Month: November 2022

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

On April 22, 2021, Berlin, Michael; Dong, Hanqing; Sherman, Dan; Snyder, Lawrence; Wang, Jing; Zhang, Wei published a patent.COA of Formula: C15H29N3O2 The title of the patent was Bifunctional molecules containing an E3 ubiquitin ligase binding moiety linked to a BCL6 targeting moiety and their preparation. And the patent contained the following:

Bifunctional compounds of formula I, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. Bifunctional compounds of formula I wherein ULM is a small E3 ubiquitin ligase binding moiety that bonds Von Hippel-Lindau, cereblon; PTM is a small mol. comprising a B-cell lymphoma 6 protein targeting moiety; L is a bond and a chem. linker; pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, and polymorphs thereof, are claimed. The bifunctional compounds of the disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the disclosure. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their BCL6 protein degradation activity (some data given). 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 bifunctional mol preparation bcl6 protein degrader, 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 March 15, 2007, Silverman, Lisa S.; Caldwell, John P.; Greenlee, William J.; Kiselgof, Eugenia; Matasi, Julius J.; Tulshian, Deen B.; Arik, Leyla; Foster, Carolyn; Bertorelli, Rosalia; Monopoli, Angela; Ongini, Ennio published an article.Formula: C12H16N2O2 The title of the article was 3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists. And the article contained the following:

A novel series of 3-substituted-8-aryl-[1,2,4]triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochem. properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound I (R = MeOCH2CH2O) displayed both superior in vitro and highly promising in vivo profiles. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to triazolopurinamine preparation adenosine a2a antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C12H16N2O2

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

On October 8, 2020, Yang, Bin; Hayhow, Thomas George Christopher; Fallan, Charlene; Scott, James Stewart; Diene, Coura; Barlaam, Bernard Christophe; Nissink, Johannes Wilhelmus Maria published a patent.Application of 1211568-27-2 The title of the patent was Pyrimidinyltetrahydropyridoindoles as estrogen receptor degrading PROTACs and their preparation. And the patent contained the following:

The specification relates to compounds of formula I and pharmaceutically acceptable salts thereof. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them. Compounds of formula I wherein A and G are independently CR5 and N; E and Q are independently CH and N; R1 and R2 are H; R1R2 can be taken together to form oxo; R3 and R4 are independently H and OMe; R5 is H, F, Cl, CN, Me and OMe; R6 and R7 are independently H, Me and F; R6R7 can be taken together to form cyclopropyl and oxetanyl; R8 is H, Me, F, CH2F, CN, etc.; Linker is (un)substituted. (un)branched, (un)cyclized, (un)saturated 6 to 15 carbon atom moiety where 1 ot 6 carbon atoms may optionally be replaced with O, N and S; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen binding affinity and estrogen degradation activity. From the assay, it was determined that compound II exhibited IC50 values of 3.1 nM and 1.1 nM toward ER binding and ER degradation, resp. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Application of 1211568-27-2

The Article related to pyrimidinylpyridoindole preparation er degrading protac, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1211568-27-2

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

On June 2, 2022, Zhang, Chen; Liao, Yuting; Ye, Fei; Tang, Pingming; Chen, Xiaogang; Lu, Yonghua; Gao, Qiu; Li, Yao; Ni, Jia; Yan, Pangke published a patent.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Benzene ring derivative, and composition and pharmaceutical use thereof. And the patent contained the following:

Disclosed are a compound or a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, and an intermediate thereof, and the use thereof in AR or AR splicing mutant-related diseases such as cancer. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to benzene ring derivative preparation treatment cancer disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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

On March 17, 2022, Ryu, Hyung-Chul; Kim, Jae-Sun; Lim, Jee-Woong; Lee, Ju Young; Choi, Kwanghyun; Rajesh, Rengasamy; Chang, Duk-Ho; Gwon, Hyeok Jun; Kang, Hyo Jin published a patent.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of pyrimidinamine derivatives for suppressing EGFR mutant cancer and pharmaceutical use thereof. And the patent contained the following:

The invention relates to pyrimidinamine derivatives of formula I, pharmaceutically acceptable salts, or pharmaceutical compositions thereof which have the activity of inhibiting and/or degrading mutant EGFR protein and are useful for the treatment or prevention of cancer with EGFR mutation, especially lung cancer. The present disclosure also provides a method for the treatment or prevention of EGFR mutation cancer, especially lung cancer, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing same to a subject in need of treatment. Compounds of formula I wherein R1 and R2 are independently H, (halo)alkyl, or trideuteromethyl; R3 – R6 are independently H, halo, cyano, (halo)alkyl, (halo)alkoxy, etc.; m and n are independently 0-4; A is heterocyclyl; L is a connecting group through covalent bond; B is Q1 or Q2; X is single bond, (CH2)1-6, O-(CH2)0-6, C(O)-(CH2)0-6, N(R13)-(CH2)0-6, C(O)-N(R13)-(CH2)0-6, N(R13)-C(O)-(CH2)0-6, etc.; W is C(R14)2 or C(O); R8 is H, hydroxy, halo, (halo)alkyl, or (halo)alkoxy; R9 and R10 are independently H or alkyl; R13 and R14 are independently H or alkyl; o and p are independently 1-3; Y is (halo)alkyl, aryl, etc.; Z is O or S; R11 is H, alkyl, or (CH2)1-6-C(O); R12 is H, alkyl, or cycloalkyl; are claimed. The invention compounds were evaluated for the EGFR protein degradation activity (biol. data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to pyrimidinamine derivative preparation egfr mutant lung cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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 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

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