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作為EP4受體拮抗劑之吡啶醯胺衍生物
专利权人:
ROTTAPHARM S. P. A.
发明人:
BORRIELLO, MANUELA,柏瑞罗 玛丽拉,柏瑞羅 瑪麗拉,ROVATI, LUCIO,罗法堤 路西欧,羅法堤 路西歐,STASI, LUIGI PIERO,史黛西 路吉 皮罗,史黛西 路吉 皮羅,BUZZI, BENEDETTA,布基 般娜达塔,布基 般娜達塔,COLACE, FABRIZIO,寇拉斯 法柏瑞欧,寇拉斯 法柏瑞歐,柏瑞罗 玛丽拉,柏瑞羅 瑪麗拉,罗法堤 路西欧,羅法堤 路西歐,史黛西 路吉 皮罗,史黛西 路吉 皮羅,布基 般娜达塔,布基 般娜達塔,寇拉斯 法柏瑞欧,寇拉斯 法柏瑞歐
申请号:
TW100145246
公开号:
TW201307314A
申请日:
2011.12.08
申请国别(地区):
TW
年份:
2013
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 indipendently 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 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.本發明係關於式(I)吡啶醯胺衍生物或其醫藥上可接受鹽,其中R1以及R2係獨立為氫、直鏈或分支(C1-C3)烷基或一起連接而形成環丙基環;R係獨立選自由鹵素與三氟甲基組成之群且p係1、2或3;A係C或N;E係式(B)或(C)之基團,其中B係C(O)OH、C(O)O(C1-C3)烷基,以及C係選自由以下組成之群:m係1、2或3,n係0或1,W係-O-、-O(C1-C3烷基)-;-(C1-C3烷基)O-;-C(O)-;-C(=N-O(C1-C3烷基))-;-NH-或-NH(C1-C3烷基)-;Ar係苯基、視需要經1或多個選自由鹵素、三氟甲基、三氟甲氧基、甲基、-NH(C1-C3烷基)-所組成之群之取代基所取代;-N(C1-C3烷基)(C1-C3烷基)-、從5至7員雜環,其包含一個共鍵價鍵結至Ar的氮原子且需要包含1或2個選自N、O以及S的
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