4244-59-1Relevant articles and documents
2-AMINO-QUINOLINE DERIVATIVES
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Paragraph 0174; 0200-0202, (2018/11/22)
Described herein are 2-amino-quinoline derivatives that are agonists of toll-like receptors 7 and 8 (TLR7/8), pharmaceutical compositions, and methods of use of the compounds and compositions to treat various diseases, such as viral, cancer, and allergic diseases, in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 000455; 000456, (2018/01/17)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
Novel bi-cyclic or tri-cyclic heterocyclic compound
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Paragraph 4067 - 4069, (2016/10/07)
The present invention provides novel bi-cyclic or tri-cyclic compound represented by formula (I) or pharmaceutical acceptable salt thereof, [wherein, ring A is an aromatic group which may be substituted, one of X1 and X2 is a carbon atom, and another is a nitrogen atom, X3 is a nitrogen atom or CR2, X4 is a nitrogen atom or CR3, X5 is a sulfur atom or -CH=CH-, Z1 is an oxygen atom, -C(R6)(R7)-, -NH-, -C(R6)(R7)-NH-, -NH-C(R6)(R7)-, -C(R6)(R7)-O-, -O-C(R6)(R7)- or a single bone, one of Z2 and Z3 is CH and another one is a nitrogen atom, or both are nitrogen atoms, the other symbols are same as those defined in the specification.]
P38 MAP KINASE INHIBITORS
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Page/Page column 42, (2010/07/02)
The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes,particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD
AMINOALCOHOL DERIVATIVES AND THEIR THERAPEUTIC USE
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Page/Page column 11, (2008/12/06)
A compound of formula (1 ) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3
SUBSTITUTED CYCLOHEXYL-1,4-DIAMINE DERIVATIVES WITH A CHAIN EXTENSION
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Page/Page column 25, (2008/06/13)
The invention relates to substituted cyclohexyl-1,4-diamine derivatives, to a method for their production, to medicaments containing said compounds and to the use of substituted cyclohexyl-1,4-diamine derivatives for producing medicaments.
Hepatic enzymatic synthesis and hydrolysis of CoA esters of solvent-derived oxa acids
Panuganti, Sree D.,Penn, Jill M.,Moore, Kathleen H.
, p. 76 - 85 (2007/10/03)
Many ethylene glycol-derived solvents are oxidized to xenobiotic alkoxyacetic acids (3-oxa acids) by hepatic enzymes. The toxicity of these ubiquitous solvents has been associated with their oxa acid metabolites. For many xenobiotic carboxylic acids, the toxicity is associated with the CoA ester of the acid. In this study, related alkoxyacetic acids were evaluated as potential substrates for acyl-CoA synthetases found in mitochondrial, peroxisomal, and microsomal fractions isolated from rat liver. Likewise, chemically synthesized oxa acyl-CoAs were used as substrates for acyl-CoA hydrolases associated with the same rat liver fractions. Activities of the xenobiotic oxygen-substituted substrates were compared with analogous physiologic aliphatic substrates by UV-vis spectrophotometric methods. All of the solvent-derived oxa acids were reasonable substrates for the acyl-CoA synthetases, although their activity was usually less than the corresponding physiologic acid. Acyl-CoA hydrolase activities were decreased compared with acyl-CoA synthetase activities for all substrates, especially for the oxa acyl-CoAs. These studies suggest that these xenobiotic carboxylic acids may be converted to reactive acyl-CoA moieties which will persist in areas of the cell proximal to lipid synthesis, β-oxidation, protein acylation, and amino acid conjugation. The interaction of these xenobiotic acyl-CoAs with those processes may be important to their toxicity and/or detoxification.
Phosphonic acid derivatives having carboxypeptidase b inhibitory activity
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, (2008/06/13)
A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2and R3represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7and R8represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9and R10represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.
Methods for lowering serum cholesterol
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, (2008/06/13)
A method of lowering serum cholesterol levels comprising administering to a patient a serum cholesterol lowering amount of a compound having the formula STR1 wherein n is 0, 1 or 2; R is hydroxyl, methoxy, C1 -C7 alkanoyloxy, C3
