Pyrimidines

On May 31, 2020, Yin, Yuan; Chen, Cheng-Juan; Yu, Ru-Nan; Shu, Lei; Wang, Zhi-Jian; Zhang, Tian-Tai; Zhang, Da-Yong published an article.Synthetic Route of 4433-40-3 The title of the article was Novel 1H-pyrazolo[3,4-d]pyrimidin-6-amino derivatives as potent selective Janus kinase 3 (JAK3) inhibitors. Evaluation of their improved effect for the treatment of rheumatoid arthritis. And the article contained the following:

Selective JAK3 inhibitors have been shown to have a potential benefit in the treatment of autoimmune disorders. Here we report the identification of a series of pyrazolopyrimidine derivatives as potent JAK3 inhibitors that exploit a unique cysteine (Cys909) residue in JAK3. Most of these compounds (13k, 13n and 13 t), displayed stronger anti-JAK3 kinase activity and selectivity than tofacitinib. Furthermore, the most active inhibitor 13t (IC50 = 0.1 nM), also exhibited favorable selectivity for JAK3 in a panel of 9 kinases which contain the same cysteine. In a series of cytokine-stimulated cellular anal., compound 13 t, could potently block the JAK3-STAT signaling pathway. Further biol. studies, including cellular antiproliferative activity assays and a rat adjuvant-induced arthritis model for in vivo evaluation, also indicated its efficacy and low toxicity in the treatment of rheumatoid arthritis. The results of these exptl. explorations suggested that 13t is a promising lead compound for the development of selective JAK3 inhibitor with therapeutic potential in rheumatoid arthritis. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Synthetic Route of 4433-40-3

The Article related to pyrazolo pyrimidin amino derivative preparation jak3 inhibitor rheumatoid arthritis, 4-d]pyrimidin, autoimmune diseases, jak3 inhibitors, pyrazolo[3, rheumatoid arthritis and other aspects.Synthetic Route of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 5, 2016, Ruehter, Gerd; Koch, Uwe; Nussbaumer, Peter; Schulz-Fademrecht, Carsten; Eickhoff, Jan published a patent.Application of 1187830-46-1 The title of the patent was Pharmaceutically active disubstituted triazine derivatives. And the patent contained the following:

The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunol. diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Application of 1187830-46-1

The Article related to triazine derivative infection immune autoimmune cardiovascular proliferation disease preparation, erectile dysfunction stroke triazine derivative protein kinase inhibitor and other aspects.Application of 1187830-46-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 7, 2012, Ruehter, Gerd; Koch, Uwe; Nussbaumer, Peter; Schultz-Fademrecht, Carsten; Eickhoff, Jan published a patent.Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride The title of the patent was Pharmaceutically active disubstituted triazine derivatives. And the patent contained the following:

The invention discloses disubstituted triazine derivatives and/or pharmaceutically acceptable salts and the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunol. diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts,. Furthermore, the invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase and the preparation of said compounds The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

The Article related to triazine derivative infection immune autoimmune cardiovascular proliferation disease preparation, erectile dysfunction stroke triazine derivative protein kinase inhibitor and other aspects.Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Brumfitt, W.; Hamilton-Miller, J. M. T.; Grey, Daphne published an article in 1977, the title of the article was Antibacterial activity of combinations of clindamycin and antifolate agents.Quality Control of 5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine 2-hydroxypropanoate And the article contains the following content:

The antibacterial activities of clindamycin-HCl (I-HCl) [21462-39-5] in combination with the folate antagonists trimethoprim lactate [23256-42-0] or sulfamethoxazole [723-46-6] were only additive, suggesting that I is not an antifolate agent. Thus, some other mechanism of action must be responsible for the therapeutic effects of I against malaria and toxoplasmosis, conditions known to be susceptible to treatment with antifolate compounds Inhibition of protein synthesis is the most likely explanation for the action of I, but other antibiotics which inhibit bacterial protein synthesis have generally shown little activity against malaria. The experimental process involved the reaction of 5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine 2-hydroxypropanoate(cas: 23256-42-0).Quality Control of 5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine 2-hydroxypropanoate

