500789-41-3Relevant academic research and scientific papers
CYANO-SUBTITUTED HETEROCYCLES WITH ACTIVITY AS INHIBITORS OF USP30
-
Page/Page column 47, (2018/04/17)
The present invention relates to a class of cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction. (I)
SPIROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
-
Page/Page column 234, (2017/12/01)
This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
JAK INHIBITOR
-
Paragraph 0231; 0232; 0233, (2017/12/15)
The present invention discloses a series of JAK inhibitors, and particularly discloses a compound of formula (I) or a pharmaceutically acceptable salt thereof and the use thereof in preparation of drugs for treating diseases related to JAK.
IMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
-
Page/Page column 175, (2014/02/15)
A series of imidazo[l,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Discovery of novel tricyclic compounds as squalene synthase inhibitors
Ichikawa, Masanori,Ohtsuka, Masami,Ohki, Hitoshi,Haginoya, Noriyasu,Itoh, Masao,Sugita, Kazuyuki,Usui, Hiroyuki,Suzuki, Makoto,Terayama, Koji,Kanda, Akira
experimental part, p. 3072 - 3093 (2012/06/30)
In the present article, we have reported the design, synthesis, and identification of highly potent benzhydrol derivatives as squalene synthase inhibitors (compound 1). Unfortunately, the in vivo efficacies of the compounds were not enough for acquiring the clinical candidate. We continued our investigation to obtain a more in vivo efficacious template than the benzhydrol template. In our effort, we focused on a benzoxazepine ring and designed a new tricyclic scaffold by the incorporation of heterocycle into it. Prepared pyrrolobenzoxazepine derivatives showed further efficient in vitro and in vivo activities.
N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
-
Page/Page column 153-154, (2012/08/08)
The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 196, (2012/08/08)
The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
MK2 INHIBITORS
-
Page/Page column 53-54, (2011/07/07)
The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone re
PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
-
Page/Page column 77, (2011/04/14)
The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
HETEROARYL COMPOUNDS AS KINASE INHIBITORS
-
Page/Page column 78, (2011/04/14)
The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor
