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Joseph Vacca

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Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.

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2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Bioorganic & medicinal chemistry letters 2012;22(23):7207-13.
2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Bioorganic & medicinal chemistry letters 2012;22(23):7201-6.
2012: Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
Antimicrobial agents and chemotherapy 2012;56(8):4161-7.
2012: Ian M Bell; Joseph G Bruno; Amy Calamari; Christine Fandozzi; Steven N Gallicchio; Samuel L Graham; Stefanie A Kane; Amanda L Kemmerer; Eric L Moore; Scott D Mosser; Nova Sain; Harold G Selnick; Donnette D Staas; Craig A Stump; Mark Urban; Joseph P Vacca; Rebecca B White; C Blair Zartman; Matthew M Zrada; Christopher A Salvatore
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Bioorganic & medicinal chemistry letters 2012;22(12):3941-5.
2011: Robert Gomez; Samson Jolly; Ming-Tain Lai; Yuexia Liang; Georgia B McGaughey; Mike Miller; Vandna Munshi; Brenda Paton; Rosa Sanchez; Sinoeun Touch; Thomas Tucker; Robert Tynebor; Joseph P Vacca; Bang-Lin Wan; Theresa Williams; Youwei Yan; Daniel DeStefano; Peter J Felock; Neville J Anthony
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters 2011;21(24):7344-50.
2011: Robert Gomez; Samson J Jolly; Ming-Tain Lai; Yuexia Liang; Georgia B McGaughey; Mike Miller; Vandna Munshi; Brenda Paton; John Reid; Rosa Sanchez; Maricel Torrent; Joseph P Vacca; Bang-Lin Wan; Theresa Williams; Youwei Yan; Daniel J DiStefano; Peter J Felock; Jessica Flynn; Neville J Anthony
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
Journal of medicinal chemistry 2011;54(22):7920-33.
2011: C Blair Zartman; Ian M Bell; Steven N Gallicchio; Samuel L Graham; Stefanie A Kane; John J Mallee; Ruth Z Rutledge; Christopher A Salvatore; Joseph P Vacca; Theresa M Williams
Identification of a novel RAMP-independent CGRP receptor antagonist.
Bioorganic & medicinal chemistry letters 2011;21(22):6705-8.
2011: Sophie Parmentier-Batteur; Hemaka A Rajapakse; Christopher P Regan; Ian J Reynolds; John M Sanders; Sujata Sharma; Joseph P Vacca; Theresa M Williams; Hong Zhu; Eleftheria N Finger; J Fred Hess; Kandpal Geeta; Raghu Krishnan; Robert J Mark; Keith P Moore; Philippe G Nantermet
Attenuation of scratch-induced reactive astrogliosis by novel EphA4 kinase inhibitors.
Journal of neurochemistry 2011;118(6):1016-31.
2011: Daniel V Paone; Diem N Nguyen; Anthony W Shaw; Christopher S Burgey; Craig M Potteiger; James Z Deng; Scott D Mosser; Christopher A Salvatore; Sean Yu; Shane Roller; Stefanie A Kane; Harold G Selnick; Joseph P Vacca; Theresa M Williams
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
Bioorganic & medicinal chemistry letters 2011;21(9):2683-6.
2011: Hemaka A Rajapakse; Abbas M Walji; Keith P Moore; Hong Zhu; Aurpon W Mitra; Alison R Gregro; Elizabeth Tinney; Christine Burlein; Sinoeun Touch; Brenda L Paton; Steven S Carroll; Daniel J DiStefano; Ming-Tain Lai; Jay A Grobler; Rosa I Sanchez; Theresa M Williams; Joseph P Vacca; Philippe G Nantermet
Strategies towards improving the pharmacokinetic profile of ε-substituted lysinol-derived HIV protease inhibitors.
ChemMedChem 2011;6(2):253-7.
2010: Peter D Williams; Donnette D Staas; Shankar Venkatraman; H Marie Loughran; Rowena D Ruzek; Theresa M Booth; Terry A Lyle; John S Wai; Joseph P Vacca; Bradley P Feuston; Linda T Ecto; Jessica A Flynn; Daniel J DiStefano; Daria J Hazuda; Carolyn M Bahnck; Amy L Himmelberger; Geetha Dornadula; Renee C Hrin; Kara A Stillmock; Marc V Witmer; Michael D Miller; Jay A Grobler
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.
Bioorganic & medicinal chemistry letters 2010;20(22):6754-7.
2010: Michael R Wood; Kathy M Schirripa; June J Kim; Rodney A Bednar; John F Fay; Joseph G Bruno; Eric L Moore; Scott D Mosser; Shane Roller; Christopher A Salvatore; Joseph P Vacca; Harold G Selnick
Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.
Bioorganic & medicinal chemistry letters 2010;20(22):6827-30.
2010: Dai-Shi Su; John J Lim; Elizabeth Tinney; Thomas J Tucker; Sandeep Saggar; John T Sisko; Bang-Lin Wan; Mary Beth Young; Kenneth D Anderson; Deanne Rudd; Vandna Munshi; Carolyn Bahnck; Peter J Felock; Meiquing Lu; Ming-Tain Lai; Sinoeun Touch; Gregory Moyer; Daniel J Distefano; Jessica A Flynn; Yuexia Liang; Rosa Sanchez; Rebecca Perlow-Poehnelt; Mike Miller; Joseph P Vacca; Theresa M Williams; Neville J Anthony
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
Bioorganic & medicinal chemistry letters 2010;20(15):4328-32.
2010: Kristen L G Jones; M Katharine Holloway; Hua-Poo Su; Steven S Carroll; Christine Burlein; Sinoeun Touch; Daniel J DiStefano; Rosa I Sanchez; Theresa M Williams; Joseph P Vacca; Craig A Coburn
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(14):4065-8.
2010: Craig A Stump; Ian M Bell; Rodney A Bednar; John F Fay; Steven N Gallicchio; James C Hershey; Richard Jelley; Constantine Kreatsoulas; Eric L Moore; Scott D Mosser; Amy G Quigley; Shane A Roller; Christopher A Salvatore; Steven S Sharik; Cory R Theberge; C Blair Zartman; Stefanie A Kane; Samuel L Graham; Harold G Selnick; Joseph P Vacca; Theresa M Williams
Identification of potent, highly constrained CGRP receptor antagonists.
Bioorganic & medicinal chemistry letters 2010;20(8):2572-6.
2010: Christopher A Salvatore; Eric L Moore; Amy Calamari; Jacquelynn J Cook; Maria S Michener; Stacey O'Malley; Patricia J Miller; Cyrille Sur; David L Williams; Zhizhen Zeng; Andrew Danziger; Joseph J Lynch; Christopher P Regan; John F Fay; Yui S Tang; Chi-Chung Li; Nicole T Pudvah; Rebecca B White; Ian M Bell; Steven N Gallicchio; Samuel L Graham; Harold G Selnick; Joseph P Vacca; Stefanie A Kane
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
The Journal of pharmacology and experimental therapeutics 2010;333(1):152-60.
2010: John A McCauley; Charles J McIntyre; Michael T Rudd; Kevin T Nguyen; Joseph J Romano; John W Butcher; Kevin F Gilbert; Kimberly J Bush; M Katharine Holloway; John Swestock; Bang-Lin Wan; Steven S Carroll; Jillian DiMuzio; Donald J Graham; Steven W Ludmerer; Shi-Shan Mao; Mark W Stahlhut; Christine M Fandozzi; Nicole Trainor; David B Olsen; Joseph P Vacca; Nigel J Liverton
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
Journal of medicinal chemistry 2010;53(6):2443-63.
2010: Hemaka A Rajapakse; Philippe G Nantermet; Harold G Selnick; James C Barrow; Georgia B McGaughey; Sanjeev Munshi; Stacey R Lindsley; Mary Beth Young; Phung L Ngo; M Katharine Holloway; Ming-Tain Lai; Amy S Espeseth; Xiao-Ping Shi; Dennis Colussi; Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Qian Huang; Min Xu; Adam J Simon; Lawrence Kuo; Daria J Hazuda; Samuel Graham; Joseph P Vacca
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Bioorganic & medicinal chemistry letters 2010;20(6):1885-9.
2010: Hong Zhu; Mary Beth Young; Philippe G Nantermet; Samuel L Graham; Dennis Colussi; Ming-Tain Lai; Beth L Pietrak; Eric A Price; Sethu Sankaranarayanan; Xiao-Ping Shi; Katherine Tugusheva; Marie A Holahan; Maria S Michener; Jacquelynn J Cook; Adam Simon; Daria J Hazuda; Joseph P Vacca; Hemaka A Rajapakse
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(5):1779-82.
2010: Nigel J Liverton; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Donald J Graham; Daria J Hazuda; M Katherine Holloway; Steven W Ludmerer; John A McCauley; Charles J McIntyre; David B Olsen; Michael T Rudd; Mark Stahlhut; Joseph P Vacca
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Antimicrobial agents and chemotherapy 2010;54(1):305-11.
2009: Dai-Shi Su; John J Lim; Elizabeth Tinney; Bang-Lin Wan; Mary Beth Young; Kenneth D Anderson; Deanne Rudd; Vandna Munshi; Carolyn Bahnck; Peter J Felock; Meiquing Lu; Ming-Tain Lai; Sinoeun Touch; Gregory Moyer; Daniel J DiStefano; Jessica A Flynn; Yuexia Liang; Rosa Sanchez; Rebecca Perlow-Poehnelt; Mike Miller; Joseph P Vacca; Theresa M Williams; Neville J Anthony
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
Journal of medicinal chemistry 2009;52(22):7163-9.
2009: Christopher S Burgey; Craig M Potteiger; James Z Deng; Scott D Mosser; Christopher A Salvatore; Sean Yu; Shane Roller; Stefanie A Kane; Joseph P Vacca; Theresa M Williams
Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Bioorganic & medicinal chemistry letters 2009;19(22):6368-72.
2009: Michael R Wood; Kathy M Schirripa; June J Kim; Amy G Quigley; Craig A Stump; Ian M Bell; Rodney A Bednar; John F Fay; Joseph G Bruno; Eric L Moore; Scott D Mosser; Shane Roller; Christopher A Salvatore; Stefanie A Kane; Joseph P Vacca; Harold G Selnick
Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.
Bioorganic & medicinal chemistry letters 2009;19(19):5787-90.
2009: Dai-Shi Su; John J Lim; Elizabeth Tinney; Bang-Lin Wan; Mary Beth Young; Kenneth D Anderson; Deanne Rudd; Vandna Munshi; Carolyn Bahnck; Peter J Felock; Meiqing Lu; Ming-Tain Lai; Sinoeun Touch; Gregory Moyer; Daniel J Distefano; Jessica A Flynn; Yuexia Liang; Rosa Sanchez; Sridhar Prasad; Youwei Yan; Rebecca Perlow-Poehnelt; Maricel Torrent; Mike Miller; Joseph P Vacca; Theresa M Williams; Neville J Anthony
Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.
Bioorganic & medicinal chemistry letters 2009;19(17):5119-23.
2009: Ian M Bell; Rodney A Bednar; Halea A Corcoran; John F Fay; Steven N Gallicchio; Victor K Johnston; James C Hershey; Cynthia Miller-Stein; Eric L Moore; Scott D Mosser; Shane A Roller; Christopher A Salvatore; Cory R Theberge; Bradley K Wong; C Blair Zartman; Stefanie A Kane; Theresa M Williams; Samuel L Graham; Joseph P Vacca
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Bioorganic & medicinal chemistry letters 2009;19(16):4740-2.
2009: Shawn J Stachel; Craig A Coburn; Diane M Rush; Kristen L G Jones; Hong Zhu; Hemaka Rajapakse; Samuel L Graham; Adam Simon; M Katharine Holloway; Timothy Allison; Sanjeev Munshi; Amy S Espeseth; Paul Zuck; Dennis Colussi; Abigail Wolfe; Beth L Pietrak; Ming-Tain Lai; Joseph P Vacca
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Bioorganic & medicinal chemistry letters 2009;19(11):2977-80.
2009: Philippe G Nantermet; Hemaka A Rajapakse; Mathew G Stanton; Shaun R Stauffer; James C Barrow; Allison R Gregro; Keith P Moore; Melissa A Steinbeiser; John Swestock; Harold G Selnick; Samuel L Graham; Georgia B McGaughey; Dennis Colussi; Ming-Tain Lai; Sethu Sankaranarayanan; Adam J Simon; Sanjeev Munshi; Jacquelynn J Cook; Marie A Holahan; Maria S Michener; Joseph P Vacca
Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.
