578729-05-2

Usage

Uses

Used in Pharmaceutical Industry:
Carbamic acid, [(1R)-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl]-, 1,1-dimethylethyl ester is used as a novel drug candidate for the development of new therapeutic agents. Its unique structure and properties make it a promising candidate for further research and development in the field of medicinal chemistry.
Used in Agrochemical Industry:
Carbamic acid, [(1R)-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl]-, 1,1-dimethylethyl ester is used as a building block for the synthesis of other bioactive compounds in the agrochemical industry. Its unique structure and properties can contribute to the development of new agrochemicals with improved efficacy and selectivity.
Used in Medicinal Chemistry Research:
Carbamic acid, [(1R)-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl]-, 1,1-dimethylethyl ester is used as a research tool in medicinal chemistry to explore its potential as a novel drug candidate. Its unique structure and properties make it an interesting target for further investigation and development in the field of chemical synthesis and drug discovery.

Upstream product

• 578729-21-2 [(R)-1-(4-bromo-phenyl)-ethyl]-carbamic acid tert-butyl ester 
• 73183-34-3 bis(pinacol)diborane 
• 24358-62-1 (R)-1-(4-bromophenyl)ethylamine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 27298-99-3 (R)-1-(4-chlorophenyl)ethylamine 

Downstream Products

• 1338544-26-5 (R)-tert-butyl methyl(1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)ethyl)carbamate 
• 1346819-06-4 (R)-1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)ethanamine hydrochloride 
• 1431551-93-7 tert-butyl ((R)-1-(4'-((4S,5R)-3-(2,2-dichloroacetyl)-4-(fluoromethyl)-2,2-dimethyloxazolidin-5-yl)-[1,1'-biphenyl]-4-yl)ethyl)carbamate 
• 871720-08-0 (R)-(4-(1-((tert-butoxycarbonyl)amino)ethyl)phenyl)boronic acid 
• 1338545-57-5 (R)-tert-butyl 1-(4-(8-methoxy-6-methyl-4-oxo-4,5-dihydrothieno[2,3-c]quinolin-9-yl)phenyl)ethylcarbamate 

Relevant academic research and scientific papers

Potential Foldamers Based on an ortho-Terphenyl Amino Acid

We describe the synthesis and characterization of a new class of oligomers built from a terphenyl-based amino acid. These oligomeric amides are of interest because the adoption of specific conformations could potentially be driven by the coordinated formation of inter-residue hydrogen bonds and aromatic interactions. Although high-resolution structural data have proven inaccessible, circular dichroism and nuclear magnetic resonance studies suggest that the new oligomers fold concomitantly with discrete self-association in chloroform.

DUAL KINASE-BROMODOMAIN INHIBITORS

Provided herein are compounds of Formula (I) that are dual inhibitors of kinases and bromo-domain proteins. The disclosure also relates to pharmaceutical compositions containing such compounds, methods for using such compounds in the treatment of cancers, particularly, the treatment of multiple myeloma cancers, and to related uses.

Design, synthesis and biological evaluation of novel 1-phenyl phenanthridin-6(5H)-one derivatives as anti-tumor agents targeting TOPK

T–lymphokine-activated killer cell–originated protein kinase (TOPK) is a serine-threonine mitogen-activated protein kinase that is highly expressed in many types of human cancer. Due to its important role in cancer progression, TOPK is becoming an attractive target in chemotherapeutic drug design. In this study, a series of 1-phenyl phenanthridin-6(5H)-one derivatives have been identified as a novel chemical class of TOPK inhibitors. Some of them displayed very potent anti-cancer activity with IC50s less than 100 nM, superior than reference compound OTS964. The most potent compound, 9g suppressed the growth of cancer cells by apoptosis and specifically inhibited the activities of TOPK. Oral administration of 9g effectively suppressed tumor growth with TGI >79.7% in colorectal cancer xenograft models, demonstrating superior efficacy compared to OTS964. Pharmacokinetic studies reveal its good oral bioavailability. Our findings therefore show that 9g is a specific inhibitor of TOPK both in vitro and in vivo that may be further developed as a potential therapeutic agent against colorectal cancer.

6 - Phenanthridone derivative and its preparation and use (by machine translation)

The invention belongs to the chemical field, and in particular relates to 6 - phenanthridone derivative and its preparation and use. The invention provides a 6 - phenanthridone derivatives, its structural formula as formula I shown. In addition, the inven

PHARMACEUTICALLY ACTIVE COMPOUNDS

The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Pyrrolopyrimidines and Pyrrolopyridines

Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

ALPHA-HYDROXY AMIDES AS BRADYKININ ANTAGONISTS OR INVERSE AGONISTS

α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd.(4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or(b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra.and (7)(CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3-to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl;

N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives

N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.