837392-64-0

Usage

Uses

Used in Organic Synthesis:
5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) indolin-2-one is used as a reagent in organic synthesis for its ability to participate in various synthetic transformations. The presence of the boron atom in the molecule allows for the construction of complex organic molecules, making it a valuable tool in the synthesis of a wide range of compounds.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) indolin-2-one is used as a potential scaffold for the development of pharmaceutical drugs. Its indolin-2-one backbone may possess bioactive properties that can be exploited to create new drugs with therapeutic potential.
Used in Chemical Research:
5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) indolin-2-one is also used in chemical research to explore its unique structure and potential applications. Researchers are interested in understanding the compound's properties and reactivity, as well as its potential to contribute to the advancement of chemical science.
Used in Pharmaceutical Drug Development:
In the pharmaceutical industry, 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) indolin-2-one is used as a starting material for the development of new drugs. Its potential bioactive properties and unique structure make it a promising candidate for the creation of innovative therapeutic agents.
Used in Material Science:
Although not explicitly mentioned in the provided materials, the unique structure of 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) indolin-2-one may also find applications in material science. Its boron-containing structure could potentially be utilized in the development of new materials with specific properties, such as high thermal stability or unique electronic characteristics.

InChI:InChI=1/C14H18BNO3/c1-13(2)14(3,4)19-15(18-13)10-5-6-11-9(7-10)8-12(17)16-11/h5-7H,8H2,1-4H3,(H,16,17)

Upstream product

• 20870-78-4 5-bromo-2-indolin-2-one 
• 73183-34-3 bis(pinacol)diborane 
• 87-48-9 5-Bromo-1H-indole-2,3-dione 
• 59-48-3 2-oxoindole 

Downstream Products

• 1040376-80-4 5-{5-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-6-methyl-pyridin-3-yl}-1,3-dihydro-indol-2-one 
• 1279104-21-0 2-(2,3-Difluoro-phenyl)-5-(2-methyl-5-pyridin-3-yl-2H-pyrazol-3-yl)-1H-indole 
• 1220696-38-7 1-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3-dihydro-2H-indol-2-one 
• 1613639-40-9 spiro(cyclopropane-1,3-indolin)-2-one-5-boronic acid pinacol ester 
• 1464155-56-3 tert-butyl 4-(4-(3-(2-oxoindolin-5-yl)imidazo[1,2-b]pyridazin-6-yl)benzoyl)-1,4-diazepane-1-carboxylate 
• 1613639-02-3 N-{(R)-2-[5-(2-oxo-2,3-dihydro-1H-indol-5-yl)pyridin-3-ylamino]-2-phenylethyl}acetamide 
• 1613638-62-2 5-{5-[(S)-1-(2-chlorophenyl)-2-hydroxyethylamino]pyridin-3-yl}-1,3-dihydroindol-2-one 
• 1613638-60-0 5-{5-[(R)-1-(2-chlorophenyl)-2-hydroxyethylamino]pyridin-3-yl}-1,3-dihydroindol-2-one 
• 1464151-31-2 5-(6-(4-(4-morpholinopiperidine-1-carbonyl)phenyl)imidazo[1,2-b]pyridazin-3-yl)indolin-2-one 
• 1464151-30-1 5-(6-(4-(1,4-diazepane-1-carbonyl)phenyl)imidazo[1,2-b]pyridazin-3-yl)isoindolin-1-one 

Relevant academic research and scientific papers

KMU-1170, a novel multi-protein kinase inhibitor, suppresses inflammatory signal transduction in THP-1 cells and human osteoarthritic fibroblast-like synoviocytes by suppressing activation of NF-κB and NLRP3 inflammasome signaling pathway

Protein kinases regulate protein phosphorylation, which are involved in fundamental cellular processes such as inflammatory response. In this study, we discovered a novel multi-protein kinase inhibitor, KMU-1170, a derivative of indolin-2-one, and investigated the mechanisms of its inflammation-inhibiting signaling in both THP-1 cells and human osteoarthritic fibroblast-like synoviocytes (FLS). We demonstrated that in THP-1 cells, KMU-1170 inhibited lipopolysaccharide (LPS)-induced upregulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and, furthermore, suppressed LPS-induced phosphorylation of transforming growth factor- β-activated kinase 1, JNK, ERK, inhibitor of NF-κB kinase α/β (IKKα/α), and NF-κB p65 as well as nuclear translocation of NF-κB p65. Moreover, KMU-1170 suppressed LPS-induced upregulation of proinflammatory cytokines such as IL-1β, TNF-α, and IL-6, and, notably, inhibited LPS-induced upregulation of the NLRP3 inflammasome in THP-1 cells. Importantly, KMU-1170 attenuated LPS-mediated inflammatory responses in human osteoarthritic FLS, such as the upregulation of IL-1β, TNF-α, IL-6, iNOS, and COX-2 and the phosphorylation of IKKα/β and NF-κB p65. Collectively, these results suggest that KMU-1170 inhibits inflammatory signal transduction and could be developed as a potential anti-inflammatory agent.

KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Disclosed are kinase inhibitor compounds having the following structure: (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3,R4, R5, R6, N-Ar, X, Y, Z, and AA are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Disclosed herein are kinase inhibitor compounds having structure (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, X, Y, Z, and (AA) are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

Anti-inflammatory effects of the novel PIM kinase inhibitor KMU-470 in raw 264.7 cells through the TLR4-NF-κb-NLRP3 pathway

PIM kinases, a small family of serine/threonine kinases, are important intermediates in the cytokine signaling pathway of inflammatory disease. In this study, we investigated whether the novel PIM kinase inhibitor KMU-470, a derivative of indolin-2-one, inhibits lipopolysaccharide (LPS)-induced inflammatory responses in RAW 264.7 cells. We demonstrated that KMU-470 suppressed the production of nitric oxide and inducible nitric oxide synthases that are induced by LPS in RAW 264.7 cells. Furthermore, KMU-470 inhibited LPS-induced up-regulation of TLR4 and MyD88, as well as the phosphorylation of IκB kinase and NF-κB in RAW 264.7 cells. Additionally, KMU-470 suppressed LPS-induced up-regulation at the transcriptional level of various proinflammatory cytokines such as IL-1β, TNF-α, and IL-6. Notably, KMU-470 inhibited LPS-induced up-regulation of a major component of the inflammasome complex, NLRP3, in RAW 264.7 cells. Importantly, PIM-1 siRNA transfection attenuated up-regulation of NLRP3 and pro-IL-1β in LPStreated RAW 264.7 cells. Taken together, these findings indicate that PIM-1 plays a key role in inflammatory signaling and that KMU-470 is a potential anti-inflammatory agent.

INHIBITORS OF FIBROBLAST ACTIVATION PROTEIN

Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.

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

NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE

The present invention relates to compound of Formula (I) or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula (I).

NOVEL BI-RING PHENYL-PYRIDINES/PYRAZINES FOR THE TREATMENT OF CANCER

The invention provides novel compounds having the general formula: wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.

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.

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.