| Year |
Citation |
Score |
| 2020 |
McDaniel J, Farley CA, Ramirez A, Sandhu B, Sarjeant A, Shi Q, Han A, Gallagher WP, Hynes J, Dhar TGM, Gonzalez-Bobes F, Coombs JR, Marcoux D. Discovery of Annulating Reagents Enabling the One-Step and Highly Stereoselective Synthesis of Cyclopentyl and Cyclohexyl Cores. Organic Letters. PMID 33351641 DOI: 10.1021/acs.orglett.0c03695 |
0.331 |
|
| 2020 |
Shi Q, Xiao Z, Yang MG, Marcoux D, Cherney RJ, Yip S, Li P, Wu DR, Weigelt CA, Sack J, Khan J, Ruzanov M, Wang J, Yarde M, Ellen Cvijic M, ... ... Hynes J, et al. Tricyclic Sulfones as Potent, Selective and Efficacious RORγt Inverse Agonists - Exploring C6 and C8 SAR Using Late-Stage Functionalization. Bioorganic & Medicinal Chemistry Letters. 127521. PMID 32882417 DOI: 10.1016/J.Bmcl.2020.127521 |
0.342 |
|
| 2020 |
Marcoux D, Beaudoin Bertrand M, Weigelt CA, Yip S, Galella M, Park H, Wu DR, Wang J, Yarde M, Ellen Cvijic M, Li S, Hynes J, Tino JA, Zhao Q, Murali Dhar TG. Annulation Reaction Enables the identification of an Exocyclic Amide Tricyclic Chemotype as Retinoic Acid Receptor-Related Orphan Receptor Gamma (RORγ/RORc) Inverse Agonists. Bioorganic & Medicinal Chemistry Letters. 127466. PMID 32763309 DOI: 10.1016/J.Bmcl.2020.127466 |
0.383 |
|
| 2020 |
Nair S, Kumar SR, Paidi VR, Sistla R, Kantheti D, Polimera SR, Thangavel S, Mukherjee AJ, Das M, Bhide RS, Pitts WJ, Murugesan N, Dudhgoankar S, Nagar J, Subramani S, ... ... Hynes J, et al. Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis. Acs Medicinal Chemistry Letters. 11: 1402-1409. PMID 32676146 DOI: 10.1021/Acsmedchemlett.0C00082 |
0.306 |
|
| 2019 |
Shi Q, Greenwood NS, Meehan MC, Park H, Galella M, Sandhu B, Khandelwal P, Coombs JR, Gallagher WP, Guerrero CA, Hynes J, Dhar TGM, Gonzalez Bobes F, Marcoux D. One-Step Diastereoselective Pyrrolidine Synthesis Using a Sulfinamide Annulating Reagent. Organic Letters. PMID 31647672 DOI: 10.1021/Acs.Orglett.9B03560 |
0.404 |
|
| 2019 |
Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin Bertrand M, Weigelt CA, Khandelwal P, Pushparaj S, Selvakumar K, Karmakar A, Gupta AK, ... ... Hynes J, et al. Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt ‒ Identification of a Potent, Selective Series with Biologic-Like In Vivo Efficacy. Journal of Medicinal Chemistry. PMID 31638797 DOI: 10.1021/Acs.Jmedchem.9B01369 |
0.308 |
|
| 2019 |
Arunachalam PN, Kuppusamy P, Ganesan S, Krishnamoorthy S, Nimje RY, Jarugu LB, Chikkananjaiah NK, Reddy CA, Anjanappa P, Botlagunta M, Vanteru S, Maddala N, Shankar M, Nair S, Hynes J, et al. Development of a Scalable Synthesis for the Potent Kinase Inhibitor BMS-986236; 1-(5-(4-(3-Hydroxy-3-methylbutyl)-1H-1,2,3-triazol-1-yl)-4-(isopropylamino)pyridin-2-yl)-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile Organic Process Research & Development. 23: 912-918. DOI: 10.1021/Acs.Oprd.9B00023 |
0.305 |
|
| 2017 |
Shi Q, Meehan MC, Galella M, Park H, Khandelwal P, Hynes J, Dhar TGM, Marcoux D. Protected Chloroethyl and Chloropropyl Amines as Conformationally Unrestricted Annulating Reagents. Organic Letters. PMID 29283585 DOI: 10.1021/Acs.Orglett.7B03548 |
0.343 |
|
| 2017 |
Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J, Wu H, Tokarski J, Sack JS, et al. Discovery of highly potent, selective, covalent inhibitors of JAK3. Bioorganic & Medicinal Chemistry Letters. PMID 28927786 DOI: 10.1016/J.Bmcl.2017.09.023 |
0.337 |
|
| 2017 |
Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, ... ... Hynes J, et al. Identification of a potent, selective, and efficacious phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor for the treatment of immunological disorders. Journal of Medicinal Chemistry. PMID 28541707 DOI: 10.1021/Acs.Jmedchem.7B00618 |
