The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I):

##STR00001##

[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I):

##STR00001##

[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

The present invention relates to novel compounds of general formula (I):

##STR00001##

with A being A1 or A.sup.2:

##STR00002##

and
in which T, X, Y, Ro, R.sup.1, R.sup.10 and R.sup.11 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

The present invention relates to novel compounds of general formula (I):

##STR00001##

with A being A1 or A.sup.2:

##STR00002##

and
in which T, X, Y, Ro, R.sup.1, R.sup.10 and R.sup.11 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): ##STR00001##
[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): ##STR00001##
[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.

Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.

Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.

The present invention provides a method for controlling soybean rust fungus having an amino acid replacement of F129L in mitochondrial cytochrome b protein. A compound represented by formula (I) [wherein: Q represents a group represented by Q1 etc. (wherein “•” represents a position bonding to benzene ring); E represents C1-C6 chain hydrocarbon group, etc.; R.sup.1 represents C1-C3 chain hydrocarbon group, etc.; n is 0, 1, 2 or 3; when n is 2 or 3, two or more of R.sup.2 may be identical to or different from each other; and R.sup.2 represents C1-C3 chain hydrocarbon group, etc.] can be used for controlling soybean rust fungus having an amino acid replacement of F129L in mitochondrial cytochrome b protein.

##STR00001##