- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Paragraph 0490-0491
(2019/05/15)
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- Synthesis of Amides by Nucleophilic Substitution of Hydrogen in 3-Nitropyridine
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3-Nitropyridine reacted with nitrogen-centered carboxylic acid amide anions in anhydrous DMSO in the presence of K3Fe(CN)6 via oxidative nucleophilic substitution of hydrogen to give previously unknown N-(5-nitropyridin-2-yl) carboxa
- Amangasieva,Borovlev,Demidov,Avakyan,Borovleva
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p. 867 - 872
(2018/07/31)
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- Pyridines IRAK4 inhibitors, preparation method and application thereof (by machine translation)
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The invention belongs to the field of medicine, in particular to a formula (I) of the structural features of pyridine of compound or its pharmaceutically acceptable salt, preparation method thereof, and their use as IRAK4 inhibitors. Experimental results show that, the compound of the invention IRAK4 has prominent inhibit function, can be used for the treatment of autoimmune disease, inflammatory disease, cancer, autoimmune disease and thromboembolism as heterogeneous. (by machine translation)
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Paragraph 0094; 0095; 0096
(2017/09/01)
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- Convenient N-acetylation of amines in N,N-dimethylacetamide with N,N-carbonyldiimidazole
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Dimethylacetamide (DMAc) acts as an efficient source of acetyl and dimethylamine gas in the presence of N,N-carbonyldiimidazole (CDI). Addition of amines to the reaction mixture delivers the corresponding amides in good to excellent yields. The acetylation of amines reported herein, which relies on the in situ generation of N-acetylimidazole on warming of DMAc with CDI at 120-125 °C, serves as a convenient alternative to other acetylation methods.
- Chikkulapalli, Anil,Aavula, Sanjeev Kumar,Mona Np, Rifahath,Karthikeyan, Karthikeyan,Kumar C.H., Vinodh,Sulur G., Manjunatha,Sumathi, Shanmugam
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supporting information
p. 3799 - 3803
(2015/06/08)
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- Esterification catalysis by pyridinium p -toluenesulfonate revisited - Modification with a lipid chain for improved activities and selectivities
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The lipid analogs of pyridinium p-toluenesulfonate (PPTS) were examined for catalysis of the condensation of an equimolar mixture of carboxylic acids and alcohols under mild conditions without removal of water. Although PPTS is a poor catalyst, the introduction of a lipid chain and nitro group significantly improved the activity of PPTS and led to selectivity at suppressing the elimination side reactions of alcohols. 2-Oleamido-5-nitro-pyridinium p-toluenesulfonate (6) is a lead catalyst that promoted various esterification reactions with yields up to 99%.
- Wang, Wei,Liu, Huimin,Xu, Shaoyi,Gao, Yong
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supporting information
p. 2906 - 2912
(2013/09/02)
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- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 64
(2010/11/04)
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- QUINOLINE DERIVATIVES FOR MODULATING DNA METHYLATION
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Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
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Page/Page column 139
(2008/06/13)
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- AMIDE COMPOUND
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There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, -CO-, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.
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Page/Page column 85
(2008/06/13)
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- Thiazolidinones, their production and use as pharmaceutical agents
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Thiazolidinones of general formula I in which Q, A, B, X, R1 and R2 have the meanings that are indicated in the description, as well as those of general formula IA in which Q, A, B, X, R1 and R2a have the meanings that are indicated in the description, their production and use as inhibitors of the polo-like kinase (PLK) for treating various diseases as well as intermediate products for the production of thiazolidinones are described.
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- SUBSTITUTED-3-CYANO-[1.7],[1.5], AND [1.8]-NAPHTHYRIDINE INHIBITORS OF TYROSINE KINASES
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This invention provides compounds of formula (I) having structure (a) wherein A'' is a diavalent moiety selected from the group (a, b, c) which are useful as inhibitors of protein tyrosine kinase.
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- HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS
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Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
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- Aminopyridine compounds
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An aminopyridine compound represented by the formula: STR1 wherein n represents 0 or 1; Z represents =S, =NCN or =CHNO2 ; R1 represents --NR3 R4, --NHNR3 R4, --NHCONHR3 or --NHSO2 R3 ; R2 represents H, or substituted or unsubstituted alkyl; R3 and R4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R3 and R4 may form a heterocyclic ring together with a nitrogen atom to which R3 and R4 are bound, through another heteroatom or without it; an optical isomer thereof or art acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.
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- Aminopyridine compounds
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An aminopyridine compound represented by the formula: STR1 wherein n represents 0 or 1; Z represents =S, =O, =NCN or =CHNO2 ; R1 represents --CN, --NR3 R4, --CONR3 R4, --NHNR3 R4, --NHCONHR3, --NHSO2 R3 or --SR3 ; R2 represents H, or substituted or unsubstituted alkyl; R3 and R4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R3 and R4 may form a heterocyclic ring together with a nitrogen atom to which R3 and R4 are bound, through another heteroatom or without it; or an acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.
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