36669-02-0

Upstream product

• 186581-53-3 diazomethane 
• 16534-14-8 3-hydroxy-phthalic acid-1-methyl ester 
• 67-56-1 methanol 
• 37418-88-5 3-hydroxyphthalic anhydride 
• 67609-49-8 3-Trimethylsilanyloxy-cyclohexa-1,4-diene-1,2-dicarboxylic acid dimethyl ester 
• 496-64-0 3-hydroxy-2-pyrone 
• 762-42-5 dimethyl acetylenedicarboxylate 
• 108298-54-0 3-Trimethylsilyloxy-dimethyl-phthalate 
• 75232-81-4 2-Trimethylsilanyl-buta-1,3-dien-1-one 
• 74-88-4 methyl iodide 
• 601-97-8 3-hydroxyphthalic acid 
• 18063-93-9 dimethyl 1,4-dimethyl-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate 
• 85-44-9 phthalic anhydride 
• 684-93-5 1-methyl-1-nitrosourea 

Downstream Products

• 123732-28-5 3-benzyloxy-phthalic acid dimethyl ester 
• 365425-59-8 3-(2-amino-4-methoxycarbonyl-phenoxy)-phthalic acid dimethyl ester 
• 365425-55-4 dimethyl 3-(4-methoxycarbonyl-2-nitrophenoxy)phthalate 
• 365425-57-6 dimethyl 3-[4-methoxycarbonyl-2-(4-octadecanoylaminobenzoylamino)phenoxy]phthalate 
• 63382-37-6 4-(benzyloxy)isobenzofuran-1,3-dione 
• 92497-14-8 3-(benzyloxy)phthalic acid 
• 1054623-84-5 (3R,4R)-4-[4-(2-Benzyloxy-6-benzyloxycarbonyl-benzoyl)-3,5-bis-methoxymethoxy-benzoyloxy]-3-[4-(tert-butyl-dimethyl-silanyloxy)-benzoylamino]-azepane-1-carboxylic acid tert-butyl ester 
• 64208-33-9 dimethyl 3-allyloxyphthalate 
• 1061605-96-6 3-(3-bromo-benzyloxy)-phthalic acid dimethyl ester 
• 1061606-07-2 3-(3-methoxy-benzyloxy)-phthalic acid dimethyl ester 
• 1061606-47-0 3-(4-methoxy-benzyloxy)-phthalic acid dimethyl ester 
• 1061605-99-9 3-(3-methyl-benzyloxy)-phthalic acid dimethyl ester 
• 1061605-92-2 3-(3-fluoro-benzyloxy)-phthalic acid dimethyl ester 
• 1061605-82-0 3-(3-chloro-benzyloxy)-phthalic acid dimethyl ester 

Relevant academic research and scientific papers

BIFUNCTIONAL DEGRADERS OF HEMATOPOIETIC PROGENITOR KINASE AND THERAPEUTIC USES THEREOF

The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteosome pathway, and method for treating diseases modulated by HPK1.

DIELS- ALDER RING-OPENING PROCESS

The invention is directed to a process for the ring-opening of a cycloadduct of formula I obtainable from a reaction of a furanic compound and a diene, said process comprising contacting the cycloadduct with an acidic mixture comprising sulfuric acid and an activating agent to obtain a ring-opened product. The present invention is particularly directed a continuous process.

From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1)

Protein-protein interactions (PPIs) have emerged as significant targets for therapeutic development, owing to their critical nature in diverse biological processes. An ideal PPI-based target is the protein myeloid cell leukemia 1 (MCL1), a critical prosurvival factor in cancers such as multiple myeloma where MCL1 levels directly correlate to disease progression. Current strategies for halting the antiapoptotic properties of MCL1 revolve around inhibiting its sequestration of proapoptotic factors. Existing inhibitors disrupt endogenous regulatory proteins; however, this strategy actually leads to an increase of MCL1 protein levels. Here, we show the development of hetero-bifunctional small molecules capable of selectively targeting MCL1 using a proteolysis targeting chimera (PROTAC) methodology leading to successful degradation. We have confirmed the involvement of the E3 ligase CUL4A-DDB1 cereblon ubiquitination pathway, making these PROTACs a first step toward a new class of antiapoptotic B-cell lymphoma 2 family protein degraders.

