Category: 16230-24-3

On October 13, 2016, Ferguson, Fleur M.; Ni, Jing; Zhang, Tinghu; Tesar, Bethany; Sim, Taebo; Kim, Nam Doo; Deng, Xianming; Brown, Jennifer R.; Zhao, Jean J.; Gray, Nathanael S. published an article.COA of Formula: C9H10N2O The title of the article was Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors. And the article contained the following:

Dual inhibition of PI3K-δ and PI3K-γ is an established therapeutic strategy for treatment of hematol. malignancies. Reported mols. targeting PI3K-δ/γ selectively are chem. similar and based upon isoquinolin-1(2H)-one or quinazolin-4(3H)-one scaffolds. Here we report a chem. distinct series of potent, selective PI3K-δ/γ inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold with comparable biochem. potency and cellular effects on PI3K signaling. We envisage these mols. will provide useful leads for development of next-generation PI3K-δ/γ targeting therapeutics. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to pi3k delta gamma inhibitor benzopyrimidodiazepinone preparation structure activity kinome, pi3k-γ, pi3k-δ, kinase inhibitor, p110-γ, p110-δ, phosphatidylinositol-4,5-bisphosphate 3-kinase-delta and other aspects.COA of Formula: C9H10N2O

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

On July 28, 2017, Liu, He; Qu, Menghua; Xu, Lina; Han, Xu; Wang, Changyuan; Shu, Xiaohong; Yao, Jihong; Liu, Kexin; Peng, Jinyong; Li, Yanxia; Ma, Xiaodong published an article.Product Details of 16230-24-3 The title of the article was Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. And the article contained the following:

A new series of diphenylpyrimidine derivatives (SFA-DPPYs) were synthesized by introducing a functional sulfonamide into the C-2 aniline moiety of pyrimidine template, and then were biol. evaluated as potent Bruton’s tyrosine kinase (BTK) inhibitors. Among these mols., inhibitors 10c, 10i, 10j and 10k (I – IV, resp.) displayed high potency against the BTK enzyme, with IC50 values of 1.18 nM, 0.92 nM, 0.42 nM and 1.05 nM, resp. In particular, compound 10c could remarkably inhibit the proliferation of the B lymphoma cell lines at concentrations of 6.49 μM (Ramos cells) and 13.2 μM (Raji cells), and was stronger than the novel agent spebrutinib. In addition, the inhibitory potency toward the normal PBMC cells showed that inhibitor 10c possesses low cell cytotoxicity. All these explorations indicated that mol. 10c could serve as a valuable inhibitor for B-cell lymphoblastic leukemia treatment. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Product Details of 16230-24-3

The Article related to sulfonamide phenylpyrimidine bruton tyrosine kinase inhibitor lymphoblastic leukemia, b cell lymphoblastic leukemia sulfonamide phenylpyrimidine, btk, inhibitor, leukemia, pyrimidine, sulfonamide and other aspects.Product Details of 16230-24-3

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

On April 15, 2016, Huang, Zhenhua; Zhang, Qian; Yan, Lianzhong; Zhong, Guizhen; Zhang, Linqi; Tan, Xiaojuan; Wang, Yanli published an article.Electric Literature of 16230-24-3 The title of the article was Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton’s tyrosine kinase for treatment of Rheumatoid arthritis. And the article contained the following:

By applying conformational restrictions, the authors were able to discover highly potent 1,3-diaminopyrimidine based covalent inhibitors of BTK, such as (I) (IC50 = 3.76 nM), and providing useful information of its active conformation. The authors are developing these novel small mol. covalent inhibitors of BTK toward oral agents for Rheumatoid arthritis. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3

The Article related to diaminopyrimidine preparation conformation bruton tyrosine kinase inhibitor antirheumatic, 1,3-diamino-pyrimidine, bruton’s tyrosine kinase (btk), collagen-induced arthritis (cia), rheumatoid arthritis (ra) and other aspects.Electric Literature of 16230-24-3

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

On May 15, 2017, Song, Anran; Zhang, Jianbin; Ge, Yang; Wang, Changyuan; Meng, Qiang; Tang, Zeyao; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Computed Properties of 16230-24-3 The title of the article was C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRT790M mutant. And the article contained the following:

With the aim to overcome the drug resistance induced by the EGFR T790M mutation (EGFRT790M), herein, a family of diphenylpyrimidine derivatives (Sty-DPPYs) bearing a C-2 (E)-4-(styryl)aniline functionality were designed and synthesized as potential EGFRT790M inhibitors. Among them, the compound 10e (N-[3-[[5-fluoro-2-[(E)-4-(3,5-dimethylstyryl)phenylamino]-4-pyrimidinyl]amino]phenyl]-2-acrylamide) displayed strong potency against the EGFRT790M enzyme, with the IC50 of 11.0 nM. Compound 10e also showed a higher SI value (SI = 49.0) than rociletinib (SI = 21.4), indicating its less side effect. In addition, compound 10e could effectively inhibit the proliferation of H1975 cells harboring the EGFRT790M mutation, within the concentration of 2.91 μM. Significantly, compound 10e has low toxicity against the normal HBE cell (IC50 = 22.48 μM). This work provided new insights into the discovery of potent and selective inhibitor against EGFRT790M over wild-type (EGFRWT). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Computed Properties of 16230-24-3

The Article related to styrylaniline diphenylpyrimidine derivative preparation egfr mutant kinase inhibitor, nonsmall cell lung carcinoma antitumor resistance diphenylpyrimidine derivative egf, diphenylpyrimidine, egfr(t790m), inhibitor, nsclc, resistance and other aspects.Computed Properties of 16230-24-3

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

On January 15, 2020, Ren, Jing; Shi, Wei; Zhao, Damin; Wang, Qinglin; Chang, Xiayun; He, Xiangyi; Wang, Xiaojin; Gao, Yong; Lu, Peng; Zhang, Xiquan; Xu, Hongjiang; Zhang, Yinsheng published an article.Category: amides-buliding-blocks The title of the article was Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. And the article contained the following:

Bruton’s tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are very promising targets for hematol. malignancies and autoimmune diseases. In recent years, a few compounds have been approved as a marketed medicine, and several are undergoing clin. trials. By recombining the dominant backbone of known active compounds, constructing a focused library, and screening a broad panel of kinases, we found a class of compounds with dual activities of anti-BTK and anti-JAK3. Some of the compounds have shown 10-folds more active in the enzyme and cell-based assays than a known active compound Furthermore, liver microsome stability experiments show that these compounds have better stability than ibrutinib. These explorations offered new clues to discover benzoxaborole fragment and pyrimidine scaffold as more effective BTK and JAK3 dual inhibitors. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to boron diphenyl pyrimidine derivative preparation btk jak3 inhibitor cancer, autoimmune disease boron diphenyl pyrimidine derivative preparation, autoimmune diseases, btk, benzoxaborole, dual inhibitor, hematological, jak3, pyrimidine and other aspects.Category: amides-buliding-blocks

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

On August 2, 2018, Lee, Jun; Lee, Young Hun; Park, Byung Sun; Yoo, Hee Won published a patent.Recommanded Product: 16230-24-3 The title of the patent was Preparation of fused pyrimidine derivatives as multi-target kinase inhibitors. And the patent contained the following:

The present invention provides fused pyrimidine derivatives I [X = direct bond, O, NH, C(O) or heterocycloalkyl; Y = alkoxyalkyl, heterocycloalkyl or heterocycloalkylalkyl; W = O or NH; Z = A or B; R1 = H, alkoxy or halogen; R2 = H or dialkylaminoalkyl], or their pharmaceutically acceptable salts or stereoisomers, and pharmaceutical compositions containing them. For example, N-[3-[(2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)oxy]phenyl]acrylamide (preparation given) was coupled with 4-[4-(pyrrolidin-1-yl)piperidin-1-yl]aniline (preparation given) to provide compound II. The invention compounds are useful as multi-target kinase inhibitors for the prevention or treatment of cancers or immune-related diseases such as rheumatoid arthritis, Sjoegren’s syndrome, psoriasis, systemic lupus erythematosus, atopy, asthma and multiple sclerosis. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to fused pyrimidine derivative preparation multitarget kinase inhibitor cancer treatment, immune related disease rheumatoid arthritis sjoegren syndrome psoriasis treatment, systemic lupus erythematosus atopy asthma multiple sclerosis treatment and other aspects.Recommanded Product: 16230-24-3

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

On July 18, 2019, Hardy, Jeanne A.; Meka, Penchala Narasimhara published a patent.Formula: C9H10N2O The title of the patent was Preparation of furoxan-based compounds for treating neurodegenerative diseases. And the patent contained the following:

This invention relates to the title compounds I [R1 = H or aryl; R2 = H or aryl; X1 and X2 = (independently) N, N+-O- or CR3 (wherein R3 = H or alkyl and only one of X1 and X2 can be N+-O-); with the proviso] or pharmaceutically acceptable salts, polymorphs, prodrugs, solvates or clathrates thereof, as well as to pharmaceutical compositions comprising such compounds, and to methods for using such compounds/pharmaceutical compositions for treating neurodegenerative diseases including Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and multiple sclerosis (MS). Over fifty compounds I were prepared E.g., a multi-step synthesis of II, starting from cyclohexanone, was described. A method for inhibiting caspase-6 with a compound that reacts with the sulhydryl group (SH) on cysteine 246 of caspase-6 was disclosed (no biol. data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to furoxan derivative preparation neurodegenerative alzheimer’s parkinson’s huntington’s disease treatment, caspase 6 inhibitor furoxan derivative triazolobenzooxadiazole preparation, multiple sclerosis treatment furoxan derivative triazolobenzooxadiazole preparation and other aspects.Formula: C9H10N2O

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

On January 15, 2015, Xu, Xiao; Wang, Xiaobo; Mao, Long; Zhao, Li; Xi, Biao published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of pyrimidine compounds as Btk and Jak kinase inhibitors. And the patent contained the following:

The present invention relates to heterocyclic compounds [I; R1 = H, NRcRd, or 3-7 member cyclic ring substituted with C1-5 alkyl optionally substituted with halo; Rc = H, C1-4 alkyl or 3-7 member cyclic ring; Rd = H or C1-4 alkyl optionally substituted with OZ; Z = H or C1-4 alkyl; R2 = H, halo, C1-4 alkyl, or C1-4 alkoxy; R3 = H, halo, C1-4 alkyl, or C1-4 alkoxy; R5 = H, halo, C1-4 alkyl, or C1-4 alkoxy; R6 = H, halo, C1-4 alkyl, or C1-4 alkoxy; or R1 and R5 are part of 3-7 member cyclic ring, optionally substituted with C1-4 alkyl substituted with OZ; or R1 and R2 are part of 3-7 member cyclic ring, optionally substituted with C1-4 alkyl substituted with OZ; or R2 and R6 are part of 3-7 member cyclic ring, optionally substituted with C1-4 alkyl substituted with OZ; R4 = C2 alkenyl optionally substituted with C1-4 alkyl, CH2OMe, or -CH2NMe2; X = O, C1-4 alkyl optionally substituted with halo, or NRb; Rb = H, or C1-5 alkyl optionally substituted with halo; Y = CH optionally substituted with halo, or N, wherein at least one of R2, R3, R5 and R6 is not H] or pharmaceutically acceptable salts thereof. It also relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, cancer, tumor, inflammatory disease, autoimmune disease, psoriasis, dry eye or immunol. related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the resp. pathways. Thus, etherification of 2,4-dichloro-5-methoxypyrimidine with 3-nitrophenol in the presence of K2CO3 in DMF at 30 ° for 24 h gave 2-chloro-5-methoxy-4-(3-nitrophenoxy)pyrimidine which was coupled with 4-(4-methylpiperazin-1-yl)aniline in the presence of X-Phos and Pd2(dba)3, and K2CO3 in tert-Bu alc. at refluxing for 4 h to give 5-methoxy-N-[4-(4-methylpiperazin-1-yl)phenyl]-4-(3-nitrophenoxy)pyrimidin-2-amine (II; R = NO2). Hydrogenation of II (R = NO2) in the presence of 10% Pd-C in THF under hydrogen pressure of 15 MPa gave II (R = NH2) which was acylated by acryloyl chloride in the presence of diisopropylethylamine in a mixture of MeOH and THF at 0° with stirring for 1 h to give II (R = acryloylamino), namely N-[3-[[5-methoxy-2-[[4-(4-methylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]oxy]phenyl]acrylamide. II (R = acryloylamino) showed IC50 of ≤200 nM against Jak3 phosphorylation in NK-92 cells and that of ≤10 nM against Btk Tyr223 phosphorylation in Ramos cells. 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 piperazinylphenylaminopyrimidine preparation btk jak kinase inhibitor, pyrimidine preparation btk jak kinase inhibitor, piperazinylphenylaminopyrimidinyloxyphenylacrylamide preparation btk jak kinase inhibitor, proliferative disorder cancer tumor treatment pyrimidine preparation and other aspects.Related Products of 16230-24-3

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

On December 15, 2020, Teng, Yu; Li, Xinyu; Ren, Shengnan; Cheng, Yu; Xi, Kun; Shen, Hongtao; Ma, Wenzhuo; Luo, Guoshun; Xiang, Hua published an article.Quality Control of N-(3-Aminophenyl)acrylamide The title of the article was Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. And the article contained the following:

Herein, a series of quinazoline derivatives I [R1 = Br, 3-pyridyl, (6-fluoro-3-pyridyl), (6-chloro-3-pyridyl), 3-quinolyl; R2 = vinyl, Et, HC=CH2CH3, C≡CCH3; R3 = H, Me] bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me]. Compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, compoundI [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] could be identified as a promising PI3Kδ inhibitor worthy of further profiling. 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 quinazoline preparation pi3k delta inhibitor docking human, bromoquinazolinyl amino phenyl boric acid suzuki coupling catalyst palladium, boric acid bromoquinazolinyl oxy phenyl suzuki coupling catalyst palladium, quinolineboronic acid bromoquinazolinyl amino phenyl suzuki coupling catalyst palladium, b-cell malignancies, pi3kδ, quinazoline derivatives and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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