Tag: M.W:400-500

Chemistry is traditionally divided into organic and inorganic chemistry. Formula: C27H30N6O3. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1022150-11-3

TARGETED COVALENT PROBES AND INHIBITORS OF PROTEINS CONTAINING REDOX-SENSITIVE CYSTEINES

Covalent, irreversible small-molecule inhibitors that modify the sulfenyl form (i.e., sulfenic acid, RSOH and sulfenamide, RSNR’2) of therapeutically important proteins (particularly kinases and phosphatases) are disclosed, where the compositions include a compound having a substituted aryl or heterocyclic core structure that promotes binding interactions with a specific protein, and a nucleophilic reaction center (carbon, nitrogen, sulfur, or phosphorous) that is capable of forming a covalent bond with a sulfenic acid- or sulfenamide-modified cysteine residue in the protein. Methods for synthesizing these compounds are also disclosed, as well as methods of using them for determining the bioactivity of a chemical composition comprising an active compound toward a specific protein and for determining the potency of an inhibitor against a specific protein.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Formula: C27H30N6O3, you can also check out more blogs about1022150-11-3

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Chemistry is an experimental science, Computed Properties of C23H21ClN2O3, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 1443437-74-8, Name is CCG-203971

Pharmacological inhibition of myocardin-related transcription factor pathway blocks lung metastases of RhoC-Overexpressing melanoma

Melanoma is the most dangerous form of skin cancer with the majority of deaths arising from metastatic disease. Evidence implicates Rho-activated gene transcription in melanoma metastasis mediated by the nuclear localization of the transcriptional coactivator, myocardin-related transcription factor (MRTF). Here, we highlight a role for Rho and MRTF signaling and its reversal by pharmacologic inhibition using in vitro and in vivo models of human melanoma growth and metastasis. Using two cellular models of melanoma, we clearly show that one cell type, SK-Mel-147, is highly metastatic, has high RhoC expression, and MRTF nuclear localization and activity. Conversely, SK-Mel-19 melanoma cells have low RhoC expression, and decreased levels of MRTF-regulated genes. To probe the dependence of melanoma aggressiveness to MRTF transcription, we use a previously developed smallmolecule inhibitor, CCG-203971, which at low micromolar concentrations blocks nuclear localization and activity of MRTF-A. In SK-Mel-147 cells, CCG-203971 inhibits cellular migration and invasion, and decreases MRTF target gene expression. In addition, CCG-203971-mediated inhibition of the Rho/MRTF pathway significantly reduces cell growth and clonogenicity and causes G1 cell-cycle arrest. In an experimental model of melanoma lung metastasis, the RhoC-overexpressing melanoma cells (SK-Mel-147) exhibited pronounced lung colonization compared with the low RhoC-expressing SK-Mel-19. Furthermore, pharmacologic inhibition of the MRTF pathway reduced both the number and size of lung metastasis resulting in a marked reduction of total lung tumor burden. These data link Rho and MRTF-mediated signaling with aggressive phenotypes and support targeting the MRTF transcriptional pathway as a novel approach to melanoma therapeutics.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Computed Properties of C23H21ClN2O3, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 1443437-74-8, in my other articles.

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Electric Literature of 1022150-11-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1022150-11-3, Name is (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, molecular formula is C27H30N6O3. In a Patent£¬once mentioned of 1022150-11-3

Method of treating or inhibiting colonic polyps

This invention provides a method of treating or inhibiting colonic polyps in a mammal in need thereof which comprises administering to said mammal a compound having the formula wherein:X is phenyl which is optionally substituted;R and R1 are each, independently, hydrogen, halogen, alkyl, alkoxy, hydroxy, or trifluoromethyl;R2 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl;Y is a radical selected from the group consisting of R3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl;n=2-4;or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Electric Literature of 1022150-11-3, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 1022150-11-3

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ name: (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, Which mentioned a new discovery about 1022150-11-3

H based on the quinazoline structure2S donor compound and and its application (by machine translation)

The invention discloses a based on the quinazoline structure H2 S donor compound and and its application, its are of the formula (I) indicated by the compound or its pharmaceutically acceptable salt, wherein Ar is substituted or non-substituted phenyl, substituted ethylenically: halogen, nitro, C1 – 4 Alkyl, C1 – 4 Haloalkyl, C1 – 4 Alkoxy, C1 – 4 Haloalkyl oxy in one or several; X is C1 – 4 Alkoxy, B – NH – or A – CH2 CO – NH – group, Y is H, B – Cn H2n O – or A – Cn H2n O – group, respectively A or B H2 S donor group, n is 1 – 5 integer, and X is C1 – 3 Alkoxyl basetime Y is not H. The present invention is based on the synthesis of a series of 4 – anilinoquinazoline structure of H2 S donor compound, through the H2 S and 4 – anilinoquinazoline derivatives of synergistic effects, thereby improving the antitumor activity of the medicament. (by machine translation)

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, name: (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 1022150-11-3

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ Formula: C27H30N6O3, Which mentioned a new discovery about 1022150-11-3

O-toluene amino acetyl amino methoxy phenyl and aza * base kuikui zuo lin apperception compound in the preparation of a drug for treating cervical carcinoma in the application of the (by machine translation)

The invention discloses a O-toluene amino acetyl amino methoxy phenyl and aza Base kuikui zuo lin apperception compound in preparation for preventing or treating tumor application of the medicament, in particular for the production in the prevention or treatment of human cervical carcinoma in the medicament application, its Siha activity inhibiting human cervical carcinoma cell has a remarkable effect. (by machine translation)

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Formula: C27H30N6O3, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 1022150-11-3

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Electric Literature of 129029-23-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.129029-23-8, Name is Ocaperidone, molecular formula is C24H25FN4O2. In a Article£¬once mentioned of 129029-23-8

[35S]guanosine-5′-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: Actions of antiparkinsonian and antipsychotic agents

Recombinant human dopamine D4.4 receptor-mediated G protein activation was characterized in membranes of transfected mammalian (Chinese hamster ovary) cells by the use of [35S]guanosine-5′-O-(3-thio)triphosphate (35S]GTPgammaS) binding. An initial series of experiments defined the conditions (3 muM GDP, 100 mM NaCl, 3 mM MgCl2) under which optimal stimulation (2.2-fold increase in specific [35S]GTPgammaS binding) was achieved with the endogenous agonist dopamine. The number of dopamine- activated G proteins in Chinese hamster ovary-D4.4 membranes was determined through [35S]GTPgammaS isotopic dilution saturation binding, yielding a B(max) value of 2.29 pmol/mg. This compared with a D4.4 receptor B(max) value of 1.40 pmol/mg determined by [3H]spiperone saturation binding, indicating that 1 or 2 G proteins were activated per D4.4 receptor and that there were few or no ‘spare receptors’ in this cell line. Under these conditions, the efficacy for stimulation of [35S]GTPgammaS binding at D4.4 receptors of 12 dopaminergic agonists was determined. Several antiparkinsonian drugs, including ropinirole, quinerolane and lisuride, exhibited agonist activity at D4.4 receptors (E(max) = 74.3%, 72.4% and 32.2%, respectively, compared with dopamine = 100%). The EC50 values for agonist stimulation of [35S]GTPgammaS binding correlated well with the inhibition constants derived from competition binding with [3H]spiperone (r = +.99). However, other antiparkinsonian drugs (bromocriptine, L-DOPA and terguride) showed low affinity and/or were devoid of agonist activity at D4.4 receptors. The potency at D4.4 receptors of the novel, selective D4.4 receptor antagonist L 745,870 was determined, indicating that it has high affinity (K(l) = 1.99 nM) without detectable agonist activity. Furthermore, L 745,870 completely inhibited dopamine-stimulated [35S]GTPgammaS binding with a K(b) value of 1.07 nM. The action of an additional 20 chemically diverse dopaminergic ligands, including clozapine, ziprasidone, sertindole, olanzapine and several other ‘atypical’ antipsychotics, in advanced development was investigated. Each of these ligands shifted the dopamine stimulation curve to the right in a parallel manner consistent with competitive antagonism at this site and yielding K(b) values (32.6, 22.4, 17.2 and 26.5 nM, respectively) that agreed closely with their K(l) values (38.0, 14.9, 18.5 and 26.1 nM). In contrast, raclopride and seroquel exhibited low affinity at D4.4 receptors (K(l) > 1000 nM). Other compounds that showed antagonist activity at D4.4 receptors included the 5- hydroxytryptamine(2A) receptor antagonist fananserin (RP 62203), the sigma ligand BMY 14,802 and the D3 receptor antagonist GR 103,691. In conclusion, dopamine D4.4 receptor activity is unlikely to be an important factor in the clinical effectiveness of antiparkinsonian drugs, although low agonist efficacy at D4.4 receptors might be associated with a lesser incidence of side effects. Furthermore, antagonist activity at D4.4 receptors is a common property of many typical and atypical antipsychotic agents.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 129029-23-8

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1022150-11-3,(R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound (IV) (Pgi = Pg2 = Boc) (2.93 g, 5 mmol) was dissolved in MeOH (15 ml), then 33% HC1 (3 ml) was added, and the reaction mass was heated at 50C for 4 st with intensive stirring (note: a foam is forming during the reaction due to isolation of gaseous by-products). After completion of the reaction the resulting solution was cooled to room temperature and evaporated to dryness (note: the vapor contains HC1). Saturated Na2CO3 solution (5 ml) was added to the dry residue and the mixture was extracted with EtOAc (3 x 10 ml). The extract was dried over Na2SO4 and evaporated in vacuum. Yield 1.89 g (98%), white amorphous mass., 1022150-11-3

As the paragraph descriping shows that 1022150-11-3 is playing an increasingly important role.

Reference£º
Patent; LATVIAN INSTITUTE OF ORGANIC SYNTHESIS; LEBEDEVS, Antons; PONOMARJOVS, Jurijs; VARACEVA, Larisa; CERNAKS, Dmitrijs; CERNOBROVIJS, Aleksandrs; LAVRINOVICS, Edvards; (15 pag.)WO2017/39425; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.503614-92-4,1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid,as a common compound, the synthetic route is as follows.,503614-92-4

General procedure: A solution of 5,6-dihydro-3- (4-morpholinyl) -1- [4- (2-oxo-1-piperidinyl) phenyl]2 (1H) -pyridone and ethyl [(4-methoxyphenyl) hydrazino] chloroacetate,In the triethylamine for the acid binding agent under the conditions of condensation, and then by hydrochloric acid deprotection,The resulting intermediates,In the ethylene glycol under high temperature conditions with ammonia reaction in the preparation of an average of apixaban, the purity of 95.4%.In the 50L reactor,Add 2 kg of apixaban crude (purity 95. 4%) and 16L with 10% ammonia in ethylene glycol solution, heated to 90 C dissolved, then add 16L water cooling, stirring at 40 ~ 50 C for 2 hours , Cooling to 0 ~ 10 C. And then filtered to dryness to give 8 kg of a white solid, 90% yield, and an HPLC purity of 99. 97%.

503614-92-4 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid 22240440, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhongmei HuashitongBiotechnology Pharmaceutical Technology (Wuhan) Co.,Ltd; HU, MINGLONG; WU, HAOHAO; CUI, JIAN; QIAN, LINA; (13 pag.)CN106188036; (2016); A;,
Piperidine – Wikipedia
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1022150-11-3, (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 2.5g (5.1mmol) of formula 10 was added to the methanol solution in 25ml of hydrochloric acid, stirred at room temperature 2hour. Concentrated under reduced pressure, the residue was added 30ml of water, extracted with ethyl acetate, the organic phase was washed with 5% aqueousSodium hydroxide solution was washed until neutral. The organic phase was concentrated under reduced pressure to give a pale yellow oil 1.82g, yield 92%

1022150-11-3, The synthetic route of 1022150-11-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Okuura Dayton (Shanghai) Pharmaceutical Co., Ltd.; Yu, Libing; Guo, Maojun; Yang, Qingang; Ren, Huasen; (19 pag.)CN105622613; (2016); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.923036-30-0,N-((3R,4R)-1-Benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine,as a common compound, the synthetic route is as follows.

Example 9; Preparation of [(3R, 4R)-1-benEyl-4-methyl-piperidin-3-yl]-methyl-(7H-pyrrolo[2,3-cl]pyrimidin-4-y.)-amine:; To a clean, nitrogen-purged reactor were charged 50% sodium hydroxide solution (210 ml) and (1-benzyl-4-methyl-piperidin-3-yl)-methyl-[7-(toluene-4-sulfonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-amine (30.0 g, 0.061 mol). The mixture was heated to 95-105C for a minimum of 5 hours then cooled to 70- 900C and water (300 ml) was added. The slurry was cooled to room temperature over a minimum of 1.5 hours and held at room temperature for 1 hour. The solids were isolated by filtration and washed with water (120.0 ml) to obtain 25.2 g of the title compound, water wet.1H NMR (400 MHz, CD3OD): delta 8.05 (s, 1H), 7.36-7.28 (m, 5H)1 7.24-7.20 (m, 1H), 7.06 (d, J=3.7 Hz, 1H), 6.62 (d, J=3.7 Hz, 1H), 5.08 (bs, 1H), 3.58-3.52 (m, 5H), 2.85 (dd, J=11.2, 7.0 Hz, 1H), 2.68 (dd, J=11.2, 3.7 Hz, 1H), 2.65-2.59 (m, 1 H), 2.45-2.39 (m, 1H), 2.29-2.20 (m, 1H), 1.90-1.81 (m, 1 H), 1.70- 1.63 (m, 1 H), 0.98 (d, J=7.0 Hz, 3H). 13C NMR (400 MHz, Of6-DMSO1 mixture of isomers): delta 166.8, 164.4, 158.6, 155.1 , 138.4, 137.9, 137.8, 136.6, 135.5, 135.3, 112.7, 110.0, 72.4, 64.3 (b), 62.4, (b), 60.3 (b), 44.5, 41.8, 40.9, 30.5, 24.8.

923036-30-0, The synthetic route of 923036-30-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2007/12953; (2007); A2;,
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