AR101561A1 - Nucleósidos de 2-cloro aminopirimidinona y pirimidina diona - Google Patents
Nucleósidos de 2-cloro aminopirimidinona y pirimidina dionaInfo
- Publication number
- AR101561A1 AR101561A1 ARP150102625A ARP150102625A AR101561A1 AR 101561 A1 AR101561 A1 AR 101561A1 AR P150102625 A ARP150102625 A AR P150102625A AR P150102625 A ARP150102625 A AR P150102625A AR 101561 A1 AR101561 A1 AR 101561A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- independently
- group
- formula
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: R¹ se selecciona de NH y N; la línea punteada (- - - -), en conjunto con la línea sólida a la que es paralela, representa un doble enlace opcional; R² se selecciona de oxo o NH₂, con la condición de que, cuando R² es oxo, R¹ es NH y el enlace representado por la línea punteada (- - - -), en conjunto con la línea sólida a la que es paralela, es un enlace sencillo; y con la condición de que, cuando R² es NH₂, R¹ es N y el enlace representado por la línea punteada (- - - -), en conjunto con la línea sólida a la que es paralela, es un enlace doble; R³ se selecciona del grupo de H, F, CH₂F, CHF₂, y CF₃; R⁵ se selecciona del grupo de CN, alquilo C₁₋₄ no sustituido, alquilo C₁₋₄ sustituido con 1, 2, ó 3 halógenos, alquilo C₁₋₄ sustituido con 1 sustituyente seleccionado de -S-CH₃ y -O-CH₃, alquenilo C₂₋₄, alquinilo C₂₋₄, cicloalquilo C₃₋₆ no sustituido, cicloalquilo C₃₋₆ sustituido por 1, 2, ó 3 sustituyentes seleccionados de F y CH₃; R⁴ se selecciona del grupo de H, -C(=O)R⁶, -C(=O)OR⁶, y -C(=O)NR⁶R⁷; R⁴ se selecciona del grupo de H, -C(=O)R⁶, -C(=O)OR⁶, y -C(=O)NR⁶R⁷; o c) R⁴ es un grupo de la fórmula (2), en donde: cada Y es O, S, NR, ⁺N(O)(R), N(O), ⁺N(O)(O), o N-NR₂; y W¹ y W², cuando se toman juntos, son -Y³(C(Rʸ)₂)₃Y³-; o uno de W¹ o W² junto con R⁴ es -Y³- y el otro de W¹ o W² es de fórmula (3); o W¹ y W² son cada uno, independientemente, un grupo de la fórmula (3), en donde: cada Y¹ es, independientemente, O, S, NR, ⁺N(O)(R), N(O), ⁺N(O)(O), o N-NR₂; cada Y² es independientemente un enlace, O, CR₂, -O-CR₂-, NR, ⁺N(O)(R), N(O), ⁺N(O)(O), N-NR₂, S, S-S, S(O), o S(O)₂; cada Y³ es un enlace sencillo; M1 es 0, 1, 2, ó 3; cada Rˣ es independientemente Rʸ o el compuesto de fórmula (4), en donde: cada M2a, M2b, y M2c es independientemente 0 ó 1; M2d es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ó 12; cada Rʸ es independientemente H, F, Cl, Br, I, OH, R, -C(=Y¹)R, -C(=Y¹)O, -C(=Y¹)N(R)₂, -⁺N(R)₃, -SR, -S(O)R, -S(O)₂R, -S(O)(O), -S(O)₂(O), -OC(=Y¹)R, -OC(=Y¹)O, -OC(=Y¹)(N(R)₂), -SC(=Y¹)R, -SC(=Y¹)O, -SC(=Y¹)(N(R)₂), -N(R)C(=Y¹)R, -N(R)C(=Y¹)O, -N(R)C(=Y¹)N(R)₂, -SO₂NR², -CN, -N₃, -NO₂, -O, o W³; o cuando se toman juntos, dos Rʸ en el mismo átomo de carbono forman un anillo carbocíclico que tiene 3, 4, 5, 6, ó 7 átomos de carbono en el anillo; o cuando se toman juntos, dos Rʸ en el mismo átomo de carbono forman junto con el átomo de carbono un heterociclo que tiene 3, 4, 5, 6, ó 7 átomos de anillo en donde un átomo del anillo se selecciona de O ó N y todos los otros átomos de anillo son carbono; cada R es independientemente H, alquilo C₁₋₈, alquilo C₁₋₈ sustituido, alquenilo C₂₋₈, alquenilo C₂₋₈ sustituido, alquinilo C₂₋₈, alquinilo C₂₋₈ sustituido, arilo C₆₋₁₀, arilo C₆₋₁₀ sustituido, un heterociclo de 3 a 10 miembros, un heterociclo de 3 a 10 miembros sustituido, un heteroarilo de 5 a 12 miembros, un heteroarilo de 5 a 12 miembros sustituido, arilalquilo, arilalquilo sustituido, heteroarilalquilo, o heteroarilalquilo sustituido; y W³ es W⁴ o W⁵; W⁴ es R, -C(Y¹)Rʸ, -C(Y¹)W⁵, -SO₂Rʸ, o -SO₂W⁵; W⁵ se selecciona de fenilo, naftilo, un