Month: November 2022

On April 28, 2022, Berlin, Michael; Crew, Andrew; Dong, Hanqing; Hornberger, Keith; Snyder, Lawrence; Wang, Jing; Zimmermann, Kurt published a patent.Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of bifunctional compounds and methods for the targeted degradation of androgen receptor protein. And the patent contained the following:

Bifunctional compounds e.g. I, which find utility as modulators of androgen receptor (AR), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds AR, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. Example I was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their androgen receptor modulatory activity (some data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to bifunctional preparation targeted degradation androgen receptor modulator anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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

On February 1, 2022, Zhang, Chen; Liao, Yuting; He, Ping; Chen, Xiaogang; Xuan, Zhaoli; Ye, Fei; Tang, Pingming; Wan, Songlin; Li, Yao; Ni, Jia; Yan, Pangke published a patent.COA of Formula: C15H29N3O2 The title of the patent was Preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. And the patent contained the following:

The present invention relates to preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. In particular, the BTK inhibitor ring derivative B-L-K (wherein, L = -Ak1-Cy1-Ak2-Cy2-Ak3-Cy3-Ak4-Cy4-Ak5-; Ak1 – Ak5 = CH2, O, -NRb0-, C=O, C=C or bond; Cy1 – Cy4 = optionally substituted 3-12 membered heterocycle, optionally substituted 3-12 membered cycloalkyl, optionally substituted 6-10 membered aryl, or bond; B = B1-W1-B2-B3-B4- or I, when B = B1-W1-B2-B3-B4-, Cy1, Cy2, Cy3, and Cy4 cannot be bonds at the same time; when B = B1-W1-B2-B3-B4-, and Ak1, Ak2, Ak3, Ak4 or Ak5 are not bonds, they cannot be directly connected to each other). Further, (B1 and B2 = optionally substituted 6-membered heteroaromatic ring or phenyl; W1 = -O-, -S-, -NH-, -NHCO- or -CONH-; B3 = optionally substituted heterocyclic ring; B4 = optionally substituted 4-7-membered monocycloalkyl, optionally substituted 6-12-membered spirocycloalkyl, optionally substituted 5-10-membered cycloalkyl derivative etc.; B5 or B6 = optionally substituted Ph or 5-6-membered heteroaryl; Rb6 = H, C1-4 alkyl, halogen-substituted C1-4 alkyl or hydroxy-substituted C1-4 alkyl; Rb7 and Rb8 = H, F, Cl, Br, I, OH, NH2, CN, CF3, -C(=O)NH2 etc.; m = 0, 1 or 2; K = heterocyclic group, cycloalkyl carbonyl-group, aralkyl carbonyl-group etc.) or stereoisomer, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof were prepared The inventive BTK inhibitor cyclic derivatives are useful for treating BTK-related diseases such as tumors or autoimmune system diseases. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2

The Article related to azaheterocyclic compound preparation btk inhibitor antitumor autoimmune disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

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

On August 31, 2006, Kauffman, Goss Stryker; Li, Chao; Lippa, Blaise Scott; Morris, Joel; Pan, Gonghua published a patent.Safety of 4-Ethyl-piperazine-1-carbonyl chloride The title of the patent was Preparation of bicyclic heteroaromatic derivatives as anticancer agents. And the patent contained the following:

The title compounds I [X, Z, V and W = N or CR1 (R1 = H, halo, CN, etc.); R4 = H, alkyl, (CR11R12)t(aryl), (CR11R12)t(4-10 membered heterocyclyl); R5 = H, alkyl, or R4 and R5 are taken together to form an oxo moiety; R6 and R7 are taken together to form a 4-10 membered (bi)cyclic or hetero(bi)cyclic ring system; B represents a fused 5-6 membered aromatic ring containing 0-2 heteroatoms; with provisos], useful for treating abnormal cell growth in mammals (no specific data given), were prepared Thus, reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine with tert-Bu 5-chloro-1,2-dihydro-1’H-spiro[indole-3,4′-piperidine]-1′-carboxylate followed by deprotection afforded II. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds I and to pharmaceutical compositions for treating such disorders which contain the compounds I. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Safety of 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to bicyclic heteroaromatic pyrrolopyrimidine pyrazolopyrimidine spiroindolepiperidine preparation antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 4-Ethyl-piperazine-1-carbonyl chloride

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

On December 12, 2019, Beri, Aashima; Kaur, Rupinder; Banipal, Parampaul K.; Banipal, Tarlok S. published an article.Electric Literature of 86393-32-0 The title of the article was Expliciting the {Ciprofloxacin Hydrochloride + (Glycine/L-Isoleucine)} Interactions in Aqueous Solution over the Temperature range T = 288.15-323.15 K and at Pressure p = 1 × 105 Pa: Volumetric, Acoustic, Calorimetric, and Absorption studies. And the article contained the following:

Like the drug-salt interactions, drug-amino acid interaction in the aqueous medium is dependent upon different physiol. events occurring in the body. In this context, investigations on the interactions of ciprofloxacin hydrochloride (CFX) being a second-generation antibiotic with both nonessential amino acid and essential amino acid have been done. The physicochem. properties like apparent molar volume (V2,ϕ) and apparent molar isentropic compression (Ks,2,ϕ) of drug, CFX in water and in the presence of glycine (GLY), and L-isoleucine (ILU) at mB (molality of GLY or ILU) = 10, 20, 35, 50, and 75 mmol·kg-1 have been determined over the temperature range of 288.15-323.15 K and at p = 1 × 105 Pa. These data have further been used to calculate different parameters, which help to obtain valuable information corresponding to the distinct kinds of interactions present in the ternary systems. The volumes and compressibility studies have shown that the predominant interactions are hydrophilic-hydrophilic and hydrophilic-ionic in the studied systems. It may be postulated that the effect of CFX prevails through the hydrophilic groups of the constituents of proteins. Dehydration behavior of drug is also observed using hydration number and calorimetry at higher mB values. Both hyperchromic and hypsochromic changes have been observed from the absorption spectra for the CFX/ILU system. 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).Electric Literature of 86393-32-0

The Article related to volumetric calorimetric property ciprofloxacin hydrochloride glycine isoleucine aqueous mixture, Phase Equilibriums, Chemical Equilibriums, and Solutions: Nonelectrolytic Solutions and other aspects.Electric Literature of 86393-32-0

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

On June 30, 1985, Takeuchi, Isao; Sugiura, Michiharu; Yamamoto, Kazuko; Ito, Tomiyoshi; Hamada, Yoshiki published an article.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Syntheses and antimicrobial activities of cis-1-[2-phenyl-4-(phenoxy or phenylthio)methyl-1,3-dioxolan-2-ylmethyl]-1H-imidazole derivatives. And the article contained the following:

Substitution reactions of glycerol ketals I (R, R1 = H, MeO; Br, Br; Cl, Cl) with heterocycles gave II (R2 = 1-imidazolyl, 1-pyrazolyl, 1,2,4-triazol-1-yl) which underwent successive saponification, mesylation, and substitution reaction with R3R4C6H3XH (R3, R4 = H, MeO, Cl, Me, Br; X = O, S) to give ketoconazole analogs III. Antimicrobial test of the synthesized compounds III (R2 = 1-imidazolyl; R, R1, R3, R4, X = Cl, Cl, H, 4-Cl, S; Cl, Cl, 2-Cl, 6-Cl, S; Br, Br, 2-Cl, 6-Cl, S) showed strong antimicrobial activities against Penicillium chrysogenum and Trichophyton rubrum. Most compounds synthesized had strong preventive effects against downy mildew and sheath blight. Triazole derivatives III (R2 = 1-triazolyl; R = R1 = Cl; R3 = H, 2-Cl; R4 = Cl; X = S, O) showed similar effects against not only such diseases but gray mold rot. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to ketoconazole analog preparation bactericide fungicide, dioxolanylmethylimidazole phenoxy phenylthio, Heterocyclic Compounds (More Than One Hetero Atom): Dioxoles, Oxathioles, Dithioles and other aspects.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On June 9, 2022, Banipal, Tarlok S.; Kaur, Sandeep; Beri, Aashima; Banipal, Parampaul K. published an article.Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Elucidation of Interactions between Ciprofloxacin Hydrochloride Monohydrate and Constituents of Nucleic Acids in Aqueous Solutions at Different Temperatures. And the article contained the following:

The interaction of drugs with nucleic acids is one of the most essential parts of biol. research in the drug discovery and pharmaceutical development processes. Furthermore, physicochem. studies of the solution behavior of such systems are extremely desirable to elucidate the various interactions in aqueous solutions So, in this context, measurements of d. (ρ), speed of sound (u), viscosity (η) and enthalpy of dilution (q) for uracil, thymine, uridine, and thymidine in water and in aqueous solutions of ciprofloxacin hydrochloride monohydrate (Cfx) at mB (molality of Cfx in water) = (5, 10, 15, 20, 25) mmol·kg-1 across the temperature range T = (288.15 to 318.15) K and at p = 1 x 105 Pa were performed. Further, these data were utilized to evaluate partial molar volumes, partial molar isentropic compressions, viscosity B-coefficients, standard molar enthalpy of dilution, and their corresponding transfer parameters (ΔtrV2,Φ0, ΔtrKs,2,Φ0, ΔtrB and ΔtrΔdilH°). These properties were used to elucidate the presence of solute-solvent interactions. The solute-Cfx interactions are exothermic in nature, according to calorimetry studies. Furthermore, the UV-visible studies show that the interactions between the pyrimidine based mols. and drug result in shift in wavelength (λ) as well as change in absorption. 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).Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to elucidation interactions ciprofloxacin hydrochloride monohydrate, constituent nucleic acid aqueous solution, Phase Equilibriums, Chemical Equilibriums, and Solutions: Nonelectrolytic Solutions and other aspects.Safety of 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 May 27, 2010, Aissaoui, Hamed; Boss, Christoph; Corminboeuf, Olivier; Frantz, Marie-Celine; Grisostomi, Corinna published a patent.HPLC of Formula: 890092-19-0 The title of the patent was Novel bis-amides as antimalarial agents and their preparation and use in the treatment of protozoal infections. And the patent contained the following:

The invention relates to bis-amide derivatives of formula I and their use as active ingredients in the preparation of pharmaceutical compositions The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. Compounds of formula I wherein R1 is (un)substituted aryl and (un)substituted heteroaryl; R2 is (un)substituted aryl and (un)substituted heteroaryl: R3 is (un)substituted aryl and (un)substituted heteroaryl; R4R5 together with the N they are attached form morpholinyl, 2,3-dihydroindolinyl, 1,3-dihydroisoindolinyl, etc.; when R4 is H and C1-4 alkyl, then R5 is 1-benzylpyrrolidin-3-yl and 1-azabicyclo[2.2.2]oct-3-yl; when R4 is C1-4 alkyl then R5 is hydroxyethyl, alkoxyethyl, aminoethyl, etc.; and salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their antimalarial activity. From the assay, it was determined that compound II exhibited an IC value of 5 nM. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).HPLC of Formula: 890092-19-0

The Article related to bis amide preparation antimalarial treatment protozoal infection, Aliphatic Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.HPLC of Formula: 890092-19-0

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

On March 15, 2005, Liu, Yong; Wang, Jingkang; Yin, Qiuxiang 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 The crystal habit of ciprofloxacin hydrochloride monohydrate crystal. And the article contained the following:

Crystals with two different habits (e.g. needle-like and plate-like) of ciprofloxacin hydrochloride monohydrate (CPFX) were prepared from aqueous solution by varied methods. These crystals were identified by various means such as scanning electron microscope (SEM), DSC, TG, and x-ray powder diffraction (XRPD). According to the anal. of crystals by DSC, TG and XRPD, it is concluded that CPFX crystals produced in cooling or dilution crystallization experiment should have the same crystal structure. Using the XRPD data, the unit cell parameters were calculated by software TREOR90. Systematic absence and statistics of reflexion indicate that CPFX crystals in this work have a high possibility of being the space group P21/c. The crystal habit transition was observed in the salting-out crystallization when 0.2M KCl solution works as precipitant. 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 hydrochloride hydrate crystal morphol structure, Crystallography and Liquid Crystals: Crystal Morphology (Habit), Orientation, Crystallinity 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 February 6, 2015, Fujimoto, Teppei; Ritter, Tobias published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was PhenoFluorMix: Practical Chemoselective Deoxyfluorination of Phenols. And the article contained the following:

A practical deoxyfluorination with novel deoxyfluorinating reagent PhenoFluorMix, a mixture of N,N’-1,3-bis(2,6-diisopropylphenyl)chloroimidazolium chloride and CsF, is presented. PhenoFluorMix overcomes the challenges associated with hydrolysis of PhenoFluor. PhenoFluorMix does not hydrolyze, is readily available on decagram scale, and is storable in air. In this paper, we demonstrate the practicality of the reagent and exhibit the deoxyfluorination of a variety of phenols and heterocycles. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to aryl halide chemoselective synthesis, phenol heterocycle deoxyfluorination phenofluormix, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Halides and Halonium Compounds and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On August 24, 2007, Yagneskumar, Trivedi Amit; Pandurang, Gaitonde Shrikant; Anant, Shrikhande Atul; Pravichandra, Mehta Bharat published a patent.Application In Synthesis of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the patent was Preparation methodology of piperazinylquinolones as antibacterial agents. And the patent contained the following:

The invention relates to the methodol. of reacting halogenated quinolinones with piperazine derivatives in a chem. system comprising of alkali salts of aromatic acids and a ternary mixture of (alkyl)pyridine, polar solvent represented by hydrophobic alkanols or DMSO, and N,N-dimethylglyoxime or biacetyl. Quinolinones reacted in this way with even equimolar of piperazines, good yields of the products were achieved. Another innovation is achieved by the use of moistured piperazines, including recycling of the unreacted piperazine solution in pyridine with substantial presence of water by adding dialkylsulfosuccinate , which has a surprisingly beneficial effect to the process. Example compound I•HCl•H2O (ciprofloxacin) was prepared by N-arylation of piperazine with 1-cyclopropyl-7-chloro-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. 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).Application In Synthesis of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to piperazinyl quinolone preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Application In Synthesis of 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