Patent classifications
C07D213/75
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
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.
N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),
##STR00001## wherein A.sup.1, Y and Z all represent rings.
N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),
##STR00001## wherein A.sup.1, Y and Z all represent rings.
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Joseph D. Eckelbarger ,
- Daniel I. Knueppel ,
- Ronald J. Heemstra ,
- Ronald Ross, Jr. ,
- Kyle A. DeKorver ,
- Kaitlyn Gray ,
- Peter Vednor ,
- Timothy P. Martin ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich W. Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary D. Crouse ,
- John F. Daeuble, SR. ,
- Fangzheng Li ,
- Jeffrey Nissen ,
- Michelle Riener ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
##STR00001##
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- Ronald Ross, Jr. ,
- Kyle A. DeKorver ,
- Ronald J. Heemstra ,
- Daniel I. Knueppel ,
- Peter Vednor ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich W. Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary D. Crouse ,
- John F. Daeuble, SR. ,
- Fangzheng Li ,
- Jeffrey Nissen ,
- Michelle Riener ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
##STR00001##
ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME
The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.
ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME
The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.
NEW CHEMICAL PROCESS FOR MAKING 6-CHLORO-4-(4-FLUORO-2-METHYLPHENYL)PYRIDIN-3-AMINE A KEY INTERMEDIATE OF NT-814
The invention relates to a new process for producing compound 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide (Compound IX) which is useful in the manufacture of compound 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide (Compound A).
NEW CHEMICAL PROCESS FOR MAKING 6-CHLORO-4-(4-FLUORO-2-METHYLPHENYL)PYRIDIN-3-AMINE A KEY INTERMEDIATE OF NT-814
The invention relates to a new process for producing compound 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide (Compound IX) which is useful in the manufacture of compound 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide (Compound A).