http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-039971-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5dfc0b033ac4c841466d97a5f28ea32b |
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| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D235-10 |
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| filingDate | 2003-05-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-039971-A1 |
| titleOfInvention | BENZOIMIDAZOL DERIVATIVES ANTAGONISTS OF THE NOCICEPTINE UNION WITH THE ENT RECEIVER1 |
| abstract | These compounds have a high affinity for nociceptin receptors and therefore inhibit the action of nociceptin and are useful as analgesics, as an anti-obesity medication, as an agent to improve brain function, as agents for the treatment of Alzheimer's disease. and dementia, and as therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like. Claim 1: Benzoimidazole derivatives which are represented by a general formula (1) in which X is equivalent to H or halogen, B is equivalent to halogen, cyano or optionally lower alkyl substituted with F; D is equivalent to a group selected from a group consisting of the following formulas (2), (3) and (4) in which R1 is equivalent to H or a lower alkyl which may be optionally substituted with at least one substituent selected from the group consisting of halogen, hydroxyl, lower alkyloxy and lower cycloalkyl; R2 may be the same or different when m1 is 2, which bind to optional carbon atom (s) in the aliphatic heterocyclic ring containing N D1, D2 or D3, and equivalent to a lower alkyl that may be optionally substituted with a substituent selected from a group consisting of halogen, hydroxyl, lower alkyloxy optionally substituted with F, lower alkylcarbonyl, carboxyl, lower alkyloxycarbonyl, carbamoyl, lower mono-alkylcarbamoyl and di-lower alkylcarbamoyl or R1 and R2 together form a C2-4 alkylene, said alkylene being optionally substituted by a substituent selected from a group consisting of halogen, hydroxy, lower alkyloxy, lower cycloalkyl, lower alkylcarbonyl, lower mono-alkylcarbamoyl and lower di-alkylcarbamoyl; m1 is 0 or an integer of value 1 or 2; E equals a junction bridge, -NR- or -O-, where R equals H, methyl or ethyl, formula (5) is equivalent to a 5- to 10-membered mono- or dicyclic aliphatic heterocyclic ring containing N , which has two atoms of N; formulas (6) and (7) each equals a 3- to 10-membered mono- or dicyclic aliphatic heterocyclic ring containing N, which has an N atom; G is equivalent to a group represented by a formula (8) in which a is 0 or 1 ;. R3 is equivalent to H, a substituent selected from a group consisting of list a, or a lower alkyl that may be optionally substituted with a substituent selected from the group consisting of the same list a. R4 and R5 may be the same or different, and each equals H, a substituent selected from the group consisting of the list a, or a lower alkyl or lower cycloalkyl which may be optionally substituted with a substituent selected from the group consisting of the list a, or R4 and R5 together form, in combination with the C atom with which they are attached, an alicyclic group of 3 to 10 members that optionally presents a heteroatom selected from the group consisting of N and O, of the formula (9) in which b is 0 or an integer of value 1-4; R8 may be the same or different when b is 2-4, and bind to an optional atom (s) in the aliphatic ring, each being equivalent to a substituent selected from the group consisting of the list a or a lower alkyl that it may be optionally substituted with a substituent selected from the group consisting of the list a, or two R8 together form -NH-C (O) -O-CH2-, or an oxo group, Y1 equals -CH2-, -NR9- or -O-, when R9 is equivalent to a substituent selected from the group consisting of H, lower alkyl optionally substituted with F, lower alkylcarbonyl, lower alkyloxycarbonyl, lower alkylsulfonyl, carbamoyl, lower mono-alkylcarbamoyl and lower dialkylcarbamoyl; [list a] halogen, hydroxy, amino, lower mono-alkylamino, lower dialkylamino, lower alkyloxy optionally substituted with F, lower alkyloxycarbonyl, (alkyloxycarbonyl) lower amino, (lower alkyloxycarbonyl) lower alkylamino, carboxyl, lower alkylcarbonyl, lower alkylcarbonyloxy, ( lower alkylcarbonyl) lower amino, (lower alkylcarbonyl) lower alkylamino, carbamoyl, lower mono-lower alkylcarbamoyl, lower dialkylcarbamoyl, carbamoylamino, lower mono-lower alkylcarbamoylamino, di-lower alkylcarbamoylamino, (lower mono-lower alkylcarbamoyl) lower alkylamino, (di-lower alkylcarbamoyl) lower, carbamoyloxy, lower mono-alkylcarbamoyloxy, lower di-alkylcarbamoyloxy, lower alkylsulfonyl, lower alkylsulfonylamino, sulfamoyl, mono-lower alkylsulfamoyl, lower di-alkylsulfamoyl, sulfamoylamino, (lower mono-alkylsulfamoyl) amino, (di-alkylsulfamoyl) lower amino, (lower mono-alkylsulfamoyl) lower alkylamino, (di-lower alkylsulfamoyl) lower alkylamino, phenyl which may be optionally substituted with lower alkyl, and tetrazolyl or oxadiazolyl which may optionally be substituted with lower alkyl; or its salts acceptable for pharmaceutical use. |
| priorityDate | 2002-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 124.