicycloalkenyl, - (C8-C20) tricycloalkenyl, -heterocycle (3 to 7 members), or -bicycloheterocycle (7 to 10 members), each of which is unsubstituted or is substituted with 1, 2 or 3 independently selected R8 groups; or (c) -phenyl, -naphthalenyl, - (C14) aryl, or -heteroaryl (5 to 10 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R7 groups; or (d) - (C1-C6) alkyl (= O) W1, - (C1-C6) alkyl (= NH) W1, -C (O) OV1, -C (O) N (V1) 2, -S (O) 2N (V1) 2, or -S (O) 2 (C1-C6) alkyl; or (e) - (C1-C4) alkyl substituted with 1, 2 or 3 substituents independently selected from - (C3-C7) cycloalkyl, - (C3-C7) cycloalkenyl, - (C3-C7) cycloalkoxy, - (C6- C14) bicycloalkyl, - (C8-C20) tricycloalkyl, - (C5-C10) cycloalkenyl, - (C7-C14) bicycloalkenyl, - (C8-C20) tricycloalkenyl, -heterocycle (3 to 7 members), -bicycloheterocycle (de 7 to 10 members), -phenyl, -naphthalenyl, - (C14) aryl, or -heteroaryl (5 to 10 members); or (f) - (C1-C3) alkyl substituted with a substituent selected from -N (R6) 2, -S (O) 2N (V1) 2, -N (R9) C (O) W1, -N (R9 ) S (O) 2W1, and -C (O) N (V1) 2; each W1 is independently selected from: (a) -H, - (C1-C6) alkyl, - (C3-C7) cycloalkyl, -O (C1-C6) alkyl, - (C3-C7) cycloalkoxy, -CH2CH2OH, - N (R6) 2; or (b) -heteroaryl (5- or 6-membered) optionally substituted with 1, 2 or 3 - (C1-C6) independently selected alkyl; each V1 is independently selected from -H, - (C1-C6) alkyl, - (C3-C7) cycloalkyl, -phenyl, or -benzyl; each Y is independently selected from O or S; A and B are independently selected from: (a) -H, -CN, -C (O) OT3, -C (O) N (T) 1 (T2), - (C3-C12) cycloalkyl, - (C3- C12) cycloalkoxy, - (C1-C6) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl or - (C1-C6) alkoxy, each of which is unsubstituted - (C3-C12) cycloalkyl , - (C3-C12) cycloalkoxy, - (C1-C6) alkyl, - (C2-C6) alkenyl or - (C2-C6) alkynyl or being substituted with 1 or 2 substituents independently selected from -OH, -S (O ) 2NH2, -N (R6) 2, = NR6, -C (O) OT3, -C (O) N (R6) 2, -N (R6) C (O) R9 and -heterocycle (5 or 6 members ) or 1, 2 or 3 -halo independently selected; or (b) AB together form a bridge (C2-C6), which is not substituted or substituted with 1, 2 or 3 independently selected R8 groups, and optionally containing said bridge, -HC = CH- within the bridge ( C2-C6); wherein the piperazine ring that is fused with the phenyl group may be in the endo- or exo- conformation with respect to the A-B bridge; or (c) AB together form a bridge -CH2-N (Ra) -CH2-, a bridge ** (See formula) ** or a bridge ** (See formula) ** where the piperazine ring that is fused with the phenyl group it may be in the endo- or exo- conformation with respect to the AB bridge; Ra is selected from -H, - (C1-C6) alkyl, - (C3-C7) cycloalkyl, -CH2-C (O) -Rc, - (CH2) -C (O) -ORc, - (CH2) -C (O) -N (Rc) 2, - (CH2) 2-O-Rc, - (CH2) 2-S (O ) 2-N (Rc) 2, Fc, or - (CH2) 2-N (Rc) S (O) 2-Rc; Rb is selected from: (a) -H, - (C1-C6) alkyl, - (C3-C7) cycloalkyl, -heterocycle (3 to 7 members), -N (Rc) 2, -N (Rc) - (C3-C7) cycloalkyl, or -N (Rc) -heterocycle (3 to 7 members); or (b) -phenyl, -naphthalenyl, or -heteroaryl (5 or 6 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R7 groups; or (c) -N (Rc) -phenyl, -N (Rc) -naphthalenyl, -N (Rc) - (C14) aryl, or -N (Rc) -heteroaryl (5 to 10 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R7 groups; each Rc is independently selected from -H or - (C1-C4) alkyl; C is selected from -H, -halo, -CN, -OT3, -C (O) OT3, -C (O) N (T) 1 (T2), - (C3-C12) cycloalkyl, - (C3-C12 ) cycloalkoxy, -N (R6) 2, -N (R6) C (O) R9, -NR6SO2N (R6) 2, -NR6-C (= NR6) N (P-6) 2, - (C1-C6) alkyl, - (C2-C6) alkenyl, or - (C2-C6) alkynyl, each of said being unsubstituted - (C1-C6) alkyl, - (C2-C6) alkenyl or - (C2-C6) alkynyl or being substituted with 1 or 2 substituents independently selected from -OH, -S (O) 2NH2, -N (R6) 2, = NR6, -C (O) OT3, -C (O) N (R6) 2, -N (R6) C (O) R9 and -heterocycle (5 or 6 members) or 1 to 3 -halo independently selected; The dashed line on the piperidine or the central piperidine bridge ring indicates the presence or absence of a bond and when the dashed line indicates the presence of a bond, then D is absent, otherwise D is: (a) -H, -CN, -C (O) OT3, or -C (O) N (T1) (T2); or (b) - (C1-C10) alkyl which is not substituted or substituted with 1, 2 or 3 independently selected R8 groups and, optionally, in which any carbon atom of group D except the carbon atom directly bonded to the piperidine or central ring of piperidine by bridge, is independently replaced by O or S; or (c) -phenyl, -naphthalenyl, or -heteroaryl (5 or 6 members), each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R7 groups; Z is a link; R1 is selected from: ** (See formula) ** m is an integer selected from 0, 1, 2, 3, 4, 5, 6 or 7; e and f are, each of them, an integer, where e is selected from 1, 2, 3, 4 or 5 and f is independently selected from 0, 1, 2, 3, 4, or 5 whenever 2 <= q (e + f) <= q 5; j and k are, each of them, an integer independently selected from 0, 1, 2, 3 or 4 provided that 1 <= q (j + k) <= q 4; each T1, T2, and T3 is independently -H or - (C1-C10) alkyl that is not substituted or substituted with 1, 2 or 3 independently selected R8 groups and, optionally, in which any carbon atom is independently substituted by O or S, or T1 and T2 can together form a 5 to 8 member ring where the number of atoms in the ring includes the nitrogen atom to which T1 and T2 are linked, said 5 to 8 member ring is not substituted or is substituted with 1, 2 or 3 independently selected R8 groups and, optionally, any carbon atom in said 5 to 8 member ring is independently replaced by O or S; each R6 is independently selected from -H, - (C1-C6) alkyl, or - (C3-C7) cycloalkyl, or two R6 groups attached to the same nitrogen atom can form a 5- to 8-membered ring, so that the number of atoms in the ring includes the nitrogen atom, in which one of the carbon atoms in the ring is optionally substituted by O or S; each R7 is independently selected from - (C1-C4) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl, -OR9, -SR9, -C (halo) 3, -CH (halo) 2, -CH2 (halo), -CN, -halo, -N3, -NO2, -CH = NR9, -NR9OH, -C (O) OR9, -OC (O) R9, -OC (O) OR9, -S ( O) R9, or -S (O) 2R9; each R8 is independently selected from (C1-C4) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl, -OR9, -SR9, -C (halo) 3, -CH (halo) 2, - CH2 (halo), -CN, oxo, = S, -halo, -N3, -NO2, -CH = NR9, -NR9OH, -C (O) OR9, -OC (O) R9, -OC (O) OR9 , -S (O) R9, or -S (O) 2R9; each R9 is independently selected from -H, - (C1-C6) alkyl, - (C2-C6) alkenyl, - (C2-C6) alkynyl, - (C3-C8) cycloalkyl, - (C5-C8) cycloalkenyl, - phenyl, -benzyl, -heterocycle (3 to 7 members), -C (halo) 3, -CH (halo) 2, or -CH2 (halo); each p is an integer independently selected 0 or 1; R11 is selected from -H, -C (O) OR9, -C (O) N (R6) 2 or - (C1-C4) alkyl which is not substituted or substituted with -OH, - (C1-C4) alkoxy , -N (R6) 2, -C (O) OR9, or -C (O) N (R6) 2; and each halo is independently selected from -F, -Cl, -Br, or -I, and wherein the pharmaceutically acceptable derivative is selected from the group: salt, solvate, radiolabeled, stereoisomer, enantiomer, diastereomer, other stereoisomeric form, racemic mixture , pharmaceutically acceptable geometric isomer, and / or tautomer. |
| priorityDate | 2007-01-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 1034.