WO2013052613A1 - Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication - Google Patents

Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication Download PDF

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Publication number
WO2013052613A1
WO2013052613A1 PCT/US2012/058674 US2012058674W WO2013052613A1 WO 2013052613 A1 WO2013052613 A1 WO 2013052613A1 US 2012058674 W US2012058674 W US 2012058674W WO 2013052613 A1 WO2013052613 A1 WO 2013052613A1
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WO
WIPO (PCT)
Prior art keywords
fee
esse
inhibitors
iss
disease
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2012/058674
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English (en)
French (fr)
Inventor
Andrea Cuconati
Xiaodong Xu
Timothy M. Block
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
Original Assignee
INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to US14/349,014 priority Critical patent/US20140249154A1/en
Priority to CA2850779A priority patent/CA2850779A1/en
Priority to BR112014007963A priority patent/BR112014007963A2/pt
Priority to JP2014534680A priority patent/JP6240078B2/ja
Priority to SG11201401207XA priority patent/SG11201401207XA/en
Priority to PH1/2014/500724A priority patent/PH12014500724A1/en
Priority to EP12838333.8A priority patent/EP2763674A4/en
Priority to KR1020147011691A priority patent/KR20140071472A/ko
Priority to AU2012318670A priority patent/AU2012318670B2/en
Priority to CN201280059490.1A priority patent/CN103957908A/zh
Application filed by INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH filed Critical INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
Priority to HK15101053.5A priority patent/HK1200361A1/xx
Publication of WO2013052613A1 publication Critical patent/WO2013052613A1/en
Priority to IL231923A priority patent/IL231923A0/en
Anticipated expiration legal-status Critical
Priority to US15/258,393 priority patent/US10087173B2/en
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • 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
    • 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
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
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  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PCT/US2012/058674 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication Ceased WO2013052613A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
AU2012318670A AU2012318670B2 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
BR112014007963A BR112014007963A2 (pt) 2011-10-04 2012-10-04 aminotiazoles substituídos como inibidores de cãncer, incluindo carcinoma hepatocelular, e como inibidores da replicação do vírus da hepatite
JP2014534680A JP6240078B2 (ja) 2011-10-04 2012-10-04 肝細胞癌を含む癌の阻害剤、および肝炎ウイルス複製の阻害剤としての置換アミノチアゾール
SG11201401207XA SG11201401207XA (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
PH1/2014/500724A PH12014500724A1 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
EP12838333.8A EP2763674A4 (en) 2011-10-04 2012-10-04 SUBSTITUTED AMINOTHIAZOLE AS ANTIBODIES OF CANCER CELLS INCLUDING HEPATOCELLULAR CARCINOMA AND AS HEPATITIS VIRUS REPLICATION INHIBITORS
KR1020147011691A KR20140071472A (ko) 2011-10-04 2012-10-04 간세포 암종을 포함하는 암의 저해제로서 그리고 간염 바이러스 복제의 저해제로서의 치환된 아미노티아졸
US14/349,014 US20140249154A1 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
CA2850779A CA2850779A1 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
CN201280059490.1A CN103957908A (zh) 2011-10-04 2012-10-04 作为包括肝细胞癌在内的癌症的抑制剂和作为肝炎病毒复制抑制剂的取代的氨基噻唑
HK15101053.5A HK1200361A1 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
IL231923A IL231923A0 (en) 2011-10-04 2014-04-03 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
US15/258,393 US10087173B2 (en) 2011-10-04 2016-09-07 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication

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US10407435B2 (en) 2014-10-29 2019-09-10 Karus Therapeutics Limited Diheteroaryl histone deacetylase inhibitors and their use in therapy
US10426775B2 (en) 2017-09-11 2019-10-01 Fratagene Therapeutics Srl Methods for treating Friedreich's ataxia with etravirine
US10442779B2 (en) 2014-09-22 2019-10-15 Fratagene Therapeutics S.R.L. Compositions and methods for treating Friedreich's ataxia
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US20150361074A1 (en) * 2012-11-07 2015-12-17 Karus Therapeutics Ltd Novel histone deacetylase inhibitors and their use in therapy
US9676765B2 (en) * 2012-11-07 2017-06-13 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
US10150763B2 (en) 2012-11-07 2018-12-11 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
US9862685B2 (en) 2013-05-10 2018-01-09 Karus Therapeutics Limited Histone deacetylase inhibitors
US10870624B2 (en) 2013-05-10 2020-12-22 Karus Therapeutics Limited Histone deacetylase inhibitors
WO2016046759A2 (en) 2014-09-22 2016-03-31 Fratagene Therapeutics Ltd. Compositions and methods for treating friedreich's ataxia
US10442779B2 (en) 2014-09-22 2019-10-15 Fratagene Therapeutics S.R.L. Compositions and methods for treating Friedreich's ataxia
US10407435B2 (en) 2014-10-29 2019-09-10 Karus Therapeutics Limited Diheteroaryl histone deacetylase inhibitors and their use in therapy
US10533003B2 (en) 2014-10-29 2020-01-14 Karus Therapeutics Limited Polyheteroarl histone deacetylase inhibitors and their use in therapy
US10426775B2 (en) 2017-09-11 2019-10-01 Fratagene Therapeutics Srl Methods for treating Friedreich's ataxia with etravirine
WO2025151517A1 (en) * 2024-01-08 2025-07-17 Wavebreak Therapeutics Limited Thiazole compounds, compositions and methods of treating disorders associated with missfolding of alpha-synuclein protein

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JP2014528450A (ja) 2014-10-27
AU2012318670A1 (en) 2014-05-22
PH12014500724A1 (en) 2014-05-19
SG11201401207XA (en) 2014-05-29
US20140249154A1 (en) 2014-09-04
CA2850779A1 (en) 2013-04-11
IL231923A0 (en) 2014-05-28
EP2763674A4 (en) 2015-04-29
KR20140071472A (ko) 2014-06-11
HK1200361A1 (en) 2015-08-07
BR112014007963A2 (pt) 2013-04-11
US10087173B2 (en) 2018-10-02
US20170066758A1 (en) 2017-03-09
JP2017149753A (ja) 2017-08-31

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