Day: November 3, 2022

On February 28, 2011, Konstantopoulos, Nicky; Foletta, Victoria C.; Segal, David H.; Shields, Katherine A.; Sanigorski, Andrew; Windmill, Kelly; Swinton, Courtney; Connor, Tim; Wanyonyi, Stephen; Dyer, Thomas D.; Fahey, Richard P.; Watt, Rose A.; Curran, Joanne E.; Molero, Juan-Carlos; Krippner, Guy; Collier, Greg R.; James, David E.; Blangero, John; Jowett, Jeremy B.; Walder, Ken R. published an article.Synthetic Route of 132-20-7 The title of the article was A gene expression signature for insulin resistance. And the article contained the following:

Insulin resistance is a heterogeneous disorder caused by a range of genetic and environmental factors, and we hypothesize that its etiol. varies considerably between individuals. This heterogeneity provides significant challenges to the development of effective therapeutic regimes for long-term management of type 2 diabetes. We describe a novel strategy, using large-scale gene expression profiling, to develop a gene expression signature (GES) that reflects the overall state of insulin resistance in cells and patients. The GES was developed from 3T3-L1 adipocytes that were made “insulin resistant” by treatment with tumor necrosis factor-α (TNF-α) and then reversed with aspirin and troglitazone (“resensitized”). The GES consisted of five genes whose expression levels best discriminated between the insulin-resistant and insulin-resensitized states. We then used this GES to screen a compound library for agents that affected the GES genes in 3T3-L1 adipocytes in a way that most closely resembled the changes seen when insulin resistance was successfully reversed with aspirin and troglitazone. This screen identified both known and new insulin-sensitizing compounds including nonsteroidal anti-inflammatory agents, β-adrenergic antagonists, β-lactams, and sodium channel blockers. We tested the biol. relevance of this GES in participants in the San Antonio Family Heart Study (n = 1240) and showed that patients with the lowest GES scores were more insulin resistant (according to HOMA_IR and fasting plasma insulin levels; P < 0.001). These findings show that GES technol. can be used for both the discovery of insulin-sensitizing compounds and the characterization of patients into subtypes of insulin resistance according to GES scores, opening the possibility of developing a personalized medicine approach to type 2 diabetes. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Synthetic Route of 132-20-7

The Article related to gene expression signature insulin resistance, Pharmacology: Effects Of Agents For Treating Metabolic and Endocrine Disorders and other aspects.Synthetic Route of 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 1, 2011, Danila, Ion; Riobe, Francois; Piron, Flavia; Puigmarti-Luis, Josep; Wallis, John D.; Linares, Mathieu; Agren, Hans; Beljonne, David; Amabilino, David B.; Avarvari, Narcis published an article.Electric Literature of 75449-26-2 The title of the article was Hierarchical Chiral Expression from the Nano- to Mesoscale in Synthetic Supramolecular Helical Fibers of a Nonamphiphilic C3-Symmetrical π-Functional Molecule. And the article contained the following:

The controlled preparation of chiral structures is a contemporary challenge for supramol. science because of the interesting properties that can arise from the resulting materials, and here we show that a synthetic nonamphiphilic C3 compound containing π-functional tetrathiafulvalene units can form this kind of object. We describe the synthesis, characterization, and self-assembly properties in solution and in the solid state of the enantiopure materials. CD measurements show optical activity resulting from the presence of twisted stacks of preferential helicity and also reveal the critical importance of fiber nucleation in their formation. Mol. mechanics (MM) and mol. dynamics (MD) simulations combined with CD theor. calculations demonstrate that the (S) enantiomer provides the (M) helix, which is more stable than the (P) helix for this enantiomer. This relationship is for the first time established in this family of C3 sym. compounds In addition, we show that introduction of the “wrong” enantiomer in a stack decreases the helical reversal barrier in a nonlinear manner, which very probably accounts for the absence of a “majority rules” effect. Mesoscopic chiral fibers, which show inverted helicity, i.e. (P) for the (S) enantiomer and (M) for the (R) one, have been obtained upon reprecipitation from dioxane and analyzed by optical and electronic microscopy. The fibers obtained with the racemic mixture present, as a remarkable feature, opposite homochiral domains within the same fiber, separated by points of helical reversal. Their formation can be explained through an “oscillating” crystallization mechanism. Although C3 sym. disk-shaped mols. containing a central benzene core substituted in the 1,3,5 positions with 3,3′-diamido-2,2′-bipyridine based wedges have shown peculiar self-assembly properties for amphiphilic derivatives, the present result shows the benefits of reducing the nonfunctional part of the mol., in our case with short chiral isopentyl chains. The research reported herein represents an important step toward the preparation of functional mesostructures with controlled helical architectures. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Electric Literature of 75449-26-2

The Article related to hierarchical chiral expression nanoscale mesoscale synthetic supramol helical fiber, Physical Organic Chemistry: Optical Rotatory Dispersion and Circular Dichroism and other aspects.Electric Literature of 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 31, 1996, Satoh, Hideharu; Tokuda, Koichi; Ohsaka, Takeo published an article.Synthetic Route of 52243-87-5 The title of the article was Observation of intermolecular charge-transfer spectra for propyl viologen dihalides in a series of polyether media. And the article contained the following:

1,1′-Dipropyl-4,4′-bipyridinium diiodide (PV2+·2I-) in a series of polyethers (PEOs, HO(CH2CH2O)nH, n = 1 ∼ 14) gave an intermol. charge-transfer spectrum, which shifted to longer wavelength with larger absorbance in less polar medium, in the visible region. An increase in temperature resulted in an increase in absorbance as a result of an ion-dipole interaction between PV2+ cation and polyether solvent. The experimental process involved the reaction of 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide(cas: 52243-87-5).Synthetic Route of 52243-87-5

The Article related to intermol charge transfer spectra viologen polyether, uv spectra viologen polyether, Physical Properties of Synthetic High Polymers: Physical Properties Of Polymers and other aspects.Synthetic Route of 52243-87-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 24, 1995, Kelly, T. Ross; Lang, Fengrui published an article.Quality Control of Methyl 6-bromo-5-methoxypicolinate The title of the article was Total synthesis of dimethyl sulfomycinamate. And the article contained the following:

The first total synthesis of di-Me sulfomycinamate is described. Highlights of the synthesis include a selective palladium-catalyzed coupling reaction on a bromo triflate, and a condensation reaction to form the oxazole ring. The experimental process involved the reaction of Methyl 6-bromo-5-methoxypicolinate(cas: 170235-18-4).Quality Control of Methyl 6-bromo-5-methoxypicolinate

The Article related to sulfomycinamate total synthesis, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.Quality Control of Methyl 6-bromo-5-methoxypicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 24, 2014, Xu, Wei; Wang, Yong; Ma, Sunghoon; Koltun, Elena S.; Kim, Byung Gyu; Jeong, Joon Won; Dhar, T.g. Murali; Bannen, Lynn Canne published a patent.Recommanded Product: 4-Chloro-2,6-difluoropyridine The title of the patent was Pyrimidine derivatives as RORγ modulators and their preparation. And the patent contained the following:

Described are RORγ modulators of formula I, and N-oxides, pharmaceutically acceptable salts, solvates and hydrates thereof, and their compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune. Compounds of formula I wherein R1 is H, halo, CN, NO2, OH, etc.; dashed bonds are single and double bond; R2 is H, halo, CN, NO2, N3, etc.; R4 and R5 are independently H, Me and F; m and n are independently 0, 1, 2, and 3; each R6 is halo, CN, NO2, N3, OH, etc.; each Ra is H, halo, CN, NO2, etc.; Z is CO, CS, SO2 and CH2; G is a single bond, CH2, CHD, CD2, etc.; B is Ph, pyridyl, naphthyl, thiazolyl and pyrimidinyl; L is CONHCH2, CONHCH2CH2O, oxadiazolyl, etc.; A is Ph, pyridyl, pyrimidinyl, thiazolyl, pyrazolyl and pyrazinyl; and stereoisomeric forms, N-oxides, pharmaceutically acceptable salts, solvates and hydrates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their RORγ modulatory activity. From the assay, it was determined that compound II exhibited IC50 value of 4.7 nM. The experimental process involved the reaction of 4-Chloro-2,6-difluoropyridine(cas: 34968-33-7).Recommanded Product: 4-Chloro-2,6-difluoropyridine

The Article related to pyrimidine preparation rorgamma modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 4-Chloro-2,6-difluoropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 30, 2018, Bartolome-Nebreda, Jose Manuel; Trabanco-Suarez, Andres Avelino; Alcazar-Vaca, Manuel Jesus published a patent.Related Products of 1820711-82-7 The title of the patent was [1,2,4]Triazolo[1,5-a]pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as OGA inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I as O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising compounds of formula I, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathol., in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. Compounds of formula I wherein X1 and X3 are independently CRxa, N and NH and derivatives; X2 is CH; X4 is C and N; X5, X6, X7 and X8 are independently C, CRxb and N; with the proviso that at least one of X1 and X3 is N and NH and derivatives; Rxa and Rxb are independently H, halo, CN, (un)substituted C1-4 alkyl, etc.; La is a bond, CHR1, O and NR1; Ra is CHR1, O, NR1, (un)substituted piperidinyl, (un)substituted morpholinyl, etc.; R1 is H and (un)substituted C1-4 alkyl; dashed bonds are single and double bonds; and tautomers and stereoisomeric forms thereof, are claimed. Example compound II was prepared by N-sulfonylation of 7-((3R)-piperidin-3-yl)-[1,2,4]triazolo[1,5-a]pyrimidine with 2-acetylaminothiazole-5-sulfonyl chloride. The invention compounds were evaluated for their OGA inhibitory activity. From the assay, it was determined that compound II exhibited pIC50 value of 6.06 and Emax of 94.20 %. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Related Products of 1820711-82-7

