911010-88-3Relevant academic research and scientific papers
Heterocyclic compound, pharmaceutical composition and application
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Paragraph 0085-0093, (2021/02/10)
The invention discloses a heterocyclic compound which is a heterocyclic compound shown as a formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a hydrate, a solvate, a metabolite or a prodrug thereof. The heterocyclic compound can be used for preparing medicines for treating and/or preventing cancers related to KRAS G12C mutation. The invention also discloses a pharmaceutical composition containing the heterocyclic compound, and application of the compound shown in the formula I, or pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, solvate, metabolite, prodrug or pharmaceutical composition thereof in preparation of drugs.
KRAS MUTANT PROTEIN INHIBITORS
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Paragraph 0201-0202, (2021/04/02)
The invention relates to a KRAS mutant protein inhibitor, a composition containing the inhibitor and the use thereof.
Fused cyanopyridine compound and preparation method and application thereof
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Paragraph 0138-0140, (2021/01/11)
The invention discloses a fused cyanopyridine compound shown as a general formula I-1 or I-2, or a pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a torsional isomer, a solvate, a polymorphic substance or a prodrug thereof, and a preparation method and a pharmaceutical application of the fused cyanopyridine compound, wherein the definition of each group is shown in the specification.
Saturated six-membered ring heterocyclic compound as well as preparation method and application thereof
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Paragraph 0145-0147, (2020/12/30)
The invention discloses a saturated six-membered ring heterocyclic compound as well as a preparation method and application thereof. The invention discloses a saturated six-membered ring heterocycliccompound shown as a general formula I, or pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a torsional isomer, a solvate, a polymorphic substance or prodrug thereof, as well as a preparation method and a pharmaceutical application of the saturated six-membered ring heterocyclic compound. The definition of each group is as described in the specification.
Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H
Kankanala, Jayakanth,Kirby, Karen A.,Huber, Andrew D.,Casey, Mary C.,Wilson, Daniel J.,Sarafianos, Stefan G.,Wang, Zhengqiang
supporting information, p. 149 - 161 (2017/10/16)
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) is the only HIV enzymatic function not targeted by current antiviral drugs. Although various chemotypes have been reported to inhibit HIV RNase H, few have s
TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 80; 81, (2015/12/30)
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists
Lanier, Marion C.,Feher, Miklos,Ashweek, Neil J.,Loweth, Colin J.,Rueter, Jaimie K.,Slee, Deborah H.,Williams, John P.,Zhu, Yun-Fei,Sullivan, Susan K.,Brown, Michael S.
, p. 5590 - 5603 (2008/03/15)
The present article describes a selection of a new class of small molecule antagonists for the h-GnRH receptor, their preparation, and evaluation in vitro. Three computational methods were combined into a consensus score, to rank order virtual templates. The top 5% of templates were further evaluated in silico and assessed for novelty and synthetic accessibility. The tetrahydropyrido[4,3-d]pyrimidine-2,4-dione core was selected for synthesis and evaluated in vitro. Using an array approach for analog design and synthesis, we were able to drive the binding below 10 nM for the h-GnRH receptor after two rounds of optimization.
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
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Page/Page column 34, (2008/06/13)
Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including huma
