- HPTP-BETA INHIBITORS
-
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility ar
- -
-
Paragraph 0213-0214
(2015/10/05)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 86
(2012/02/15)
-
- HEPATITIS C VIRUS INHIBITORS
-
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
- -
-
Page/Page column 237; 239
(2012/04/10)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 177
(2011/06/16)
-
- HEPATITIS C VIRUS INHIBITORS
-
The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
- -
-
Page/Page column 88, 90
(2011/06/16)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 83; 85
(2011/07/07)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 145; 148
(2010/11/04)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 136
(2010/12/26)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 92; 94
(2010/12/26)
-
- Hepatitis C Virus Inhibitors
-
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.
- -
-
Page/Page column 52
(2010/10/19)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 210; 212
(2010/11/03)
-
- Hepatitis C Virus Inhibitors
-
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.
- -
-
Page/Page column 42-43
(2009/09/28)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 92
(2009/10/09)
-
- Hepatitis C Virus Inhibitors
-
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.
- -
-
Page/Page column 56-57
(2008/06/13)
-
- HEPATITIS C VIRUS INHIBITORS
-
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.
- -
-
Page/Page column 96; 98
(2009/01/20)
-
- Amino acids as a chiral pool: Synthesis of (S)- and (R)-2-N-carbomethoxy-5- aminoindane from (S)- and (R)-phenylalanines
-
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.
-
p. 1445 - 1454
(2008/02/02)
-
- HETEROCYCLIC AMINES HAVING CENTRAL NERVOUS SYSTEM ACTIVITY
-
Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are inde
- -
-
-
- Sustained release tablet formulation to treat Parkinson's disease
-
The sustained release tablet of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) which is disclosed permits twice daily administration of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (
- -
-
-
- Probing the mechanisms of enantioselective hydrogenation of simple olefins with chiral rhodium catalysts in the presence of anions
-
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.
-
p. 139 - 150
(2007/10/03)
-
- Synthesis of the Selective D2 Receptor Agonist PNU-95666E from D-Phenylalanine Using a Sequential Oxidative Cyclization Strategy
-
Compound 1 (PNU-95666E) is a selective and high-affinity agonist at the dopamine D2 receptor subtype and is of interest as a potential agent for the treatment of Parkinson's disease. Requiring a synthetic route amenable to scale-up, a synthesis
- Romero, Arthur G.,Darlington, William H.,McMillan, Moses W.
-
p. 6582 - 6587
(2007/10/03)
-
- Heterocyclic amines having central nervous system activity
-
Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: STR1 and pharmaceutically acceptable salts thereof wherein R1 and R2 are
- -
-
-
- A re-examination of two linear pentapeptides claimed to be serine protease mimics
-
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.
-
p. 8787 - 8790
(2007/10/03)
-
- Stereoselective Micellar Catalysis. Part V. Deacylation Behaviour in the Cleavage of Enantiomeric Esters by Optically Active Catalysts containing the Imidazolyl Group
-
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
-
p. 607 - 612
(2007/10/02)
-
- STEREOSELECTIVE HYDROLYSIS OF AMINO ACID ESTERS BY MODIFIED POLY(ETHYLENIMINE)S WITH COVALENTLY-LINKED DIPEPTIDE CONTAINING A HISTIDYL RESIDUE
-
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
-
p. 429 - 432
(2007/10/02)
-
- STEREOSELECTIVE HYDROLYSIS OF AMINO ACID ESTERS IN MODIFIED LINEAR POLY(ETHYLENIMINE) DOMAINS
-
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.
-
p. 433 - 436
(2007/10/02)
-
- 1,4-Oxazines via Intramolecular Ring Closure of β-Hydroxydiazoacetamides: Phenylalanine to Tetrahydroindeno-1,4-oxazin-3(2H)-ones
-
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.
-
p. 2675 - 2679
(2007/10/02)
-
- STEREOSELECTIVE MICELLAR CATALYSIS IN THE HYDROLYSIS OF ENANTIOMERIC ESTERS BY DIPEPTIDE DERIVATIVES CONTAINING HISTIDINE RESIDUE
-
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
-
p. 667 - 670
(2007/10/02)
-
- Co-operative Effects in the Catalytic Action of N-Decanoyl-L-histidine in Micelles
-
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
-
p. 393 - 394
(2007/10/02)
-
- Stereoselective micellar catalysis. Reactions of amino-acid ester derivatives with N-acyl-L-histidine in micelles
-
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
-
p. 1483 - 1487
(2007/10/02)
-