C07D213/71

DOCK1-INHIBITING COMPOUND AND USE THEREOF

Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof:

##STR00001## wherein X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group, or a hydrocarbon group; R.sup.1 and R.sup.2 are different, and each represents a hydrogen atom or a group represented by the following formula (A-1):

##STR00002## (wherein R.sup.6 represents a pyrrolidino group or a phenyl group, and n.sup.2 is 0 or 1); R.sup.3 represents —CO—R.sup.7 (wherein R.sup.7 is an alkoxy group, an alkyl group, or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom, or an oxygen atom; R.sup.4 represents a hydrogen atom, an oxygen atom, or a hydrocarbon group in which one or more hydrogen atoms may be replaced by one or more substituents; R.sup.5 represents a halogen atom, a halogenated alkyl group, or a halogenated alkylthio group; and n.sup.1 is an integer of 0 to 5; and in the skeleton of the compound of formula (A), each single solid line represents a single bond; each double line consisting of a solid line and a dotted line represents a single bond or a double bond; and two dotted lines represent no bond or a double bond.

DOCK1-INHIBITING COMPOUND AND USE THEREOF

Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof:

##STR00001## wherein X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group, or a hydrocarbon group; R.sup.1 and R.sup.2 are different, and each represents a hydrogen atom or a group represented by the following formula (A-1):

##STR00002## (wherein R.sup.6 represents a pyrrolidino group or a phenyl group, and n.sup.2 is 0 or 1); R.sup.3 represents —CO—R.sup.7 (wherein R.sup.7 is an alkoxy group, an alkyl group, or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom, or an oxygen atom; R.sup.4 represents a hydrogen atom, an oxygen atom, or a hydrocarbon group in which one or more hydrogen atoms may be replaced by one or more substituents; R.sup.5 represents a halogen atom, a halogenated alkyl group, or a halogenated alkylthio group; and n.sup.1 is an integer of 0 to 5; and in the skeleton of the compound of formula (A), each single solid line represents a single bond; each double line consisting of a solid line and a dotted line represents a single bond or a double bond; and two dotted lines represent no bond or a double bond.

PYRIDINYL SULFONAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
20210353608 · 2021-11-18 ·

The invention relates to new pyridinyl sulfonamide derivatives of the formula

##STR00001##

wherein R.sup.1, A and n are as defined herein, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

PROCESS FOR PREPARING A NOVEL PHENICOL ANTIBACTERIAL AGENT

The present invention provides a novel process for preparing a diastereomeric mixture of the phenicol of Formula (1), its use for the treatment of bacterial infections in animals, and veterinary compositions containing the Formula (1) compound, diastereomers thereof, and veterinary acceptable salts thereof.

##STR00001##

PROCESS FOR PREPARING A NOVEL PHENICOL ANTIBACTERIAL AGENT

The present invention provides a novel process for preparing a diastereomeric mixture of the phenicol of Formula (1), its use for the treatment of bacterial infections in animals, and veterinary compositions containing the Formula (1) compound, diastereomers thereof, and veterinary acceptable salts thereof.

##STR00001##

BIARYL DERIVATIVE

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein X.sup.1 represents a nitrogen atom or CR.sup.9, R.sup.1 represents a hydrogen atom, a C.sup.1-C.sup.6 alkyl group, or a C.sup.1-C.sup.6 alkoxy group, R.sup.2 represents a halogen atom, R.sup.3 represents a hydrogen atom or a halogen atom, R.sup.4 represents a hydrogen atom or a halogen atom, and R5 represents a C.sup.1-C.sup.3 alkylsulfonyl group, a substituted C.sup.1-C.sup.6 alkyl group, a substituted C.sup.1-C.sup.6 haloalkyl group, a substituted C.sup.1-C.sup.6 alkoxy group, or a substituted C.sup.1-C.sup.6 alkylamino group, or a pharmacologically acceptable salt thereof.

##STR00001##

BIARYL DERIVATIVE

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein X.sup.1 represents a nitrogen atom or CR.sup.9, R.sup.1 represents a hydrogen atom, a C.sup.1-C.sup.6 alkyl group, or a C.sup.1-C.sup.6 alkoxy group, R.sup.2 represents a halogen atom, R.sup.3 represents a hydrogen atom or a halogen atom, R.sup.4 represents a hydrogen atom or a halogen atom, and R5 represents a C.sup.1-C.sup.3 alkylsulfonyl group, a substituted C.sup.1-C.sup.6 alkyl group, a substituted C.sup.1-C.sup.6 haloalkyl group, a substituted C.sup.1-C.sup.6 alkoxy group, or a substituted C.sup.1-C.sup.6 alkylamino group, or a pharmacologically acceptable salt thereof.

##STR00001##

PARG INHIBITORS AND METHOD OF USE THEREOF
20210355103 · 2021-11-18 ·

Provided herein are, inter alia, methods of treating cancer using compounds of the invention.

HALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF

The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

HALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF

The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.