Patent classifications
C07D207/337
N-cycloalkyl-N-[(fusedphenyl)methylene]-(thio)carboxamide derivatives
The present invention relates to fungicidal N-cycloalkyl-N-[(fusedphenyl)methylene] carboxamide derivatives, for example, compounds of formula (I), and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control ofphytopathogenic fungi of plants using these compounds or their compositions. ##STR00001##
N-cycloalkyl-N-[(fusedphenyl)methylene]-(thio)carboxamide derivatives
The present invention relates to fungicidal N-cycloalkyl-N-[(fusedphenyl)methylene] carboxamide derivatives, for example, compounds of formula (I), and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control ofphytopathogenic fungi of plants using these compounds or their compositions. ##STR00001##
Modulators of calcium release-activated calcium channel
Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
Modulators of calcium release-activated calcium channel
Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
Compounds for controlling arthropods
The invention relates inter alia to compounds of the general formula (I) ##STR00001##
in which the A.sub.1-A.sub.4, T, n, W, Q, R.sup.1 and B.sub.1-B.sub.4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
Compounds for controlling arthropods
The invention relates inter alia to compounds of the general formula (I) ##STR00001##
in which the A.sub.1-A.sub.4, T, n, W, Q, R.sup.1 and B.sub.1-B.sub.4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
Epitope-Based Approach for Allergy Treatments and Inhibitors for Crohn's Disease
The present disclosure relates to pharmaceutical compounds and compositions and methods for treating an allergy and Crohn's disease. Methods for treating an allergy can include (a) predicting potential epitopes based proteomes of microbiome and that of an allergen, (b) filtering the potential epitopes obtained in step a) to result in a list of epitopes; and (c) reengineering the list of epitopes obtained in step b) to result in the new epitope. Methods for treating Crohn's disease can include (a), identifying one or more binding regions of an HLA class II protein and/or hemagglutinin to I2 superantigen; (b) determining a first peptide sequence corresponding to the one or more binding regions, and (c) producing a peptide inhibitor having a second peptide sequence that is a mutation of the first peptide sequence, wherein the second peptide sequence has a stronger binding affinity to the I2 superantigen than the first peptide sequence.
Pyrrole derivatives as PLK1 inhibitors
The invention provides compounds of the formula (3): ##STR00001##
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R.sup.1 is selected from various substituents:
R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.4 is selected from various substituents;
R.sup.5 is selected from various substituents;
Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group;
R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b;
Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker;
R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c;
R.sup.b is selected from hydrogen and various substituents;
and R.sup.7 is selected from R.sup.4. The compounds are useful in the treatment of cancers.
Method of treating or preventing Ras-mediated diseases
Disclosed are compounds, for example, a compound of formula I, ##STR00001##
wherein R, R.sub.0, R.sub.1-R.sub.8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.
Method of treating or preventing Ras-mediated diseases
Disclosed are compounds, for example, a compound of formula I, ##STR00001##
wherein R, R.sub.0, R.sub.1-R.sub.8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.