ChemMedChem 2009;4(1):37-40.
2009: Craig A Stump; Ian M Bell; Rodney A Bednar; Joseph G Bruno; John F Fay; Steven N Gallicchio; Victor K Johnston; Eric L Moore; Scott D Mosser; Amy G Quigley; Christopher A Salvatore; Cory R Theberge; C Blair Zartman; Xu-Fang Zhang; Stefanie A Kane; Samuel L Graham; Joseph P Vacca; Theresa M Williams
The discovery of highly potent CGRP receptor antagonists.
Bioorganic & medicinal chemistry letters 2009;19(1):214-7.
2008: Cory R Theberge; Rodney A Bednar; Ian M Bell; Halea A Corcoran; John F Fay; James C Hershey; Victor K Johnston; Stefanie A Kane; Scott Mosser; Christopher A Salvatore; Theresa M Williams; C Blair Zartman; Xu-Fang Zhang; Samuel L Graham; Joseph P Vacca
Potent benzimidazolone-based CGRP receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(23):6122-5.
2008: Thomas J Tucker; John T Sisko; Robert M Tynebor; Theresa M Williams; Peter J Felock; Jessica A Flynn; Ming-Tain Lai; Yuexia Liang; Georgia B McGaughey; Meiquing Liu; Mike Miller; Gregory Moyer; Vandna Munshi; Rebecca Perlow-Poehnelt; Sridhar Prasad; John C Reid; Rosa Sanchez; Maricel Torrent; Joseph P Vacca; Bang-Lin Wan; Youwei Yan
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Journal of medicinal chemistry 2008;51(20):6503-11.
2008: James C Barrow; Shaun R Stauffer; Kenneth E Rittle; Phung L Ngo; ZhiQiang Yang; Harold G Selnick; Samuel L Graham; Sanjeev Munshi; Georgia B McGaughey; M Katharine Holloway; Adam J Simon; Eric A Price; Sethu Sankaranarayanan; Dennis Colussi; Katherine Tugusheva; Ming-Tain Lai; Amy S Espeseth; Min Xu; Qian Huang; Abigail Wolfe; Beth Pietrak; Paul Zuck; Dorothy A Levorse; Daria J Hazuda; Joseph P Vacca
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Journal of medicinal chemistry 2008;51(20):6259-62.
2008: Jeffrey Y Melamed; Melissa S Egbertson; Sandor L Varga; Joseph P Vacca; Gregory Moyer; Lori Gabryelski; Peter J Felock; Kara A Stillmock; Marc V Witmer; William A Schleif; Daria J Hazuda; Yvonne M Leonard; Lixia Jin; Joan D Ellis; Steven D Young
Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Bioorganic & medicinal chemistry letters 2008;18(19):5307-10.
2008: Catherine M Wiscount; Peter D Williams; Lekhanh O Tran; Mark W Embrey; Thorsten E Fisher; Vanessa Sherman; Carl F Homnick; D Donnette Staas; Terry A Lyle; John S Wai; Joseph P Vacca; ZiQiang Wang; Peter J Felock; Kara A Stillmock; Marc V Witmer; Michael D Miller; Daria J Hazuda; Alysha M Day; Lori Gabryelski; Linda T Ecto; William A Schleif; Daniel J DiStefano; Christopher J Kochansky; M Reza Anari
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Bioorganic & medicinal chemistry letters 2008;18(16):4581-3.
2008: Thomas J Tucker; Sandeep Saggar; John T Sisko; Robert M Tynebor; Theresa M Williams; Peter J Felock; Jessica A Flynn; Ming-Tain Lai; Yuexia Liang; Georgia B McGaughey; Meiquing Liu; Mike Miller; Gregory Moyer; Vandna Munshi; Rebecca Perlow-Poehnelt; Sridhar Prasad; Rosa Sanchez; Maricel Torrent; Joseph P Vacca; Bang-Lin Wan; Youwei Yan
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Bioorganic & medicinal chemistry letters 2008;18(9):2959-66.
2008: Nigel J Liverton; M Katharine Holloway; John A McCauley; Michael T Rudd; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Kevin F Gilbert; Shi-Shan Mao; Charles J McIntyre; Kevin T Nguyen; Joseph J Romano; Mark Stahlhut; Bang-Lin Wan; David B Olsen; Joseph P Vacca
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease.
Journal of the American Chemical Society 2008;130(14):4607-9.
2008: Christopher A Salvatore; James C Hershey; Halea A Corcoran; John F Fay; Victor K Johnston; Eric L Moore; Scott D Mosser; Christopher S Burgey; Daniel V Paone; Anthony W Shaw; Samuel L Graham; Joseph P Vacca; Theresa M Williams; Kenneth S Koblan; Stefanie A Kane
Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
The Journal of pharmacology and experimental therapeutics 2008;324(2):416-21.
2008: Zhijian Zhao; Scott E Wolkenberg; Philip E J Sanderson; Meiqing Lu; Vandna Munshi; Gregory Moyer; Meizhen Feng; Anthony V Carella; Linda T Ecto; Lori Gabryelski; Ming-Tain Lai; Sridar G Prasad; Youwei Yan; Georgia B McGaughey; Michael D Miller; Craig W Lindsley; George D Hartman; Joseph P Vacca; Theresa M Williams
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Bioorganic & medicinal chemistry letters 2008;18(2):554-9.
2008: H Marie Langford; Peter D Williams; Carl F Homnick; Joseph P Vacca; Peter J Felock; Kara A Stillmock; Marc V Witmer; Daria J Hazuda; Lori Gabryelski; William A Schleif
Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(2):721-5.
2008: Diem N Nguyen; Daniel V Paone; Anthony W Shaw; Christopher S Burgey; Scott D Mosser; Victor Johnston; Christopher A Salvatore; Yvonne M Leonard; Cynthia Miller-Stein; Stefanie A Kane; Kenneth S Koblan; Joseph P Vacca; Samuel L Graham; Theresa M Williams
Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.
Bioorganic & medicinal chemistry letters 2008;18(2):755-8.
2008: John A McCauley; Michael T Rudd; Kevin T Nguyen; Charles J McIntyre; Joseph J Romano; Kimberly J Bush; Sandor L Varga; Charles W Ross; Steven S Carroll; Jillian DiMuzio; Mark W Stahlhut; David B Olsen; Terry A Lyle; Joseph P Vacca; Nigel J Liverton
Bismacrocyclic inhibitors of hepatitis C NS3/4a protease.
Angewandte Chemie (International ed. in English) 2008;47(47):9104-7.
2007: Thorsten E Fisher; Boyoung Kim; Donnette D Staas; Terry A Lyle; Steven D Young; Joseph P Vacca; Matthew M Zrada; Daria J Hazuda; Peter J Felock; William A Schleif; Lori Gabryelski; M Reza Anari; Christopher J Kochansky; John S Wai
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(23):6511-5.
2007: Daniel V Paone; Anthony W Shaw; Diem N Nguyen; Christopher S Burgey; James Z Deng; Stefanie A Kane; Kenneth S Koblan; Christopher A Salvatore; Scott D Mosser; Victor K Johnston; Bradley K Wong; Cynthia Miller-Stein; James C Hershey; Samuel L Graham; Joseph P Vacca; Theresa M Williams
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
Journal of medicinal chemistry 2007;50(23):5564-7.
2007: Keith P Moore; Hong Zhu; Hemaka A Rajapakse; Georgia B McGaughey; Dennis Colussi; Eric A Price; Sethu Sankaranarayanan; Adam J Simon; Nicole T Pudvah; Jerome H Hochman; Timothy Allison; Sanjeev Munshi; Samuel L Graham; Joseph P Vacca; Philippe G Nantermet
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(21):5831-5.
2007: John S Wai; Boyoung Kim; Thorsten E Fisher; Linghang Zhuang; Mark W Embrey; Peter D Williams; Donnette D Staas; Chris Culberson; Terry A Lyle; Joseph P Vacca; Daria J Hazuda; Peter J Felock; William A Schleif; Lori Gabryelski; Lixia Jin; I-Wu Chen; Joan D Ellis; Rama Mallai; Steven D Young
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(20):5595-9.
2007: Anthony W Shaw; Daniel V Paone; Diem N Nguyen; Craig A Stump; Christopher S Burgey; Scott D Mosser; Christopher A Salvatore; Ruth Z Rutledge; Stefanie A Kane; Kenneth S Koblan; Samuel L Graham; Joseph P Vacca; Theresa M Williams
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
Bioorganic & medicinal chemistry letters 2007;17(17):4795-8.
2007: Matthew G Stanton; Shaun R Stauffer; Alison R Gregro; Melissa A Steinbeiser; Philippe G Nantermet; Sethu Sankaranarayanan; Eric A Price; Guoxin Wu; Ming-Chih Crouthamel; Joan Ellis; Ming-Tain Lai; Amy S Espeseth; Xiao-Ping Shi; Lixia Jin; Dennis Colussi; Beth L Pietrak; Qian Huang; Min Xu; Adam J Simon; Samuel L Graham; Joseph P Vacca; Harold G Selnick
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
Journal of medicinal chemistry 2007;50(15):3431-3.
2007: Stacey R Lindsley; Keith P Moore; Hemaka A Rajapakse; Harold G Selnick; Mary Beth Young; Hong Zhu; Sanjeev Munshi; Lawrence Kuo; Georgia B McGaughey; Dennis Colussi; Ming-Chih Crouthamel; Ming-Tain Lai; Beth L Pietrak; Eric A Price; Sethu Sankaranarayanan; Adam J Simon; Guy R Seabrook; Daria J Hazuda; Nicole T Pudvah; Jerome H Hochman; Samuel L Graham; Joseph P Vacca; Philippe G Nantermet
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(14):4057-61.
2007: Ivory D Hills; Joseph P Vacca
Progress toward a practical BACE-1 inhibitor.
Current opinion in drug discovery & development 2007;10(4):383-91.
2007: James C Barrow; Kenneth E Rittle; Phung L Ngo; Harold G Selnick; Samuel L Graham; Steven M Pitzenberger; Georgia B McGaughey; Dennis Colussi; Ming-Tain Lai; Qian Huang; Katherine Tugusheva; Amy S Espeseth; Adam J Simon; Sanjeev K Munshi; Joseph P Vacca
Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1.
ChemMedChem 2007;2(7):995-9.
2007: Shaun R Stauffer; Matthew G Stanton; Alison R Gregro; Melissa A Steinbeiser; Jennifer R Shaffer; Philippe G Nantermet; James C Barrow; Kenneth E Rittle; Dennis Collusi; Amy S Espeseth; Ming-Tain Lai; Beth L Pietrak; M Katharine Holloway; Georgia B McGaughey; Sanjeev Munshi; Jerome H Hochman; Adam J Simon; Harold G Selnick; Samuel L Graham; Joseph P Vacca
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.
Bioorganic & medicinal chemistry letters 2007;17(6):1788-92.
2007: Melissa S Egbertson; H Marie Moritz; Jeffrey Y Melamed; Wei Han; Debra S Perlow; Michelle Kuo; Mark W Embrey; Joseph P Vacca; Matthew M Zrada; Amanda R Cortes; Audrey Wallace; Yvonne M Leonard; Daria J Hazuda; Michael D Miller; Peter J Felock; Kara A Stillmock; Marc V Witmer; William A Schleif; Lori Gabryelski; Gregory Moyer; Joan D Ellis; Lixia Jin; Wei Xu; Matthew P Braun; Kelem Kassahun; Nancy N Tsou; Steven D Young
A potent and orally active HIV-1 integrase inhibitor.
Bioorganic & medicinal chemistry letters 2007;17(5):1392-8.
2006: Ian M Bell; Rodney A Bednar; John F Fay; Steven N Gallicchio; Jerome H Hochman; Daniel R McMasters; Cynthia Miller-Stein; Eric L Moore; Scott D Mosser; Nicole T Pudvah; Amy G Quigley; Christopher A Salvatore; Craig A Stump; Cory R Theberge; Bradley K Wong; C Blair Zartman; Xu-Fang Zhang; Stefanie A Kane; Samuel L Graham; Joseph P Vacca; Theresa M Williams
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(24):6165-9.
