948571-47-9

Usage

Uses

Used in Pharmaceutical Applications:
2-(4-Amino-1H-pyrazol-1-yl)ethanol is used as a pharmaceutical compound for its potential anticonvulsant properties and its potential use in the treatment of neurological disorders.
Used in Chemical Research:
2-(4-Amino-1H-pyrazol-1-yl)ethanol is used as a reagent in organic synthesis and chemical research to facilitate the development of new compounds and materials.
Used in Organic Synthesis Industry:
2-(4-Amino-1H-pyrazol-1-yl)ethanol is used as a reagent in the organic synthesis industry for the synthesis of various organic compounds, contributing to the advancement of chemical research and the development of new pharmaceuticals and materials.

Upstream product

• 2075-46-9 4-nitro-1H-pyrazole 
• 540-51-2 2-bromoethanol 
• 42027-81-6 1-β-hysroxyethyl-4-nitropyrazole 

Downstream Products

• 1403894-06-3 2-(4-(7-(2-fluorobenzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-1H-pyrazol-1-yl)ethanol 
• 1421856-75-8 C₂₂H₂₁F₂N₇O₃ 
• 1394162-42-5 N-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)-5-(m-tolyl)oxazole-4-carboxamide 
• 1394161-75-1 5-m-tolyl-oxazole-4-carboxylic acid {1-[2-(4,6-dimethoxy-pyrimidin-2-yloxy)-ethyl]-1H-pyrazol-4-yl}-amide 
• 1394161-09-1 5-m-tolyl-oxazole-4-carboxylic acid {1-[2-(benzo[1,3]dioxol-5-yloxy)-ethyl]-1H-pyrazol-4-yl}-amide 
• 1394162-45-8 2-(4-(5-(m-tolyl)oxazole-4-carboxamido)-1H-pyrazol-1-yl)ethyl 4-methyl-benzenesulfonate 
• 1394162-44-7 2-(4-(5-(m-tolyl)oxazole-4-carboxamido)-1H-pyrazol-1-yl)ethyl methanesulfonate 
• 1453212-89-9 tert-butyl 4-{2-[4-({5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]pyrimidin-2-yl}amino)-1H-pyrazol-1-yl]ethyl}piperazine-1-carboxylate 
• 1453212-32-2 2-[4-({5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]pyrimidin-2-yl}amino)-1H-pyrazol-1-yl]ethyl methanesulfonate 
• 1453208-66-6 2-[4-({5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]pyrimidin-2-yl}amino)-1H-pyrazol-1-yl]ethanol 

Relevant academic research and scientific papers

FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF

The present disclosure relates to a class of fused pyrimidine compounds of Formula I, their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to a process of preparation of these fused pyrimidine compounds, and to pharmaceutical compositions containing them.

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

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 favourable selectivity for JAK3 in a panel of 9 kinases which contain the same cysteine. In a series of cytokinestimulated cellular analysis, compound 13 t, could potently block the JAK3-STAT signaling pathway. Further biological 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 experimental explorations suggested that 13t is a promising lead compound for the development of selective JAK3 inhibitor with therapeutic potential in rheumatoid arthritis.

Preparation method and application of novel 6-amino-1H-pyrazolo[3,4-d]pyrimidine JAK kinase inhibitors

The present invention provides drugs used for preventing, treating and/or ameliorating autoimmune diseases (such as psoriasis, rheumatoid arthritis, inflammatory enteritis diseases, Sjogren's syndrome, Behcet's disease, multiple sclerosis and systemic lupus erythematosus). The drugs have excellent JAK kinase inhibitory activity. The present invention also provides pharmaceutically acceptable compositions including the above compounds, and methods for preparing the compounds.

Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors

Janus kinases (JAKs) play a key role in the proliferation, apoptosis and differentiation of immune cells, and JAKs are considered as an attractive target for the treatment of inflammatory and autoimmune diseases. Here we show the design and optimization of pyrimidine-4,6-diamine derivatives as selectivity JAK3 inhibitors. Compound 11e, which might interact with unique cysteine (Cys909) residue in JAK3, exhibited excellent JAK3 inhibitory activity (IC50 = 2.1 nM) and high JAK kinase selectivity. In cellular assay, 11e showed moderate potency inhibiting IL-2-stimulated T cell proliferation. The data supports the further development of novel JAKs inhibitors.

Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors

A series of 4-aminoquinazolines derivatives containing hydrophilic group were designed and identified as potent Pan-PI3K inhibitors in this study. The results of antiproliferative assays in vitro showed that this series of compounds had strong inhibition of tumor growth, especially compound 7b for MCF-7 cells but weak inhibition to normal cells. PI3K kinase assay showed that 7b had high activity for three PI3K isoforms with the IC50 values of picomole. The western blot assay indicated that 7b could decrease the phospho-Akt (S473) in a dose-dependent manner. Further experiments showed that 7b could induce apoptosis in MCF-7 cells. Four key hydrogen bonding interactions were found in the docking of 7b with PI3K kinase. All these results suggested that 7b is a potent PI3K inhibitor and could be considered as a potential candidate for the development of anticancer agents.

2-substituted parazoleamino-4-substituted amino-5-pyrimidine formamide compound, composition and application thereof

The invention relates to a series of new compounds as a JAK inhibitor, as well as compositions and applications thereof, and particularly provides a series of compounds (I) that have a strong JAK inhibiting activity, or stereisomers, geometrical isomers, tautomers, pharmaceutically acceptable salts, prodrugs, metabolites, isotope derivatives, and solvates, as well as medicine compositions comprising such compounds. The invention also discloses applications of the compounds or the medicine compositions in preparation of a medicine, which is used for treatment of autoimmune diseases or cancer.

Preparation and application of novel 4,6-disubstituted aminopyrimidine JAK (janus kinase) inhibitor

The invention discloses preparation and application of novel 4,6-disubstituted aminopyrimidine JAK (janus kinase) inhibitors, and provide drugs which can be used for preventing, treating and/or improving autoimmune diseases (for example, psoriasis, rheumatoid arthritis, inflammatory enteritis diseases, Jagren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), and have excellent JAK inhibitory activity. The invention also provides pharmaceutically acceptable composition containing the compounds and methods for preparing the compounds.

Substitutive phenyl pyrimidine derivative as JAK kinase inhibitor or medicinal salt, preparation method and application thereof

The invention discloses a substitutive phenyl pyrimidine derivative as shown in a formula (I) as a JAK kinase inhibitor or medicinal salt, a preparation method and application thereof. The compound has excellent JAK inhibiting action and is used for preparing a drug for preventing, treating or improving autoimmune disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus and the like. The high activity JAK-3 inhibiting action IC50 shown by the compound can reach 1.7 n. The substitutive phenyl pyrimidine derivative is simple in synthetic route and high in implementation.

FUSED RING PYRIMIDINE COMPOUND, INTERMEDIATE, AND PREPARATION METHOD, COMPOSITION AND USE THEREOF

Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.

Preparation method and application of 4-arylamino-6-arylheterocyclyl-quinoline (quinazoline) antitumor compounds

The invention belongs to the technical field of medicine, and discloses a preparation method and application of 4-arylamino-6-arylheterocyclyl-quinoline (quinazoline) antitumor compounds. The derivatives have a structural formula represented by a formula I shown in the description, in the formula I, R1, R2, R3, R4, X, Y and n are defined as in the claims and in the description. The compounds provided by the invention have better antitumor activity, and can be used as kinase inhibitors for preparation of antitumor drugs.