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DÉRIVÉS DE PYRIDINAMIDE EN TANT QU'ANTAGONISTES DE RÉCEPTEUR EP4
专利权人:
ROTTAPHARM S.P.A.;BUZZI, Benedetta;STASI, Luigi Piero;ROVATI, Lucio;COLACE, Fabrizio;BORRIELLO, Manuela
发明人:
BORRIELLO, Manuela,ROVATI, Lucio,STASI, Luigi Piero,BUZZI, Benedetta,COLACE, Fabrizio
申请号:
EPEP2010/069355
公开号:
WO2012/076063A1
申请日:
2010.12.10
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is -O-, -O(C1-C3 alkyl)-; -(C1-C3 alkyl)O-; -C(O)-; -C(=N-O(C1-C3 alkyl))-; -NH- or -NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, -NH(C1-C3alkyl)-; -N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is convalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid artrhritis, cancer, endometriosis and migraine.L'invention concerne un dérivé de pyridinamide de formule (I) ou un sel pharmaceutiquement acceptable de celui-ci, dans lequel R1 et R2 sont indépendamment un hydrogène, un alkyle en C1-C3 linéaire ou ramifié ou assemblés conjointement ils forment un cycle cyclopropyle; R est indépendamment choisi dans le groupe constitué d'halogènes et du trifluorométhyle et p est 1, 2
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