Display Settings:

Format
Items per page
Sort by

Send to:

Choose Destination

Results: 1 to 20 of 87

1.

The discovery of novel calcium sensing receptor negative allosteric modulators.

Balan G, Bauman J, Bhattacharya S, Castrodad M, Healy DR, Herr M, Humphries P, Jennings S, Kalgutkar AS, Kapinos B, Khot V, Lazarra K, Li M, Li Y, Neagu C, Oliver R, Piotrowski DW, Price D, Qi H, Simmons HA, Southers J, Wei L, Zhang Y, Paralkar VM.

Bioorg Med Chem Lett. 2009 Jun 15;19(12):3328-32. doi: 10.1016/j.bmcl.2009.04.044. Epub 2009 Apr 18.

PMID:
19442519
[PubMed - indexed for MEDLINE]
2.

Discovery and structure-activity relationships of trisubstituted pyrimidines/pyridines as novel calcium-sensing receptor antagonists.

Yang W, Ruan Z, Wang Y, Van Kirk K, Ma Z, Arey BJ, Cooper CB, Seethala R, Feyen JH, Dickson JK Jr.

J Med Chem. 2009 Feb 26;52(4):1204-8. doi: 10.1021/jm801178c.

PMID:
19143533
[PubMed - indexed for MEDLINE]
3.

Characterization of the effect of chronic administration of a calcium-sensing receptor antagonist, ronacaleret, on renal calcium excretion and serum calcium in postmenopausal women.

Caltabiano S, Dollery CT, Hossain M, Kurtinecz MT, Desjardins JP, Favus MJ, Kumar R, Fitzpatrick LA.

Bone. 2013 Sep;56(1):154-62. doi: 10.1016/j.bone.2013.05.021. Epub 2013 Jun 10.

PMID:
23756230
[PubMed - indexed for MEDLINE]
4.

An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation.

Kumar S, Matheny CJ, Hoffman SJ, Marquis RW, Schultz M, Liang X, Vasko JA, Stroup GB, Vaden VR, Haley H, Fox J, DelMar EG, Nemeth EF, Lago AM, Callahan JF, Bhatnagar P, Huffman WF, Gowen M, Yi B, Danoff TM, Fitzpatrick LA.

Bone. 2010 Feb;46(2):534-42. doi: 10.1016/j.bone.2009.09.028. Epub 2009 Sep 26.

PMID:
19786130
[PubMed - indexed for MEDLINE]
5.

Structure based evolution of a novel series of positive modulators of the AMPA receptor.

Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. doi: 10.1016/j.bmcl.2010.11.098. Epub 2010 Nov 25.

PMID:
21190850
[PubMed - indexed for MEDLINE]
6.

Ronacaleret, a calcium-sensing receptor antagonist, has no significant effect on radial fracture healing time: results of a randomized, double-blinded, placebo-controlled Phase II clinical trial.

Fitzpatrick LA, Smith PL, McBride TA, Fries MA, Hossain M, Dabrowski CE, Gordon DN.

Bone. 2011 Oct;49(4):845-52. doi: 10.1016/j.bone.2011.06.017. Epub 2011 Jun 30.

PMID:
21742071
[PubMed - indexed for MEDLINE]
7.

Calcilytics: antagonists of the calcium-sensing receptor for the treatment of osteoporosis.

Widler L.

Future Med Chem. 2011 Apr;3(5):535-47. doi: 10.4155/fmc.11.17. Review.

PMID:
21526895
[PubMed - indexed for MEDLINE]
8.

Novel and potent calcium-sensing receptor antagonists: discovery of (5R)-N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide monotosylate (TAK-075) as an orally active bone anabolic agent.

Yoshida M, Mori A, Morimoto S, Kotani E, Oka M, Notoya K, Makino H, Ono M, Shirasaki M, Tada N, Fujita H, Ban J, Ikeda Y, Kawamoto T, Goto M, Kimura H, Baba A, Yasuma T.

Bioorg Med Chem. 2011 Mar 15;19(6):1881-94. doi: 10.1016/j.bmc.2011.02.001. Epub 2011 Feb 24.

PMID:
21353570
[PubMed - indexed for MEDLINE]
9.

Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.

Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, Zawistoski M, Li J, Oliver R, Guzman-Perez A, Liu KK, Walker DP, Benbow JW, Morris J.

Chem Res Toxicol. 2010 Jun 21;23(6):1115-26. doi: 10.1021/tx100137n.

PMID:
20507089
[PubMed - indexed for MEDLINE]
10.

Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.

Hao J, Dehlinger V, Fivush AM, Rudyk HC, Britton TC, Hollinshead SP, Vokits BP, Clark BP, Henry SS, Massey SM, Peng L, Dressman BA, Heinz BA, Roberts EF, Bracey-Walker MR, Swanson S, Catlow JT, Love PL, Tepool AD, Peters SC, Simmons RM, Iyengar S, McKinzie DL, Monn JA.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1249-52. doi: 10.1016/j.bmcl.2013.01.009. Epub 2013 Jan 12.

PMID:
23374867
[PubMed - indexed for MEDLINE]
11.

Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.

Marquis RW, Lago AM, Callahan JF, Rahman A, Dong X, Stroup GB, Hoffman S, Gowen M, DelMar EG, Van Wagenen BC, Logan S, Shimizu S, Fox J, Nemeth EF, Roethke T, Smith BR, Ward KW, Bhatnagar P.

J Med Chem. 2009 Nov 12;52(21):6599-605. doi: 10.1021/jm900563e.

PMID:
19821575
[PubMed - indexed for MEDLINE]
12.

Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols.

Gustafsson M, Jensen J, Bertozzi SM, Currier EA, Ma JN, Burstein ES, Olsson R.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5918-21. doi: 10.1016/j.bmcl.2010.07.077. Epub 2010 Jul 23.

PMID:
20727747
[PubMed - indexed for MEDLINE]
13.

Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration.

Eskildsen J, Redrobe JP, Sams AG, Dekermendjian K, Laursen M, Boll JB, Papke RL, Bundgaard C, Frederiksen K, Bastlund JF.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):288-93. doi: 10.1016/j.bmcl.2013.11.022. Epub 2013 Nov 20.

PMID:
24291041
[PubMed - indexed for MEDLINE]
14.

Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.

Gavai AV, Vaz RJ, Mikkilineni AB, Roberge JY, Liu Y, Lawrence RM, Corte JR, Yang W, Bednarz M, Dickson JK Jr, Ma Z, Seethala R, Feyen JH.

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5478-82. Epub 2005 Oct 10.

PMID:
16216508
[PubMed - indexed for MEDLINE]
15.

The calcium-sensing receptor in bone cells: a potential therapeutic target in osteoporosis.

Marie PJ.

Bone. 2010 Mar;46(3):571-6. doi: 10.1016/j.bone.2009.07.082. Epub 2009 Aug 4. Review.

PMID:
19660583
[PubMed - indexed for MEDLINE]
16.

Positive and negative allosteric modulators of the Ca2+-sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain.

Petrel C, Kessler A, Dauban P, Dodd RH, Rognan D, Ruat M.

J Biol Chem. 2004 Apr 30;279(18):18990-7. Epub 2004 Feb 19.

PMID:
14976203
[PubMed - indexed for MEDLINE]
Free Article
17.

Agonists and allosteric modulators of the calcium-sensing receptor and their therapeutic applications.

Saidak Z, Brazier M, Kamel S, Mentaverri R.

Mol Pharmacol. 2009 Dec;76(6):1131-44. doi: 10.1124/mol.109.058784. Epub 2009 Sep 24. Review.

PMID:
19779033
[PubMed - indexed for MEDLINE]
Free Article
18.

Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.

Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8.

PMID:
19625189
[PubMed - indexed for MEDLINE]
19.

Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.

Marquis RW, Lago AM, Callahan JF, Trout RE, Gowen M, DelMar EG, Van Wagenen BC, Logan S, Shimizu S, Fox J, Nemeth EF, Yang Z, Roethke T, Smith BR, Ward KW, Lee J, Keenan RM, Bhatnagar P.

J Med Chem. 2009 Jul 9;52(13):3982-93. doi: 10.1021/jm900364m.

PMID:
19492813
[PubMed - indexed for MEDLINE]
20.

Investigational anabolic therapies for osteoporosis.

Trivedi R, Goswami R, Chattopadhyay N.

Expert Opin Investig Drugs. 2010 Aug;19(8):995-1005. doi: 10.1517/13543784.2010.501077. Review.

PMID:
20629616
[PubMed - indexed for MEDLINE]

Display Settings:

Format
Items per page
Sort by

Send to:

Choose Destination

Supplemental Content

Write to the Help Desk