C07F9/6558

Heterocycle substituted pyridine derivative antifungal agents

Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

Therapeutics for the treatment of glaucoma

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K.sub.ATP channel to reduce an intraocular pressure.

Bortezomib conjugates and methods using same

The present invention provides compositions and methods for providing controllable local delivery of a conjugate of bortezomib (Btz) and a bisphosphonate to promote bone formation. In certain embodiments, the invention is used as a treatment for a subject with diseases and disorders characterized by bone loss.

Organic electronic device comprising an organic semiconductor layer

The present invention relates to a compound of formula 1 and an organic electronic device comprising an organic semiconductor layer, wherein at least one organic semiconductor layer comprises a compound of formula (1), wherein L.sup.1 has the formula (2) and L.sup.2 has the formula (3), wherein L.sup.1 and L.sup.2 are bonded at “*” via a single bond independently to the same or different arylene groups or heteroarylenes group of Ar.sup.1; and wherein X.sup.1, X.sup.2 are independently selected from O, S and Se; Ar.sup.1 is selected from substituted or unsubstituted C.sub.20 to C.sub.52 arylene or C.sub.14 to C.sub.64 heteroarylene, wherein the substituent of the substituted C.sub.20 to C.sub.52 arylene or C.sub.14 to C.sub.64 heteroarylene are independently selected from C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 alkoxy, CN, halogen, OH, C.sub.6 to C.sub.25 aryl and C.sub.2 to C.sub.21 heteroaryl; R.sup.1, R.sup.2 are independently selected from substituted or unsubstituted C.sub.1 to C.sub.16 alkyl, wherein the substituent of substituted C.sub.1 to C.sub.16 alkyl is selected from C.sub.6 to C.sub.18 arylene or C.sub.2 to C.sub.12 heteroarylene; R.sup.3, R.sup.4 are independently selected from substituted or unsubstituted C.sub.1 to C.sub.16 alkyl, substituted or unsubstituted C.sub.6 to C.sub.18 arylene, C.sub.2 to C.sub.20 heteroarylene, wherein the substituent of substituted C.sub.1 to C.sub.16 alkyl, the substituent of the substituted C.sub.6 to C.sub.18 arylene, C.sub.2 to C.sub.20 heteroarylene are independently selected from C.sub.6 to C.sub.18 arylene or C.sub.2 to C.sub.12 heteroarylene; n is selected from 1 to 5, wherein n is an integer number.

THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K.sub.ATP channel to reduce an intraocular pressure.

Heteroaryl Compounds For Kinase Inhibition

Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.

RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND PREPARATION METHOD AND USE THEREOF

The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).

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PROCESSES FOR PREPARING PHOSPHORODIAMIDATE MORPHOLINO OLIGOMERS

Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomersynthesis while maintaining overall yield and purity of a synthesized oligomer.

TROPOMYOSIN-RELATED KINASE (trk) INHIBITORS

Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

Benzimidazol derivatives for treating filovirus infection

The present invention relates to compounds comprising a benzimidazole scaffold, and the use of such compounds for the treatment of viral diseases. The invention also relates to pharmaceutical compositions comprising said compounds as an active ingredient. In particular the compounds of the invention comprising a benzimidazole scaffold are used for the treatment of filoviruses or retroviruses, and preferably for the treatment of Ebola virus or HIV virus.