- Compound used for inhibiting hepatitis C virus, and pharmaceutical applications thereof
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The invention relates to a compound which is represented by formula I, is used for inhibiting hepatitis C virus, and possesses excellent bioavailability, and a nontoxic pharmaceutically acceptable salt thereof. The compound possesses extremely high inhibition effect on HCV of all genotypes. In the formula I, R is used for representing hydrogen atom, glycyl, L-alanyl, L-leucyl, L-valyl, or L-isoleucyl.
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Paragraph 0011; 0012
(2018/04/01)
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- Deuterated antiviral active compounds for hepatitis C viruses
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The invention relates to antiviral compounds for hepatitis C viruses (HCVs) and nontoxic pharmacologically-acceptable salts thereof, wherein the compounds are represented by a formula I shown in the description and have good bioavailability, and the compounds have potent inhibiting effects on the all-genotypic HCVs. In the structural formula I, R1, R2, R3 and R4 are independently selected from methyl (-CH3) or deuterated methyl (-CD3); X1, X2, X3, X4 and X5 are separately hydrogen (H) or deuterium (D); and one of the R1, the R2, the R3 and the R4 must be deuterated methyl (-CD3) or one of theX1, the X2, the X3, the X4, and the X5 must be deuterium (D).
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Paragraph 0010-0012
(2018/04/01)
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- BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided herein is a bridged bring compound of formula (I) or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore provided herein are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions thereof in the treatment of HCV infection or hepatitis C.
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Paragraph 0218; 0219; 0220; 0221
(2017/04/11)
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- BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided herein is a bridged bring compound of formula (I) or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore provided herein are pharmaceutical compositions containing the compounds and the method of using the compounds or harmaceutical com ositions thereof in the treatment of HCV infection or he atitis C.
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Paragraph 00161
(2015/08/06)
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- PROCESSES FOR PREPARING ANTIVIRAL COMPOUNDS
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The present disclosure provides processes for the preparation of a compound of formula: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates.
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Paragraph 0385
(2015/12/30)
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- ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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Paragraph 0311; 0312
(2015/12/31)
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- ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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Paragraph 0248
(2014/07/08)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 102
(2013/07/31)
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- HEPATITIS C VIRUS INHIBITORS
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The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
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Paragraph 0423
(2013/05/21)
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- CONDENSED IMIDAZOLYLIMIDAZOLES AS ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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Page/Page column 131; 132
(2013/06/05)
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- ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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Paragraph 0344
(2013/12/03)
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- Discovery, structure - Activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
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A series of (5-substituted pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of diabetes and obesity. X-ray crystallography data show that these inhibitors bind to the catalytic site of DPPIV with the cyano group forming a covalent bond with the serine residue of DPPIV. The C5-substituents make various interactions with the enzyme and affect potency, chemical stability, selectivity, and PK properties of the inhibitors. Optimized analogues are extremely potent with subnanomolar Ki's, are chemically stable, show very little potency decrease in the presence of plasma, and exhibit more than 1,000-fold selectivity against related peptidases. The best compounds also possess good PK and are efficacious in lowering blood glucose in an oral glucose tolerance test in ZDF rats.
- Pei, Zhonghua,Li, Xiaofeng,Longenecker, Kenton,Von Geldern, Thomas W.,Wiedeman, Paul E.,Lubben, Thomas H.,Zinker, Bradley A.,Stewart, Kent,Ballaron, Stephen J.,Stashko, Michael A.,Mika, Amanda K.,Beno, David W. A.,Long, Michelle,Wells, Heidi,Kempf-Grote, Anita J.,Madar, David J.,McDermott, Todd S.,Bhagavatula, Lakshmi,Fickes, Michael G.,Pireh, Daisy,Solomon, Larry R.,Lake, Marc R.,Edalji, Rohinton,Fry, Elizabeth H.,Sham, Hing L.,Trevillyan, James M.
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p. 3520 - 3535
(2007/10/03)
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