2006: Hemaka A Rajapakse; Philippe G Nantermet; Harold G Selnick; Sanjeev Munshi; Georgia B McGaughey; Stacey R Lindsley; Mary Beth Young; Ming-Tain Lai; Amy S Espeseth; Xiao-Ping Shi; Dennis Colussi; Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Qian Huang; Min Xu; Adam J Simon; Lawrence Kuo; Daria J Hazuda; Samuel Graham; Joseph P Vacca
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Journal of medicinal chemistry 2006;49(25):7270-3.
2006: Shawn J Stachel; Craig A Coburn; Sethu Sankaranarayanan; Eric A Price; Guoxin Wu; Ming-Chih Crouthamel; Beth L Pietrak; Qian Huang; Janet Lineberger; Amy S Espeseth; Lixia Jin; Joan Ellis; M Katharine Holloway; Sanjeev Munshi; Timothy Allison; Daria J Hazuda; Adam J Simon; Samuel L Graham; Joseph P Vacca
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Journal of medicinal chemistry 2006;49(21):6147-50.
2006: Donnette D Staas; Kelly L Savage; Vanessa L Sherman; Heidi L Shimp; Terry A Lyle; Lekhanh O Tran; Catherine M Wiscount; Daniel R McMasters; Philip E J Sanderson; Peter D Williams; Bobby J Lucas; Julie A Krueger; S Dale Lewis; Rebecca B White; Sean Yu; Bradley K Wong; Christopher J Kochansky; M Reza Anari; Youwei Yan; Joseph P Vacca
Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.
Bioorganic & medicinal chemistry 2006;14(20):6900-16.
2006: Christopher S Burgey; Craig A Stump; Diem N Nguyen; James Z Deng; Amy G Quigley; Beth R Norton; Ian M Bell; Scott D Mosser; Christopher A Salvatore; Ruth Z Rutledge; Stefanie A Kane; Kenneth S Koblan; Joseph P Vacca; Samuel L Graham; Theresa M Williams
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Bioorganic & medicinal chemistry letters 2006;16(19):5052-6.
2006: Craig A Coburn; Shawn J Stachel; Kristen G Jones; Thomas G Steele; Diane M Rush; Jillian DiMuzio; Beth L Pietrak; Ming-Tain Lai; Qian Huang; Janet Lineberger; Lixia Jin; Sanjeev Munshi; M Katharine Holloway; Amy S Espeseth; Adam Simon; Daria J Hazuda; Samuel L Graham; Joseph P Vacca
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Bioorganic & medicinal chemistry letters 2006;16(14):3635-8.
2006: James P Guare; John S Wai; Robert P Gomez; Neville J Anthony; Samson M Jolly; Amanda R Cortes; Joseph P Vacca; Peter J Felock; Kara A Stillmock; William A Schleif; Gregory Moyer; Lori Gabryelski; Lixia Jin; I-Wu Chen; Daria J Hazuda; Steven D Young
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(11):2900-4.
2006: Theresa M Williams; Craig A Stump; Diem N Nguyen; Amy G Quigley; Ian M Bell; Steven N Gallicchio; C Blair Zartman; Bang-Lin Wan; Kimberly Della Penna; Priya Kunapuli; Stefanie A Kane; Kenneth S Koblan; Scott D Mosser; Ruth Z Rutledge; Christopher A Salvatore; John F Fay; Joseph P Vacca; Samuel L Graham
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Bioorganic & medicinal chemistry letters 2006;16(10):2595-8.
2006: Shawn J Stachel; Craig A Coburn; Thomas G Steele; Ming-Chih Crouthamel; Beth L Pietrak; Ming-Tain Lai; M Katharine Holloway; Sanjeev Munshi; Samuel L Graham; Joseph P Vacca
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(3):641-4.
2005: James Z Deng; Daniel R McMasters; Philippe M A Rabbat; Peter D Williams; Craig A Coburn; Youwei Yan; Lawrence C Kuo; S Dale Lewis; Bobby J Lucas; Julie A Krueger; Berta Strulovici; Joseph P Vacca; Terry A Lyle; Christopher S Burgey
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.
Bioorganic & medicinal chemistry letters 2005;15(20):4411-6.
2005: Mark W Embrey; John S Wai; Timothy W Funk; Carl F Homnick; Debra S Perlow; Steven D Young; Joseph P Vacca; Daria J Hazuda; Peter J Felock; Kara A Stillmock; Marc V Witmer; Gregory Moyer; William A Schleif; Lori Gabryelski; Lixia Jin; I-Wu Chen; Joan D Ellis; Bradley K Wong; Jiunn H Lin; Yvonne M Leonard; Nancy N Tsou; Linghang Zhuang
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Bioorganic & medicinal chemistry letters 2005;15(20):4550-4.
2005: Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Janet Lineberger; Min Xu; Jillian DiMuzio; Thomas G Steele; Amy S Espeseth; Shawn J Stachel; Craig A Coburn; Samuel L Graham; Joseph P Vacca; Xiao-Ping Shi; Adam J Simon; Daria J Hazuda; Ming-Tain Lai
Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
Analytical biochemistry 2005;342(1):144-51.
2005: Philippe G Nantermet; Christopher S Burgey; Kyle A Robinson; Janetta M Pellicore; Christina L Newton; James Z Deng; Harold G Selnick; S Dale Lewis; Bobby J Lucas; Julie A Krueger; Cynthia Miller-Stein; Rebecca B White; Bradley Wong; Daniel R McMasters; Audrey A Wallace; Joseph J Lynch; Youwei Yan; Zhongguo Chen; Lawrence Kuo; Stephen J Gardell; Jules A Shafer; Joseph P Vacca; Terry A Lyle
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Bioorganic & medicinal chemistry letters 2005;15(11):2771-5.
2004: Shawn J Stachel; Craig A Coburn; Thomas G Steele; Kristen G Jones; Elizabeth F Loutzenhiser; Alison R Gregro; Hemaka A Rajapakse; Ming-Tain Lai; Ming-Chih Crouthamel; Min Xu; Katherine Tugusheva; Janet Lineberger; Beth L Pietrak; Amy S Espeseth; Xiao-Ping Shi; Elizabeth Chen-Dodson; M Katharine Holloway; Sanjeev Munshi; Adam J Simon; Lawrence Kuo; Joseph P Vacca
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Journal of medicinal chemistry 2004;47(26):6447-50.
2004: Craig A Coburn; Shawn J Stachel; Yueming Li; Diane M Rush; Thomas G Steele; Elizabeth Chen-Dodson; M Katharine Holloway; Min Xu; Qian Huang; Ming-Tain Lai; Jillian DiMuzio; Ming-Chih Crouthamel; Xiao-Ping Shi; Vinod Sardana; Zhongguo Chen; Sanjeev Munshi; Lawrence Kuo; Gergely M Makara; D Allen Annis; Praveen K Tadikonda; Huw M Nash; Joseph P Vacca; Tong Wang
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
Journal of medicinal chemistry 2004;47(25):6117-9.
2004: Matthew M Morrissette; Kenneth J Stauffer; Peter D Williams; Terry A Lyle; Joseph P Vacca; Julie A Krueger; S Dale Lewis; Bobby J Lucas; Bradley K Wong; Rebecca B White; Cynthia Miller-Stein; Elizabeth A Lyle; Audrey A Wallace; Yvonne M Leonard; Denise C Welsh; Joseph J Lynch; Daniel R McMasters
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Bioorganic & medicinal chemistry letters 2004;14(16):4161-4.
2004: Daria J Hazuda; Steven D Young; James P Guare; Neville J Anthony; Robert P Gomez; John S Wai; Joseph P Vacca; Larry Handt; Sherri L Motzel; Hilton J Klein; Geethanjali Dornadula; Robert M Danovich; Marc V Witmer; Keith A Wilson; Lynda Tussey; William A Schleif; Lori S Gabryelski; Lixia Jin; Michael D Miller; Danilo R Casimiro; Emilio A Emini; John W Shiver
Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques.
Science (New York, N.Y.) 2004;305(5683):528-32.
2004: Mary Beth Young; James C Barrow; Kristen L Glass; George F Lundell; Christina L Newton; Janetta M Pellicore; Kenneth E Rittle; Harold G Selnick; Kenneth J Stauffer; Joseph P Vacca; Peter D Williams; Dennis Bohn; Franklin C Clayton; Jacquelynn J Cook; Julie A Krueger; Lawrence C Kuo; S Dale Lewis; Bobby J Lucas; Daniel R McMasters; Cynthia Miller-Stein; Beth L Pietrak; Audrey A Wallace; Rebecca B White; Bradley Wong; Youwei Yan; Philippe G Nantermet
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
Journal of medicinal chemistry 2004;47(12):2995-3008.
2004: Philippe G Nantermet; James C Barrow; Stacey R Lindsley; MaryBeth Young; Shi-Shan Mao; Steven Carroll; Carolyn Bailey; Michele Bosserman; Dennis Colussi; Daniel R McMasters; Joseph P Vacca; Harold G Selnick
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Bioorganic & medicinal chemistry letters 2004;14(9):2141-5.
2004: Stephen F Brady; Satendra Singh; Ming-Chih Crouthamel; M Katharine Holloway; Craig A Coburn; Victor M Garsky; Michael J Bogusky; Michael Pennington; Joseph P Vacca; Daria J Hazuda; Ming-Tain Lai
Rational design and synthesis of selective BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(3):601-4.
2003: James C Barrow; Philippe G Nantermet; Shaun R Stauffer; Phung L Ngo; Melissa A Steinbeiser; Shi-Shan Mao; Steven S Carroll; Carolyn Bailey; Dennis Colussi; Michele Bosserman; Christine Burlein; Jacquelynn J Cook; Gary R Sitko; Philip R Tiller; Cynthia Miller-Stein; Mark Rose; Daniel R McMasters; Joseph P Vacca; Harold G Selnick
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
Journal of medicinal chemistry 2003;46(25):5294-7.
2003: Kenneth E Rittle; James C Barrow; Kellie J Cutrona; Kristen L Glass; Julie A Krueger; Lawrence C Kuo; S Dale Lewis; Bobby J Lucas; Daniel R McMasters; Matthew M Morrissette; Philippe G Nantermet; Christina L Newton; William M Sanders; Youwei Yan; Joseph P Vacca; Harold G Selnick
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Bioorganic & medicinal chemistry letters 2003;13(20):3477-82.
2003: Philippe G Nantermet; James C Barrow; Christina L Newton; Janetta M Pellicore; MaryBeth Young; S Dale Lewis; Bobby J Lucas; Julie A Krueger; Daniel R McMasters; Youwei Yan; Lawrence C Kuo; Joseph P Vacca; Harold G Selnick
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Bioorganic & medicinal chemistry letters 2003;13(16):2781-4.
2003: Christopher S Burgey; Kyle A Robinson; Terry A Lyle; Philippe G Nantermet; Harold G Selnick; Richard C A Isaacs; S Dale Lewis; Bobby J Lucas; Julie A Krueger; Rominder Singh; Cynthia Miller-Stein; Rebecca B White; Bradley Wong; Elizabeth A Lyle; Maria T Stranieri; Jacquelynn J Cook; Daniel R McMasters; Janetta M Pellicore; Swati Pal; Audrey A Wallace; Franklin C Clayton; Dennis Bohn; Denise C Welsh; Joseph J Lynch; Youwei Yan; Zhongguo Chen; Lawrence Kuo; Stephen J Gardell; Jules A Shafer; Joseph P Vacca
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Bioorganic & medicinal chemistry letters 2003;13(7):1353-7.
2003: Linghang Zhuang; John S Wai; Mark W Embrey; Thorsten E Fisher; Melissa S Egbertson; Linda S Payne; James P Guare; Joseph P Vacca; Daria J Hazuda; Peter J Felock; Abigail L Wolfe; Kara A Stillmock; Marc V Witmer; Gregory Moyer; William A Schleif; Lori Gabryelski; Yvonne M Leonard; Joseph J Lynch; Stuart R Michelson; Steven D Young
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Journal of medicinal chemistry 2003;46(4):453-6.
2002: Jay A Grobler; Kara A Stillmock; Binghua Hu; Marc V Witmer; Peter J Felock; Amy S Espeseth; Abigail Wolfe; Melissa S Egbertson; Michele Bourgeois; Jeffrey Y Melamed; John S Wai; Steve Young; Joseph P Vacca; Daria J Hazuda
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.
