AU2013267209B2 - Modulation of hepatitis B virus cccDNA transcription - Google Patents

Modulation of hepatitis B virus cccDNA transcription Download PDF

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Publication number
AU2013267209B2
AU2013267209B2 AU2013267209A AU2013267209A AU2013267209B2 AU 2013267209 B2 AU2013267209 B2 AU 2013267209B2 AU 2013267209 A AU2013267209 A AU 2013267209A AU 2013267209 A AU2013267209 A AU 2013267209A AU 2013267209 B2 AU2013267209 B2 AU 2013267209B2
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AU
Australia
Prior art keywords
group
hydrogen
inhibitor
alkyl
hbv
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Ceased
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AU2013267209A
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AU2013267209A1 (en
Inventor
Harold R. Almond
Timothy M. Block
Jinhong Chang
Ju-Tao Guo
William A. Kinney
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BARUCH S BLUMBERG INSTITUTE
Drexel University
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BARUCH S BLUMBERG INST
Drexel University
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Priority to AU2017202675A priority Critical patent/AU2017202675A1/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/123—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/126—Tetrapeptides

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2013267209A 2012-06-01 2013-05-31 Modulation of hepatitis B virus cccDNA transcription Ceased AU2013267209B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2017202675A AU2017202675A1 (en) 2012-06-01 2017-04-21 Modulation of hepatitis b virus cccdna transcription

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261654374P 2012-06-01 2012-06-01
US61/654,374 2012-06-01
PCT/US2013/043691 WO2013181584A2 (en) 2012-06-01 2013-05-31 Modulation of hepatitis b virus cccdna transcription

Related Child Applications (1)

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AU2017202675A Division AU2017202675A1 (en) 2012-06-01 2017-04-21 Modulation of hepatitis b virus cccdna transcription

Publications (2)

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AU2013267209A1 AU2013267209A1 (en) 2014-12-18
AU2013267209B2 true AU2013267209B2 (en) 2017-02-02

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AU2013267209A Ceased AU2013267209B2 (en) 2012-06-01 2013-05-31 Modulation of hepatitis B virus cccDNA transcription
AU2017202675A Abandoned AU2017202675A1 (en) 2012-06-01 2017-04-21 Modulation of hepatitis b virus cccdna transcription

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US (3) US9623071B2 (enExample)
EP (1) EP2854832A4 (enExample)
JP (1) JP6431478B2 (enExample)
KR (1) KR101945578B1 (enExample)
CN (1) CN104507488A (enExample)
AU (2) AU2013267209B2 (enExample)
BR (1) BR112014029697A2 (enExample)
CA (1) CA2874828A1 (enExample)
HK (1) HK1208823A1 (enExample)
IL (1) IL235912A0 (enExample)
PH (1) PH12014502659A1 (enExample)
SG (1) SG11201407970VA (enExample)
WO (1) WO2013181584A2 (enExample)

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CAS Registry Number 1126426-60-5; STN Entry Date 25 March 2009; Cyclo[L-alanyl-(2R)-2-amino-8-oxodecanoyl-L-tryptophyl-L-leucyl] *
CAS Registry Number 1126426-63-8; STN Entry Date 25 March 2009; Cyclo[N-methyl-L-alanyl-(2S)-2-amino-8-oxodecanoyl-L-tryptophyl-L-leucyl] *
CAS Registry Number 1187754-56-8; STN Entry Date 09 October 2009; Cyclo-[L-alanyl-(2S)-2-amino-8-oxodecanoyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1187754-57-9; STN Entry Date 09 October 2009; Cyclo[L-alanyl-(2S)-2-amino-8-(hydroxyamino)-8-oxooctanoyl-L-trytophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1187754-68-2; STN Entry Date 09 October 2009; Cyclo[(3S)-3-amino-5-methylhexanoyl-N6-acetyl-L-lysyl-(2S)-2-amino-8-oxodecanoyl-L-tryptophyl] *
CAS Registry Number 1187754-69-3; STN Entry Date 09 October 2009; 1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone, 3-(1H-indol-3-ylmethyl)-13-(2-methylproperyl)-6,9-bis(6-oxooctyl)-(3S,6S,9S,13S)- *
CAS Registry Number 1187754-77-3; STN Entry Date 09 October 2009, Cyclo[(3S)-3-amino-5-methylhexanoyl-L-phenylalanyl-(2S)-2-amino-8-oxodecanoyl-L-tryptophyl] *
CAS Registry Number 1187754-79-5; STN Entry Date 09 October 2009, Cyclo[(2S)-2-amino-8-(hydroxyamino)-8-oxooctanoyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl-L-phenylalanyl] *
CAS Registry Number 1316753-00-0; STN Entry Date 12 August 2011; 1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone,3-(1H-indol-3-ylmethyl)-9,10-dimethyl-13-(2-methylpropyl)-6-(6-oxooctyl)-(3S,6S,9S,13S)- *
CAS Registry Number 1316753-02-2; STN Entry Date 12 August 2011; 1,4,7,10-tetraazocyclotridecane-2,5,8,1-tetrone,3-(1H-indol-3-ylmethyl)-9-methyl-13-(2-methyl-13-(2-methylpropyl)-6-(6-oxooctyl)-(3S,6S,9R,13S)- *
CAS Registry Number 1349396-08-2; STN Entry Date 06 December 2011; Compound according to formula II where R8 is iso-butyl, R1 is CH2, R2 is -C(O)NH-, R3 is (CH2)5NHAc and R6 is (CH2)5C(O)CH2CH3 *
CAS Registry Number 1373504-57-4; STN Entry Date 14 May 2012; Cyclo[L-alanyl-(2S)-2-aminooctanoyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-63-2; STN Entry Date 14 May 2012; Cyclo[L-alanyl-L-norleucyl-L-tryptophyl-(3)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-64-3; STN Entry Date 14 May 2012; Cyclo[L-alanyl-L-norvalyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-65-4; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoyl-3-methoxy-L-phenylalanyl-L-norvalyl-L-tryptophyl] *
CAS Registry Number 1373504-66-5; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoyl-L-phenylalanyl-L-norvalyl-L-tryptophyl] *
CAS Registry Number 1373504-68-7; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoyl-(2S)-2-phenylglycyl-L-norvalyl-L-tryptophyl] *
CAS Registry Number 1373504-69-8; STN Entry Date 14 May 2012; Cyclo[3-(3-pyridinyl)-L-alanyl-L-norvalyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-70-1; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoyl-L-leucyl-L-norvalyl-L-tryptophyl] *
CAS Registry Number 1373504-71-2; STN Entry Date 14 May 2012; Cyclo[D-alanyl-L-norvalyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-72-3; STN Entry Date 14 May 2012; Cyclo[(2S)-2-aminobutanoyl-L-norvalyl-L-tryptophyl-(3S)-3-amino-5-methylhexanoyl] *
CAS Registry Number 1373504-73-4; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoylglycyl-L-norvalyl-L-tryptophyl] *
CAS Registry Number 1373504-74-5; STN Entry Date 14 May 2012; Cyclo[(3S)-3-amino-5-methylhexanoyl-L-asparaginyl-L-norvalyl-L-tryptophyl] *
POLLICINO, T. et al. "Hepatitis B Virus Replication Is Regulated by the Acetylation Status of Hepatitis B Virus cccDNA-Bound H3 and H4 Histones" Gastroenterology (2006) vol. 130, pages 823-837 *

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