Category: 16230-24-3

On April 5, 2017, Zhang, Yinsheng; Gao, Yong; Wang, Qinglin; Wang, Zhao published a patent.Application of 16230-24-3 The title of the patent was Preparation of deuterated diphenylamino pyrimidine compounds for treating cancer. And the patent contained the following:

The title compound I [wherein R1-R7 and R10-R26 = independently H or D; with the proviso that at least one of them is D; R8 = trifluoromethyl; R9 = H; with exclusions] or pharmaceutically acceptable salts thereof were prepared for treating EGFR related disease, such as cancer. For example, II was prepared in a multi-step synthesis. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to preparation deuteration diphenylaminopyrimidine treatment proliferation human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 7, 2016, Chen, Wei; Yan, Shunqi; Loury, David J.; Frye, Leah Lynn; Greenwood, Jeremy Robert; Shelley, Mee Yoo; Wang, Longcheng published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Inhibitors of bruton’s tyrosine kinase. And the patent contained the following:

Disclosed herein are compounds that form covalent bonds with Bruton’s tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

The Article related to purine preparation bruton tyrosine kinase inhibitor autoimmune disease cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 27, 2017, Zhao, Dan; Huang, Shanshan; Qu, Menghua; Wang, Changyuan; Liu, Zhihao; Li, Zhen; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong; Shu, Xiaohong published an article.Category: amides-buliding-blocks The title of the article was Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. And the article contained the following:

A new series of diphenylpyrimidine derivatives (DPPYs) bearing various aniline side chains at the C-2 position of pyrimidine core were synthesized as potent BTK inhibitors. Most of these inhibitors displayed improved activity against B leukemia cell lines compared with lead compound spebrutinib. Subsequent studies showed that the peculiar inhibitor I, with IC50 values of 10.5 μM against Ramos cells and 19.1 μM against Raji cells, also displayed slightly higher inhibitory ability than the novel agent ibrutinib. Moreover, compound I is not sensitive to normal cells PBMC, indicating low cell cytotoxicity. In addition, flow cytometry anal. indicated that I significantly induced the apoptosis of Ramos cells, and arrested the cell cycle at the G0/G1 phase. These explorations provided new clues to discover pyrimidine scaffold as more effective BTK inhibitors. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to diphenylpyrimidine preparation bruton tyrosine kinase inhibitory activity, btk, inhibitor, leukemia, pyrimidine, synthesis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 24, 2022, Zhao, Hong-Yi; Wang, Hai-Peng; Mao, Yu-Ze; Zhang, Hao; Xin, Minhang; Xi, Xiao-Xiao; Lei, Hao; Mao, Shuai; Li, Dong-Hui; Zhang, San-Qi published an article.SDS of cas: 16230-24-3 The title of the article was Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. And the article contained the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).SDS of cas: 16230-24-3

The Article related to pyrimidine preparation antitumor egfr inhibition sar mol docking, purine preparation antitumor egfr inhibition sar mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 27, 2018, Cho, Seong Yun; Kim, Pil Ho; Lee, Jeong Ok; Kim, Hyeong Rae; Ha, Jae Du; Jung, Hui Jeong; Yoon, Chang Su; Park, Ji Hun; Hwang, Jong Yeon published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Fused pyrimidine derivative as Bruton’s tyrosine kinase inhibitor, and method for the preparation thereof. And the patent contained the following:

Disclosed are compound I [n = 0 or 1; A = single bond, -NH- or -O-; D1 = CR4 or N; R4 = H or alkyl; D2 = CH or N; D3 = N or NH; a dotted line accompanied by a solid line represents a single bond or a double bond; R1 = (un)substituted aryl; R2, R3 = independently H, (un)substituted aryl, (un)substituted cycloalkyl, etc.; or its optical isomer or pharmaceutically acceptable salt] and pharmaceutical compositions For example, compound II was prepared from malononitrile via conversion to 4,6-dichloro-3-methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine followed by treatment with K2CO3/N-(1s,4s)-(4-aminocyclohexyl)acrylamide and Pd2(dba)3-catalyzed reaction with 4-morpholinoaniline. The invention compound showed high inhibitory activity for Bruton’s tyrosine kinase (BTK), e.g., IC50 value of II was 0.001 μM. Compound I is claimed useful for the treatment of cancer or autoimmune disease. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

The Article related to fused pyrimidine preparation bruton tyrosine kinase inhibitor, cancer autoimmune disease treatment fused pyrimidine btk inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 1, 2021, Wang, Zhengjie; Liu, Limin; Dai, Honglin; Si, Xiaojie; Zhang, Luye; Li, Erdong; Yang, Zhang; Chao, Gao; Zheng, Jiaxin; Ke, Yu; Shan, Lihong; Zhang, Qiurong; Liu, Hongmin published an article.Related Products of 16230-24-3 The title of the article was Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway. And the article contained the following:

In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound I had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound I also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound I exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound I could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound I targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Mol. docking showed that compound I could bind into the active pocket of EGFR. Those work suggested that compound I would have remarkable implications for further design of anti-tumor agents. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Related Products of 16230-24-3

The Article related to quinazoline preparation antiproliferation antitumor mol docking apoptosis egfr, antiproliferation, cell cycle analysis, egfr, quinazoline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 16, 2017, Song, Zhendong; Huang, Shanshan; Yu, Haiqing; Jiang, Yu; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Sun, Hunjun; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Category: amides-buliding-blocks The title of the article was Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). And the article contained the following:

Potential new EGFRT790M inhibitors comprising of structurally modified diphenylpyrimidine derivatives bearing a morpholine functionality (Mor-DPPYs), e.g., I were synthesized and used to improve the activity and selectivity of gefitinib-resistant non-small cell lung cancer (NSCLC) treatment. This led to the identification of inhibitor I, which displayed high activity against EGFRT790M/L858R kinase (IC50 = 0.71 nM) and repressed H1975 cell replication harboring EGFRT790M mutations at a concentration of 0.037 μM. Inhibitor I demonstrated high selectivity (SI = 631.9) for T790M-containing EGFR mutants over wild type EGFR and suggested that it will cause few side effects. Moreover, this compound also shows promising antitumor efficacy in a murine EGFRT790M/L858R-driven H1975 xenograft model without affecting body weight This study provides new potential lead compounds for further development of anti-NSCLC drugs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to acrylamide diphenylaminopyrimidinyl morpholino preparation antitumor egfr kinase mol modeling, egfr t790m, inhibitors, nsclc, pyrimidine, resistance, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On October 16, 2018, Shu, Xiaohong; Chi, Fuyun; Yang, Song; Ma, Xiaodong; Li, Chuangang; Li, Hong; Wu, Moli; Zhen, Yuhong; Diao, Yunpeng; Song, Danyang; Li, Hui; Jin, Junmei published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Thiopyrimidine heterocyclic antitumor compound and preparation method and its use. And the patent contained the following:

A thiopyrimidine heterocyclic antitumor compound for the treatment of small cell lung cancer, non-small cell lung cancer, EGFR-T790M mutant non-small cell lung cancer is provided. The compound is represented by the formula I, or a pharmaceutically acceptable salt thereof, which inhibits wild-type EGFR, mutant EGFR-T790M epidermal factor receptor protein tyrosine kinase, where X is O or NH; M is S(O)n; n is 0 or 1; R is alkyl-morpholine. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).HPLC of Formula: 16230-24-3

The Article related to thiopyrimidine heterocyclic antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.HPLC of Formula: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On September 25, 2014, Alexander, Matthew David; McDonald, Joseph John; Ni, Yike; Niu, Deqiang; Petter, Russell C.; Qiao, Lixin; Singh, Juswinder; Wang, Tao; Zhu, Zhendong published a patent.Recommanded Product: N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of heteroaryl compounds as Mk2 kinase inhibitors. And the patent contained the following:

The title compound with general formula I [wherein Ring A = optionally substituted group selected from a 3-8 membered carbocyclic ring, a 4-7 membered heterocylic ring, a 5-6 membered monocyclic heteroaryl ring, a 7-10 membered bicyclic aryl ring, etc.; Y = CR’ or N, where each R’ is independently hydrogen, halo, an optionally substituted Ph, a 3-8 membered carbocyclic ring, etc.; R1 = a warhead group; q = 0-6; R2 = independently halogen, -OH, -SH, -CN, etc.; R3 and R4 = independently optionally substituted Ph, a 3-8 membered carbocyclic ring, a 4-7 membered heterocylic ring, etc.; R5 = independently hydrogen or an optionally substituted C1-6 aliphatic group; T = a covalent bond, -O-, -S-, -C(O)-, etc.] or pharmaceutically acceptable salts thereof were prepared as Mk2 kinase inhibitors. For example, compound II was prepared in a multi-step synthesis. The title compounds can be used for the treatment of autoimmune disorder, chronic or acute inflammatory disorder, auto-inflammatory disorder, neoplasia, cardiovascular, or cerebrovascular disease. (pharmaceutical assay data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: N-(3-Aminophenyl)acrylamide

The Article related to preparation heteroaryl compound mk2 kinase inhibitor human, treatment neoplasia autoimmune chronic acute inflammatory cardiovascular cerebrovascular disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Recommanded Product: N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 15, 1999, Park, Kyung Jae; Oh, In Hwan; Mun, Jae Jun; Jung, Shin Hae published a patent.Formula: C9H10N2O The title of the patent was Method for the preparation of polymeric pigment. And the patent contained the following:

A process for preparing an acrylic based polymer pigment polymerized with a pigment itself by polymerizing an acrylic/azo based pigment monomer with a vinyl monomer is provided, which has excellent coloring property and workability for general plastic and engineering plastic as substantial matrix resin. This process comprises the steps of: preparing raw material for synthesizing 3-nitroacrylanilide by using 3-nitroaniline and acryloyl chloride in acetone as a solvent and sodium hydroxide as a catalyst; reducing 3-nitroacrylanilide using iron/hydrochloric acid in 50% methanol as a solvent; preparing an acrylic/azo based color monomer by reacting 3-aminoacrylanilide with sodium nitrate and coupling with a coupler; and polymerizing the acrylic/azo based color monomer and Me methacrylate. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to acrylic azo polymer pigment preparation, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Other Dyes and Pigments and other aspects.Formula: C9H10N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics