Search Results - "Iyengar, Rajesh"

The CNS-penetrant soluble guanylate cyclase stimulator CYR119 attenuates markers of inflammation in the central nervous system by Correia, Susana S, Liu, Guang, Jacobson, Sarah, Bernier, Sylvie G, Tobin, Jenny V, Schwartzkopf, Chad D, Atwater, Emily, Lonie, Elisabeth, Rivers, Sam, Carvalho, Andrew, Germano, Peter, Tang, Kim, Iyengar, Rajesh R, Currie, Mark G, Hadcock, John R, Winrow, Christopher J, Jones, Juli E

“…Inflammation in the central nervous system (CNS) is observed in many neurological disorders. Nitric oxide-soluble guanylate cyclase-cyclic guanosine…”
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The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases by Correia, Susana S., Iyengar, Rajesh R., Germano, Peter, Tang, Kim, Bernier, Sylvie G., Schwartzkopf, Chad D., Tobin, Jenny, Lee, Thomas W.-H., Liu, Guang, Jacobson, Sarah, Carvalho, Andrew, Rennie, Glen R., Jung, Joon, Renhowe, Paul A., Lonie, Elisabeth, Winrow, Christopher J., Hadcock, John R., Jones, Juli E., Currie, Mark G.

“…Effective treatments for neurodegenerative diseases remain elusive and are critically needed since the burden of these diseases increases across an aging…”
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Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator by Rennie, Glen R., Barden, Timothy C., Bernier, Sylvie G., Carvalho, Andrew, Deming, Renee, Germano, Peter, Hudson, Colleen, Im, G-Yoon J., Iyengar, Rajesh R., Jia, Lei, Jung, Joon, Kim, Elise, Lee, Thomas W.-H., Mermerian, Ara, Moore, Joel, Nakai, Takashi, Perl, Nicholas R., Tobin, Jenny, Zimmer, Daniel P., Renhowe, Paul A.

“…[Display omitted] Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC…”
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Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor by Zhao, Gang, Souers, Andrew J, Voorbach, Martin, Falls, H. Doug, Droz, Brian, Brodjian, Sevan, Lau, Yau Yi, Iyengar, Rajesh R, Gao, Ju, Judd, Andrew S, Wagaw, Seble H, Ravn, Matthew M, Engstrom, Kenneth M, Lynch, John K, Mulhern, Mathew M, Freeman, Jennifer, Dayton, Brian D, Wang, Xiaojun, Grihalde, Nelson, Fry, Dennis, Beno, David W. A, Marsh, Kennan C, Su, Zhi, Diaz, Gilbert J, Collins, Christine A, Sham, Hing, Reilly, Regina M, Brune, Michael E, Kym, Philip R

“…A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of obesity and postprandial chylomicron excursion to validate DGAT-1…”
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Revisiting a Classic Approach to the Aspidosperma Alkaloids:  An Intramolecular Schmidt Reaction Mediated Synthesis of (+)-Aspidospermidine by Iyengar, Rajesh, Schildknegt, Klaas, Morton, Martha, Aubé, Jeffrey

“…A total synthesis of (+)-aspidospermidine (1) is described. The key reactions used in the synthesis of this pentacyclic Aspidosperma alkaloid were a…”
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Regiocontrol in an Intramolecular Schmidt Reaction:  Total Synthesis of (+)-Aspidospermidine by Iyengar, Rajesh, Schildknegt, Klaas, Aubé, Jeffrey

“…A total synthesis of (+)-aspidospermidine (1) is described, featuring an intramolecular Schmidt reaction as the key step. The effects of stereochemistry and…”
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Discovery and SAR development of thienopyridones: A class of small molecule AMPK activators by Zhao, Gang, Iyengar, Rajesh R., Judd, Andrew S., Cool, Barbara, Chiou, William, Kifle, Lemma, Frevert, Ernst, Sham, Hing, Kym, Philip R.

“…AMP-activated protein kinase (AMPK) is well established as a sensor and regulator of intracellular and whole-body energy metabolism. A high-throughput screen…”
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An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists by Iyengar, Rajesh R., Lynch, John K., Mulhern, Mathew M., Judd, Andrew S., Freeman, Jennifer C., Gao, Ju, Souers, Andrew J., Zhao, Gang, Wodka, Dariusz, Doug Falls, H., Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Swanson, Sue, Su, Zhi, Martin, Ruth L., Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Collins, Christine A., Sham, Hing L., Kym, Philip R.

“…The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety…”
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Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity by Judd, Andrew S., Souers, Andrew J., Wodka, Dariusz, Zhao, Gang, Mulhern, Mathew M., Iyengar, Rajesh R., Gao, Ju, Lynch, John K., Freeman, Jennifer C., Falls, H. Douglas, Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Gintant, Gary, Limberis, James T., Mikhail, Ann, Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Bush, Eugene N., Shapiro, Robin, Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Sham, Hing L., Collins, Christine A., Kym, Philip R.

“…A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human…”
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Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: The effects of chirality on substituted indan-1-ylamines by Souers, Andrew J., Iyengar, Rajesh R., Judd, Andrew S., Beno, David W.A., Gao, Ju, Zhao, Gang, Brune, Michael E., Napier, James J., Mulhern, Mathew M., Lynch, John K., Freeman, Jennifer C., Wodka, Dariusz, Chen, Chong J., Falls, H. Doug, Brodjian, Sevan, Dayton, Brian D., Diaz, Gilbert J., Bush, Eugene N., Shapiro, Robin, Droz, Brian A., Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Reilly, Regina M., Sham, Hing L., Collins, Christine A., Kym, Philip R.

“…The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the…”
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Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome by Cool, Barbara, Zinker, Bradley, Chiou, William, Kifle, Lemma, Cao, Ning, Perham, Matthew, Dickinson, Robert, Adler, Andrew, Gagne, Gerard, Iyengar, Rajesh, Zhao, Gang, Marsh, Kennan, Kym, Philip, Jung, Paul, Camp, Heidi S., Frevert, Ernst

“…AMP-activated protein kinase (AMPK) is a key sensor and regulator of intracellular and whole-body energy metabolism. We have identified a thienopyridone family…”
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Utility of the APACHE IV, PPI, and Combined APACHE IV With PPI for Predicting Overall and Disease-Specific ICU and ACU Mortality by Burkmar, Jennifer A., Iyengar, Rajesh

“…Background: The Acute Physiology and Chronic Health Evaluation (APACHE) IV and Palliative Performance Index (PPI) are scales commonly used to assess prognosis…”
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APACHE IV Versus PPI for Predicting Community Hospital ICU Mortality by Shrope-Mok, Shaffer R., Propst, Katie A., Iyengar, Rajesh

“…Background: Both the Acute Physiology and Chronic Health Evaluation (APACHE) IV and Palliative Performance Index (PPI) are scales used to estimate intensive…”
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Optimization of Chromone-2-carboxamide Melanin Concentrating Hormone Receptor 1 Antagonists:  Assessment of Potency, Efficacy, and Cardiovascular Safety by Lynch, John K, Freeman, Jennifer C, Judd, Andrew S, Iyengar, Rajesh, Mulhern, Mathew, Zhao, Gang, Napier, James J, Wodka, Dariusz, Brodjian, Sevan, Dayton, Brian D, Falls, Doug, Ogiela, Christopher, Reilly, Regina M, Campbell, Thomas J, Polakowski, James S, Hernandez, Lisa, Marsh, Kennan C, Shapiro, Robin, Knourek-Segel, Victoria, Droz, Brian, Bush, Eugene, Brune, Michael, Preusser, Lee C, Fryer, Ryan M, Reinhart, Glenn A, Houseman, Kathryn, Diaz, Gilbert, Mikhail, Ann, Limberis, James T, Sham, Hing L, Collins, Christine A, Kym, Philip R

“…Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to…”
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Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety by Basso, Ana M., Bratcher, Natalie A., Gallagher, Kelly B., Cowart, Marlon D., Zhao, Chen, Sun, Minghua, Esbenshade, Timothy A., Brune, Michael E., Fox, Gerard B., Schmidt, Martin, Collins, Christine A., Souers, Andrew J., Iyengar, Rajesh, Vasudevan, Anil, Kym, Philip R., Hancock, Arthur A., Rueter, Lynne E.

“…The aim of this study was to validate melanin-concentrating hormone (MCH)-1 receptor antagonism as a potential treatment of mood disorders. We attempted to…”
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Discovery of IWP-051, a Novel Orally Bioavailable Soluble Guanylate Cyclase Stimulator with Sustained and Dose-Dependent Hemodynamic Effects by Nakai, Takashi, Perl, Nicholas R, Iyengar, Rajesh R, Mermerian, Ara, Im, G-Yoon J, Lee, Thomas W-H, Rennie, Glen R, Jia, James, Renhowe, Paul A, Barden, Timothy C, Sheppeck, James E, Iyer, Karthik, Jung, Joon, Milne, G Todd, Segal, Chrissie, Long, Kimberly, Miyashiro, Joy, Bernier, Sylvie, Jacobson, Sarah, Tobin, Jenny, Shea, Courtney, Germano, Peter, Chien, Yueh-tyng, Zimmer, Daniel

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Screening for Cardiovascular Safety:  A Structure−Activity Approach for Guiding Lead Selection of Melanin Concentrating Hormone Receptor 1 Antagonists by Kym, Philip R, Souers, Andrew J, Campbell, Thomas J, Lynch, John K, Judd, Andrew S, Iyengar, Rajesh, Vasudevan, Anil, Gao, Ju, Freeman, Jennifer C, Wodka, Dariusz, Mulhern, Mathew, Zhao, Gang, Wagaw, Seble H, Napier, James J, Brodjian, Sevan, Dayton, Brian D, Reilly, Regina M, Segreti, Jason A, Fryer, Ryan M, Preusser, Lee C, Reinhart, Glenn A, Hernandez, Lisa, Marsh, Kennan C, Sham, Hing L, Collins, Christine A, Polakowski, James S

“…An inactin-anesthetized rat cardiovascular (CV) assay was employed in a screening mode to triage multiple classes of melanin-concentrating hormone receptor 1…”
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Lead optimization strategies and tactics applied to the discovery of melanin concentrating hormone receptor 1 antagonists by Kym, Philip R, Judd, Andrew S, Lynch, John K, Iyengar, Rajesh, Vasudevan, Anil, Souers, Andrew J

“…The discovery of small molecule melanin concentrating hormone receptor (MCHr1) antagonists as novel therapeutic agents for the treatment of obesity has been…”
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Stereoselective syntheses of substituted pterocarpans with anti-HIV activity, and 5-aza-/5-thia-pterocarpan and 2-aryl-2,3-dihydrobenzofuran analogues by Engler, Thomas A., LaTessa, Kenneth O., Iyengar, Rajesh, Chai, Wenying, Agrios, Konstantinos

“…Oxygenated pterocarpans and 5-azapterocarpans are prepared utilizing Lewis acid-promoted reactions of 2-alkoxy-1,4-benzoquinones with 2 H-chromenes and…”
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Asymmetric Reactions of 2-Methoxy-1,4-benzoquinones with Styrenyl Systems:  Enantioselective Syntheses of 8-Aryl-3-methoxybicyclo[4.2.0]oct-3-en-2,5-diones, 7-Aryl-3-hydroxybicyclo[3.2.1]oct-3-en-2,8-diones, 2-Aryl-6-methoxy-2,3-dihydrobenzofuran-5-ols, and Pterocarpans by Engler, Thomas A, Letavic, Michael A, Iyengar, Rajesh, LaTessa, Kenneth O, Reddy, Jayachandra P

“…Reactions of 2-methoxy-1,4-benzoquinones 2 and 3 with (E)-propenylbenzenes 1 promoted at −78 °C by Ti(IV)−TADDOLates prepared from diol-(+)-4 afford…”
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