Abstract: Provided are a method for producing a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate, including reacting an acidic salt of 5-hydroxy-1H-imidazole-4-carboxamide or a hydrate thereof with a base selected from the group consisting of a phosphate and an amino acid in the presence of an acidic solvent to obtain a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate; and a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate obtained by the production method.

Abstract: Provided are a method for producing a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate, including reacting an acidic salt of 5-hydroxy-1H-imidazole-4-carboxamide or a hydrate thereof with a base selected from the group consisting of a phosphate and an amino acid in the presence of an acidic solvent to obtain a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate; and a 5-hydroxy-1H-imidazole-4-carboxamide•¾ hydrate obtained by the production method.

Abstract: Provided is a method for producing 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate, including: reacting 2-aminomalonamide with a compound represented by the following formula [1] in the presence of a carboxylic acid to obtain 5-hydroxy-1H-imidazole-4-carboxamide: wherein, in formula [1], each R independently represents a C1-3 alkyl group; reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide with an acidic compound to obtain a 5-hydroxy-1H-imidazole-4-carboxamide acid salt or a hydrate thereof; and reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide acid salt or hydrate thereof with a salt in the presence of an acidic solvent to obtain the 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate.

Abstract: Provided is a method for producing 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate, including: reacting 2-aminomalonamide with a compound represented by the following formula [1] in the presence of a carboxylic acid to obtain 5-hydroxy-1H-imidazole-4-carboxamide: wherein, in formula [1], each R independently represents a C1-3 alkyl group; reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide with an acidic compound to obtain a 5-hydroxy-1H-imidazole-4-carboxamide acid salt or a hydrate thereof; and reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide acid salt or hydrate thereof with a salt in the presence of an acidic solvent to obtain the 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: Provided is a method for producing 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate, including: reacting 2-aminomalonamide with a compound represented by the following formula [1] in the presence of a carboxylic acid to obtain 5-hydroxy-1H-imidazole-4-carboxamide: wherein, in formula [1], each R independently represents a C1-3 alkyl group; reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide with an acidic compound to obtain a 5-hydroxy-1H-imidazole-4-carboxamide acid salt or a hydrate thereof; and reacting the resulting 5-hydroxy-1H-imidazole-4-carboxamide acid salt or hydrate thereof with a salt in the presence of an acidic solvent to obtain the 5-hydroxy-1H-imidazole-4-carboxamide.3/4 hydrate.

Abstract: The present invention relates to novel nucleic acid molecules, called aptamers, that bind specifically to a small molecule fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.

Abstract: The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.

Abstract: Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described.

Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The present invention relates to a compound of the formula 1

Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1

Abstract: Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.

Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.