The Article related to clindamycin bactericidal action, trimethoprim clindamycin bactericidal activity, sulfamethoxazole clindamycin bactericidal activity, folate antagonist clindamycin bacteria and other aspects.Quality Control of 5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine 2-hydroxypropanoate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 31, 2022, Ma, Siqi; Cong, Zhaoqing; Wei, Jiaxing; Chen, Weiya; Ge, Di; Yang, Feifei; Liao, Yonghong published an article.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Pulmonary delivery of size-transformable nanoparticles improves tumor accumulation and penetration for chemo-sonodynamic combination therapy. And the article contained the following:

Very little is currently known about how inhaled nanomedicine for lung cancer treatment overcomes biol. barriers hampering the tumor availability of drug and nanoparticles. Here, we developed a size-transformable nanocarrier (∼ 119 nm) in which small-size nanoparticles (∼ 28 nm) were loaded in the large nanocarrier after the addition of modified hyaluronan and could be released upon size-transformation at tumor tissue. Subsequently, the pulmonary and tumor pharmacokinetics of the two nanocarriers containing 7-ethyl-10-hydroxycamptothecin (SN38) and a covalently linked fluorescent sonosensitizer were comparatively investigated after intratracheal instillation to mice bearing orthotopic Lewis lung carcinoma tumors. The results showed that both instilled nanoparticles seemed to transport drug to tumor by direct access and transcytosis of nanoparticles, and diffusion of the released drug with the latter accounting for a great proportion of the drug tumor bioavailability. Relative to the small-size nanocarrier, the size-transformable counterpart appeared to restrict the mucociliary and absorption clearances from the lung and the clearance from the tumor interstitium to circulation, leading to increases in lung and tumor bioavailability of SN38 by 58.5% and 199%, resp. In addition, the size-transformable nanoformulation conferred deep tumor penetration and sustained levels of both sonosensitizer and SN38 within tumors and simultaneously exerted sonodynamic- and chemo-therapies. Overall, the pulmonary delivery of size-transformable nanocarrier could co-deliver sonosensitizer and drug to deep tumor sites with enhanced tumor accumulation to realize combination therapy in lung cancer. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to sn38 nanoparticle drug delivery sonodynamic therapy lewis lung carcinoma, inhaled nanomedicine, lung cancer, size-transformation, tumor penetration, tumor pharmacokinetics and other aspects.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 31, 2020, Fernandez Montes, A.; Vazquez Rivera, F.; Martinez Lago, N.; Covela Rua, M.; Cousillas Castineiras, A.; Gonzalez Villarroel, P.; de la Camara Gomez, J.; Mendez Mendez, J. C.; Salgado Fernandez, M.; Candamio Folgar, S.; Reboredo Lopez, M.; Carmona Campos, M.; Gallardo Martin, E.; Jorge Fernandez, M.; Pellon Augusto, M. L.; Paris Bouzas, L.; Garcia Gomez, J. published an article.Electric Literature of 65-71-4 The title of the article was Efficacy and safety of trifluridine/tipiracil in third-line and beyond for the treatment of patients with metastatic colorectal cancer in routine clinical practice: patterns of use and prognostic nomogram. And the article contained the following:

Introduction: Trifluridine/tipiracil combination has shown a benefit over placebo in the treatment of patients with chemorefractory metastatic colorectal cancer (mCRC). We evaluated the efficacy and safety of this combination in the real-life setting at eight Galician centers in Spain. Patients and methods: This is a retrospective study of a cohort of patients with mCRC in treatment with trifluridine/tipiracil within usual clin. practice who have been previously treated or are not considered candidates for treatment with available therapies. Results: A total of 160 mCRC patients were included. Our data showed that 11.9% of patients achieved disease control. Median progression-free survival was 2.75 mo; at 5.66 mo follow-up, median overall survival was 7.94 mo. Asthenia and neutropenia (48.1% both) were the most frequent adverse events. Overall survival was lower in patients with ECOG 2, multiple metastatic sites, platelets count 350,000/μl, alk. phosphatase > 500 IU/l, and carcinoembryonic antigen > 10 ng/mL. Conclusion: The results of this study confirm the efficacy and safety of trifluridine/tipiracil in chemorefractory mCRC patients. However, patients in clin. practice differ from patients in clin. trials. Due to this, prognostic factors have special importance to offer the best therapeutic approach. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Electric Literature of 65-71-4

