Pyrimidines

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

On July 21, 2017, Zhang, Zhaochao; Li, Chong; Tang, Dandan; Jin, Weixin; Wang, Miao published a patent.Electric Literature of 63931-21-5 The title of the patent was Organic compounds based on pyridine and benzimidazole use as OLED device. And the patent contained the following:

The present invention provides chem. structural formula I of the organic compound, in which X1-X6 independently represents N or C atom, the number of N atoms is 2; p is 0, 1, 2, 3 or 4; m or n independently represents 0, 1, 2 or 3, m+n+z=4, Ar1-3 independently represents C1-10 linear chain or branched chain alkyl, halogen atom, protinium, deuterium, triterium atom substituted or unsubstituted Ph, naphthyl, anthracyl or pyridyl; pyrimidyl, pyrazinyl, pyridazinyl, dibenzopyrane, 9,9-di-Me fluorene, N-Ph carbazole, quinolyl, isoquinolyl or naphthyridinyl, Ar1 also represents single bond etc. The compound of this invention has higher glass transition temperature and mol. heat endurance; and it has low absorptivity and high refractive index in visible light domain. After applied to the CPL layer of OLED device, title compound can effectively enhance the light extraction efficiency of OLED device. The compound of this invention also has deep HOMO energy level and high electron mobility, so it can be used as material of hole barrier/electron transport layer of OLED device, and can effectively stop the conveyance of hole or energy from luminescent layer to electronic shell side, so as to enhance the compounding efficiency of hole and electron in luminescent layer, and enhance the luminous efficiency and service life of OLED device. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Electric Literature of 63931-21-5

The Article related to pyridine benzimidazole oled, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wang, Han; Wen, Kun; Wang, Le; Xiang, Ye; Xu, Xiaocheng; Shen, Yongjia; Sun, Zhihua published an article in 2012, the title of the article was Large-scale solvent-free chlorination of hydroxy-pyrimidines, -pyridines, -pyrazines and -amides using equimolar POCl3.Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione And the article contains the following content:

Chlorination with equimolar POCl3 can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxypyridines, -quinoxalines, or even -amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to chlorination hydroxy pyrimidine pyridine quinoxaline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 16, 2020, Liu, Shiqiang; Yuan, Yida; Bao, Meng; Huang, Shengai; Bao, Rudi published a patent.COA of Formula: C6H6ClN3O2 The title of the patent was Regulator of nitrogen-containing heteroaromatic derivatives, preparation method and application.. And the patent contained the following:

The invention disclosed a kind of regulator of nitrogen-containing heteroaromatic derivatives, their preparation method and application. The claimed compound is shown in structure I (W = CR4 or N; Q = CR5 or N; R4,R5 = H, D, alkyl, haloalkyl, etc.; L1 = bond, O, S, alkylene, alkenyl, etc.; L2 == bond , O or S; ring A = cycloalkyl, heterocyclo, aryl, heteroaryl, etc.; ring B = cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; R1 = H, D, alkyl, halo, etc.; R2 = H, D, halolakyl, amino, nitro, etc.; R3 = alkyl, alkenyl, alkynyl, etc.; x,y = 0, 1-5 integers). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used as protein tyrosine phosphatase-2C (SHP2) inhibitor, can be used for treating diseases or conditions such as Noonan syndrome, leopard skin syndrome, leukemia, neuroblastoma, melanoma, esophageal cancer, head and neck tumors, breast cancer, lung cancer and colon cancer, etc. , preferably non-small cell lung cancer, esophagus cancer and head and neck tumors. The experimental process involved the reaction of Methyl 6-amino-2-chloropyrimidine-4-carboxylate(cas: 944129-00-4).COA of Formula: C6H6ClN3O2

The Article related to heteroaromatic derivative preparation shp2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C6H6ClN3O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 11, 2020, Xing, Qifeng; Feng, Peichuan; Chen, Yue; Hu, Lingfeng; Chen, Yili published a patent.HPLC of Formula: 160377-42-4 The title of the patent was Organic compounds and its applications. And the patent contained the following:

An organic compound having simple and easy implementation, readily available raw materials, suitable for mass production scale-up and used as light emitting layer in an OLED device is provided. The class of organic compounds is represented by the following structural formula I as an example. The application of organic compound used in organic electroluminescent device. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).HPLC of Formula: 160377-42-4

The Article related to organic compound application electroluminescent device, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.HPLC of Formula: 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 26, 2018, Wang, Fang; Zhang, Zhaochao; Li, Chong; Zhang, Xiaoqing published a patent.Category: pyrimidines The title of the patent was Process for preparation of organic compound based on pyridine and quinoxaline. And the patent contained the following:

The invention relates to preparation of organic compound based on pyridine and quinoxaline and application to OLED device. Compound I was prepared via multi step synthesis with coupling reactions as key steps. The compound has low absorption and high refractive index in visible light field, and can effectively improve light extraction efficiency of the OLED device when applied to CPL layer of the OLED device. The compound has deep HOMO energy level and high electronic mobility, can be used as a hole blocking/electron transport layer material of the OLED device, and can effectively block the hole or energy from being transferred from a light-emitting layer to one side of an electronic layer, so as to improve compounding efficiency of the hole and electron in the light-emitting layer, and further improve light emission efficiency and prolong service life of the OLED device. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Category: pyrimidines

The Article related to quinoxaline pyridine based organ compound preparation oled, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On November 23, 2017, Fischer, John P.; Fell, Jay Bradford; Blake, James F.; Hinklin, Ronald Jay; Mejia, Macedonio J.; Hicken, Erik James; Chicarelli, Mark Joseph; Gaudino, John J.; Vigers, Guy P.A.; Burgess, Laurence E.; Marx, Matthew Arnold; Christensen, James Gail; Lee, Matthew Randolf; Savechenkov, Pavel; Zecca, Henry J. published a patent.Related Products of 175357-98-9 The title of the patent was Preparation of substituted pyridopyrimidines as KRas G12C inhibitors for treating cancer. And the patent contained the following:

The title compounds I [X = (un)substituted 4-12 membered saturated or partially saturated monocyclic, bridged or spirocyclic ring; Y = a bond, O, S or NR5; R1 = C(O)C(Ra)( or =)C(Rb)p or SO2C(Ra)( or =)C(Rb)p; R2 = H, alkyl, hydroxyalkyl, etc.; R3 = (independently) alkyl, oxo, haloalkyl; L = a bond, C(O), alkylene; R4 = H, cycloalkyl, heterocyclyl, etc.; R5 = (independently) H, alkyl; m = 0-2; Ra = absent, H, alkyl; each Rb = (independently) H, alkyl, alkylaminylalkyl, dialkylaminylalkyl or heterocyclylalkyl; p = 0 or 2] or a pharmaceutically acceptable salts thereof that inhibit KRas G12C, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4-chloro-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate and benzyl 1-piperazinecarboxylate, was described. Exemplified compounds I were tested for inhibition of KRas G12C activity (data given). In particular, the present invention relates to compounds I that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds I and methods of use therefor. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Related Products of 175357-98-9

The Article related to pyridopyrimidine preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 11, 2016, Claremon, David A.; Dong, Chengguo; Fan, Yi; Leftheris, Katerina; Lotesta, Stephen D.; Singh, Suresh B.; Tice, Colin M.; Zhao, Wei; Zheng, Yajun; Zhuang, Linghang published a patent.Electric Literature of 596114-50-0 The title of the patent was Preparation of piperazine derivatives as liver X receptor modulators. And the patent contained the following:

Provided are novel compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of formula I and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer’s disease, dermatitis, dyslipidemia, cancer and other diseases or disorders. Title compounds I [Q = alkyl-OC(O), heteroaryl, aryl-alkyl-OC(O), etc.; R1 = alkyl, cycloalkyl, aryl-alkyl, etc.; R2 = H, halo, cyano, etc.; R3 = alkyl, halo-alkyl, cycloalkyl, etc.; R4 = H or alkyl], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of (R)-tert-Bu 2-isopropylpiperazine-1-carboxylate with [3-(methylsulfonyl)phenyl]boronic acid. Compounds of the invention were evaluated for their LXr α/β binding ad agonist activity, e.g., II showed Ki value of 1690 nM and 157 nM on LXRα and LXRβ, resp. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Electric Literature of 596114-50-0

The Article related to piperazine derivative preparation liver receptor lxr modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia