The present disclosure relates to a novel adamantyl derivative or a pharmaceutically acceptable salt thereof, and a use thereof. The adamantyl derivative may be a dipeptidyl peptidase-4 (DPP4) inhibitor and may be utilized in the prevention or treatment of cancer, rheumatoid arthritis, Parkinson's disease, autoimmune diseases, skin diseases, non-alcoholic steatohepatitis, aortic valve contraction, cerebrovascular diseases, or the like. In particular, the adamantyl derivative suppresses DPP4 in a tumor microenvironment (TME) and guides T cells to tumor tissues, thereby killing cancer cells, and thus can be effectively used for preventing or treating cancer or inhibiting cancer metastasis. The cancer may be prostate cancer, thyroid cancer, kidney cancer, carcinoma, endometrial cancer, lung cancer, urinary epithelial cancer, colorectal cancer, breast cancer, rectal cancer, cervical cancer, glioma, colon cancer, head and neck cancer, stomach cancer, liver cancer, pancreatic cancer, testicular cancer, ovarian cancer, blood cancer, skin cancer, brain tumor, etc.

The present disclosure relates to a novel adamantyl derivative or a pharmaceutically acceptable salt thereof, and a use thereof. The adamantyl derivative may be a dipeptidyl peptidase-4 (DPP4) inhibitor and may be utilized in the prevention or treatment of cancer, rheumatoid arthritis, Parkinson's disease, autoimmune diseases, skin diseases, non-alcoholic steatohepatitis, aortic valve contraction, cerebrovascular diseases, or the like. In particular, the adamantyl derivative suppresses DPP4 in a tumor microenvironment (TME) and guides T cells to tumor tissues, thereby killing cancer cells, and thus can be effectively used for preventing or treating cancer or inhibiting cancer metastasis. The cancer may be prostate cancer, thyroid cancer, kidney cancer, carcinoma, endometrial cancer, lung cancer, urinary epithelial cancer, colorectal cancer, breast cancer, rectal cancer, cervical cancer, glioma, colon cancer, head and neck cancer, stomach cancer, liver cancer, pancreatic cancer, testicular cancer, ovarian cancer, blood cancer, skin cancer, brain tumor, etc.

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and sternness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

The invention provides novel antibacterial diamide compounds, pharmaceutical compositions comprising the compounds and methods for treating or preventing an infection in a subject using the compounds.

The invention provides novel antibacterial diamide compounds, pharmaceutical compositions comprising the compounds and methods for treating or preventing an infection in a subject using the compounds.

The present invention provides a process for producing a compound of the formula (1) wherein X represents a hydrogen atom, etc., and Y represents a hydrogen atom, etc., which comprises step 1 of reacting a compound of the formula (2) and a compound of the formula (3) in the presence of a Lewis acid wherein R represents a hydrogen atom, etc., to obtain an adduct, and step 2 of reacting the adduct obtained in the step 1 and hydrazine to obtain the compound of the formula (1). ##STR00001##

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

A new composition of matter has the molecular structure [I]: Formula (I) wherein R.sub.1 is an alkyl, cycloalkyl, aralkyl group having 1 to 10 carbon atoms; R.sub.2 is selected from the group consisting of an aliphatic C.sub.1-C.sub.10 group, an unsaturated C.sub.1-C.sub.10 chain, C.sub.4-C.sub.9 group with a cyclic portion and C.sub.4-C.sub.10 group with an aromatic portion, and combinations thereof; R.sub.3 is selected from the group consisting of hydrogen, an aliphatic C.sub.1-C.sub.10 group, an unsaturated C.sub.2-C.sub.10 chain, a C.sub.4-C.sub.10 group with a cyclic portion, C.sub.4-C.sub.10 group with an aromatic portion, and combinations thereof; and R.sub.4 is a terminal functional group selected from the group consisting of amide [CONH.sub.2], acid [COOH], amine [CH.sub.2NH.sub.2], guanamine [(C.sub.3N.sub.3)(NH.sub.2).sub.2], organic heterocyclic [CHN.sub.4], and combinations thereof; and wherein said composition of matter of the molecular structure [I] excludes 2-[(3-amino-1-ethylpropyl)amino]ethanol.

##STR00001##

A new composition of matter has the molecular structure [I]: Formula (I) wherein R.sub.1 is an alkyl, cycloalkyl, aralkyl group having 1 to 10 carbon atoms; R.sub.2 is selected from the group consisting of an aliphatic C.sub.1-C.sub.10 group, an unsaturated C.sub.1-C.sub.10 chain, C.sub.4-C.sub.9 group with a cyclic portion and C.sub.4-C.sub.10 group with an aromatic portion, and combinations thereof; R.sub.3 is selected from the group consisting of hydrogen, an aliphatic C.sub.1-C.sub.10 group, an unsaturated C.sub.2-C.sub.10 chain, a C.sub.4-C.sub.10 group with a cyclic portion, C.sub.4-C.sub.10 group with an aromatic portion, and combinations thereof; and R.sub.4 is a terminal functional group selected from the group consisting of amide [CONH.sub.2], acid [COOH], amine [CH.sub.2NH.sub.2], guanamine [(C.sub.3N.sub.3)(NH.sub.2).sub.2], organic heterocyclic [CHN.sub.4], and combinations thereof; and wherein said composition of matter of the molecular structure [I] excludes 2-[(3-amino-1-ethylpropyl)amino]ethanol.

##STR00001##