- FUSED-RING COMPOUNDS, PHARMACEUTICAL COMPOSITION AND USES THEREOF
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This disclosure is related to a fused-ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the fused ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, preparation methods thereof, and use thereof in modulating activity of indoleamine 2, 3-dioxygenase (IDO) and/or tryptophan 2, 3-dioxygenase (TDO). This disclosure further provides methods of treating IDO and/or TDO-associated diseases, including cancer, viral infection and autoimmune diseases.
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Paragraph 324; 325; 326
(2016/09/15)
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- INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
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This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11
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Page/Page column 33
(2011/02/26)
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- CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
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Page/Page column 41
(2010/12/29)
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- CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 Vl, Vla, VIb, VII, Vila, VIIb, VIII, Vllla, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
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Page/Page column 46-47
(2009/12/05)
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- Synthesis and antiviral activity of metabolites of rimantadine
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The hydroxy metabolites of rimantadine (3-5) were synthesized and compared to amantadine (1) and rimantadine (2) for their ability to inhibit the replication of influenza viruses in vitro. All three metabolites were inhibitory to wild-type influenza A viruses (H3N2 and H1N1). In particular, 2-hydroxyrimantadine (3) showed similar activity to amantadine, but the 3- and 4-hydroxy metabolites (4 and 5, respectively), both of which are found in rimantadine-treated patients, showed only modest inhibitory activity. A rimantadine-resistant isolate of influenza A virus exhibited cross-resistance to amantadine and to each of the metabolites 3-5. None of the compounds were effective against influenza B virus.
- Manchand,Cerruti,Martin,Hill,Merrett,Keech,Belshe,Connell,Sim
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p. 1992 - 1995
(2007/10/02)
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- Oxy-Functionalization of Adamante-1-acetic Acid and Adamantane-1-carboxylic Acid by the Ferrous Iron-Molecular Oxygen System in Aqueous Solution
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Oxygenation reactions of adamantanes with ferrous iron-molecular oxygen in phosphate buffer were investigated and the structures of the products were elucidated.In the reaction of adamantane-1-acetic acid (1a), five oxygenated products, the C(2)-oxo, C(4)-oxo, C(2),C(6)-dioxo, C(4)-ol, and C(3)-ol derivatives, were obtained.Similar oxygenation also occurred in the reaction of adamantane-1-carboxylic acid (2a) to give three products, the C(4)-oxo, C(4)-ol, and C(3)-ol derivatives.The oxy-functionalization of 1a and 2a in 0.5M phosphate buffer (pH 6.8) was found to occur almost quantitatively on addition of an appropriate amount of ferrous iron.
- Miura, Toshiaki,Shibata, Kunihiko,Sawaya, Takuji,Kimura, Michiya
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- SYNTHESIS AND ISOLATION OF THE INDIVIDUAL STEREOISOMERS OF SOME 4-SUBSTITUTED 1-ADAMANTANECARBOXYLIC ACIDS
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Methyl 4e- and 4a-hydroxy-1-adamantanecarboxylates were obtained from methyl 4-keto-1-adamantanecarboxylate and isolated.The synthesis of 4e- an 4a-hydroxy-, 4e- and 4a-methoxy-, 4e- and 4a-chloro-, and 4e- and 4a-bromo-1-adamantanecarboxylic acids and their methyl esters were synthesized from the products.
- Lantvoev, V. I.
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p. 1409 - 1414
(2007/10/02)
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