Patent classifications
C07D213/85
Krüppel-Like Factor 15 (KLF15) Small Molecule Agonists in Kidney Disease
The present disclosure is concerned with small molecule modulators of KLF15 signaling useful for treating various disorders such as, for example, kidney disease (e.g., chronic kidney disease), heart disease, obesity, or a neurodegenerative disorder (e.g., amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
ACLY inhibitors and uses thereof
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation
The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. ##STR00001##
PESTICIDALLY ACTIVE CYCLIC AMINE COMPOUNDS
- Ottmar Franz Hueter ,
- Damien BONVALOT ,
- Farhan Bou Hamdan ,
- Andrew Edmunds ,
- Julien Daniel Henri Gagnepain ,
- Elke Maria HILLESHEIM ,
- Olivier JACOB ,
- Pierre Joseph Marcel Jung ,
- Amandine KOLLETH KRIEGER ,
- Thomas Pitterna ,
- Martin POULIOT ,
- Sebastian RENDLER ,
- Peter Renold ,
- Christopher Charles SCARBOROUGH ,
- Vikas SIKERVAR ,
- Carmela NAPOLITANO
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.
##STR00001##
PESTICIDALLY ACTIVE CYCLIC AMINE COMPOUNDS
- Ottmar Franz Hueter ,
- Damien BONVALOT ,
- Farhan Bou Hamdan ,
- Andrew Edmunds ,
- Julien Daniel Henri Gagnepain ,
- Elke Maria HILLESHEIM ,
- Olivier JACOB ,
- Pierre Joseph Marcel Jung ,
- Amandine KOLLETH KRIEGER ,
- Thomas Pitterna ,
- Martin POULIOT ,
- Sebastian RENDLER ,
- Peter Renold ,
- Christopher Charles SCARBOROUGH ,
- Vikas SIKERVAR ,
- Carmela NAPOLITANO
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.
##STR00001##
PHOSPHINE REAGENTS FOR AZINE FLUOROALKYLATION
A new set of bench-stable fluoroalkylphosphines that directly convert C—H bonds in pyridine building blocks, drug-like fragments, and pharmaceuticals, into fluoroalkyl derivatives. No pre-installed functional groups or directing motifs are required. The reaction tolerates a variety of sterically and electronically distinct pyridines and is exclusively selective for the 4-position in most cases. The reaction proceeds via initial phosphonium salt formation followed by sp.sup.2-sp.sup.3 phosphorus ligand-coupling, an underdeveloped manifold for C—C bond formation.
Heterocyclic compound
- Koji Ono ,
- Masahiro Ito ,
- Toshio Tanaka ,
- Moriteru Asano ,
- Takaharu Hirayama ,
- Jun Fujimoto ,
- Nobuki Sakauchi ,
- Yasuhiro Hirata ,
- Akinori Toita ,
- Nao Morishita ,
- Hironori Kokubo ,
- Yasuhiro Imaeda ,
- Hironobu Maezaki ,
- Douglas Robert Cary ,
- Ryo Mizojiri ,
- Nobuo Cho ,
- Hiroshi Banno ,
- Hidekazu Tokuhara ,
- Yasuyoshi Arikawa
Provided is a compound that may have a superior CDK12 inhibitory action and is expected to be useful as a prophylactic or therapeutic drug for cancer and the like. A compound represented by the following formula (I): ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
SUBSTITUTED PYRIDINES AS DNMT1 INHIBITORS
The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.
SUBSTITUTED PYRIDINES AS DNMT1 INHIBITORS
The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.