- HETEROCYCLIC COMPOUNDS
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The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof has an BET family protein inhibitory action, and is useful as an agent for the prophylaxis or treatment of autoimmune diseases and/or inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis, idiopathic pulmonary fibrosis, psoriasis, atopic dermatitis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, systemic lupus erythematosus etc.), cancer and the like.
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Page/Page column 0288
(2016/12/26)
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- INHIBITORS OF FATTY ACID AMIDE HYDROLASE
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The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
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Paragraph 1040
(2016/01/15)
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- The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile - Part 1
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Nonstructural protein 5A (NS5A) represents a novel target for the treatment of hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol-Myers-Squibb, is a potent NS5A inhibitor currently under investigation in phase 3 clinical trials. While the performance of daclatasvir has been impressive, the emergence of resistance could prove problematic and as such, improved analogues are being sought. By varying the biphenyl-imidazole unit of daclatasvir, novel inhibitors of HCV NS5A were identified with an improved resistance profile against mutant strains of the virus while retaining the picomolar potency of daclatasvir. One compound in particular, methyl ((S)-1-((S)-2-(4-(4-(6-(2-((S)-1-((methoxycarbonyl)-L-valyl)pyrrolidin-2-yl) -1H-imidazol-5-yl)quinoxalin-2-yl)phenyl)-1H-imidazol-2-yl)pyrrolidin-1-yl) -3-methyl-1-oxobutan-2-yl)carbamate (17), exhibited very promising activity and showed good absorption and a long predicted human pharmacokinetic half-life. This compound represents a promising lead that warrants further evaluation. Resisting resistance: An investigation into the anti-hepatitis C virus (HCV) replicon activity of a series of biaryl-linked pyrrolidine NS5A inhibitors explored a diverse range of core structure modifications as key determinants of antiviral activity and susceptibility to common resistance mutations. Further evaluation of several core structure designs identified a compound with excellent pharmacokinetics, suitable for once daily dosing.
- Tran, Thien Duc,Wakenhut, Florian,Pickford, Chris,Shaw, Stephen,Westby, Mike,Smith-Burchnell, Caroline,Watson, Lesa,Paradowski, Michael,Milbank, Jared,Brimage, Rebecca A.,Halstead, Rebecca,Glen, Rebecca,Wilson, Craig P.,Adam, Fiona,Hay, Duncan,Chiva, Jean-Yves,Nichols, Carly,Blakemore, David C.,Gardner, Iain,Dayal, Satish,Pike, Andrew,Webster, Rob,Pryde, David C.
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p. 1378 - 1386
(2014/07/21)
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- ANTIVIRAL COMPOUNDS
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The present invention provides 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 62
(2012/09/22)
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- HEPATITIS C VIRUS INHIBITORS
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The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
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Page/Page column 106
(2011/02/24)
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- SUBSTITUTED BENZOTRIAZINES AND QUINOXALINES AS INHIBITORS OF P7OS6 KINASE
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The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O ); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.
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Page/Page column 46; 47
(2010/12/26)
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- ANTI-INFECTIVE PYRIMIDINES AND USES THEREOF
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This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
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Page/Page column 185
(2009/04/25)
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- TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE
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Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
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Page/Page column 84
(2010/11/28)
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- A FACILE SYNTHESIS OF NOVEL TRICYCLIC COMPOUNDS, TETRAZOLOQUINOXALINES AND 1,2,4-TRIAZOLOQUINOXALINES
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Novel 5-methyltetrazoloquinoxalin-4-ones (5) and 5-methyl-1,2,4-triazoloquinoxalin-4-ones (7) could be synthesized from 1-methyl-3-chloroquinoxalin-2-ones (3) and 1-methyl-3-hydrazinoquinoxalin-2-ones (6), respectively.Further extensive study was carried out to synthesize 4- or 7- substituted and 4,7-disubstituted tetrazoloquinoxalines (10) and 1,2,4-triazoloquinoxalines (12).
- Makino, Kenzi,Sakata, Gozyo,Morimoto, Katsushi
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p. 2025 - 2034
(2007/10/02)
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