C07D307/78

METHOD FOR PRODUCING DIPHENYLMETHANE DERIVATIVE

The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

Triazolopyrimidine compounds and uses thereof

A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and n are as defined herein.

CHROMANS AND BENZOFURANS AS 5-HT1A AND TAAR1 AGONISTS

Provided herein are compounds, pharmaceutical compositions, and methods of use thereof, including methods of treating a neurological or psychiatric disease or disorder. For example, provided herein is a compound of Formula I:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., Ring A, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5) are as disclosed herein. The compounds disclosed herein (e.g., compounds of Formula I, or pharmaceutically acceptable salts thereof) and pharmaceutical compositions can be used to treat a neurological or psychiatric disease or disorder.

ORGANIC ELECTROLUMINESCENT ELEMENT

By manufacturing an organic EL element using a material for a light emitting layer including a pyrene-based compound represented by the following formula (2) as a host material and a polycyclic aromatic compound in which a plurality of aromatic rings is linked with a boron atom and a nitrogen atom or an oxygen atom as a dopant material, an organic EL element having, for example, excellent light emission efficiency is provided.

##STR00001##

In the above formula (2), at least one hydrogen atom in a pyrene moiety may be substituted by an aryl having 6 to 10 carbon atoms or the like. Ar represents an aryl having 14 to 40 carbon atoms or a heteroaryl having 12 to 40 carbon atoms. These groups may be substituted by an aryl having 6 to 10 carbon atoms or the like. s and p each independently represent an integer of 1 or 2. s and p do not simultaneously represent 2. One or more hydrogen atoms in a compound represented by formula (2) may be each independently substituted by a halogen atom, cyano, or a deuterium atom.

METHOD FOR PRODUCING DIPHENYLMETHANE DERIVATIVE

The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

HETEROCYCLIC CARBOXYLIC ACID AMIDE LIGAND AND APPLICATIONS THEREOF IN COPPER CATALYZED COUPLING REACTION OF ARYL HALOGENO SUBSTITUTE

Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having CN, CO, CS and other bonds.

##STR00001##

HETEROCYCLIC CARBOXYLIC ACID AMIDE LIGAND AND APPLICATIONS THEREOF IN COPPER CATALYZED COUPLING REACTION OF ARYL HALOGENO SUBSTITUTE

Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having CN, CO, CS and other bonds.

##STR00001##

PYRIDAZINONE HERBICIDES

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof,

##STR00001##

wherein X is O, S or NR.sup.5; or X is C(R.sup.6)C(R.sup.7), wherein the carbon atom bonded to R.sup.6 is also bonded to the carbon atom bonded to R.sup.4, and the carbon atom bonded to R.sup.7 is also bonded to the phenyl ring moiety in Formula 1; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, G and W are as defined in the disclosure.

Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

FATTY ACID AMIDE HYDROLASE (FAAH) CLEAVABLE PRODRUGS OF BRAIN TARGETING ACTIVES AND COMBINATION WITH PERIPHERALLY RESTRICTED FAAH INHIBITORS

Provided herein are fatty acid amide (FAAH) cleavable prodrugs of compounds that modulate a target in the brain including sphingosine-1-phosphate receptor (S1P1), lysophosphatidic acid receptor 1 (LPA1), G-protein coupled receptor 120 (GPR120), prostacyclin (PGI2), and transthyretin (TTR). Pharmaceutical compositions comprising these prodrugs, including in combination with a peripherally restricted FAAH inhibitor, and at least one pharmaceutically acceptable excipient, are also provided, and the use of these compounds and compositions in the treatment of CNS diseases or disorders.

Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof

Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof are provided. Specifically, amide derivatives represented by general formula (I) are provided. The amide derivatives represented by general formula (I) can be used as a therapeutic agent, particularly as an inhibitor for microsomal prostaglandin E synthase-1 (mPGES-1), and also to treat and/or prevent diseases or illnesses such as inflammation and/or pain etc. The definition of each substituent group in general formula (I) is the same as the definition in the description. ##STR00001##