Patent classifications
C07D475/00
Immune system modulators
The present invention relates to a compound of Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Immune system modulators
The present invention relates to a compound of Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Compounds as modulators of RORγ
The present invention encompasses compounds of the formula (I) ##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
Compounds as modulators of RORγ
The present invention encompasses compounds of the formula (I) ##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
Method for Preparing Volasertib and Intermediate thereof
Disclosed is a method for preparing Volasertib (I), comprising the following steps: an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) is nucleophilically substituted with an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenzamide (III), so as to prepare Volasertib (I). The preparation method has a simple process, mild conditions and few side effects, which meets the requirements for industrial enlargement. In addition, also disclosed are an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenza-mide (III) of Volasertib and the preparation methods thereof.
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
Substituted quinoxalines and benzo[c][1,2,5]oxadiazoles as DNA-PK inhibitors
Provided are compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.
Substituted quinoxalines and benzo[c][1,2,5]oxadiazoles as DNA-PK inhibitors
Provided are compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.
COMPOUNDS AS MODULATORS OF ROR GAMMA
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
COMPOUNDS AS MODULATORS OF ROR GAMMA
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.