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    PROCESS FOR THE PRODUCTION OF SUBSTITUTED 2-[2-(PHENYL) ETHYLAMINO]ALKANEAMIDE DERIVATIVES
    6.
    发明申请
    PROCESS FOR THE PRODUCTION OF SUBSTITUTED 2-[2-(PHENYL) ETHYLAMINO]ALKANEAMIDE DERIVATIVES 审中-公开

    公开(公告)号：WO2020212352A1

    公开(公告)日：2020-10-22

    申请号：PCT/EP2020/060470

    申请日：2020-04-14

    Applicant: NEWRON PHARMACEUTICALS S.P.A.

    Inventor： LEONG, William ,  LAN, Dongxiao ,  ZHANG, Weifang ,  FANG, Xiang ,  WU, Sizhong

    IPC: C07C237/06 ,  C07C231/12 ,  C07C41/30

    Abstract: The present invention refers to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R is (C 3 -C 10 )alkyl, or ω-trifluoro(C 3 -C 10 )alkyl; R 1 and R 2 are, independently, hydrogen, hydroxy, (C 1 -C 8 ) alkoxy, (C 1 -C 8 ) alkylthio, halo, trifluoromethyl or 2,2,2-trifluoroethyl; or one of R 1 and R 2 is in ortho position to the R-O- group and, taken together with the same R-O-, represents a Formula (A) group where R o is (C 2 -C 9 )alkyl; R 3 and R 4 are, independently, hydrogen, (C 1 -C 4 )alkyl; or R 4 is hydrogen and R 5 is a group selected from -CH 2 -OH, -CH 2 -O-(C 1 -C 6 )alkyl, -CH(CH 3 )-OH, -(CH 2 ) 2 -S-CH 3 , benzyl and 4-hydroxybenzyl; or R 4 and R 5 , taken together with the adjacent carbon atom, form a (C 3 -C 6 )cycloalkyl residue; R 5 and R 6 are independently hydrogen or (C 1 -C 6 )alkyl; or taken together with the adjacent nitrogen atom form a 5-6 membered monocyclic saturated heterocycle, optionally containing one additional heteroatom chosen among -O-, -S- and -NR 7 - where R 7 is hydrogen or (C 1 -C 6 ) alkyl; and wherein optionally one or more hydrogen atom in the groups R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 , preferably in the R group, can be substituted by a deuterium atom.

    FLUORINATED AMIDE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS
    9.
    发明申请
    FLUORINATED AMIDE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS 审中-公开
    氟化酰胺衍生物及其作为治疗剂的用途

    公开(公告)号：WO2017070795A1

    公开(公告)日：2017-05-04

    申请号：PCT/CA2016/051260

    申请日：2016-10-31

    Applicant: TRILLIUM THERAPEUTICS INC.

    Inventor： SLASSI, Abdelmalik

    IPC: C07C235/20 ,  A61K31/165 ,  A61P25/00 ,  C07C237/06

    CPC classification number: C07C237/06 ,  C07B2200/07 ,  C07C235/20

    Abstract: The present application relates to novel fluorinated amide derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain and other related CNS disorders.

    Abstract translation: 本申请涉及式（I）的新型氟化酰胺衍生物，制备它们的方法，含有它们的药物组合物及其在治疗或预防急性和/或慢性神经疾病中的用途 如精神病，癫痫，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷，以及慢性和急性疼痛以及其他相关的CNS疾病。

    NEW SUBSTITUTED ETHYLENE-DIAMINE-TETRAACETIC-ACID-BIS(AMIDE) DERIVATIVES AND USE THEREOF AS LIGAND CONTAINING MN (II) OF MRI CONTRAST AGENT
    10.
    发明申请
    NEW SUBSTITUTED ETHYLENE-DIAMINE-TETRAACETIC-ACID-BIS(AMIDE) DERIVATIVES AND USE THEREOF AS LIGAND CONTAINING MN (II) OF MRI CONTRAST AGENT 审中-公开
    新替代的乙烯 - 二胺 - 四氨基酸（酰胺）衍生物及其作为含有MRI对比剂的MN（II）的配体的用途

    公开(公告)号：WO2016135523A1

    公开(公告)日：2016-09-01

    申请号：PCT/HU2015/000074

    申请日：2015-11-23

    Applicant: DEBRECENI EGYETEM

    Inventor： BARANYAI, Zsolt ,  GARDA, Zoltán ,  KÁLMÁN, Ferenc, Krisztián ,  KRUSPER, László ,  TIRCSÓ, Gyula ,  TÓTH, Imre

    IPC: C07D401/12 ,  C07C237/06

    CPC classification number: A61K49/106 ,  A61B5/055 ,  A61B2503/40 ,  A61K49/103 ,  C07C237/06 ,  C07D207/325 ,  C07D207/34 ,  C07D211/16 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/62 ,  C07D221/22 ,  C07D295/185 ,  C07D295/192 ,  C07D401/12 ,  C07D403/12 ,  C07D471/08 ,  C07D491/107 ,  G01N24/08 ,  G01N33/58

    Abstract: The subject of the invention is the compounds of the formula (I) their isomers, their physiologically acceptable salts and/or their Mn(II) complexes wherein the formula (I) R 1 and R 2 are jointly unsaturated or aromatic rings of 5 to 7 carbon atoms together with the enclosed ethylene group and R 3 and R 4 are jointly saturated, unsaturated or aromatic rings of 5 to 7 members together with the connecting N atom, in given case optionally substituted with alkyl group of 1 to 4 carbon atoms, carboxyl, nitro, amino groups or phenyl-alkyl group of 1 to 4 carbon atoms, which can be optionally in given case substituted with carboxyl, nitro or amino group in its phenyl part, or R 1 and R 2 are jointly saturated ring of 5 to 7 carbon atoms together with the enclosed ethylene group R 3 and R 4 are jointly saturated, unsaturated or aromatic ring of 5 to 7 members together with the connecting atom N, substituted with alkyl group of 1 to 4 carbon atoms, carboxyl, nitro or amino group or phenyl-alkyl group of 1 to 4 carbon atoms, which can be optionally substituted with carboxyl, nitro or amino group in its phenyl part, or R 1 and R 2 are jointly saturated, unsaturated or aromatic ring of 5 to 7 carbon atoms together with the enclosed ethylene group, R 3 is hydrogen atom and R 4 is alkyl group of 2 to 6 carbon atoms with straight or branching open carbon chain. The subject of the invention is the MRI diagnostic agents as well, which are containing the above compounds.

    Abstract translation: 本发明的主题是式（I）化合物的异构体，其生理学上可接受的盐和/或其Mn（II）络合物，其中式（I）R 1和R 2是5至7个碳的共同不饱和或芳环 原子与封闭的亚乙基一起，R3和R4是连接的N原子在连接的N原子上连接的5至7个成员的共同饱和的，不饱和的或芳香环，在任何情况下任选被1-4个碳原子的烷基取代，羧基，硝基， 氨基或1至4个碳原子的苯基 - 烷基，其任选地在一定的情况下在其苯基部分被羧基，硝基或氨基取代，或者R1和R2是5至7个碳原子的共同饱和环，连同 封闭的亚乙基R3和R4是与连接原子N一起为5-7个的连续的饱和，不饱和或芳环，被1-4个碳原子的烷基，羧基，硝基或氨基或苯基 - 烷基取代 可以在其苯基部分任选被羧基，硝基或氨基取代，或者R1和R2是带有5至7个碳原子的饱和的，不饱和的或芳族的环与封闭的亚乙基，R3 是氢原子，R4是具有2-6个碳原子的直链或支链开链碳链的烷基。 本发明的主题也是含有上述化合物的MRI诊断剂。

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