219504-20-8

Upstream product

• 52555-34-7 (1-iminoethyl)glycine 
• 68-12-2 N,N-dimethyl-formamide 
• 56481-32-4 5-bromo-2-methylimidazole-4-carboxaldehyde 
• 144-55-8 sodium hydrogencarbonate 
• 1093261-70-1 4-chloro-2-methyl-5-{[(phenylmethyl)oxy]methyl}-1H-imidazole 
• 1093261-68-7 N-(2-(benzyloxy)-1-cyanoethyl)acetamide 

Downstream Products

• 1093349-48-4 C₁₉H₁₂Cl₃FN₄O₂ 
• 279252-27-6 4-chloro-1-(2-chloro-4-iodobenzyl)-2-methylimidazole-5-carbaldehyde 
• 279252-80-1 3-(4-(N,N-bis-(tert-butoxycarbonyl)amino)-2-chlorobenzyl)-5-chloro-2-methylimidazole-4-carbaldehyde 

Relevant academic research and scientific papers

COMPOSITIONS FOR INHIBITING UBIQUITIN SPECIFIC PROTEASE 1

This disclosure relates to modulating ubiquitin specific protease 1 (USP1) and provides novel chemical compounds useful as inhibitors of USP1, as well as various uses of these compounds. USP1 inhibiting compounds are useful in the treatment of diseases and disorders associated with USP1, such as cancer.

Method for recovering and utilizing byproduct of chlorination of phosphorus pentachloride

The invention relates to a technology for comprehensively utilizing the byproduct of chlorination of phosphorus pentachloride, and mainly relates to a post treatment, which scientifically utilizes the excess phosphorus pentachloride reagent. The byproduct is converted into an organic synthesis reagent with a wide application range. The wastes are converted into a valuable resource. The discharge of waste water, waste gas, and waste solid is reduced. The obtained reagent is an excellent active reagent, which is widely used in the chemical industry, pharmacy industry, and material industry. The production cost is reduced, and the environment is protected.

Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallography of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led directly to the design of compound 43 that exhibits remarkable antiviral activity (EC50 1 nM) against a wide range of NNRTI-resistant viruses and a favorable pharmacokinetic profile across multiple species.

CHEMICAL COMPOUNDS

The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.

Aromatic ring derivatives

Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1and ch2each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.

IMIDAZOLE COMPOUNDS AND MEDICINAL USE THEREOF

Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.

Synthesis and calcium channel antagonist activity of nifedipine analogues containing 4(5)-chloro-2-methyl-5(4)-imidazolyl substituent

Dihydropyridine having substituted imidazole at 4-position in conjunction with various C3, C5 diesters have calcium channel antagonist activity. In this paper a group of dialkyl, dicycloalkyl and diaryl ester analogues of nifedipine, in which the ortho-nitro phenyl group at position 4 replaced by 2-methyl-4(5)-chloro-5(4)-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists using the high K+ contraction of guinea-pig ileal longitudinal smooth muscle (GPILSM). The results for the symmetrical ester series showed that increasing the length chain in C3 and C5 ester substituents increased activity. When increasing of the length or lipophilicity accompany with increasing the hindrance, the activity decreased. In asymmetrical diester series, the results showed when R1 is methyl or ethyl, increasing of the lipophilic property in R substituent increases the activity if this high lipophilicity don't accompany with steric hindrance. Our results demonstrate that in symmetrical and asymmetrical series aromatic compounds were more active than aliphatic compounds. In symmetrical diesters compounds, the most active compound was diphenylethyl ester derivative, that it was more active than the reference drug nifedipine. These structure activity data indicate that the 2-methyl-4(5)chloro5(4)-imidazolyl moiety is bioisoester of 2-nitrophenyl and 2-chlorophenyl moieties.