Month: October 2022

On April 12, 2018, Crew, Andrew P.; Hornberger, Keith R.; Snyder, Lawrence B.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Crews, Craig M.; Dong, Hanqing published a patent.Category: piperazines The title of the patent was Preparation of bifunctional compounds for the targeted degradation of androgen receptor. And the patent contained the following:

The invention relates to bifunctional compounds, which find utility to degrade and (inhibit) androgen receptor. In particular, the invention is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds androgen receptor, such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of androgen receptor. The invention exhibits a broad range of pharmacol. activities associated with compounds according to the present invention, consistent with the degradation/inhibition of androgen receptor (data given). The invention compounds are claimed to be useful for the treatment of cancer or Kennedy’s disease, or both. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Category: piperazines

The Article related to protac modulator preparation targeted ubiquitination androgen receptor degradation inhibition, preparation bifunctional compound degradation androgen receptor, treatment cancer kennedy disease preparation bifunctional compound and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 1, 2017, Lin, Xiao-Xiao; Zhang, Xiao-Fang; Wang, Ai-Jun; Fang, Ke-Ming; Yuan, Junhua; Feng, Jiu-Ju published an article.Computed Properties of 67914-60-7 The title of the article was Simple one-pot aqueous synthesis of AuPd alloy nanocrystals/reduced graphene oxide as highly efficient and stable electrocatalyst for oxygen reduction and hydrogen evolution reactions. And the article contained the following:

Herein, the authors develop a simple 1-pot aqueous method to prepare AuPd alloy nanocrystals on reduced graphene oxide (AuPd NCs/rGO), by using 1-acetyl-4-(p-hydroxyphenyl) piperazine (AHPP) as the reductant, stabilizing agent and structure-director, without any other additives (e.g., seed, surfactant or polymer). The product is mainly characterized by TEM, XPS, x-ray diffraction and TGA. The obtained AuPd NCs/rGO displays enlarged electrochem. active surface area and superior catalytic performances toward O reduction reaction (ORR) and H evolution reaction (HER) relative to Pt/C, Pd/C, Pd/rGO and Au/rGO catalysts, showing promising applications in energy storage and conversion. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to synthesis gold palladium alloy nanocrystal reduced graphene oxide catalyst, electrocatalyst oxygen reduction hydrogen evolution, aupd nanocrystals, hydrogen evolution reaction, oxygen reduction reaction, reduced graphene oxide and other aspects.Computed Properties of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 15, 2006, Power, Eoin C.; Ganellin, C. Robin; Benton, David C. H. published an article.Application of 67914-60-7 The title of the article was Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BKCa). And the article contained the following:

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the Ph and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application of 67914-60-7

The Article related to potassium channel calcium activated large conductance ketoconazole fragment preparation, kcnm family potassium channel ketoconazole fragment preparation, channel blocker opener potassium calcium ketoconazole analog preparation and other aspects.Application of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 2021, Mizuno, Takahito; Sakai, Takamasa; Tanabe, Kouichi; Kozaki, Koji; Umemura, Takumi; Higashikawa, Mariko; Kimura, Tomoki; Yamada, Tetsuya; Goto, Nobuyuki; Ohtsu, Fumiko published an article.Category: piperazines The title of the article was Identification of target small molecule tyrosine kinase inhibitors that need monitoring and clinical application of protocol for early detection of cancer therapeutics-related cardiac dysfunction using signal detection: An investigation of real world data. And the article contained the following:

Purpose: In order to detect cancer therapeutics-related cardiac dysfunction (CTRCD) early, we identified which drugs were to be monitored using signal detection and the package insert, and created and applied a protocol to address this. Methods: Adverse event data recorded in the Japanese Adverse Drug Event Report (JADER) database between Apr. 2004 and Jan. 2018 were used. We applied our findings clin. by creating a protocol to detect CTRCD early. All cases at Tosei General Hospital where the target tyrosine kinase inhibitors were administered from when they were first released in Nov. 2019 were included. We compared the results from before and after we began the protocol to clarify its effects. Results: We found that CTRCD was not described in the serious side-effect section of the package inserts for Bosutinib, Alectinib, and Osimertinib even though CTRCD signals were detected for them. Therefore, it is possible that we may have previously overlooked CTRCD. When we applied our protocol using Osimertinib as the target drug, we were able to detect CTRCD early in 5/21 (24%) patients. Conclusions: It was clarified that the drug identification method used in this study for early detection of adverse events leads to early detection of adverse events when applied clin. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Category: piperazines

The Article related to cancer cardiac dysfunction tyrosine kinase inhibitor therapeutics side effect, cancer therapeutics-related cardiac dysfunction, japanese adverse drug event report database, osimertinib, small molecule tyrosine kinase inhibitors and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 2020, Pushpam, Deepam; Bakhshi, Sameer published an article.Computed Properties of 380843-75-4 The title of the article was Pharmacology of tyrosine kinase inhibitors in chronic myeloid leukemia; a clinician’s perspective. And the article contained the following:

