144464-64-2

Upstream product

• 3470-50-6 6-Hydroxy-1-tetralone 
• 407-25-0 trifluoroacetic anhydride 
• 37595-74-7 N,N-phenylbistrifluoromethane-sulfonimide 
• 1493-13-6 trifluorormethanesulfonic acid 
• 1078-19-9 6-methoxy-3,4-dihydro-1(2H)-naphthalenone 
• 1025373-45-8 trifluoromethanesulfonic acid anhydride 
• 358-23-6 trifluoromethylsulfonic anhydride 

Downstream Products

• 144464-66-4 5-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid methyl ester 
• 90401-84-6 6-cyano-1-tetralone 
• 71912-46-4 6-phenyl-3,4-dihydronaphthalene-1(2H)-one 
• 945632-75-7 6-octyl-3,4-dihydro-2H-naphthalen-1-one 
• 1262388-30-6 6-(2-methoxyphenyl)-1-naphthol 
• 6939-35-1 5-methyl-1-tetralone 
• 517874-22-5 6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,4-dihydronaphthalen-1(2H)-one 
• 26673-31-4 6-chloro-3,4-dihydronaphthalen-1(2H)-one 
• 3470-46-0 5-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid 
• 945632-52-0 2-amino-2-(6-octyl-1,2,3,4-tetrahydro-naphthalen-2-yl)propane-1,3-diol 
• 945632-77-9 2-bromo-6-octyl-3,4-dihydro-2H-naphthalen-1-one 
• 1118948-68-7 N-[2-hydroxy-1-hydroxymethyl-1-(6-octyl-1,2,3,4-tetrahydro-naphthalen-2-yl)ethyl]-acetamide 
• 945632-81-5 2-acetylamino-2-(6-octyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-malonic acid diethyl ester 
• 945632-79-1 2-acetylamino-2-(6-octyl-1-oxo-1,2,3,4-tetrahydro-naphthalen-2-yl)-malonic acid diethyl ester 

Relevant academic research and scientific papers

A short, efficient synthesis of 6-cyano-1-tetralones

A new, short and high-yield synthesis of 6-cyano-1-tetralones is described. Triflate intermediates 8 and 9 are versatile intermediates for the synthesis of other 6-substituted tetralones.

A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core

The bradykinin 1 (B1) receptor is upregulated during times of inflammation and is important for maintaining inflamed and chronic pain states. Blocking this receptor has been shown to reverse and/or ameliorate pain and inflammation in animal models. In this report, we describe a new class of B1 receptor antagonists that contain the piperidine acetic acid tetralin core. A structure-activity relationship for these analogs is described in this paper. The most potent compounds from this class have IC50s 20 nM in a B1 receptor functional assay. One of these compounds, 13g, shows modest oral bioavailability in rats.

Design, synthesis, and biological evaluation of Cyclobentinib (CB1107) as a potential anti-CML agent

Cyclobentinib was designed and synthesized as a novel anti-CML agent, its in vitro activity against K562 cells was evaluated by MTT assay. CB1107 showed remarkable cytotoxicity against K562 cell line with an IC50 of 0.037 ± 0.028 μmol/L, and thus it was 17-fold more potent than the reference drug Imatinib. Inducing cell apoptosis and affecting cell cycling of this compound in K562 cells were estimated by using flow cytometry and Acridine Orange/Ethidium Bromide (AO/EB) staining. The results showed that CB1107 was capable of arresting cell cycle at G0/G1 phase as well as inducing cell apoptosis significantly. Molecular mechanism of CB1107 was detected by the protein expression of Bcr-AblP210 using western blotting analysis. Downregulation of expression of Bcr-AblP210 was obviously revealed in the treatment of this tetralin amide compound. Of note, the results of these investigations suggested that CB1107 is more potent than the reference drug Imatinib against K562 cells. Additionally, in vivo results indicated that CB1107 significantly decreased tumor growth in K562 tumor-bearing Non-obese Diabetic/Severe Combined Immunodeficiency (NOD/SCID) mice. Histopathological investigation revealed that CB1107 without notable toxicity in a given dose range. These findings collectively demonstrate CB1107 is a promising candidate as a novel anti-CML agent.

MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF

The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.

PROCESSES AND INTERMEDIATES FOR PREPARING MCL1 INHIBITORS

The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.

Farnesoid X receptor (FXR) stimulant

The invention belongs to the technical field of medicines, and particularly relates to a compound as shown in the formula (I), and pharmaceutically acceptable salt and ester or a stereisomer thereof.R1, R2, R3, M1, M2, m, n, Q, L, ring A, ring B and ring

Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1

Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders. Herein we describe the structure-activity relationship of a novel tetralone series of DGAT1 inhibitors and our strategies for overcoming genotoxic liability of the anilines embedded in the chemical structures, leading to the discovery of a candidate compound, (S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid (GSK2973980A, 26d). Compound 26d is a potent and selective DGAT1 inhibitor with excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice. Based on the overall biological and developability profiles and acceptable safety profiles in the 7-day toxicity studies in rats and dogs, compound 26d was selected as a candidate compound for further development in the treatment of metabolic disorders.

CARBOXAMIDE INHIBITORS

The present invention provides a compound of formula I The compounds of formula I demonstrate properties as Smurf-1 inhibitors and are thus useful in the treatment of a range of disorders, particularly pulmonary arterial hypertension.

A DOR receptor antagonist compound as

The invention provides a compound used as a DOR receptor antagonist. The structural formula of the compound is as shown in the specification. In comparison with the prior art, the invention expounds a pharmaceutical composition and a preparation containin

COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS AND PHARMACEUTICAL USES THEREOF

The invention provides compounds as hepatitis C virus inhibitors and pharmaceutical uses thereof. Specifically, the invention provides compounds of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a