148077-69-4Relevant articles and documents
CAMPTOTHECIN DERIVATIVES WITH A DISULFIDE MOIETY AND A PIPERAZINE MOIETY
-
Page/Page column 31, (2021/01/29)
This invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof (wherein X, Y, Z and n are defined herein). These compounds are useful in the treatment of diseases mediated by topoisomerase I enzyme such as cancers. The prese
Discovery and Structural Optimization of 4-(Aminomethyl)benzamides as Potent Entry Inhibitors of Ebola and Marburg Virus Infections
Gaisina, Irina N.,Peet, Norton P.,Wong, Letitia,Schafer, Adam M.,Cheng, Han,Anantpadma, Manu,Davey, Robert A.,Thatcher, Gregory R. J.,Rong, Lijun
, p. 7211 - 7225 (2020/09/11)
The recent Ebola epidemics in West Africa underscore the great need for effective and practical therapies for future Ebola virus outbreaks. We have discovered a new series of remarkably potent small molecule inhibitors of Ebola virus entry. These 4-(aminomethyl)benzamide-based inhibitors are also effective against Marburg virus. Synthetic routes to these compounds allowed for the preparation of a wide variety of structures, including a conformationally restrained subset of indolines (compounds 41-50). Compounds 20, 23, 32, 33, and 35 are superior inhibitors of Ebola (Mayinga) and Marburg (Angola) infectious viruses. Representative compounds (20, 32, and 35) have shown good metabolic stability in plasma and liver microsomes (rat and human), and 32 did not inhibit CYP3A4 nor CYP2C9. These 4-(aminomethyl)benzamides are suitable for further optimization as inhibitors of filovirus entry, with the potential to be developed as therapeutic agents for the treatment and control of Ebola virus infections.
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents
Zuo, Sai-Jie,Zhang, Sai,Mao, Shuai,Xie, Xiao-Xiao,Xiao, Xue,Xin, Min-Hnag,Xuan, Wei,He, Yuan-Yuan,Cao, Yong-Xiao,Zhang, San-Qi
, p. 179 - 190 (2015/12/31)
In present study, 4-anilinoquinazolines scaffold, arylurea and tertiary amine moiety were combined to design, synthesize gefitinib analogs and discover novel anticancer agents. A series of 4-anilinoquinazoline derivatives (1, 2, 3 and 4) bearing arylurea and tertiary amine moiety at its 6-position were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against A431 cell and A549 cell. The SAR of the title compounds was discussed. The compounds 2d, 2i and 2j with potent antiproliferative activities were evaluated their inhibitory activity against EGFR-TK. Compound 2j displayed potent inhibitory activity against EGFR-TK. In addition, compound 2j, at 50 mg/kg, can completely inhibit cancer growth in established nude mouse A549 xenograft model in vivo. These results suggest that the 4-anilinoquinazoline derivatives bearing diarylurea and tertiary amino moiety at its 6-position can serve as anticancer agents and EGFR inhibitors.
Hydrazinopyrimidines as cysteine protease inhibitors
-
Page/Page column 53-54, (2008/12/04)
Substituted heteroaryl nitrile derivatives of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
Kinase array design, back to front: Biaryl amides
Baldwin, Ian,Bamborough, Paul,Haslam, Claudine G.,Hunjan, Suchete S.,Longstaff, Tim,Mooney, Christopher J.,Patel, Shila,Quinn, Jo,Somers, Don O.
scheme or table, p. 5285 - 5289 (2009/04/10)
New kinase inhibitors can be found by synthesis of targeted arrays of compounds designed using system-based knowledge as well as through screening focused or diverse compounds. Most array strategies aim to add functionality to a fragment that binds in the
PURINES AS CYSTEINE PROTEASE INHIBITORS
-
Page/Page column 49; 50, (2008/12/07)
Substituted heteroaryl nitrile derivatives of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS
-
Page/Page column 21-22, (2008/12/08)
The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula (I) which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.
Identification of a series of highly potent activators of the Nurr1 signaling pathway
Hintermann, Samuel,Chiesi, Michele,von Krosigk, Ulrike,Mathe, Daniele,Felber, Richard,Hengerer, Bastian
, p. 193 - 196 (2007/10/03)
The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e, a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.
AMINOPYRIMIDINE COMPOUNDS AND THEIR SALTS, PROCESS FOR PREPARATION AND PHARMACEUTICAL USE THEREOF
-
Page/Page column 10, (2008/06/13)
The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R1, R2, R3, R4, R5, R6, Q, Z, L, m, n are defined as the description, the methods for preparation thereof, the uses thereof and the pharmaceutical compositions comprising the effective amount of compounds of formula (I). The compounds of formula (I) and their salts can be used as protein kinase inhibitors.
NOVEL CYSTEINE PROTEASE INHIBITORS
-
Page/Page column 57, (2010/11/26)
Substituted heteroaryl nitrile derivatives of Formula (I), processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