0.322 |
|
| 2017 |
Hynes J, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, et al. Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 28539220 DOI: 10.1016/J.Bmcl.2017.05.043 |
0.351 |
|
| 2017 |
Marcoux D, Qin LY, Ruan Z, Shi Q, Ruan Q, Weigelt C, Qiu H, Schieven G, Hynes J, Bhide R, Poss M, Tino J. Identification of highly potent and selective PI3Kδ inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 28209465 DOI: 10.1016/J.Bmcl.2017.01.077 |
0.322 |
|
| 2015 |
Hong Y, Hynes J, Tian Y, Balasubramanian B, Bonacorsi S. Synthesis and characterization of tritium labeled N-((R)-1-((S)-4-(4-chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)-3-sulfamoylbenzamide. Journal of Labelled Compounds & Radiopharmaceuticals. 58: 414-8. PMID 26228905 DOI: 10.1002/Jlcr.3320 |
0.324 |
|
| 2015 |
Khan JA, Camac DM, Low S, Tebben AJ, Wensel DL, Wright MC, Su J, Jenny V, Gupta RD, Ruzanov M, Russo KA, Bell A, An Y, Bryson JW, Gao M, ... ... Hynes J, et al. Developing Adnectins that target SRC co-activator binding to PXR: a structural approach toward understanding promiscuity of PXR. Journal of Molecular Biology. 427: 924-42. PMID 25579995 DOI: 10.1016/J.Jmb.2014.12.022 |
0.355 |
|
| 2014 |
Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, et al. Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. Bioorganic & Medicinal Chemistry Letters. 24: 5721-6. PMID 25453808 DOI: 10.1016/J.Bmcl.2014.10.061 |
0.364 |
|
| 2013 |
Gardner DS, Santella JB, Duncia JV, Carter PH, Dhar TG, Wu H, Guo W, Cavallaro C, Van Kirk K, Yarde M, Briceno SW, Grafstrom RR, Liu R, Patel SR, Tebben AJ, ... ... Hynes J, et al. The discovery of BMS-457, a potent and selective CCR1 antagonist. Bioorganic & Medicinal Chemistry Letters. 23: 3833-40. PMID 23707259 DOI: 10.1016/J.Bmcl.2013.04.079 |
0.379 |
|
| 2012 |
Cavallaro CL, Briceno S, Chen J, Cvijic ME, Davies P, Hynes J, Liu RQ, Mandlekar S, Rose AV, Tebben AJ, Van Kirk K, Watson A, Wu H, Yang G, Carter PH. Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis. Journal of Medicinal Chemistry. 55: 9643-53. PMID 23075267 DOI: 10.1021/Jm300896D |
0.437 |
|
| 2012 |
Shi Z, Kiau S, Lobben P, Hynes J, Wu H, Parlanti L, Discordia R, Doubleday WW, Leftheris K, Dyckman AJ, Wrobleski ST, Dambalas K, Tummala S, Leung S, Lo E. Development of a practical synthesis of a p38 kinase inhibitor via a safe and robust amination Organic Process Research and Development. 16: 1618-1625. DOI: 10.1021/Op300181R |
0.367 |
|
| 2010 |
Carter PH, Hynes J. N-aryl pyrazoles, indazoles and azaindazoles as antagonists of CC chemokine receptor 1: Patent cooperation treaty applications WO2010/036632, WO2009/134666 and WO2009/137338 Expert Opinion On Therapeutic Patents. 20: 1609-1618. PMID 20858032 DOI: 10.1517/13543776.2010.518144 |
0.318 |
|
| 2010 |
Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, et al. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. Journal of Medicinal Chemistry. 53: 6629-39. PMID 20804198 DOI: 10.1021/Jm100540X |
0.333 |
|
| 2010 |
Lin S, Wrobleski ST, Hynes J, Pitt S, Zhang R, Fan Y, Doweyko AM, Kish KF, Sack JS, Malley MF, Kiefer SE, Newitt JA, McKinnon M, Trzaskos J, Barrish JC, et al. Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 5864-8. PMID 20732813 DOI: 10.1016/J.Bmcl.2010.07.102 |
0.353 |
|
| 2009 |
Zhao R, Wang B, Wu H, Hynes J, Leftheris K, Balasubramanian B, Barrish JC, Chen B. Improved procedure for the preparation of 7-methoxy-2-methyl-1-(2-morpholinoethyl)-1H-indole-3-carboxylic acid, key intermediate in the synthesis of novel 3-amidoindole and indolopyridone cannabinoid ligands Arkivoc. 2010. DOI: 10.3998/Ark.5550190.0011.610 |
0.348 |
|
| 2008 |
