- Identification of novel azaindazole CCR1 antagonist clinical candidates
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Exploring various cyclization strategies, using a submicromolar pyrazole HTS screening hit 6 as a starting point, a novel indazole based CCR1 antagonist core was discovered. This report presents the design and SAR of CCR1 indazole and azaindazole antagonists leading to the identification of three development compounds, including 19e that was advanced to early clinical trials.
- Harcken, Christian,Kuzmich, Daniel,Cook, Brain,Mao, Can,Disalvo, Darren,Razavi, Hossein,Swinamer, Alan,Liu, Pingrong,Zhang, Qiang,Kukulka, Alison,Skow, Donna,Patel, Mita,Patel, Monica,Fletcher, Kimberly,Sherry, Tara,Joseph, David,Smith, Dustin,Canfield, Melissa,Souza, Donald,Bogdanffy, Matthew,Berg, Karen,Brown, Maryanne
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p. 441 - 448
(2019/01/04)
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- INDAZOLE AND PYRAZOLOPYRIDINE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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Diclosed are CCRl receptor antagonists of the formula (I), wherein X is nitrogen or, C-R2; Ar1 is carbocycle, heteroaryl or heterocyclyl each optionally substituted by one to three Ra; Ar2 is carbocycle, heteroaryl or heterocyclyl, each optionally substituted by one to three Rb; Cyclic G is carbocycle, or heterocyclyl each optionally substituted by one to two R8; R1 is hydrogen, C1-6 alkyl or C 1-6 alkoxyC1-6 alkyl. Also disclosed are compositions, methods of making and using compounds of the formula (I).
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Page/Page column 41
(2011/05/06)
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- AZAINDAZOLE AMIDE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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Disclosed are CCR1 inhibitor compounds of the formula (I): which are useful in the treatment of autoimmune and other diseases. Also disclosed a pharmaceutical compositions containing the same, and methods of making and using same.
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Page/Page column 18-19
(2011/11/13)
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- AZAINDAZOLE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
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Page/Page column 109
(2010/04/27)
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