http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038235-A1
Outgoing Links
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_05a203d85ee01909eaf728dc16f0f6cb |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 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/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-02 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-107 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4745 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-06 |
filingDate | 2003-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2005-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-038235-A1 |
titleOfInvention | N-SUBSTITUTED SPIROPIPERIDINE COMPOUNDS AS LIGANDS FOR ORL-1 RECEIVER |
abstract | These compounds are ligands for the ORL-1 receptor and especially are antagonists of said receptor. Claim 1: A compound of the following formula (1): or a pharmaceutically acceptable salt or solvate thereof, characterized in that R1 to R12 are independently selected from the group consisting of hydrogen; halo; hydroxy; C1-6 alkyl; C1-6 alkyl substituted with one to five halos that may be the same or different; C1-6 alkyl substituted with one to five substituents independently selected from the group consisting of hydroxy, amino, [C1-6 alkyl] NH-, [C1-6 alkyl] 2N-, H2NC (= O) -, [C1-6 alkyl ] NHC (= O) -, [C1-6 alkyl] 2NC (= O) -, C1-6 alkoxy and a fully saturated five to six membered heterocyclyl containing one to two heteroatoms independently selected from nitrogen and oxygen; C1-6 alkoxy; C1-6 alkoxy substituted with one to five halos that may be the same or different; C1-6 alkoxy substituted with one to five substituents independently selected from the group consisting of hydroxy, amino, [C1-6 alkyl] NH-, [C1-6 alkyl] 2N-, H2NC (= O) -, [C1-6 alkyl ] NHC (= O) - and [C1-6 alkyl] 2NC (= O) -; Not me; carboxy; [C1-6 alkoxy] C (= O) -; H2NC (= O) -; [C1-6 alkyl] NHC (= O) -; [C1-6 alkyl] NHC (= O) - wherein said C1-6 alkyl is substituted with a hydroxy; [C1-6 alkyl] 2NC (= O) -, [C1-6 alkyl] 2NC (= O) -, in which one or both of the C1-6 alkyl are substituted with a hydroxyl; aryl selected from phenyl and naphthyl; and a four to eight membered heterocyclyl containing one to four ring heteroatoms independently selected from nitrogen, oxygen and sulfur; or of the groups R1, R2, R3 and R4 taken together form -CH2- or - (CH2) 2-, and the two remaining groups are defined as above; X1 and X2 are independently selected from CH2; CH-hydroxy; OR; NH; S; C (= O); SO2 and [C1-6 alkyl] N; or X1 and X2 taken together form CH = CH; R13 is selected from the group consisting of hydrogen; hydroxy; C1-6 alkyl; C1-6 alkyl substituted with one to five halos that may be the same or different; and C1-6 alkyl substituted with one to five substituents independently selected from the group consisting of hydroxy, amino, [C1-6 alkyl] NH-, [C1-6 alkyl] 2N-, H2NC (= O) -, [C1- alkyl 6] NHC (= O) -, [C1-6 alkyl] 2NC (= O) -, C1-6 alkoxy and a fully saturated five to six membered heterocyclyl containing one to two heteroatoms independently selected from nitrogen and oxygen; or R12 and R13 taken together with the three ring atoms of the dihydroquinoline or tetrahydroquinoline ring that separates said substituents form a five to seven member ring that is partially or totally unsaturated, in which the ring atom not shared with the ring of dihydroquinoline or tetrahydroquinoline and adjacent to the nitrogen atom in the dihydroquinoline or tetrahydroquinoline ring is a carbon atom; the remaining one to three ring atoms not shared with the dihydroquinoline or tetrahydroquinoline ring are carbon atoms, one of said carbon atoms being optionally replaced by a nitrogen, oxygen or sulfur atom; and one or two of the carbon and nitrogen atoms not shared with the dihydroquinoline or tetrahydroquinoline ring are optionally substituted with substituents independently selected from oxo; hydroxy; C1-6 alkyl; C1-6 alkyl substituted with one to five halos that may be the same or different; C1-6 alkyl substituted with one to five substituents independently selected from the group consisting of hydroxy, amino [C1-6 alkyl] NH-, [C1-6 alkyl] 2N-, -H2NC (= O) -, [C1-6 alkyl ] NHC (= O) -, C1-6 alkoxy and a fully saturated five to six membered heterocyclyl containing one to two heteroatoms independently selected from nitrogen and oxygen; C1-6 alkoxy; C1-6 alkoxy substituted with one to five halos that may be the same or different; C1-6 alkoxy substituted with one to five substituents independently selected from the group consisting of hydroxy, amino, [C1-6 alkyl] NH-, [C1-6 alkyl] 2N-, H2NC (= O) -, [C1-6NHC alkyl (= O) - and [C1-6 alkyl] 2NC (= O) -, amino; both R14 and R15 are hydrogen or taken together form an oxo group and the dashed line represents a single or double bond. |
priorityDate | 2002-01-28-04:00^^<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: 95.