Search

Your search keyword '"Moody, Jeanne"' showing total 13 results
Start Over Author "Moody, Jeanne"
13 results on '"Moody, Jeanne"'

1. (7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists

Author

Ben Johnson, Tawfik Gharbaoui, Moody Jeanne, David J. Unett, Kevin Whelan, Ibragim Gaidarov, Michael Morgan, Lars Thoresen, Michelle Kasem, Abu J.M. Sadeque, Robert M. Jones, Chuan Chen, Sun Hee Kim, Hussien A. Al-Shamma, Minh Le, Joel Gatlin, Lorene Calvano, Andrew M. Kawasaki, Lixia Fu, Yinghong Gao, Scott Stirn, Weichao Chen, Jeremy Barden, Dominic P. Behan, Krishnan Ashwin M, Xiuwen Zhu, Graeme Semple, Dipanjan Sengupta, Christopher Ronald J, Jeff Edwards, Luis Lopez, Jayant Thatte, Daniel J. Buzard, Anthony C. Blackburn, Michelle Solomon, Todd Anthony, Thomas O. Schrader, and Khawja A. Usmani

Subjects
Autoimmune disease, Chemistry, Stereochemistry, Organic Chemistry, Pharmacology, medicine.disease, Biochemistry, Fingolimod, chemistry.chemical_compound, Pharmacokinetics, Drug Discovery, medicine, Sphingosine-1-phosphate, Direct acting, medicine.drug
Abstract

S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acids as potent, centrally available, direct acting S1P1 functional antagonists, with favorable pharmacokinetic and safety properties.

Published
2014

2. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor

Author

Weichao Chen, Andrew M. Kawasaki, Dominic P. Behan, Jeff Edwards, You-An Ma, Tawfik Gharbaoui, Sun Hee Kim, Jayant Thatte, Hussien A. Al-Shamma, Carleton R. Sage, Jeremy Barden, Anthony C. Blackburn, Michelle Solomon, Xiuwen Zhu, Christopher Ronald J, David Mills, Ibragim Gaidarov, Antonio Garrido Montalban, Sangdon Han, Luis Lopez, Dipanjan Sengupta, Michael Morgan, Juerg Lehmann, Daniel J. Buzard, Graeme Semple, Kevin Whelan, Yinghong Gao, Joel Gatlin, Moody Jeanne, David J. Unett, Imelda Calderon, Lars Thoresen, Robert M. Jones, Brett Ullman, Todd Anthony, Chuan Chen, Minh Le, Khawja A. Usmani, Scott Stirn, Jaimie Karyn Rueter, Lixia Fu, Lorene Calvano, and Abu J.M. Sadeque

Subjects
business.industry, S1p1 receptor, Multiple sclerosis, Lymphocyte, Organic Chemistry, Experimental autoimmune encephalomyelitis, Antagonist, Pharmacology, medicine.disease, Biochemistry, Fingolimod, chemistry.chemical_compound, medicine.anatomical_structure, chemistry, Drug Discovery, medicine, Sphingosine-1-phosphate, business, Receptor, medicine.drug
Abstract

APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD334 is a potent functional antagonist of S1P1 and has a favorable PK/PD profile, producing robust lymphocyte lowering at relatively low plasma concentrations in several preclinical species. This new agent was efficacious in a mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model and was found to have appreciable central exposure.

Published
2014

3. Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease

Author

Joel Gatlin, Kevin Whelan, Michael Morgan, Juerg Lehmann, Lixia Fu, Yinghong Gao, Moody Jeanne, Minh Le, Hussien A. Al-Shamma, Jeremy Barden, Khawja A. Usmani, Jeff Edwards, Chuan Chen, Jayant Thatte, Dipanjan Sengupta, Xiuwen Zhu, Abu J.M. Sadeque, Imelda Calderon, Michelle Solomon, Lars Thoresen, Tawfik Gharbaoui, Robert M. Jones, Ling Liu, Luis Lopez, Daniel J. Buzard, Brett Ullman, Krishnan Ashwin M, Sheryll Espinola, Charles Xing, Sangdon Han, and Andrew M. Kawasaki

Subjects
Autoimmune disease, chemistry.chemical_classification, Chemistry, Sphingosine-1-phosphate receptor, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, medicine.disease, Biochemistry, In vitro, Sprague dawley, In vivo, Drug Discovery, medicine, Molecular Medicine, Structure–activity relationship, lipids (amino acids, peptides, and proteins), Receptor, Molecular Biology, Tricyclic
Abstract

Two series of fused tricyclic indoles were identified as potent and selective S1P(1) agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoimmune disease. Importantly, these agonists were devoid of any activity at the S1P(3) receptor in vitro, and correspondingly did not produce S1P(3) mediated bradycardia in telemeterized rat.

Published
2012

5. Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P1 agonists

Author

Lixia Fu, Jeremy Barden, Joel Gatlin, Andrew M. Kawasaki, Minh Le, Jeff Edwards, Hussien A. Al-Shamma, Jayant Thatte, Charles Xing, Yinghong Gao, Moody Jeanne, Michelle Solomon, Sangdon Han, Carleton R. Sage, Thomas O. Schrader, Sheryll Espinola, Luis Lopez, Daniel J. Buzard, Ling Liu, Lars Thoresen, and Robert M. Jones

Subjects
Autoimmune disease, S1p1 receptor, Chemistry, Sphingosine-1-phosphate receptor, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Butanoic Acids, medicine.disease, Biochemistry, Drug Discovery, medicine, Molecular Medicine, Molecular Biology
Abstract

S1P1 receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P1 receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P1 receptor agonists.

Published
2011

6. Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor

Author

Jeremy Barden, Andrew M. Kawasaki, Xiuwen Zhu, Joel Gatlin, Juerg Lehmann, Sun Hee Kim, Luis Lopez, Daniel J. Buzard, Sangdon Han, Ben Johnson, Yinghong Gao, Jeff Edwards, Moody Jeanne, Jayant Thatte, Thomas O. Schrader, Robert M. Jones, and Michelle Kasem

Subjects
Indoles, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Biochemistry, Rats, Sprague-Dawley, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Dogs, Pharmacokinetics, Drug Discovery, medicine, Potency, Animals, Humans, Protein Isoforms, Sphingosine-1-phosphate, Molecular Biology, Autoimmune disease, Indole test, chemistry.chemical_classification, S1p1 receptor, Organic Chemistry, medicine.disease, Bioavailability, Rats, Receptors, Lysosphingolipid, chemistry, Drug Design, Molecular Medicine, Tricyclic, Half-Life, Protein Binding
Abstract

Modulators of S1P1 have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P1 chemotypes were designed and optimized for potency and oral bioavailability. These new agents are characterized by a ‘tricyclic fused indole array’ and are highly potent agonists of the S1P1 receptor.

Published
2014

7. Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease

Author

Buzard, Daniel J., Han, Sangdon, Lopez, Luis, Kawasaki, Andrew, Moody, Jeanne, Thoresen, Lars, Ullman, Brett, Lehmann, Juerg, Calderon, Imelda, Zhu, Xiuwen, Gharbaoui, Tawfik, Sengupta, Dipanjan, Krishnan, Ashwin, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Morgan, Michael, Usmani, Khawja, Chen, Chuan, Sadeque, Abu, Thatte, Jayant, Solomon, Michelle, Fu, Lixia, Whelan, Kevin, Liu, Ling, Al-Shamma, Hussien, Gatlin, Joel, Le, Minh, Xing, Charles, Espinola, Sheryll, and Jones, Robert M.

Published
2012
Full Text
View/download PDF

8. Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P 1 agonists

Author

Buzard, Daniel, Han, Sangdon, Thoresen, Lars, Moody, Jeanne, Lopez, Luis, Kawasaki, Andrew, Schrader, Thomas, Sage, Carleton, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Liu, Ling, Al-Shamma, Hussien, Gatlin, Joel, Le, Minh, Xing, Charles, Espinola, Sheryll, and Jones, Robert M.

Published
2011
Full Text
View/download PDF

9. (7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists

Author

Buzard, Daniel J., primary, Lopez, Luis, additional, Moody, Jeanne, additional, Kawasaki, Andrew, additional, Schrader, Thomas O., additional, Kasem, Michelle, additional, Johnson, Ben, additional, Zhu, Xiuwen, additional, Thoresen, Lars, additional, Kim, Sun Hee, additional, Gharbaoui, Tawfik, additional, Sengupta, Dipanjan, additional, Calvano, Lorene, additional, Krishnan, Ashwin, additional, Gao, Yinghong, additional, Semple, Graeme, additional, Edwards, Jeff, additional, Barden, Jeremy, additional, Morgan, Michael, additional, Usmani, Khawja, additional, Chen, Chuan, additional, Sadeque, Abu, additional, Chen, Weichao, additional, Christopher, Ronald J., additional, Thatte, Jayant, additional, Fu, Lixia, additional, Solomon, Michelle, additional, Whelan, Kevin, additional, Al-Shamma, Hussien, additional, Gatlin, Joel, additional, Gaidarov, Ibragim, additional, Anthony, Todd, additional, Le, Minh, additional, Unett, David J., additional, Stirn, Scott, additional, Blackburn, Anthony, additional, Behan, Dominic P., additional, and Jones, Robert M., additional

Published
2014
Full Text
View/download PDF

10. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor

Author

Buzard, Daniel J., primary, Kim, Sun Hee, additional, Lopez, Luis, additional, Kawasaki, Andrew, additional, Zhu, Xiuwen, additional, Moody, Jeanne, additional, Thoresen, Lars, additional, Calderon, Imelda, additional, Ullman, Brett, additional, Han, Sangdon, additional, Lehmann, Juerg, additional, Gharbaoui, Tawfik, additional, Sengupta, Dipanjan, additional, Calvano, Lorene, additional, Montalban, Antonio Garrido, additional, Ma, You-An, additional, Sage, Carleton, additional, Gao, Yinghong, additional, Semple, Graeme, additional, Edwards, Jeff, additional, Barden, Jeremy, additional, Morgan, Michael, additional, Chen, Weichao, additional, Usmani, Khawja, additional, Chen, Chuan, additional, Sadeque, Abu, additional, Christopher, Ronald J., additional, Thatte, Jayant, additional, Fu, Lixia, additional, Solomon, Michelle, additional, Mills, David, additional, Whelan, Kevin, additional, Al-Shamma, Hussien, additional, Gatlin, Joel, additional, Le, Minh, additional, Gaidarov, Ibragim, additional, Anthony, Todd, additional, Unett, David J., additional, Blackburn, Anthony, additional, Rueter, Jaimie, additional, Stirn, Scott, additional, Behan, Dominic P., additional, and Jones, Robert M., additional

Published
2014
Full Text
View/download PDF

11. Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P1 agonists

Author

Buzard, Daniel, primary, Han, Sangdon, additional, Thoresen, Lars, additional, Moody, Jeanne, additional, Lopez, Luis, additional, Kawasaki, Andrew, additional, Schrader, Thomas, additional, Sage, Carleton, additional, Gao, Yinghong, additional, Edwards, Jeff, additional, Barden, Jeremy, additional, Thatte, Jayant, additional, Fu, Lixia, additional, Solomon, Michelle, additional, Liu, Ling, additional, Al-Shamma, Hussien, additional, Gatlin, Joel, additional, Le, Minh, additional, Xing, Charles, additional, Espinola, Sheryll, additional, and Jones, Robert M., additional

Published
2011
Full Text
View/download PDF

12. Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease

Author

Buzard, Daniel J., Han, Sangdon, Lopez, Luis, Kawasaki, Andrew, Moody, Jeanne, Thoresen, Lars, Ullman, Brett, Lehmann, Juerg, Calderon, Imelda, Zhu, Xiuwen, Gharbaoui, Tawfik, Sengupta, Dipanjan, Krishnan, Ashwin, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Morgan, Michael, Usmani, Khawja, Chen, Chuan, and Sadeque, Abu

Subjects
*AUTOIMMUNE diseases, *INDOLE compounds, *DRUG efficacy, *DRUG synergism, *SPHINGOSINE-1-phosphate, *LYMPHOCYTES, *LABORATORY rodents, *BRADYCARDIA, *LABORATORY rats
Abstract

Abstract: Two series of fused tricyclic indoles were identified as potent and selective S1P1 agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoimmune disease. Importantly, these agonists were devoid of any activity at the S1P3 receptor in vitro, and correspondingly did not produce S1P3 mediated bradycardia in telemeterized rat. [Copyright &y& Elsevier]

Published
2012
Full Text
View/download PDF

13. Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P1 agonists

Author

Buzard, Daniel, Han, Sangdon, Thoresen, Lars, Moody, Jeanne, Lopez, Luis, Kawasaki, Andrew, Schrader, Thomas, Sage, Carleton, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Liu, Ling, Al-Shamma, Hussien, Gatlin, Joel, Le, Minh, Xing, Charles, and Espinola, Sheryll

Subjects
*PHARMACEUTICAL research, *DRUG synergism, *BUTYRIC acid, *LYMPHOPENIA, *AUTOIMMUNE disease treatment, *SPHINGOSINE, *PHOSPHATES, *DRUG receptors
Abstract

Abstract: S1P1 receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P1 receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P1 receptor agonists. [Copyright &y& Elsevier]

Published
2011
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results