629626-40-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 111-46-6 diethylene glycol 
• 139115-91-6 2-(2-tert-butyloxycarbonylaminoethoxy)ethanol 
• 603-35-0 triphenylphosphine 
• 34619-03-9 tert-butyldicarbonate 
• 192132-77-7 2-(2-(tert-butoxycarbonylamino)ethoxy)ethyl 4-methylbenzenesulfonate 

Downstream Products

• 629626-41-1 ethyl (Z)-2-(2-triphenylmethylaminothiazol-4-yl)-2-[2-(2-N-BOC-aminoethoxy)ethoxyimino]acetate 

Relevant academic research and scientific papers

ISOINDOLINE DERIVATIVES WHICH BIND TO AN ATP BINDING SITE

The present invention relates to novel probe compounds of formulae I and II defined herein. The present invention also relates to methods of synthesising these novel probe compounds and to their use in assays and screens for determining the binding of a test molecule to the ATP-binding site of a target protein, such as, for example, the Mismatch Repair (MMR) component proteins PMS2 and MLH1, or for determining the location and/or quantity of such target proteins in a biological sample.

Near-infrared fluorescence probe for targeting CYPPP1B1 enzyme as well as preparation method and application thereof

The present invention provides a near-infrared fluorescent probe targeting a CYP1B1 enzyme, and preparation and use thereof. The fluorescent probe comprises an affinity ligand, a signal group, and a linking chain for linking the ligand and the signal group. The linking chain comprises a plurality of ethylene glycol fragments. The affinity ligand is an alpha-naphthoflavone derivative, and the signal group is a near infrared fluorescent molecule. The near-infrared molecular probe targeting a tumor specific marker CYP1B1 enzyme effectively avoids the influence of introduction of the signal groupon inhibitory activity for the CYP1B1 enzyme, promotes application of the near-infrared molecular probe in the tumor in-vivo imaging, and has a good application prospect and clinical transformation value in the field of early diagnosis of tumor.

Agent for Preventing or Ameliorating Hearing Impairment

It is to provide an agent for preventing or improving hearing loss, which comprises a low molecular compound which can be produced relatively easily and inexpensively as an active ingredient. One or more compounds selected from the group consisting of compounds represented by the following formulas (I0), (II), and (III) and a pharmaceutically acceptable salt of the compounds when R3 is OH are used as an agent for preventing or improving hearing loss.

SUBSTITUTED 1-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINE MOLECULES AS PCSK9 ALLOSTERIC BINDERS

The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.

Design, Synthesis, and Biological Evaluation of Cytochrome P450 1B1 Targeted Molecular Imaging Probes for Colorectal Tumor Detection

Cytochrome P450 1B1 (CYP1B1) was found to be universally expressed in various tumors. Herein, we reported near-infrared fluorescent imaging probes for tumor detection via visualizing CYP1B1. After introducing the linker to a CYP1B1 selective inhibitor we found previously, we got the resulting compound 5b which kept strong inhibition ability against CYP1B1 (IC50 = 8.7 ± 1.2 nM) and high selectivity. Then, in vitro microscope studies and cell binding assay of probes indicated that the corresponding probe 6b could specifically be accumulated in CYP1B1 overexpressed colorectal cancer cell HCT-15 and showed satisfying binding affinity to target. During the in vivo noninvasive optical imaging, 6b was proved to rapidly lighten tumor in vivo as early as 6 h after injection. This work is the first attempt to visualize CYP1B1 for noninvasive imaging of tumor which could provide new approach for tumor diagnosis.

Erythropoietin Expression Promoter

The present invention provides an erythropoietin expression-enhancing agent that can cancel the suppression of erythropoietin production or promote erythropoietin production, and a therapeutic or preventive drug for anemia, a liver function-improving agent, an ischemic injury-improving agent, a renal protective agent, and an insulin secretagogue comprising the erythropoietin expression-enhancing agent. The erythropoietin expression-enhancing agent of the present invention comprises one or more compounds selected from the group consisting of compounds represented by the following general formulas (I), (II), and (III) and pharmaceutically acceptable salts thereof when R3 is OH.

Covalent Protein Labeling by Enzymatic Phosphocholination

We present a new protein labeling method based on the covalent enzymatic phosphocholination of a specific octapeptide amino acid sequence in intact proteins. The bacterial enzyme AnkX from Legionella pneumophila has been established to transfer functional phosphocholine moieties from synthetically produced CDP-choline derivatives to N-termini, C-termini, and internal loop regions in proteins of interest. Furthermore, the covalent modification can be hydrolytically removed by the action of the Legionella enzyme Lem3. Only a short peptide sequence (eight amino acids) is required for efficient protein labeling and a small linker group (PEG-phosphocholine) is introduced to attach the conjugated cargo.

COMPOSITIONS AND METHODS FOR TREATING CONDITIONS THAT AFFECT EPIDERMIS

The present invention relates to the compositions and methods for treating or alleviating conditions that affect the epidermis (e.g., wrinkles, sun damaged skin, symptoms of aged skin, or the like).

FUSED HETEROCYCLIC COMPOUND

A compound of the formula: wherein ring'' A is a 7-membered or 8-membered nitrogen- containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by -NR3-Y1-, -0-, -S-, -SO-, -SO2- or -CHR3- wherein R3 is a hydrogen atom or'' an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted C1-4 alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula = shows a single bond or a double bond, when ===R2 is - R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when ===R2 is =R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally, substituted imino group.

ALKYLOXY SUBSTITUTED THIAZOLOQUINOLINES AND THIAZOLONAPHTHYRIDINES

Thiazoloquinolines and thiazolonaphthyridines with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.