Spirocyclic NK1 antagonists I:: [4.5] and [5.5]-spiroketals

被引：25
|
作者：
Seward, EM
Carlson, E
Harrison, T
Haworth, KE
Herbert, R
Kelleher, FJ
Kurtz, MM
Moseley, J
Owen, SN
Owens, AP
Sadowski, SJ
Swain, CJ
Williams, BJ
机构：
[1] Merck Sharp & Dohme Res Labs, Dept Med Chem, Ctr Res Neurosci, Harlow, Essex, England
[2] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Ctr Res Neurosci, Harlow, Essex, England
[3] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期
关键词：
D O I：
10.1016/S0960-894X(02)00506-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel spiroketal-based NK1 antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2515 / 2518
页数：4
相关论文
共 50 条
  • [1] Spirocyclic NK1 antagonists II:: [4.5]-spiroethers
    Williams, BJ
    Cascieri, MA
    Chicchi, GG
    Harrison, T
    Owens, AP
    Owen, SN
    Rupniak, NMJ
    Tattersall, DF
    Williams, A
    Swain, CJ
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (19) : 2719 - 2722
  • [2] Tetrahydroindolizinone NK1 antagonists
    Bao, Jianming
    Lu, Huagang
    Morriello, Gregori J.
    Carlson, Emma J.
    Wheeldon, Alan
    Chicchi, Gary G.
    Kurtz, Marc M.
    Tsao, Kwei-Lan C.
    Zheng, Song
    Tong, Xinchun
    Mills, Sander G.
    DeVita, Robert J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (07) : 2354 - 2358
  • [3] Spotlight on NK1 antagonists
    Graul, AI
    DRUG NEWS & PERSPECTIVES, 1996, 9 (09) : 570 - 571
  • [4] NK1 receptor antagonists
    Lloyd, AW
    DRUG DISCOVERY TODAY, 1996, 1 (04) : 169 - 169
  • [5] NK1 receptor antagonists
    Lloyd, AW
    DRUG DISCOVERY TODAY, 1998, 3 (04) : 191 - 191
  • [6] Nonpeptide antagonists of the NK1 tachykinin receptor
    McLean, S
    MEDICINAL RESEARCH REVIEWS, 1996, 16 (04) : 297 - 317
  • [7] Therapeutic profile: NK1 receptor antagonists
    Swain, CJ
    DRUG DISCOVERY TODAY, 1996, 1 (06) : 265 - 266
  • [8] Synthesis of tetrahydropyran NK1 receptor antagonists
    Huffman, Mark A.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 231
  • [9] Design and synthesis of NK1 antagonists.
    Elliott, JM
    Chicchi, GG
    Hargreaves, R
    Hollingworth, GJ
    Rupniak, NMJ
    Swain, CJ
    Tattersall, D
    Watt, A
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U693 - U693
  • [10] Serine derived NK1 antagonists.
    Elliott, JM
    Cascieri, MA
    Davies, S
    Huscroft, IT
    Kelleher, FJ
    Lewis, RT
    MacLeod, AM
    Merchant, KJ
    Sadowski, S
    Stevenson, GL
    Sharp, M
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1996, 211 : 75 - MEDI
12345