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    2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES
    5.
    发明申请
    2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES 有权
    2-苯胺-4-芳基取代的噻唑衍生物

    公开(公告)号：US20110269748A1

    公开(公告)日：2011-11-03

    申请号：US12063689

    申请日：2008-02-13

    申请人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    发明人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    IPC分类号： A61K31/426 ,  C07D417/04 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/437 ,  A61K31/429 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/5513 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/20 ,  A61P25/24 ,  C07D277/42

    CPC分类号： C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl or C1-6alkyl-O—; Het1 represents morpholinyl; pyrazolyl or imidazolyl; Het4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.

    摘要翻译： 本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z是氢，卤素，C 1-6烷基，Het 1，HO-C 1 C 1-6烷基 - ，氰基-C 1-6烷基 - ，氨基-C（= O）-C 1-6烷基 - ，甲酰基氨基-C 1-6烷基 - ，C 1-6烷基-C（= O）-NH-C 1-6烷基 - 或二（C 1-6烷基）氨基-C（= O）-C 1-6烷基 - ，苯基-C 1-6烷基 - 或Het 4 -C 1-6烷基 - ; Q是苯基，吡啶基，苯并呋喃基，2,3-二氢 - 苯并呋喃基，吡唑基，异恶唑基或吲唑基，其中每个所述环系统任选地被至多三个独立地选自卤素，氰基，C 1-6烷基， C 1-6烷基-O-，C 1-6烷硫基，Ar或多卤代C 1-6烷基; L是苯基，吡啶基，嘧唑基，8-氮杂唑基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环系可任选地被一个或两个或多个取代基取代，每个取代基独立地选自卤素，羟基，氨基，氰基，C 1 -6-烷基或C 1-6烷基-O-; Het1表示吗啉基; 吡唑基或咪唑基; Het4表示吗啉基，吡唑基或咪唑基; Ar表示任选被卤素，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基取代的苯基; 用于制备用于预防或治疗或预防精神病，智力障碍或其中α7烟碱受体的调节有益的疾病或病症的药物。

    2-aniline-4-aryl substituted thiazole derivatives
    6.
    发明授权
    2-aniline-4-aryl substituted thiazole derivatives 有权
    2-苯胺-4-芳基取代的噻唑衍生物

    公开(公告)号：US09388175B2

    公开(公告)日：2016-07-12

    申请号：US12063689

    申请日：2008-02-13

    申请人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    发明人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    IPC分类号： C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    CPC分类号： C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl or C1-6alkyl-O—; Het1 represents morpholinyl; pyrazolyl or imidazolyl; Het4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.

    摘要翻译： 本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中Z是氢，卤素，C 1-6烷基，Het 1，HO-C 1 氰基-C 1-6烷基 - ，氨基-C（= O）-C 1-6烷基 - ，甲酰基氨基-C 1-6烷基 - ，C 1-6烷基-C（= O）-NH-C 1-6烷基 - 或二（C 1-6烷基）氨基-C（= O）-C 1-6烷基 - ，苯基-C 1-6烷基 - 或Het 4 -C 1-6烷基 - ; Q是苯基，吡啶基，苯并呋喃基，2,3-二氢 - 苯并呋喃基，吡唑基，异恶唑基或吲唑基，其中每个所述环系统任选被至多三个独立地选自卤素，氰基，C 1-6烷基， C 1-6烷基-O-，C 1-6烷硫基，Ar或多卤代C 1-6烷基; L是苯基，吡啶基，嘧唑基，8-氮杂唑基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环体系可以任选地被一个或两个或多个取代基取代，每个取代基独立地选自卤素，羟基，氨基，氰基，C 1 -6-烷基或C 1-6烷基-O-; Het1表示吗啉基; 吡唑基或咪唑基; Het4表示吗啉基，吡唑基或咪唑基; Ar表示任选被卤素，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基取代的苯基; 用于制备用于预防或治疗或预防精神病，智力障碍或其中α7烟碱受体的调节有益的疾病或病症的药物。

    1,3,5-trisubstituted triazole derivative
    7.
    发明授权
    1,3,5-trisubstituted triazole derivative 有权
    1,3,5-三取代三唑衍生物

    公开(公告)号：US08404851B2

    公开(公告)日：2013-03-26

    申请号：US12738725

    申请日：2008-10-15

    申请人： Johannes Wilhelmus John F. Thuring ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    发明人： Johannes Wilhelmus John F. Thuring ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    IPC分类号： C07D401/00 ,  A61K31/44

    CPC分类号： C07D405/14

    摘要： The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

    摘要翻译： 本发明涉及2- [3-（2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基氨基）-5-（2,6-二甲基 - 吡啶-4-基） - [1,2 ，4]三唑-1-基] -N-乙基 - 乙酰胺及其类似物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。 本发明特别涉及具有增加烟碱受体激动剂功效的烟碱型乙酰胆碱受体的有效的正变构兴奋剂调节剂。

    1,3,5-TRISUBSTITUTED TRIAZOLE DERIVATIVE
    8.
    发明申请
    1,3,5-TRISUBSTITUTED TRIAZOLE DERIVATIVE 有权
    1,3,5-三唑并噻唑衍生物

    公开(公告)号：US20100240707A1

    公开(公告)日：2010-09-23

    申请号：US12738725

    申请日：2008-10-15

    申请人： Johannes Wilhelmus John F. Thuring ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    发明人： Johannes Wilhelmus John F. Thuring ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    IPC分类号： A61K31/4439 ,  C07D405/14 ,  A61P25/00 ,  A61P25/18 ,  A61P29/00

    CPC分类号： C07D405/14

    摘要： The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

    摘要翻译： 本发明涉及2- [3-（2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基氨基）-5-（2,6-二甲基 - 吡啶-4-基） - [1,2 ，4]三唑-1-基] -N-乙基 - 乙酰胺及其类似物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。 本发明特别涉及具有增加烟碱受体激动剂功效的烟碱型乙酰胆碱受体的有效的正变构兴奋剂调节剂。

    Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands
    10.
    发明授权
    Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands 有权
    放射性标记喹啉和喹啉酮衍生物及其作为代谢型谷氨酸受体配体的用途

    公开(公告)号：US07517517B2

    公开(公告)日：2009-04-14

    申请号：US10509069

    申请日：2003-03-26

    申请人： Anne Simone Josephine Lesage ,  François Paul Bischoff ,  Cornelus Gerardus Maria Janssen ,  Hilde Lavreysen

    发明人： Anne Simone Josephine Lesage ,  François Paul Bischoff ,  Cornelus Gerardus Maria Janssen ,  Hilde Lavreysen

    IPC分类号： A61K51/00 ,  A61M36/14 ,  G01N33/00

    CPC分类号： A61K51/0459 ,  A61K51/0463

    摘要： The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of of 3H, 11C and 18F. The invention also relates to their use in a diagnostic method, in particular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET.

    摘要翻译： 本发明涉及式（I-A）*或（I-B）*的放射性标记喹啉和喹啉酮衍生物，其表现出代谢型谷氨酸受体拮抗活性，特别是mGlu1受体活性及其制备; 它还涉及包含它们的组合物，以及它们用于标记和鉴定代谢型谷氨酸受体位点和成像器官的用途。 在优选的实施方案中，X表示O; R1表示C1-6烷基; 环C 3-12烷基或（环C 3-12烷基）C 1-6烷基，其中C 1-6烷基部分或环C 3-12烷基部分中的一个或多个氢原子任选地可被C 1-6烷氧基，芳基，卤代或噻吩基取代; R2表示氢; 光环; C 1-6烷基或氨基; R3和R4各自独立地表示氢或C1-6烷基; 或者R 2和R 3可以一起形成-R 2 -R 3 - ，其表示式-Z 4 -CH 2 -CH 2 -CH 2 - 或-Z 4 -CH 2 - 的二价基团，其中Z 4为O或NR 11，其中R 11为C 1 -6-烷基; 并且其中每个二价基团任选被C 1-6烷基取代; 或者R 3和R 4可以一起形成式-CH 2 -CH 2 -CH 2 -CH 2 - 的二价基团; R5代表氢; Y表示O; 芳基表示任选被卤素取代的苯基。 最优选的是放射性标记的化合物，其中放射性同位素选自3H，11C和18F。 本发明还涉及其在诊断方法中的用途，特别是用于在生物材料中标记和鉴定mGluR1受体，以及其用于成像器官，特别是使用PET的用途。