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    PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
    2.
    发明申请
    PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 有权
    吡啶酰胺衍生物作为EP4受体拮抗剂

    公开(公告)号：US20130261100A1

    公开(公告)日：2013-10-03

    申请号：US13992258

    申请日：2010-12-10

    申请人： Manuela Borriello ,  Lucio Rovati ,  Luigi Piero Stasi ,  Benedetta Buzzi ,  Fabrizio Colace

    发明人： Manuela Borriello ,  Lucio Rovati ,  Luigi Piero Stasi ,  Benedetta Buzzi ,  Fabrizio Colace

    IPC分类号： C07D413/14 ,  C07D401/14 ,  C07D401/04

    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 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.

    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） - ，含有一个氮原子的5至7元杂环，其与Ar共价键合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 ，类风湿性关节炎，癌症，子宫内膜异位症和偏头痛。

    CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS
    3.
    发明申请
    CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS 有权
    循环胺衍生物作为EP4受体激动剂

    公开(公告)号：US20140243373A1

    公开(公告)日：2014-08-28

    申请号：US14127474

    申请日：2011-07-04

    申请人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    发明人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    IPC分类号： C07F1/02

    CPC分类号： C07F1/02 ,  C07D207/16 ,  C07D211/60

    摘要： There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity.Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity.The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.

    摘要翻译： 描述了一组具有EP4受体激动活性的新型环胺衍生物化合物。 具体地说，根据本发明的化合物具有镇痛，抗炎，抗青光眼活性，并具有抗骨质疏松和抗溃疡活性。 因此，本发明涉及新型环胺衍生物化合物，其制备方法，含有它们的药物组合物及其作为药物的用途，特别是用于治疗或缓解前列腺素E介导的疾病如疼痛，青光眼，溃疡性结肠炎和骨质疏松症。

    Pyridine amide derivatives as EP4 receptor antagonists
    6.
    发明授权
    Pyridine amide derivatives as EP4 receptor antagonists 有权
    吡啶酰胺衍生物作为EP4受体拮抗剂

    公开(公告)号：US08828987B2

    公开(公告)日：2014-09-09

    申请号：US13992258

    申请日：2010-12-10

    申请人： Manuela Borriello ,  Lucio Rovati ,  Luigi Piero Stasi ,  Benedetta Buzzi ,  Fabrizio Colace

    发明人： Manuela Borriello ,  Lucio Rovati ,  Luigi Piero Stasi ,  Benedetta Buzzi ,  Fabrizio Colace

    IPC分类号： A61K31/00 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

    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 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.

    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） - ，含有一个氮原子的5至7元杂环，其与Ar共价键合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 ，类风湿性关节炎，癌症，子宫内膜异位症和偏头痛。

    Cyclic amine derivatives as EP4 receptor agonists
    8.
    发明授权
    Cyclic amine derivatives as EP4 receptor agonists 有权
    环胺衍生物作为EP4受体激动剂

    公开(公告)号：US09120824B2

    公开(公告)日：2015-09-01

    申请号：US14127474

    申请日：2011-07-04

    申请人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    发明人： Manuela Borriello ,  Sabrina Pucci ,  Luigi Piero Stasi ,  Lucio Rovati

    IPC分类号： C07F1/02 ,  C07D207/16 ,  C07D211/60

    CPC分类号： C07F1/02 ,  C07D207/16 ,  C07D211/60

    摘要： There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity.Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity.The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.

    摘要翻译： 描述了一组具有EP4受体激动活性的新型环胺衍生物化合物。 具体地说，根据本发明的化合物具有镇痛，抗炎，抗青光眼活性，并具有抗骨质疏松和抗溃疡活性。 因此，本发明涉及新型环胺衍生物化合物，其制备方法，含有它们的药物组合物及其作为药物的用途，特别是用于治疗或缓解前列腺素E介导的疾病如疼痛，青光眼，溃疡性结肠炎和骨质疏松症。

    Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction
    10.
    发明授权
    Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction 有权
    适用于治疗睡眠障碍和药物成瘾的螺状氨基化合物

    公开(公告)号：US08859608B2

    公开(公告)日：2014-10-14

    申请号：US13384166

    申请日：2010-07-15

    申请人： Luigi Piero Stasi ,  Lucio Rovati

    发明人： Luigi Piero Stasi ,  Lucio Rovati

    IPC分类号： A61K31/40 ,  A61K31/44 ,  C07D221/00 ,  C07D209/54 ,  C07D417/14 ,  C07D417/06 ,  C07D401/14 ,  C07D401/12

    CPC分类号： C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06

    摘要： A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式（VI）的螺氨基化合物，其中m为1或2或3，n为1或2，R选自5或6元芳族环和5或6元杂芳族环，其包含1 至3个选自S，O和N的杂原子，该环被一个或两个选自（C 1 -C 3）烷基，卤素，（C 3 -C 5）环烷氧基，（C 1 -C 3）烷基羰基，苯基 任选地被一个或多个卤素原子取代，包含至少一个氮原子的5-或6-元杂环; P是取代基Q或COQ，其中Q选自苯基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹喔啉基，苯并呋喃基，咪唑并三唑基，其任选地被一个或多个选自以下的取代基取代：（ C 1 -C 3）烷基，卤素，三氟甲基，碳酰氨基，甲基氨基甲酰基，羧基，甲基羧基或其药学上可接受的盐。