847728-89-6

Usage

Uses

Used in Chemical Research:
(S)-[1-(4-BROMO-PHENYL)-ETHYL]-CARBAMIC ACID TERT-BUTYL ESTER is used as a reagent in chemical research for the synthesis of various organic compounds. Its unique structure allows for versatile reactions and the formation of new chemical entities.
Used in Pharmaceutical Synthesis:
In the pharmaceutical industry, (S)-[1-(4-BROMO-PHENYL)-ETHYL]-CARBAMIC ACID TERT-BUTYL ESTER is used as an intermediate in the synthesis of pharmaceuticals. Its presence in the synthesis process can contribute to the development of new drugs with potential therapeutic benefits.
Used in Medicinal Chemistry:
(S)-[1-(4-BROMO-PHENYL)-ETHYL]-CARBAMIC ACID TERT-BUTYL ESTER is used as a building block in medicinal chemistry for the design and development of new pharmaceutical agents. Its structural features may offer advantages in the creation of molecules with specific biological activities.
Used in Agricultural Chemistry:
Although not explicitly mentioned in the provided materials, given its potential applications in medicinal chemistry, (S)-[1-(4-BROMO-PHENYL)-ETHYL]-CARBAMIC ACID TERT-BUTYL ESTER could also be used in agricultural chemistry, potentially for the development of new agrochemicals or pesticides.
It is important to handle and use (S)-[1-(4-BROMO-PHENYL)-ETHYL]-CARBAMIC ACID TERT-BUTYL ESTER with care, following safety guidelines to prevent any potential harm to human health and the environment.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 27298-97-1 (S)-1-(4-bromophenyl)ethylamine 
• 84499-77-4 (S)-α-(p-bromophenyl)ethylamine hydrochloride 

Downstream Products

• 1014644-95-1 4-[(1S)-1-(tert-butoxycarbonylamino)ethyl]benzoic acid 
• 847728-90-9 (S)-methyl 4-(1-((tert-butoxycarbonyl)amino)ethyl)benzoate 
• 878805-06-2 t-butyl {(1S)-1-[4-(pyrazin-2-ylamino)phenyl]ethyl}carbamate 
• 1037252-32-6 [(S)-1-(4-formyl-phenyl)ethyl]carbamic acid tertbutyl ester 
• 1037252-24-6 tert-butyl ((1S)-1-{4-[hydroxy(pyridin-2-yl)methyl]phenyl}ethyl)carbamate 
• 1037251-45-8 tert-butyl [(1S)-1-(4-acetylphenyl)ethyl]carbamate 
• 1038801-13-6 benzyl (2S)-2-[(4-{(1S)-1-[(tert-butoxycarbonyl)amino]ethyl}phenyl)(hydroxy)methyl]-2-methylpyrrolidine-1-carboxylate 
• 1037254-24-2 benzyl (2S)-2-[(4-{(1S)-1-[(tert-butoxycarbonyl)amino]ethyl}phenyl)(hydroxy)methyl]-2-methylpyrrolidine-1-carboxylate 
• 1446006-99-0 (S)-N-(1-{4-[3-(4-ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethyl)-2,2,2-trifluoro-acetamide 
• 1446007-00-6 (S)-1-(1-{4-[3-(4-ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethyl)-3-pyrimidin-4-yl-urea 
• 1446007-17-5 (S)-4-(1-{4-[3-(4-ethoxy-phenoxy)-azetidin-1-yl]-phenyl}-ethylamino)-5H-furan-2-one 
• 1556019-43-2 tert-butyl N-[(1S)-1-[4-(trimethylsilylmethylcarbamoyl)phenyl]ethyl]carbamate 
• 1556019-44-3 tert-butyl N-[(1S)-1-[4-(trimethylsilylmethylcarbamothioyl)phenyl]ethyl]carbamate 
• 1556019-46-5 tert-butyl N-[(1S)-1-[4-[5-(3,4,5-trichlorophenyl)-3-(trifluoromethyl)-2,4-dihydropyrrol-3-yl]phenyl]ethyl]carbamate 

Relevant academic research and scientific papers

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Src homology 2 domain-containing phosphatase 2 (SHP2) is an attractive therapeutic target for human cancers and other human diseases. Herein, we report our discovery of potent small-molecule SHP2 degraders whose design is based upon the proteolysis-targeting chimera (PROTAC) concept. This work has led to the discovery of potent and effective SHP2 degraders, exemplified by SHP2-D26. SHP2-D26 achieves DC50 values of 6.0 and 2.6 nM in esophageal cancer KYSE520 and acute myeloid leukemia MV4;11 cells, respectively, and is capable of reducing SHP2 protein levels by >95% in cancer cells. SHP2-D26 is >30-times more potent in inhibition of phosphorylation of extracellular signal-regulated kinase (ERK) and of cell growth than SHP099, a potent SHP2 inhibitor, in KYSE520 and MV4;11 cancer cell lines. This study demonstrates that induced SHP2 degradation is a very effective approach to inhibit the function of SHP2. Further optimization of these SHP2 degraders may lead to the development of a new class of therapies for cancers and other human diseases.

Discovery and characterization of a potent and selective EP4 receptor antagonist

Abstract EP4 is a prostaglandin E2 receptor that is a target for potential anti-nociceptive therapy. Described herein is a class of amphoteric EP4 antagonists which reverses PGE2-induced suppression of TNFα prod

BRM TARGETING COMPOUNDS AND METHODS OF USE THEREOF

The present invention relates to bifunctional compounds comprising a binding fraction to a target protein and a binding fraction to ubiquitin ligase E3, and associated methods of use.

TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.

SUBSTITUTED PYRAZOLE COMPOUNDS AS TOLL RECEPTOR INHIBITORS

Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Aptamer-PROTAC Conjugates (APCs) for Tumor-Specific Targeting in Breast Cancer

Development of proteolysis targeting chimeras (PROTACs) is emerging as a promising strategy for targeted protein degradation. However, the drug development using the heterobifunctional PROTAC molecules is generally limited by poor membrane permeability, low in vivo efficacy and indiscriminate distribution. Herein an aptamer-PROTAC conjugation approach was developed as a novel strategy to improve the tumor-specific targeting ability and in vivo antitumor potency of conventional PROTACs. As proof of concept, the first aptamer-PROTAC conjugate (APC) was designed by conjugating a BET-targeting PROTAC to the nucleic acid aptamer AS1411 (AS) via a cleavable linker. Compared with the unmodified BET PROTAC, the designed molecule (APR) showed improved tumor targeting ability in a MCF-7 xenograft model, leading to enhanced in vivo BET degradation and antitumor potency and decreased toxicity. Thus, the APC strategy may pave the way for the design of tumor-specific targeting PROTACs and have broad applications in the development of PROTAC-based drugs.

GPX4 protein degradation agent, preparation method and application thereof, and antitumor cell drug

The invention provides a GPX4 protein degradation agent, a preparation method thereof, and an anti-tumor cell drug, and belongs to the technical field of drug application. The GPX4 protein degradation agent provided by the invention has a protein degradation targeting chimera (PROTAC) molecular structure, a mother nucleus structure of the GPX4 protein degradation agent is used as a small molecule ligand for combining target protein, an A2 substituent is used as a small molecule ligand for combining an E3 ubiquitin ligase compound, and an A1 substituent is used as a connecting group for connecting the two ligands. The GPX4 protein degradation agent with the structure can specifically recognize GPX4 protein and effectively ubiquitinate and degrade the GPX4 protein, so that tumor cell ferroptosis is induced.

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 1 PROTEINS

The present invention relates to compounds comprising an interleukin-1 receptor-associated kinase 1 (IRAK1) protein binding moiety and a Von Hippel-Lindau (VHL) E3 ubiquitin ligase binding moiety, and associated methods of use. The compounds are useful as modulators of targeted ubiquitination, especially with respect to IRAK1, which is degraded by the compounds according to the invention.

SMARCA2-VHL DEGRADERS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF KRAS

Bifunctional compounds, which find utility as modulators of Kirsten ras sarcoma protein (KRas or KRAS), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the Von Hippel-Lindau E3 ubiquitin ligase and on the other end a moiety which binds KRas, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The heterobifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.