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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Gastroenterology & Hepatology (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (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 |
|---|---|
| PE20170197A1 true PE20170197A1 (es) | 2017-03-22 |
Family
ID=52824598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016001816A PE20170197A1 (es) | 2014-03-28 | 2015-03-26 | Derivados de nucleosido 4'-sustitutos como inhibidores de la transcriptasa reversa de vih |
Country Status (42)
Families Citing this family (51)
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| WO2017027645A1 (en) | 2015-08-13 | 2017-02-16 | Merck Sharp & Dohme Corp. | Cyclic di-nucleotide compounds as sting agonists |
| US11453697B1 (en) | 2015-08-13 | 2022-09-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| AU2016328303B2 (en) | 2015-09-23 | 2019-05-02 | Merck Sharp & Dohme (Uk) Limited | 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 |
| WO2017223414A1 (en) | 2016-06-24 | 2017-12-28 | Incyte Corporation | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS |
| CR20190168A (es) | 2016-10-04 | 2019-05-17 | Merck Sharp & Dohme | Compuestos de benzo[b]tiofeno como agonistas de 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 |
| EP3621624B1 (en) | 2017-05-12 | 2023-08-30 | Merck Sharp & Dohme LLC | Cyclic di-nucleotide compounds as sting agonists |
| WO2019027857A1 (en) | 2017-08-04 | 2019-02-07 | Merck Sharp & Dohme Corp. | COMBINATIONS OF PD-1 ANTAGONISTS AND STING BENZO [B] THIOPHENIC AGONISTS FOR THE TREATMENT OF CANCER |
| EP3661498A4 (en) | 2017-08-04 | 2021-04-21 | Merck Sharp & Dohme Corp. | BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT |
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| WO2019171285A1 (en) * | 2018-03-07 | 2019-09-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Compounds useful in hiv therapy |
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| WO2020031131A1 (en) * | 2018-08-09 | 2020-02-13 | Glaxosmithkline Intellectual Property (No.2) Limited | Compounds useful in hiv therapy |
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2014
- 2014-03-28 WO PCT/CN2014/074294 patent/WO2015143712A1/en not_active Ceased
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2015
- 2015-03-18 AR ARP150100818A patent/AR099788A1/es active IP Right Grant
- 2015-03-19 JO JOP/2015/0049A patent/JO3636B1/ar active
- 2015-03-20 TW TW104109078A patent/TWI660967B/zh active
- 2015-03-26 CA CA2943792A patent/CA2943792C/en active Active
- 2015-03-26 CR CR20160451A patent/CR20160451A/es unknown
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