carbociclo C₃₋₈, o un heterociclo de 3 a 10 miembros, en donde W⁵ está independientemente sustituido con 0, 1, 2, 3, 4, 5, o 6 grupos Rʸ; cada R⁶ y R⁷ es independientemente H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, carbociclilalquilo C₄₋₈, arilo C₆₋₁₀, arilo C₆₋₁₀ sustituido, heteroarilo de 5 a 10 miembros, heteroarilo de 5 a 10 miembros sustituido, -C(=O)alquilo C₁₋₈, -S(O)ₙ-alquilo C₁₋₈ o arilo-alquilo C₁₋₈; o R⁶ y R⁷ tomados junto con un nitrógeno al cual ambos están unidos forman un heterociclo de 3 a 7 miembros en donde cualquier átomo de carbono del anillo de dicho heterociclo se puede reemplazar opcionalmente con -O-, -S- o -NRᵃ-; y en donde cada alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈ o arilo-alquilo C₁₋₈ de cada R⁶ o R⁷ está, independientemente, opcionalmente sustituido con uno, dos, tres, o cuatro sustituyentes seleccionados de halo, hidroxi, CN, N₃, N(Rᵃ)₂ o ORᵃ; y en donde uno, dos, o tres de los átomos de carbono no terminales de cada dicho alquilo C₁₋₈ se pueden reemplazar opcionalmente con -O-, -S- o -NRᵃ-; o b) R⁴ es un grupo seleccionado de las fórmulas (5) y (6) en donde: R⁸ se selecciona de fenilo, 1-naftilo, 2-naftilo, un resto de fórmula (7) y (8); R⁹ se selecciona de H y CH₃; R¹⁰ se selecciona de H o alquilo C₁₋₆; R¹⁰ se selecciona de H o alquilo C₁₋₆; o R¹⁰ y R¹⁰, junto con el átomo de carbono al que están enlazados, forman un espirociclo de 3, 4, 5 ó 6 miembros en donde todos los átomos de anillo del espirociclo son carbono; o R¹⁰ y R¹⁰, junto con el átomo de carbono al que están enlazados, forman un espirociclo de 3, 4, 5 ó 6 miembros en donde 1 ó 2 de los átomos de anillo del espirociclo son seleccionados del grupo de O, S, y N, y todos los otros átomos de anillo del espirociclo son carbono; R¹¹ se selecciona de H, alquilo C₁₋₈, bencilo, cicloalquilo C₃₋₆, -CH₂-cicloalquilo C₃₋₆, -CH₂CH₂-S-C(O)-alquilo C₃₋₆, un resto de fórmula (9) y (10); R⁷ se selecciona de alquilo C₁₋₈, -O-alquilo C₁₋₈, bencilo, -O-bencilo, -CH₂-cicloalquilo C₃₋₆, y CF₃; o e) R⁴ y R⁴ se combinan para formar la estructura seleccionada de fórmulas (11) y (12).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462040349P | 2014-08-21 | 2014-08-21 |
Publications (1)
Publication Number | Publication Date |
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AR101561A1 true AR101561A1 (es) | 2016-12-28 |
Family
ID=54066190
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP150102625A AR101561A1 (es) | 2014-08-21 | 2015-08-14 | Nucleósidos de 2-cloro aminopirimidinona y pirimidina diona |
Country Status (17)
Country | Link |
---|---|
US (6) | US9617295B2 (es) |
EP (2) | EP3738969A1 (es) |
JP (2) | JP6765364B2 (es) |
KR (1) | KR102528928B1 (es) |
CN (1) | CN106573954A (es) |
AR (1) | AR101561A1 (es) |
AU (1) | AU2015305593C1 (es) |
BR (1) | BR112017003242A2 (es) |
CA (1) | CA2958546C (es) |
EA (1) | EA201790234A1 (es) |
ES (1) | ES2808868T3 (es) |
IL (1) | IL250426A0 (es) |
MX (1) | MX2017002288A (es) |
NZ (1) | NZ728707A (es) |
SG (1) | SG11201700810SA (es) |
TW (1) | TWI673283B (es) |
WO (1) | WO2016028866A1 (es) |
Families Citing this family (10)
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SG10201913554YA (en) | 2011-12-22 | 2020-03-30 | Alios Biopharma Inc | Substituted nucleosides, nucleotides and analogs thereof |
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USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
TWI673283B (zh) * | 2014-08-21 | 2019-10-01 | 美商基利科學股份有限公司 | 2’-氯胺基嘧啶酮及嘧啶二酮核苷類 |
CR20170157A (es) * | 2014-09-26 | 2017-07-03 | Riboscience Llc | Derivados de nucleósidos sustituidos con 4´-vinilo como inhibidores de la replicación del arn del virus respiratorio sincitial |
