63725-52-0Relevant academic research and scientific papers
AMINE-SUBSTITUTED ARYL OR HETEROARYL COMPOUNDS AS EHMT1 AND EHMT2 INHIBITORS
-
Paragraph 0550-0553, (2017/11/10)
The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
INDAZOLE AND AZAINDAZOLE COMPOUNDS AS IRAK-4 INHIBITORS
-
, (2017/02/09)
The present invention provides indazole and aza indazole compounds of formula (I) or (II) and pharmaceutically acceptable salts thereof, and their use to inhibit IRAK-4 and/or for the treatment of diseases or disorders induced by IRAK-4.
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin- 3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): A highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator
Zhang, Lei,Balan, Gayatri,Barreiro, Gabriela,Boscoe, Brian P.,Chenard, Lois K.,Cianfrogna, Julie,Claffey, Michelle M.,Chen, Laigao,Coffman, Karen J.,Drozda, Susan E.,Dunetz, Joshua R.,Fonseca, Kari R.,Galatsis, Paul,Grimwood, Sarah,Lazzaro, John T.,Mancuso, Jessica Y.,Miller, Emily L.,Reese, Matthew R.,Rogers, Bruce N.,Sakurada, Isao,Skaddan, Marc,Smith, Deborah L.,Stepan, Antonia F.,Trapa, Patrick,Tuttle, Jamison B.,Verhoest, Patrick R.,Walker, Daniel P.,Wright, Ann S.,Zaleska, Margaret M.,Zasadny, Kenneth,Shaffer, Christopher L.
, p. 861 - 877 (2014/03/21)
A novel series of pyrazolopyrazines is herein disclosed as mGluR5 negative allosteric modulators (NAMs). Starting from a high-throughput screen (HTS) hit (1), a systematic structure-activity relationship (SAR) study was conducted with a specific focus on balancing pharmacological potency with physicochemical and pharmacokinetic (PK) properties. This effort led to the discovery of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo[3,4-b] pyrazine (PF470, 14) as a highly potent, selective, and orally bioavailable mGluR5 NAM. Compound 14 demonstrated robust efficacy in a 1-methyl-4-phenyl-1,2, 3,6-tetrahydropyridine (MPTP)-rendered Parkinsonian nonhuman primate model of l-DOPA-induced dyskinesia (PD-LID). However, the progression of 14 to the clinic was terminated because of a potentially mechanism-mediated finding consistent with a delayed-type immune-mediated type IV hypersensitivity in a 90-day NHP regulatory toxicology study.
PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED THIAZOLE AND THIADIAZOLE DERIVATIVES
-
Page/Page column 53, (2013/11/05)
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.
