130200-01-0

Usage

Uses

Used in Organic Synthesis:
7-Bromo-2,2-dimethylchroman-4-one is used as an intermediate in the synthesis of various organic compounds. Its unique structure and functional groups make it a valuable building block for the preparation of complex organic molecules.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, 7-Bromo-2,2-dimethylchroman-4-one is used as a starting material for the development of new pharmaceutical drugs. Its potential biological activities and structural features make it a promising candidate for drug discovery and design.
Used in Antioxidant Research:
7-Bromo-2,2-dimethylchroman-4-one has been investigated for its potential antioxidant properties. Its ability to scavenge free radicals and protect cells from oxidative damage makes it a subject of interest in the field of natural products and drug discovery. 7-Bromo-2,2-dimethylchroman-4-one could potentially be used in the development of antioxidants for various applications, such as in the prevention of chronic diseases and the preservation of food products.
Used in Pharmaceutical Drug Synthesis:
As an intermediate in the synthesis of pharmaceutical drugs, 7-Bromo-2,2-dimethylchroman-4-one plays a crucial role in the development of new medications. Its unique structure and functional groups can be modified to create novel drug candidates with potential therapeutic benefits.

Upstream product

• 30186-18-6 4'-bromo-2'-hydroxyacetophenone 
• 67-64-1 acetone 
• 591-20-8 3-Bromophenol 
• 112090-04-7 3-methyl-but-2-enoic acid 4-bromo-phenyl ester 

Downstream Products

• 264265-10-3 bis[4-(dimethylamino)phenyl](2,2-dimethyl-7-chromenyl)methanol 
• 130200-02-1 2,2-dimethyl-4-oxo-3,4-dihydro-2H-1-benzopyran-7-carbonitrile 

Relevant academic research and scientific papers

NOVEL COMPOUNDS HAVING INHIBITORY ACTIVITY AGAINST GLUCOSYLCERAMIDE SYNTHASE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PROCESSES FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention provides a novel compound having a chromane, isochromane, thiochromane, or tetrahydroquinoline moiety or pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof. The compound having a chromane, isochromane, thiochromane, or tetrahydroquinoline moiety or pharmaceutically acceptable salt thereof has an inhibitory activity against glucosylceramide synthase (GCS), and therefore can be usefully applied for preventing or treating various diseases associated with GCS, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Parkinson's disease, etc.

Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes

A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK profiling led to multiple compounds with good physical properties, excellent oral bioavailability, and a clean in vitro safety profile. Compound 13 was identified as a lead compound as evidenced by the reversal of sulprostone-induced suppression of glucose-stimulated insulin secretion in INS 1E β-cells in vitro and in a rat ivGTT model in vivo. A glutathione adduction liability was eliminated by replacing the naphthalene of structure 13 with the indazole ring of structure 43.

BICYCLIC COMPOUND AND USE THEREOF

The present disclosure relates to a compound derivative containing a 6-7 bicyclic ring and use thereof. The compound according to the present invention can be effectively used in the prevention or treatment of diseases caused by PRMT5 by acting as a PRMT5 inhibitor.

BICYCLIC COMPOUND AND USE THEREOF

The present invention relates to a compound derivative comprising 6 -7 bicyclic rings and the use thereof. The compound according to the present invention may be used as PRMT5 inhibitor to prevent or treat diseases caused by PRMT5.

PYRIDIN-2-ONE DERIVATIVES OF FORMULA (II) USEFUL AS EP3 RECEPTOR ANTAGONISTS

The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.

PYRIDIN-2-ONE DERIVATIVES OF FORMULA (I) USEFUL AS EP3 RECEPTOR ANTAGONISTS

The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.

PYRIDIN-2-ONE DERIVATIVES OF FORMULA (III) USEFUL AS EP3 RECEPTOR ANTAGONISTS

The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.

Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors: SAR and in vivo efficacy in hyperalgesia pain model

A series of substituted tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives have been synthesized and their mPGES-1 biological activity has been disclosed in detail. Structure-activity relationship (SAR) optimization provided inhibitors with excellent mPGES-1 potency and low to moderate PGE2 release A549 cell potency. Among the mPGES-1 inhibitors studied, 7, 9 and 11l provided excellent selectivity over COX-2 (>200-fold) and >70-fold selectivity for COX-1 except 11l, which exhibited dual mPGES-1/COX-1 activity. Furthermore, the above tested mPGES-1 inhibitors demonstrated good metabolic stability in liver microsomes, high plasma protein binding (PPB) and no significant inhibition observed in clinically relevant CYP isoforms. Besides, selected mPGES-1 tool compounds 9 and 11l provided good in vivo pharmacokinetic profile and oral bioavailability (%F?=?33 and 85). Additionally, the representative mPGES-1 tool compounds 9 and 11l revealed moderate in vivo efficacy in the LPS-induced thermal hyperalgesia guinea pig pain model.

N-(1-HYDROXY-3-(PYRROLIDINYL)PROPAN-2-YL)PYRROLIDINE-3-CARBOXAMIDE DERIVATIVES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and compounds I for use to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS

The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)