cas 1985605-59-1, (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

Articles about 1985605-59-1Total 10 be found

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.
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(2020/06/20)

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.
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(2020/08/30)

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.
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(2020/04/25)

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.
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Paragraph 00141

(2020/09/19)

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.
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(2019/04/04)

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.
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Paragraph 0079-0081

(2020/10/04)

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.
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(2018/03/13)

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)
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Paragraph 0099; 0101; 0106; 0107; 0108; 0165; 0166; 0167

(2018/09/13)

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.
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(2018/06/30)

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)
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(2016/10/27)