会员体验
专利管家（专利管理）
工作空间（专利管理）
风险监控（情报监控）
数据分析（专利分析）
侵权分析（诉讼无效）
联系我们
交流群
官方交流：
QQ群： 891211   
微信请扫码    >>>
现在联系顾问~
下载
著录项
PDF全文
热词
    • 71. 发明专利
      NZ520484A Substituted arylpyrazines that are modulators of CRF (corticotropin releasing factor) receptor and methods of treatment using them 未知
    • Substituted arylpyrazines that are modulators of CRF (corticotropin releasing factor) receptor and methods of treatment using them
    • NZ520484A
    • 2005-03-24
    • NZ52048401
    • 2001-02-16
    • NEUROGEN CORP
    • YOON TAEYOUNG , GE PING , HORVATH RAYMOND F , DE LOMBAERT STEPHANE , HODGETTS KEVIN J , DOLLER DARIO , ZHANG CUNYU
    • A61K31/4965 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P9/10 , A61P9/12 , A61P15/00 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D241/00 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D403/06 , C07D401/06 , A61K31/497 , A61K31/5355 , A61P3/04
    • Compounds of Formula I which bind with high selectivity and/or affinity to CRF1 receptors (Corticotropin Releasing Factor type 1 Receptors) are described wherein: R1 is selected from H, C1-4alkyl, C2-4alkenyl, C2-4 alkynyl, halogen, trifluoromethyl, trifluoromethoxy, -NH(C1-4alkyl), - N(C1-4alkyl)(C1-4 alkyl), -O(C1-4alkyl), and S (O)n(C1-4alkyl); R2 is selected from -XRA and Y, wherein-X, RA, and Y are defined below; and with the proviso that R2 is not -NH2; R3 is selected from the group consisting of hydrogen, halogen, C1-4alkyl , -O(C1-4alkyl), NH(C1-4alkyl), -N(C1- 4alkyl)(C1-4alkyl), and-S (O)n(C1-4alkyl), haloalkyl, trifluoromethyl, trifluoromethoxy, -XRA and Y; R4 is absent or an oxygen atom; Ar is phenyl, mono-, di-, or tri-substituted with RC, or Ar is selected from naphthyl, pyridyl, pyridonyl, pyrimidinyl, and thiophenyl, each of which is unsubstituted or mono-, di-, or tri-substituted with RC; with the proviso that if Ar is phenyl substituted with halogen, napthyl, or naphthyl substituted with halogen, then the compounds where R3 is hydrogen are excluded; RA and RB which may be the same or different, are selected from hydrogen and straight, branched, or cyclic alkyl groups consisting of 1 to 8 carbon atoms, which may contain one or more double or triple bonds, each of which may be further substituted with one or more substituent(s) selected from oxo, hydroxy, halogen, -O(C1-4alkyl), -NH(C1-4alkyl), -N(C1- 4alkyl)(C1-4alkyl), -NHC(O)(C1-4alkyl), -N(C1-4alkyl)C(=O)(C1-4alkyl), -NHS(O)n(C1-4 alkyl), -S(O)n(C1-4alkyl), - S(O)nNH(C1-4alkyl), -S(O)nN(C1-4alkyl)(C1-4alkyl), and Z; RC is selected from halogen, cyano, haloalkyl, trifluoromethyl, trifluoromethoxy, hydroxy, amino, and C1-6alkyl optionally substituted with 0-2 RD, C2-6alkenyl substituted with 0-2 RD, C1-4alkynyl substituted with 0-2 RD, C3-7cycloalkyl substituted with 0-2RD, (C3-7cycloalkyl)C1-4 alkyl substituted with 0-2 RD, -O(C1-4alkyl) substituted with 0-2 RD, -NH (C1-4alkyl) substituted with 0-2 RD, -N(C1-4alkyl)(C1-4 alkyl) each independently substituted with 0-2 RD, -XRA, and Y; RD is selected from halogen, hydroxy, cyano, C1-4alkyl, -O(C1-4alkyl), -NH(C1-4alkyl), -N(C1-4alkyl)(C1-4alkyl), morpholino, pyrrolidino, piperidino, thiomorpholino, piperazino, 4 hydroxypiperidino, -S(O)n(C1-4alkyl), trifluoromethyl, trifluoromethoxy, CO(C1-4alkyl), CONH(C1-4alkyl), CON(C1-4alkyl)(C1-4alkyl), -XRA, and Y; X is from -CH2-, -CHRB-, -O-, -C(=O)-, -C(=O)O-, -S(O)n-, -NH-, -NRB-, -C(=O)NH-, -C(=O)NRB-, -S(O)nNH-, - S(O)nNRB-, -OC(=S)S-, -NHC(=O)-, -NRBC(=O)-, -NHS(O)n-, OSiH, (C1-4alkyl)2-n-, and -NRBS(O)n-; Y and Z are independently selected at each occurrence from the group consisting of : 3- to 7- membered carbocyclic and heterocyclic groups, which are saturated, unsaturated, or aromatic, which may be substituted with one or more substituents selected from halogen, haloalkyl, oxo, hydroxy, amino, C1-4alkyl, -O(C1-4 alkyl), NH(C1-4alkyl), -N(C1- 4alkyl) (C1-4alkyl), and-S(O)n(C1-4alkyl), and said 3-to 7-membered heterocyclic groups contain one or more heteroatom(s) selected from N, O, and S, with the point of attachment being either carbon or nitrogen; n is selected from 0, 1, and 2. The compounds can be used in the pharmaceutical composition for treating anxiety disorder, stress-related disorders and eating disorders and used in methods for localizing CRF receptors in tissue section samples.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
每页展示10个专利
每页展示10个专利
每页展示20个专利
每页展示50个专利
每页展示100个专利

IPRDB

最新中国发明专利 最新美国发明专利 技术领域 专利库 专利分类库 国际专利分类库

热门服务

会员版试用 API 数据接口 找代理 知嘟嘟专利交易 排行榜 大学排行榜 专利百科

关于我们

平台介绍 战略合作 网站地图

友情链接

知嘟嘟专利交易 国家知识产权局 中国商标网

联系方式


©2019-2023 上海吉码数字技术有限公司 版权所有，并保留所有权利 沪ICP备20016256号-6 沪公网安备31011702005475号