The Article related to metastatic colorectal cancer safety trifluridine tipiracil prognosis, metastatic colorectal cancer, nomogram, prognostic factors, real-life, refractory, trifluridine/tipiracil and other aspects.Electric Literature of 65-71-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 31, 2022, Xu, Shiqiang; Sun, Mingyang; Mei, Yu; Gu, Yan; Huang, Ding; Wang, Jihua published an article.Formula: C5H6N2O2 The title of the article was The complete chloroplast genome sequence of the medicinal plant Abrus pulchellus subsp. cantoniensis: genome structure, comparative and phylogenetic relationship analysis. And the article contained the following:

Abrus pulchellus subsp. cantoniensis, an endemic medicinal plant in southern China, is clin. used to treat jaundice hepatitis, cholecystitis, stomachache and breast carbuncle. Here, we assembled and analyzed the first complete chloroplast (cp) genome of A. pulchellus subsp. cantoniensis. The A. pulchellus subsp. cantoniensis cp genome size is 156,497 bp with 36.5% GC content. The cp genome encodes 130 genes, including 77 protein-coding genes, 30 tRNA genes and four rRNA genes, of which 19 genes are duplicated in the inverted repeats (IR) regions. A total of 30 codons exhibited codon usage bias with A/U-ending. Moreover, 53 putative RNA editing sites were predicted in 20 genes, all of which were cytidine to thymine transitions. Repeat sequence anal. identified 45 repeat structures and 125 simple-sequence repeats (SSRs) in A. pulchellus subsp. cantoniensis cp genome. In addition, 19 mononucleotides (located in atpB, trnV-UAC, ycf3, atpF, rps16, rps18, clpP, rpl16, trnG-UCC and ndhA) and three compound SSRs (located in ndhA, atpB and rpl16) showed species specificity between A. pulchellus subsp. cantoniensis and Abrus precatorius, which might be informative sources for developing mol. markers for species identification. Furthermore, phylogenetic anal. inferred that A. pulchellus subsp. cantoniensis was closely related to A. precatorius, and the genus Abrus formed a subclade with Canavalia in the Millettioid/Phaseoloid clade. These data provide a valuable resource to facilitate the evolutionary relationship and species identification of this species. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Formula: C5H6N2O2

The Article related to genome atpb atpf biomarker chloroplast phylogenetic analysis abrus, abrus pulchellus subsp. cantoniensis, chloroplast genome, phylogenetic analysis, structural characteristics and other aspects.Formula: C5H6N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 1, 2022, Li, Zhijun; Bao, Haiying published an article.Recommanded Product: 4433-40-3 The title of the article was Anti-tumor effect of Inonotus hispidus petroleum ether extract in H22 tumor-bearing mice and analysis its mechanism by untargeted metabonomic. And the article contained the following:

The mushroom Inonotus hispidus is traditional Chinese medicine, which has been used to treat tumor illness for many years in China. However, the potential anti-tumor mechanisms of I. hispidus remain unclear. This study aimed to reveal the anti-tumor mechanism of I. hispidus petroleum ether extract (IPE) on H22 tumor-bearing mice from the point of view of metabonomics. The model of H22 tumor-bearing mice was constructed according to the histopathol. data and biochem. parameters, while the serum metabolomics was analyzed by non-targeted ultra-high performance liquid chromatog. and high-resolution mass spectrometry (UPLC-MS/MS) to study the potential anti-tumor mechanisms of IPE. These results indicated that IPE has significant anti-tumor effect on H22 tumor-bearing mice and no obvious adverse reactions were observed After the intervention of IPE, the biosynthesis of cortisol and corticosterone as the metabolics in the downstream of steroid biosynthesis pathway and the biosynthesis of succinate, fumarate and malate as the metabolics in the downstream of tricarboxylic acid cycle pathway were inhibited; but the metabolic pathways of the amino acids as tryptophan, lysine degradation, alanine, aspartate and glutamate and other amino acid were activated. IPE has significant anti-tumor effect in H22 tumor-bearing mice, and the anti-tumor activity of IPE is main through the regulation of energy, amino acids, and steroid hormone biosynthesis pathways expression. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Recommanded Product: 4433-40-3

The Article related to inonotus hepatic carcinoma petroleum ether extract amino acid antitumor, anti-tumor, inonotus hispidus petroleum-ether-extract (ipe), mechanisms, serum metabonomic, uplc-ms/ms and other aspects.Recommanded Product: 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 16, 2010, Smaill, Jeffrey Bruce; Patterson, Adam Vorn; Denny, William Alexander; Wilson, William Robert; Lu, Guo-Liang; Anderson, Robert Forbes; Lee, Ho Huat; Ashoorzaden, Amir published a patent.Electric Literature of 175357-98-9 The title of the patent was Preparation of novel prodrug compounds containing a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger and their use as anti-proliferative agents. And the patent contained the following:

The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a pos. charge. Title compounds I [where X = neg. charged counterion; R1 = group of the formula -(CH2)nTr, wherein Tr = an aromatic nitroheterocycle or aromatic nitrocarbocycle and -(CH2)nTr acts as a reductively-activated fragmenting trigger, and n = 0-6; R2, R3, and R4 independently = aliphatic or aromatic groups of a tertiary amine kinase inhibitor, (R2)(R3)(R4)N; or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor; or one of R2, R3, and R4 may be absent and two of R2, R3, and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor] are claimed. For example, compound II was prepared via alkylation of (2E)-N-[4-(3-bromoanilino)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide with 2-nitrobenzyl bromide. Select I were assayed for their ability to inhibit erbB1 tyrosine kinase and compound II was found to possess an IC50 value of 0.20 nM. The compounds of the invention are useful in treating proliferative diseases such as cancer. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Electric Literature of 175357-98-9

The Article related to alkylammonium bromide derivative preparation kinase inhibitor antiproliferative agent, alkyl ammonium trifluoroacetate derivative preparation kinase inhibitor treatment cancer and other aspects.Electric Literature of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pelclova, Daniela; Zdimal, Vladimir; Schwarz, Jaroslav; Dvorackova, Stepanka; Komarc, Martin; Ondracek, Jakub; Kostejn, Martin; Kacer, Petr; Vlckova, Stepanka; Fenclova, Zdenka; Popov, Alexey; Lischkova, Lucie; Zakharov, Sergey; Bello, Dhimiter published an article in 2018, the title of the article was Markers of oxidative stress in the exhaled breath condensate of workers handling nanocomposites.Formula: C5H6N2O3 And the article contains the following content:

This study investigated airway oxidative stress status in the exhaled breath condensate (EBC). Nineteen employees (42.4 ± 11.4 y/o), working in nanocomposites research for 18.0 ± 10.3 years were examined pre-shift and post-shift on a random workday, together with nineteen controls (45.5 ± 11.7 y/o). Panels of oxidative stress biomarkers derived from lipids, nucleic acids, and proteins were analyzed in the EBC. Aerosol exposures were monitored during three major nanoparticle generation operations: smelting and welding (workshop 1) and nanocomposite machining (workshop 2) using a suite of real-time and integrated instruments. Mass concentrations during these operations were 0.120, 1.840, and 0.804 mg/m3, resp. Median particle number concentrations were 4.8 × 104, 1.3 × 105, and 5.4 × 105 particles/cm3, resp. Nanoparticles accounted for 95, 40, and 61%, resp., with prevailing Fe and Mn. All markers of nucleic acid and protein oxidation, malondialdehyde, and aldehydes C6-C13 were elevated, already in the pre-shift samples relative to controls in both workshops. Significant associations were found between working in nanocomposite synthesis and EBC biomarkers. More research is needed to understand the contribution of nanoparticles from nanocomposite processing in inducing oxidative stress, relative to other co-exposures generated during welding, smelting, and secondary oxidation processes, in these workshops. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Formula: C5H6N2O3

The Article related to exhaled breath condensate oxidative stress nanocomposite, exhaled breath condensate, inhalation, nanocomposites, nanoparticles, occupational exposure, oxidative stress, workers and other aspects.Formula: C5H6N2O3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia