1021918-86-4

Usage

Uses

Used in Pharmaceutical Research:
1H-Benzimidazole-1-carboxylic acid, 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-, 1,1-dimethylethyl ester is used as a building block for the development of new drugs and biologically active compounds. Its benzimidazole core is a common structural motif in various pharmaceutical agents, making it a valuable component in medicinal chemistry.
Used in Organic Synthesis:
In the field of organic synthesis, 1H-BenziMidazole-1-carboxylic acid, 5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-, 1,1-diMethylethyl ester is utilized as a protected intermediate, taking advantage of the tetramethyl-1,3,2-dioxaborolane group to selectively modify specific functional groups in complex organic molecules. This selective protection allows for more controlled and efficient synthetic routes to target compounds.
Used in Drug Development:
1H-Benzimidazole-1-carboxylic acid, 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-, 1,1-dimethylethyl ester is employed as a precursor in the synthesis of drug candidates, particularly those with benzimidazole-based structures. Its stability and solubility-enhancing modifications make it an attractive starting material for the development of novel therapeutic agents.
Used in Chemical Research:
In the realm of chemical research, 1H-BenziMidazole-1-carboxylic acid, 5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-, 1,1-diMethylethyl ester serves as a model system for studying the reactivity and properties of benzimidazole derivatives. Its unique structural features provide insights into the fundamental chemistry of this important class of heterocyclic compounds, contributing to the broader understanding of organic and medicinal chemistry.

Upstream product

• 942590-05-8 1,1-dimethylethyl 5-bromo-1H-benzimidazole-1-carboxylate 
• 73183-34-3 bis(pinacol)diborane 
• 4887-88-1 5-bromo-1H-benzo[d]imidazole 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1426095-41-1 4-(1H-benzimidazol-5-yl)-N-{[(3R)-1-cyclopropylcarbonyl-3-pyrrolidinyl]methyl}-N-(phenylmethyl)benzamide 
• 1426095-32-0 4-(1H-benzimidazol-5-yl)-N-{[(3R)-1-cyclopropylcarbonyl-3-pyrrolidinyl]methyl}-N-(1-methylethyl)benzamide 

Relevant academic research and scientific papers

Heterocyclic compound with Wnt signal path inhibitory activity and application thereof

The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY

PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS

The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

FATTY ACID SYNTHASE INHIBITORS

This invention relates to carboxamides and reverse carboxamides according to Formula (I) and the use of carboxamides and reverse carboxamides for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of carboxamides and reverse carboxamides in the treatment of cancer.

ANTIMICROBIAL 4-OXOQUINOLIZINES

This invention provides novel 4-oxoquinolizine compounds and their uses for a series of broad-spectrum antibiotics having no cross-resistance to existing or emerging classes of antibiotics. In addition the novel 4-oxoquinolizine compounds are useful again

Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2- ones as potent and selective mTOR kinase inhibitors

We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency and exquisite kinase selectivity. Potent compounds from this series show >1000-fold selectivity over the related PI3Kα lipid kinase. Further, compounds such as 2 achieve mTOR pathway inhibition, blocking both mTORC1 and mTORC2 signaling, in PC3 cancer cells as measured by inhibition of pS6 and pAkt (S473).

AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS

This invention relates to the use of azabenzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of azabenzimidazoles in the treatment of cancer.

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS

The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

COMPOUND - 946

A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use intherapy, for example in the treatment of proliferative disease such as cancer and partic

HETEROARYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.