LT3236972T (lt) | 2014-12-26 | 2021-11-10 | Emory University | Antivirusiniai n4-hidroksicitidino dariniai |
WO2018009623A1 (en) * | 2016-07-08 | 2018-01-11 | Atea Pharmaceuticals, Inc. | β-D-2'-DEOXY-2'-SUBSTITUTED-4'-SUBSTITUTED-2-SUBSTITUTED-N6-SUBSTITUTED-6-AMINOPURINE NUCLEOTIDES FOR THE TREATMENT OF PARAMYXOVIRUS AND ORTHOMYXOVIRUS INFECTIONS |
BR122022008466B1 (pt) | 2017-12-07 | 2023-12-05 | Emory University | Uso de um composto |
WO2023085242A1 (ja) * | 2021-11-12 | 2023-05-19 | 国立大学法人北海道大学 | 抗ウイルス剤 |
WO2024016639A1 (zh) * | 2022-07-21 | 2024-01-25 | 华创合成制药股份有限公司 | 一种抗病毒感染的化合物及其制备方法和用途 |
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2015
- 2015-08-07 TW TW104125796A patent/TWI673283B/zh active
- 2015-08-14 AR ARP150102625A patent/AR101561A1/es unknown
- 2015-08-19 CN CN201580044979.5A patent/CN106573954A/zh active Pending
- 2015-08-19 SG SG11201700810SA patent/SG11201700810SA/en unknown
- 2015-08-19 ES ES15760544T patent/ES2808868T3/es active Active
- 2015-08-19 EA EA201790234A patent/EA201790234A1/ru unknown
- 2015-08-19 JP JP2017508531A patent/JP6765364B2/ja active Active
- 2015-08-19 BR BR112017003242A patent/BR112017003242A2/pt not_active Application Discontinuation
- 2015-08-19 AU AU2015305593A patent/AU2015305593C1/en active Active
- 2015-08-19 NZ NZ728707A patent/NZ728707A/en unknown
- 2015-08-19 US US14/830,121 patent/US9617295B2/en active Active
- 2015-08-19 KR KR1020177006312A patent/KR102528928B1/ko active IP Right Grant
- 2015-08-19 WO PCT/US2015/045849 patent/WO2016028866A1/en active Application Filing
- 2015-08-19 EP EP20180058.8A patent/EP3738969A1/en active Pending
- 2015-08-19 EP EP15760544.5A patent/EP3183261B1/en active Active
- 2015-08-19 CA CA2958546A patent/CA2958546C/en active Active
- 2015-08-19 MX MX2017002288A patent/MX2017002288A/es unknown
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2017
- 2017-02-02 IL IL250426A patent/IL250426A0/en unknown
- 2017-02-24 US US15/441,561 patent/US9982006B2/en active Active
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2018
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- 2018-12-06 US US16/212,374 patent/US20190202852A1/en not_active Abandoned
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2019
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2020
- 2020-04-10 JP JP2020070958A patent/JP2020111608A/ja not_active Withdrawn
Also Published As
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MX2017002288A (es) | 2017-05-22 |
BR112017003242A2 (pt) | 2017-11-28 |
KR102528928B1 (ko) | 2023-05-08 |
US20170327526A1 (en) | 2017-11-16 |
US9982006B2 (en) | 2018-05-29 |
ES2808868T3 (es) | 2021-03-02 |
US20190202852A1 (en) | 2019-07-04 |
CA2958546C (en) | 2020-06-23 |
NZ728707A (en) | 2018-06-29 |
EP3183261A1 (en) | 2017-06-28 |
US20160052953A1 (en) | 2016-02-25 |
EA201790234A1 (ru) | 2017-07-31 |
AU2015305593B2 (en) | 2018-05-17 |
IL250426A0 (en) | 2017-03-30 |
EP3738969A1 (en) | 2020-11-18 |
JP2020111608A (ja) | 2020-07-27 |
WO2016028866A1 (en) | 2016-02-25 |
AU2015305593C1 (en) | 2018-11-15 |
JP6765364B2 (ja) | 2020-10-07 |
US20200157137A1 (en) | 2020-05-21 |
JP2017525699A (ja) | 2017-09-07 |
US20180340004A1 (en) | 2018-11-29 |
US9617295B2 (en) | 2017-04-11 |
TWI673283B (zh) | 2019-10-01 |
CA2958546A1 (en) | 2016-02-25 |
US20200087337A1 (en) | 2020-03-19 |
CN106573954A (zh) | 2017-04-19 |
EP3183261B1 (en) | 2020-06-17 |
KR20170042643A (ko) | 2017-04-19 |
TW201619178A (zh) | 2016-06-01 |
SG11201700810SA (en) | 2017-03-30 |
AU2015305593A1 (en) | 2017-02-23 |
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