Category: 890092-19-0

On August 11, 1998, De Laszlo, Stephen E.; Liverton, Nigel J.; Ponticello, Gerald S.; Selnick, Harold G.; Mantlo, Nathan B. published a patent.Electric Literature of 890092-19-0 The title of the patent was Preparation of arylpyrroles as cytokine inhibitors. And the patent contained the following:

Title compounds [I; R1 = H, alkyl, heterocyclyl, aryl, etc.; R2 = alk(en)yl, alkynyl, heterocyclyl, etc.; R3 = H, halo, alkyl, heterocyclyl, etc.; R4 = (un)substituted heteroaryl; R5 = ZR; R = 1-3 of halo, alkyl, acyl, (hetero)aryl, etc.; Z = (hetero)arylene] were prepared Thus, R5COCH2R4 (R4 = 4-pyridyl, R5 = 4-FC6H4) was α-alkylated by ClCH2COR2 (R2 = 1-benzyloxycarbonyl-4-piperidinyl)(preparation each given) and the product cyclocondensed with NH4Ac to give, after reduction, I (R1 = R3 = H, R2 = 1-methyl-4-piperidinyl, R4 = 4-pyridyl, R5 = 4-FC6H4). Data for biol. activity of I were given. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Electric Literature of 890092-19-0

The Article related to arylpyrrole preparation cytokine inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 890092-19-0

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

On August 11, 1998, De Laszlo, Stephen E.; Liverton, Nigel J.; Ponticello, Gerald S.; Selnick, Harold G.; Mantlo, Nathan B. published a patent.Electric Literature of 890092-19-0 The title of the patent was Preparation of arylpyrroles as cytokine inhibitors. And the patent contained the following:

Title compounds [I; R1 = H, alkyl, heterocyclyl, aryl, etc.; R2 = alk(en)yl, alkynyl, heterocyclyl, etc.; R3 = H, halo, alkyl, heterocyclyl, etc.; R4 = (un)substituted heteroaryl; R5 = ZR; R = 1-3 of halo, alkyl, acyl, (hetero)aryl, etc.; Z = (hetero)arylene] were prepared Thus, R5COCH2R4 (R4 = 4-pyridyl, R5 = 4-FC6H4) was α-alkylated by ClCH2COR2 (R2 = 1-benzyloxycarbonyl-4-piperidinyl)(preparation each given) and the product cyclocondensed with NH4Ac to give, after reduction, I (R1 = R3 = H, R2 = 1-methyl-4-piperidinyl, R4 = 4-pyridyl, R5 = 4-FC6H4). Data for biol. activity of I were given. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Electric Literature of 890092-19-0

The Article related to arylpyrrole preparation cytokine inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 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

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

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

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 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

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

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

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