AR109433A1 - SULFONIMIDOILPURINONA 7-SUBSTITUTED AND DERIVATIVE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION - Google Patents

SULFONIMIDOILPURINONA 7-SUBSTITUTED AND DERIVATIVE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION

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Publication number
AR109433A1
AR109433A1 ARP170102378A ARP170102378A AR109433A1 AR 109433 A1 AR109433 A1 AR 109433A1 AR P170102378 A ARP170102378 A AR P170102378A AR P170102378 A ARP170102378 A AR P170102378A AR 109433 A1 AR109433 A1 AR 109433A1
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AR
Argentina
Prior art keywords
alkyl
carbonyl
benzyl
amino
propylsulfonimidoyl
Prior art date
Application number
ARP170102378A
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Spanish (es)
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Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR109433A1 publication Critical patent/AR109433A1/en

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Abstract

Composiciones que incluyen los compuestos y métodos de utilización de los compuestos en el tratamiento de la infección por el virus de la hepatitis B. Reivindicación 1: Compuesto de formula (1), en la que: R¹ es alquilo C₁₋₆; R² es bencilo, estando dicho bencilo no sustituido o sustituido con uno, dos o tres sustituyentes seleccionados independientemente de entre halógeno y alquilo C₁₋₆; R³ es -NR⁴R⁵, en la que R⁴ es alquilo C₁₋₆ o alcoxi C₁₋₆-alquilo C₁₋₆; R⁵ es (alquil C₁₋₆)₂NCOO-alquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, alcoxi C₁₋₆-carbonil(alquil C₁₋₆)amino-alquilo C₁₋₆, alcoxi C₁₋₆-carbonil(fenil)alquilo C₁₋₆, alcoxi C₁₋₆-carbonil-alquilo C₁₋₆, alcoxi C₁₋₆-carboniloxi-alquilo C₁₋₆, alquilo C₁₋₆, alquil C₁₋₆-carbonil(alquil C₁₋₆)amino-alquilo C₁₋₆ o pirrolidinilcarbamoiloxi-alquilo C₁₋₆, o R⁴ y R⁵ conjuntamente con el nitrógeno se unen para formar un heterociclilo; o una sal, enantiómero o diastereómero farmacéuticamente aceptable de los mismos, con la condición de que: 6-amino-9-bencil-2-(propilsulfonimidoil)-7-(pirrolidin-1-carbonil)purín-8-ona, 6-amino-9-bencil-7-(piperidin-1-carbonil)-2-(propilsulfonimidoil)purín-8-ona, 6-amino-9-bencil-7-(morfolin-4-carbonil)-2-(propilsulfonimidoil)purín-8-ona, 6-amino-9-bencil-7-(3,3-dimetilpirrolidin-1-carbonil)-2-(propilsulfonimidoil)purín-8-ona, 1-[6-amino-9-bencil-8-oxo-2-(propilsulfonimidil)purín-7-carbonil]pirrolidin-2-carboxilato de etilo, 6-amino-7-(2-azaspiro[3.3]heptano-2-carbonil)-9-bencilo-2-(propilsulfonimidoil)purín-8-ona, 6-amino-9-bencil-7-(2-oxa-6-azaspiro[3.3]heptano-6-carbonil)-2-(propilsulfonimidoil)purín-8-ona, 6-amino-9-bencil-7-(3,3-difluoropirrolidin-1-carbonil)-2-(propilsulfonimidoil)purín-8-ona, 6-amino-9-bencil-7-(3-fluoro-3-metilpirrolidin-1-carbonil)-2-(propilsulfonimidoil)purín-8-ona, y los enantiómeros o diastereómeros de los mismos están excluidos.Compositions including the compounds and methods of using the compounds in the treatment of hepatitis B virus infection. Claim 1: Compound of formula (1), wherein: R¹ is C₁₋₆ alkyl; R² is benzyl, said benzyl being unsubstituted or substituted with one, two or three substituents independently selected from halogen and C₁₋₆ alkyl; R³ is -NR⁴R⁵, wherein R⁴ is C₁₋₆ alkyl or C₁₋₆ alkoxy-C₁₋₆ alkyl; R⁵ is (C₁₋₆ alkyl) ₂NCOO-C₁₋₆ alkyl, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₁₋₆ alkoxycarbonyl (C₁₋₆ alkyl) aminoC₁₋₆ alkyl, C₁₋₆-carbonyl alkoxy (phenyl) C₁₋₆ alkyl, C₁₋₆-carbonyl-C₁₋₆ alkyl, C₁₋₆-carbonyloxy-C₁₋₆ alkyl, C alquilo alkyl, C₁₋₆-carbonyl (C₁₋₆ alkyl) amino -C₁₋₆ alkyl or pyrrolidinylcarbamoyloxy-C₁₋₆ alkyl, or R⁴ and R⁵ together with the nitrogen join to form a heterocyclyl; or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof, with the proviso that: 6-amino-9-benzyl-2- (propylsulfonimidoyl) -7- (pyrrolidin-1-carbonyl) purine-8-one, 6- amino-9-benzyl-7- (piperidin-1-carbonyl) -2- (propylsulfonimidoyl) purin-8-one, 6-amino-9-benzyl-7- (morpholin-4-carbonyl) -2- (propylsulfonimidoyl) purine-8-one, 6-amino-9-benzyl-7- (3,3-dimethylpyrrolidin-1-carbonyl) -2- (propylsulfonimidoyl) purine-8-one, 1- [6-amino-9-benzyl- Ethyl 8-oxo-2- (propylsulfonimidyl) purin-7-carbonyl] pyrrolidin-2-carboxylate, 6-amino-7- (2-azaspiro [3.3] heptane-2-carbonyl) -9-benzyl-2- ( propylsulfonimidoyl) purine-8-one, 6-amino-9-benzyl-7- (2-oxa-6-azaspiro [3.3] heptane-6-carbonyl) -2- (propylsulfonimidoyl) purine-8-one, 6-amino -9-benzyl-7- (3,3-difluoropyrrolidin-1-carbonyl) -2- (propylsulfonimidoyl) purin-8-one, 6-amino-9-benzyl-7- (3-fluoro-3-methylpyrrolidin-1 -carbonyl) -2- (propylsulfonimidoyl) purine-8-one, and the enantiomers or diastereomers thereof are excluded.

ARP170102378A 2016-08-29 2017-08-28 SULFONIMIDOILPURINONA 7-SUBSTITUTED AND DERIVATIVE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION AR109433A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2016097140 2016-08-29

Publications (1)

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AR109433A1 true AR109433A1 (en) 2018-11-28

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ARP170102378A AR109433A1 (en) 2016-08-29 2017-08-28 SULFONIMIDOILPURINONA 7-SUBSTITUTED AND DERIVATIVE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION

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