Tag: 100-200

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

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 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

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 September 7, 2012, Ruehter, Gerd; Koch, Uwe; Nussbaumer, Peter; Schultz-Fademrecht, Carsten; Eickhoff, Jan published a patent.Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride The title of the patent was Pharmaceutically active disubstituted triazine derivatives. And the patent contained the following:

The invention discloses disubstituted triazine derivatives and/or pharmaceutically acceptable salts and the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunol. diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts,. Furthermore, the invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase and the preparation of said compounds The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

The Article related to triazine derivative infection immune autoimmune cardiovascular proliferation disease preparation, erectile dysfunction stroke triazine derivative protein kinase inhibitor and other aspects.Reference of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 5, 2016, Ruehter, Gerd; Koch, Uwe; Nussbaumer, Peter; Schulz-Fademrecht, Carsten; Eickhoff, Jan published a patent.Application of 1187830-46-1 The title of the patent was Pharmaceutically active disubstituted triazine derivatives. And the patent contained the following:

The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunol. diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Application of 1187830-46-1

The Article related to triazine derivative infection immune autoimmune cardiovascular proliferation disease preparation, erectile dysfunction stroke triazine derivative protein kinase inhibitor and other aspects.Application of 1187830-46-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 31, 2020, Yin, Yuan; Chen, Cheng-Juan; Yu, Ru-Nan; Shu, Lei; Wang, Zhi-Jian; Zhang, Tian-Tai; Zhang, Da-Yong published an article.Synthetic Route of 4433-40-3 The title of the article was Novel 1H-pyrazolo[3,4-d]pyrimidin-6-amino derivatives as potent selective Janus kinase 3 (JAK3) inhibitors. Evaluation of their improved effect for the treatment of rheumatoid arthritis. And the article contained the following:

Selective JAK3 inhibitors have been shown to have a potential benefit in the treatment of autoimmune disorders. Here we report the identification of a series of pyrazolopyrimidine derivatives as potent JAK3 inhibitors that exploit a unique cysteine (Cys909) residue in JAK3. Most of these compounds (13k, 13n and 13 t), displayed stronger anti-JAK3 kinase activity and selectivity than tofacitinib. Furthermore, the most active inhibitor 13t (IC50 = 0.1 nM), also exhibited favorable selectivity for JAK3 in a panel of 9 kinases which contain the same cysteine. In a series of cytokine-stimulated cellular anal., compound 13 t, could potently block the JAK3-STAT signaling pathway. Further biol. studies, including cellular antiproliferative activity assays and a rat adjuvant-induced arthritis model for in vivo evaluation, also indicated its efficacy and low toxicity in the treatment of rheumatoid arthritis. The results of these exptl. explorations suggested that 13t is a promising lead compound for the development of selective JAK3 inhibitor with therapeutic potential in rheumatoid arthritis. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Synthetic Route of 4433-40-3

The Article related to pyrazolo pyrimidin amino derivative preparation jak3 inhibitor rheumatoid arthritis, 4-d]pyrimidin, autoimmune diseases, jak3 inhibitors, pyrazolo[3, rheumatoid arthritis and other aspects.Synthetic Route of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 31, 2013, Manivannan, C.; Sambathkumar, S.; Renganathan, R. published an article.Synthetic Route of 626-48-2 The title of the article was Interaction of acriflavine with pyrimidines: A spectroscopic approach. And the article contained the following:

The interaction of acriflavine with uracils was studied by using spectroscopic tools viz., UV-visible absorption, steady state and time resolved fluorescence measurements. The spectroscopic data were analyzed using Stern-Volmer equation to determine the quenching process. The bimol. quenching rate constant (kq), binding constant (K) and number of binding sites (n) were calculated at different temperature from the relevant fluorescence data. The exptl. results obtained from life-time measurement indicate that the quenching mechanism was static via the formation of ground state complex. The free energy change (ΔGet) for electron transfer process was calculated by Rehm-Weller equation. The existence of binding forces and the interactions of acriflavine with uracils were examined The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Synthetic Route of 626-48-2

The Article related to acriflavine pyrimidine spectroscopic, acriflavine, fluorescence quenching, uracils, Physical Organic Chemistry: Absorption, Emission, Reflection, and Scattering Spectra (Ultraviolet and Visible, Infrared and Fourier Transform Infrared, Raman, Microwave, Photoelectron, Fluorescence, Phosphorescence, etc.) and other aspects.Synthetic Route of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 3, 2014, Sasidharanpillai, Swaroop; Loppnow, Glen R. published an article.HPLC of Formula: 626-48-2 The title of the article was Initial Excited-State Structural Dynamics of 5,6-Dimethyluracil from Resonance Raman Spectroscopy. And the article contained the following:

In order to understand the effect of Me substitution patterns on the initial excited-state structural dynamics of uracil derivatives, we measured the resonance Raman spectra of 5,6-dimethyluracil (5,6-DMU). The results show that the resonance Raman spectrum is a combination of that of 5-methyl- and 6-methyluracil. The resonance Raman excitation profiles (RREPs) and absorption spectrum are simulated with a self-consistent, time-dependent formalism to yield the excited-state slopes and broadening parameters. The initial excited-state structural dynamics occur primarily along the C5=C6 stretching mode, as expected, but with lesser excited-state slopes along each mode compared to 5-methyluracil and 6-methyluracil. This study along with previous experiments with different uracil derivatives show that the presence and positions of the Me groups seems to determine the partitioning of initial excited-state structural dynamics. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).HPLC of Formula: 626-48-2

The Article related to excited state structural dynamics dimethyluracil resonance raman spectra, Physical Organic Chemistry: Absorption, Emission, Reflection, and Scattering Spectra (Ultraviolet and Visible, Infrared and Fourier Transform Infrared, Raman, Microwave, Photoelectron, Fluorescence, Phosphorescence, etc.) and other aspects.HPLC of Formula: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Grosmaire, L.; Delarbre, J.-L. published an article in 2012, the title of the article was Vibrational spectra of 6-methyluracil, 6-methyl-2-thiouracil and their deuterated analogues.Name: 6-Methylpyrimidine-2,4(1H,3H)-dione And the article contains the following content:

FTIR and Raman spectra of 6-methyluracil (6MU), 6-methyl-2-thiouracil (6M2TU) and the deuterated forms were recorded and analyzed in the regions 400-4000 cm-1 and 100-4000 cm-1, resp. The vibrational spectra are assigned using the frequency shifts upon N-deuteration, especially for bands due to NH modes. For both mols., the isotopic ratio frequency was calculated for each NH/ND vibrations. The sulfur substitution at C2 position in the 6MU mol. has an effect on the N1H and N3H vibrational frequencies. The assignments of C2=O and C4=O modes were supported by the absence of the C2=O group in the thio-derivative The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Name: 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to vibrational spectra methyluracil methylthiouracil deuterated analog, Physical Organic Chemistry: Absorption, Emission, Reflection, and Scattering Spectra (Ultraviolet and Visible, Infrared and Fourier Transform Infrared, Raman, Microwave, Photoelectron, Fluorescence, Phosphorescence, etc.) and other aspects.Name: 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia