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1

Three-carbon annelations. Regiocontrolled reactivity of trimethylsilyl- and ethoxyethyl-protected cyanohydrins. Versatile homoenolate and acyl anion equivalents

Jacobson, Richard M., Lahm, George P., Clader, John W.

Journal:

Journal of Organic Chemistry

Année:

1980

Langue:

english

Fichier:

PDF, 1.37 MB

english, 1980

2

ChemInform Abstract: Diphenylsulfone Muscarinic Antagonists: Piperidine Derivatives with High M2 Selectivity and Improved Potency.

John W. Clader, et al. et al.

Journal:

Année:

2000

Fichier:

PDF, 30 KB

2000

3

ChemInform Abstract: Synthesis of Fluorescent Biochemical Tools Related to the 2-Azetidinone Class of Cholesterol Absorption Inhibitors.

Duane A. Burnett, Mary Ann Caplen, Margaret E. Browne, Hongrong Zhau, Scott W. Altmann, Harry R. Davis Jr., John W. Clader

Journal:

Année:

2002

Fichier:

PDF, 29 KB

2002

4

ChemInform Abstract: Synthesis of Iodinated Biochemical Tools Related to the 2-Azetidinone Class of Cholesterol Absorption Inhibitors.

Duane A. Burnett, Mary Ann Caplen, Martin S. Domalski, Margaret E. Browne, Harry R. Davis Jr., John W. Clader

Journal:

Année:

2002

Fichier:

PDF, 28 KB

2002

5

Oximino-Piperidino-Piperidine-Based CCR5 Antagonists. Part 2. Synthesis, SAR and Biological Evaluation of Symmetrical Heteroaryl Carboxamides.

Anandan Palani, Sherry Shapiro, John W. Clader, William J. Greenlee, Susan Vice, Stuart McCombie, Kathleen Cox, Julie Strizki, Bahige M. Baroudy

Journal:

Année:

2003

Fichier:

PDF, 171 KB

2003

6

The Discovery of Ezetimibe: A View from Outside the Receptor

Journal:

Année:

2004

Fichier:

PDF, 52 KB

2004

7

Isopropyl Amide Derivatives of Potent and Selective Muscarinic M2 Receptor Antagonists.

Anandan Palani, Sundeep Dugar, John W. Clader, William J. Greenlee, Vilma Ruperto, Ruth A. Duffy, Jean E. Lachowicz

Journal:

Année:

2004

Fichier:

PDF, 64 KB

2004

8

Trans diastereoselective synthesis of 3-alkyl substituted β-lactams via the acid chloride-imine reaction of nonactivated acid chlorides

Margaret Browne, Duane A. Burnett, Mary Ann Caplen, Lian-Yong Chen, John W. Clader, Martin Domalski, Sundeep Dugar, Pradeep Pushpavanam, Rosy Sher, Wayne Vaccaro, Monica Viziano, Hongrong Zhao

Journal:

Tetrahedron Letters

Année:

1995

Langue:

english

Fichier:

PDF, 226 KB

english, 1995

9

Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity

John W Clader, William Billard, Herbert Binch III, Lian-Yong Chen, Gordon Crosby Jr., Ruth A Duffy, Jennifer Ford, Joseph A Kozlowski, Jean E Lachowicz, Shengjian Li, Charles Liu, Stuart W McCombie, S

Journal:

Bioorganic & Medicinal Chemistry

Année:

2004

Langue:

english

Fichier:

PDF, 240 KB

english, 2004

10

Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists

Ruo Xu, Shengjian Li, Jaroslava Paruchova, Mark D. McBriar, Henry Guzik, Anandan Palani, John W. Clader, Kathleen Cox, William J. Greenlee, Brian E. Hawes, Timothy J. Kowalski, Kim O’Neill, Brian D. S

Journal:

Bioorganic & Medicinal Chemistry

Année:

2006

Langue:

english

Fichier:

PDF, 241 KB

english, 2006

11

Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists

Jing Su, Haiqun Tang, Brian A. McKittrick, Huizhong Gu, Tao Guo, Gang Qian, Duane A. Burnett, John W. Clader, William J. Greenlee, Brian E. Hawes, Kim O’Neill, Brian Spar, Blair Weig, Timothy Kowalski

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 237 KB

english, 2007

12

Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors

Mark D. McBriar, John W. Clader, Inhou Chu, Robert A. Del Vecchio, Leonard Favreau, William J. Greenlee, Lynn A. Hyde, Amin A. Nomeir, Eric M. Parker, Dmitri A. Pissarnitski, Lixin Song, Lili Zhang, Z

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 252 KB

english, 2008

13

Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability

Hubert Josien, Thomas Bara, Murali Rajagopalan, John W. Clader, William J. Greenlee, Leonard Favreau, Lynn A. Hyde, Amin A. Nomeir, Eric M. Parker, Lixin Song, Lili Zhang, Qi Zhang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2009

Langue:

english

Fichier:

PDF, 1.22 MB

english, 2009

14

Design and synthesis of tricyclic sulfones as γ-secretase inhibitors with greatly reduced Notch toxicity

Ruo Xu, David Cole, Ted Asberom, Tom Bara, Chad Bennett, Duane A. Burnett, John Clader, Martin Domalski, William Greenlee, Lynn Hyde, Hubert Josien, Hongmei Li, Mark McBriar, Brian McKittrick, Andrew

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 664 KB

english, 2010

15

Gamma-lactams and related compounds as cholesterol absorption inhibitors: homologs of the beta-lactam cholesterol absorption inhibitor SCH 484611

Sundeep Dugar, Michael P. Kirkup, John W. Clader, Sue-Ing Lin, Razia Rizvi, Mark E. Snow, Harry R. Davis Jr., Stuart W. McCombie

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1995

Langue:

english

Fichier:

PDF, 264 KB

english, 1995

16

Metabolism and structure activity data based drug design: discovery of (−) SCH 53079 an analog of the potent cholesterol absorption inhibitor (−) SCH 48461

Syndeep Dugar, Nathan Yumibe, John W. Clader, Monica Vizziano, Keith Huie, Margaret Van Heek, Douglas S. Compton, Harry R. Davis Jr.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1996

Langue:

english

Fichier:

PDF, 180 KB

english, 1996

17

(−)-SCH 57939: synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor

Michael P. Kirkup, Razia Rizvi, Bandarpalle B. Shankar, Sundeep Dugar, John W. Clader, Stuart W. McCombie, Sue-Ing Lin, Nathan Yumibe, Keith Huie, Margaret Van Heek, Douglas S. Compton, Harry R. Davis

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1996

Langue:

english

Fichier:

PDF, 250 KB

english, 1996

18

Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors

Brian A. McKittrick, Ke Ma, Sundeep Dugar, John W. Clader, Harry Davis Jr., Michael Czarniecki, Andrew T. McPhail

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1996

Langue:

english

Fichier:

PDF, 223 KB

english, 1996

19

SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: Taming hERG

Jing Su, Brian A. McKittrick, Haiqun Tang, Duane A. Burnett, John W. Clader, William J. Greenlee, Brian E. Hawes, Kim O’Neill, Brian Spar, Blair Weig, Timothy Kowalski, Steve Sorota, Cheng Li, Tongton

Journal:

Bioorganic & Medicinal Chemistry

Année:

2007

Langue:

english

Fichier:

PDF, 260 KB

english, 2007

20

Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists

Anandan Palani, Sundeep Dugar, John W. Clader, William J. Greenlee, Vilma Ruperto, Ruth A. Duffy, Jean E. Lachowicz

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 193 KB

english, 2004

21

Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications

Mark D. McBriar, Henry Guzik, Sherry Shapiro, Ruo Xu, Jaroslava Paruchova, John W. Clader, Kim O’Neill, Brian Hawes, Steve Sorota, Michael Margulis, Kristal Tucker, Daniel J. Weston, Kathleen Cox

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 124 KB

english, 2006

22

Tetrahydroquinoline sulfonamides as γ-secretase inhibitors

Theodros Asberom, Thomas A. Bara, John W. Clader, William J. Greenlee, Henry S. Guzik, Hubert B. Josien, Wei Li, Eric M. Parker, Dmitri A. Pissarnitski, Lixin Song, Lili Zhang, Zhiqiang Zhao

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 151 KB

english, 2007

23

Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease

Theodros Asberom, Zhiqiang Zhao, Thomas A. Bara, John W. Clader, William J. Greenlee, Lynn A. Hyde, Hubert B. Josien, Wei Li, Andrew T. McPhail, Amin A. Nomeir, Eric M. Parker, Murali Rajagopalan, Lix

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 263 KB

english, 2007

24

Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as γ-secretase inhibitors

Tao Guo, Huizhong Gu, Doug W. Hobbs, Laura L. Rokosz, Tara M. Stauffer, Biji Jacob, John W. Clader

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 173 KB

english, 2007

25

Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors

Hubert Josien, Thomas Bara, Murali Rajagopalan, Theodros Asberom, John W. Clader, Leonard Favreau, William J. Greenlee, Lynn A. Hyde, Amin A. Nomeir, Eric M. Parker, Dmitri A. Pissarnitski, Lixin Song

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 209 KB

english, 2007

26

Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors

Hongmei Li, Theodros Asberom, Thomas A. Bara, John W. Clader, William J. Greenlee, Hubert B. Josien, Mark D. McBriar, Amin Nomeir, Dmitri A. Pissarnitski, Murali Rajagopalan, Ruo Xu, Zhiqiang Zhao, Li

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 410 KB

english, 2007

27

Tetracyclic sulfones as potent γ-secretase inhibitors: Synthesis and structure–activity relationship studies

T.K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Chad Bennett, David Cole, Ruo Xu, William J. Greenlee, John Clader, Lili Zhang, Lynn Hyde

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 1005 KB

english, 2010

28

Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure–activity relationship studies

T.K. Sasikumar, Li Qiang, Duane A. Burnett, David Cole, Ruo Xu, Hongmei Li, William J. Greenlee, John Clader, Lili Zhang, Lynn Hyde

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 583 KB

english, 2010

29

Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

Hongmei Li, Ruo Xu, David Cole, John W. Clader, William J. Greenlee, Amin A. Nomeir, Lixin Song, Lili Zhang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 1.71 MB

english, 2010

30

Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators

Jun Qin, Pawan Dhondi, Xianhai Huang, Mihirbaran Mandal, Zhiqiang Zhao, Dmitri Pissarnitski, Wei Zhou, Robert Aslanian, Zhaoning Zhu, William Greenlee, John Clader, Lili Zhang, Mary Cohen-Williams, Ni

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 1.96 MB

english, 2011

31

Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positions

Jing Su, Haiqun Tang, Brian A. McKittrick, Ruo Xu, John W. Clader, William J. Greenlee, Lynn Hyde, Lili Zhang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 514 KB

english, 2011

32

Three carbon annelation reagents: unsaturated alpha aminonitriles as homoenolate equivalents

Richard M. Jacobson, John W. Clader

Journal:

Tetrahedron Letters

Année:

1980

Langue:

english

Fichier:

PDF, 209 KB

english, 1980

33

Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists

Yuguang Wang, Samuel Chackalamannil, Zhiyong Hu, John W Clader, William Greenlee, William Billard, Herbert Binch III, Gordon Crosby, Vilma Ruperto, Ruth A Duffy, Robert McQuade, Jean E Lachowicz

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 148 KB

english, 2000

34

Metabolic stabilization of benzylidene ketal M2 muscarinic receptor antagonists via halonaphthoic acid substitution

Craig D. Boyle, Samuel Chackalamannil, John W. Clader, William J. Greenlee, Hubert B. Josien, James J. Kaminski, Joseph A. Kozlowski, Stuart W. McCombie, Dennis V. Nazareno, Jayaram R. Tagat, Yuguang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2001

Langue:

english

Fichier:

PDF, 129 KB

english, 2001

35

Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Duane A Burnett, Mary Ann Caplen, Margaret E Browne, Hongrong Zhau, Scott W Altmann, Harry R Davis Jr., John W Clader

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2002

Langue:

english

Fichier:

PDF, 139 KB

english, 2002

36

Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Duane A Burnett, Mary Ann Caplen, Martin S Domalski, Margaret E Browne, Harry R Davis, Jr, John W Clader

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2002

Langue:

english

Fichier:

PDF, 125 KB

english, 2002

37

Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides

Anandan Palani, Sherry Shapiro, John W. Clader, William J. Greenlee, Susan Vice, Stuart McCombie, Kathleen Cox, Julie Strizki, Bahige M. Baroudy

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 149 KB

english, 2003

38

Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist

Anandan Palani, Sherry Shapiro, John W. Clader, William J. Greenlee, David Blythin, Kathleen Cox, Nicole E. Wagner, Julie Strizki, Bahige M. Baroudy, Niya Dan

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2003

Langue:

english

Fichier:

PDF, 133 KB

english, 2003

39

SAR of tricyclic sulfones as γ-secretase inhibitors

Ruo Xu, David Cole, Ted Asberom, Tom Bara, Chad Bennett, Duane A. Burnett, John Clader, Martin Domalski, William J. Greenlee, Lynn Hyde, Hubert Josien, HongMei Li, Mark McBriar, Brian McKittrick, Dmit

