Search Results - "Palovich, Michael R"

Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases by Salmon, Michael, Luttmann, Mark A, Foley, James J, Buckley, Peter T, Schmidt, Dulcie B, Burman, Miriam, Webb, Edward F, DeHaas, Christopher J, Kotzer, Charles J, Barrett, Victoria J, Slack, Robert J, Sarau, Henry M, Palovich, Michael R, Lainé, Dramane I, Hay, Douglas W P, Rumsey, William L

“…Activation of muscarinic subtype 3 (M3) muscarinic cholinergic receptors (mAChRs) increases airway tone, whereas its blockade improves lung function and…”
Get more information

Quality guidelines for oral drug candidates: dose, solubility and lipophilicity by Bayliss, Martin K., Butler, James, Feldman, Paul L., Green, Darren V.S., Leeson, Paul D., Palovich, Michael R., Taylor, Anthony J.

“…[Display omitted] •Experimental properties of GSK's oral portfolio were compared with marketed drugs.•Properties were dose, solubility and the property…”
Get full text

Comparison of N, N′-diarylsquaramides and N, N′-diarylureas as antagonists of the CXCR2 chemokine receptor by McCleland, Brent W., Davis, Roderick S., Palovich, Michael R., Widdowson, Katherine L., Werner, Michelle L., Burman, Miriam, Foley, James J., Schmidt, Dulcie B., Sarau, Henry M., Rogers, Martin, Salyers, Kevin L., Gorycki, Peter D., Roethke, Theresa J., Stelman, Gary J., Azzarano, Leonard M., Ward, Keith W., Busch-Petersen, Jakob

“…N, N′-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2…”
Get full text

Discovery of Novel 1-Azoniabicyclo[2.2.2]octane Muscarinic Acetylcholine Receptor Antagonists by Lainé, Dramane I, McCleland, Brent, Thomas, Sonia, Neipp, Christopher, Underwood, Brian, Dufour, Jeremy, Widdowson, Katherine L, Palovich, Michael R, Blaney, Frank E, Foley, James J, Webb, Edward F, Luttmann, Mark A, Burman, Miriam, Belmonte, Kristen, Salmon, Michael

“…A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure−activity…”
Get full text

Tyrosine urea muscarinic acetylcholine receptor antagonists: Achiral quaternary ammonium groups by Jin, Qi, Davis, Roderick S., Bullion, Ann M., Jin, Jian, Wang, Yonghui, Widdowson, Katherine L., Palovich, Michael R., Foley, James J., Schmidt, Dulcie B., Buckley, Peter T., Webb, Edward F., Salmon, Michael, Belmonte, Kristen E., Sarau, Henry M., Busch-Petersen, Jakob

“…Novel tyrosine-based, long-acting inhaled muscarinic antagonists: preparation, SAR and biological evaluation. Tyrosine ureas had been identified as potent…”
Get full text

Design, synthesis and structure–activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists by Lainé, Dramane I., Yan, Hongxing, Xie, Haibo, Davis, Roderick S., Dufour, Jeremy, Widdowson, Katherine L., Palovich, Michael R., Wan, Zehong, Foley, James J., Schmidt, Dulcie B., Hunsberger, Gerald E., Burman, Miriam, Bacon, Alicia M., Webb, Edward F., Luttmann, Mark A., Salmon, Michael, Sarau, Henry M., Umbrecht, Sandra T., Landis, Philip S., Peck, Brian J., Busch-Petersen, Jakob

“…Novel tropane-based, ultra long-acting inhaled muscarinic antagonists: preparation, biological evaluation and developability. A novel series of N-substituted…”
Get full text

Design, Synthesis, and Structure−Activity Relationship of Tropane Muscarinic Acetylcholine Receptor Antagonists by Lainé, Dramane I, Wan, Zehong, Yan, Hongxing, Zhu, Chongjie, Xie, Haibo, Fu, Wei, Busch-Petersen, Jakob, Neipp, Christopher, Davis, Roderick, Widdowson, Katherine L, Blaney, Frank E, Foley, James, Bacon, Alicia M, Webb, Edward F, Luttmann, Mark A, Burman, Miriam, Sarau, Henry M, Salmon, Michael, Palovich, Michael R, Belmonte, Kristen

“…Novel tropane derivatives were characterized as muscarinic acetylcholine receptor antagonists (mAChRs). Through optimization of the structure−activity…”
Get full text

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists by Wang, Yonghui, Busch-Petersen, Jakob, Wang, Feng, Ma, Lanping, Fu, Wei, Kerns, Jeffrey K, Jin, Jian, Palovich, Michael R, Shen, Jing-Kang, Burman, Miriam, Foley, James J, Schmidt, Dulcie B, Hunsberger, Gerald E, Sarau, Henry M, Widdowson, Katherine L

