Tag: 100-200

On May 31, 2021, Tang, Lei published an article.Recommanded Product: 4433-40-3 The title of the article was Walking through chromatin modifications. And the article contained the following:

The Cell-TALKING technique probes DNA modifications around a histone modification in fixed cells. Chromatin is a highly organized structure composed of repeating DNA-histone complexes decorated with DNA modifications and histone post-translational modifications (PTMs). To study the composition of chromatin modifications, Zhao’s lab developed Cell-TALKING, a method that leverages DNA walking to index one-to-many combinations of a histone modification with various DNA modifications within a 10-nm nanoenvironment. In Cell-TALKING, the PTM target site is labeled with a DNA walking probe (WP), and DNA modifications including 5-hydroxymethyluracil (5hmU), 5-hydroxymethylcytosine (5hmC) and 5-formyluracil (5fU) are labeled with unique barcoding probes (BPs) that are inactivated with blocked 3′ ends. The researchers applied Cell-TALKING to study the changes in chromatin modifications during the cell cycle and identified combinations of DNA modifications and histone modifications near each other. 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 cell talking chromatin modification, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Recommanded Product: 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Singh, Rajinder; Tanaka, Hiroko; Zeng, Yibin; Zhang, Penglie published a patent.Category: pyrimidines The title of the patent was 6-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:

The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A0 is Nh and CO; A1 and A3 are independently N, NH, CH, CO and CR4; A2, A5 and A6 are independently N, CH and CR4; A4 is N, NC1-4 alkyl, CH and CR4; provided that no more than two of A3, A4, A5 and A6 are N; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is heteroaryl, C6-10 aryl, C1-8 alkylene-heteroaryl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, and OH; two R3 groups can be taken together to form oxo; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; 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 C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Category: pyrimidines

The Article related to indazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 15, 2017, Nguyen, Kim; Fazio, Michael; Kubota, Miles; Nainar, Sarah; Feng, Chao; Li, Xiang; Atwood, Scott X.; Bredy, Timothy W.; Spitale, Robert C. published an article.Formula: C5H6N2O3 The title of the article was Cell-Selective Bioorthogonal Metabolic Labeling of RNA. And the article contained the following:

Stringent chem. methods to profile RNA expression within discrete cellular populations remains a key challenge in biol. To address this issue, the authors developed a chem.-genetic strategy for metabolic labeling of RNA. Cell-specific labeling of RNA can be profiled and imaged using bioorthogonal chem. The authors anticipate that this platform will provide the community with a much-needed chem. toolset for cell-type specific profiling of cell-specific transcriptomes derived from complex biol. systems. 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 cell bioorthogonal labeling rna, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Formula: C5H6N2O3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 30, 2022, Bonifacio, Lillian Gonzalez; Melo, Mirele; Ayo, Christiane Maria; Assoni, Leticia Carolina Paraboli; Olimpio, Larissa Martins; Nogueira, Mariana Reis; Spegiorin, Ligia Cosentino Junqueira Franco; Barbosa, Deusenia Machado Ulisses; de Mattos, Luiz Carlos; Pereira-Chioccola, Vera Lucia; Brandao, Cinara Cassia published an article.Formula: C5H6N2O2 The title of the article was TNFalpha rs1799964 TT genotype may be a susceptibility factor for vertical transmission of Toxoplasma gondii and clinical signs in newborns from pregnant women with acute toxoplasmosis. And the article contained the following:

One of the main impacts of Toxoplasma gondii infection occurs during pregnancy and is related to the vertical transmission of the parasite (congenital toxoplasmosis), which can cause severe clin. outcomes and fetal death. During acute infection, in order to control the rapid replication of tachyzoites, different host immune response genes are activated, and these include cytokine-encoding genes. Considering that polymorphisms in cytokine genes may increase susceptibility to vertical transmission of T. gondii by determining the immune status of the pregnant woman, this study evaluated the influence of polymorphisms of tumor necrosis factor alpha (TNFα) rs1799964 (- 1031) and interleukin 1 beta (IL1β) rs16944 (- 511) genes on gestational toxoplasmosis and on the vertical transmission of the parasite and verified the allele and genotype frequency of these polymorphisms in pregnant patients whose resp. newborn did or did not present clin. abnormalities suggestive of congenital toxoplasmosis. Methods and results: A total of 204 pregnant patients with (n = 114) or without (n = 90) infection by T. gondii were enrolled. No associations were found involving the polymorphisms rs1799964 (- 1031) of the TNFα gene and rs16944 (- 511) of the IL1β gene with the increased chance of T. gondii infection during pregnancy. However, it was observed that the maternal TT genotype referring to the polymorphism of the TNFα gene seems to influence the vertical transmission of the parasite (P = 0.01; χ2 = 6.05) and the presence of clin. manifestation in newborns from pregnancies with acute toxoplasmosis (P = 0.007; χ2 = 9.68). Conclusion: The TNFα rs1799964 TT genotype may act as a susceptibility factor for the vertical transmission of parasite and for the presence of clin. signs in newborns from pregnant women with acute toxoplasmosis. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Formula: C5H6N2O2

