Search Results - "ILLIG, Carl R"

JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia by Manthey, Carl L, Johnson, Dana L, Illig, Carl R, Tuman, Robert W, Zhou, Zhao, Baker, Judith F, Chaikin, Margery A, Donatelli, Robert R, Franks, Carol F, Zeng, Lee, Crysler, Carl, Chen, Yanmin, Yurkow, Edward J, Boczon, Lisa, Meegalla, Sanath K, Wilson, Kenneth J, Wall, Mark J, Chen, Jinsheng, Ballentine, Shelley K, Ott, Heidi, Baumann, Christian, Lawrence, Danielle, Tomczuk, Bruce E, Molloy, Christopher J

“…There is increasing evidence that tumor-associated macrophages promote the malignancy of some cancers. Colony-stimulating factor-1 (CSF-1) is expressed by many…”
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Design and Optimization of Benzimidazole-Containing Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists by Parks, Daniel J, Parsons, William H, Colburn, Raymond W, Meegalla, Sanath K, Ballentine, Shelley K, Illig, Carl R, Qin, Ning, Liu, Yi, Hutchinson, Tasha L, Lubin, Mary Lou, Stone, Dennis J, Baker, Judith F, Schneider, Craig R, Ma, Jianya, Damiano, Bruce P, Flores, Christopher M, Player, Mark R

“…Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel that is thermoresponsive to cool to cold temperatures (8−28 °C) and also may…”
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Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors by Meegalla, Sanath K., Huang, Hui, Illig, Carl R., Parks, Daniel J., Chen, Jinsheng, Lee, Yu-Kai, Wilson, Kenneth J., Patel, Sharmila K., Cheung, Wing S., Lu, Tianbao, Kirchner, Thomas, Askari, Hossein B., Geisler, John, Patch, Raymond J., Gibbs, Alan C., Rady, Brian, Connelly, Margery, Player, Mark R.

“…[Display omitted] Design and optimization of a novel series of imidazo[1,2-b]pyridazine PDE10a inhibitors are described. Compound 31 displays excellent…”
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Optimization of a Potent Class of Arylamide Colony-Stimulating Factor-1 Receptor Inhibitors Leading to Anti-inflammatory Clinical Candidate 4-Cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141) by Illig, Carl R, Manthey, Carl L, Wall, Mark J, Meegalla, Sanath K, Chen, Jinsheng, Wilson, Kenneth J, Ballentine, Shelley K, DesJarlais, Renee L, Schubert, Carsten, Crysler, Carl S, Chen, Yanmin, Molloy, Christopher J, Chaikin, Margery A, Donatelli, Robert R, Yurkow, Edward, Zhou, Zhao, Player, Mark R, Tomczuk, Bruce E

“…A class of potent inhibitors of colony-stimulating factor-1 receptor (CSF-1R or FMS), as exemplified by 8 and 21, was optimized to improve pharmacokinetic and…”
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Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors by Wall, Mark J., Chen, Jinsheng, Meegalla, Sanath, Ballentine, Shelley K., Wilson, Kenneth J., DesJarlais, Renee L., Schubert, Carsten, Chaikin, Margery A., Crysler, Carl, Petrounia, Ioanna P., Donatelli, Robert R., Yurkow, Edward J., Boczon, Lisa, Mazzulla, Marie, Player, Mark R., Patch, Raymond J., Manthey, Carl L., Molloy, Christopher, Tomczuk, Bruce, Illig, Carl R.

“…A series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as FMS inhibitors. A series of 3,4,6-substituted 2-quinolones has been…”
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Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors by Illig, Carl R., Manthey, Carl L., Meegalla, Sanath K., Wall, Mark J., Chen, Jinsheng, Wilson, Kenneth J., DesJarlais, Renee L., Ballentine, Shelley K., Schubert, Carsten, Crysler, Carl S., Chen, Yanmin, Molloy, Christopher J., Chaikin, Margery A., Donatelli, Robert R., Yurkow, Edward, Zhou, Zhao, Player, Mark R., Tomczuk, Bruce E.

“…Structure–activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase…”
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Discovery of novel FMS kinase inhibitors as anti-inflammatory agents by Illig, Carl R., Chen, Jinsheng, Wall, Mark J., Wilson, Kenneth J., Ballentine, Shelley K., Rudolph, M. Jonathan, DesJarlais, Renee L., Chen, Yanmin, Schubert, Carsten, Petrounia, Ioanna, Crysler, Carl S., Molloy, Christopher J., Chaikin, Margery A., Manthey, Carl L., Player, Mark R., Tomczuk, Bruce E., Meegalla, Sanath K.

“…Discovery of a series of novel 2,4-disubstituted arylamides as potential anti-inflammatory agents is described. Compound 8 was utilized in an in vivo CIA model…”
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Structure-based optimization of a potent class of arylamide FMS inhibitors by Meegalla, Sanath K., Wall, Mark J., Chen, Jinsheng, Wilson, Kenneth J., Ballentine, Shelley K., DesJarlais, Renee L., Schubert, Carsten, Crysler, Carl S., Chen, Yanmin, Molloy, Christopher J., Chaikin, Margery A., Manthey, Carl L., Player, Mark R., Tomczuk, Bruce E., Illig, Carl R.

“…Potent FMS inhibitors possessing a 1,2,4-phenylenetriamine core structure were optimized with the aid of structure-based modeling to alleviate the potential…”
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Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors by WILSON, Kenneth J, ILLIG, Carl R, ZHANG, Marie, LEWANDOWSKI, Frank A, ZHAO ZHOU, SHARP, Celia, MAGUIRE, Diane, GRASBERGER, Bruce, DESJARLAIS, Renee L, SPURLINO, John, SUBASINGHE, Nalin, HOFFMAN, James B, RUDOLPH, M. Jonathan, SOLL, Richard, MOLLOY, Christopher J, BONE, Roger, GREEN, David, RANDALL, Troy

“…The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis…”
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Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors by Wilson, Kenneth J., Illig, Carl R., Chen, Jinsheng, Wall, Mark J., Ballentine, Shelley K., DesJarlais, Renee L., Chen, Yanmin, Schubert, Carsten, Donatelli, Robert, Petrounia, Ioanna, Crysler, Carl S., Molloy, Christopher J., Chaikin, Margery A., Manthey, Carl L., Player, Mark R., Tomczuk, Bruce E., Meegalla, Sanath K.

“…During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were…”
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A novel series of potent and selective small molecule inhibitors of the complement component C1s by Subasinghe, Nalin L., Ali, Farah, Illig, Carl R., Jonathan Rudolph, M., Klein, Scott, Khalil, Ehab, Soll, Richard M., Bone, Roger F., Spurlino, John C., DesJarlais, Renee L., Crysler, Carl S., Cummings, Maxwell D., Morris, Philip E., Kilpatrick, John M., Sudhakara Babu, Y.

“…Graphic Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and…”
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Design and Synthesis of 4,5-Disubstituted-thiophene-2-amidines as Potent Urokinase Inhibitors by Rudolph, M.Jonathan, Illig, Carl R., Subasinghe, Nalin L., Wilson, Kenneth J., Hoffman, James B., Randle, Troy, Green, David, Molloy, Chris J., Soll, Richard M., Lewandowski, Frank, Zhang, Marie, Bone, Roger, Spurlino, John C., Deckman, Ingrid C., Manthey, Carl, Sharp, Celia, Maguire, Diane, Grasberger, Bruce L., DesJarlais, Renée L., Zhou, Zhao

“…A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of…”
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Structural Analysis of Thrombin Complexed with Potent Inhibitors Incorporating a Phenyl Group as a Peptide Mimetic and Aminopyridines as Guanidine Substitutes by Bone, Roger, Lu, Tianbao, Illig, Carl R, Soll, Richard M, Spurlino, John C

“…The structure of the noncovalent complex of human α-thrombin with a nonpeptide inhibitor containing a central phenyl scaffold,…”
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In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors by Lu, Tianbao, Tomczuk, Bruce, Illig, Carl R., Bone, Roger, Murphy, Larry, Spurlino, John, Salemme, F.Raymond, Soll, Richard M.

“…We describe the in vitro evaluation and crystallographic analysis of a new class of potent and selective, non-aminoacid-based, small-molecule thrombin…”
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Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor by TIANBAO LU, SOLL, R. M, ILLIG, C. R, BONE, R, MURPHY, L, SPURLINO, J, SALEMME, F. R, TOMCZUK, B. E

“…The structure activity relationships of a novel series of non-amide-based thrombin inhibitors are described. Exploration of the P2 and the aryl binding region…”
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1,3,5-Trialkyl-2,4,6-triiodobenzenes:  Novel X-ray Contrast Agents for Gastrointestinal Imaging by Estep, Kimberly G, Josef, Kurt A, Bacon, Edward R, Illig, Carl R, Toner, John L, Mishra, Dinesh, Blazak, William F, Miller, Dennis M, Johnson, David K, Allen, Jack M, Spencer, Andy, Wilson, Susan A

“…Examination of the gastrointestinal (GI) tract has been performed for decades using barium sulfate. Although this agent has many recognized limitations…”
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Optimization of a Potent Class of Arylamide Colony-Stimulating Factor-1 Receptor Inhibitors Leading to Anti-inflammatory Clinical Candidate 4-Cyano- N -[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1 H -imidazole-2-carboxamide (JNJ-28312141) by Illig, Carl R., Manthey, Carl L., Wall, Mark J., Meegalla, Sanath K., Chen, Jinsheng, Wilson, Kenneth J., Ballentine, Shelley K., DesJarlais, Renee L., Schubert, Carsten, Crysler, Carl S., Chen, Yanmin, Molloy, Christopher J., Chaikin, Margery A., Donatelli, Robert R., Yurkow, Edward, Zhou, Zhao, Player, Mark R., Tomczuk, Bruce E.

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Stereoselective synthesis of (.+-.)-cyanocycline by Evans, David A, Illig, Carl R, Saddler, John C

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Synthesis of thiophene-2-carboxamidines containing 2-amino-thiazoles and their biological evaluation as urokinase inhibitors by Wilson, Kenneth J., Illig, Carl R., Subasinghe, Nalin, Hoffman, James B., Jonathan Rudolph, M., Soll, Richard, Molloy, Christopher J., Bone, Roger, Green, David, Randall, Troy, Zhang, Marie, Lewandowski, Frank A., Zhou, Zhao, Sharp, Celia, Maguire, Diane, Grasberger, Bruce, DesJarlais, Renee L., Spurlino, John

“…The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis…”
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Amidinohydrazones as guanidine bioisosteres : Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors by SOLL, R. M, LU, T, TOMCZUK, B, ILLIG, C. R, FEDDE, C, EISENNAGEL, S, BONE, R, MURPHY, L, SPURLINO, J, SALEMME, F. R

“…We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a…”
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