Meta-anal. of tyrosine kinase inhibitors pharmacol. in chronic myeloid leukemia patients. Upcoming concepts and related trials in the management of chronic myeloid leukemia (CML) along with future directions have been touched upon. Evidence acquisition: PubMed, Embase, Google, Cochrane library and Medline were searched to identify relevant literature for the review. Clinicaltrial.gov was searched for upcoming data and trials. Results: There are lot of gap in pharmacokinetics and pharmacodynamics of TKI. Imatinib appears to be the safest TKI. Newer TKI’s achieve better achievement of therapeutic milestones, deeper mol. response and less chances of progression of CML compared to imatinib. Newer TKI appears to be better choice for achieving TFR. When the objective is survival, imatinib is still the TKI of choice. Primary prophylaxis with antiplatelet drugs for TKI having cardiovascular and thromboembolic side effects should be considered. Conclusion: Pharmacogenetic data of TKI is still immature to guide in therapeutic decision making in clin. practice. There is need for further research in pharmacol. and pharmacogenomics of newer TKI’s. Randomized controlled trials are required to decide the optimum TKI for TFR. Safe and effective TKI for targeting T315I mutation, CML accelerated phase and blast crisis are an active area of research. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to meta analysis chronic myeloid leukemia tyrosine kinase pharmacol, gene polymorphism and imatinib, pharmacology of tyrosine kinase inhibitors, selection of tyrosine kinase inhibitors, tyrosine kinase inhibitors in chronic myeloid leukemia and other aspects.Computed Properties of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 1, 2017, Xiao, Ganyuan; Li, Yan; Qiang, Xiaoming; Xu, Rui; Zheng, Yunxiaozhu; Cao, Zhongcheng; Luo, Li; Yang, Xia; Sang, Zhipei; Su, Fu; Deng, Yong published an article.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride The title of the article was Design, synthesis and biological evaluation of 4′-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease. And the article contained the following:

A series of 4′-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50 = 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic anal. of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42 aggregation and Cu2+-induced Aβ1-42 aggregation by 89.5% and 79.7% at 25 μM resp., as well as acted as a selective monoamine oxidase B inhibitor (IC50 = 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer’s disease. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to aminochalcone revastigmine hybrid synthesis blood brain barrier alzheimer disease, acetylcholinesterase inhibitors, alzheimer’s disease, aβ aggregation inhibitors, chalcone carbamate derivatives, monoamine oxidase b inhibitors, multifunctional agents and other aspects.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 1, 2020, Koller, Dora; Vaitsekhovich, Viktoryia; Mba, Cecile; Steegmann, Juan L.; Zubiaur, Pablo; Abad-Santos, Francisco; Wojnicz, Aneta published an article.Computed Properties of 380843-75-4 The title of the article was Effective quantification of 11 tyrosine kinase inhibitors and caffeine in human plasma by validated LC-MS/MS method with potent phospholipids clean-up procedure. application to therapeutic drug monitoring. And the article contained the following:

Therapeutic drug monitoring (TDM) help to improve treatment efficacy and safety. Therefore, a simple and sensitive liquid chromatog.-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous monitoring of 11 tyrosine kinase inhibitors (TKIs) in human plasma. TKIs included in the assay are used in the treatment of chronic myeloid leukemia (CML: imatinib, dasatinib, nilotinib, bosutinib, ponatinib), polycythemia vera (ruxolitinib), chronic lymphocytic leukemia (ibrutinib) and rheumatoid arthritis (filgotinib, tofacitinib, baricitinib, peficitinib). Caffeine was also included in the method. Caffeine increases the acidity of the stomach and decreases its pH as well as is a competitive inhibitor of cytochrome P 450 isoenzymes. Thus, it may influence absorption and metabolism of some TKIs, by modifying their plasma levels. The analytes of interest and their stable isotope-labeled internal standards were extracted from 200μL of human plasma. Microelution-solid phase extraction (μ-SPE) was optimized for method validation and compared to simple protein precipitation (PPT). A gradient elution on a Poroshell 120 EC-C18 column at 60°C and a flow rate of 0.5 mL/min was applied for analyte separation The anal. run lasted 8 min and it was followed by a re-equilibration time of 4 min. Dynamic multiple reaction monitoring scan in the pos. ionization mode was applied to improve method sensitivity. Endogenous plasma phospholipids can strongly affect MS anal. Hence, the monitoring of endogenous phospholipids was included in the assay. Full validation of the method was achieved, including tests of precision, accuracy, trueness, linearity, extraction recovery, matrix effect, process efficiency, stability, sensitivity (with excellent LLOQs), selectivity, identity confirmation and carry-over effect. Regarding sample cleanup, more than 91% of early eluting and more than 96% of late eluting endogenous phospholipids were eliminated by μ-SPE when compared to PPT. This method enables the simultaneous plasma monitoring of 11 TKIs and caffeine and ensures high effectiveness in phospholipids elimination. The present approach is currently used in our clin. practice, being applied to TDM of dasatinib, imatinib, nilotinib and ponatinib. TKIs plasma monitoring helps to individualize dose adjustment and manage adverse effects in CML patients. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to tyrosine kinase inhibitor therapeutic drug monitoring hplc mass spectrometry, blood plasma analysis, caffeine, liquid chromatography-tandem mass spectrometry, phospholipids, solid phase extraction, therapeutic drug monitoring, tyrosine kinase inhibitors and other aspects.Computed Properties of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hubicka, Urszula; Zmudzki, Pawel; Talik, Przemyslaw; Zuromska-Witek, Barbara; Krzek, Jan published an article in 2013, the title of the article was Photodegradation assessment of ciprofloxacin, moxifloxacin, norfloxacin and ofloxacin in the presence of excipients from tablets by UPLC-MS/MS and DSC.COA of Formula: C17H21ClFN3O4 And the article contains the following content:

Background: Ciprofloxacin (CIP), moxifloxacin (MOX), norfloxacin (NOR) and ofloxacin (OFL), are the antibacterial synthetic drugs, belonging to the fluoroquinolones group. Fluoroquinolones are compounds susceptible to photodegradation process, which may lead to reduction of their antibacterial activity and to induce phototoxicity as a side effect. This paper describes a simple, sensitive UPLC-MS/MS method for the determination of CIP, MOX, NOR and OFL in the presence of photodegradation products. Results: Chromatog. separations were carried out using the Acquity UPLC BEH C18 column; (2.1 × 100 mm, 1.7 μm particle size). The column was maintained at 40°C and the following gradient was used: 0 min, 95% of eluent A and 5% of eluent B; 10 min, 0% of eluent A and 100% of eluent B, at a flow rate of 0.3 mL min-1. Eluent A: 0.1% (volume/volume) formic acid in water; eluent B: 0.1% (volume/volume) formic acid in acetonitrile. The method was validated and all the validation parameters were in the ranges acceptable by the guidelines for anal. method validation. The photodegradation of examined fluoroquinolones in solid phase in the presence of excipients followed kinetic of the first order reaction and depended upon the type of analyzed drugs and coexisting substances. Photodegradation process of analyzed drugs was confirmed by differential scanning calorimetry. In addition, the identification of degradation products was carried out by mass spectrometry. Conclusion: The developed UPLC-MS/MS method enables the determination of CIP, MOX, NOR and OFL in the presence of photodegradation products and identification of photodegradation products. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).COA of Formula: C17H21ClFN3O4

The Article related to antibacterial agent excipient photodegradation uplc msms dsc, ciprofloxacin, differential scanning calorimetry, kinetic evaluation, moxifloxacin, norfloxacin, ofloxacin, photodegradation, tandem mass spectrometry, ultra performance liquid chromatography and other aspects.COA of Formula: C17H21ClFN3O4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Gentili, P.; Carenini, G. published an article.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride The title of the article was Antidepressant activity of cyclohexylphenoxymorpholines. And the article contained the following:

2-[(Cyclohexylphenoxy)methyl]morpholines I (R = H, alkyl, aminoalkyl, piperazinopropionyl or -propyl, benzoylalkyl; R1 = 2-, 3-, or 4-cyclohexyl) were prepared by different methods and they showed antidepressant, tranquilizer, analgesic, and spasmolytic activity; I also inhibited blood platelet aggregation. The phenoxyisopropanolamine II reacted with ClCH2COCl to yield a 2-(phenoxymethyl)morpholin-5-one, the product was reduced (LiAlH4) to give a N-benzylmorpholine derivative, and hydrogenolysis of the latter gave I (R = H, R1 = 2-cyclohexyl). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

The Article related to morpholine phenoxymethyl preparation antidepressant, phenoxymethylmorpholine preparation antidepressant analgesic, tranquilizer phenoxymethylmorpholine preparation, spasmolytic phenoxymethylmorpholine preparation, blood platelet phenoxymethylmorpholine preparation and other aspects.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On November 14, 2003, Tanoury, Gerald J.; Hett, Robert; Wilkinson, H. Scott; Wald, Stephen A.; Senanayake, Chris H. published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Total synthesis of (2R,4S,2’S,3’R)-hydroxyitraconazole: implementations of a recycle protocol and a mild and safe phase-transfer reagent for preparation of the key chiral units. And the article contained the following:

A convergent total synthesis of enantiomerically-pure (2R,4S,2’S,3’R)-hydroxyitraconazole is described. The left dioxolane portion of the mol. was prepared in good yield by the conversion of (4S)-2,2-dimethyl-1,3-dioxolane-4-methanol to the corresponding enantiomerically and diastereomerically-pure acetonide (2R,4R)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolane-4-methanol by a recycle protocol involving diastereoselective crystallization of the tosylate salt, followed by re-equilibration of the mother liquor and crystallization The right-hand triazolone moiety was generated by alkylation of a triazolone derivative with an enantiomerically pure cyclic sulfate [(4R,5R)-4,5-dimethyl-1,2,3-dioxathiolane 2,2-dioxide] under mild and essentially non-hazardous reaction conditions (TDA-1, K2CO3, acetonitrile). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to hydroxyitraconazole total synthesis preparation, tda cost effective hydroxyitraconazole total synthesis preparation, alkylation tda cost effective hydroxyitraconazole total synthesis preparation, cost effective hydroxyitraconazole total synthesis preparation, asym synthesis hydroxyitraconazole preparation and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics