C07D311/04

Geranyl flavonoid derivative with improved water solubility, a method for preparing the same, and a method for treating cancer using the same

The present invention relates to a novel geranyl flavonoid derivative with improved water-solubility or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a method for treating cancer using the same. Particularly, the novel geranyl flavonoid derivative of the present invention inhibits the expression of STAT3 target protein by suppressing the phosphorylation of STAT3 (Signal Transducers and Activators of Transcription 3) protein, suggesting that it has cancer cell growth inhibiting effect in various cancer cell lines. Also, the compound of the invention has the effect of reducing the size and weight of a tumor significantly in vivo, so that the geranyl flavonoid derivative or the pharmaceutically acceptable salt thereof can be efficiently used for the treatment of cancer.

N-SUBSTITUTED PYRIDINIOPHOSPHINES, PROCESSES FOR THEIR PREPARATION AND THEIR USE

The present invention deals with the synthesis and applications of new cationic compounds being useful as metal ligands. Specifically, N-alkyl/aryl substituted pyridiniophosphines are prepared and used as ligands for transition metals. The so-obtained metal complexes and their use as catalysts in chemical synthesis is also described. It also worth mentioning that N-alkyl/aryl pyridiniophosphines can be synthesized through a short, scalable and highly modular route.

N-SUBSTITUTED PYRIDINIOPHOSPHINES, PROCESSES FOR THEIR PREPARATION AND THEIR USE

The present invention deals with the synthesis and applications of new cationic compounds being useful as metal ligands. Specifically, N-alkyl/aryl substituted pyridiniophosphines are prepared and used as ligands for transition metals. The so-obtained metal complexes and their use as catalysts in chemical synthesis is also described. It also worth mentioning that N-alkyl/aryl pyridiniophosphines can be synthesized through a short, scalable and highly modular route.

Inhibitors of the interaction between MDM2 and P53

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: ##STR00001##
wherein n, m, p, s, t, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.20, X, Y, Q and Z have defined meanings.

6-substituted phenoxychroman carboxylic acid derivatives

Provided herein are compounds of Formula I: ##STR00001##
in which A.sup.1, A.sup.2, W, L, G, R.sup.7a, R.sup.7b, R.sup.8, R.sup.9 and R.sup.10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.

SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS
20170022180 · 2017-01-26 ·

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

PROCESS FOR THE PRODUCTION OF CANNABIDIOL AND DELTA-9-TETRAHYDROCANNABINOL
20170008868 · 2017-01-12 ·

The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.

PROCESS FOR THE PRODUCTION OF CANNABIDIOL AND DELTA-9-TETRAHYDROCANNABINOL
20170008869 · 2017-01-12 ·

The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.

PARTIALLY SATURATED TRICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

COMPOUNDS FOR THE TREATMENT OF A CENTRAL NERVOUS SYSTEM DISEASE OR DISORDER

Disclosed herein are substituted compounds, salts, and pharmaceutical formulations thereof, for the treatment of a central nervous system disease or disorder.