Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

Co-crystals of itanapraced; methods of preparation of the co-crystals; uses of the co-crystals as APIs; formulations containing the co-crystals; uses of the co-crystals and formulations for prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries; and methods of prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries are described.

Novel Halogenated Benzylidine derivatives are provided which exhibit activity for the treatment of immunological diseases and inflammation

Novel Halogenated Benzylidine derivatives are provided which exhibit activity for the treatment of immunological diseases and inflammation

The object of the present invention is to provide a mitochondrial dysfunction improving agent comprising a vitamin K derivative having a high deliverability to mitochondria.

A mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising at least one of a carboxylic acid ester of an active vitamin K represented by a general formula (1) or a salt thereof, and

##STR00001##

(wherein, R.sub.1 and R.sub.2 are a hydrogen atom, respectively, or a substituent selected from glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof; and at least either of R.sub.1 and R.sub.2 is glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof. R.sub.3 is a group represented by a general formula (2), or a general formula (3). n is an integer of 1 to 7)

##STR00002##

a mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising a carboxylic acid ester of an active vitamin K or a salt thereof (in the general formula (1), R.sub.1 and R.sub.2 is a carboxylic acid residue selected from a group consisting of R.sub.4OOCCH.sub.2CH.sub.2CO— and R.sub.4OOCCH.sub.2CH.sub.2CH.sub.2CO—. R.sub.3 represents the above general formula (2) or (3). R.sub.4 is a C1-C3 alkyl group.).

The object of the present invention is to provide a mitochondrial dysfunction improving agent comprising a vitamin K derivative having a high deliverability to mitochondria.

A mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising at least one of a carboxylic acid ester of an active vitamin K represented by a general formula (1) or a salt thereof, and

##STR00001##

(wherein, R.sub.1 and R.sub.2 are a hydrogen atom, respectively, or a substituent selected from glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof; and at least either of R.sub.1 and R.sub.2 is glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof. R.sub.3 is a group represented by a general formula (2), or a general formula (3). n is an integer of 1 to 7)

##STR00002##

a mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising a carboxylic acid ester of an active vitamin K or a salt thereof (in the general formula (1), R.sub.1 and R.sub.2 is a carboxylic acid residue selected from a group consisting of R.sub.4OOCCH.sub.2CH.sub.2CO— and R.sub.4OOCCH.sub.2CH.sub.2CH.sub.2CO—. R.sub.3 represents the above general formula (2) or (3). R.sub.4 is a C1-C3 alkyl group.).

The present disclosure relates, in certain embodiments, to the finding that certain compounds that modulate the activity(ies) of Sigma receptors can be used to disrupt virus lifecycle, infection, and/or dissemination. The compounds contemplated in the disclosure are useful in the prevention, treatment, and/or amelioration of virus infection, either alone or in combination with at least one additional therapeutic agent, which can be an antiviral agent and/or an agent that treats, ameliorates, and/or prevents one or more virus infection symptoms and/or co-morbidities. In certain embodiments, the Sigma receptor is a Sigma-1 receptor (also known as Sigma1) or Sigma-2 receptor (also known as Sigma2 or TMEM97). In certain embodiments, Sigma1 inhibitors/antagonists that cause and/or trigger ER stress and/or autophagy are useful within the methods of the disclosure.

The present disclosure relates, in certain embodiments, to the finding that certain compounds that modulate the activity(ies) of Sigma receptors can be used to disrupt virus lifecycle, infection, and/or dissemination. The compounds contemplated in the disclosure are useful in the prevention, treatment, and/or amelioration of virus infection, either alone or in combination with at least one additional therapeutic agent, which can be an antiviral agent and/or an agent that treats, ameliorates, and/or prevents one or more virus infection symptoms and/or co-morbidities. In certain embodiments, the Sigma receptor is a Sigma-1 receptor (also known as Sigma1) or Sigma-2 receptor (also known as Sigma2 or TMEM97). In certain embodiments, Sigma1 inhibitors/antagonists that cause and/or trigger ER stress and/or autophagy are useful within the methods of the disclosure.