The Article related to triazolopyrimidine preparation oga inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 10, 2015, Scobie, Martin; Wallner, Olov; Koolmeister, Tobias; Vallin, Karl Sven Axel; Henriksson, Carl Martin; Homan, Evert; Helleday, Thomas; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline; Fiskesund, Roland Julius Yu published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Diaminopyrimidines as MTH1 inhibitors for treatment of inflammatory and autoimmune conditions and their preparation. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions. Compounds of formula I wherein R2 is (un)substituted Ph, substituted 6-membered heteroaryl, 5- to 10-membered (mono/bi)cyclic heteroaryl, etc.; R2 is H, halo, CN, (un)substituted C1-3 alkyl, etc.; R3 is X-L-J, (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; X is (un)substituted C1-6 alkylene, and (un)substituted C0-2 alkyl-heterocycloalkylene-C0-2 alkyl; L is single bond, O, S, O-C1-6 alkylene, etc.; J is (un)substituted 6- to 10-membered aryl and (un)substituted 5- to 11-membered (mono/bi)cyclic heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of less than 200 nM. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to diaminopyrimidine preparation mth1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 7, 2022, Borjesson, Ulf; Perry, Matthew William Dampier; Grebner, Christoph; Michaelides, Iacovos Neal; Hayhow, Thomas George Christopher; Kettle, Jason Grant; Collie, Gavin William; Storer, Robert Ian; Bagal, Sharanjeet Kaur; Fallan, Charlene published a patent.SDS of cas: 1820711-82-7 The title of the patent was Synthesis of heterocyclic substituted pyrimidine anticancer agents. And the patent contained the following:

The synthesis of heterocyclic substituted pyrimidine anticancer agents I, wherein A is a protein binder unit; Z can be a bicyclic heterocyclic ring system with multiple heteroaroms N, O, S; Y can be a pyrimidine dione moiety; R can be a substituent on any available C or N such that alkyl, alkenyl, alkynyl or related groups with optional halo, nitrile, amino or similar groups; L, as a linker, can be an (un)saturated framework comprising C and H atoms and at least one heteroatom; and n can be an integer between 0-3 are prepared as pharmaceutically acceptable salts. Of note, II demonstrated a Cereblon HTRF IC50 binding of 2.1μM and can be employed in the treatment of cancers in humans or animals such that solid tumors, BRD4-sensitive tumors. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).SDS of cas: 1820711-82-7

The Article related to heterocyclic pyrimidine anticancer preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Scobie, Martin; Helleday, Thomas; Koolmeister, Tobias; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline published a patent.SDS of cas: 199522-66-2 The title of the patent was Preparation of pyrimidine-2,4-diamine derivatives for treatment of cancer. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1. Compounds of formula I wherein R1 is (un)substituted heteroaryl and (un)substituted aryl; R2 is H, halo, CN, (un)substituted C1-12 alkyl, etc.; R3 is (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; R2R3 can be taken together to form 5- to 8-membered nonaromatic ring; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity (data given). The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).SDS of cas: 199522-66-2

The Article related to pyrimidinediamine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 2, 2021, Bartolozzi, Alessandra; Proudfoot, John Robert; Briggs, Timothy; Mancuso, John; Bos, Maxence; Guo, Tianlin; Ly, Vu Linh; Blois, Anna; Lanter, Bernard; Taylor, Steven John; Buckbinder, Leonard published a patent.Synthetic Route of 1820711-82-7 The title of the patent was Synthesis of fused azole heterocycles as AHR antagonists treating cancers. And the patent contained the following:

The synthesis of fused azole heterocycles, I, wherein the dashed bonds can be independently single or double bonds; X can selectively be N, S,CH, or NH depending on bond arrangements; Y can independently be N or CH as it relates to the fused azole; ring A and B are chosen from optionally substituted aryl, heteraryl, cycloalkyl or heterocycloalky moieties; and L is chosen from a bond and -NT-C(O)-, wherein T can be H or Me are presented as pharmaceutically acceptable salts for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. Of note, II was synthesized and demonstrated an HEPG2 Luc IC50 of less than 100 nM; an aqueous solubility of less than 0.1μM at pH 7/4; and a human hepatocyte clearance of between 20 and 50 mL/min/Kg. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Synthetic Route of 1820711-82-7

The Article related to fused azole heterocycle ahr antagonist anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem