Patent classifications
C07C233/81
PFKFB3 INHIBITORS AND THEIR USES
- Petr Olegovich FEDICHEV ,
- Kevin GREENMAN ,
- Chang CHIH-TSUNG ,
- Maksim Nikolaevich KHOLIN ,
- Evgeny Gennadievich GETMANTSEV ,
- Tatiana Vladimirovna ZHIDKOVA ,
- Alexandr Viktorovich KADUSHKIN ,
- Timofey Vladimirovich PYRKOV ,
- Dmitry Veniaminovich SHISHOV ,
- Juan Pedro BOLANOS-HERNANDEZ ,
- Kristina Aleksandrovna ZAKURDAEVA ,
- Olga Andreevna BURMISTROVA
This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.
TRANSMEMBRANE PORES FORMED BY AROMATIC OLIGOAMIDE FOLDAMERS AND USES OF SAME
Provided are aromatic oligoamide foldamers and self-assembled compositions of the same. The aromatic oligoamide foldamers and compositions can form tube-like structures that can form pores in membranes. The pores can be used to transport ions and molecules, such as, for example, cryoprotective agents or therapeutic agents, through the membrane. The tube-like structures exhibit desirable stability at low temperatures.
MASP-2 inhibitors and methods of use
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
COMPOUNDS AND THEIR USE
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
COMPOUNDS AND THEIR USE
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
Small molecule inhibitors selective for polo-like kinase proteins
Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of ##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.
Small molecule inhibitors selective for polo-like kinase proteins
Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of ##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.
Composition Containing Polyamideimide Precursor or Polyamideimide, and Polyamideimide Film Produced Using the Same
The present disclosure relates to a composition containing a polyamideimide precursor and/or polyamideimide, a polyamideimide film produced using the composition, and a display device including the polyamideimide film. The polyamideimide film produced using the composition and the display device including the polyamideimide film have excellent mechanical and optical properties.
Composition Containing Polyamideimide Precursor or Polyamideimide, and Polyamideimide Film Produced Using the Same
The present disclosure relates to a composition containing a polyamideimide precursor and/or polyamideimide, a polyamideimide film produced using the composition, and a display device including the polyamideimide film. The polyamideimide film produced using the composition and the display device including the polyamideimide film have excellent mechanical and optical properties.
SALICYLAMIDE DERIVATIVES AND RELATED METHODS OF MAKING
Certain embodiments describe antiviral compounds and related methods of using such compounds.