The present invention relates to a compounds of general formula (I) inhibiting DDR1 and DDR2, particularly the invention relates to compounds that are benzylamine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of DDRs, in particular fibrosis.

The present invention relates to a compounds of general formula (I) inhibiting DDR1 and DDR2, particularly the invention relates to compounds that are benzylamine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of DDRs, in particular fibrosis.

The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.

The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.

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.

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.

Compounds of Formula 1a, 1b, or Ic, (Ia); (Ib); or (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

##STR00001##

Compounds of Formula 1a, 1b, or Ic, (Ia); (Ib); or (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

##STR00001##

Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi. ##STR00001##