Tag: 200-300

On October 24, 2013, McLure, Kevin G.; Young, Peter R. published a patent.HPLC of Formula: 890092-19-0 The title of the patent was Preparation of quinazolin-4(3H)-one derivatives and for the treatment of diseases by epigenetic regulation. And the patent contained the following:

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. Title compounds I [Q and V independently = CH or N; Ra1 and Ra3 independently = H, alkyl,alkoxy, halogen, amino, amide, hydroxy, heterocycle, or cycloalkyl; Rb2 and Rb6independently = H; Rb3 and Rb5 independently = H, halogen, alkyl, alkoxy, cycloalkyl,hydroxy, or amino; W = C or N; Z = O, S, S(O), SO2; R3, R4, and R5 independently = H, alkyl,alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, aryloxy, etc.], and their stereoisomers, tautomers, pharmaceutically acceptable salts, or hydrates, are prepared and disclosed. Thus, e.g., II was prepared by reaction of 5,7-dimethoxy-2-[4-(piperazin-1-yl)phenyl]quinazolin-4(3H)-one with 2-bromoethanol. Compounds of the invention showed tetra-acetylated histone H4 binding individual BET bromodomains and had an IC50 value less than 50 渭M. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor. 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 preparation epigenetic regulation bet protein, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 890092-19-0

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

On November 28, 2013, Mclure, Kevin G.; Young, Peter Ronald published a patent.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde The title of the patent was Preparation of quinazolin-4(3H)-one derivatives and for the treatment of diseases by epigenetic regulation. And the patent contained the following:

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. Title compounds I [Q and V independently = CH or N; Ra1 and Ra3 independently = H, alkyl,alkoxy, halogen, amino, amide, hydroxy, heterocycle, or cycloalkyl; Rb2 and Rb6independently = H; Rb3 and Rb5 independently = H, halogen, alkyl, alkoxy, cycloalkyl,hydroxy, or amino; W = C or N; Z = O, S, S(O), SO2; R3, R4, and R5 independently = H, alkyl,alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, aryloxy, etc.], and their stereoisomers, tautomers, pharmaceutically acceptable salts, or hydrates, are prepared and disclosed. Thus, e.g., II was prepared by reaction of 5,7-dimethoxy-2-[4-(piperazin-1-yl)phenyl]quinazolin-4(3H)-one with 2-bromoethanol. Compounds of the invention showed tetra-acetylated histone H4 binding individual BET bromodomains and had an IC50 value less than 50 渭M. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

The Article related to preparation epigenetic regulation bet protein, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

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

Mrachkovskaya, L. B.; Turchin, K. F.; Yakhontov, L. N. published an article in 1975, the title of the article was Reduction fragmentation of 4-methyl-1-piperazinylmethylidenemalonate.Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride And the article contains the following content:

Di-Et 4-methyl-1-piperazinylmethylidenemalonate (I), prepared in 83.5% yield from 1-methylpiperazine (II) and EtOCH:C(CO2Et)2, was reductively cleaved by NaBH4 in absolute EtOH at 20-5掳 to give 65% of a mixture of II and methylmalonic acid (III). Analogous reduction in dioxane gave 11% II-III and in cyclohexane 5% II-III were obtained. Similar results were obtained by catalytic reduction with Pt. The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

The Article related to reduction cleavage piperazinylmethylenemalonic acid, pyruvoyl hydrazone reaction hydrazide, triazole acetyl anilino, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines and other aspects.Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

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

Mrachkovskaya, L. B.; Anisimova, O. S.; Turchin, K. F.; Yakhontov, L. N. published an article in 1976, the title of the article was Formation of the bis(N-methylpiperazide) of monothiooxalic acid from 3-(N-methylpiperazinyl)propionic acid under conditions of the Zelinsky reaction.Formula: C8H18Cl2N2O2 And the article contains the following content:

The title compound I was obtained from piperazinepropionic acid (II) by boiling 2 hr with SOCl2, 2 hr with Br-CHCl3, and 5 hr with EtOH. The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Formula: C8H18Cl2N2O2

The Article related to piperazine thiooxalylbismethyl, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines and other aspects.Formula: C8H18Cl2N2O2

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

On June 27, 2013, Fauber, Benjamin; Rene, Olivier published a patent.Formula: C13H16N2O2 The title of the patent was Preparation of benzylsulfonamide derivatives as RORγ modulators for treatment of arthritis. And the patent contained the following:

The title compounds I [m = 0-4; n = 0-2; X1-4 = N or CRa, wherein Ra = independently H, cyano, C1-5 alkyl, etc.; R1 = independently C1-6 alkyl, halo, C1-6 alkoxy, etc.; R2 = C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-6 alkyl, etc.; R3a-3b, R4a-4b= independently H or C1-6 alkyl; A = P1, P2 or NR11R12; wherein Y = CR13 or N; Z = O, S(O)x, CR14R15, or NR16; Q = CH2, CO, C(O)NH, etc.; p = 1 or 2; q = 1-3; x = 0-2; Rb, R14 = H, C1-6 alkyl or halo; Rc = H, C1-6 alkyl, halo, etc.; R11, R13 = H or C1-6 alkyl; R12 = C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl-C1-6 alkyl; R15 = H, C1-6 alkyl, C3-6 cycloalkyl, etc.; R16 = H, C1-6 alkyl, C3-6 cycloalkyl, etc.] or pharmaceutically acceptable salts thereof were prepared Compounds I are retinoid-related orphan receptor gamma (RORγ) modulators and useful for treatment of inflammatory diseases such as arthritis. Compound II was prepared in a multi-step synthesis and displayed IC50 of 0.006 μM for RORc affinity. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Formula: C13H16N2O2

The Article related to benzylsulfonamide preparation ror gamma modulator arthritis treatment, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Others and other aspects.Formula: C13H16N2O2

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 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 July 15, 2008, Irie, Osamu; Ehara, Takeru; Iwasaki, Atsuko; Yokokawa, Fumiaki; Sakaki, Junichi; Hirao, Hajime; Kanazawa, Takanori; Teno, Naoki; Horiuchi, Miyuki; Umemura, Ichiro; Gunji, Hiroki; Masuya, Keiichi; Hitomi, Yuko; Iwasaki, Genji; Nonomura, Kazuhiko; Tanabe, Keiko; Fukaya, Hiroaki; Kosaka, Takatoshi; Snell, Christopher R.; Hallett, Allan published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Discovery of selective and nonpeptidic cathepsin S inhibitors. And the article contained the following:

Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an inhouse pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to arylmethylpyrrolopyrimidinecarbonitrile preparation cathepsin s inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On February 8, 2018, Hou, Jinqiang; Kovacs, Michael S.; Dhanvantari, Savita; Luyt, Leonard G. published an article.HPLC of Formula: 67914-60-7 The title of the article was Development of Candidates for Positron Emission Tomography (PET) Imaging of Ghrelin Receptor in Disease: Design, Synthesis, and Evaluation of Fluorine-Bearing Quinazolinone Derivatives. And the article contained the following:

Mol. imaging with positron emission tomog. (PET) is an attractive platform for noninvasive detection and assessment of disease. The development of a PET imaging agent targeting the ghrelin receptor (growth hormone secretagogue receptor type 1a or GHS-R1a) has the potential to lead to the detection and assessment of the higher than normal expression of GHS-R1a in diseases such as prostate, breast, and ovarian cancer. To enable the development of 18F radiopharmaceuticals, we have designed and synthesized three series of quinazolinone derivatives, resulting in the identification of two compound with subnanomolar binding affinity and one fluorine-bearing compound I with picomolar binding affinity (20 pM), representing the highest binding affinity for GHS-R1a reported to date. Two lead compounds (II, IC50 = 20.6 nM; III, IC50 = 9.3 nM) were successfully 18F-radiolabeled with radiochem. purity of greater than 99%. Mol. modeling studies were performed to shed light on ligand-receptor interactions. 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 quinazolinone fluorine bearing preparation ghrelin receptor pet imaging, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 67914-60-7

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

Buhrmann, Mike; Wiedemann, Bianca M.; Muller, Matthias P.; Hardick, Julia; Ecke, Maria; Rauh, Daniel published an article in 2017, the title of the article was Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38伪 MAPK.COA of Formula: C13H16N2O2 And the article contains the following content:

In protein kinase research, identifying and addressing small mol. binding sites other than the highly conserved ATP-pocket are of intense interest because this line of investigation extends our understanding of kinase function beyond the catalytic phosphotransfer. Such alternative binding sites may be involved in altering the activation state through subtle conformational changes, control cellular enzyme localization, or in mediating and disrupting protein-protein interactions. Small organic mols. that target these less conserved regions might serve as tools for chem. biol. research and to probe alternative strategies in targeting protein kinases in disease settings. Here, the structure-based design and synthesis of a focused library of 2-arylquinazoline derivatives to target the lipophilic C-terminal binding pocket in p38伪 MAPK, for which a clear biol. function has yet to be identified is presented. The interactions of the ligands with p38伪 MAPK was analyzed by SPR measurements and validated by protein X-ray crystallog. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).COA of Formula: C13H16N2O2

The Article related to arylquinazoline preparation crystallization p38 map kinase ligand, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C13H16N2O2

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