Wrobleski ST, Lin S, Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, et al. Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 18: 2739-44. PMID 18364256 DOI: 10.1016/J.Bmcl.2008.02.067 |
0.375 |
|
| 2008 |
Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, et al. The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 18: 1762-7. PMID 18313298 DOI: 10.1016/J.Bmcl.2008.02.031 |
0.349 |
|
| 2008 |
Hynes J, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, et al. Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors. Journal of Medicinal Chemistry. 51: 4-16. PMID 18072718 DOI: 10.1021/Jm7009414 |
0.352 |
|
| 2007 |
Parlanti L, Discordia RP, Hynes J, Miller MM, O'Grady HR, Shi Z. Amination of heterocyclic compounds with o-benzoylhydroxylamine derivatives. Organic Letters. 9: 3821-4. PMID 17718497 DOI: 10.1021/Ol701730R |
0.374 |
|
| 2005 |
Hynes J, Leftheri K. Small molecule p38 inhibitors: novel structural features and advances from 2002-2005. Current Topics in Medicinal Chemistry. 5: 967-85. PMID 16178741 DOI: 10.2174/1568026054985920 |
0.338 |
|
| 2004 |
Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, et al. The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. Journal of Medicinal Chemistry. 47: 6283-91. PMID 15566298 DOI: 10.1021/Jm049521D |
0.39 |
|
| 2004 |
Hynes J, Doubleday WW, Dyckman AJ, Godfrey JD, Grosso JA, Kiau S, Leftheris K. N-Amination of pyrrole and indole heterocycles with monochloramine (NH2Cl). The Journal of Organic Chemistry. 69: 1368-71. PMID 14961694 DOI: 10.1021/Jo035587P |
0.384 |
|
| 2004 |
Abrous L, Jokiel PA, Friedrich SR, Hynes J, Smith AB, Hirschmann R. Novel chimeric scaffolds to extend the exploration of receptor space: hybrid beta-D-glucose-benzoheterodiazepine structures for broad screening. Effect of amide alkylation on the course of cyclization reactions. The Journal of Organic Chemistry. 69: 280-302. PMID 14725439 DOI: 10.1021/Jo0352068 |
0.612 |
|
| 2003 |
Wrobleski ST, Chen P, Hynes J, Lin S, Norris DJ, Pandit CR, Spergel S, Wu H, Tokarski JS, Chen X, Gillooly KM, Kiener PA, McIntyre KW, Patil-Koota V, Shuster DJ, et al. Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties. Journal of Medicinal Chemistry. 46: 2110-6. PMID 12747783 DOI: 10.1021/Jm020329Q |
0.381 |
|
| 2002 |
Hynes J, Leftheris K, Wu H, Pandit C, Chen P, Norris DJ, Chen BC, Zhao R, Kiener PA, Chen X, Turk LA, Patil-Koota V, Gillooly KM, Shuster DJ, McIntyre KW. C-3 Amido-indole cannabinoid receptor modulators. Bioorganic & Medicinal Chemistry Letters. 12: 2399-402. PMID 12161142 DOI: 10.1016/S0960-894X(02)00466-3 |
0.33 |
|
| 2002 |
Hynes J, Nasser T, Overman LE, Watson DA. Preparation of alpha-sulfenyl enones by thermal fragmentation of beta-sulfenyl enol triflates. Organic Letters. 4: 929-31. PMID 11893188 DOI: 10.1021/Ol017303Y |
0.614 |
|
| 2001 |
Abrous L, Hynes J, Friedrich SR, Smith AB, Hirschmann R. Design and synthesis of novel scaffolds for drug discovery: hybrids of beta-D-glucose with 1,2,3,4-tetrahydrobenzo[e][1,4]diazepin-5-one, the corresponding 1-oxazepine, and 2- and 4-pyridyldiazepines. Organic Letters. 3: 1089-92. PMID 11277802 DOI: 10.1021/Ol015698F |
0.607 |
|
| 1996 |
Hirschmann R, Yao W, Cascieri MA, Strader CD, Maechler L, Cichy-Knight MA, Hynes J, van Rijn RD, Sprengeler PA, Smith AB. Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic. Journal of Medicinal Chemistry. 39: 2441-8. PMID 8691440 DOI: 10.1021/Jm960281E |
0.594 |
|
| 1995 |
Hirschmann R, Hynes J, Spoors P, Smith AB. Chemoselective monoalkylation of 5-trifluoroacetamido- and 5-acetamido-1-pentanol derivatives via N,O-bisdeprotonation. Quantitation of evolved H2 as a probe of anion formation Tetrahedron Letters. 36: 2373-2376. DOI: 10.1016/0040-4039(95)00280-P |
0.543 |
|
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