867333-30-0

Upstream product

• 586-75-4 4-chlorobenzoyl chloride 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 1122-91-4 4-bromo-benzaldehyde 
• 586-76-5 4-Bromobenzoic acid 

Downstream Products

• 1018070-76-2 tert-butyl 4-(4-{[7-(2-chloro-5-methoxyphenyl)-5-methyl-1,2,4-benzotriazin-3-yl]amino}benzoyl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

KINASE MODULATORS AND METHODS OF USE THEREOF

The present invention relates to novel compounds that modulate the activity of one or more kinases, such as TYK2 or mutants thereof. The compounds, which may be kinase inhibitors or activators, are useful for treating autoimmune diseases, such as, such as psoriasis, lupus, multiple sclerosis, and inflammatory bowel disease.

NaI-mediated oxidative amidation of benzyl alcohols/aromatic aldehydes to benzamides via electrochemical reaction

In this research, we have developed a mild electrochemical process for oxidative amidation of benzyl alcohols/aromatic aldehydes with cyclic amines into the corresponding benzamides. This electroorganic synthetic method proceeds using NaI as a redox mediator under ambient temperature in undivided cell, providing more than 25 examples of amide products in moderate to good yields. The benefits of this reaction include one-pot synthesis, open air condition, proceed in aqueous media and no requirement of external conducting salt, base and oxidant.

Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1

JNJ4796, a small molecule fuse inhibitor targeting the conserved stem region of hemagglutinin, effectively neutralized a broad spectrum of group 1 influenza A virus (IAV), and protected mice against lethal and sublethal influenza challenge after oral admi

Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms

We report the synthesis and biochemical evaluation of a series of substituted 4-(4-aroylpiperazine-1-carbonyl)benzenesulfonamides (5a-s) developed as inhibitors of druggable carbonic anhydrase (CA) isoforms, as tools for the identification of new therapeu

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, comprising same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

Oxazolo[4,5-b]pyridine-Based Piperazinamides as GSK-3β Inhibitors with Potential for Attenuating Inflammation and Suppression of Pro-Inflammatory Mediators

Recent studies reveal that glycogen synthase kinase-3β (GSK-3β) acts as a pro-inflammatory enzyme, and by inhibiting this kinase, inflammation can be controlled. In this regard, a series of 17 piperazine-linked oxazolo[4,5-b]pyridine-based derivatives was

PIPERAZINE DERIVATIVES AS FASN INHIBITORS

Compounds of the formula (I), in which R, X1, X2, X3, X4, R1, R2 and q have the meanings indicated in Claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for th

NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN

The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)- 2H-phthalazin-1-ones as potent PARP-1 inhibitors

We have developed a series of substituted 4-(thiophen-2-ylmethyl)-2H- phthalazin-1-ones as potent PARP-1 inhibitors. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to, or higher than AZD-2281. Among these compounds, 18q appeared to be the most notable one, which displayed an 8-fold improvement in enzymatic activity compared to AZD-2281. These efforts lay the foundation for our further investigation.

TRICYCLIC HETEROCYCLE DERIVATIVES AS HISTAMINE H3 ANTAGONISTS

The present invention relates to novel Tricyclic Heterocylce Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is -CH-. -C(halo)- or -N-; Y is -C(O)-, -S-. -S(O)-, -S(O)2-, -CH2- or -O-, such that Y is not -O- when an adjacent atom is N.