Patent classifications
C07D263/34
OXAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION
The present invention provides an oxazole compound represented by Formula (1), or a salt thereof:
##STR00001##
wherein R.sup.1 is an aryl group which may have one or more substituents; R.sup.2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y.sup.1-A.sup.1- or —Y.sup.2—C(═O)— wherein Y.sup.1 is a group such as —C(═O)—, A.sup.1 is a group such as a tower alkylene group, and Y.sup.2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
OXAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION
The present invention provides a oxazole compound represented by Formula (1), or a salt thereof:
##STR00001##
wherein R.sup.1 is an aryl group which may have one or more substituents; R.sup.2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y.sup.1-A.sup.1- or —Y.sup.2—C(═O)— wherein Y.sup.1 is a group such as —C(═O)—, A.sup.1 is a group such as a lower alkylene group, and Y.sup.2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
(2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID
In one aspect, the invention relates to a compound of the structure:
##STR00001##
or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
(2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID
In one aspect, the invention relates to a compound of the structure:
##STR00001##
or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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.
##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.
##STR00001##
ESTERS OF NON- AROMATIC HETEROCYCLIC COMPOUNDS HAVING A NEMATOCIDAL ACTIVITY, THEIR AGRONOMIC COMPOSITIONS AND USE THEREOF
Non-aromatic fluoroalkenyl heterocyclic compounds having general formula (I), agronomic compositions containing said compounds having formula (I) and their use for the control of nematodes in agricultural crops, are described.
ESTERS OF NON- AROMATIC HETEROCYCLIC COMPOUNDS HAVING A NEMATOCIDAL ACTIVITY, THEIR AGRONOMIC COMPOSITIONS AND USE THEREOF
Non-aromatic fluoroalkenyl heterocyclic compounds having general formula (I), agronomic compositions containing said compounds having formula (I) and their use for the control of nematodes in agricultural crops, are described.
HBV INHIBITOR AND ITS USE
The present invention provides anti-HBV compounds, pharmaceutically acceptable compounds or stereoisomers thereof, and preparation methods and uses for treating, eradicating or inhibiting HBV infection or for alleviating liver injury caused by HBV infection, and so on.
HBV INHIBITOR AND ITS USE
The present invention provides anti-HBV compounds, pharmaceutically acceptable compounds or stereoisomers thereof, and preparation methods and uses for treating, eradicating or inhibiting HBV infection or for alleviating liver injury caused by HBV infection, and so on.