Proceedings of the National Academy of Sciences of the United States of America 2002;99(10):6661-6.
2000: John S Wai; Melissa S Egbertson; L S Payne; Thorsten E Fisher; Mark W Embrey; L O Tran; Jeffrey Y Melamed; H M Langford; James P Guare; Linghang Zhuang; V E Grey; Joseph P Vacca; M Katharine Holloway; Adel M Naylor-Olsen; Daria J Hazuda; Peter J Felock; Abigail L Wolfe; Kara A Stillmock; William A Schleif; Lori Gabryelski; Steven D Young
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Journal of medicinal chemistry 2000;43(26):4923-6.
2000: Bruce D Dorsey; Colleen McDonough; S L McDaniel; R B Levin; Christina L Newton; J M Hoffman; Paul L Darke; Joan Zugay-Murphy; Emilio A Emini; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Jiunn H Lin; I-Wu Chen; Stuart R Michelson; M Katharine Holloway; Joel R Huff; Joseph P Vacca
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry 2000;43(18):3386-99.
2000: Joseph P Vacca
New advances in the discovery of thrombin and factor Xa inhibitors.
Current opinion in chemical biology 2000;4(4):394-400.
2000: Craig A Coburn; Diane M Rush; Peter D Williams; Carl F Homnick; Elizabeth A Lyle; S Dale Lewis; Bobby J Lucas; J M Di Muzio-Mower; M Juliano; Julie A Krueger; KJ Vastag; I-Wu Chen; Joseph P Vacca
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.
Bioorganic & medicinal chemistry letters 2000;10(10):1069-72.
1999: Nigel J Liverton; John W Butcher; Christopher F Claiborne; David A Claremon; Brian E Libby; Kevin T Nguyen; Steven M Pitzenberger; Harold G Selnick; Garry R Smith; Andrew J Tebben; Joseph P Vacca; Sandor L Varga; L Agarwal; KB Dancheck; A J Forsyth; Daniel S Fletcher; B Frantz; William A Hanlon; C F Harper; S J Hofsess; M Kostura; J Lin; Silvi Luell; Edward A O'Neill; Stephen J O'Keefe
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Journal of medicinal chemistry 1999;42(12):2180-90.
1999: Jacquelynn J Cook; Stephen J Gardell; Marie A Holahan; Gary R Sitko; Gary L Stump; Audrey A Wallace; David B Gilberto; TR Hare; Julie A Krueger; Dona L Dyer; Philip E J Sanderson; Joseph P Vacca; Jules A Shafer; Joseph J Lynch
Antithrombotic efficacy of thrombin inhibitor L-374,087: intravenous activity in a primate model of venous thrombus extension and oral activity in a canine model of primary venous and coronary artery thrombosis.
The Journal of pharmacology and experimental therapeutics 1999;289(1):503-10.
1998: Philip E J Sanderson; Terry A Lyle; Kellie J Cutrona; Dona L Dyer; Bruce D Dorsey; Colleen McDonough; Adel M Naylor-Olsen; I-Wu Chen; Zhongguo Chen; Jacquelynn J Cook; CM Cooper; Stephen J Gardell; TR Hare; Julie A Krueger; S Dale Lewis; Jiunn H Lin; Bobby J Lucas; Elizabeth A Lyle; Joseph J Lynch; Maria T Stranieri; KJ Vastag; Youwei Yan; Jules A Shafer; Joseph P Vacca
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Journal of medicinal chemistry 1998;41(23):4466-74.
1998: Thomas J Tucker; Stephen F Brady; William C Lumma; S Dale Lewis; Stephen J Gardell; Adel M Naylor-Olsen; Youwei Yan; John T Sisko; Kenneth J Stauffer; Bobby J Lucas; Joseph J Lynch; Jacquelynn J Cook; Maria T Stranieri; Marie A Holahan; Elizabeth A Lyle; Elizabeth P Baskin; I-Wu Chen; KB Dancheck; Julie A Krueger; CM Cooper; Joseph P Vacca
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Journal of medicinal chemistry 1998;41(17):3210-9.
1998: M Chiba; JA Nishime; I-Wu Chen; KJ Vastag; Y S Sahly; B M Kim; Bruce D Dorsey; Joseph P Vacca; Jiunn H Lin
Metabolite-P450 complex formation by methylenedioxyphenyl HIV protease inhibitors in rat and human liver microsomes.
Biochemical pharmacology 1998;56(2):223-30.
1998: Richard C A Isaacs; Kellie J Cutrona; Christina L Newton; Philip E J Sanderson; Mark G Solinsky; Elizabeth P Baskin; I-Wu Chen; CM Cooper; Jacquelynn J Cook; Stephen J Gardell; S Dale Lewis; R J Lucas; Elizabeth A Lyle; Joseph J Lynch; Adel M Naylor-Olsen; Maria T Stranieri; KJ Vastag; Joseph P Vacca
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Bioorganic & medicinal chemistry letters 1998;8(13):1719-24.
1998: Adel M Naylor-Olsen; Gerald S Ponticello; S Dale Lewis; AM Mulichak; Zhongguo Chen; C N Habecker; B T Phillips; William M Sanders; Thomas J Tucker; Jules A Shafer; Joseph P Vacca
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.
Bioorganic & medicinal chemistry letters 1998;8(13):1697-702.
1998: Philip E J Sanderson; Kellie J Cutrona; Bruce D Dorsey; Dona L Dyer; Colleen McDonough; Adel M Naylor-Olsen; I-Wu Chen; Zhongguo Chen; Jacquelynn J Cook; Stephen J Gardell; Julie A Krueger; S Dale Lewis; Jiunn H Lin; Bobby J Lucas; Elizabeth A Lyle; Joseph J Lynch; Maria T Stranieri; KJ Vastag; Jules A Shafer; Joseph P Vacca
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Bioorganic & medicinal chemistry letters 1998;8(7):817-22.
1998: William C Lumma; KM Witherup; Thomas J Tucker; Stephen F Brady; John T Sisko; Adel M Naylor-Olsen; S Dale Lewis; Bobby J Lucas; Joseph P Vacca
Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.
Journal of medicinal chemistry 1998;41(7):1011-3.
