171504-98-6Relevant academic research and scientific papers
BRM TARGETING COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0462, (2021/12/31)
The present invention relates to bifunctional compounds comprising a binding fraction to a target protein and a binding fraction to ubiquitin ligase E3, and associated methods of use.
Imidazotetrazines as Weighable Diazomethane Surrogates for Esterifications and Cyclopropanations
Svec, Riley L.,Hergenrother, Paul J.
supporting information, p. 1857 - 1862 (2019/12/27)
Diazomethane is one of the most versatile reagents in organic synthesis, but its utility is limited by its hazardous nature. Although alternative methods exist to perform the unique chemistry of diazomethane, these suffer from diminished reactivity and/or correspondingly harsher conditions. Herein, we describe the repurposing of imidazotetrazines (such as temozolomide, TMZ, the standard of care for glioblastoma) for use as synthetic precursors of alkyl diazonium reagents. TMZ was employed to conduct esterifications and metal-catalyzed cyclopropanations, and results show that methyl ester formation from a wide variety of substrates is especially efficient and operationally simple. TMZ is a commercially available solid that is non-explosive and non-toxic, and should find broad utility as a replacement for diazomethane.
Piperazine compound and application thereof in preparation of chemokine receptor CCR2 antagonist
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, (2020/07/28)
The invention relates to a piperazine compound as shown in a formula (I) and an application of the piperazine compound in preparation of a chemokine receptor CCR2 antagonist or a medicine for treatingCCR2-mediated diseases.
DIHYDROPYRIMIDINE COMPOUNDS AND USES THEREOF IN MEDICINE
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Paragraph 00384, (2019/05/10)
Provided herein are a dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B. Specifically, provided herein is a compound having Formula (I) or (Ia), or a stereisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B.
Dihydropyridine compound and application thereof to drugs
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Paragraph 0982-0985, (2019/05/08)
The invention relates to a dihydropyridine compound and application of the dihydropyridine compound serving as a drug, in particular to application of the dihydropyridine compound serving as a drug for treating and preventing hepatitis B. Specifically, the invention relates to the compound shown as the general formula (I) or (Ia) (please see the specifications for the general formula (I) or (Ia))or stereoisomers, tautomer, a nitrogen oxide, solvate, metabolites and medically acceptable salt of the compound or a prodrug of the compound, wherein all variables are defined in the specification. The invention further relates to application of the compound shown as the general formula (I) or (Ia) or enantiomers, non-enantiomers, the tautomer, hydrates, the solvate or the medically acceptable salt of the compound serving as drugs, in particular to application of the compound or the enantiomers, the non-enantiomers, the tautomer, the hydrates, the solvate or the medically acceptable salt of the compound serving as the drugs for treating and preventing hepatitis B.
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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, (2018/03/01)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
FUSED RING HETEROARYL COMPOUNDS AND THEIR USE AS TRK INHIBITORS
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Paragraph 0577; 0578, (2016/07/05)
The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases. In some compounds of Formula I, Q is —CH═CR3C(O)NR4R5, —C≡CC(O)NR4R5, or
Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection
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Paragraph 0557; 0558; 0559, (2015/11/02)
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, X, Y, W and n are as described herein, compositions including the compounds and methods of using the compounds.
IMIDAZO [4, 5 - B] PYRIDINE DERIVATIVES AS ALK AND JAK MODULATORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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Page/Page column 207, (2013/08/15)
This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS AND THEIR USES AS IDH1 MUTANTS INHIBITORS FOR TREATING CANCERS
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, (2013/02/28)
Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses as IDH1 mutants inhibitors for treating cancers are also provided
