Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-(4,5-d)azepines as novel TRPV1 antagonists.

Hawryluk NA; Merit JE; Lebsack AD; Branstetter BJ; Hack MD; Swanson N; Ao H; Maher MP; Bhattacharya A; Wang Q; Freedman JM; Scott BP; Wickenden AD; Chaplan SR; Breitenbucher JG

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Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-(4,5-d)azepines as novel TRPV1 antagonists.

机译：发现和合成6,7,8,9-四氢-5H-嘧啶-（4,5-d）氮杂环庚烷作为新型TRPV1拮抗剂。

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Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro and in vivo potency and acceptable physical properties.

机译：利用四氢嘧啶并氮杂core核作为哌嗪-脲的生物等效替代物导致发现了一系列新的TRPV1强效拮抗剂。已经确定四氢嘧啶并氮杂pine具有良好的体外和体内效力以及可接受的物理性质。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共5页
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Hawryluk NA; Merit JE; Lebsack AD; Branstetter BJ; Hack MD; Swanson N; Ao H; Maher MP; Bhattacharya A; Wang Q; Freedman JM; Scott BP; Wickenden AD; Chaplan SR; Breitenbucher JG;
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1. Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-(4,5-d)azepines as novel TRPV1 antagonists. [J] . Hawryluk NA, Merit JE, Lebsack AD, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：发现和合成6,7,8,9-四氢-5H-嘧啶-（4,5-d）氮杂环庚烷作为新型TRPV1拮抗剂。
2. 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido(4,5-d)azepines as TRPV1 antagonists with improved properties. [J] . Lebsack AD, Rech JC, Branstetter BJ, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：1,2-二氨基乙烷取代的6,7,8,9-四氢-5H-嘧啶（4,5-d）氮杂作为TRPV1拮抗剂，具有改善的性能。
3. Multiparameter Optimization in CNS Drug Discovery: Design of Pyrimido[4,5-d]azepines as Potent 5-Hydroxytryptamine 2C (5-HT_(2C)) Receptor Agonists with Exquisite Functional Selectivity over 5-HT_(2A) and 5-HT_(2B) Receptors [J] . R. Ian Storer, Paul E. Brennan, Alan D. Brown, Journal of Medicinal Chemistry . 2014,第12期

机译：在中枢神经系统药物发现中的多参数优化：嘧啶基[4,5-d]氮杂烷作为有效的5-羟色胺2C（5-HT_（2C））受体激动剂的设计，在5-HT_（2A）和5-HT_（ 2B）受体
4. Synthesis of Annulated Anilines and Azepines via Electrocyclization Reactions of 2-Aza-hepta-2,4-dien-6-ynyl Anions(Abstracts) [C] . Volodymyr Lyaskovskyy, Pramod Sagar, Ernst-Ulrich Wurthwein European Symposium on Organic Chemistry . 2007

机译：通过2-AZA-庚酮-2,4-DIEN-6-炔酮（摘要）的电阳性反应合成所述环苯胺和偶氮胺（摘要）
5. Application of organocatalysis to the synthesis of pharmaceutically relevant scaffolds: Chiral aziridines and beta-fluoroamines; total synthesis of stemaphylline; and discovery of selective PAR4 antagonists. [D] . Schulte, Michael L. 2013

机译：有机催化在药物相关支架合成中的应用：手性氮丙啶和β-氟胺；茶碱的全合成；和发现选择性PAR4拮抗剂。
6. Solid-phase synthesis of a library of amphipatic hydantoins. Discovery of new hits for TRPV1 blockade [O] . Guillermo Gerona-Navarro, Rosario González-Muñiz, Asia Fernández-Carvajal, -1

机译：两性留下文库的固相合成。发现TRPV1封锁的新命中
7. Design and Microwave-Assisted Synthesis of Novel Macrocyclic Peptides Active at Melanocortin Receptors: Discovery of Potent and Selective hMC5R Receptor Antagonists. [O] . Grieco P., Cai M., Liu L., 2008

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8. Method for the Synthesis of Tetranitroglycoluril from Imidazo-[4,5-d]-imidazoles with Loss of Dinitrogen Oxide. [R] . Sherrill, W. M., Johnson, E. C., Banning, J. E. 2014

机译：从咪唑 - [4,5-d] - 咪唑合成四硝基甘油的方法，其中氧化二氮的损失。

Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-(4,5-d)azepines as novel TRPV1 antagonists.

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