1998: Stephen F Brady; Kenneth J Stauffer; William C Lumma; G M Smith; Harri G Ramjit; S Dale Lewis; Bobby J Lucas; Stephen J Gardell; Elizabeth A Lyle; SD Appleby; Jacquelynn J Cook; Marie A Holahan; Maria T Stranieri; Joseph J Lynch; Jiunn H Lin; I-Wu Chen; KJ Vastag; Adel M Naylor-Olsen; Joseph P Vacca
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Journal of medicinal chemistry 1998;41(3):401-6.
1997: Dong-Mei Feng; Stephen J Gardell; S Dale Lewis; Mark G Bock; Zhongguo Chen; Roger M Freidinger; Adel M Naylor-Olsen; Harri G Ramjit; RF Woltmann; Elizabeth P Baskin; Joseph J Lynch; R Lucas; Jules A Shafer; KB Dancheck; I-Wu Chen; Shi-Shan Mao; Julie A Krueger; TR Hare; AM Mulichak; Joseph P Vacca
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Journal of medicinal chemistry 1997;40(23):3726-33.
1997: Thomas J Tucker; William C Lumma; S Dale Lewis; Stephen J Gardell; Bobby J Lucas; John T Sisko; Joseph J Lynch; Elizabeth A Lyle; Elizabeth P Baskin; RF Woltmann; SD Appleby; I-Wu Chen; KB Dancheck; Adel M Naylor-Olsen; Julie A Krueger; CM Cooper; Joseph P Vacca
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Journal of medicinal chemistry 1997;40(22):3687-93.
1997: Thomas J Tucker; William C Lumma; S Dale Lewis; Stephen J Gardell; Bobby J Lucas; Elizabeth P Baskin; RF Woltmann; Joseph J Lynch; Elizabeth A Lyle; SD Appleby; I-Wu Chen; KB Dancheck; Joseph P Vacca
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.
Journal of medicinal chemistry 1997;40(11):1565-9.
1995: M K Holloway; J M Wai; T A Halgren; P M Fitzgerald; Joseph P Vacca; Bruce D Dorsey; R B Levin; W J Thompson; L J Chen; S Jane deSolms
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Journal of medicinal chemistry 1995;38(2):305-17.
1994: Bruce D Dorsey; R B Levin; S L McDaniel; Joseph P Vacca; James P Guare; Paul L Darke; J A Zugay; Emilio A Emini; William A Schleif; J C Quintero
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Journal of medicinal chemistry 1994;37(21):3443-51.
1994: Randall W Hungate; J L Chen; K E Starbuck; Joseph P Vacca; S L McDaniel; R B Levin; Bruce D Dorsey; James P Guare; M K Holloway; W Whitter
Synthesis, antiviral activity, and bioavailability studies of gamma-lactam derived HIV protease inhibitors.
Bioorganic & medicinal chemistry 1994;2(9):859-79.
1994: Joseph P Vacca; Bruce D Dorsey; William A Schleif; R B Levin; S L McDaniel; Paul L Darke; J Zugay; J C Quintero; O M Blahy; E Roth
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(9):4096-100.
1994: Joseph P Vacca
Design of tight-binding human immunodeficiency virus type 1 protease inhibitors.
Methods in enzymology 1994;241():311-34.
1991: S Jane deSolms; E A Giuliani; James P Guare; Joseph P Vacca; W M Sanders; Samuel L Graham; J M Wiggins; Paul L Darke; I S Sigal; J A Zugay
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
Journal of medicinal chemistry 1991;34(9):2852-7.
1991: Joseph P Vacca; James P Guare; S Jane deSolms; W M Sanders; E A Giuliani; S D Young; Paul L Darke; J Zugay; I S Sigal; William A Schleif
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Journal of medicinal chemistry 1991;34(3):1225-8.
1991: Paul L Darke; Nancy E Kohl; M G Hanobik; C T Leu; Joseph P Vacca; James P Guare; J C Heimbach; R A Dixon
Interaction of mutant forms of the HIV-1 protease with substrate and inhibitors.
Advances in experimental medicine and biology 1991;306():483-7.
1988: M A Polokoff; G H Bencen; Joseph P Vacca; S Jane deSolms; S D Young; Joel R Huff
Metabolism of synthetic inositol trisphosphate analogs.
The Journal of biological chemistry 1988;263(24):11922-7.
1988: W C Randall; Joel R Huff; Joseph P Vacca; James P Guare; R Chen; A Rosegay; JJ Baldwin
[3H]L-654,284 as a probe of the central alpha 2 adrenoceptor.
Naunyn-Schmiedeberg's archives of pharmacology 1988;338(1):47-52.
1988: B V Clineschmidt; Douglas J Pettibone; V J Lotti; H B Hucker; B M Sweeney; Duane R Reiss; Edward V Lis; Joel R Huff; Joseph P Vacca
A peripherally acting alpha-2 adrenoceptor antagonist: L-659,066.
The Journal of pharmacology and experimental therapeutics 1988;245(1):32-40.
1988: Joel R Huff; JJ Baldwin; S Jane deSolms; James P Guare; C A Hunt; W C Randall; W S Sanders; S J Smith; Joseph P Vacca; M M Zrada
Structure-affinity relationships of arylquinolizines at alpha-adrenoceptors.
Journal of medicinal chemistry 1988;31(3):641-5.
1987: Douglas J Pettibone; B V Clineschmidt; V J Lotti; JJ Baldwin; Joel R Huff; W C Randall; Joseph P Vacca; S D Young
Pharmacological profile of a new potent and specific alpha 2-adrenoceptor antagonist, L-657,743.
Naunyn-Schmiedeberg's archives of pharmacology 1987;336(2):169-75.
1986: Douglas J Pettibone; B V Clineschmidt; V J Lotti; G E Martin; Joel R Huff; W C Randall; Joseph P Vacca; JJ Baldwin
L-654,284 a new potent and selective alpha 2-adrenoceptor antagonist.
Naunyn-Schmiedeberg's archives of pharmacology 1986;333(2):110-6.
1985: Joel R Huff; P S Anderson; JJ Baldwin; B V Clineschmidt; James P Guare; V J Lotti; Douglas J Pettibone; W C Randall; Joseph P Vacca
N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.
Journal of medicinal chemistry 1985;28(12):1756-9.