1401464-07-0Relevant articles and documents
ALKYNYL QUINAZOLINE COMPOUNDS
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Paragraph 1159, (2021/02/19)
The present disclosure relates to compounds of Formula (I'): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the prevention or treatment of abnormal cell growth in mammals, especially humans.
QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITOR, COMPOSITIONS, METHODS OF MAKING THEM AND THEIR USE
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, (2020/05/13)
The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).
Synthesis and evaluation of 6-pyrazoylamido-3N-substituted azabicyclo[3,1,0]hexane derivatives as T-type calcium channel inhibitors for treatment of neuropathic pain
Kim, Jung Hyun,Nam, Ghilsoo
supporting information, p. 5028 - 5035 (2016/10/24)
A new series of aryls, including benzo[d]imidazole/isoxazole/pyrazole, conjugated to 3N-substituted-azabicyclo[3.1.0]hexane derivatives were designed and synthesized as inhibitors of T-type calcium channels. Among the synthesized compounds, 3N-R-substituted azabicyclo[3.1.0]hexane carboxamide derivatives containing 5-isobutyl-1-phenyl-pyrazole ring exhibited potent and selective T-channel inhibition and good metabolic stability without CYP450 inhibition. Compounds 10d and 10e contained hydrophobic substituents at the 3N-position and exhibited potent in vitro efficacy, as well as neuropathic pain alleviation in rats.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 35, (2015/05/19)
The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis
NOVEL 6-PYRAZOLYLAMIDO-3-SUBSTITUTED AZABICYCLO[3.1.0]HEXANE COMPOUNDS AS CALCIUM CHANNEL INHIBITORS
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Paragraph 0087; 0088; 0089, (2014/12/09)
The present invention relates to a 6-pyrazolylamido-3-substituted azabicyclo[3.1.0]hexane derivatives useful as calcium channel blockers, pharmaceutically acceptable salts thereof and medical use of the calcium channel inhibiting effect of the compounds for treatment of diseases.
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead
Jones, Carrie K.,Sheffler, Douglas J.,Williams, Richard,Jadhav, Sataya B.,Felts, Andrew S.,Morrison, Ryan D.,Niswender, Colleen M.,Daniels, J. Scott,Conn, P. Jeffrey,Lindsley, Craig W.
, p. 1067 - 1070 (2014/03/21)
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach that provided a robust intellectual property position, in lieu of a traditional, expensive HTS campaign. Members within this new [3.1.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, CNS penetration and efficacy in a preclinical model of schizophrenia (prepulse inhibition).
