Patent classifications
C07D333/24
HETEROCYCLIC TRPML1 AGONISTS
Disclosed is a compound of formula (I)
##STR00001## or a stereoisomer thereof, or a salt of any of the foregoing and to processes for its preparation. The compounds of formula (I) are useful in the treatment TRPML1-mediated disorders or diseases.
T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.
HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
##STR00001##
HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
##STR00001##
METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.
VISIBLE-LIGHT MEDIATED ORGANOPHOTOREDOX CATALYTIC DEUTERATION OF AROMATIC AND ALIPHATIC ALDEHYDES
Described are methods for preparing a deuterated aldehyde using with a photocatalyst and a hydrogen atom transfer agent in a H.sub.2O free solvent comprising D.sub.2O and an organic solvent under an inert gas. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions.
METAL-ORGANIC FRAMEWORK HAVING TEREPHTHALIC ACID BASED LIGAND
Despite the fact that the amount and type of gas to be stored may vary in accordance with the type of substituent, metal-organic frameworks only using a terephthalic acid having substituents within the limited range have been produced conventionally. An object of the present invention is to provide a novel metal-organic framework using a 2,5-disubstituted terephthalic acid. A metal-organic framework comprising a carboxylate ion of formula (I) and a multivalent metal ion bound to each other is a novel metal-organic framework, enabling a gas such as hydrogen and nitrogen to be store efficiently. (wherein in formula (I), X is an unsubstituted or substituted cycloalkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted heterocyclyl group or —Si(R.sup.1) (R.sup.2) (R.sup.3) ; and Y is a single bond, an alkylene group, —O—, —S—, —S(O)—, —SO.sub.2—, —N(R.sup.4)— or a group formed by a combination thereof; provided that X—Y— is a phenyl group, a benzyloxy group, a pyrazol-1-yl group or a group of formula (II) except for a case where m is 3, 6, 8, 9, 10, 11 and 12).
##STR00001##
IDO/TDO Inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:
—(CH.sub.2).sub.n—Y—R.sup.4
wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents
##STR00001##
wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom
##STR00002##
IDO/TDO Inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:
—(CH.sub.2).sub.n—Y—R.sup.4
wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents
##STR00001##
wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom
##STR00002##
HDAC8 inhibitors for treating cancer
Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.