C07D417/12

CONJUGATED POLYMERS BASED ON TERTHIOPHENE AND THEIR APPLICATIONS
20180013069 · 2018-01-11 ·

Disclosed are conjugated polymers based on terthiophene. Such polymers exhibit good solubility and great solution processibility, and that enable highly efficient OPVs.

2-benzopyrazinyl-n-heteroaryl-2-phenyl-acetamide compounds

The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

2-benzopyrazinyl-n-heteroaryl-2-phenyl-acetamide compounds

The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF

This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R.sup.4, R.sup.q, o, R.sup.A, W and R.sup.B and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.

##STR00001##

QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF

This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R.sup.4, R.sup.q, o, R.sup.A, W and R.sup.B and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.

##STR00001##

CHROMENONE INHIBITORS OF MONOCARBOXYLATE TRANSPORTERS

The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.

CHROMENONE INHIBITORS OF MONOCARBOXYLATE TRANSPORTERS

The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.

Human plasma kallikrein inhibitors

Disclosed are compounds of formula I ##STR00001## as described herein, and pharmaceutically acceptable salts thereof. The compounds are disclosed to be inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

Human plasma kallikrein inhibitors

Disclosed are compounds of formula I ##STR00001## as described herein, and pharmaceutically acceptable salts thereof. The compounds are disclosed to be inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamides useful as CCR6 inhibitors

The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) ##STR00001##
or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.