Patent classifications
C07D487/10
NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
##STR00001##
KRas G12C inhibitors
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
IMIDAZOLE DERIVATIVE USED AS ANTIVIRAL AGENT AND USE THEREOF IN PREPARATION OF MEDICAMENT
Disclosed are an antiviral compound and a use thereof in the preparation of a medicament for the treatment of virus infections. Specifically, the present invention relates an imidazole derivative for treating respiratory syncytial virus infection.
IMIDAZOLE DERIVATIVE USED AS ANTIVIRAL AGENT AND USE THEREOF IN PREPARATION OF MEDICAMENT
Disclosed are an antiviral compound and a use thereof in the preparation of a medicament for the treatment of virus infections. Specifically, the present invention relates an imidazole derivative for treating respiratory syncytial virus infection.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
##STR00001##
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
##STR00001##
Immunomodulator compounds
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Immunomodulator compounds
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
5-alkylquinazoline derivative, method of preparing the same, and method of using the same
A 5-methoxyquinazoline derivative compound I, having a structure represented by formula I: ##STR00001## A 5-methylquinazoline derivative compound II, having a structure represented by formula II ##STR00002## A method for preparing crystals of a 5-methoxyquinazoline derivative compound I and a 5-methylquinazoline derivative compound I, includes: adding 0.8847 g of 5-methoxyisatin, 0.8256 g of 5-methylisatin, 2.6963 g of ammonium formate, and 100 mL of anhydrous methanol in a 250 mL round-bottomed flask; heating and stirring a resulting mixture for refluxing for 48 hrs, stopping reaction, and performing rotary filtration and obtaining a crude filter residue; and performing column chromatography on the crude filter residue using dichloromethane and anhydrous methanol at a volume ratio of 1:1, and respectively obtaining the crystal of 5-methoxyquinazoline derivative compound I and the crystal of 5-methylquinazoline derivative compound II.
5-alkylquinazoline derivative, method of preparing the same, and method of using the same
A 5-methoxyquinazoline derivative compound I, having a structure represented by formula I: ##STR00001## A 5-methylquinazoline derivative compound II, having a structure represented by formula II ##STR00002## A method for preparing crystals of a 5-methoxyquinazoline derivative compound I and a 5-methylquinazoline derivative compound I, includes: adding 0.8847 g of 5-methoxyisatin, 0.8256 g of 5-methylisatin, 2.6963 g of ammonium formate, and 100 mL of anhydrous methanol in a 250 mL round-bottomed flask; heating and stirring a resulting mixture for refluxing for 48 hrs, stopping reaction, and performing rotary filtration and obtaining a crude filter residue; and performing column chromatography on the crude filter residue using dichloromethane and anhydrous methanol at a volume ratio of 1:1, and respectively obtaining the crystal of 5-methoxyquinazoline derivative compound I and the crystal of 5-methylquinazoline derivative compound II.