- SMALL MOLECULE ACTIVATORS OF TIE-2
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Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for vascular disorders that can include, for example, retinopathies, ocular edema, and ocular neovascularization.
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Paragraph 00297
(2021/05/07)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 86
(2012/02/15)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds
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Page/Page column 237; 239
(2012/04/10)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 177
(2011/06/16)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
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Page/Page column 88, 90
(2011/06/16)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 83; 85
(2011/07/07)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 145; 148
(2010/11/04)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 136
(2010/12/26)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 92; 94
(2010/12/26)
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- Hepatitis C Virus Inhibitors
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 52
(2010/10/19)
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- HEPATITIS C VIRUS INHIBITORS
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This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 210; 212
(2010/11/03)
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- Possible origin of electronic effects in Rh(I)-catalyzed enantioselective hydrogenation
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(Chemical Equation Presented) Reducing the electron density of ligands switches the regioselectivity of Rh(I)-catalyzed hydrometalation. A reversal of the sense of chiral induction was also observed when chiral ligands are electronically tuned in the same
- Wu, Hai-Chen,Hamid, Shafida Abd,Yu, Jin-Quan,Spencer, Jonathan B.
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supporting information; experimental part
p. 9604 - 9605
(2011/03/19)
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- Hepatitis C Virus Inhibitors
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 42-43
(2009/09/28)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to (4-4' -diimidazolyl) biphenyls compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 92
(2009/10/09)
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- Hepatitis C Virus Inhibitors
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 56-57
(2008/06/13)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein A and B are each phenyl; D and E are each five-membered aromatic rings containing one, two, or three i hcteroatoms independently selected from nitrogen, oxygen, and sulfur; provided that ', at least one of D and E is other than imidazole; compositions and methods for the treatment of Hepatitis C virus (HCV) inf ection. Also disclosed are pharmaceutical compositions containing such compounds and methods f or using these compounds in the treatment of HCV inf ection.
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Page/Page column 96; 98
(2009/01/20)
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- Amino acids as a chiral pool: Synthesis of (S)- and (R)-2-N-carbomethoxy-5- aminoindane from (S)- and (R)-phenylalanines
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Enantioselective syntheses of (R)-and (S)-2-N-carbomethoxy-5-aminoindanes from (R)- and (S)-phenylalanines, respectively, are described. A Friedel-Crafts reaction employing N-carbomethoxy phenylalanine leads to chiral 2-N-carbomethoxy-1-indanone, which is
- Waykole, Liladhar M.,McKenna, Joseph J.,Bach, Andrew,Prashad, Mahavir,Repic, Oljan,Blacklock, Thomas J.
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p. 1445 - 1454
(2008/02/02)
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- Lysine sulfonamides as novel HIV-protease inhibitors: Nε-Acyl aromatic α-amino acids
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A series of lysine sulfonamide analogues bearing Nε-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.
- Stranix, Brent R.,Lavallee, Jean-Francois,Sevigny, Guy,Yelle, Jocelyn,Perron, Valerie,LeBerre, Nicholas,Herbart, Dominik,Wu, Jinzi J.
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p. 3459 - 3462
(2007/10/03)
-
- Probing the mechanisms of enantioselective hydrogenation of simple olefins with chiral rhodium catalysts in the presence of anions
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The strong influence of various anions upon the hydrogenation of 2-phenyl-1-butene, catalyzed by chiral rhodium catalysts was investigated. Both sulfonates and halides exert large increases in the enantioselectivity when [Rh{(-)-bdpp}(NBD)]ClO4 (bdpp = 2,4-bis(diphenylphosphino)pentane, NBD=2,5-norbornadiene) is used as the catalyst precursor at high pressures (70 atm) of dihydrogen in nonpolar solvents. A dihydride mechanism similar to that for Wilkinson's catalyst [RhCl(PPh3)3] was shown to be operating at both high- and low-pressure conditions through a combination of catalytic studies, 31P, 1H and parahydrogen-induced polarization (PHIP) NMR experiments. With sulfonate and in neat methanol, however, a mechanistic switch takes place from a dihydride route (dihydrogen addition before olefin binding) at high pressure to an unsaturate route (olefin binding before dihydrogen addition) at low pressures (30 atm). Olefin isomerization is inhibited by halide addition, but occurs with sulfonate and in neat methanol through what is most likely a π-allyl mechanism. A detailed understanding of the effects of addition of these anions is crucial for development of new classes of catalysts capable of efficient enantioselective reduction of prochiral olefins lacking a secondary polar binding group.
- Buriak, Julian M.,Klein, Jason C.,Herrington, Deborah G.,Osborn, John A.
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p. 139 - 150
(2007/10/03)
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- A re-examination of two linear pentapeptides claimed to be serine protease mimics
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The synthesis, characterization, and kinetic study of two linear pentapeptides L-threonyl-L-alanyl-L-seryl-L-histidyl-L-aspartic acid (TASHD) and L-seryl-γ-aminobutyryl-L-histidyl-γ-aminobutyryl-L-aspartic acid (Ser-Gaba-His-Gaba-Asp) that were previously
- Vandersteen, Anthony M.,Janda, Kim D.
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p. 8787 - 8790
(2007/10/03)
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- Friedel-Crafts α-Aminoacylation of Alkylbenzene with a Chiral N-Carboxy-α-amino Acid Anhydride without Loss of Chirality
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A Friedel-Crafts-type α-aminoacylation of alkylbenzene with N-carboxy anhydrides of five L-α-amino acids was developed.Five new α-aminoalkyl p-methylphenyl ketones and other α-aminoalkyl aryl ketones were obtained and isolated as free bases or hydrochloride salts.The chiralities of the original L-α-amino acids were retained during this acylation.
- Itoh, Osamu,Honnami, Toshiya,Amano, Akira,Murata, Kouichi,Koichi, Youta,Sugita, Toshio
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p. 7334 - 7338
(2007/10/02)
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- Mechanism of Enantioselective Ester Cleavage by Histidine-Containing Dipeptides at a Micellar Interface
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Chiral p-nitrophenyl esters derived from the amino acid phenylalanine are cleaved by histidine-containing dipeptides at a micellar interface.High enantioselectivities (up to kL/kD = 30.4 at 0 deg C) are observed.Both the substrates and the catalysts contain an alternating sequence of hydrophobic and hydrophilic groups.Due to the need for hydration of the hydrophilic groups, the hydrophobic groups cannot dissolve completely into the micellar hydrocarbon phase.The kinetic data suggest that the micellar interface is capable of discriminating between transition states that have different hydrophilic and hydrophobic properties.One of the diastereomeric transition states is characterized by a hydrogen bond between the amide CO group of the ester and an NH group of the histidine-containing dipeptide.Upon formation of this hydrogen bond these polar CO and NH groups lose their hydrophilicity which allows the transfer of the adjacent apolar groups to the micellar hydrocarbon phase.The other diastereomeric transition state cannot form this hydrogen bond and the hydrophobic groups remain hydrated.Consequently, the latter transition state is of higher energy.The kinetic data reveal that it is important to prevent steric hinderance between the reactants in order to allow the unhindered formation of the hydrogen bond.
- Cleij, Marco C.,Drenth, Wiendelt,Nolte, Roeland J. M.
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p. 3883 - 3891
(2007/10/02)
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- Stereoselective Micellar Catalysis. Part V. Deacylation Behaviour in the Cleavage of Enantiomeric Esters by Optically Active Catalysts containing the Imidazolyl Group
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The rate constants of both acylation and deacylation in the cleavage of the enantiomers of amino acid p-nitrophenyl esters catalysed by optically active catalysts containing the imidazolyl group have been determined in the presence of surfactant micelles
- Ihara, Yasuji,Okamoto, Mari,Kawamura, Yoeko,Nakanishi, Eiji,Nango, Mamoru,Koga, Joichi
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p. 607 - 612
(2007/10/02)
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- N,N-DIALKOXYCARBONYLAMINO ACID FORMATION FROM A MIXED ANHYDRIDE THROUGH INTRAMOLECULAR URETHANE ACYLATION
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Methoxycarbonylation at the urethane nitrogen of N-benzyloxycarbonyl- and N-methoxycarbonylvaline has been identified as a side reaction accompanying the aminolysis of the mixed anhydride formed from the acid and methyl chloroformate when the anhydride is coupled in aqueuos dimethylformamide and the nucleophile is an amino acid anion.The side reaction occurs to a lesser but still significant extent when the activated residue is leucyl.
- Chen, Francis M. F.,Benoiton, N. Leo
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p. 1228 - 1229
(2007/10/02)
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- STEREOSELECTIVE HYDROLYSIS OF AMINO ACID ESTERS BY MODIFIED POLY(ETHYLENIMINE)S WITH COVALENTLY-LINKED DIPEPTIDE CONTAINING A HISTIDYL RESIDUE
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Stereoselective hydrolyses of chiral substrates were examined in poly(ethylenimine) derivatives with optically active groups.A high stereoselective effect, kL/kD = 3.6, is observed.The effect of the substrate structure influenced both the rate constant and the stereoselective ratio in the hydrolyses by poly(ethylenimine) derivatives.
- Kimura, Yoshiharu,Nango, Mamoru,Ihara, Yasuji,Kuroki, Nobuhiko
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p. 429 - 432
(2007/10/02)
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- STEREOSELECTIVE HYDROLYSIS OF AMINO ACID ESTERS IN MODIFIED LINEAR POLY(ETHYLENIMINE) DOMAINS
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A large rate enhancement and a stereoselective preference are exhibited in the hydrolysis catalysed by N-decanoyl-L-histidine (2a) and a dipeptide containing L-histidyl residue (2b) in the domain of linear poly(ethylimine) derivatives.
- Kimura, Yoshiharu,Kanda, Shinichi,Nango, Mamoru,Ihara, Yasuji,Koga, Joichi,et al.
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p. 433 - 436
(2007/10/02)
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- 1,4-Oxazines via Intramolecular Ring Closure of β-Hydroxydiazoacetamides: Phenylalanine to Tetrahydroindeno-1,4-oxazin-3(2H)-ones
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The synthesis of the tetrahydroindeno-1,4-oxazin-3(2H)-one system from phenylalanine is described.Conversion of the intermediate vicinal amino alcohol to the 1,4-oxazine was accomplished via BF3*Et2O-catalyzed ring closure of a β-hydroxydiazoacetam
- McClure, D. E.,Lumma, P. K.,Arison, B. H.,Jones, J. H.,Baldwin, J. J.
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p. 2675 - 2679
(2007/10/02)
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- STEREOSELECTIVE MICELLAR CATALYSIS IN THE HYDROLYSIS OF ENANTIOMERIC ESTERS BY DIPEPTIDE DERIVATIVES CONTAINING HISTIDINE RESIDUE
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The catalytic hydrolysis of enantiomeric substrates is examined using optically active dipeptide derivatives containing histidine residue in the presence of CTABr micelles.A very high stereoselectivity, kc(L)/kc(D), of 12.2 is observed in the reaction with the enantiomers of p-nitrophenyl N-methoxycarbonylphenylalanate (MocPheONp) and N-(benzyloxycarbonyl-L-leucyl)-L-histidine (ZLeuHis).
- Ihara, Yasuji,Kunikiyo, Noriko,Kunimasa, Tomoko,Nango, Mamoru,Kuroki, Nobuhiko
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p. 667 - 670
(2007/10/02)
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- Co-operative Effects in the Catalytic Action of N-Decanoyl-L-histidine in Micelles
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A comparison of catalytic effects in the hydrolysis of the enantiomeric esters (2) by N-decanoyl-L-histidine (1a) and its methyl ester (1b) in the presence of cetyltrimethylammonium bromide micelle strongly suggests that the carboxylate ion of (1a) enhanc
- Ihara, Yasuji,Hosako, Reiko,Nango, Mamoru,Kuroki, Nobuhiko
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p. 393 - 394
(2007/10/02)
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- VALIDITY OF METHOXYCARBONYL AS AN N-PROTECTING GROUP IN PEPTIDE SYNTHESIS: NEW SYNTHESIS OF MSH-RELEASE INHIBITING FACTOR
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N-Methoxycarbonyl (MOC)-amino acids regenerate the parent amino acids by treatment with dimethyl sulphide and methanesulphonic acid.Synthesis of MSH-Release Inhibiting Factor was accomplished using MOC-amino acids and applying the above mentioned deblocking method.
- Irie, Hiroshi,Nakanishi, Hiromi,Fujii, Nobutaka,Mizuno, Yukio,Fushimi, Tamaki,et al.
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p. 705 - 708
(2007/10/02)
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- Stereoselective micellar catalysis. Reactions of amino-acid ester derivatives with N-acyl-L-histidine in micelles
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Mixed micelles of the N-acyl-L-histidines (I) and cetyltrimethylammonium bromide (CTABr) are effective stereoselective catalysts for cleavage of the enantiomeric amino-acid ester derivatives (II). The rate enhancements and stereoselective effects depend on the hydrophobicity of (I) in micelles, and an increase in the chain length of the acyl part of (I) increases both the reaction rates and the enantiomer rate ratio. Mixed micelles with anionic and nonionic surfactants are relatively less effective stereoselective catalysts. Kinetic analysis indicates that the stereoselectivity in mixed micelles is mainly determined by catalytic acyl transfer to the optically active imidazole group of (I).
- Ihara, Yasuji
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p. 1483 - 1487
(2007/10/02)
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