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1

ChemInform Abstract: The De Novo Design and Synthesis of Cyclic Urea Inhibitors of Factor Xa: Optimization of the S4 Ligand.

Robert A. Galemmo Jr., et al. et al.

Journal:

Année:

2000

Fichier:

PDF, 30 KB

2000

2

Improved Solution- and Solid-Phase Preparation of Hydroxamic Acids from Esters.

Chih Y. Ho, Eric Strobel, Janet Ralbovsky, Robert A. Jr. Galemmo

Journal:

Année:

2005

Fichier:

PDF, 15 KB

2005

3

Preparative routes to methyl 2-acetamido-2,6-dideoxy-α-d-glucopyranoside

Robert A. Galemmo Jr., Derek Horton

Journal:

Carbohydrate Research

Année:

1983

Langue:

english

Fichier:

PDF, 702 KB

english, 1983

4

The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: A new class of Aurora-A kinase inhibitors

Kevin J. Moriarty, Holly K. Koblish, Thomas Garrabrant, Jahanvi Maisuria, Ehab Khalil, Farah Ali, Ioanna P. Petrounia, Carl S. Crysler, Anna C. Maroney, Dana L. Johnson, Robert A. Galemmo Jr.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 360 KB

english, 2006

5

1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa

Donald J.P. Pinto, Michael J. Orwat, Mimi L. Quan, Qi Han, Robert A. Galemmo Jr., Eugene Amparo, Brian Wells, Christopher Ellis, Ming Y. He, Richard S. Alexander, Karen A. Rossi, Angela Smallwood, Pan

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 184 KB

english, 2006

6

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties

Donald J.P. Pinto, Robert A. Galemmo Jr., Mimi L. Quan, Michael J. Orwat, Charles Clark, Renhua Li, Brian Wells, Francis Woerner, Richard S. Alexander, Karen A. Rossi, Angela Smallwood, Pancras C. Won

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 590 KB

english, 2006

7

Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues

Jennifer X. Qiao, Xuhong Cheng, Joanne M. Smallheer, Robert A. Galemmo, Spencer Drummond, Donald J.P. Pinto, Daniel L. Cheney, Kan He, Pancras C. Wong, Joseph M. Luettgen, Robert M. Knabb, Ruth R. Wex

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 414 KB

english, 2007

8

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration

Gary D. Probst, Simeon Bowers, Jennifer M. Sealy, Anh P. Truong, Roy K. Hom, Robert A. Galemmo Jr., Andrei W. Konradi, Hing L. Sham, David A. Quincy, Hu Pan, Nanhua Yao, May Lin, Gergley Tóth, Dean R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 1.86 MB

english, 2011

9

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor

Simeon Bowers, Anh P. Truong, R. Jeffrey Neitz, Martin Neitzel, Gary D. Probst, Roy K. Hom, Brian Peterson, Robert A. Galemmo Jr., Andrei W. Konradi, Hing L. Sham, Gergley Tóth, Hu Pan, Nanhua Yao, De

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 1.28 MB

english, 2011

10

A facile synthesis of multigram quantity of ethyl 3-ethylmorpholine-3-carboxylate

Jacek J. Jagodzinski, Danielle L. Aubele, David A. Quincy, Michael S. Dappen, Lee H. Latimer, Roy K. Hom, Robert A. Galemmo Jr., Andrei W. Konradi, Hing L. Sham

Journal:

Tetrahedron Letters

Année:

2011

Langue:

english

Fichier:

PDF, 230 KB

english, 2011

11

The introduction of a new sulfamoylation reagent: n-carbo-(trimethylsilyloxy)sulfamoylchloride. Versatile syntheses of 3-amino-4-n-alkyl and 3-amino-2-n-alkyl-5-aryloxy-1,2,4,6-thiatriazine-1,1-dioxides.

Pamela J. Durham, Robert A. Galemmo Jr.

Journal:

Tetrahedron Letters

Année:

1986

Langue:

english

Fichier:

PDF, 202 KB

english, 1986

12

Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core

John M. Fevig, Donald J. Pinto, Qi Han, Mimi L. Quan, James R. Pruitt, Irina C. Jacobson, Robert A. Galemmo, Jr, Shuaige Wang, Michael J. Orwat, Lori L. Bostrom, Robert M. Knabb, Pancras C. Wong, Patr

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2001

Langue:

english

Fichier:

PDF, 222 KB

english, 2001

13

(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors

Robert A. Galemmo Jr., John M. Fevig, David J. Carini, Joseph Cacciola, Brian L. Wells, Gregory L. Hillyer, Joseph Buriak Jr., Karen A. Rossi, Pieter F.W. Stouten, Richard S. Alexander, Richard Hilmer

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1996

Langue:

english

Fichier:

PDF, 372 KB

english, 1996

14

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: Initial sar studies

Robert A. Galemmo Jr., Thomas P. Maduskuie, Celia Dominguez, Karen A. Rossi, Robert M. Knabb, Ruth R. Wexler, Pieter F.W. Stouten

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1998

Langue:

english

Fichier:

PDF, 340 KB

english, 1998

15

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors

Celia Dominguez, Daniel E. Duffy, Qi Han, Richard S. Alexander, Robert A. Galemmo Jr., Jeongsook M. Park, Pancras C. Wong, Eugene C. Amparo, Robert M. Knabb, Joseph Luettgen, Ruth R. Wexler

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1999

Langue:

english

Fichier:

PDF, 338 KB

english, 1999

16

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand

Robert A. Galemmo Jr., Brian L. Wells, Karen A. Rossi, Richard S. Alexander, Celia Dominguez, Thomas P. Maduskuie, Pieter F.W. Stouten, Matthew R. Wright, Bruce J. Aungst, Pancras C. Wong, Robert M. K

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 222 KB

english, 2000

17

Small molecule inhibitors of methionine aminopeptidase type 2 (MetAP-2) fail to inhibit endothelial cell proliferation or formation of microvessels from rat aortic rings in vitro

Thomas Garrabrant, Robert Tuman, Don Ludovici, Rose Tominovich, Richard Simoneaux, Robert Galemmo

Journal:

Année:

2004

Langue:

english

Fichier:

PDF, 141 KB

english, 2004

18

Structure-Based Design of Novel Guanidine/Benzamidine Mimics: Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants

Lam, Patrick Y. S., Clark, Charles G., Li, Renhua, Pinto, Donald J. P., Orwat, Michael J., Galemmo, Robert A., Fevig, John M., Teleha, Christopher A., Alexander, Richard S., Smallwood, Angela M.

Journal:

Journal of Medicinal Chemistry

Année:

2003

Langue:

english

Fichier:

PDF, 402 KB

english, 2003

19

Design, Synthesis, and Biological Evaluation of Potent and Selective Amidino Bicyclic Factor Xa Inhibitors

Han, Qi, Dominguez, Celia, Stouten, Pieter F. W., Park, Jeongsook M., Duffy, Daniel E., Galemmo, Robert A., Rossi, Karen A., Alexander, Richard S., Smallwood, Angela M., Wong, Pancras C.

Journal:

Journal of Medicinal Chemistry

Année:

2000

Langue:

english

Fichier:

PDF, 445 KB

english, 2000

20

Improved Solution- and Solid-Phase Preparation of Hydroxamic Acids from Esters

Ho, Chih Y., Strobel, Eric, Ralbovsky, Janet, Galemmo, Robert A.

Journal:

Journal of Organic Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 164 KB

english, 2005

21

Oral coadministration of β-glucuronidase to increase exposure of extensively glucuronidated drugs that undergo enterohepatic recirculation

Gary Eichenbaum, C.-P. Hsu, Vangala Subrahmanyam, Jing Chen, Jan Scicinski, Robert A. Galemmo Jr., Robert W. Tuman, Dana L. Johnson

Journal:

Journal of Pharmaceutical Sciences

Année:

2012

Langue:

english

Fichier:

PDF, 349 KB

english, 2012

22

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Simeon Bowers, Anh P. Truong, R. Jeffrey Neitz, Roy K. Hom, Jennifer M. Sealy, Gary D. Probst, David Quincy, Brian Peterson, Wayman Chan, Robert A. Galemmo Jr., Andrei W. Konradi, Hing L. Sham, Gergel

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 1.08 MB

english, 2011

23

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity

Huang, Fu Chih, Galemmo, Robert A., Johnson, William H., Poli, Gregory B., Morrissette, Matthew M., Mencel, James J., Warus, James D., Campbell, Henry F., Nuss, George W.

Journal:

Journal of Medicinal Chemistry

Année:

1990

Langue:

english

Fichier:

PDF, 970 KB

english, 1990

24

The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency

Galemmo, Robert A., Johnson, William H., Learn, Keith S., Lee, Thomas D. Y., Huang, Fu Chih, Campbell, Henry F., Youssefyeh, Raymond, O'Rourke, Susan V., Schuessler, Glenn

Journal:

Journal of Medicinal Chemistry

Année:

1990

Langue:

english

Fichier:

PDF, 1.85 MB

english, 1990

25

Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl- N - [3-fluoro-2‘-(aminosulfonyl)[1,1‘-biphenyl)]-4-yl]-1 H -pyrazole-5-carboxyamide (DPC602), a Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor 1

Pruitt, James R., Pinto, Donald J. P., Galemmo,, Robert A., Alexander, Richard S., Rossi, Karen A., Wells, Brian L., Drummond, Spencer, Bostrom, Lori L., Burdick, Debra, Bruckner, Robert, Chen, Haiyin

Journal:

Journal of Medicinal Chemistry

Année:

2003

Langue:

english

Fichier:

PDF, 555 KB

english, 2003

26

A Novel Series of [2-[Methyl(2-phenethyl)amino]-2-oxoethyl]benzene-Containing Leukotriene B 4 Antagonists: Initial Structure−Activity Relationships

Huang, Fu-Chih, Chan, Wan-Kit, Moriarty, Kevin J., Poli, Gregory, Morrissette, Matthew M., Galemmo, Robert A., Warus, James D., Dankulich, William P., Sutherland, Charles A.

Journal:

Journal of Medicinal Chemistry

Année:

1996

Langue:

english

Fichier:

PDF, 365 KB

english, 1996

27

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain

Aubele, Danielle L., Hom, Roy K., Adler, Marc, Galemmo, Robert A., Bowers, Simeon, Truong, Anh P., Pan, Hu, Beroza, Paul, Neitz, R. Jeffrey, Yao, Nanhua, Lin, May, Tonn, George, Zhang, Heather, Bova,

Journal:

Année:

2013

Langue:

english

Fichier:

PDF, 1.56 MB

english, 2013

28

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Bowers, Simeon, Truong, Anh P., Ye, Michael, Aubele, Danielle L., Sealy, Jennifer M., Neitz, R. Jeffrey, Hom, Roy K., Chan, Wayman, Dappen, Michael S., Galemmo, Robert A., Konradi, Andrei W., Sham, Hi

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2013

Langue:

english

Fichier:

PDF, 4.73 MB

english, 2013

29

Synthesis of the alleged structure of senoxydene, the triquinane sesquiterpene derived from Senecio oxyodontus

Paquette, Leo A., Galemmo, Robert A., Springer, James P.

Journal:

Journal of the American Chemical Society

Année:

1983

Langue:

english

Fichier:

PDF, 275 KB

english, 1983

30

Contrasting directed-Aldol reactivity of a pair of epimeric trimethylsilyl enol ethers

Galemmo, Robert A., Paquette, Leo A.

Journal:

Journal of Organic Chemistry

Année:

1985

Langue:

english

Fichier:

PDF, 459 KB

english, 1985

31

4,7,7-Trimethyl-cis-bicyclo[3.3.0]oct-3-en-2-one. Potentially useful synthon for triquinane natural products

Paquette, Leo A., Farkas, Eugene, Galemmo, Robert

Journal:

Journal of Organic Chemistry

Année:

1981

Langue:

english

Fichier:

PDF, 459 KB

english, 1981

32

Structure−Activity Relationships Study of Two Series of Leukotriene B 4 Antagonists: Novel Indolyl and Naphthyl Compounds Substituted with a 2-[Methyl(2-phenethyl)amino]-2-oxoethyl Side Chain

Chan, Wan K., Huang, Fu-Chih, Morrissette, Matthew M., Warus, James D., Moriarty, Kevin J., Galemmo, Robert A., Dankulich, William D., Poli, Gregory, Sutherland, Charles A.

Journal:

Journal of Medicinal Chemistry

Année:

1996

Langue:

english

Fichier:

PDF, 774 KB

english, 1996

33

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity

Huang, Fu Chih, Galemmo, Robert A., Poli, Gregory B., Learn, Keith S., Morrissette, Mathew M., Johnson, William H., Dankulich, William P., Campbell, Henry F., Carnathan, Gilbert W., Van Inwegen, Richa

Journal:

Journal of Medicinal Chemistry

Année:

1991

Langue:

english

Fichier:

PDF, 539 KB

english, 1991

34

Synthetic studies relating to the structure of senoxydene. A sequential annulation approach to angular triquinane construction capable of varied tetramethyl substitution patterns

Paquette, Leo A., Galemmo, Robert A., Caille, Jean Claude, Valpey, Richard S.

Journal:

Journal of Organic Chemistry

Année:

1986

Langue:

english

Fichier:

PDF, 1.49 MB

english, 1986

35

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships

Youssefyeh, Raymond D., Magnien, Ernest, Lee, Thomas D. Y., Chan, Wan Kit, Lin, Clara J., Galemmo, Robert A., Johnson, William H., Tan, Jenny, Campbell, Henry F.

Journal:

Journal of Medicinal Chemistry

Année:

1990

Langue:

english

Fichier:

PDF, 1.17 MB

english, 1990

36

Overview: Recent Developments in Sulphidopeptide Leukotriene Receptor Antagonists

Galemmo, Robert A, Gavai, Ashvin, Huang, Fu-Chih

Journal:

Expert Opinion on Therapeutic Patents

Année:

1992

Langue:

english

Fichier:

PDF, 1.45 MB

english, 1992

37

Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment

Owusu, Benjamin, Galemmo, Robert, Janetka, James, Klampfer, Lidija

Journal:

Année:

2017

Langue:

english

Fichier:

PDF, 2.29 MB

english, 2017

38

Inhibition of Factor Xa Reduces Ischemic Brain Damage After Thromboembolic Stroke in Rats

Wang, Xinkang, Xu, Lin, Wang, Hugh, Grzanna, Reinhard, Zhan, Yutian, Knabb, Robert M., Luettgen, Joseph M., Bozarth, Tracy A., Galemmo, Robert A., Wong, Pancras C., Bernard, Roberta, Vargas, Hugo, Cho

Journal:

Année:

2003

Langue:

english

Fichier:

PDF, 401 KB

english, 2003