179250-25-0

Usage

Uses

Used in Pharmaceutical Research and Development:
TERT-BUTYL 4-(2-CYANOPHENYL)PIPERAZINE-1-CARBOXYLATE is utilized as a building block for the synthesis of biologically active molecules, contributing to the development of new pharmaceuticals with potential therapeutic applications.
Used in Medicinal Chemistry:
TERT-BUTYL 4-(2-CYANOPHENYL)PIPERAZINE-1-CARBOXYLATE is employed in medicinal chemistry as a valuable component for designing and creating novel drug candidates, given its unique chemical structure and properties.
Used in the Treatment of Various Diseases and Conditions:
TERT-BUTYL 4-(2-CYANOPHENYL)PIPERAZINE-1-CARBOXYLATE has potential therapeutic applications for addressing a range of diseases and conditions, although specific uses may vary depending on the synthesized molecules and their biological activities.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 111373-03-6 2-(piperazin-1-yl)benzonitrile 
• 2042-37-7 o-cyanobromobenzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 77278-40-1 tert-butyl 4-(benzoyloxy)piperazine-1-carboxylate 
• 100-47-0 benzonitrile 
• 394-47-8 2-fluorobenzonitrile 

Downstream Products

• 849106-84-9 4-(4-chloro-2-cyano-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 95371-99-6 2-(piperazin-1-yl)benzonitrile hydrochloride 
• 111373-03-6 2-(piperazin-1-yl)benzonitrile 
• 849106-87-2 5-chloro-2-piperazin-1-yl-benzoic acid methyl ester 
• 849106-86-1 4-(4-chloro-2-methoxycarbonyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 849106-85-0 4-(2-carboxy-4-chloro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 182181-36-8 2-(1-piperazinyl)-5-chlorobenzonitrile 
• 199105-20-9 1-tert-butoxycarbonyl-4-[2-(((methylsulfonyl)amino)methyl)phenyl]piperazine 
• 174855-53-9 tert-butyl 4-(2-(aminomethyl)phenyl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

A class of GPR40 agonist compounds with amide structure, and uses thereof

The present invention relates to a class of amide compounds with a novel structure, and a pharmaceutical composition thereof, wherein the structure of the amide compound is represented by a general formula (I). According to the present invention, the amide compound (I) can regulate GPR40 activity, and can be used for GPR40 activity related diseases such as diabetes and metabolic syndrome. The formula I is defined in the specification.

Site-Selective Copper-Catalyzed Amination and Azidation of Arenes and Heteroarenes via Deprotonative Zincation

Arene amination is achieved by site-selective C-H zincation followed by copper-catalyzed coupling with O-benzoylhydroxylamines under mild conditions. Key to this success is ortho-zincation mediated by lithium amidodiethylzincate base that is effective for a wide range of arenes, including nonactivated arenes bearing simple functionalities such as fluoride, chloride, ester, amide, ether, nitrile, and trifluoromethyl groups as well as heteroarenes including indole, thiophene, pyridine, and isoquinoline. An analogous C-H azidation is also accomplished using azidoiodinane for direct introduction of a useful azide group onto a broad scope of arenes and heteroarenes. These new transformations offer rapid access to valuable and diverse chemical space of aminoarenes. Their broad applications in organic synthesis and drug discovery are demonstrated in the synthesis of novel analogues of natural product (-)-nicotine and antidepressant sertraline by late-stage amination and azidation reactions.

TRICYCLIC COMPOUNDS

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers or congenital diseases. Specific cancers and congenital disease includes those that are mediated by YAP/TAZ.

CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Identification of novel GLUT inhibitors

The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

BMP INHIBITORS AND METHODS OF USE THEREOF

The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

Chemokine receptor antagonists and methods of use thereof

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.

Synthesis and Structure-Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor

The melanocortin receptors have been implicated as potential targets for a number of important therapeutic indications, including inflammation, sexual dysfunction, and obesity. We identified compound 1, an arylpiperazine attached to the dipeptide H-D-Tic-D-p-Cl-Phe-OH, as a novel melanocortin subtype-4 receptor (MC4R) agonist through iterative directed screening of nonpeptidyl G-protein-coupled receptor biased libraries. Structure-activity relationship (SAR) studies demonstrated that substitutions at the ortho position of the aryl ring improved binding and functional potency. For example, the o-isopropyl-substituted compound 29 (Ki = 720 nM) possessed 9-fold better binding affinity compared to the unsubstituted aryl ring (Ki = 6600 nM). Sulfonamide 39 (Ki = 220 nM) fills this space with a polar substituent, resulting in a further 2-fold improvement in binding affinity. The most potent compounds such as the diethylamine 44 (Ki = 60 nM) contain a basic group at this position. Basic heterocycles such as the imidazole 50 (Ki = 110 nM) were similarly effective. We also demonstrated good oral bioavailability for sulfonamide 39.

Substituted aryl piperazines as neurokinin antagonists

Disclosed are substituted aryl piperazines of Formula I STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.