Tag: 100-200

On January 15, 2015, Hu, Shaojing; Liu, Xiangyong; Bai, Jinlong; Long, Wei published a patent.COA of Formula: C9H10N2O The title of the patent was Preparation of pyrimidines as protein tyrosine kinase modulators. And the patent contained the following:

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. Compounds I [X = absent, O, S, or NR16; R16 = H or alkyl; Y = halogen, OH, NH2, CN, N3, NO2, or (un)substituted alkyl; Z = O, S, NR20, or CR20R21; and each R20 or R21 independently = H, halogen, (un)substituted alkyl, or alkoxy; R1 = hydroxy, alkyl, haloalkyl, aryl, arylalkyl, etc.; R2 = H, F, or alkyl; or R3 = H, halogen, or a 5 or 6 member heterocyclic ring; R4 = H, alkoxy, alkenyloxy, cycloalkyloxy, halogen, etc.; R5 = H, F, alkyl, haloalkyl, alkoxy, etc.; R6 = H, halo, CN, NO2, cycloalkyl, etc.; R7 = H, halo, alkyl, alkoxy, alkenyloxy, etc.], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by. Compound II showed IC50 value of 27.9 nM in ALK assay, 44.3 nM in EGFR (ErB1) L858R assay and 4.08 nM in EGFR (ErbB1) T790M L858R assay. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to pyrimidine preparation protein tyrosine kinase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C9H10N2O

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

On April 19, 2017, Ma, Xiaodong; Song, Anran; Wang, Luhong; Liu, He; Zhang, Baojing; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Zhen, Yuhong; Liu, Kexin published a patent.Category: amides-buliding-blocks The title of the patent was Preparation of distyryl pyrimidine derivatives as antitumor agents. And the patent contained the following:

Title compounds I [wherein X = NH or O; R1 = Cl, F, CF3, or NO2; R2 = H, Me, OMe, or CN; R3 = (R4)n, n is 1 to 4, R4 is H, Me, OMe, OH, F, Cl, or Br], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors useful as antitumor agents. Thus, the invention compound II was prepared and gave an EGFR inhibition IC50 value of 51.34nmmol. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to distyryl pyrimidine antitumor egfr preparation, 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 May 16, 2018, Na, Yun Su; Bang, Geuk Chan; Park, Jun Seok published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of novel pyrrolopyrimidine derivatives as BTK inhibitors and pharmaceutical composition comprising the same. And the patent contained the following:

The invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, and the compound according to the invention can be usefully used for the prevention or treatment of diseases in which the BTK inhibitory action is beneficial. Compounds of formula I wherein X is NH and O; L is a bod and CO; R is H, (un)substituted C6-10 aryl and (un)substituted C3-10 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 20.9 n< and 100 % inhibition at 1 μM. 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 pyrrolopyrimidine preparation btk inhibitor, 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

A. K., Ajeesh Kumar; Bodke, Yadav D.; Gowda, Ashwath N.; Sambasivam, Ganesh; Bhat, Kishore G. published an article in 2017, the title of the article was Design, Synthesis, and Evaluation of the Anticancer Properties of a Novel Series of Imidazolone Fused Pyrazolo[1,5-a]pyrimidine Derivatives.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

A novel series of imidazolone fused pyrazolo[1,5-a]pyrimidine derivatives has been designed and synthesized using a convergent approach, and the structures of these compounds were confirmed by 1H NMR, 13C NMR, ESI-MS, and IR analyses. These new compounds were tested for their in vitro antiproliferative activity using an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Out of the 20 derivatives prepared in the current study, some compounds exhibited good anticancer activities tested against HeLa cells and HepG2 cells. However, the in vitro anticancer activity of compound I against HeLa, HepG2, and MCF-7 cell lines is superior to the marketed drugs Paclitaxel and SAHA. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Name: 2-(4-Methylbenzamido)acetic acid

The Article related to imidazolone fused pyrazolopyrimidine preparation anticancer activity, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-(4-Methylbenzamido)acetic acid

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

On March 31, 2019, Spranitz, Peter; Soregi, Petra; Botlik, Bence Bela; Berta, Mate; Soos, Tibor published an article.Name: N,N-Diethylacetamide The title of the article was Organocatalytic Desymmetrisation of Fittig’s Lactones: Deuterium as a Reporter Tag for Hidden Racemisation. And the article contained the following:

Highly enantioselective desymmetrisation of Fittig’s lactones with alcs. was promoted by bifunctional cinchona squaramides to yield corresponding glutaric acid derivatives I [R = Me, cyclohexyl, Ph, etc.]. The reactions were carried out with monodeuterated methanol to detect possible hidden racemization of the stereogenic center. Current evidence suggested that racemization was not a relevant process for most substrates, partial erosion of enantioselectivity was only detected with ortho-substituted aryl derivates. The resultant glutaric acid derivatives possess a scaffold that was common in natural products and the compounds were also useful chiral building blocks for further synthetic endeavours. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Name: N,N-Diethylacetamide

The Article related to glutaric acid derivative enantioselective preparation, bicyclic fittig lactone organocatalytic desymmetrisation, Aliphatic Compounds: Esters, Linear Anhydrides, Acyl Peroxides, and Acyl Halides and other aspects.Name: N,N-Diethylacetamide

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

On December 3, 2021, Wu, Xiaoyun; Li, Qinlan; Guo, Qian; Wan, Shanhe; Li, Zhonghuang; Zhang, Jiajie published a patent.Formula: C9H10N2O The title of the patent was Preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. And the patent contained the following:

The present invention relates to the preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. In particular, the dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative I (wherein, L contains at least one of an alkyl group, a carbonyl group, an ether bond or an amine group) were prepared The inventive compound can be used as an EFGR inhibitor, has strong inhibitory activity against the cell line H1975 with high expression of EGFRL858R/T790M, and can effectively inhibit the growth of lung cancer cells, which can be used for preparing drugs for treating, preventing, delaying, assisting in treating or treating diseases related to EGFR activity and drugs for treating tumor diseases. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to dioxopiperidinyl isoindolyl alkylamidophenylamino piperazinyl oxopentaneamide preparation efgr inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C9H10N2O

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

On March 5, 2020, Krainc, Dimitri; Silverman, Richard B.; Zheng, Jianbin published a patent.SDS of cas: 16230-24-3 The title of the patent was Preparation of pyrrolopyrimidine compounds and uses thereof for modulating glucocerebrosidase activity. And the patent contained the following:

The invention relates to preparation of new small mols. having a pyrrolopyrimidine (I) core structure and the uses thereof for modulating glucocerebrosidase activity. Compounds I wherein m is o-6; R1 is aryl, heteroaryl, etc.; R2 is C1-6 alkyl or pyridinyl, are claimed. The example compound II was prepared via 3-step synthesis (procedure given). Also disclosed are pharmaceutical compositions comprising the small mols. which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurol. diseases and disorders such as Gaucher’s disease and Parkinson’s disease. Compounds I may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase can be administered in enzyme replacement therapy and/or utilized in screening assays for new small mols. that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase. 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 pyrrolopyrimidine preparation glucocerebrosidase modulator neurodegenerative metabolic disease treatment, 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 April 13, 2016, Yao, Li published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of pyrimidine derivatives as EGFR and ALK kinase inhibitors for treatment of cancer. And the patent contained the following:

The present invention discloses compounds represented by formula I [wherein R1 and R2 are selected from H, halogen, cyano, etc.; R3 is selected from H, halogen, substituted or unsubstituted C1-C6 alkyl and C3-C8 cycloalkyl; R are independently selected from H, halo, CN, OH, NH2, etc.; X and Y are independently selected from CH, C-halo, C-CN, N, etc. with the proviso that at least one of X and Y is N; and so on] or their pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs, and preparation method and pharmaceutical application thereof. For example, compound II was prepared in a multi-step synthesis. The compounds of the present invention have good kinase inhibitory activity, particularly on EGFR and ALK kinases and mutants thereof, and have good prospect in medicine for the treatment of cancer. (assay data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide

The Article related to preparation pyrimidine derivative human egfr alk kinase inhibitors, treatment cancer antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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

Chandraprakash, B.; Sarangapani, M. published an article in 2021, the title of the article was Synthesis, characterization, anticancer and antibacterial activity of 4-(benzylidene)-1-(pyrimidin-2-amino)-2-(p-tolyl)-1, 4-dihydro-4H-imidazol-5-one.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

In present study, conventional synthesis of 4-(benzylidene)-1-(pyrimidin-2-amino)-2-(p-tolyl)-1, 4-dihydro-4H-imidazol-5-ones I [R = H, Me, Cl, etc.; R1 = H, MeO, NO2] was performed. All the synthesized products I were purified through column chromatog. and structures of these compounds were characterized by IR, 1H NMR and mass spectral data. All the final compounds I were screened for their anticancer and antibacterial activity and their efficacy were matched with standard drugs. The synthesized compounds I [R = Me, NO2, MeO, Br; R1 = H, MeO] showed good anticancer activities whereas others exhibited significant activities. The compounds I [R = Cl, MeO, NO2; R1 = H, MeO] has showed maximum antibacterial activity compare with streptomycin as a standard drug. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Name: 2-(4-Methylbenzamido)acetic acid

The Article related to benzylidene pyrimidinyl amino tolyl dihydroimidazolone preparation antibacterial antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-(4-Methylbenzamido)acetic acid

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

On May 21, 2019, Li, Jiarui; Xu, Ruyi; Cao, Qinyuan published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Anti-tumor compound, and its preparation method and application in preparing drug for treating myelocytic leukemia. And the patent contained the following:

The invention relates to N-(3-((5-chloro-2-((4-((4-hydroxypiperidin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide I (named as BY4009) and its pharmaceutically acceptable salts (sulfate, pyrosulfate, etc.). Compound I was prepared starting from 1-(bromomethyl)-4-nitrobenzene, 4-hydroxypiperidine, and 3-nitroaniline by using benzylation, reduction, amidation and amination as the key steps. A pharmaceutical composition comprises the anti-tumor compound or its pharmaceutically acceptable salt, and pharmaceutically acceptable carrier. The pharmaceutical composition has application in preparing drug for treating tumor (myelocytic leukemia) by inhibiting BTK Tyrosine kinase phosphorylation. The anti-tumor compound has new mechanism of action, and is more effective. 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 piperidinyl pyrimidinyl phenyl acrylamide preparation btk treatment myelocytic leukemia, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 16230-24-3

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