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Derivatives of N - arilmetilo sulfonamide as negative modulators of NR2A

机译:N-阿里美洛磺酰胺作为N​​R2A负调节剂的衍生物

摘要

Compounds that selectively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are described. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, tautomer or stereoisomer thereof where: A, B, C and D are independently CR or N provided that at least one A, B, C or D is N; each R is independently selected from the group consisting of H, halogen, C₁₋₅-alkyl,haloalkyl C₁₋₅,CN and O-alkyl; or when both A and B are CR, the R groups in A and B can form, with A and B, a 5,6 or 6,6 bicyclic aryl group or heteroaryl group; R¹ is aryl or heteroaryl both are optionally substituted with one or more substituents which are selected from the group consisting of halogen, C₁₋₅ alkyl,alquilo -C (O) Chaloalkyl, CN, O-aryl, O-alkyl, aryl, and heteroaryl; or R¹ is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R² and R² are independently selected from the group consisting of H, and C₁₋₅ alkyl;O r 2 and R 2 can form a bicycle with the carbon they are connected to; X is equal to or equal to C;And selected from group H, lessor c83318325;And a group - A,P¹ is selected from the group consisting of H, and C₁₋₅ alkyl;P² is alkyl O (C₁₋₅) optionally substituted with one or more hydroxy and / or alkoxy groups; or P² is selected from the group consisting of OC (O) R⁴,OC (O) OROC (O) NHROC (O) NR ROC (O) -alquilo-NR Ry O (PO) OOr P1 and P2,they form a cycloalkyl or a heterocycle; R⁴ and R⁵ are independently selected from the group consisting of H, and C₁₋₅ alkyl with the proviso that when P² is OC (O) OR⁴,R830808 is not hydrogen, R3 is - l1-ar1,L¹-N (C₁₋₆ alkyl) ₂,Or other formula (2);1 l83216c83318325 is a linear or separable tar replaced by - Oh, tar - oc832183316c8332625;it is life.Z selected from lease group H and c.83218c833183258t;Or Z and R3,with the nitrogen to which they are connected they can form a heterocycle; Ar¹ is aryl optionally substituted with one or more substituents selected from the group consisting of C₁₋₅ alkyl,Halogen, halogen c83217c83183226,n. And o-rent; or AR1 is an optional heterosexual, replaced by one or more alternatives selected from the c833213125 rental group;Halogen, halogen c83217c83183226,1 Two, two, three, three
机译:描述了选择性调节含有NR2A亚基的NMDA受体的化合物,包含该化合物的药物组合物以及使用该化合物治疗疾病的方法。 1.式(1)的化合物或其药学上可接受的盐,前药,溶剂化物,水合物,互变异构体或立体异构体,其中:A,B,C和D独立地为CR或N,条件是至少一个A,B,C或D是N;每个R独立地选自H,卤素,C 1-8烷基,卤代烷基C 4,CN和O-烷基。或者,当A和B都为CR时,A和B中的R基团可以与A和B形成5,6或6,6双环芳基或杂芳基。 R 1是芳基或杂芳基,两者都任选地被一个或多个选自卤素,C 1-4烷基,-C(O)卤代烷基,CN,O-芳基,O-烷基,芳基和杂芳基R 1选自任选取代的烷基,任选取代的环烷基或任选取代的杂环烷基;或R 2和R 2独立地选自H和C 1-4烷基; O r 2和R 2可以与它们相连的碳形成自行车; X等于或等于C;并且选自H基团,出租人为c83318325;并且基团-A,P 1选自H和C 1-6烷基; P 2任选为烷基O(C 1-4)被一个或多个羟基和/或烷氧基取代;或P 2选自由OC(O)R 4,OC(O)OROC(O)NHROC(O)NR ROC(O)-alquilo-NR Ry​​ O(PO)O或P1和P2组成的组,它们形成环烷基或杂环; R 5和R 5独立地选自H和C 1-8烷基,条件是当P 2是OC(O)OR 3时,R 830808不是氢,R 3是-l 1 -ar 1,L 1 -N(C 5)。烷基)2或其他式(2); 1 l83216c83318325是线性或可分离的焦油,由-哦,焦油-oc832183316c8332625取代;它是life.Z,选自租赁组H和c.83218c833183258t;或Z和R3,其中它们所连接的氮可以形成杂环; Ar 1是任选地被一个或多个选自C 1-4烷基,卤素,卤素c83217c83183226,n的取代基取代的芳基。还有租金或AR1是可选的异性恋,被c833213125租赁组中的一个或多个替代物替代;卤素,卤素c83217c83183226,1两个,两个,三个,三个

著录项

  • 公开/公告号AR097795A1

    专利类型

  • 公开/公告日2016-04-13

    原文格式PDF

  • 申请/专利权人 MNEMOSYNE PHARMACEUTICALS INC.;

    申请/专利号AR2014P103585

  • 发明设计人 DAVID R. ANDERSON;ROBERT A. VOLKMANN;

    申请日2014-09-26

  • 分类号C07D213/81;A61K31/44;A61K31/4436;A61K31/4439;A61K31/444;A61K31/4965;A61K31/497;A61K31/501;A61K31/506;A61P25/28;C07D237/24;C07D241/24;C07D401/12;C07D403/12;C07D405/12;C07D409/12;C07D413/12;C07D417/12;C07D417/14;

  • 国家 AR

  • 入库时间 2022-08-21 14:27:39

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