Patent classifications
C07D239/56
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
A Process for the Steroselective Preparation of Chiral 2-[(Hetero)Arylalkylsulfanyl]Pyrimidines and Products Obtainable Therefrom
Described herein is a process for the preparation of a compound of Formula I,
##STR00001##
wherein R.sup.1 and R.sup.2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
A Process for the Steroselective Preparation of Chiral 2-[(Hetero)Arylalkylsulfanyl]Pyrimidines and Products Obtainable Therefrom
Described herein is a process for the preparation of a compound of Formula I,
##STR00001##
wherein R.sup.1 and R.sup.2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
Substituted quinazolines as matrix metalloproteinase-9 hemopexin domain inhibitors
A compound of Formula I: ##STR00001##
wherein: Y is —C(O)NHR.sup.1 or —NHC(O)R.sup.1; R.sup.1 is aryl; ##STR00002## is ##STR00003## optionally substituted with one or more substituents selected from the group consisting of oxo, F, Cl, Br, I, alkyl, NH.sub.2, NHR.sup.4, NHC(O)R.sup.4, NHC(O)OR.sup.4, NR.sup.5R.sup.6, OH, OR.sup.4, SR.sup.4, cycloalkyl and aryl; or ##STR00004## is ##STR00005## optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, I, CN, NO.sub.2, alkyl, C(O)R.sup.4, C(O)NHR.sup.4, C(O)NR.sup.5R.sup.6, C(O)OH, C(O)OR.sup.4, NH.sub.2, NHR.sup.4, NHC(O)OR.sup.4, NR.sup.5R.sup.6, OH, OR.sup.4, SR.sup.4, cycloalkyl and aryl; each R.sup.4 is independently alkyl, cycloalkyl, or aryl; each R.sup.5 is independently alkyl, cycloalkyl, or aryl; each R.sup.6 is independently alkyl, cycloalkyl, or aryl; or each R.sup.5 and R.sup.6, together with the nitrogen atom to which they are attached, independently form an unsubstituted heterocyclic alkyl or unsubstituted heterocyclic aryl; and X is —S— or —O—; and n is 2, 3, or 4.
Substituted quinazolines as matrix metalloproteinase-9 hemopexin domain inhibitors
A compound of Formula I: ##STR00001##
wherein: Y is —C(O)NHR.sup.1 or —NHC(O)R.sup.1; R.sup.1 is aryl; ##STR00002## is ##STR00003## optionally substituted with one or more substituents selected from the group consisting of oxo, F, Cl, Br, I, alkyl, NH.sub.2, NHR.sup.4, NHC(O)R.sup.4, NHC(O)OR.sup.4, NR.sup.5R.sup.6, OH, OR.sup.4, SR.sup.4, cycloalkyl and aryl; or ##STR00004## is ##STR00005## optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, I, CN, NO.sub.2, alkyl, C(O)R.sup.4, C(O)NHR.sup.4, C(O)NR.sup.5R.sup.6, C(O)OH, C(O)OR.sup.4, NH.sub.2, NHR.sup.4, NHC(O)OR.sup.4, NR.sup.5R.sup.6, OH, OR.sup.4, SR.sup.4, cycloalkyl and aryl; each R.sup.4 is independently alkyl, cycloalkyl, or aryl; each R.sup.5 is independently alkyl, cycloalkyl, or aryl; each R.sup.6 is independently alkyl, cycloalkyl, or aryl; or each R.sup.5 and R.sup.6, together with the nitrogen atom to which they are attached, independently form an unsubstituted heterocyclic alkyl or unsubstituted heterocyclic aryl; and X is —S— or —O—; and n is 2, 3, or 4.
Pyrimidine derivative
Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR. Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I): General formula (I): ##STR00001##
wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C.sub.1-C.sub.3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C.sub.1-C.sub.6 alkyl group, etc.; R.sup.1 represents a C.sub.1-C.sub.6 alkyl group, etc.; R.sup.2 represents a C.sub.1-C.sub.6 alkyl group that may have 1 to 3 substituents independently selected from the following group A, or a group selected from the following group B: Group A: a phenyl group and a pyridyl group, wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; Group B: —OH, —O-M, —SH, —S-M, —NH.sub.2, —NH-M, and —N-M.sub.2, wherein M is a C.sub.1-C.sub.6 alkyl group that may have 1 or 2 substituents independently selected from the following group C, or a C.sub.3-C.sub.6 cycloalkyl group that may have 1 or 2 substituents independently selected from the following group C; Group C: a halogen atom, a cyano group, a phenyl group, a pyridyl group, etc., wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; and Group D: a halogen atom, a cyano group, a C.sub.1-C.sub.6 alkyl group, etc.
Electroplating composition and electroplating method
The present invention relates to a electroplating composition and an electroplating method using the same. The electroplating composition of the present invention comprising a first leveling agent and a second leveling agent, wherein the first leveling agent and the second leveling agent each, independently, comprise a compound represented by Chemical Formula 1 below: ##STR00001##
Bromodomain inhibitors
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
Bromodomain inhibitors
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
DACOS Type NNRTIS Amino Acid Ester Derivative, Preparation Method Thereof, Pharmaceutical Composition, and Application Thereof
Disclosed is a DACOs-type NNRTIs amino acid ester derivative, a preparation method thereof, a pharmaceutical composition, and an application thereof. The structure of the DACOs-type NNRTIs amino acid ester derivative is represented by formula (I). The DACOs-type NNRTIs amino acid ester derivative represented by formula (I) can be used as HIV-1 inhibitors and for the preparation of a drug for treating and/or preventing immunodeficiency viruses.
##STR00001##