NOVEL BROMINATED FURANONE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel brominated furanone derivative, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient, wherein the novel brominated furanone derivative or a pharmaceutically acceptable 5 salt thereof according to the present invention exhibits a quorum sensing inhibitory activity of bacteria and also can effectively inhibit the formation of biofilm of bacteria, and thus can be used as a pharmaceutical composition containing the same as an active ingredient, thereby having an effect of being useful, 10 for example, for periodontal diseases such as gingivitis and periodontitis, oral diseases, and the like.

Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

Here we report the development of a proteolysis targeting chimera (PROTAC) based on the combination of the unique features of the sirtuin rearranging ligands (SirReals) as highly potent and isotype-selective Sirt2 inhibitors with thalidomide, a bona fide

CLIPTAC COMPOSITION

This invention relates to proteolysis targeting chimeric molecules formed from the intracellular self-assembly of precursors via bioorthogonal click chemistry (CLIPTACs), as well as related precursor compositions, methods and therapeutic applications.

New bicyclic brominated furanones as potent autoinducer-2 quorum-sensing inhibitors against bacterial biofilm formation

Bacterial behaviors such as virulence factor secretion and biofilm formation are critical for survival, and are effectively regulated through quorum sensing, a mechanism of intra- and interspecies communication in response to changes in cell density and species complexity. Many bacterial species colonize host tissues and form a defensive structure called a biofilm, which can be the basis of inflammatory diseases. Periodontitis, a chronic inflammatory disease affecting the periodontium, is caused by subgingival biofilms related to periodontopathogens. In particular, Fusobacterium nucleatum is a major co-aggregation bridge organism in the formation and growth of subgingival biofilms, linking the early and late colonizers in periodontal biofilms. According to our previous study, the intergeneric quorum-sensing signal molecule autoinducer-2 (AI-2) of F. nucleatum plays a key role in intra- and interspecies interactions of periodontopathogens, and may be a good target for periodontal biofilm inhibition. Recently, brominated furanones produced by the macroalga Delisea pulchra were shown to inhibit biofilm formation via AI-2, and have been investigated toward the goal of increasing the inhibition effect. In this study, we describe the synthesis of new bromofuranone analogs, i.e., 3-(dibromomethylene)isobenzofuran-1(3H)-one derivatives, and demonstrate their inhibitory activities against biofilm formation by periodontopathogens, including F. nucleatum, Porphyromonas gingivalis, and Tannerella forsythia.

4'-O-SUBSTITUTED ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME

Provided are 4'-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Compounds and pharmaceutical use thereof

PCT No. PCT/JP97/00291 Sec. 371 Date Aug. 6, 1998 Sec. 102(e) Date Aug. 6, 1998 PCT Filed Feb. 6, 1997 PCT Pub. No. WO97/29079 PCT Pub. Date Aug. 14, 1997The compounds of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The Compound (I) and pharmaceutically acceptable salts thereof of the present invention selectively act on cannabinoid receptors, particularly peripheral receptors, cause less side effects on the central system, and have superior immunoregulating action, antiinflammatory action, antiallergic action and therapeutic effect on nephritis. Therefore, they are useful as cannabinoid receptor, particularly peripheral cannabinoid receptor activators and antagonists, immunoregulators, therapeutic agents for autoimmune diseases, antiinflammatory agents, antiallergic agents and therapeutic agents for nephritis.

Total synthesis of enantiomerically pure (-)-Balanol

The total synthesis of enantiomerically pure (-)-Balanol (1), using tri-O-acetyl-D-glucal as a chiral template for the central azepane fragment is described.