http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-059026-A1
Outgoing Links
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| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_757c3a30eee57315f364b0563b0ecea6 |
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| filingDate | 2006-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-03-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-059026-A1 |
| titleOfInvention | TRIAZOLIC DERIVATIVES AS LEGAL ANALOGS OF GHRELINA RECEPTORS OF THE HORMONE SECRETAGOGOS OF PHARMACEUTICAL COMPOSITIONS. |
| abstract | Triazolic derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (1) that are useful in the treatment or prophylaxis of physiological and / or pathophysiological conditions in mammals, preferably human, which are mediated by GHS receptors In addition GHS receptor antagonists and agonists that can be used for the modulation of these receptors and are useful for treating the above conditions, in particular growth retardation, cachexia, short, medium and / or long term regulation of energy balance; short, medium and / or long term regulation (stimulation and / or inhibition) of food intake; adipogenesis, adiposity and / or obesity; increase and / or reduction of body weight; diabetes, type I diabetes, type II diabetes, tumor cell proliferation; inflammation, inflammatory effects, post-operative gastric ileus, post-operative ileus and / or gasterectomy (ghrelin replacement therapy) ö. Claim 1: The use of a compound according to formula (1) wherein R1 and R2 are independently selected from each other, from the group consisting of hydrogen atom, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl , heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, alkylsulfonyl, arylsulfonyl, arylalkyl sulfonylö which are optionally substituted in the alkyl group, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, substituted by 3-heterocyclyl independently of the group consisting of ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, - OH, -NO2, alkyl, aryl, arylalkyl, -O-alkyl, -O- aryl, -O-arylalkyl; and preferably are selected from the group consisting of "alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl" optionally are substituted by up to 3 substituents independently selected from the group consisting of "halogen, -F, -CI, -Br, -I , -N3, -CN, -NR7R8, -OH, -NO2, alkyl, aryl, arylalkyl, -O-alkyl, -O-aryl, -O-arylalkyl; one of the radicals R3 and R4 is a hydrogen atom, while the other radical is selected from the group consisting of hydrogen atom, alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -alkyl-O-aryl, -alkyl-O-arylalkyl, -alkyl-O-heteroaryl, -alkyl-O-heteroarylalkyl, -alkyl-O-heterocyclyl, alkyl-O-heterocyclylalkyl, -alkyl-CO-aryl, -alkyl-CO-arylalkyl, alkyl- CO-heteroaryl, alkyl-CO-heteroarylalkyl, -alkyl-CO-heterocyclyl, -alkyl-CO-heterocyclylalkyl, - alkyl-C (O) O-aryl, -alkyl-C (O) O-arylalkyl, -alkyl-C (O) O-heteroaryl, -alkyl-C (O) O-heteroarylalkyl, -alkyl-C (O) O-heterocyclyl, alkyl-C (O) O-heterocyclylalkyl, -alkyl-CO-NH2, - alkyl-CO -OH, -alkyl-NH2, -alkyl-NH-C (NH) -NH2, alkylsulfonyl, arylsulfonyl, arylalkyl sulfonyl, alkyl-S-alkyl, alkyl-S-Hö which are optionally substituted in the aryl, heteroaryl group, arylalkyl, heteroarylalkyl, heterocyclyl and / or heterocyclic lilalkyl for up to 3 substituents independently selected from the group consisting of ôhalogen, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alkyl, aryl, arylalkyl, - O-alkyl, -O-aryl, -O-arylalkyl and are preferably selected from the group consisting of ôarylalkyl, heteroarylalkyl, heterocyclylalkyl, -alkyl-O-aryl, -alkyl-O-arylalkyl, -alkyl-O-heteroaryl, -alkyl-O-heteroarylalkyl, -alkyl-O-heterocyclyl, alkyl-O-heterocyclylalkyl, -alkyl-CO-aryl, -alkyl-CO-arylalkyl, alkyl-CO-heteroariIo, alkyl-CO-heteroarylalkyl, -alkyl-CO -heterocyclyl, -alkyl-CO-heterocyclylalkyl, -alkyl-C (O) O-aryl, -alkyl-C (O) O-arylalkyl, -alkyl-C (O) O-heteroaryl, -alkyl-C (O) O-heteroarylalkyl, -alkyl-C (O) O-heterocyclyl, alkyl-C (O) O-heterocyclylalkyl, -alkyl-CO-NH2, - alkyl-CO-OH, -alkyl-NH2, -alkyl-NH-C (NH) -NH2ö, optionally substituted in the group aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and / or heterocyclylalkyl by up to 3 substituents independently selected from the group consisting of ôhalogen, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alkyl, aryl, arylalkyl, - O-alkyl, -O-aryl, -O-arylalkyl; R5 is selected from the group consisting of hydrogen atom, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -CO-alkyl, -CO-cycloalkyl, -CO-cycloalkylalkyl, -CO-aryl, -CO-arylalkyl, -CO-heteroaryl, -CO-heteroarylalkyl, -CO-heterocyclyl, -CO-heterocyclylalkyl, -CO-C * (R9R10) -NH2, -CO-CH2-C * (R9R10) -NH2, - CO-C * (R9R10) -CH2-NH2, alkylsulfonyl, arylsulfonyl, arylalkylsulfonylö which are optionally substituted by up to 3 substituents independently selected from the group consisting of ôhalogen, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alkyl, aryl, arylalkyl, -O-alkyl, -O-aryl, -O-arylalkyl, and preferably selected from the group consisting of hydrogen atom, - CO-alkyl, -CO-cycloalkyl, -CO-aryl, -CO-heteroaryl, -CO-arylalkyl, -CO- heteroarylalkyl, -CO-heterocyclyl, -CO-C * (R9R10) -NH2, -CO-CH2- C * (R9R10) -NH2, -CO-C * (R9R10) -CH2 -NH2, are optionally substituted by up to 3 substituents independently selected from the group consisting of ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alkyl, aryl, arylalkyl, -O-alkyl, -O-aryl, -O-arylalkyl; R6 is selected from the group consisting of hydrogen atom, alkyl, cycloalkyl, cycloalkylalkyl, and preferably is a hydrogen atom; R7 and R8 are independently selected from each other from the group consisting of ô H atom, alkyl, cycloalkyl, cycloalkylalkyl ′ and preferably are an H atom; R9 and R10 are selected, independently from each other, from the group consisting of hydrogen atom, alkyl, natural alpha-amino acid side chain, non-natural alpha-amino acid side chain, and are preferably selected from the group consisting of hydrogen atom, alkyl; m is 0, 1 or 2 and preferably is 0; and * means a carbon atom of R or S configuration when it is chiral; for the manufacture of a medicament for the treatment or prophylaxis of physiological and / or pathophysiological conditions in mammals that are mediated by GHS receptors. |
| priorityDate | 2005-08-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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