Month: November 2022

On May 26, 2011, Carpenter, Andrew J.; Fang, Jing; Peckham, Gregory published a patent.Related Products of 596114-50-0 The title of the patent was Chemical compounds and uses. And the patent contained the following:

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to pyridazinyl derivative preparation gpr119 agonist treatment metabolic disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 27, 2019, Duvey, Guillaume; Celanire, Sylvain published a patent.SDS of cas: 1209459-32-4 The title of the patent was Preparation of novel heterocyclic compounds 1-oxo-5,6,7,8-tetrahydro-2H-phthalazine derivatives and analogs, as mGluR7 modulators. And the patent contained the following:

The invention is related to the preparation of compounds I [G = N, CR7; E = N, CR8; provided that at least one of G or E is N; Y = CR9, N; X = (CR5R6)n; R1-9 = independently H, halo, CN, CF3, etc.; wherein any two radicals R1 and R2, R3 and R4, and R5 and R6 may be taken together to form an oxo; wherein optionally any two radicals selected from R1-9 may be taken together to form an (un)substituted 3 to 10-membered non aromatic carbocyclic or heterocyclic ring or a 5 to 10-membered aromatic heterocyclic ring; n = 0-1; Ar1, Ar2 = (un)substituted aryl or heteroaryl], their N-oxide forms , their pharmaceutically acceptable salts and solvates, their optical isomers, racemates, diastereoisomers, enantiomers and tautomers which are modulators of the metabotropic glutamate receptors (mGluR), preferably of the metabotropic glutamate receptor subtype 7 (mGluR7), to pharmaceutical composition comprising such compound and to their use for the treatment of prevention of disorders associated with glutamate dysfunction. Thus, II was prepared by a multi-step synthesis from 1-bromo-2,4-dimethylbenzene and 1,4-dioxaspiro[4.5]decan-8-one. Compounds I are antagonists or neg. modulators of the mGluR7 as they reduce or inhibit the mGluR7 response induced by glutamate or a mGluR7 agonist, such as L-AP4 as shown in an inositol monophosphate production assay. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).SDS of cas: 1209459-32-4

The Article related to oxotetrahydrophthalazine cyclopentapyridazinone pyridopyrimidinone preparation metabotropic glutamate receptor mglur7 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.SDS of cas: 1209459-32-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 4, 2019, Duvey, Guillaume; Celanire, Sylvain published a patent.Formula: C8H10BrN3O The title of the patent was Preparation of novel heterocyclic compounds 1-oxo-5,6,7,8-tetrahydro-2H-phthalazine derivatives and analogs, as mGluR7 modulators. And the patent contained the following:

The invention is related to the preparation of compounds I [G = N, CR7; E = N, CR8; provided that at least one of G or E is N; Y = CR9, N; X = (CR5R6)n; R1-9 = independently H, halo, CN, CF3, etc.; wherein any two radicals R1 and R2, R3 and R4, and R5 and R6 may be taken together to form an oxo; wherein optionally any two radicals selected from R1-9 may be taken together to form an (un)substituted 3 to 10-membered non aromatic carbocyclic or heterocyclic ring or a 5 to 10-membered aromatic heterocyclic ring; n = 0-1; Ar1, Ar2 = (un)substituted aryl or heteroaryl], their N-oxide forms , their pharmaceutically acceptable salts and solvates, their optical isomers, racemates, diastereoisomers, enantiomers and tautomers which are modulators of the metabotropic glutamate receptors (mGluR), preferably of the metabotropic glutamate receptor subtype 7 (mGluR7), to pharmaceutical composition comprising such compound and to their use for the treatment of prevention of disorders associated with glutamate dysfunction. Thus, II was prepared by a multi-step synthesis from 1-bromo-2,4-dimethylbenzene and 1,4-dioxaspiro[4.5]decan-8-one. Compounds I are antagonists or neg. allosteric modulators of the mGluR7 as they reduce or inhibit the mGluR7 response induced by glutamate or a mGluR7 agonist, such as L-AP4 as shown in an inositol monophosphate production assay. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Formula: C8H10BrN3O

The Article related to oxotetrahydrophthalazine cyclopentapyridazinone pyridopyrimidinone preparation metabotropic glutamate receptor mglur7 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Formula: C8H10BrN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 1, 2019, Zueva, Irina; Dias, Jose; Lushchekina, Sofya; Semenov, Vyacheslav; Mukhamedyarov, Marat; Pashirova, Tatiana; Babaev, Vasiliy; Nachon, Florian; Petrova, Natalia; Nurullin, Leniz; Zakharova, Lucia; Ilyin, Victor; Masson, Patrick; Petrov, Konstantin published an article.Quality Control of 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was New evidence for dual binding site inhibitors of acetylcholinesterase as improved drugs for treatment of Alzheimer’s disease. And the article contained the following:

Profound synaptic dysfunction contributes to early loss of short-term memory in Alzheimer’s disease. This study was set up to analyze possible neuroprotective effects of two dual binding site inhibitors of acetylcholinesterase (AChE), a new 6-methyluracil derivative, C-35, and the clin. used inhibitor donepezil. Crystal structure of the complex between human AChE and C-35 revealed tight contacts of ligand along the enzyme active site gorge. Mol. dynamics simulations indicated that the external flexible part of the ligand establishes multiple transient interactions with the enzyme peripheral anionic site. Thus, C-35 is a dual binding site inhibitor of AChE. In transgenic mice, expressing a chimeric mouse/human amyloid precursor protein and a human presenilin-1 mutant, C-35 (5 mg/kg, i.p) and donepezil (0.75 mg/kg, i.p) partially reversed synapse loss, decreased the number of amyloid plaques, and restored learning and memory. To sep. temporal symptomatic therapeutic effects, associated with the increased lifetime of acetylcholine in the brain, from possible disease-modifying effect, an exptl. protocol based on drug withdrawal from therapy was performed. When administration of C-35 and donepezil was terminated three weeks after the trial started, animals that were receiving C-35 showed a much better ability to learn than those who received vehicle or donepezil. Our results provide addnl. evidence that dual binding site inhibitors of AChE have Alzheimer’s disease-modifying action. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Quality Control of 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to alzheimers disease acetylcholinesterase c35 donepezil, alzheimer’s disease, inhibitors of cholinesterase, methyluracil derivatives, β-amyloid, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Quality Control of 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 20, 2016, Noh, Hyo-Jin; Yoon, Kyung-Jin; Yoon, Dae-Wi; Shin, In-Ae; Kim, Jun-Yun published a patent.Application of 160377-42-4 The title of the patent was Space-through charge transfer compound, and organic light emitting diode and display device using the same. And the patent contained the following:

Discussed is a space-through charge transfer compound for OLEDs exhibiting thermally activated delayed fluoroscence. The compound includes a naphthalene core; an electron donor moiety D selected from carbazole and phenylcarbazole; and an electron acceptor moiety A selected from pyridine, diazine, triazole and Ph benzodiazole, wherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, resp., according to the following formula:. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Application of 160377-42-4

The Article related to charge transfer compound light emitting diode, Electric Phenomena: Photoconductivity, Photoconductors, Photovoltaic Effect, Photoelectric Devices and other aspects.Application of 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 11, 2018, Ilyina, Margarita G.; Khamitov, Edward M.; Ivanov, Sergey P.; Mustafin, Akhat G.; Khursan, Sergey L. published an article.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Theoretical Models for Quantitative Description of the Acid-Base Equilibria of the 5,6-Substituted Uracils. And the article contained the following:

The acidities of 18 5,6-substituted uracils have been numerically estimated as pKa values in terms of three theor. models. The first scheme includes the calculation of the gas-phase acidity of uracil with the G3MP2B3 method and taking into account the solvent effect using the polarizable continuum approximation PCM(SMD)-TPSS/aug-cc-pVTZ. The second model is one-step and implies calculating of the free Gibbs energies of the hydrate complex of uracil (and its anion) with 5 water mols. by the TPSS/aug-cc-pVTZ method. This model accounts the solvent effect corresponding to both specific and nonspecific solvation. The third scheme required high time and computational resources and includes the strong features of the two previous schemes. Here, the theor. estimation of pKa is performed by the CBS-QB3 composite method. As in the second approach, both specific (as pentahydrate) and nonspecific solvent effects are accounted. We have analyzed the advantages and model restrictions of the considered schemes for the pKa calculations All models have the systematic errors, which have been corrected with the linear empirical regression relations. Herewith, the absolute mean deviations of the pKa values of uracils dissociating via the N1-H bonds diminish to 0.25, 0.28 and 0.23 pKa units (resp., for I, II, and III models) that corresponds to ∼0.3 kcal/mol on the energy scale. The applicability of our computational schemes to uracils dissociating via N3-H, O-H (orotic acids) and C-H bonds is discussed. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to acid base equilibrium acidity uracil derivative water solution, Phase Equilibriums, Chemical Equilibriums, and Solutions: Acid-Base Equilibriums, Complex Formation and other aspects.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 14, 2017, Mansour, Tarek Suhayl; Chafeev, Mikhail; Yudin, Mikhail; Gezentsvey, Yury; Nikitin, Aleksandr published a patent.COA of Formula: C7H9ClN2 The title of the patent was Preparation of compounds containing benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide or benzo[d][1,3]oxathiole 3,3-dioxide and methods/uses thereof as agonists of g protein-coupled receptor 119. And the patent contained the following:

There are provided benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide, and benzo[d][1,3]oxathiole 3,3-dioxide compounds of formula I, as well as uses/methods related thereto, including treatment of diseases and condition associated with GPR119 dysregulation, type 2 diabetes mellitus, and related metabolic disorders. Compounds of formula I wherein one of X1 and X2 is O and the other one is SO2; X3 is CH, CF and N; X4 is independently CH and N; A is (un)substituted piperazinyl, (un)substituted pyrrolidinyl, (un)substituted piperidinyl, etc.; and enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, are claimed. Example compound II was prepared by etherification of (1-tert-butylpiperidin-4-yl)methanol with 4-(3,3-dioxido-1,3-benzoxathiol-6-yl)-2-fluorophenol. The invention compounds were evaluated for their GPR119 agonistic activity. From the assay, it was determined that compound II exhibited EC50 value of 833 nM and 75 % of cAMP stimulation. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).COA of Formula: C7H9ClN2

