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1. 发明申请

WO2012076063A1 PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡啶酰胺衍生物作为EP4受体拮抗剂
公开(公告)号：WO2012076063A1
公开(公告)日：2012-06-14
申请号：PCT/EP2010/069355
申请日：2010-12-10
申请人： ROTTAPHARM S.P.A. , BORRIELLO, Manuela , ROVATI, Lucio , STASI, Luigi Piero , BUZZI, Benedetta , COLACE, Fabrizio
发明人： BORRIELLO, Manuela , ROVATI, Lucio , STASI, Luigi Piero , BUZZI, Benedetta , COLACE, Fabrizio
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/4439 , A61P29/00
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14
摘要： The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 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.
摘要翻译：本发明涉及式（I）的吡啶酰胺衍生物或其药学上可接受的盐，其中R 1和R 2独立地为氢，直链或支链（C 1 -C 3）烷基或连接在一起形成环丙基环; R独立地选自卤素和三氟甲基，p是1,2或3; A是C或N; E是式（B）或（C）的基团，其中B是C（O）OH，C（O）O（C1-C3）烷基，C选自式（I） 1,2或3，n为0或1，W为-O - ， - O（C 1 -C 3烷基） - ; - （C 1 -C 3烷基）O-; -C（O） - ; -C（= N-O（C 1 -C 3烷基）） - ; -NH-或-NH（C 1 -C 3烷基） - ; Ar是任选被一个或多个选自卤素，三氟甲基，三氟甲氧基，甲基，-NH（C 1 -C 3烷基） - 的取代基取代的苯基。 -N（C 1 -C 3烷基）（C 1 -C 3烷基） - ，含有一个与Ar共价结合的氮原子的5至7元杂环，并任选地含有一个或两个选自N，O和S的杂原子; 和含有1至3个选自S，O e N的杂原子的5或6元杂芳环，所述杂芳环被一个或两个选自（C 1 -C 3）烷基，（C 3 -C 5））环烷基氧基，（C1-C3）烷基羰基。本发明的化合物可用于制备用于治疗需要使用EP4受体拮抗剂的病症的药物，例如治疗急性和慢性疼痛，炎性疼痛，骨关节炎，炎症相关疾病作为关节炎，类风湿性肾炎，癌症，子宫内膜异位症和偏头痛。

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