Category: 16230-24-3

On November 24, 2017, Chen, Wenteng; Liu, Xingyu; Shao, Jiaan; Chen, En; Yu, Yongping published a patent.Application of 16230-24-3 The title of the patent was Preparation of 2-aminooimidazole pyridine derivatives as antitumor agents. And the patent contained the following:

The invention provides 2-aminooimidazole pyridine derivatives and method for preparing them, therfore. Experiments prove that the derivative has obvious proliferation inhibition effect on tumor cells (human epidermal carcinoma cell strain A431 overexpressing wild type EGFR, and Gefitinib-resistant human lung adenocarcinoma cell strain H1975) related with activity of EGFR tyrosine kinase activity at mol. level, particularly has preferable inhibition on drug-resistant cell strain H1975, has weak inhibitory activity on human colon cancer cell strain SW620 low expressing EGFR, and can be applied to prepare corresponding tumor cell-resistant drugs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to aminooimidazole pyridine preparation antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 16230-24-3

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

On December 10, 2015, Xu, Yong; Wang, Xuehai; Li, Li’e; Huang, Lu; Tian, Hua; Yang, Zhongwen; Xia, Qingfeng; Xiao, Qiang; Guo, Diliang; Tu, Ronghua; Yu, Yanping; Yu, Jing; Huang, Xiang; Fan, Zhaoze; He, Zhenyu; Zhang, Yi; Yang, Jing published a patent.Category: amides-buliding-blocks The title of the patent was Purine compounds as kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention provides purine compounds of formula I and their preparing method and application. The inventive compounds can serve as Bruton’s tyrosine kinase (BTK) inhibitors. Compound of formula I wherein X is (un)substituted Ph, (un)substituted 3- to 7-membered saturated or unsaturated carbon ring, (un)substituted 8- to 10-membered saturated or unsaturated bicyclic ring or aryl ring, etc.; R1 is -R, halo, -OR, -O(CH2)aOR, -CN, -NO2, -SO2R, -SO2N(R)2, -SOR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, -NRC(O)NR2, -NRSO2R or -N(R)2; R2 is -R, halo, -OR, -O(CH2)aOR, -CN, -NO2, -SO2R, -SO2N(R)2, -SOR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, -NRC(O)NR2, -NRSO2R or -N(R)2; R is H, (un)substituted C1-6 alkyl, (un)substituted Ph, (un)substituted 4- to 7-membered heterocycle having 1-2 heteroatoms, (un)substituted 5- to 6-membered monocyclic heteroaryl ring including 1-4 heteroatoms, and the heteroatoms are selected from N, O, and S; and their stereoisomers, tautomers, pharmaceutically active metabolites, pharmaceutically acceptable salts, hydrates, solvates, or prodrugs as kinase inhibitors in the treatment of diseases thereof, are claimed. Compound of formula I were prepared via condensation of 2-chloro-9H-purin-6-amine with 4-hydroxypiperidine; the resulting 2-chloro-9-(4-piperidinyl)-9H-purin-6-amine underwent acylation with acryloyl chloride to give to give 2-chloro-6-(acryloylamino)-9-(1-acryloylamino-4-piperidinyl)-9H-purine, which underwent condensation with amines to give I. All the invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that two of the tested compounds exhibited the IC50 value of 0.016 μM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to purine preparation btk kinase inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: amides-buliding-blocks

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

On October 8, 2014, Xu, Yong; Wang, Xuehai; Li, Lie; Huang, Lu; Tian, Hua; Yang, Zhongwen; Xia, Qingfeng; Xiao, Qiang; Guo, Diliang; Tu, Ronghua; Yu, Yanping; Yu, Jing; Huang, Xiang; Fan, Zhaoze; He, Zhenyu; Zhang, Yi; Yang, Jing published a patent.Name: N-(3-Aminophenyl)acrylamide The title of the patent was Purine compounds as kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention provides purine compounds of formula I and their preparing method and application. The inventive compounds can serve as Bruton’s tyrosine kinase (BTK) inhibitors. Compound of formula I wherein X is (un)substituted Ph, (un)substituted 3- to 7-membered saturated or unsaturated carbon ring, (un)substituted 8- to 10-membered saturated or unsaturated bicyclic ring or aryl ring, etc.; R1 is -R, halo, -OR, -O(CH2)aOR, -CN, -NO2, -SO2R, -SO2N(R)2, -SOR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, -NRC(O)NR2, -NRSO2R or -N(R)2; R2 is -R, halo, -OR, -O(CH2)aOR, -CN, -NO2, -SO2R, -SO2N(R)2, -SOR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, -NRC(O)NR2, -NRSO2R or -N(R)2; R is H, (un)substituted C1-6 alkyl, (un)substituted Ph, (un)substituted 4- to 7-membered heterocycle having 1-2 heteroatoms, (un)substituted 5- to 6-membered monocyclic heteroaryl ring including 1-4 heteroatoms, and the heteroatoms are selected from N, O, and S; and their stereoisomers, tautomers, pharmaceutically active metabolites, pharmaceutically acceptable salts, hydrates, solvates, or prodrugs as kinase inhibitors in the treatment of diseases thereof, are claimed. Compound of formula I were prepared via condensation of 2-chloro-9H-purin-6-amine with 4-hydroxypiperidine; the resulting 2-chloro-9-(4-piperidinyl)-9H-purin-6-amine underwent acylation with acryloyl chloride to give to give 2-chloro-6-(acryloylamino)-9-(1-acryloylamino-4-piperidinyl)-9H-purine, which underwent condensation with amines to give I. All the invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that two of the tested compounds exhibited the IC50 value of 0.016 μM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Name: N-(3-Aminophenyl)acrylamide

The Article related to purine preparation btk kinase inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: N-(3-Aminophenyl)acrylamide

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

On June 30, 2017, Zhang, Yinsheng; Gao, Yong; Ren, Jing; Wang, Qinglin; Wang, Zhao published a patent.Related Products of 16230-24-3 The title of the patent was 2,4-Disubstituted pyrimidine compounds as EGFR or/and ALK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to 2,4-disubstituted pyrimidine compounds of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and application thereof in treating diseases induced by EGFR or/and ALK. Compounds of formula I wherein X and Y are independently N and CH; R1 is H, halo, CF3, CN; R2 and R6 are independently H, C1-6 alkoxy; R3 and R5 are independently H, acroylamino; R4 is (un)substituted 3- to 8-membered heterocyclic ring, -Z-(CH2)1-4-NR9R10; R7 is H, C1-6 alkoxy, -Z-(CH2)1-4-NR9R10, (un)substituted piperazinyl; R9 and R10 are independently H and C1-4 alkyl; Z is O, S, NH and derivatives; and their pharmaceutically acceptable salts as EGFR or/and ALK inhibitors in the treatment of diseases thereof, are claimed. Compounds of formula I were prepared by using condensation and reduction as the key steps. All the invention compounds were evaluated for their EGFR or/and ALK inhibitory activity. 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 pyrimidine preparation egfr alk inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 16230-24-3

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

On March 22, 2022, Chen, Yong; Zhuang, Xiaoxiao published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of rociletinib as epidermal cell growth factor receptor mutation inhibitor. And the patent contained the following:

The present invention relates to preparation of rociletinib as epidermal cell growth factor receptor mutation inhibitor. In particular, the preparation method comprises of following steps; (a) substitution reaction between 1-[4-(4-amino-3-methoxyphenyl)piperazin-1-yl]ethan-1-one and di-tert-Bu dicarbonate under the action of a base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)carbamate; (b) substitution reaction of step (a) product and 2,4-dichloro-5-(trifluoromethyl)pyrimidine under the action of a base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)(4-chloro-5-(trifluoromethyl)pyrimidin-2-yl)carbamate; (c) substitution reaction of step (b) product and N-(3-aminophenyl)prop-2-enamide under the action of base and an organic solvent to obtain tert-Bu (4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)(4-((3-acrylamidophenyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)carbamate, and (d) hydrolysis reaction reaction of step (c) product under the action of an acid and an organic solvent to obtain the compound rociletinib. The preparation method of the epidermal cell growth factor receptor mutation inhibitor of the present invention has the advantages that the raw materials required for each step are cheap, easy to purchase, and the synthesis route is short, no isomers are produced, the intermediates are easy to sep. and purify, no column chromatog. is required, and the obtained product has high purity, high atom utilization, high yield, convenient purification, safe and simple reaction, and can be industrially produced. 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 rociletinib preparation epidermal cell growth factor receptor mutation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 16230-24-3

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

On March 30, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application of 16230-24-3 The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 16230-24-3

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

On July 28, 2016, Chen, Yi published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as selective Bruton’s tyrosine kinase inhibitors. And the patent contained the following:

The invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for Bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of Bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On April 9, 2015, Chen, Yi published a patent.Recommanded Product: 16230-24-3 The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as inhibitors of bruton’s tyrosine kinase. And the patent contained the following:

The present invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 16230-24-3

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

On April 5, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides EGFR kinase inhibitor and its preparation method and application.Specifically, the invention provides a compound shown in formula (I), wherein the definition of each group is as noted in the instruction book.Described compound is the effective EGFR inhibitor. The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. 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 trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

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

On January 31, 2020, Rodriguez, Frederic; Saffon, Nathalie; Sammartino, Jose Camilla; Degiacomi, Giulia; Pasca, Maria Rosalia; Lherbet, Christian published an article.Safety of N-(3-Aminophenyl)acrylamide The title of the article was First triclosan-based macrocyclic inhibitors of InhA enzyme. And the article contained the following:

Two macrocyclic derivatives based on the triclosan frame were designed and synthesized as inhibitors of Mycobacterium tuberculosis InhA enzyme. One of the two mols. M02 displayed promising inhibitory activity against InhA enzyme with an IC50 of 4.7μM. Mol. docking studies of these two compounds were performed and confirmed that M02 was more efficient as inhibitor of InhA activity. These mols. are the first macrocyclic direct inhibitors of InhA enzyme able to bind into the substrate pocket. Furthermore, these biaryl ether compounds exhibited antitubercular activities comparable to that of triclosan against M. tuberculosis H37Rv strain. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to preparation triclosan derivative macrocyclic inhibitor inha enzyme tuberculosis, enoyl-acp-reductase, inha, macrocycle, marchantin analogue, mycobacterium tuberculosis, triclosan and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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