PE20170197A1 - Derivados de nucleosido 4'-sustitutos como inhibidores de la transcriptasa reversa de vih - Google Patents
Derivados de nucleosido 4'-sustitutos como inhibidores de la transcriptasa reversa de vihInfo
- Publication number
- PE20170197A1 PE20170197A1 PE2016001816A PE2016001816A PE20170197A1 PE 20170197 A1 PE20170197 A1 PE 20170197A1 PE 2016001816 A PE2016001816 A PE 2016001816A PE 2016001816 A PE2016001816 A PE 2016001816A PE 20170197 A1 PE20170197 A1 PE 20170197A1
- Authority
- PE
- Peru
- Prior art keywords
- reverse transcriptase
- transcriptase inhibitors
- nucleoside
- hiv reverse
- alkyl
- 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
- C07H19/14—Pyrrolo-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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- 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
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
-
- 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
- C07H19/12—Triazine radicals
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)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Describe derivados de nucleosidos 4´ sustituidos de formula (I) como inhibidores de la transcriptasa reversa de VIH, profilaxis y tratamiento de infeccion por VIH, profilaxis, tratamiento y retraso en la aparicion o progresion de SIDA y/o complejo realcionado al SIDA (ARC). Donde: R es uno de formula i), ii), etc.; X es O, S, etc.; Y es -CN, etc.; R1 H, -C(O)R6, etc.; R2 es H, -C(O)R6a, etc.; R3 es H, F u OH; R4 es H, alquilo C1-C6, etc.; R5 es H, alquilo C1-C6, etc.; R6 y R6a son H, alquilo C1-C6, etc.; m es 0 o 1; R9 es H, halo, etc. Son compuestos preferidos: (2R,3S,5R)-5-(4-amino-5-fluoro-7H-pirrolo[2,3-d]pirimidin-7-il)-2-etinil-2-(hidroximetil)tetrahidrofuran-3-ol; (2R,3S,5R)-5-(4-amino-2-cloro-7H-pirrolo[2,3-d]pirimidin-7-il)-2-etinil-2-(hidroximetil)tetrahidrofuran-3-ol; entre otros
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2014/074294 WO2015143712A1 (en) | 2014-03-28 | 2014-03-28 | 4'-substituted nucleoside reverse transcriptase inhibitors |
Publications (1)
Publication Number | Publication Date |
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PE20170197A1 true PE20170197A1 (es) | 2017-03-22 |
Family
ID=52824598
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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PE2016001816A PE20170197A1 (es) | 2014-03-28 | 2015-03-26 | Derivados de nucleosido 4'-sustitutos como inhibidores de la transcriptasa reversa de vih |
Country Status (41)
Families Citing this family (38)
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MA42608A (fr) | 2015-08-13 | 2018-06-20 | Merck Sharp & Dohme | Composés de di-nucléotide cyclique en tant qu'agonistes sting (stimulateur de gène interféron) |
WO2017053216A2 (en) | 2015-09-23 | 2017-03-30 | Merck Sharp & Dohme Corp. | 4'-substituted nucleoside reverse transcriptase inhibitors and preparations thereof |
JOP20170038B1 (ar) | 2016-02-12 | 2021-08-17 | Merck Sharp & Dohme | مركبات للاستخدام لعلاج عدوى بفيروس hiv والوقاية منه |
US10138248B2 (en) | 2016-06-24 | 2018-11-27 | Incyte Corporation | Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors |
UA125223C2 (uk) | 2016-10-04 | 2022-02-02 | Мерк Шарп І Доум Корп. | СПОЛУКИ БЕНЗО[b]ТІОФЕНУ ЯК АГОНІСТИ STING |
JP7125714B2 (ja) * | 2016-12-13 | 2022-08-25 | ヤマサ醤油株式会社 | 抗ウイルス活性を有する2’-デオキシ-7-デアザプリンヌクレオシド誘導体 |
WO2018208667A1 (en) | 2017-05-12 | 2018-11-15 | Merck Sharp & Dohme Corp. | Cyclic di-nucleotide compounds as sting agonists |
AU2018311966A1 (en) | 2017-08-04 | 2020-02-13 | Merck Sharp & Dohme Llc | Benzo[b]thiophene sting agonists for cancer treatment |
RU2020109328A (ru) | 2017-08-04 | 2021-09-06 | Мерк Шарп И Доум Корп. | Комбинации антагонистов pd-1 и бензо[b]тиофеновых агонистов sting для лечения рака |
EA202090775A1 (ru) * | 2017-09-18 | 2020-07-06 | Янссен Байофарма, Инк. | Замещенные нуклеозиды, нуклеотиды и их аналоги |
US11685761B2 (en) | 2017-12-20 | 2023-06-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
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JP2021515771A (ja) * | 2018-03-07 | 2021-06-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited | Hiv療法に有用な化合物 |
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US11702430B2 (en) | 2018-04-03 | 2023-07-18 | Merck Sharp & Dohme Llc | Aza-benzothiophene compounds as STING agonists |
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- 2016-09-28 GT GT201600201A patent/GT201600201A/es unknown
- 2016-09-28 DO DO2016000265A patent/DOP2016000265A/es unknown
- 2016-09-28 SV SV2016005290A patent/SV2016005290A/es unknown
- 2016-10-28 EC ECIEPI201685206A patent/ECSP16085206A/es unknown
-
2017
- 2017-08-24 US US15/685,824 patent/US20180002366A1/en not_active Abandoned
- 2017-09-07 AU AU2017225090A patent/AU2017225090B2/en active Active
-
2021
- 2021-10-25 CY CY20211100925T patent/CY1124829T1/el unknown
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