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Items: 1 to 50 of 129

1.

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1830-4. doi: 10.1016/j.bmcl.2008.12.050. Epub 2008 Dec 24.

PMID:
19237282
2.

3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.

Butora G, Jiao R, Parsons WH, Vicario PP, Jin H, Ayala JM, Cascieri MA, Yang L.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3636-41. Epub 2007 Apr 25.

PMID:
17482462
3.

Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.

Yang L, Butora G, Jiao RX, Pasternak A, Zhou C, Parsons WH, Mills SG, Vicario PP, Ayala JM, Cascieri MA, MacCoss M.

J Med Chem. 2007 May 31;50(11):2609-11. Epub 2007 Apr 27.

PMID:
17461566
4.

Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.

Zhou C, Guo L, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Cascieri MA, Springer MS, Yang L.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):309-14. Epub 2006 Oct 25.

PMID:
17092717
5.

4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties.

Butora G, Morriello GJ, Kothandaraman S, Guiadeen D, Pasternak A, Parsons WH, MacCoss M, Vicario PP, Cascieri MA, Yang L.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4715-22. Epub 2006 Jul 25.

PMID:
16870431
6.

Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.

Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. Epub 2006 Jul 10.

PMID:
16831551
7.

Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.

Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. Epub 2006 Jul 7.

PMID:
16824752
8.

Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.

Yang L, Zhou C, Guo L, Morriello G, Butora G, Pasternak A, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Ayala JM, Goyal S, Hanlon WA, Cascieri MA, Springer MS.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3735-9. Epub 2006 May 15.

PMID:
16698264
9.

Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608.

Rupniak NM, Carlson EJ, Shepheard S, Bentley G, Williams AR, Hill A, Swain C, Mills SG, Di Salvo J, Kilburn R, Cascieri MA, Kurtz MM, Tsao KL, Gould SL, Chicchi GG.

Neuropharmacology. 2003 Aug;45(2):231-41.

PMID:
12842129
10.

CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Finke PE, Caldwell CG, Mills SG, MacCoss M, Shen DM, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini E.

Org Lett. 2003 Jul 10;5(14):2473-5.

PMID:
12841758
11.

Expression and characterization of the chemokine receptor CCR2B from rhesus monkey.

Jin H, Vicario PP, Zweerink H, Goyal S, Hanlon WA, Dorn CP, Mills SG, DeMartino JA, Cascieri MA, Struthers M.

Biochem Pharmacol. 2003 Jul 15;66(2):321-30.

PMID:
12826275
12.

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.

Willoughby CA, Rosauer KG, Hale JJ, Budhu RJ, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):427-31.

PMID:
12565944
13.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23.

PMID:
12467630
14.

Identification, localization and receptor characterization of novel mammalian substance P-like peptides.

Kurtz MM, Wang R, Clements MK, Cascieri MA, Austin CP, Cunningham BR, Chicchi GG, Liu Q.

Gene. 2002 Aug 21;296(1-2):205-12.

PMID:
12383518
15.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4.

PMID:
12270193
16.

Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.

Williams BJ, Cascieri MA, Chicchi GG, Harrison T, Owens AP, Owen SN, Rupniak NM, Tattersall DF, Williams A, Swain CJ.

Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22.

PMID:
12217362
17.

The potential for novel anti-inflammatory therapies for coronary artery disease.

Cascieri MA.

Nat Rev Drug Discov. 2002 Feb;1(2):122-30. Review.

PMID:
12120093
18.

CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.

Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):677-9.

PMID:
11844699
19.

An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.

Harrison T, Owens AP, Williams BJ, Swain CJ, Williams A, Carlson EJ, Rycroft W, Tattersall FD, Cascieri MA, Chicchi GG, Sadowski S, Rupniak NM, Hargreaves RJ.

J Med Chem. 2001 Nov 22;44(24):4296-9.

PMID:
11708932
20.

Substituted imidazoles as glucagon receptor antagonists.

Chang LL, Sidler KL, Cascieri MA, de Laszlo S, Koch G, Li B, MacCoss M, Mantlo N, O'Keefe S, Pang M, Rolando A, Hagmann WK.

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2549-53.

PMID:
11549467
21.

Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys.

Hom GJ, Forrest MJ, Bach TJ, Brady E, Candelore MR, Cascieri MA, Fletcher DJ, Fisher MH, Iliff SA, Mathvink R, Metzger J, Pecore V, Saperstein R, Shih T, Weber AE, Wyvratt M, Zafian P, MacIntyre DE.

J Pharmacol Exp Ther. 2001 Apr;297(1):299-307.

PMID:
11259557
22.

Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.

Brockunier LL, Candelore MR, Cascieri MA, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE, Parmee ER.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):379-82.

PMID:
11212115
23.

The CXCR4 agonist ligand stromal derived factor-1 maintains high affinity for receptors in both Galpha(i)-coupled and uncoupled states.

Di Salvo J, Koch GE, Johnson KE, Blake AD, Daugherty BL, DeMartino JA, Sirotina-Meisher A, Liu Y, Springer MS, Cascieri MA, Sullivan KA.

Eur J Pharmacol. 2000 Dec 8;409(2):143-54.

PMID:
11104827
24.

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.

Parmee ER, Brockunier LL, He J, Singh SB, Candelore MR, Cascieri MA, Deng L, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2283-6.

PMID:
11055339
25.

Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.

Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

J Med Chem. 2000 Oct 19;43(21):3832-6.

PMID:
11052788
26.

Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.

Liu J, Underwood DJ, Cascieri MA, Rohrer SP, Cantin LD, Chicchi G, Smith AB 3rd, Hirschmann R.

J Med Chem. 2000 Oct 19;43(21):3827-31. No abstract available.

PMID:
11052787
27.

L-750355, a human beta3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey.

Forrest MJ, Hom G, Bach T, Candelore MR, Cascieri MA, Strader C, Tota L, Fisher MH, Szumiloski J, Ok HO, Weber AE, Wyvratt M, Vicario P, Marko O, Deng L, Cioffe C, Hegarty-Friscino B, MacIntyre E.

Eur J Pharmacol. 2000 Oct 27;407(1-2):175-81.

PMID:
11050305
28.

Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Brockunier LL, Parmee ER, Ok HO, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Sep 18;10(18):2111-4.

PMID:
10999482
29.

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.

Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1971-3.

PMID:
10987429
30.

The chemokine/chemokine-receptor family: potential and progress for therapeutic intervention.

Cascieri MA, Springer MS.

Curr Opin Chem Biol. 2000 Aug;4(4):420-7. Review.

PMID:
10959770
31.

Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.

Ok HO, Reigle LB, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang P, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1531-4.

PMID:
10915043
32.

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.

Biftu T, Feng DD, Liang GB, Kuo H, Qian X, Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Forrest MJ, Hom GJ, MacIntyre DE, Stearns RA, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1431-4.

PMID:
10888325
33.

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9.

PMID:
10888324
34.

Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.

Hale JJ, Mills SG, MacCoss M, Dorn CP, Finke PE, Budhu RJ, Reamer RA, Huskey SE, Luffer-Atlas D, Dean BJ, McGowan EM, Feeney WP, Chiu SH, Cascieri MA, Chicchi GG, Kurtz MM, Sadowski S, Ber E, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, Metzger JM, MacIntyre DE.

J Med Chem. 2000 Mar 23;43(6):1234-41.

PMID:
10737756
35.

Generation of mice expressing the human glucagon receptor with a direct replacement vector.

Shiao LL, Cascieri MA, Trumbauer M, Chen H, Sullivan KA.

Transgenic Res. 1999 Aug;8(4):295-302.

PMID:
10621976
36.

Potent and selective human beta(3)-adrenergic receptor antagonists.

Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE.

J Pharmacol Exp Ther. 1999 Aug;290(2):649-55.

PMID:
10411574
37.

Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.

Mathvink RJ, Barritta AM, Candelore MR, Cascieri MA, Deng L, Tota L, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1869-74.

PMID:
10406657
38.

Receptor for motilin identified in the human gastrointestinal system.

Feighner SD, Tan CP, McKee KK, Palyha OC, Hreniuk DL, Pong SS, Austin CP, Figueroa D, MacNeil D, Cascieri MA, Nargund R, Bakshi R, Abramovitz M, Stocco R, Kargman S, O'Neill G, Van Der Ploeg LH, Evans J, Patchett AA, Smith RG, Howard AD.

Science. 1999 Jun 25;284(5423):2184-8.

39.

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

Shih TL, Candelore MR, Cascieri MA, Chiu SH, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4.

PMID:
10340609
40.

Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.

Naylor EM, Parmee ER, Colandrea VJ, Perkins L, Brockunier L, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):755-8.

PMID:
10201842
41.

Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54.

PMID:
10201841
42.

Potent, orally absorbed glucagon receptor antagonists.

de Laszlo SE, Hacker C, Li B, Kim D, MacCoss M, Mantlo N, Pivnichny JV, Colwell L, Koch GE, Cascieri MA, Hagmann WK.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):641-6.

PMID:
10201821
43.

Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.

Cascieri MA, Koch GE, Ber E, Sadowski SJ, Louizides D, de Laszlo SE, Hacker C, Hagmann WK, MacCoss M, Chicchi GG, Vicario PP.

J Biol Chem. 1999 Mar 26;274(13):8694-7.

44.

3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.

Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3087-92.

PMID:
9873681
45.

L-tryptophan urea amides as NK1/NK2 dual antagonists.

Qi H, Shah SK, Cascieri MA, Sadowski SJ, MaCcoss M.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2259-62.

PMID:
9873524
46.

3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.

Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6.

PMID:
9873496
47.

Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.

Elliott JM, Broughton H, Cascieri MA, Chicchi G, Huscroft IT, Kurtz M, MacLeod AM, Sadowski S, Stevenson GI.

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1851-6.

PMID:
9873446
48.

Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.

Elliott JM, Cascieri MA, Chicchi G, Davies S, Kelleher FJ, Kurtz M, Ladduwahetty T, Lewis RT, MacLeod AM, Merchant KJ, Sadowski S, Stevenson GI.

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1845-50.

PMID:
9873445
49.

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.

Harrison T, Korsgaard MP, Swain CJ, Cascieri MA, Sadowski S, Seabrook GR.

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1343-8.

PMID:
9871763
50.

High affinity phenylglycinol-based NK1 receptor antagonists.

Owens AP, Harrison T, Moseley JD, Swain CJ, Sadowski S, Cascieri MA.

Bioorg Med Chem Lett. 1998 Jan 6;8(1):51-6.

PMID:
9871627

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