A61P19/06

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein ring A, R.sup.1, R.sup.3, R.sup.4, R.sup.5, and each R.sup.e have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (II):

##STR00001##

wherein

##STR00002##

R.sup.1, R.sup.2, R.sup.5 and R.sup.13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

AZOLE BENZENE DERIVATIVE AND CRYSTALLINE FORM THEREOF

There are provided: 4-methyl-2-[4-(2-methylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-1,3-thiazole-5-carboxylic acid, a sodium salt thereof and crystals of these, useful as a therapeutic agent and a prophylactic agent for gout, hyperuricemia and the like, and a method for producing the same.

Flap modulators

The present invention relates to compounds of Formula (I), or a form thereof wherein ring A.sub.1, R.sub.1, R.sub.2, R.sub.3, R.sub.3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##

Melanocortin Receptor Ligands
20170240595 · 2017-08-24 · ·

The present invention is directed to compounds according to formula,


(R.sup.2R.sup.3)-A.sup.1-c(A.sup.2-A.sup.3-A.sup.4-A.sup.5-A.sup.6-A.sup.7-A.sup.8-A.sup.9)-A.sup.10-R.sup.1,

and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

Oxazoline and isoxazoline derivatives as CRAC modulators

The present invention relates to compounds of Formula (I), ##STR00001##
along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).

Complex of glucose derivative and proline, crystal, preparation method and use

Disclosed are a complex of glucose derivative and proline, a crystal, a preparation method and a use. In an X-ray powder diffraction diagram of the eutectic crystal when the diffraction angle is 2θ, characteristic diffraction peaks comprise 4.339, 11.499, 12.835, 13.921, 15.294, 16.212, 16.804, 17.154, 18.335, 19.274, 19.982, 22.710, 23.218, 24.885, 27.940, 29.612 and 30.313, and the 2θ error range is ±0.1. The method comprises: mixing a compound A solution with an L-proline solution, and performing cooling and crystallization. The present invention further provides a of the crystal in medicine preparation. The eutectic crystal in the present invention features high water-solubility, low hygroscopicity and high stability, and is suitable for manufacturing a variety of preparations. ##STR00001##

FUSED HETEROAROMATIC PYRROLIDINONES

Disclosed are compounds of Formula 1,

##STR00001##

and pharmaceutically acceptable salts thereof, wherein G, L.sup.1, L.sup.2, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

CHEMICAL COMPOUNDS AS INHIBITORS OF INTERLEUKIN-1 ACTIVITY

The present disclosure relates to novel sulfonylurea and sulfonyl thiourea compounds and related compounds and their use in treating a disease or condition responsive to modulation of cytokines such as IL-1β and IL-18, modulation of NLRP3 or inhibition of the activation of NLRP3 or related components of the inflammatory process.

AAV VIRIONS WITH DECREASED IMMUNOREACTIVITY AND USES THEREFOR

Methods of making and using recombinant AAV virions with decreased immunoreactivity are described. The recombinant AAV virions include mutated capsid proteins or are derived from non-primate mammalian AAV serotypes and isolates that display decreased immunoreactivity relative to AAV-2.