The Article related to benzoxathiole oxide preparation gpr119 agonist, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.COA of Formula: C7H9ClN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 10, 2017, Chen, Gang; Chrovian, Christa C.; Coate, Heather R.; Dvorak, Curt A.; Gelin, Christine F.; Hiscox, Afton; Letavic, Michael A.; Rech, Jason C.; Soyode-Johnson, Akinola; Stenne, Brice; Wall, Jessica L.; Zhang, Wei published a patent.Recommanded Product: 596114-50-0 The title of the patent was Preparation of substituted 1,2,3-triazoles as NR2B-selective NMDA modulators. And the patent contained the following:

The invention relates to substituted 1,2,3-triazoles of formula I as NR2B receptor ligands that may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity. Compounds of formula I, wherein Ar1 is substituted Ph, (un)substituted pyridyl, substituted thienyl; R1 is H, halo, Me; R2 is H and Me; Ar3 is (un)substituted pyridyl, (un)substituted pyridazinyl, (un)substituted pyrimidin-4-yl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by condensation of (1-(4-chloro-3-(difluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methanol with 2-chloropyrimidine. The invention compounds were evaluated for their NR2B modulatory activities. From the assay, it was determined that compound II exhibited IC50 value of 0.049 μM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Recommanded Product: 596114-50-0

The Article related to preparation substituted triazole nr2b selective nmda modulator, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 6, 2019, Chafeev, Mikhail published a patent.Product Details of 596114-50-0 The title of the patent was Preparation of compounds containing polysubstituted benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide or benzo[d][1,3]oxathiole 3,3-dioxide and uses thereof as agonists of G protein-coupled receptor 119. And the patent contained the following:

The title compounds I [X1 and X2 are selected from certain combinations of O, S, SO and SO2; X3 = CH, CF, N; X4 = (independently) CH or N; X6, X61 and X62 = (independently) H, halo, alkyl, etc.; X7 and X71 = H, halo, alkyl, etc.; or both X7 and X71, together form a cycloalkyl or heterocycle; A = (un)substituted alkoxy, piperazinyl and pyrrolidinyl] or enantiomers, diastereomers, hydrates, solvates, or pharmaceutically acceptable salts of I, or prodrugs or complexes thereof, useful in treating diseases and conditions associated with GPR119 dysregulation, type 2 diabetes mellitus, and related metabolic disorders, were prepared E.g., a multi-step synthesis of II, starting from 1-tert-butylpiperidine-4-one and trimethylsilyldiazomethane, was described. The potency of exemplified compounds I as GPR119 receptor agonists was assessed (data given). Also provided are compositions comprising compounds I. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Product Details of 596114-50-0

The Article related to benzooxathiole oxide preparation gpr119 agonist antidiabetic, diabetes mellitus type 2 metabolic disorder benzooxathiole oxide preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Product Details of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 6, 2014, Bono, Ayako; Matsuda, Daisuke; Otake, Kenichi; Kakinuma, Hiroyuki; Kobashi, Yohei; Kawamura, Madoka; Shiozawa, Fumiyasu; Shimizu, Yuki; Kawabe, Kenichi; Hamada, Makoto published a patent.Computed Properties of 596114-50-0 The title of the patent was Hypoglycemic agents containing condensed heterocyclic compounds as GPR119 agonists. And the patent contained the following:

Hypoglycemic agents contain condensed heterocyclic compounds I [A = (un)substituted Ph or 5-6 membered heteroaryl; W = bond, O, NH, OCH2, CH2O; X = N, CR21; Y1 = N, CR22; Y2 = N, CR23; Y3 = N, CR24; R21-R24 = H, C1-6 alkyl; B = (un)substituted C2-6 alkyl, C3-8 cycloalkyl, (C3-8 cycloalkyl)C1-6 alkyl, (aryl)C1-6 alkyl, (saturated heterocyclyl)C1-6 alkyl, COOR31, 5-6 membered heteroaryl; R31 = C1-6 alkyl, C3-8 cycloalkyl, etc.] or their pharmaceutically acceptable salts as active ingredients and are useful for prevention and treatment of diabetes mellitus. Thus, tert-Bu 4-[5-[4-(methylsulfonyl)phenyl]-1H-indazol-1-yl]piperidine-1-carboxylate, prepared by several steps, promoted cellular cAMP production in human GPR119-expressing cells with ED50 of 31 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Computed Properties of 596114-50-0

The Article related to condensed heterocycle preparation hypoglycemic gpr119 agonist antidiabetic, indazolylpiperidinecarboxylate preparation hypoglycemic gpr119 agonist antidiabetic, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Computed Properties of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia