669066-35-7Relevant academic research and scientific papers
Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors
Sabat, Mark,Wang, Haixia,Scorah, Nick,Lawson, J. David,Atienza, Joy,Kamran, Ruhi,Hixon, Mark S.,Dougan, Douglas R.
, p. 1955 - 1961 (2017/04/10)
A series of potent ALK5 inhibitors were designed using a SBDD approach and subsequently optimized to improve drug likeness. Starting with a 4-substituted quinoline screening hit, SAR was conducted using a ALK5 binding model to understand the binding site
HIV INTEGRASE INHIBITORS
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, (2015/09/22)
The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS
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Paragraph 00296; 00297, (2013/04/13)
Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
PYRAZOLO[4,3-B]PYRIDINE-7-AMINE INHIBITORS OF ALK5
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Page/Page column 16-17, (2011/12/04)
The present invention provides ALK5 inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, methods of making the compounds and intermediates thereof; and methods of using the compounds.
ALPHA-HYDROXY AMIDES AS BRADYKININ ANTAGONISTS OR INVERSE AGONISTS
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Page/Page column 24, (2008/06/13)
α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd.(4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or(b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra.and (7)(CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3-to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl;
