- COMPOUNDS AND METHODS FOR INHIBITING CYP26 ENZYMES
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Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.
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Page/Page column 21
(2018/07/05)
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- AMIDE-LINKED EP4 AGONIST-BISPHOSPHONATE COMPOUNDS AND USES THEREOF
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The present invention relates to EP4 agonist-bisphosphonate conjugates or related compounds and uses thereof. Said conjugates or related compounds may be used to provide delivery of an EP4 agonist or related compound to a desired site of action, such as a bone. Bisphosphonate moieties, linked to the EP4 agonists via amide linkers, have been implicated in the inhibition of bone resorption and bone targeting.
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Paragraph 00146-00147
(2017/01/31)
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- Metal-Free Direct Amidation of Naphthoquinones Using Hydroxamic Acids as an Amide Source: Application in the Synthesis of an HDAC6 Inhibitor
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A novel synthetic approach to amidoquinones by the reaction of naphthoquinones with hydroxamic acids under basic conditions was developed. The reaction is mild and operationally simple, and it affords high yields of amidoquinones. With this new method, a novel, very strong HDAC6 inhibitor, which showed high toxicity to AML cells, was successfully synthesized.
- Zhang, Cheng,Chou, C. James
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supporting information
p. 5512 - 5515
(2016/11/17)
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- TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 40
(2014/09/03)
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- HYDROXAMIC ACIDS AS HDAC6 INHIBITORS
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A hydroxamic acid of formula (I) or a pharmaceutically acceptable salt thereof for use in a method for treating or preventing an immunological, inflammatory, autoimmune or allergic disorder or disease, or a transplant rejection, or a graft-versus host dis
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Page/Page column 34
(2013/04/10)
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- CHEMICAL COMPOUNDS
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The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
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Page/Page column 113
(2008/06/13)
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- A simple method for the preparation of monomethyl esters of dicarboxylic acids by selective esterification of the nonconjugated carboxyl group in the presence of an aromatic or conjugated carboxyl group
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Various dicarboxylic acids have been converted selectively into monomethyl esters in which the nonconjugated carboxyl group is selectively esterified in the presence of an aromatic or conjugated carboxyl group at room temperature (~ 25-27°C) in methanol using a catalytic amount of thionyl chloride.
- Ram, Ram N.,Meher, Nabin Kumar
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p. 282 - 283
(2007/10/03)
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- Selective esterification of nonconjugated carboxylic acids in the presence of conjugated or aromatic carboxylic acids under mild conditions
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Nonconjugated carboxylic acids are selectively esterified in good yields in the presence of conjugated or aromatic carboxylic acids by stirring over Amberlyst-15 in alcohol at room temperature.
- Anand, Ramesh C.,Vimal,Milhotra, Archana
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p. 378 - 379
(2007/10/03)
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- Selective esterification of aliphatic nonconjugated carboxylic acids in the presence of aromatic or conjugated carboxylic acids catalysed by NiCl2.6H2O
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Unhindered aliphatic nonconjugated carboxylic acids were esterified selectively in the presence of aromatic or conjugated acids on heating in the corresponding alcoholic solutions at reflux for 3-13 hr with 10 mol% of NiCl2.6H2O catalyst.
- Ram, Ram N.,Charles
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p. 7335 - 7340
(2007/10/03)
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- Use of Phosphorus Pentoxide. Preparation of Half-esters through Selective Esterification
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Methyl 2-,3-,4-carboxyphenylacetate and methyl 2-,3-,4-carboxyphenoxyacetate have been prepared through selective esterification of the aliphatic carboxylic acid function of the corresponding dicarboxylic acids using a mixture of phosphorus pentoxide (1 part), anhydrous copper sulphate (5 parts) and anhydrous sodium sulphate (5 parts).All the isomeric half-esters have been prepared through partial hydrolysis of the corresponding dimethylesters.
- Banerjee, Amalendu,Adak, Mohini Mohan,Das, Sankar,Banerjee, Santa,Sengupta, Saumitra
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