Category: 890092-19-0

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 μM. 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

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 μM. 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

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 p38α 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 p38α MAPK, for which a clear biol. function has yet to be identified is presented. The interactions of the ligands with p38α 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

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 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 μM. 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

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 μM. 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

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 p38α 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 p38α MAPK, for which a clear biol. function has yet to be identified is presented. The interactions of the ligands with p38α 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

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 April 18, 2019, Valenti, Dominick J.; Dey, Sanjeev K.; Qin, Haihu; Freund, Wesley A.; Miracle, Gregory S. published a patent.Name: 4-(4-Acetylpiperazin-1-yl)benzaldehyde The title of the patent was Leuco compounds for cleaning composition. And the patent contained the following:

Title compound comprises ≥1 of fluorescent moiety covalently bound to ≥1 of second moiety containing leuco moieties and chromophore moieties. Thus, a compound was prepared from a leuco moiety (synthesized from N-acetylpiperazine, 4-fluorobenzaldehyde, and diethanolaniline), and a fluorescent moiety of benzenesulfonic acid-derived sodium salt. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Name: 4-(4-Acetylpiperazin-1-yl)benzaldehyde

The Article related to leuco compound cleaning composition, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Fluorescent Brighteners and other aspects.Name: 4-(4-Acetylpiperazin-1-yl)benzaldehyde

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

On December 13, 2012, Aissaoui, Hamed; Boss, Christoph; Corminboeuf, Olivier; Heidmann, Bibia; Siegrist, Romain published a patent.Synthetic Route of 890092-19-0 The title of the patent was Piperazines as antimalarial agents. And the patent contained the following:

The invention relates to novel piperazine derivatives 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. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Synthetic Route of 890092-19-0

The Article related to piperazine compound preparation antimalarial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 890092-19-0

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