Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole or a 5-heteroaryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.

Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole or a 5-heteroaryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.

The invention relates to a crystal form of 4-phenylthiazole derivative, a pharmaceutical composition comprising the same, a preparation method, and a use of the crystal form for the manufacture of a medicament for treating thrombocytopenia. ##STR00001##

The invention relates to a crystal form of 4-phenylthiazole derivative, a pharmaceutical composition comprising the same, a preparation method, and a use of the crystal form for the manufacture of a medicament for treating thrombocytopenia. ##STR00001##

The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compound of the invention.

The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compound of the invention.

Compounds represented by the structural formula (1) R1, R2, R3, R4, R5, R6 are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

Compounds represented by the structural formula (1) R1, R2, R3, R4, R5, R6 are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

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