Invention Grant
- Patent Title: Pyridine amide derivatives as EP4 receptor antagonists
- Patent Title (中): 吡啶酰胺衍生物作为EP4受体拮抗剂
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Application No.: US13992258Application Date: 2010-12-10
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Publication No.: US08828987B2Publication Date: 2014-09-09
- Inventor: Manuela Borriello , Lucio Rovati , Luigi Piero Stasi , Benedetta Buzzi , Fabrizio Colace
- Applicant: Manuela Borriello , Lucio Rovati , Luigi Piero Stasi , Benedetta Buzzi , Fabrizio Colace
- Applicant Address: IT Monza
- Assignee: Rottapharm Biotech S.R.L.
- Current Assignee: Rottapharm Biotech S.R.L.
- Current Assignee Address: IT Monza
- Agency: Ohlandt, Greeley, Ruggiero & Perle, L.L.P.
- International Application: PCT/EP2010/069355 WO 20101210
- International Announcement: WO2012/076063 WO 20120614
- Main IPC: A61K31/00
- IPC: A61K31/00 ; C07D401/04 ; C07D401/14 ; C07D413/14

Abstract:
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 covalently 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 arthritis, cancer, endometriosis and migraine.
Public/Granted literature
- US20130261100A1 PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS Public/Granted day:2013-10-03
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