The Article related to toxoplasma tnfalpha genotype acute toxoplasmosis pregnancy newborn, gestational toxoplasmosis, polymorphisms, tnfα and il1β, toxoplasmosis, Mammalian Pathological Biochemistry: Obstetrics – Gynecology and other aspects.Formula: C5H6N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

D’Antonio, Matteo; Nguyen, Jennifer P.; Arthur, Timothy D.; Matsui, Hiroko; Donovan, Margaret K. R.; D’Antonio-Chronowska, Agnieszka; Frazer, Kelly A. published an article in 2022, the title of the article was In heart failure reactivation of RNA-binding proteins is associated with the expression of 1,523 fetal-specific isoforms.COA of Formula: C5H6N2O2 And the article contains the following content:

Reactivation of fetal-specific genes and isoforms occurs during heart failure. However, the underlying mol. mechanisms and the extent to which the fetal program switch occurs remains unclear. Limitations hindering transcriptome-wide analyses of alternative splicing differences (i.e. isoform switching) in cardiovascular system (CVS) tissues between fetal, healthy adult and heart failure have included both cellular heterogeneity across bulk RNA-seq samples and limited availability of fetal tissue for research. To overcome these limitations, we have deconvoluted the cellular compositions of 996 RNA-seq samples representing heart failure, healthy adult (heart and arteria), and fetal-like (iPSC-derived cardiovascular progenitor cells) CVS tissues. Comparison of the expression profiles revealed that reactivation of fetal-specific RNA-binding proteins (RBPs), and the accompanied re-expression of 1,523 fetal-specific isoforms, contribute to the transcriptome differences between heart failure and healthy adult heart. Of note, isoforms for 20 different RBPs were among those that reverted in heart failure to the fetal-like expression pattern. We determined that, compared with adult-specific isoforms, fetal-specific isoforms encode proteins that tend to have more functions, are more likely to harbor RBP binding sites, have canonical sequences at their splice sites, and contain typical upstream polypyrimidine tracts. Our study suggests that compared with healthy adult, fetal cardiac tissue requires stricter transcriptional regulation, and that during heart failure reversion to this stricter transcriptional regulation occurs. Furthermore, we provide a resource of cardiac developmental stage-specific and heart failure-associated genes and isoforms, which are largely unexplored and can be exploited to investigate novel therapeutics for heart failure. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).COA of Formula: C5H6N2O2

The Article related to transcriptome mbnl1 fmr1 matr3 ipsc exoc7 heart failure adult, Mammalian Pathological Biochemistry: Cardiovascular Diseases and other aspects.COA of Formula: C5H6N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hao, Yiming; Yuan, Xue; Qian, Peng; Bai, Guanfeng; Wang, Yiqin published an article in 2017, the title of the article was The serum analysis of dampness syndrome in patients with coronary heart disease and chronic renal failure based on the theory of “same syndromes in different diseases”.Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione And the article contains the following content:

Aim. To analyze the serum metabolites in patients with coronary heart disease (CHD) showing dampness syndrome and patients with chronic renal failure (CRF) showing dampness syndrome and to seek the substance that serves as the underlying basis of dampness syndrome in “same syndromes in different diseases.” Methods. Metabolic spectrum by GC-MS was performed using serum samples from 29 patients with CHD showing dampness syndrome and 32 patients with CRF showing dampness syndrome. The principal component anal. and statistical anal. of partial least squares were performed to detect the metabolites with different levels of expression in patientswith CHDand CRF. Furthermore, by comparing the VIP value and data mining inMETLIN and HMDB, we identified the common metabolites in both patient groups. Results. (1) Ten differential metabolites were found in patients with CHD showing dampness syndrome when compared to healthy subjects. Meanwhile, nine differential metabolites were found in patients with CRF showing dampness syndrome when compared to healthy subjects. (2) There were 9 differential metabolites identified when the serum metabolites of the CHD patients with dampness syndrome were compared to those of CRF patients with dampness syndrome.There were 4 common metabolites found in the serums of both patient groups. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to human chd renal failure serum analysis dampness syndrome, Mammalian Pathological Biochemistry: Cardiovascular Diseases and other aspects.Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 31, 2021, Yoshida, Yoichiro; Yamada, Takeshi; Kamiyama, Hirohiko; Kosugi, Chihiro; Ishibashi, Keiichiro; Yoshida, Hiroshi; Ishida, Hideyuki; Yamaguchi, Satoru; Kuramochi, Hidekazu; Fukazawa, Atsuko; Sonoda, Hiromichi; Yoshimatsu, Kazuhiko; Matsuda, Akihisa; Hasegawa, Suguru; Sakamoto, Kazuhiro; Otsuka, Toshiaki; Koda, Keiji; TAS CC3 Study Group. published an article.Reference of 5-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Combination of TAS-102 and bevacizumab as third-line treatment for metastatic colorectal cancer: TAS-CC3 study. And the article contained the following:

Abstract: Our study exclusively examined patients receiving this combination as a third-line treatment to investigate the clin. impact beyond cytotoxic doublets. Methods: This investigator-initiated, open-label, single-arm, multi-centered phase II study was conducted in Japan. Eligible CRC patients were refractory or intolerant to fluoropyrimidine, irinotecan, and oxaliplatin in first- and second-line therapy. TAS-102 (35 mg/m2) was given orally twice daily on days 1-5 and 8-12 in a 4-wk cycle, and bevacizumab (5 mg/kg) was administered by i.v. infusion every 2 wk. The primary endpoint was PFS and the secondary endpoints were time-to-treatment failure, response rate, overall survival (OS), and safety. Results: Between June 2016 and August 2017, 32 patients were enrolled. All patients previously received bevacizumab. The median PFS was 4.5 mo; the median overall survival was 9.3 mo. Partial response was observed in two patients. The most common adverse events above grade 3 were neutropenia followed by thrombocytopenia. There were no non-hematol. adverse events above grade 3 and no treatment-related deaths occurred. Conclusions: This study met its primary endpoint of PFS, which is comparable to the results of the C-TASK FORCE study. The TAS-102 and bevacizumab combination has the potential to be a therapeutic option for third-line treatment of metastatic CRC. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Reference of 5-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to metastatic colorectal cancer tas 102 bevacizumab japan, bevacizumab, chemotherapy, colorectal cancer, neutropenia, tas-102, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Reference of 5-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ogata, Misato; Kotaka, Masahito; Ogata, Takatsugu; Hatachi, Yukimasa; Yasui, Hisateru; Kato, Takeshi; Tsuji, Akihito; Satake, Hironaga published an article in 2020, the title of the article was Regorafenib vs trifluridine/tipiracil for metastatic colorectal cancer refractory to standard chemotherapies: A multicenter retrospective comparison study in Japan.COA of Formula: C5H6N2O2 And the article contains the following content:

Regorafenib (REG) and trifluridine/tipiracil (FTD/TPI) showed survival benefits in metastatic colorectal cancer patients previously treated with standard chemotherapies; therefore, we compared the efficacy and safety of these two treatments. Patients with metastatic colorectal cancer treated with REG or FTD/TPI as a salvage-line therapy from May 2014 to Dec. 2017 were included. We retrospectively analyzed long-term survival, safety, and clin. outcomes. Among 134 patients, 57 and 77 received REG and FTD/TPI, resp. The REG group received more prior systemic chemotherapies and significantly more frequent addnl. chemotherapies than the FTD/TPI group did. The median follow-up was 6.2 mo, whereas the median overall survival was 9.9 and 11.4 mo in the REG and FTD/TPI groups, resp. (hazard ratio = 0.954, p = 0.837). The median progression-free survival was 2.0 and 3.3 mo in the REG and FTD/TPI groups, resp. (hazard ratio = 0.52, p = 0.00047), indicating significant differences, whereas the objective response and disease control rates did not differ. The median overall survival of patients with addnl. subsequent chemotherapies after disease progression was longer than that of patients without addnl. chemotherapy. The most frequent grade ≥3 adverse events were hypertension and neutropenia in the REG and FTD/TPI groups, resp. Our study suggested that sequential use of both drugs may prolong survival. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).COA of Formula: C5H6N2O2

The Article related to metastatic colorectal cancer regorafenib trifluridine tipiracil chemotherapy japan, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.COA of Formula: C5H6N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 31, 2020, Pfeiffer, Per; Yilmaz, Mette; Moller, Soren; Zitnjak, Daniela; Krogh, Merete; Petersen, Lone Noergaard; Poulsen, Laurids Oestergaard; Winther, Stine Braendegaard; Thomsen, Karina Gravgaard; Qvortrup, Camilla published an article.Recommanded Product: 65-71-4 The title of the article was TAS-102 with or without bevacizumab in patients with chemorefractory metastatic colorectal cancer: an investigator-initiated, open-label, randomised, phase 2 trial. And the article contained the following:

TAS-102 (trifluridine-tipiracil) has shown a significant overall survival benefit compared with placebo in patients with chemorefractory metastatic colorectal cancer. Inspired by the encouraging results of a small phase 1-2 study, C-TASK FORCE, which evaluated the combination of TAS-102 plus bevacizumab in patients with chemorefractory metastatic colorectal cancer, we aimed to compare the efficacy of TAS-102 plus bevacizumab vs. TAS-102 monotherapy in patients receiving refractory therapy for metastatic colorectal cancer . This investigator-initiated, open-label, randomized, phase 2 study enrolled patients (aged ≥18 years) with metastatic colorectal from four cancer centers in Denmark. The main inclusion criteria were histopathol. confirmed metastatic colorectal cancer refractory or intolerant to a fluoropyrimidine, irinotecan, oxaliplatin, and cetuximab or panitumumab (only for RAS wild-type), and WHO performance status of 0 or 1. Previous therapy with bevacizumab, aflibercept, ramucirumab, or regorafenib was allowed but not mandatory. Participants were enrolled and randomly assigned (1:1) in block sizes of two, four, or six by a web-based tool to receive oral TAS-102 (35 mg/m2 twice daily on days 1-5 and 8-12 every 28 days) alone or combined with i.v. bevacizumab (5 mg/kg on days 1 and 15) until progression, unacceptable toxicity, or patient decision to withdraw. Treatment assignment was not masked, and randomization was stratified by institution and RAS mutation status. The primary endpoint was investigator-evaluated progression-free survival. All analyses were based on intention to treat. This trial is registered with EudraCT, 2016-005241-23. From Aug 24, 2017, to Oct 31, 2018, 93 patients were enrolled and randomly assigned to TAS-102 (n = 47) or TAS-102 plus bevacizumab (n = 46). The clin. cut-off date was Feb 15, 2019, after a median follow-up of 10.0 mo (IQR 6.8-14.0). Median progression-free survival was 2.6 mo (95% CI 1.6-3.5) in the TAS-102 group vs. 4.6 mo (3.5-6.5) in the TAS-102 plus bevacizumab group (hazard ratio 0.45 [95% CI 0.29-0.72]; p = 0.0015). The most frequent grade 3 or worse adverse event was neutropenia (18 [38%] of 47 in the TAS-102 monotherapy group vs 31 [67%] of 46 in the TAS-102 plus bevacizumab group). Serious adverse events were observed in 21 (45%) patients in the TAS-102 group and 19 (41%) in the TAS-102 plus bevacizumab group. No deaths were deemed treatment related. In patients with chemorefractory metastatic colorectal cancer, TAS-102 plus bevacizumab, as compared with TAS-102 monotherapy, was associated with a significant and clin. relevant improvement in progression-free survival with tolerable toxicity. The combination of TAS-102 plus bevacizumab could be a new treatment option for patients with refractory metastatic colorectal cancer and could be a practice-changing development.Servier. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Recommanded Product: 65-71-4

The Article related to tas bevacizumab fluoropyrimidine anticancer agent colorectal cancer metastasis, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: 65-71-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 5, 2021, Heymach, John; Robichaux, Jacqulyne published a patent.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Use of quinazoline-based tyrosine kinase inhibitors for the treatment of cancers with NRG1 fusions. And the patent contained the following:

Provided herein are methods of selecting cancer patients for treatment with quinazoline-based tyrosine kinase inhibitors, either alone or in combination with anti-HER2/HER3 antibodies, as well as methods of treating cancer patients so selected. Cancer patients are selected for treatment if their cancer has an NRG1 fusion. Selected patients are then treated with quinazoline-based tyrosine kinase inhibitors alone or in combination with anti-HER2/HER3 antibodies. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to tyrosine kinase inhibitor quinazoline her antibody nrg1 fusion cancer, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia