64362-41-0Relevant academic research and scientific papers
TRIAZINE DERIVATIVE HAVING EGFR INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
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Page/Page column 33, (2022/02/24)
Disclosed are a triazine derivative having EGFR inhibitory activity, a preparation method therefor and use thereof. In particular, disclosed are an EGFR inhibitor having a structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, use thereof for preparing the EGFR inhibitor, and use thereof in preparing medicaments for treating and/or preventing cancers, tumors or metastatic diseases at least partially related to insertion, deletion or other mutation of EGFR exon 20, and in particular use thereof in preparing medicaments for treating and/or preventing hyperproliferative diseases and diseases inducing cell death disorders. The definition of each substituent of formula (I) is the same as that in the description.
NOVEL COMPOUNDS USEFUL AS POLY(ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
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Paragraph 223, (2021/11/06)
The present invention provides novel poly(ADP-ribose) polymerase (PARP) inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods for the treatment, prevention and/or amelioration of PARP mediated diseases or disorders using them. In particular, the compounds described herein are useful for the treatment of carcinoma of the breast, ovarian cancer, carcinoma of the liver, carcinoma of the lung, small cell lung cancer, esophageal cancer, gall bladder cancer, pancreatic cancer and stomach cancer.
NEW PROPANAMINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS
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Page/Page column 66; 67, (2019/02/13)
The present invention relates to new compounds of general formula (I) that show dual activity towards α2δ subunit of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit, and to the noradrenaline transporter (NET). The invention is also rel
PHARMACEUTICAL COMPOUNDS
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Paragraph 0734; 0735; 0736, (2018/04/26)
This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated
SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE
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Page/Page column 286, (2017/08/01)
The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R2, R3, R10, E1, E2, E3, Y, and Z are as defined herein.
AZAINDOLE COMPOUNDS AS MODULATORS OF RORC
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Page/Page column 43; 44, (2015/02/25)
The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
Lead optimization of 1,4-azaindoles as antimycobacterial agents
Shirude, Pravin S.,Shandil, Radha K.,Manjunatha,Sadler, Claire,Panda, Manoranjan,Panduga, Vijender,Reddy, Jitendar,Saralaya, Ramanatha,Nanduri, Robert,Ambady, Anisha,Ravishankar, Sudha,Sambandamurthy, Vasan K.,Humnabadkar, Vaishali,Jena, Lalit K.,Suresh, Rudrapatna S.,Srivastava, Abhishek,Prabhakar,Whiteaker, James,McLaughlin, Robert E.,Sharma, Sreevalli,Cooper, Christopher B.,Mdluli, Khisi,Butler, Scott,Iyer, Pravin S.,Narayanan, Shridhar,Chatterji, Monalisa
, p. 5728 - 5737 (2014/08/05)
In a previous report, we described the discovery of 1,4-azaindoles, a chemical series with excellent in vitro and in vivo antimycobacterial potency through noncovalent inhibition of decaprenylphosphoryl-β-d-ribose-2′- epimerase (DprE1). Nevertheless, high mouse metabolic turnover and phosphodiesterase 6 (PDE6) off-target activity limited its advancement. Herein, we report lead optimization of this series, culminating in potent, metabolically stable compounds that have a robust pharmacokinetic profile without any PDE6 liability. Furthermore, we demonstrate efficacy for 1,4-azaindoles in a rat chronic TB infection model. We believe that compounds from the 1,4-azaindole series are suitable for in vivo combination and safety studies.
Azaindoles: Noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo
Shirude, Pravin S.,Shandil, Radha,Sadler, Claire,Naik, Maruti,Hosagrahara, Vinayak,Hameed, Shahul,Shinde, Vikas,Bathula, Chandramohan,Humnabadkar, Vaishali,Kumar, Naveen,Reddy, Jitendar,Panduga, Vijender,Sharma, Sreevalli,Ambady, Anisha,Hegde, Naina,Whiteaker, James,McLaughlin, Robert E.,Gardner, Humphrey,Madhavapeddi, Prashanti,Ramachandran, Vasanthi,Kaur, Parvinder,Narayan, Ashwini,Guptha, Supreeth,Awasthy, Disha,Narayan, Chandan,Mahadevaswamy, Jyothi,Vishwas,Ahuja, Vijaykamal,Srivastava, Abhishek,Prabhakar, Kr,Bharath, Sowmya,Kale, Ramesh,Ramaiah, Manjunatha,Choudhury, Nilanjana Roy,Sambandamurthy, Vasan K.,Solapure, Suresh,Iyer, Pravin S.,Narayanan, Shridhar,Chatterji, Monalisa
supporting information, p. 9701 - 9708 (2014/01/06)
We report 1,4-azaindoles as a new inhibitor class that kills Mycobacterium tuberculosis in vitro and demonstrates efficacy in mouse tuberculosis models. The series emerged from scaffold morphing efforts and was demonstrated to noncovalently inhibit decaprenylphosphoryl-β-D-ribose2′-epimerase (DprE1). With "drug-like" properties and no expectation of pre-existing resistance in the clinic, this chemical class has the potential to be developed as a therapy for drug-sensitive and drug-resistant tuberculosis.
Discovery and bioactivity of 4-(2-arylpyrido[3′,2′:3,4] pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors
Wang, Jia,Wang, Xiang,Chen, Yanhong,Chen, Simeng,Chen, Guang,Tong, Linjiang,Meng, Linghua,Xie, Yuyuan,Ding, Jian,Yang, Chunhao
scheme or table, p. 339 - 342 (2012/03/11)
PI3K is a promising therapeutic target for cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3′,2′:3,4] pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had the IC50 against PI3Kα comparable with PI-103. All of the compounds showed selectivity over 15 tested protein kinases and anti-proliferative activity at micromolar concentration against several cancer cell lines.
GSK-3BETA INHIBITOR
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Page/Page column 32, (2011/04/13)
For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA): wherein each symbol is as defined in the specification. or a salt thereof or a prodrug thereof.
