BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

108 related articles for article (PubMed ID: 18662872)

  • 1. Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
    Blum CA; Zheng X; Brielmann H; Hodgetts KJ; Bakthavatchalam R; Chandrasekhar J; Krause JE; Cortright D; Matson D; Crandall M; Ngo CK; Fung L; Day M; Kershaw M; De Lombaert S; Chenard BL
    Bioorg Med Chem Lett; 2008 Aug; 18(16):4573-7. PubMed ID: 18662872
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
    Westaway SM; Thompson M; Rami HK; Stemp G; Trouw LS; Mitchell DJ; Seal JT; Medhurst SJ; Lappin SC; Biggs J; Wright J; Arpino S; Jerman JC; Cryan JE; Holland V; Winborn KY; Coleman T; Stevens AJ; Davis JB; Gunthorpe MJ
    Bioorg Med Chem Lett; 2008 Oct; 18(20):5609-13. PubMed ID: 18809327
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Spiro-piperidine azetidinones as potent TRPV1 antagonists.
    Xiao D; Palani A; Aslanian R; McKittrick BA; McPhail AT; Correll CC; Phelps PT; Anthes JC; Rindgen D
    Bioorg Med Chem Lett; 2009 Feb; 19(3):783-7. PubMed ID: 19114307
    [TBL] [Abstract][Full Text] [Related]  

  • 4. From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
    Zheng X; Hodgetts KJ; Brielmann H; Hutchison A; Burkamp F; Brian Jones A; Blurton P; Clarkson R; Chandrasekhar J; Bakthavatchalam R; De Lombaert S; Crandall M; Cortright D; Blum CA
    Bioorg Med Chem Lett; 2006 Oct; 16(19):5217-21. PubMed ID: 16870426
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Discovery of piperidine carboxamide TRPV1 antagonists.
    Cheung WS; Calvo RR; Tounge BA; Zhang SP; Stone DR; Brandt MR; Hutchinson T; Flores CM; Player MR
    Bioorg Med Chem Lett; 2008 Aug; 18(16):4569-72. PubMed ID: 18662879
    [TBL] [Abstract][Full Text] [Related]  

  • 6. 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.
    Owen DR; Rodriguez-Lens M; Corless MD; Gaulier SM; Horne VA; Kinloch RA; Maw GN; Pearce DW; Rees H; Ringer TJ; Ryckmans T; Stammen BL
    Bioorg Med Chem Lett; 2009 Mar; 19(6):1702-6. PubMed ID: 19231185
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
    Guay D; Boulet L; Friesen RW; Girard M; Hamel P; Huang Z; Laliberté F; Laliberté S; Mancini JA; Muise E; Pon D; Styhler A
    Bioorg Med Chem Lett; 2008 Oct; 18(20):5554-8. PubMed ID: 18835163
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.
    Coon T; Moree WJ; Li B; Yu J; Zamani-Kord S; Malany S; Santos MA; Hernandez LM; Petroski RE; Sun A; Wen J; Sullivan S; Haelewyn J; Hedrick M; Hoare SJ; Bradbury MJ; Crowe PD; Beaton G
    Bioorg Med Chem Lett; 2009 Aug; 19(15):4380-4. PubMed ID: 19553115
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Design and characterization of a noncompetitive antagonist of the transient receptor potential vanilloid subunit 1 channel with in vivo analgesic and anti-inflammatory activity.
    García-Martínez C; Fernández-Carvajal A; Valenzuela B; Gomis A; Van Den Nest W; Ferroni S; Carreño C; Belmonte C; Ferrer-Montiel A
    J Pain; 2006 Oct; 7(10):735-46. PubMed ID: 17018334
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.
    Berglund S; Egner BJ; Gradén H; Gradén J; Morgan DG; Inghardt T; Giordanetto F
    Bioorg Med Chem Lett; 2009 Aug; 19(15):4268-73. PubMed ID: 19500979
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
    Gomtsyan A; Bayburt EK; Keddy R; Turner SC; Jinkerson TK; Didomenico S; Perner RJ; Koenig JR; Drizin I; McDonald HA; Surowy CS; Honore P; Mikusa J; Marsh KC; Wetter JM; Faltynek CR; Lee CH
    Bioorg Med Chem Lett; 2007 Jul; 17(14):3894-9. PubMed ID: 17507218
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
    Norman MH; Zhu J; Fotsch C; Bo Y; Chen N; Chakrabarti P; Doherty EM; Gavva NR; Nishimura N; Nixey T; Ognyanov VI; Rzasa RM; Stec M; Surapaneni S; Tamir R; Viswanadhan VN; Treanor JJ
    J Med Chem; 2007 Jul; 50(15):3497-514. PubMed ID: 17585749
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.
    Becknell NC; Dandu RR; Lyons JA; Aimone LD; Raddatz R; Hudkins RL
    Bioorg Med Chem Lett; 2012 Jan; 22(1):186-9. PubMed ID: 22153342
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
    Li Y; Liang J; Siu T; Hu E; Rossi MA; Barnett SF; Defeo-Jones D; Jones RE; Robinson RG; Leander K; Huber HE; Mittal S; Cosford N; Prasit P
    Bioorg Med Chem Lett; 2009 Feb; 19(3):834-6. PubMed ID: 19097777
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
    Yoshizumi T; Miyazoe H; Ito H; Tsujita T; Takahashi H; Asai M; Ozaki S; Ohta H; Okamoto O
    Bioorg Med Chem Lett; 2008 Jul; 18(13):3778-82. PubMed ID: 18515099
    [TBL] [Abstract][Full Text] [Related]  

  • 16. The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.
    Siu T; Li Y; Nagasawa J; Liang J; Tehrani L; Chua P; Jones RE; Defeo-Jones D; Barnett SF; Robinson RG
    Bioorg Med Chem Lett; 2008 Jul; 18(14):4191-4. PubMed ID: 18550373
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.
    Berglund S; Egner BJ; Gradén H; Gradén J; Morgan DG; Inghardt T; Giordanetto F
    Bioorg Med Chem Lett; 2009 Aug; 19(15):4274-9. PubMed ID: 19500982
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Identification of biaryl sulfone derivatives as antagonists of the histamine H₃ receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).
    Semple G; Santora VJ; Smith JM; Covel JA; Hayashi R; Gallardo C; Ibarra JB; Schultz JA; Park DM; Estrada SA; Hofilena BJ; Smith BM; Ren A; Suarez M; Frazer J; Edwards JE; Hart R; Hauser EK; Lorea J; Grottick AJ
    Bioorg Med Chem Lett; 2012 Jan; 22(1):71-5. PubMed ID: 22172695
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
    Gavva NR; Bannon AW; Hovland DN; Lehto SG; Klionsky L; Surapaneni S; Immke DC; Henley C; Arik L; Bak A; Davis J; Ernst N; Hever G; Kuang R; Shi L; Tamir R; Wang J; Wang W; Zajic G; Zhu D; Norman MH; Louis JC; Magal E; Treanor JJ
    J Pharmacol Exp Ther; 2007 Oct; 323(1):128-37. PubMed ID: 17652633
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
    Voight EA; Gomtsyan AR; Daanen JF; Perner RJ; Schmidt RG; Bayburt EK; DiDomenico S; McDonald HA; Puttfarcken PS; Chen J; Neelands TR; Bianchi BR; Han P; Reilly RM; Franklin PH; Segreti JA; Nelson RA; Su Z; King AJ; Polakowski JS; Baker SJ; Gauvin DM; Lewis LR; Mikusa JP; Joshi SK; Faltynek CR; Kym PR; Kort ME
    J Med Chem; 2014 Sep; 57(17):7412-24. PubMed ID: 25100568
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 6.