“…A series of 3-arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides were prepared and shown to be novel and selective antagonists of the CXCR2 receptor…”
Get full text

N, N′-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors by Nie, Hong, Widdowson, Katherine L., Palovich, Michael R., Fu, Wei, Elliott, John D., Bryan, Deborah L., Burman, Miriam, Schmidt, Dulcie B., Foley, James J., Sarau, Henry M., Busch-Petersen, Jakob

“…A series of N-(2-hydroxy-3-sulfonamidobenzene)- N′-arylcyanoguanidines was prepared. In general, these compounds proved to be potent antagonists of CXCR2 while…”
Get full text

Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists by Lainé, Dramane I., Xie, Haibo, Buffet, Noémie, Foley, James J., Buckley, Peter, Webb, Edward F., Widdowson, Katherine L., Palovich, Michael R., Belmonte, Kristen E.

“…In the course of our research program to develop novel muscarinic receptor antagonists for the treatment of COPD, new tropane carbamate derivatives were…”
Get full text

Discovery of potent and orally bioavailable N, N′-diarylurea antagonists for the CXCR2 chemokine receptor by Jin, Qi, Nie, Hong, McCleland, Brent W., Widdowson, Katherine L., Palovich, Michael R., Elliott, John D., Goodman, Richard M., Burman, Miriam, Sarau, Henry M., Ward, Keith W., Nord, Melanie, Orr, Bonnie M., Gorycki, Peter D., Busch-Petersen, Jakob

“…A series of 3-substituted N, N′-diarylureas was prepared and CXCR2 receptor affinities as well as pharmacokinetic properties were examined. A series of…”
Get full text

Synthesis of Stereopentad Subunits of Zincophorin and Rifamycin-S through Use of Chiral Allenyltin Reagents by Marshall, James A, Palovich, Michael R

“…The anti,anti adduct 3, from addition of the allenic stannane (P)-2 to the α-methyl-β-OBn aldehyde (S)-1 promoted by SnCl4, was converted to the stereopentad 6…”
Get full text

Comparative Studies on the Synthesis of an anti,syn Stereotriad with Chiral Allenylstannane and Allenylindium Reagents by Marshall, James A, Palovich, Michael R

“…Addition of the chloroallenylstannane derived from the Bu3Sn allene (S)-2 and SnCl4 to nonracemic α-methyl-β-oxygenated aldehyde 1a afforded mixtures of…”
Get full text

Enantioselective and Diastereoselective Additions of Allylic Stannanes to Aldehydes Promoted by a Chiral (Acyloxy)borane Catalyst by Marshall, James A, Palovich, Michael R

“…A modified Yamamoto Lewis acid (CAB), prepared from the 2,6-dimethoxybenzoic ester of (R,R)-tartaric acid, and 1.5 equiv of BH3·THF was employed in additions…”
Get full text

Discovery of Novel l-Azoniabicyclo[2.2.2]octane Muscarinic Acetylcholine Receptor Antagonists by LAINE, Dramane I, MCCLELAND, Brent, WEBB, Edward F, LUTTMANN, Mark A, BURMAN, Miriam, BELMONTE, Kristen, SALMON, Michael, THOMAS, Sonia, NEIPP, Christopher, UNDERWOOD, Brian, DUFOUR, Jeremy, WIDDOWSON, Katherine L, PALOVICH, Michael R, BLANEY, Frank E, FOLEY, James J

Get full text

3-Arylamino-2 H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists by Wang, Yonghui, Busch-Petersen, Jakob, Wang, Feng, Ma, Lanping, Fu, Wei, Kerns, Jeffrey K., Jin, Jian, Palovich, Michael R., Shen, Jing-Kang, Burman, Miriam, Foley, James J., Schmidt, Dulcie B., Hunsberger, Gerald E., Sarau, Henry M., Widdowson, Katherine L.

“…Synthesis, structure and activity relationships, selectivity and developability properties for a new class of CXCR2 receptor antagonists are described. A…”
Get full text

3 -arylamino -2H-1,2,4 -benzothiadiazin -5 -ol 1,1-dioxides as novel and selective CXCR antagonists by YONGHUI WANG, BUSCH-PETERSEN, Jakob, FOLEY, James J, SCHMIDT, Dulcie B, HUNSBERGER, Gerald E, SARAU, Henry M, WIDDOWSON, Katherine L, FENG WANG, LANPING MA, WEI FU, KERNS, Jeffrey K, JIAN JIN, PALOVICH, Michael R, SHEN, Jing-Kang, BURMAN, Miriam

Get full text