368-99-0

Usage

Uses

Used in Pharmaceutical Industry:
3-(Difluoromethyl)aniline is used as a key intermediate in the synthesis of a series of selective inhibitors for herpes simplex virus types 1 and 2 (HSV1,2) Thymidine Kinases (TK). These inhibitors play a crucial role in the development of antiviral drugs targeting HSV1 and HSV2, as they can effectively inhibit the viral replication process by blocking the activity of the Thymidine Kinase enzyme.
The application of 3-(Difluoromethyl)aniline in the pharmaceutical industry is significant due to the growing need for effective antiviral agents to combat herpes simplex viruses, which are responsible for causing various illnesses, including cold sores, genital herpes, and other infections. The development of selective inhibitors for HSV1 and HSV2 Thymidine Kinases can lead to the creation of novel therapeutic options with improved efficacy and reduced side effects, benefiting patients suffering from herpes-related conditions.

Upstream product

• 403-25-8 1-(difluoromethyl)-3-nitrobenzene 
• 99-61-6 3-nitro-benzaldehyde 
• 619-28-3 m-nitrobenzylidene chloride 

Downstream Products

• 29848-59-7 1-bromo-3-difluoromethyl-benzene 
• 26029-52-7 m-benzotrifluoride 
• 1621270-68-5 4-(1-(3-(difluoromethyl)phenyl)-2,5-dioxo-2,3,4,5,6,7-hexahydro-1H-cyclopenta[d]pyrimidin-4-yl)benzonitrile 
• 1621271-17-7 4-(1-(3-(difluoromethyl)phenyl)-3-methyl-2,5-dioxo-2,3,4,5,6,7-hexahydro-1H-cyclopenta[d]pyrimidin-4-yl)benzonitrile 
• 1621271-43-9 4-(1-(3-(difluoromethyl)phenyl)-3-(methylsulfonyl)-2,5-dioxo-2,3,4,5,6,7-hexahydro-1H-cyclopenta[d]pyrimidin-4-yl)benzonitrile 
• 1621272-89-6 4-(4-bromophenyl)-1-(3-(difluoromethyl)phenyl)-3,4,6,7-tetrahydro-1H-cyclopenta [d]-pyrimidine-2,5-dione 
• 1621273-12-8 tert-butyl (4-cyano-2-(methylsulfonyl)phenyl)(2-(3-(difluoromethyl)phenylamino)-5-oxocyclopent-1-enyl)methylcarbamate 
• 1621272-88-5 3-(3-(difluoromethyl)phenylamino)cyclopent-2-enone 
• 1625672-35-6 4-(4-bromophenyl)-1-(3-(difluoromethyl)phenyl)-3,4,7,8-tetrahydroquinazoline-2,5(1H,6H)-dione 
• 1625669-54-6 4-(1-(3-(difluoromethyl)phenyl)-2,5-dioxo-1,2,3,4,5,6,7,8-octahydroquinazolin-4-yl)-benzonitrile 
• 1625672-37-8 1-(3-(difluoromethyl)phenyl)urea 
• 1625672-34-5 3-(3-(difluoromethyl)phenylamino)cyclohex-2-enone 
• 1615254-41-5 (S)-tert-butyl 1-(5-chloro-3-(3-(difluoromethyl)phenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)ethylcarbamate 

Relevant academic research and scientific papers

SUBSTITUTED PYRAZOLOPYRIMIDINES AS IRAK4 INHIBITORS

The present application relates to novel pyrazolopyrimidine derivatives for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases in humans and in animals, especially of proliferative disorders, autoimmune disorders, metabolic and inflammatory disorders characterized by an overreacting immune system, in particular rheumatological disorders, inflammatory skin disorders, cardiovascular disorders, lung disorders, eye disorders, neurological disorders, pain disorders and cancer, in human as well as of allergic and/or inflammatory diseases in animals, especially of atopic dermatitis and/or Flea Allergy Dermatitis, and especially in domestic animals, particularly in dogs.

Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity against VEGFR2, p38α, and B-Raf

A series of diarylurea inhibitors of the cardiac-specific kinase TNNI3K were developed to elucidate the biological function of TNNI3K and evaluate TNNI3K as a therapeutic target for the treatment of cardiovascular diseases. Utilizing a structure-based design, enhancements in kinase selectivity were engineered into the series, capitalizing on the established X-ray crystal structures of TNNI3K, VEGFR2, p38α, and B-Raf. Our efforts culminated in the discovery of an in vivo tool compound 47 (GSK329), which exhibited desirable TNNI3K potency and rat pharmacokinetic properties as well as promising kinase selectivity against VEGFR2 (40-fold), p38α (80-fold), and B-Raf (>200-fold). Compound 47 demonstrated positive cardioprotective outcomes in a mouse model of ischemia/reperfusion cardiac injury, indicating that optimized exemplars from this series, such as 47, are favorable leads for discovering novel medicines for cardiac diseases.

NOVEL INHIBITORS OF MAP4K1

The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.

ANIMAL AND HUMAN ANTI-MALARIAL AGENTS

Provided herein are Purine Comounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effectiv

ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.

HEPATITIS B ANTIVIRAL AGENTS

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS

The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts 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 asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Synthesis, properties, and pharmacokinetic studies of N2-phenylguanine derivatives as inhibitors of herpes simplex virus thymidine kinases

Two series of selective inhibitors of herpes simplex virus types 1 and 2 (HSV1,2) thymidine kinases (TK) have been developed as potential treatment of recurrent virus infections. Among compounds related to the potent base analog N2-[m-(trifluor