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 vih

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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
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PE
Peru
Prior art keywords
reverse transcriptase
transcriptase inhibitors
nucleoside
hiv reverse
alkyl
Prior art date
Application number
PE2016001816A
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English (en)
Inventor
Bing-Yu Tang
Jianmin Fu
Vinay M Girijavallabhan
David B Olsen
Zhibo Zhang
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Merck Sharp & Dohme
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52824598&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20170197(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20170197A1 publication Critical patent/PE20170197A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14Pyrrolo-pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12Triazine radicals

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  • 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
PE2016001816A 2014-03-28 2015-03-26 Derivados de nucleosido 4'-sustitutos como inhibidores de la transcriptasa reversa de vih PE20170197A1 (es)

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)

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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)

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US (2) US9777035B2 (es)
EP (1) EP3122752B1 (es)
JP (1) JP6182680B2 (es)
KR (1) KR101961009B1 (es)
CN (1) CN106795199B (es)
AP (1) AP2016009482A0 (es)
AR (1) AR099788A1 (es)
AU (2) AU2015236018B2 (es)
CA (1) CA2943792C (es)
CL (1) CL2016002414A1 (es)
CR (1) CR20160451A (es)
CY (1) CY1124829T1 (es)
DK (1) DK3122752T3 (es)
DO (1) DOP2016000265A (es)
EA (1) EA031476B1 (es)
EC (1) ECSP16085206A (es)
ES (1) ES2894228T3 (es)
GE (1) GEP20197009B (es)
GT (1) GT201600201A (es)
HR (1) HRP20211622T1 (es)
HU (1) HUE056913T2 (es)
IL (1) IL247923B (es)
JO (1) JO3636B1 (es)
LT (1) LT3122752T (es)
MA (1) MA39809B1 (es)
MD (1) MD4812C1 (es)
MX (1) MX367058B (es)
MY (1) MY194635A (es)
NI (1) NI201600145A (es)
NZ (1) NZ724343A (es)
PE (1) PE20170197A1 (es)
PH (1) PH12016501897A1 (es)
PL (1) PL3122752T3 (es)
PT (1) PT3122752T (es)
RS (1) RS62418B1 (es)
SG (1) SG11201608031PA (es)
SI (1) SI3122752T1 (es)
SV (1) SV2016005290A (es)
TW (1) TWI660967B (es)
UA (1) UA120758C2 (es)
WO (2) WO2015143712A1 (es)

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MY194635A (en) 2022-12-08
PL3122752T3 (pl) 2022-01-03
MA39809A (fr) 2021-04-07
AU2015236018B2 (en) 2017-09-28
US9777035B2 (en) 2017-10-03
CA2943792C (en) 2020-02-25
EP3122752B1 (en) 2021-08-25
SI3122752T1 (sl) 2021-11-30
TW201619180A (zh) 2016-06-01
RS62418B1 (sr) 2021-10-29
WO2015148746A1 (en) 2015-10-01
CR20160451A (es) 2016-12-06
PH12016501897A1 (en) 2016-12-19
ES2894228T3 (es) 2022-02-14
KR20160128437A (ko) 2016-11-07
MX2016012659A (es) 2016-12-14
CY1124829T1 (el) 2022-11-25
DK3122752T3 (da) 2021-10-25
US20180002366A1 (en) 2018-01-04
JP2017512797A (ja) 2017-05-25
MD20160117A2 (ro) 2017-02-28
CA2943792A1 (en) 2015-10-01
GT201600201A (es) 2018-12-18
LT3122752T (lt) 2021-11-10
NZ724343A (en) 2020-02-28
JO3636B1 (ar) 2020-08-27
AU2017225090A1 (en) 2017-09-28
AP2016009482A0 (en) 2016-10-31
AU2015236018A1 (en) 2016-10-06
UA120758C2 (uk) 2020-02-10
KR101961009B1 (ko) 2019-03-21
HRP20211622T1 (hr) 2022-03-04
MX367058B (es) 2019-08-02
BR112016022438A2 (pt) 2017-08-15
IL247923A0 (en) 2016-11-30
EA201691931A1 (ru) 2017-02-28
CN106795199A (zh) 2017-05-31
CN106795199B (zh) 2020-01-10
MD4812B1 (ro) 2022-06-30
HUE056913T2 (hu) 2022-03-28
NI201600145A (es) 2016-10-27
AU2017225090B2 (en) 2018-08-09
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IL247923B (en) 2021-01-31
ECSP16085206A (es) 2017-08-31
MD4812C1 (ro) 2023-01-31
AR099788A1 (es) 2016-08-17
TWI660967B (zh) 2019-06-01
SV2016005290A (es) 2018-05-03
US20150274767A1 (en) 2015-10-01
CL2016002414A1 (es) 2017-05-05
EA031476B1 (ru) 2019-01-31
SG11201608031PA (en) 2016-10-28
JP6182680B2 (ja) 2017-08-16
EP3122752A1 (en) 2017-02-01
DOP2016000265A (es) 2017-04-30
PT3122752T (pt) 2021-10-20
GEP20197009B (en) 2019-08-12
WO2015143712A1 (en) 2015-10-01

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