2250-53-5Relevant academic research and scientific papers
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone
Carter, Percy H.,Brown, Gregory D.,King, Sarah R.,Voss, Matthew E.,Tebben, Andrew J.,Cherney, Robert J.,Mandlekar, Sandhya,Lo, Yvonne C.,Yang, Gengjie,Miller, Persymphonie B.,Scherle, Peggy A.,Zhao, Qihong,Decicco, Carl P.
body text, p. 3311 - 3316 (2012/06/18)
We describe an isostere-driven approach to improve upon a previously-described series of capped dipeptide antagonists of CC Chemokine Receptor 2 (CCR2). Modification of the substitution around the isostere was combined with additional changes in a distal
CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
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Page/Page column 93, (2012/01/03)
The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
Design, synthesis and SAR of indazole and benzoisoxazole containing 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
Zhang, Xuqing,Hufnagel, Heather,Hou, Cuifen,Opas, Evan,McKenney, Sandra,Crysler, Carl,O'Neill, John,Johnson, Dana,Sui, Zhihua
supporting information; experimental part, p. 6042 - 6048 (2011/11/06)
A novel series of 4-azetidinyl-1-aryl-cyclohexanes containing indazole or benzoisoxazole moiety have been identified as potent CCR2 antagonists with high selectivity versus hERG.
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
Vasudevan, Anil,Souers, Andrew J.,Freeman, Jennifer C.,Verzal, Mary K.,Gao, Ju,Mulhern, Mathew M.,Wodka, Derek,Lynch, John K.,Engstrom, Kenneth M.,Wagaw, Seble H.,Brodjian, Sevan,Dayton, Brian,Falls, Doug H.,Bush, Eugene,Brune, Michael,Shapiro, Robin D.,Marsh, Kennan C.,Hernandez, Lisa E.,Collins, Christine A.,Kym, Philip R.
, p. 5293 - 5297 (2007/10/03)
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 46, (2010/02/11)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
Cyclic derivatives as modulators of chemokine receptor activity
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, (2008/06/13)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and
3-Aminoindazole derivatives
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, (2008/06/13)
.Iadd.Pharmaceutical compositions having muscle relaxant and analgesic activity containing 3-aminoindazoles..Iaddend.
