C07D277/24

CYCLOBUTANE CONTAINING CARBOXYLIC ACID GPR120 MODULATORS
20170247311 · 2017-08-31 ·

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

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Fungicidal 3-{phenyl[heterocyclylmethoxy)imino]methyl}-oxadiazolone derivatives

The present invention provides 4-substituted-3-{phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) ##STR00001##
Wherein A and X.sup.1 to X.sup.3 and Y1 to Y.sup.5 represent various substituents.

Fungicidal 3-{phenyl[heterocyclylmethoxy)imino]methyl}-oxadiazolone derivatives

The present invention provides 4-substituted-3-{phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) ##STR00001##
Wherein A and X.sup.1 to X.sup.3 and Y1 to Y.sup.5 represent various substituents.

Fluorine-containing ether compound, lubricant for magnetic recording medium, and magnetic recording medium

A fluorine-containing ether compound represented by Formula (1) is provided.
R.sup.1—R.sup.2—CH.sub.2—R.sup.3—CH.sub.2—R.sup.4—R.sup.5   (1)
(In Formula (1), R.sup.1 and R.sup.5 each represents a group having a heterocyclic ring and may be the same as or different from each other, R.sup.2 and R.sup.4 each represents a divalent linking group having a polar group and play be the same as or different from each other, and R.sup.3 represents a perfluoropolyether chain.)

Fluorine-containing ether compound, lubricant for magnetic recording medium, and magnetic recording medium

A fluorine-containing ether compound represented by Formula (1) is provided.
R.sup.1—R.sup.2—CH.sub.2—R.sup.3—CH.sub.2—R.sup.4—R.sup.5   (1)
(In Formula (1), R.sup.1 and R.sup.5 each represents a group having a heterocyclic ring and may be the same as or different from each other, R.sup.2 and R.sup.4 each represents a divalent linking group having a polar group and play be the same as or different from each other, and R.sup.3 represents a perfluoropolyether chain.)

COMPOUNDS FOR TREATMENT OF CANCER

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Inhibitors of lysine gingipain

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. ##STR00001##

HETEROCYCLIC MITOCHONDRIAL ACTIVITY INHIBITORS AND USES THEREOF

Heterocyclic compounds of Formula (I) and pharmaceutically acceptable salt thereof are disclosed. The use of such heterocyclic compounds and pharmaceutically acceptable salt thereof for the treatment of cancers, and more particularly cancers sensitive to mitochondrial activity inhibition and increased reactive oxygen species (ROS) levels, is also disclosed. Such cancers include acute myeloid leukemia (AML), preferably AML characterized by certain features, such as high level of expression of one or more Homeobox (HOX)-network genes, high and/or low expression of specific genes, the presence of one or more cytogenetic or molecular risk factors such as intermediate cytogenetic risk, Normal Karyotype (A/K), mutated NPM1, mutated CEBPA, mutated FLT3, mutated DNMT3A, mutated TET2, mutated IDH1, mutated IDH2, mutated RUNX1, mutated WT1, mutated SRSF2, intermediate cytogenetic risk with abnormal karyotype (intern(abnK)), trisomy 8 (+8) and/or abnormal chromosome (5/7), and/or a high leukemic stem cell (LSC) frequency.

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HETEROCYCLIC MITOCHONDRIAL ACTIVITY INHIBITORS AND USES THEREOF

Heterocyclic compounds of Formula (I) and pharmaceutically acceptable salt thereof are disclosed. The use of such heterocyclic compounds and pharmaceutically acceptable salt thereof for the treatment of cancers, and more particularly cancers sensitive to mitochondrial activity inhibition and increased reactive oxygen species (ROS) levels, is also disclosed. Such cancers include acute myeloid leukemia (AML), preferably AML characterized by certain features, such as high level of expression of one or more Homeobox (HOX)-network genes, high and/or low expression of specific genes, the presence of one or more cytogenetic or molecular risk factors such as intermediate cytogenetic risk, Normal Karyotype (A/K), mutated NPM1, mutated CEBPA, mutated FLT3, mutated DNMT3A, mutated TET2, mutated IDH1, mutated IDH2, mutated RUNX1, mutated WT1, mutated SRSF2, intermediate cytogenetic risk with abnormal karyotype (intern(abnK)), trisomy 8 (+8) and/or abnormal chromosome (5/7), and/or a high leukemic stem cell (LSC) frequency.

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Compositions and methods for inhibiting group II intron RNA

The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.