Tag: 300-400

On May 8, 2008, Shapiro, Gideon; Moncuso, John; Pierre, Tessier; Leit, Silvana; Deziel, Robert; David, Smil; Richard, Chesworth; Chantigny, Yves Andre; Patrick, Beaulieu published a patent.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the patent was Preparation of tricyclic hydroxamic acids as inhibitors of histone deacetylase. And the patent contained the following:

The title compounds I [Z = N(R1)OR2, H; L = a bond, N(OR2); when L = N(OR2), Z = H; when Z = H, L = N(OR2); R1, R2 = H, alkyl, aryl, etc.; J = a bond, :CH-, alkyl, alkyl(heteroalkyl)alkyl, etc.; Q = diazepine, pyrrolidine, diazabicyclo[3.3.1]nonane, etc.; B = dibenzo[b,f][1,4]oxazepine, benzo[b]pyrido[2,3-e][1,4]diazepine, benzo[f]thieno[2,3-b][1,4]oxazepine, etc.;], useful for the inhibition of histone deacetylase, were prepared E.g., a 3-step synthesis of II, starting from 10,11-dihydrodibenz[b,f][1,4]oxazepin-11-one, was given. All exemplified compounds I have an IC50 of ≤ 10 μM against one of more of HDAC-1 through HDAC-11 (data for representative compounds I were given). Pharmaceutical composition comprising the compound I and methods of treating polyglutamine (polyQ) expansion diseases such as Huntington’s disease, are disclosed. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to tricyclic hydroxamic acid preparation histone deacetylase hdac inhibitor, huntington’s disease treatment tricyclic hydroxamic acid preparation hdac inhibitor, dibenzoxazepine preparation histone deacetylase hdac inhibitor dentatorubralpallidoluysian atrophy treatment and other aspects.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 15, 2015, Yamashita, Hiroko; Demizu, Yosuke; Misawa, Takashi; Shoda, Takuji; Kurihara, Masaaki published an article.Application In Synthesis of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the article was Synthesis of a bis-cationic α,α-disubstituted amino acid (9-amino-bispidine-9-carboxylic acid) and its effects on the conformational properties of peptides. And the article contained the following:

A new bis-cationic cyclic amino acid, 9-amino-3,7-diazabicyclo[3.3.1]nonane-9-carboxylic acid (9-amino-bispidine-9-carboxylic acid = Abp), which is available for both solution phase and solid phase peptide synthesis, was designed and synthesized. Furthermore, a heterotripeptide Cbz-Leu-Abp-Ala-OMe containing Abp was prepared, and its dominant conformation was analyzed by examining its NMR and IR spectra and performing mol. modeling. The tripeptide Cbz-Leu-Abp-Ala-OMe formed a β-turn structure as its preferred conformation in solution The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Application In Synthesis of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to peptide amino bispidine synthesis conformation nmr ir, amino acid disubstituted amino bispidine synthesis, piperidone cyclocondensation benzylamine paraformaldehyde hydantoin bucherer berg cyclization, hydrolysis protection peptide coupling conformation mol modeling and other aspects.Application In Synthesis of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 1, 2021, Pettersson, Pontus; Patrick, Joan; Jakob, Mario; Jacobs, Malte; Kloesgen, Ralf Bernd; Wennmalm, Stefan; Maeler, Lena published an article.Related Products of 79642-50-5 The title of the article was Soluble TatA forms oligomers that interact with membranes: Structure and insertion studies of a versatile protein transporter. And the article contained the following:

The twin-arginine translocase (Tat) mediates the transport of already-folded proteins across membranes in bacteria, plants and archaea. TatA is a small, dynamic subunit of the Tat-system that is believed to be the active component during target protein translocation. TatA is foremost characterized as a bitopic membrane protein, but has also been found to partition into a soluble, oligomeric structure of yet unknown function. To elucidate the interplay between the membrane-bound and soluble forms we have investigated the oligomers formed by Arabidopsis thaliana TatA. We used several biophys. techniques to study the oligomeric structure in solution, the conversion that takes place upon interaction with membrane models of different compositions, and the effect on bilayer integrity upon insertion. Our results demonstrate that in solution TatA oligomerizes into large objects with a high degree of ordered structure. Upon interaction with lipids, conformational changes take place and TatA disintegrates into lower order oligomers. The insertion of TatA into lipid bilayers causes a temporary leakage of small mols. across the bilayer. The disruptive effect on the membrane is dependent on the liposome’s neg. surface charge d., with more leakage observed for purely zwitterionic bilayers. Overall, our findings indicate that A. thaliana TatA forms oligomers in solution that insert into bilayers, a process that involves reorganization of the protein oligomer. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Related Products of 79642-50-5

The Article related to arabidopsis soluble tata structure oligomer cell membrane, chemical crosslinking, circular dichroism, electron microscopy, fluorescence correlation spectroscopy, light scattering, membrane insertion, membrane leakage, oligomer, twin-arginine translocase, vesicles and other aspects.Related Products of 79642-50-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Pastor-Nieto, Maria A.; Gatica-Ortega, Maria E.; Sanchez-Herreros, Consuelo; Vergara-Sanchez, Aranzazu; Martinez-Mariscal, Jaime; De Eusebio-Murillo, Esther published an article in 2021, the title of the article was Sensitization to benzyl salicylate and other allergens in patients with frontal fibrosing alopecia.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate And the article contains the following content:

Contact sensitization is frequent among patients with frontal fibrosing alopecia (FFA) (52%-76%). To evaluate the frequency of sensitization/photosensitization in an FFA population. A population of FFA patients were patch tested (Spanish Contact Dermatitis Research Group [GEIDAC] baseline; cosmetic and fragrance series), and photopatch tested (sunscreen series). Thirty-six patients (mean age: 64.6 years; 35/36: women) were studied. A history of dermatitis was recorded in 69.4% (frequently involving the face). Overall, 80.5% patients showed pos. patch-test reactions. The most frequently pos. allergens were nickel sulfate (25%), benzyl salicylate (22%), gallates (16.6%), propolis (16.6%), and limonene hydroperoxides (13.8%). Benzyl salicylate was likely relevant to the dermatitis (labeled on personal care products and most patients reporting clin. improvement with allergen avoidance). Patch tests with sunscreens showed pos. reactions to 11 materials (five patients). Photopatch tests were pos. in one case. We speculate a possible relationship between sensitization to benzyl salicylate and FFA. Hypothetically, the most likely explanation is that sensitization to benzyl salicylate involving FFA patients is a consequence of increased exposure to it. It is unclear whether allergen avoidance may impact the prognosis of alopecia. However, it seems to significantly improve the patients quality of life by lessening dermatitis and pruritus. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

The Article related to benzyl salicylate allergen sensitization human frontal fibrosing alopecia, allergic contact dermatitis, benzyl salicylate (cas number 118-58-1), fragrance, frontal fibrosing alopecia, gallates, patch tests, photopatch tests, propolis, scarring alopecia, sunscreen and other aspects.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 27, 2020, Crew, Andrew P.; Dong, Hanqing; Berlin, Michael; Sparks, Steven M. published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of proteolysis targeting chimeric (PROTAC) compounds with E3 ubiquitin ligase binding activity and targeting α-synuclein protein for treating neurodegenerative diseases. And the patent contained the following:

The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. A bifunctional compounds I [ULM-L-PTM; wherein the ULM = a small mol. E3 ubiquitin ligase binding moiety; the PTM = a small mol. comprising a α-synuclein protein targeting moiety; and the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, were disclosed. E.g., a multi-step synthesis of II, starting from 2-(2-benzyloxyethoxy)ethanol and tert-Bu 2-bromoacetate, was described. Targeted degradation of sarkosyl insoluble (SI) α-synuclein via exemplary bifunctional compounds I was assessed by MJFF-14-6-4-2 conformation specific ELISA following treatment of PFF-induced A53T α-synuclein overexpressing HEK293 cells with 1μM exemplary compound compared to DMSO vehicle control (data given for representative compounds I). Diseases or disorders that result from aggregation or accumulation of the target protein are α-synucleinopathies or neurodegenerative diseases associated with α-synuclein accumulation and aggregation, such as e.g., Parkinson disease, Alzheimer’s disease, dementia, dementia with Lewy bodies or multiple system atrophy, in particular Parkinson’s disease. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Category: esters-buliding-blocks

The Article related to proteolysis targeting chimeric protac bifunctional compound preparation protein degradation, sarkosyl insoluble alpha synuclein targeted degradation bifunctional compound preparation, alpha synucleinopathy neurodegenerative disease treatment bifunctional compound preparation and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 8, 1996, Patel, Dinesh V.; Gordeev, Mikhail F.; Gordon, Eric; Grove, J. Russell; Hart, Charles P.; Kim, Moon H.; Szardenings, Anna Katrin published a patent.Related Products of 59524-07-1 The title of the patent was Preparation of peptides and compounds that bind to SH2 (src homology region 2) domains of proteins and methods for their identification. And the patent contained the following:

SH2-binding peptides comprising a core sequence of amino acids Z7XZ8X (X = a member independently selected from the group consisting of the 20 genetically coded L-amino acids and the stereoisomeric D-amino acids; Z7 = phosphotyrosine or an isostere thereof; Z8 = asparagine or an isostere thereof; the amino acid terminus is acylated; the peptide is less than 14 amino acids; provided that if Z7 is phosphotyrosine and Z8 is asparagine, then the peptide is not GDGZ7XZ8XPLL), which bind to the SH2 domain or domains of various proteins, are prepared These peptides and compounds have application as agonists and antagonists of SH2 domain containing proteins, and as diagnostic or. A library of peptides bound to a solid support, useful for identifying ligands capable of binding to SH2 domains, is also prepared therapeutic agents for the diagnosis or treatment of disease conditions. A method for identifying an SH2-binding peptide comprises contacting the resp. members of a library with an SH2 domain containing protein or SH2 domain fragment and identifying SH2-binding peptides on the basis of a binding affinity of ≤1 × 10-4 M. In particular, a method for treating a disease associated with aberrant cell growth, differentiation, or regulation which is associated with defects in receptor tyrosine kinase pathways comprises administering to a patient above peptide in an amount sufficient to partially block or inhibit a cellular signal transduction pathway. Said disease is selected from cancer, developmental and differentiation disease, and insulin-resistant (or non-insulin dependent) diabetes. Thus, a phosphotyrosine-containing peptide library on a solid support with the general sequence A-pY-X1-X2-X3-S-V (pY = phosphotyrosine residue, X1 – X3 = Ala, Arg, Asn, Asp, Glu, Gln, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Val, Tyr, Trp, Vvl, Nle, etc.) representing 17,576 peptides was prepared and one of the library sequence (ApYLNESV) showed greater affinity for the SH2 domain than did the pos. control sequence (ApYINQSV, residue from the SH2-binding domain of human EGF) (4.5 μM vs. 12 μM). The experimental process involved the reaction of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate(cas: 59524-07-1).Related Products of 59524-07-1

The Article related to peptide preparation affinity sh2 domain, combinatorial library peptide, agonist antagonist sh2 domain, cancer diagnosis treatment peptide, developmental disease diagnosis treatment peptide, differentiation disease diagnosis treatment peptide, phosphotyrosine containing peptide preparation and other aspects.Related Products of 59524-07-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 31, 2016, Shi, Qixun; Masseroni, Daniele; Rebek, Julius published an article.Safety of Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Macrocyclization of Folded Diamines in Cavitands. And the article contained the following:

In the presence of a water-soluble cavitand, long-chain alkanediamines H2N(CH2)nNH2 (n = 11, 12, 14, 16, 18) underwent chemoselective monoacylation and macrolactamization reactions in water. The cavitand binds diamines in folded conformations that bury the hydrocarbon chains and expose the amino groups to the aqueous medium. Acylation of diamines H2N(CH2)nNH2 (n = 11, 12, 14, 16) with succinic anhydride in water in the presence of the water-soluble cavitand provided monofunctionalized amido acids HO2CCH2CH2CONH(CH2)nNH2 (n = 11, 12, 14, 16) in 64-71% yields, approx. twice the yields obtained in the absence of the cavitand. The C11- and C12-amido acids underwent macrocyclization to dilactams in the presence of the water-soluble cavitand using the coupling reagent EDC and a sulfonated N-hydroxysuccinimide in higher yields than in the absence of the cavitand. Direct reaction of diamines H2N(CH2)nNH2 (n = 11, 12, 14, 16, 18) with the N-hydroxysuccinimide diesters of succinic acid and glutaric acids in the presence of the water-soluble cavitand resulted in 54-96% yields of 17- to 25-membered dilactams, with three- to ten-fold increases in yield over reactions performed in the absence of the cavitands. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Safety of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to macrolactam chemoselective preparation, succinic anhydride chemoselective acylation diamine water soluble cavitand catalyst, chemoselective macrolactamization diamine amido acid water soluble cavitand catalyst,hydroxysuccinimide succinate glutarate ester chemoselective macrolactamization diamine cavitand catalyst and other aspects.Safety of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 31, 2021, Lin, Han; Hong, Haofei; Feng, Lipeng; Shi, Jie; Zhou, Zhifang; Wu, Zhimeng published an article.Synthetic Route of 79642-50-5 The title of the article was Synthesis of DNP-modified GM3-based anticancer vaccine and evaluation of its immunological activities for cancer immunotherapy. And the article contained the following:

Tumor-associated carbohydrate antigens (TACAs) are attractive targets for vaccine development. In this context, we described a strategy combining artificial TACA and glyco-engineering for cancer vaccine development. A 2,4-ditrophenyl (DNP)-modified GM3 intermediate was synthesized chemo-enzymically and conjugated to keyhole limpet hemocyanin (KLH), and the resulting bioconjugate was tested for its potential as a vaccine candidate. Mice immunol. studies revealed that the DNP-modified GM3 (GM3-NHDNP) analog elicited strong and rapid immune responses by recruiting anti-DNP antibodies to facilitate the targeted delivery of the vaccine construct to antigen processing cells (APCs). Moreover, the endogenously produced anti-DNP antibodies, together with the elicited antibodies against GM3-NHDNP, may synergistically promote tumor binding and cancer cell death when the cancer cell surfaces are glycoengineered to express the GM3-NHDNP antigen. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Synthetic Route of 79642-50-5

The Article related to ifn il6 igg igm sialooligosaccharide preparation apoptosis, human serum albumin bioconjugate sialooligosaccharide preparation sialic aldolase, keyhole limpet hemocyanin bioconjugate vaccine tumor associated carbohydrate antigen, dnp gm3 sialooligosaccharide preparation antitumor antigen vaccine antibody prodrug and other aspects.Synthetic Route of 79642-50-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On November 12, 2009, Rogers, Kathryn; Patzke, Holger published a patent.Reference of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the patent was Preparation of benzo-fused 7-membered heterocyclic compounds and methods for treating cognitive disorders using inhibitors of histone deacetylase. And the patent contained the following:

This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit, more specifically neurodegenerative disease, polyglutamine disease, tauopathy, Alzheimer’s Disease, or Huntington’s Disease. More particularly, the disclosure provides for compounds of formula [I; Z = H, (un)substituted NHOH; L = a covalent bond, (un)substituted N(OH); when L = (un)substituted N(OH), Z = H; when Z = H, L = (un)substituted N(OH); J = a covalent bond, :CH, -C1-8 alkyl-, -C0-3 alkyl-C1-5 heteroalkyl-C0-3 alkyl-, -C0-3 alkyl-C2-5 alkenyl-C0-3 alkyl-, -C0-3 alkyl-C2-5 alkynyl-C0-3 alkyl-, -C0-6 alkylaryl-C0-6 alkyl-, -C0-6 alkylaryl-C2-6 heteroalkyl-, etc.; Q = heterocycle-containing group, a covalent bond, -C1-8 alkyl-, -C1-5 alkyl-, -C1-5 heterocyclyl-, ;N-O-, N-(un)substituted -C0-6 alkyl-NH-C0-3 alkyl-, -C0-6 alkyl-O-C0-3 alkyl-, etc.; ring B = 7-membered fused heterocycle group, etc.] or a pharmaceutically acceptable salts thereof. Thus, to a solution of (E)-1-chlorodibenzo[b,f][1,4]oxazepine (229 mg, 1.00 mmol) in DME (3 mL) was added 4-methoxycarbonylphenylboronic acid (216 mg), Pd(PPh3)4 (0.065 mg) and 2 N Na2CO3 (aqueous) (1.5 mL). The reaction mixture was stirred for 2 h at 90° to give, after workup and silica gel chromatog., (Z)-Me 4-(dibenzo[b,f][1,4]oxazepin-1-yl)benzoate (II) (327 mg, 99%) as a yellow foam. To a stirring solution of ester II (327 mg) in MeOH (4.0 mL) and THF (4.0 mL) was added 50% hydroxylamine (aqueous) (1.2 mL, excess) followed by KOH (212 mg) and the reaction mixture was stirred at room temperature for 15 min to give, after workup and silica gel chromatog., (Z)-4-(dibenzo[b,f][1,4]oxazepin-11-yl)-N-hydroxybenzamide (III). III showed IC50 of ≤0.05 μM against histone deacetylase and also IC50 of ≤1 μM for whole-cell histone deacetylase (HDAC) Inhibition assay in primary mouse cortical cultures. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Reference of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to benzo fused 7 membered heterocycle preparation histone deacetylase inhibitor, neurodegenerative disease polyglutamine disease treatment heterocycle preparation, tauopathy alzheimer disease huntington disease treatment heterocycle preparation, dibenzooxazepine benzopyridooxazepine dibenzothiazepine and other aspects.Reference of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On October 1, 2015, Lin, Wenbin; Manna, Kuntal; Zhang, Teng published a patent.Synthetic Route of 1312703-30-2 The title of the patent was Preparation of metal-organic frameworks containing nitrogen-donor ligands for efficient catalytic organic transformations. And the patent contained the following:

Metal-organic framework (MOFs) compositions based on nitrogen donor-based organic bridging ligands, including ligands based on 1,3-diketimine (NacNac), bipyridines and salicylaldimine, were synthesized and then post-synthetically metalated with metal precursors, such as complexes of first row transition metals. Metal complexes of the organic bridging ligands could also be directly incorporated into the MOFs. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asym. organic transformations. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor. For example, complex MOF [Zr6(OH)4O4L6] (bpy-UiO) (H2L = 2,2′-bipyridine-5,5′-dicarboxylic acid) is synthesized by reaction of ZrCl4 and H2L in DMF. The complex is used as catalyst for C-H borylation of arenes. Gas adsorption of the complex is measured as well. The experimental process involved the reaction of Dimethyl 2′-amino-[1,1′:4′,1”-terphenyl]-4,4”-dicarboxylate(cas: 1312703-30-2).Synthetic Route of 1312703-30-2

The Article related to transition metal oxo hydroxy bipyridinedicarboxylato complex catalyst preparation, gas adsorption transition metal oxo hydroxy bipyridinedicarboxylato complex, crystal structure transition metal oxo hydroxy bipyridinedicarboxylato complex, silylation hydrogenation catalyst transition metal oxo hydroxy bipyridinedicarboxylato complex and other aspects.Synthetic Route of 1312703-30-2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics