Tag: 600-700

Statistical optimization and validation of a novel ultra-performance liquid chromatography method for estimation of nintedanib in rat and human plasma was written by Shukla, Snehal K.;Kadry, Hossam;Bhatt, Jayshil A.;Elbatanony, Rasha;Ahsan, Fakhrul;Gupta, Vivek. And the article was included in Bioanalysis in 2020.Category: piperazines The following contents are mentioned in the article:

A high throughput ultra-performance liquid chromatog. (UPLC)-UV method for quantification of nintedanib in rat and human plasma was developed and optimized using chemometrical approach. Design of experiment and multivariate statistical approach was used for definition of optimized method. Final separation was performed using protein precipitation method on ACQUITY HSS T3 C18 column in isocratic mode using potassium phosphate buffer (pH 7.5): acetonitrile. Method was validated as per US-FDA guidelines linearly from 15-750 ng/mL. All quality control samples showed <15% relative standard deviation for precision and 85-115% accuracy along with >98% extraction recovery. The developed method is easily applicable in determining pharmacokinetic parameters in preclin. subjects along with successful implementation for quantification in human plasma samples. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Category: piperazines).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

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

Dehydrated crystalline form of (3Z)-2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl) acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate was written by Anonymous. And the article was included in IP.com Journal in 2015.Application of 656247-18-6 The following contents are mentioned in the article:

Described herein after is a dehydrated form of the hemihydrate form of (3Z)-2,3-dihydro-3- [[[4-[methyl[2-(4-methyl-1-piperazinyl) acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H- indole-6-carboxylic acid Me ester ethansulfonate (referred to as Compound A). The water content of the dehydrated form is of about 0.32%, determined by Karl Fischer (KF) method, whereas the theor. value of water content for Compound A as a hemihydrate form is 1.37%. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Application of 656247-18-6).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Application of 656247-18-6

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

Synthetic approaches to the 2014 new drugs was written by Flick, Andrew C.;Ding, Hong X.;Leverett, Carolyn A.;Kyne, Robert E. Jr.;Liu, Kevin K.-C.;Fink, Sarah J.;O’Donnell, Christopher J.. And the article was included in Bioorganic & Medicinal Chemistry in 2016.Quality Control of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate The following contents are mentioned in the article:

A review. New drugs introduced to the market every year represent privileged structures for particular biol. targets. These new chem. entities (NCEs) provide insight into mol. recognition and also serve as leads for designing future new drugs. This annual review covers the synthesis of thirty-seven NCEs that were approved for the first time in 2014 and one drug which was approved in 2013 and was not covered in a previous edition of this review. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Quality Control of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Quality Control of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate

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

An improved process for the synthesis of nintedanib esylate was written by Arava, Veerareddy;Gogireddy, Surendrareddy. And the article was included in Synthetic Communications in 2017.Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate The following contents are mentioned in the article:

Nintedanib esylate was synthesized via novel intermediates of (Z)-Me 3-(acetoxy-phenyl)methylene-1-acetyl-2-oxoindoline-6-carboxylate and N-(4-aminophenyl)-2-chloro-N-methylacetamide in good yields. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate

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

Development and validation of RP-HPLC method for the estimation of nintedanib esylate in bulk and its formulation was written by Patil, Rohan S.;Mahajan, Moreshwar P.. And the article was included in Research & Reviews: A Journal of Pharmaceutical Science in 2018.Synthetic Route of C33H39N5O7S The following contents are mentioned in the article:

A review. A simple, precise, reliable, rapid and reproducible reversed-phase high performance liquid chromatog. method (RP-HPLC) method has was developed and validated for the estimation of Nintedanib Esylate. Chromatog. was carried out with anal. technol. HPLC system consisted of UV-3000-M detector on C18 (4.6×250 mm, 5μ) column with a mobile phase composed of methanol:water (80:20 volume/volume) at a flow rate of 1 mL/min. The pH of the mobile phase was adjusted by 0.05% ortho phosphoric acid (pH-3). Detection was carried out using a UV detector at 287 nm. Parameters such as linearity, precision, accuracy, ruggedness, robustness, LOD and LOQ were studied as per the ICH Q2 (R1) guidelines. The retention time was found to be 4.67 min. The linearity range for Nintedanib esylate was 10-60μg/mL. The correlation coefficient was found to be 0.999. Developed method was found to be accurate, precise, selective and rapid for estimation of Nintedanib esylate in pharmaceutical dosage form. The proposed method can be useful in quality control of bulk manufacturing and pharmaceutical dosage form. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Synthetic Route of C33H39N5O7S).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C33H39N5O7S

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

Development and evaluation of cost effective formula of nintedanib esylate soft gelatin capsule and compare with prepared product similar to innovator was written by Gaikwad, Sonal S.;Singh, Meera C.. And the article was included in Research & Reviews: A Journal of Pharmaceutical Science in 2018.HPLC of Formula: 656247-18-6 The following contents are mentioned in the article:

Nintedanib esylate was invented by Boehringer Ingelheim Pharmaceuticals. Nintedanib esylate is an organosulfonate salt obtained by combination of Nintedanib with ethane sulfonic acid. It’s a kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer. Bioavailability and water solubility of Nintedanib esylate is very low and BCS class is not mentioned in the literature. Due to poor solubility of Nintedanib esylate at neutral conditions, the active substance cannot be formulated as solution and therefore innovator has prepared soft gelatin capsule with oil base i.e. suspended in a lipophilic fill mix. Innovator’s product (Ofev) is not available in India, so in this research, we first prepared innovator’s product (Derived on the basis of literature) and then prepared product similar to innovator’s product which is cost effective. For evaluation of product, in-vitro anal. data was compared with data available for innovator’s product literature. The product similar to innovator was successfully developed and compared with available literature. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6HPLC of Formula: 656247-18-6).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 656247-18-6

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

Solubility measurement and thermodynamic properties of Nintedanib Esylate Hemihydrate in pure solvents was written by Ma, Jinju;Huang, Jingyi;Cao, Zidan;Sha, Jiao;Sun, Renren;He, Haixia;Wan, Yameng;Li, Yu;Li, Tao;Ren, Baozeng. And the article was included in Journal of Molecular Liquids in 2022.Category: piperazines The following contents are mentioned in the article:

The thermodn. property of NE crystallization in 10 pure solvents was studied, and the solid-liquid equilibrium solubility of NE in these ten solvents was determined by laser dynamic method. The result showed that the solubility was proportional to the temperature Five models including the modified Apleblat model, λh model, Polynomial model, Van’t Hoff model, and Yaws model were adopted to fit the solubility of the solute in a single solvent, and the result showed that the Polynomial model had a high fitting degree for the solubility of NE in the single solvent chosen. The activity coefficients, as well as thermodn. properties of the mixing, were obtained and studied. The effect of solvents themselves on the solubility order of Nintedanib Esylate was also studied by correlating to the solubility of Nintedanib Esylate through the KAT-LSER model. What is more, by adopting Mol. Dynamic simulation, it was proved that the Nintedanib Esylate solubility in different solvents could be largely influenced by the interaction of the solute mols. and solvent mols. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Category: piperazines).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Category: piperazines

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

Nanostructured lipid carriers as oral delivery systems for improving oral bioavailability of nintedanib by promoting intestinal absorption was written by Zhu, Yunjing;Liang, Xue;Lu, Cong;Kong, Yihan;Tang, Xing;Zhang, Yu;Yin, Tian;Gou, Jingxin;Wang, Yanjiao;He, Haibing. And the article was included in International Journal of Pharmaceutics in 2020.HPLC of Formula: 656247-18-6 The following contents are mentioned in the article:

The aim of this study was to fabricate nanostructured lipid carriers, NLCs, of nintedanib (BIBF) to improve its oral bioavailability. Two types of NLCs loaded with BIBF (BIBF-NLCs-1 and BIBF-NLCs-2) were prepared by the melt-emulsification technique. BIBF-NLCs-1 and BIBF-NLCs-2 showed nanoscale particle sizes of 142.70 ± 0.85 nm and 7.99 ± 0.06 nm, and both were pos. zeta potential. Study on Caco-2 cells showed that BIBF-NLCs-1 exhibited distinct advantages at the cytol. level. The oral bioavailability of BIBF-NLCs-1 and BIBF-NLCs-2 was extremely improved 3.13-fold and 2.39-fold resp. compared with BIBF solution (BIBF-Sol). And in vivo anti-tumor efficiency study in mice bearing LLC lung tumor indicated that BIBF-NLCs-1 and BIBF-NLCs-2 had excellent tumor inhibition. Besides, the two NLCs did not increase the risk of liver damage and can even reduce the incidence of gastrointestinal irritation of BIBF to some extent. In summary, NLCs are a potential oral delivery system to improve the bioavailability of BIBF by promoting intestinal absorption. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6HPLC of Formula: 656247-18-6).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.HPLC of Formula: 656247-18-6

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

Development and validation of a UV-spectrophotometric method for the estimation of Nintedanib Esylate in bulk and its formulation was written by Patil, Rohan S.;Mahajan, Moreshwar P.. And the article was included in Research & Reviews: A Journal of Pharmaceutical Science in 2018.Name: (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate The following contents are mentioned in the article:

The present work represents a UV spectrophotometric method for the estimation of Nintedanib Esylate in pure and its formulation. Methanol was used as a solvent. Nintedanib Esylate exhibit absorption maxima at 391 nm. The developed method obeyed Beer-Lambert’s law in the concentration range of 3-18 μg/mL having a line equation Y = 0.065x + 0.001 with a correlation coefficient of 0.999. There is no interference from any pharmaceutical excipients. The precision of the method was determined by performing the intra-day study and inter-day study. The accuracy of the method was confirmed by recovery studies from capsules at three different levels by standard additions Results of the anal. were validated statistically and by recovery study. The anal. method was validated for various parameters as per ICH (International Conference on Harmonization) guidelines. The proposed method was found to be simple, rapid, accurate and precise and can be applied for the routine quality control studies for assay of Nintedanib Esylate in pure and its formulation. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Name: (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Name: (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate

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

The novel analytical method development and validation for related substances of Nintedanib Esylate by RP-HPLC method was written by Parmar, Yogendra B.;Shah, Dharmesh;Majmudar, Yashraj A.;Kaka, Ketul C.;Patel, Arpan S.;Kankad, Pankaj D.;Sartanpara, Uday G.. And the article was included in World Journal of Pharmaceutical Research in 2021.Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate The following contents are mentioned in the article:

An accurate, sensitive and rapid gradient reverse phase high performance liquid chromatog. (RP-HPLC) method has been developed and validated for related substances of Nintedanib Esylate. HPLC anal. was performed on YMC Triart, C18 (250 × 4.6) mm, 3μm. Column temperature maintained at 35°C conditions. Chromatog. separation was achieved with mobile phase gradient program at flow rate of 1.0mL/min. The injection volume was 10μl. The UV detection wavelength was 245nm. The method suitability was checked and validated according to the ICH guidelines Q2 (R1) for specificity, linearity, accuracy, precision, limit of quantification, limit of detection. Limit of detection of each impurity was found to be less than 0.031% weight/weight indicating that the developed method is highly sensitive. The calibration curve of each impurity was found to be linear within the concentration range of about 0.10μg/mL to 2.0μg /mL. The regression data for calibration curve shows good linear relationship. Correl coefficient (r²) of each impurity was found to be greater than 0.998. The Recovery was found to be accurate for each impurity within the spike concentration range of about 0.10μg/mL to 1.5μg /mL. The Recovery of each impurity was found to be between 80% to 120%. The experiment results are given in detail in this research article. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Safety of (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate

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