Month: November 2022

Cohen, Jonathan; Palumbo, Alison; Wing, Jason; Heinrich, Michael C. published an article in 2020, the title of the article was Case series of chronic myeloid leukemia patients who maintained deep molecular response (DMR) with very low-dose ponatinib: experience in discontinuing low-dose ponatinib and treatment-free remission (TFR) outcomes.Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile And the article contains the following content:

Chronic myeloid leukemia (CML) is a myeloproliferative disease caused by the BCR-ABL1 fusion protein resulting from chromosomal translocation, most classically the 9;22 translocation. Tyrosine kinase inhibitors (TKIs) have been the standard of care since the FDA approval of imatinib in 2001. TKIs used to treat CML include nilotinib, dasatinib, bosutinib, and ponatinib. Using modern TKI-based therapy, the annual mortality and 10-yr survival rates for chronic phase CML are currently 1-2% and 80-90%, resp. Select patients receiving TKI-based therapies that have maintained a deep mol. response (DMR) may discontinue TKI therapy, with trial of treatment-free remission (TFR). This case series supports that TFR may be successfully achieved in patients receiving ponatinib. 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).Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to ponatinib treatment free remission chronic myeloid leukemia mol response, Pharmacology: Drug Metabolism and other aspects.Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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

Yoneyama, Hiroshi; Kobayashi, Satoshi; Okachi, Ryo published an article in 1984, the title of the article was Studies on antimicrobial activity of ketoconazole (KW-1414). VI. In vitro antifungal and antibacterial activity of ketoconazole (KW-1414) and its analogs.HPLC of Formula: 67914-60-7 And the article contains the following content:

Antifungal activities of structural analogs and metabolites of the synthetic antifungal agent ketoconazole (KCZ; KW-1414) (I) were investigated. R-39519 (desacetyl derivative) and R-44319 (trans isomer) had less antifungal activity against Candida species and dermatophytes than did I. HLI-151 (oxidized derivative) had no antifungal activity against any of the yeasts or fungi. Two known physiol. metabolites of I, R-43568 and T-1141, also showed no antifungal activity. I, R-39519, R-43568, and T-1141 showed no antibacterial activity against 12 strains of Lactobacillus species which are normal flora of the vagina. In blood of human volunteers administered orally 200 mg of I, no antifungal activity was detected except for I by bioautog. seeded with Kluyveromyces fragilis. In human urine of the same volunteers, no antifungal activity was detected by the bioautog. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

The Article related to ketoconazole analog microbicide, bactericide ketoconazole derivative, fungicide ketoconazole derivative, Microbial Biochemistry: Other and other aspects.HPLC of Formula: 67914-60-7

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

On December 31, 2007, Raina, R.; Prawez, S.; Dimitrova, D. J.; Verma, P. K.; Pankaj, N. K. published an article.Product Details of 86393-32-0 The title of the article was Pharmacokinetics of ciprofloxacin following intravenous administration in WLH chickens (Gallus domesticus). And the article contained the following:

Pharmacokinetics of ciprofloxacin was studied in WLH chicken after single i.v. dose @ 4 mg.kg-1 body weight Plasma ciprofloxacin concentrations were analyzed by microbiol. assay technique using E. coli ATCC-25922 as test organisms grown. The determination of the best-fit compartment model and initial estimates of the model-dependent pharmacokinetics was analyzed for each bird by Top-Fit v. 2.0 computer program. The three compartment open model was the best fit for i.v. injection of ciprofloxacin. Statistical moments were also used to compute the noncompartmental pharmacokinetic anal. The elimination half life (t1/2β), volume of distribution from central compartment (Vc) and total body clearance (ClB) were 5.79±1.14 h, 0.85±0.07 L.kg-1 and 16.27±1.87mL.min-1.kg-1, resp. The mean residence time (MRT) and area under the plasma concentration vs time curve from 0 to ∞ (AUC0→ ∞) were 7.05±1.34 h and 4.54±0.59 μg.h.ml-1, resp. The variation coefficient of the technique for the intraassay and interassay precission was less than 10% in the range of standard concentration The lower limit of sensitivity of the ciprofloxacin assay was 0.015 μg.ml-1. The serum concentration at time zero (Cp°) and area under the curve from 0 to 24h (AUC0-24) were applied in the calculation of predictors of efficacy for concentration-dependent antibiotics. Ciprofloxacin concentration in plasma of chickens, maintaining min. inhibitory concentration (MIC <1 μg.ml-1) for upto 12 h after i.v. administration @ 4mg.kg-1, would be adequate for controlling avian bacterial diseases. 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).Product Details of 86393-32-0

The Article related to antimicrobial pharmacokinetics pharmacodynamics ciprofloxacin hydrochloride monohydrate escherichia pasteurella gallus, Pharmacology: Drug Metabolism and other aspects.Product Details of 86393-32-0

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

On June 30, 2021, Wall, Thomas P.; Crowley, Peter D.; Buggy, Donal J. published an article.Recommanded Product: 380843-75-4 The title of the article was The effect of lidocaine and bosutinib on 4T1 murine breast cancer cell behaviour In Vitro. And the article contained the following:

Systemic lidocaine has recently emerged as a promising agent possessing numerous potentially anti-neoplastic effects. In vitro studies suggest that lidocaine may prevent metastasis by acting on the tyrosine kinase enzyme Src. I.v. lidocaine has been reported to reduce pulmonary metastasis in vivo in a murine breast cancer model, however the beneficial effect is abolished by the Src inhibitor bosutinib. In this study we examined whether lidocaine and/or bosutinib affects 4TI breast cancer cell activity in vitro and whether any drug interactions similar to that seen in murine models occur. 4TI murine breast cancer cells were exposed to lidocaine and/or bosutinib. Cell viability after / h ofexposure was measured using the 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (G) assay. Cell migration after 24 h ofexposure was measured using the Oris migration assay. Lidocaine and bosutinib alone or combined inhibited 4TI cell viability and migration, but only at supratherapeutic concentrations Bosutinib did not modulate lidocaine’s effect on viability or migration at any concentration tested. Although lidocaine may inhibit 4T1 metastasis in vivo, a direct effect on 4TI cells is not detectable in vitro at non-toxic concentrations and unlike murine model testing, no unusual interaction with bosutinib was detected. Lidocaine’s anti-metastatic properties are likely to be complex and multifactorial and difficult to replicate outside ofa biol. host. 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).Recommanded Product: 380843-75-4

The Article related to lidocaine bosutinib human murine breast cancer cell behavior, lidocaine, src, bosutinib, cancer, local anesthetics, metastasis, Pharmacology: Drug Metabolism and other aspects.Recommanded Product: 380843-75-4

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

On December 4, 2008, Souza, Fabio Eduardo Silva; Oudenes, Jan; Gorin, Boris Ivanovich published a patent.Formula: C17H21ClFN3O4 The title of the patent was Anhydrous ciprofloxacin hydrochloride. And the patent contained the following:

The present invention provides a new anhydrous crystalline form of ciprofloxacin-HCl that is substantially free from solvent mols., and processes of preparation thereof. 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).Formula: C17H21ClFN3O4

The Article related to ciprofloxacin hydrochloride anhydrous, Pharmaceuticals: Pharmaceutics and other aspects.Formula: C17H21ClFN3O4

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

On May 31, 2002, Liu, Yong; Wang, Jing-kang; Yin, Qiu-xiang published an article.Related Products of 86393-32-0 The title of the article was Study on the thermodynamics of crystallization of ciprofloxacin hydrochloride monohydrate. And the article contained the following:

The melting temperature, the melting heat and the solubility of ciprofloxacin hydrochloride monohydrate in water/ethanol solution are measured in this paper. The solubility model and the expression of the relationship between the activity coefficient and the solvation constant K of ciprofloxacin hydrochloride monohydrate have been established. The dissolution heat and the solvation energy of ciprofloxacin hydrochloride monohydrate in water/ethanol solution have been estimated using the exptl. solubility data. This study aims at supplying valuable thermodn. data for the industrial manufacture of ciprofloxacin hydrochloride monohydrate. 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).Related Products of 86393-32-0

The Article related to ciprofloxacin thermodn crystallization, Pharmaceuticals: Pharmaceutics and other aspects.Related Products of 86393-32-0

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

On March 12, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmerman, Kurt published a patent.Formula: C15H29N3O2 The title of the patent was Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. And the patent contained the following:

The present disclosure relates to bifunctional compounds, ULM- L-PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Formula: C15H29N3O2

The Article related to polycyclic targeted protein kinase raf, Pharmaceuticals: Pharmaceutics and other aspects.Formula: C15H29N3O2

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

On December 2, 2004, Faour, Joaquina; Vergez, Juan A. published a patent.Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the patent was Breakable, controlled-release tablets comprising a preformed passage. And the patent contained the following:

The invention relates to a simple and improved osmotic device for the controlled release of an active agent from the core into the use environment. According to the invention, the active agent is first released through a preformed passage and, subsequently, through a second passage which is formed in situ. Optionally, the size of one or both of the passages increases during the use of the osmotic device. Moreover, the preformed passage and/or the second passage increases the release speed of the active agent and enables the release of larger particles containing the active agent and/or the release of active agents which are essentially insoluble in the use environment. Owing to the in situ formation of the second opening, the device can release a greater percentage of active agent than that which would be released without said second opening. 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).Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to drug delivery tablet controlled release, Pharmaceuticals: Pharmaceutics and other aspects.Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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

On October 1, 1996, Turel, Iztok; Bukovec, Peter published an article.Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Comparison of the thermal stability of ciprofloxacin and its compounds. And the article contained the following:

The thermal behavior of ciprofloxacin, its hydrochloride and 2 copper (II) compounds of ciprofloxacin was studied by thermogravimetry, DSC, evolved gas anal. and IR spectroscopy. In all the compounds studied, profound differences in the carboxylic (C:O) absorption were found after heating, which can be explained by the rearrangement of the hydrogen bonds. 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).Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to ciprofloxacin copper complex thermal stability, Pharmaceuticals: Pharmaceutics and other aspects.Recommanded Product: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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

On September 30, 2004, Weyenberg, W.; Vermeire, A.; D’Haese, E.; Vanhaelewyn, G.; Kestelyn, P.; Callens, F.; Nelis, H. J.; Remon, J. P.; Ludwig, A. published an article.Formula: C17H21ClFN3O4 The title of the article was Effect of different sterilisation methods on the properties of bioadhesive powders and ocular minitablets, and clinical evaluation. And the article contained the following:

The purpose of this study was to evaluate the influence of gamma-irradiation and dry heat sterilization on the properties of a bioadhesive powder mixture containing ciprofloxacin and its corresponding ocular minitablets. The mol. weight characteristics of drum dried waxy maize starch (DDWM), employed as major component of the bioadhesive formulation, the decay kinetics of radicals, the rheol. properties of the bioadhesive polymers and the microbial activity of ciprofloxacin were studied. The influence of the different sterilization methods on the characteristics of the ocular minitablets was investigated by measuring the crushing strength, the friability, and the in vitro release of ciprofloxacin from the minitablets. Finally, the clin. value of the selected sterilized minitablets was evaluated in seven healthy volunteers. Both sterilization methods similarly affected the properties of the bioadhesive formulation by inducing stable radicals and decreasing the mol. weight of DDWM, although no changes in the microbiol. activity of ciprofloxacin were measured. An obvious influence of both sterilization methods was observed in the in vitro release study. The crushing strength and friability of the minitablets were not significantly influenced by gamma-irradiation Based on these data, gamma-irradiation was more adequate as sterilization method for the bioadhesive ocular minitablets than dry heat sterilization, because it affected the least the phys. properties of the minitablets. Therefore, the gamma-sterilized minitablets were selected for an in vivo evaluation in seven volunteers. The concentration of ciprofloxacin in the tear film remained above its MIC value for the most common ocular pathogens for at least 8 h. Consequently, the gamma-irradiated minitablets containing ciprofloxacin can be considered as a promising formulation to treat bacterial keratitis and conjunctivitis. 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).Formula: C17H21ClFN3O4

The Article related to bioadhesive powder ocular minitablet sterilization, Pharmaceuticals: Pharmaceutics and other aspects.Formula: C17H21ClFN3O4

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