Journal:

Science China Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 738 KB

english, 2011

40

SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction

Dmitri A Pissarnitski, Theodros Asberom, Craig D Boyle, Samuel Chackalamannil, Madhu Chintala, John W Clader, William J Greenlee, Yueqing Hu, Stanley Kurowski, Joyce Myers, Jairam Palamanda, Andrew W

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 203 KB

english, 2004

41

Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED

Craig D. Boyle, Ruo Xu, Theodros Asberom, Samuel Chackalamannil, John W. Clader, William J. Greenlee, Henry Guzik, Yuequing Hu, Zhiyong Hu, Claire M. Lankin, Dmitri A. Pissarnitski, Andrew W. Stamford

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 141 KB

english, 2005

42

Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists

Anandan Palani, Sherry Shapiro, Mark D. McBriar, John W. Clader, William J. Greenlee, Kim O’Neill, Brian Hawes

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 103 KB

english, 2005

43

2,6-Disubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors

Dmitri A. Pissarnitski, Theodros Asberom, Thomas A. Bara, Alex V. Buevich, John W. Clader, William J. Greenlee, Henry S. Guzik, Hubert B. Josien, Wei Li, Michael McEwan, Brian A. McKittrick, Terry L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 238 KB

english, 2007

44

N-oleoyl-1,2,3,4-tetrahydroisoquinolines as conformationally restricted inhibitors of acyl-CoA:cholesterol acyl transferase (ACAT)

Sundeep Dugar, John W. Clader, Robert E. Burrier, Timothy P. Kogan

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1993

Langue:

english

Fichier:

PDF, 332 KB

english, 1993

45

Effects of a selective melanin-concentrating hormone 1 receptor antagonist on food intake and energy homeostasis in diet-induced obese mice

Timothy J. Kowalski, Brian D. Spar, Blair Weig, Constance Farley, John Cook, Lorraine Ghibaudi, Steve Fried, Kim O'Neill, Robert A. Del Vecchio, Mark McBriar, Henry Guzik, John Clader, Brian E. Hawes,

Journal:

European Journal of Pharmacology

Année:

2006

Langue:

english

Fichier:

PDF, 425 KB

english, 2006

46

Interaction of small molecule inhibitors of HIV-1 entry with CCR5

Christoph Seibert, Weiwen Ying, Svetlana Gavrilov, Fotini Tsamis, Shawn E. Kuhmann, Anandan Palani, Jayaram R. Tagat, John W. Clader, Stuart W. McCombie, Bahige M. Baroudy, Steven O. Smith, Tatjana Dr

Journal:

Année:

2006

Langue:

english

Fichier:

PDF, 495 KB

english, 2006

47

Facilitation of acetylcholine release and improvement in cognition by a selective M2 muscarinic antagonist, SCH 72788

Jean E. Lachowicz, Ruth A. Duffy, Vilma Ruperto, Joseph Kozlowski, Guowei Zhou, John Clader, William Billard, Herbert Binch III, Gordon Crosby, Mary Cohen-Williams, Catherine D. Strader, Victoria Coff

Journal:

Année:

2001

Langue:

english

Fichier:

PDF, 210 KB

english, 2001

48

SCH 57790: A novel M2 receptor selective antagonist

Jean E. Lachowicz, Derek Lowe, Ruth A. Duffy, Vilma Ruperto, Lisa A. Taylor, Henry Guzik, Joan Brown, Joel G. Berger, Melissa Tice, Robert McQuade, Joseph Kozlowski, John Clader, Catherine D. Strader,

Journal:

Année:

1999

Langue:

english

Fichier:

PDF, 385 KB

english, 1999

49

Discovery of Bicycloalkyl Urea Melanin Concentrating Hormone Receptor Antagonists: Orally Efficacious Antiobesity Therapeutics

McBriar, Mark D., Guzik, Henry, Xu, Ruo, Paruchova, Jaroslava, Li, Shengjian, Palani, Anandan, Clader, John W., Greenlee, William J., Hawes, Brian E., Kowalski, Timothy J., O'Neill, Kim, Spar, Brian,

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 61 KB

english, 2005

50

2-Azetidinones as Inhibitors of Cholesterol Absorption

Burnett, Duane A., Caplen, Mary Ann, Davis, Harry R., Burrier, Robert E., Clader, John W.

Journal:

Journal of Medicinal Chemistry

Année:

1994

Langue:

english

Fichier:

PDF, 470 KB

english, 1994