1985605-59-1

Usage

Uses

Used in Pharmaceutical Industry:
(R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione is used as a potential therapeutic agent for the treatment of various diseases. Its specific application reason is due to its unique molecular structure, which may allow it to interact with biological targets and modulate cellular pathways, leading to therapeutic effects.
Used in Antiviral Applications:
In the field of antiviral research, (R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione may be employed as an antiviral agent, particularly against influenza virus infections. It could potentially act as a selective inhibitor of viral enzymes or proteins, similar to the mechanism of action of Baloxavir marboxil, which is a known inhibitor of influenza cap-dependent endonuclease. (R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione's application reason is its potential to exhibit therapeutic activity against influenza A and B virus infections, including strains resistant to current antiviral agents.
Used in Drug Delivery Systems:
(R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione may also be utilized in the development of novel drug delivery systems. These systems could enhance the compound's delivery, bioavailability, and therapeutic outcomes by employing various organic and metallic nanoparticles as carriers. The application reason for this use is to improve the overall effectiveness of the compound in treating the targeted diseases or conditions.

Upstream product

• 455-86-7 3,4-Difluorobenzoic acid 
• 2136287-65-3 3,4-difluoro-2-((phenylthio)methyl)benzoic acid 
• 2136287-66-4 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepin-11-one 
• 2136287-59-5 methyl 1-((tert-butoxycarbonyl)amino)-3-(benzyloxy)-4-oxo-1,4-dihydropyridine-2-carboxylic acid 
• 1985607-83-7 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepine-11-ol 
• 147-93-3 Thiosalicylic acid 
• 446-57-1 1-(chloromethyl)-2,3-difluorobenzene 
• 119736-16-2 3-(benzyloxy)-1-((tert-butoxycarbonyl)amino)-4-oxo-1,4-dihydropyridine-2-carboxylic acid ethyl ester 
• 1985607-83-7 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepine-11-ol 

Relevant academic research and scientific papers

SOLID STATE FORMS OF BALOXAVIR MARBOXIL

The present disclosure relates to solid state forms of baloxavir marboxil, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Condensed ring pyridone derivative as well as preparation method and application thereof

The invention discloses a condensed ring pyridone derivative as well as a preparation method and an application thereof. The condensed ring pyridone derivative is a compound shown in a formula I, or an optical isomer, an enantiomer, a diastereomer, a raceme or a racemic mixture thereof, or a solvate, a prodrug or pharmaceutically acceptable salt thereof. The invention also discloses the application of the compound and a pharmaceutical composition containing the compound in preparation of drugs for preventing and/or treating viral infection diseases. The viral infectious disease is a disease caused by a virus having a cap-dependent endonuclease, and more specifically, an infectious disease caused by influenza A or influenza B.

A MEDICAMENT FOR TREATING INFLUENZA CHARACTERIZED BY COMBINING A CAP-DEPENDENT ENDONUCLEASE INHIBITOR AND AN ANTI-INFLUENZA DRUG

A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is each independently CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A4 is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A are each independently hydrogen, halogen, alkyl, or the like; R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R1 is or the like, is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.

TREATING INFLUENZA USING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES AND PRODRUGS THEREOF

A method for treating influenza is described. The disclosed method generally involves administering an effective amount of a compound, for example baloxavir marboxil, to a subject having influenza, where the compound is administered initially at least about 48 hours after an onset of influenza. Generally, the effective amount is sufficient to alleviate a symptom of influenza in the subject as compared to a symptom that the subject has when the compound is first administered to the subject.

Method for synthesizing novel anti-influenza drug

The invention discloses a method for synthesizing a novel anti-influenza drug baloxavir marboxil. The method comprises the following steps: directly docking a thiosalicylic acid compound 1 and a 1-(halogenated methyl)-2,3-difluorobenzene compound 2 serving as initial raw materials so as to obtain a compound 3; performing PPA ring closure to obtain a 7,8-difluorodibenzo[b,e]thiozepine-11(6H)-one compound 4, and obtaining a key chiral thiazem intermediate compound 5 under catalysis of a chiral enzyme; directly condensating the compound 5 and a key chiral fragment compound 6 by virtue of a Mitsubobu reaction so as to obtain a compound 7; finally performing dealkylation protection, and condensating with ((methoxycarbonyl)oxo)4-methyl-toluenesulfonate, so as to obtain the final product compound9, namely the baloxavir marboxil. According to the synthetic route, the process operation magnification difficulty of the route is reduced, the production of by-products is reduced, the product purity is improved, and the cost of the route is reduced.

Polycyclic pyridone compound as well as pharmaceutical composition and application thereof

The invention provides a polycyclic pyridone compound as well as pharmaceutical composition and an application thereof. Specifically, the polycyclic pyridone compound is a compound shown as the formula (I) or pharmaceutically acceptable salt, solvate or hydrate of the compound. The compound can be used for preparing drugs for preventing or treating infectious diseases of mammals, and is particularly used for preparing drugs for preventing, treating, relieving and/or treating orthomyxovirus infection such as influenza A virus, influenza B virus and influenza C virus.

Substituted polycyclic carbamoyl pyridone derivative and its prodrug (by machine translation)

The invention discloses a group of substituted polycyclic carbamoyl pyridone derivative and its prodrug and its deuterated compounds, and their use as against influenza virus 5' cap structure (CAP) dependent endo enzyme activity inhibitors, for treating influenza virus caused by use of the common cold. The invention also comprising a pharmaceutically acceptable carrier with the combination of the compound of the present invention composition, and the use of the composition to inhibit the influenza virus propagation method. (by machine translation)

Substituted polycyclic pyridone derivative prodrug containing pharmaceutical composition

The present invention provides a pharmaceutical composition containing the following compound having antiviral action:P is hydrogen or a group to form a prodrug.

Substituted polycyclic pyridone derivative and its crystal

Substituted polycyclic pyridone derivative of the manufacturing method. Formula (I): (In the formula, R1 Is hydrogen, unsubstituted alkyl or other protecting group. ) Shown in compound, and/or magnesium salt in the presence of a sodium salt, Formula: R2 - OH (In the formula, R2 A non-substituted alkyl. ) Is reacted with a compound represented by the, formula (II): (In the formula, R2 The same significance as described above. ) Production of a compound represented.

Multiple ticyclic Pyridonecarboxylic deriv. and drag substd. aggrecanase

The present invention, a compound having antiviral action. And 1 A 1 the, CR 1A R 1B, S or O; A 2 the, CR 2A R 2B, S or O; A 3 the, CR 3A R 3B, S or O; A 4 the, CR 4A R 4B, S or O; Here, A 1, A 2, A 3, A 4, A 1 adjacent to a nitrogen atom, and A 4 adjacent carbon atoms in the hetero atom of the number of atoms constituting, in 1 or 2 ; R 1A and R 1B is, independently, a hydrogen, halogen, alkyl, etc.; or R 2A and R 2B is, independently, a hydrogen, halogen, alkyl, etc.; or R 3A and R 3B is, independently, a hydrogen, halogen, alkyl, etc.; or R 4A and R 4B is, independently, a hydrogen, halogen, alkyl, etc.; or R 3A and R 3B together non-aromatic or non-aromatic heterocyclic ring, a carbon ring may form; The X, CH 2, S or O; R 1 is, independently, halogen or like hydroxyacid; M is an integer of 0-2 N is an integer of 1-2)