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1

Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs): Discovery of capromorelin

Philip A Carpino, Bruce A Lefker, Steven M Toler, Lydia C Pan, John R Hadcock, Ewell R Cook, Joseph N DiBrino, Anthony M Campeta, Shari L DeNinno, Kristin L Chidsey-Frink, William A Hada, John Inthavo

Journal:

Bioorganic & Medicinal Chemistry

Year:

2003

Language:

english

File:

PDF, 219 KB

english, 2003

2

Modulators of the ghrelin system as potential treatments for obesity and diabetes

Carpino, Philip A, Ho, Guyu

Journal:

Expert Opinion on Therapeutic Patents

Year:

2008

Language:

english

File:

PDF, 323 KB

english, 2008

3

Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)

Futatsugi, Kentaro, Kung, Daniel W., Orr, Suvi T. M., Cabral, Shawn, Hepworth, David, Aspnes, Gary, Bader, Scott, Bian, Jianwei, Boehm, Markus, Carpino, Philip A., Coffey, Steven B., Dowling, Matthew

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 816 KB

english, 2015

4

Discovery and Biological Characterization of Capromorelin Analogues with Extended Half-Lives

Philip A. Carpino, et al. et al.

Journal:

Year:

2003

File:

PDF, 143 KB

2003

5

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists

Philip A. Carpino, David A. Griffith, Subas Sakya, Robert L. Dow, Shawn C. Black, John R. Hadcock, Philip A. Iredale, Dennis O. Scott, Michael W. Fichtner, Colin R. Rose, Robert Day, Joseph Dibrino, M

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 194 KB

english, 2006

6

Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: Potent, orally-active 1,4-disubstituted imidazoles

Robert L. Dow, John R. Hadcock, Dennis O. Scott, Steven R. Schneider, Ernest S. Paight, Philip A. Iredale, Philip A. Carpino, David A. Griffith, Marlys Hammond, Paul DaSilva-Jardine

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 365 KB

english, 2009

7

A new synthesis of secondary allylic aliphatic and aromatic amines

Andreas Spaltenstein, Philip A. Carpino, Paul B. Hopkins

Journal:

Tetrahedron Letters

Year:

1986

Language:

english

File:

PDF, 274 KB

english, 1986

8

A stereocontrolled synthesis of trans-alkene isosteres of dipeptides

Andreas Spaltenstein, Philip A Carpino, Fumio Miyake, Paul B Hopkins

Journal:

Tetrahedron Letters

Year:

1986

Language:

english

File:

PDF, 279 KB

english, 1986

9

A simplified synthesis of (+)-brefeldin A

E.J. Corey, Philip Carpino

Journal:

Tetrahedron Letters

Year:

1990

Language:

english

File:

PDF, 226 KB

english, 1990

10

A new enantiospecific route to the pseudopterosins

E.J. Corey, Philip Carpino

Journal:

Tetrahedron Letters

Year:

1990

Language:

english

File:

PDF, 134 KB

english, 1990

11

A conformationally restrained series of AT1-selective angiotensin II antagonists

Philip A. Carpino, Scott F. Sneddon, Jardine Paul da Silva, Magnus-Ayritey George T., Rauch Albert L., Burkard Michael R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

1994

Language:

english

File:

PDF, 393 KB

english, 1994

12

Quantitativein vitroandin vivopharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) Receptor Antagonist

John R Hadcock, Philip A Carpino, Philip A Iredale, Robert L Dow, Denise Gautreau, Lucinda Thiede, Dawn Kelly-Sullivan, Jeffrey S Lizano, Xingrong Liu, Jeffrey Van Deusen, Karen M Ward, Rebecca E O'Co

Journal:

BMC Pharmacology

Year:

2010

Language:

english

File:

PDF, 900 KB

english, 2010

13

Discovery and biological characterization of capromorelin analogues with extended half-lives

Philip A. Carpino, Bruce A. Lefker, Steven M. Toler, Lydia C. Pan, John R. Hadcock, Marianne C. Murray, Ewell R. Cook, Joseph N. DiBrino, Shari L. DeNinno, Kristin L. Chidsey-Frink, William A. Hada, J

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2002

Language:

english

File:

PDF, 130 KB

english, 2002

14

Preclinical pharmacology of CP-424,391, and orally active pyrazolinone-piperidine growth hormone secretagogue

Lydia C. Pan, Philip A. Carpino, Bruce A. Lefker, John A. Ragan, Steven M. Toler, John C. Pettersen, David O. Nettleton, Oicheng Ng, Christine M. Pirie, Kristin Chidsey-Frink, Bihong Lu, David F. Nick

Journal:

Endocrine (Springer)

Year:

2001

Language:

english

File:

PDF, 200 KB

english, 2001

15

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents

Dow, Robert L., Carpino, Philip A., Gautreau, Denise, Hadcock, John R., Iredale, Philip A., Kelly-Sullivan, Dawn, Lizano, Jeffrey S., O’Connor, Rebecca E., Schneider, Steven R., Scott, Dennis O.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 911 KB

english, 2012

16

Diabetes area participation analysis: a review of companies and targets described in the 2008 – 2010 patent literature

Carpino, Philip A, Goodwin, Bryan

Journal:

Expert Opinion on Therapeutic Patents

Year:

2010

Language:

english

File:

PDF, 826 KB

english, 2010

17

Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor

Michael Fichtner, Eunsun Lee, Elizabeth Tomlinson, Dennis Scott, Peter Cornelius, Terrell A. Patterson, Philip A. Carpino

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 839 KB

english, 2012

18

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor

Daniel W. Kung, Steven B. Coffey, Ryan M. Jones, Shawn Cabral, Wenhua Jiao, Michael Fichtner, Philip A. Carpino, Colin R. Rose, Richard F. Hank, Michael G. Lopaze, Roger Swartz, Hou (Tommy) Chen, Zach

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 630 KB

english, 2012

19

Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries

Londregan, Allyn T., Piotrowski, David W., Futatsugi, Kentaro, Warmus, Joseph S., Boehm, Markus, Carpino, Philip A., Chin, Janice E., Janssen, Ann M., Roush, Nicole S., Buxton, Joanne, Hinchey, Terri

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 947 KB

english, 2013

20

Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9 H -purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

Griffith, David A., Hadcock, John R., Black, Shawn C., Iredale, Philip A., Carpino, Philip A., DaSilva-Jardine, Paul, Day, Robert, DiBrino, Joseph, Dow, Robert L., Landis, Margaret S., O’Connor, Rebec

Journal:

Journal of Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 145 KB

english, 2009

21

New approaches to the synthesis of trans-alkene isosteres of dipeptides

Spaltenstein, Andreas, Carpino, Philip A., Miyake, Fumio, Hopkins, Paul B.

Journal:

Journal of Organic Chemistry

Year:

1987

Language:

english

File:

PDF, 1.21 MB

english, 1987

22

Allylic selenides in organic synthesis: new methods for the synthesis of allylic amines

Shea, Regan G., Fitzner, Jeffrey N., Fankhauser, John E., Spaltenstein, Andreas, Carpino, Philip A., Peevey, Richard M., Pratt, Daniel V., Tenge, Bradley J., Hopkins, Paul B.

Journal:

Journal of Organic Chemistry

Year:

1986

Language:

english

File:

PDF, 1.39 MB

english, 1986

23

Enantiospecific total synthesis of pseudopterosins A and E

Corey, E. J., Carpino, Philip

Journal:

Journal of the American Chemical Society

Year:

1989

Language:

english

File:

PDF, 427 KB

english, 1989

24

Discovery of 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2 H -pyrazolo[3,4- f ][1,4]oxazepin-8(5 H )-one (PF-514273), a Novel, Bicyclic Lactam-Based Cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

Dow, Robert L., Carpino, Philip A., Hadcock, John R., Black, Shawn C., Iredale, Philip A., DaSilva-Jardine, Paul, Schneider, Steven R., Paight, Ernest S., Griffith, David A., Scott, Dennis O., O’Conno

Journal:

Journal of Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 191 KB

english, 2009

25

Outcome after combined carotid endarterectomy and coronary artery bypass is related to patient selection

Estes, James M., Khabbaz, Kamal R., Barnatan, Marcos, Carpino, Philip, Mackey, William C.

Journal:

Journal of Vascular Surgery

Year:

2001

Language:

english

File:

PDF, 73 KB

english, 2001

26

Investigational drugs in Phase II clinical trials for the treatment of obesity: implications for future development of novel therapies

Jackson, V Margaret, Price, David A, Carpino, Philip A

Journal:

Expert Opinion on Investigational Drugs

Year:

2014

Language:

english

File:

PDF, 325 KB

english, 2014

27

Mechanistic Characterization of a 2-Thioxanthine Myeloperoxidase Inhibitor and Selectivity Assessment Utilizing Click Chemistry–Activity-Based Protein Profiling

Ward, Jessica, Spath, Samantha N., Pabst, Brandon, Carpino, Philip A., Ruggeri, Roger B., Xing, Gang, Speers, Anna E., Cravatt, Benjamin F., Ahn, Kay

Journal:

Year:

2013

Language:

english

File:

PDF, 2.08 MB

english, 2013

28

A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

Nolte, Whitney M, Fortin, Jean-Philippe, Stevens, Benjamin D, Aspnes, Gary E, Griffith, David A, Hoth, Lise R, Ruggeri, Roger B, Mathiowetz, Alan M, Limberakis, Chris, Hepworth, David, Carpino, Philip

Journal:

Nature Chemical Biology

Year:

2014

Language:

english

File:

PDF, 715 KB

english, 2014

29

Deconstruction of Activity-Dependent Covalent Modification of Heme in Human Neutrophil Myeloperoxidase by Multistage Mass Spectrometry (MS 4 )

Geoghegan, Kieran F., Varghese, Alison H., Feng, Xidong, Bessire, Andrew J., Conboy, James J., Ruggeri, Roger B., Ahn, Kay, Spath, Samantha N., Filippov, Sergey V., Conrad, Steven J., Carpino, Philip

Journal:

Year:

2012

Language:

english

File:

PDF, 4.86 MB

english, 2012

30

Recent developments in ghrelin receptor (GHS-R1a) agonists and antagonists

Carpino, Philip A

Journal:

Expert Opinion on Therapeutic Patents

Year:

2002

Language:

english

File:

PDF, 285 KB

english, 2002

31

[Annual Reports in Medicinal Chemistry] Annual Reports in Medicinal Chemistry Volume 47 Volume 47 || Beyond PPARs and Metformin

Carpino, Philip A.

Year:

2012

Language:

english

File:

PDF, 341 KB

english, 2012

32

Latest approaches for the treatment of obesity

Jackson, V Margaret, Breen, Danna M, Fortin, Jean-Philippe, Liou, Alice, Kuzmiski, J Brent, Loomis, A Katrina, Rives, Marie-Laure, Shah, Bhavik, Carpino, Philip A

Journal:

Expert Opinion on Drug Discovery

Year:

2015

Language:

english

File:

PDF, 405 KB

english, 2015

33

Melanocortin-4 receptor modulators for the treatment of obesity: a patent analysis (2008–2014)

Lee, Esther CY, Carpino, Philip A

Journal:

Pharmaceutical Patent Analyst

Year:

2015

Language:

english

File:

PDF, 1.51 MB

english, 2015

34

MAP4K4 Is a Threonine Kinase That Phosphorylates FARP1

Schwaid, Adam G., Su, Chunyan, Loos, Paula, Wu, Jiang, Nguyen, Chong, Stone, Kathryn L., Kanyo, Jean, Geoghegan, Kieran F., Bhattacharya, Samit K., Dow, Robert L., Buckbinder, Leonard, Carpino, Philip

Journal:

ACS Chemical Biology

Year:

2015

Language:

english

File:

PDF, 1.74 MB

english, 2015

35

Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2 H )-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases

Ruggeri, Roger B., Buckbinder, Leonard, Bagley, Scott W., Carpino, Philip A., Conn, Edward L., Dowling, Matthew S., Fernando, Dilinie P., Jiao, Wenhua, Kung, Daniel W., Orr, Suvi T. M., Qi, Yingmei, R

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.64 MB

english, 2015

36

Revascularization Options for Ischemic Cardiomyopathy: On-Pump and Off-Pump Coronary Artery Bypass Surgery

Khabbaz, Kamal R., DeNofrio, David, Kazimi, Marwan, Carpino, Philip A.

Journal:

Year:

2004

Language:

english

File:

PDF, 104 KB

english, 2004

37

Development of a selective activity-based probe for glycosylated LIPA

Schwaid, Adam G., Ruangsiriluk, Wanida, Reyes, Allan R., Cabral, Shawn, Rajamohan, Francis, Tu, Meihua, Ward, Jessica, Carpino, Philip A.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2016

Language:

english

File:

PDF, 2.27 MB

english, 2016

38

Review of companies and drug classes in the 2007–2011 antihypertensive patent literature

Carpino, Philip A, Flynn, Declan

Journal:

Pharmaceutical Patent Analyst

Year:

2012

Language:

english

File:

PDF, 1.06 MB

english, 2012

39

Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution

Rose, Colin R., Zawistoski, Michael P., Lefker, Bruce A., Mangano, F. Michael, Wright, Ann S., Carpino, Philip A.

Journal:

Bioorganic & Medicinal Chemistry

Year:

2017

Language:

english

File:

PDF, 418 KB

english, 2017

40

Diabetes area patent participation analysis – Part II: Years 2011-2016

Boehm, Markus, Crawford, Matthew, Moscovitz, Jamie E., Carpino, Philip A

Journal:

Expert Opinion on Therapeutic Patents

Year:

2017

Language:

english

File:

PDF, 1.06 MB

english, 2017

41

Discovery and In Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors

Sammons, Matthew F., Kharade, Sujay V., Filipski, Kevin J., Boehm, Markus, Smith, Aaron C., Shavnya, Andre, Fernando, Dilinie P., Dowling, Matthew S., Carpino, Philip A, Castle, Neil A., Zellmer, Shan

Journal:

ACS Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 1.11 MB

english, 2018

42

Patent focus on new anti-obesity agents: September 1999 - February 2000

Carpino, Philip A

Journal:

Expert Opinion on Therapeutic Patents

Year:

2000

Language:

english

File:

PDF, 280 KB

english, 2000

43

Results of surgical septal myectomy for obstructive hypertrophic cardiomyopathy: the Tufts experience

Rastegar, Hassan, Boll, Griffin, Rowin, Ethan J., Dolan, Noreen, Carroll, Catherine, Udelson, James E., Wang, Wendy, Carpino, Philip, Maron, Barry J., Maron, Martin S., Chen, Frederick Y.

Journal:

Annals of cardiothoracic surgery

Year:

2017

Language:

english

File:

PDF, 345 KB

english, 2017