AU2012211299B2 - Small molecule RNase inhibitors and methods of use - Google Patents

Small molecule RNase inhibitors and methods of use Download PDF

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Publication number
AU2012211299B2
AU2012211299B2 AU2012211299A AU2012211299A AU2012211299B2 AU 2012211299 B2 AU2012211299 B2 AU 2012211299B2 AU 2012211299 A AU2012211299 A AU 2012211299A AU 2012211299 A AU2012211299 A AU 2012211299A AU 2012211299 B2 AU2012211299 B2 AU 2012211299B2
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AU
Australia
Prior art keywords
rnpa
substituted
unsubstituted
infection
aureus
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AU2012211299A
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AU2012211299A2 (en
AU2012211299A1 (en
Inventor
Wayne Childers
Paul M. DUNMAN
Patrick D. OLSON
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University of Rochester
Temple Univ School of Medicine
University of Nebraska System
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University of Nebraska Lincoln
University of Rochester
Temple Univ School of Medicine
University of Nebraska System
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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/44—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving esterase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/916—Hydrolases (3) acting on ester bonds (3.1), e.g. phosphatases (3.1.3), phospholipases C or phospholipases D (3.1.4)
    • G01N2333/922—Ribonucleases (RNAses); Deoxyribonucleases (DNAses)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Pyrrole Compounds (AREA)
AU2012211299A 2011-01-26 2012-01-26 Small molecule RNase inhibitors and methods of use Ceased AU2012211299B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161436342P 2011-01-26 2011-01-26
US61/436,342 2011-01-26
PCT/US2012/022662 WO2012103295A2 (en) 2011-01-26 2012-01-26 Small molecule rnase inhibitors and methods of use

Publications (3)

Publication Number Publication Date
AU2012211299A1 AU2012211299A1 (en) 2013-08-08
AU2012211299A2 AU2012211299A2 (en) 2013-11-14
AU2012211299B2 true AU2012211299B2 (en) 2017-02-02

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AU2012211299A Ceased AU2012211299B2 (en) 2011-01-26 2012-01-26 Small molecule RNase inhibitors and methods of use
AU2012211253A Ceased AU2012211253B2 (en) 2011-01-26 2012-01-26 Small molecule RNase inhibitors and methods of use

Family Applications After (1)

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AU2012211253A Ceased AU2012211253B2 (en) 2011-01-26 2012-01-26 Small molecule RNase inhibitors and methods of use

Country Status (7)

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US (4) US9089545B2 (Direct)
EP (3) EP3243513B1 (Direct)
JP (3) JP6010548B2 (Direct)
CN (2) CN103635191A (Direct)
AU (2) AU2012211299B2 (Direct)
CA (2) CA2825907C (Direct)
WO (2) WO2012103295A2 (Direct)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3243513B1 (en) 2011-01-26 2019-06-05 University Of Rochester Use of the rnase inhibitor rnpa-3000 for treating staphylococcus infections
RS63190B1 (sr) 2014-08-04 2022-06-30 Nuevolution As Opciono fuzionisani derivati pirimidina zamenjeni heterociklilom korisni za lečenje zapaljenskih, metaboličkih, onkoloških i autoimunskih bolesti
AU2015339039B2 (en) * 2014-10-31 2019-11-28 Temple University -- Of The Commonwealth System Of Higher Education Synergistic compositions for treating microbial infections
WO2016093606A1 (ko) * 2014-12-09 2016-06-16 한국과학기술원 rnpA 유전자 발현감소를 통한 재조합단백질의 제조방법
KR101765255B1 (ko) 2014-12-09 2017-08-04 한국과학기술원 rnpA 유전자 발현감소를 통한 재조합단백질의 제조방법
WO2019079369A1 (en) 2017-10-19 2019-04-25 Effector Therapeutics, Inc. BENZIMIDAZOLE INDOLE INHIBITORS OF MNK1 AND MNK2
AU2020405446A1 (en) 2019-12-20 2022-05-26 Nuevolution A/S Compounds active towards nuclear receptors
US11685727B2 (en) 2019-12-20 2023-06-27 Nuevolution A/S Compounds active towards nuclear receptors
EP4126875A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors
MX2022012260A (es) 2020-03-31 2022-11-30 Nuevolution As Compuestos activos frente a receptores nucleares.

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JPH03182742A (ja) * 1989-12-12 1991-08-08 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料
US20040180889A1 (en) * 2002-03-01 2004-09-16 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
US20050187409A1 (en) * 2003-10-21 2005-08-25 Powers Gordon D. Inhibitors of RNase P proteins as antibacterial compounds
US20090163545A1 (en) * 2007-12-21 2009-06-25 University Of Rochester Method For Altering The Lifespan Of Eukaryotic Organisms
WO2010003533A2 (en) * 2008-06-17 2010-01-14 Institut Pasteur Korea Anti-infective compounds

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EP1130091A3 (en) 2000-03-01 2001-11-14 Message Pharmaceuticals, Inc. Bacterial RNaseP Proteins and their use in identifying antibacterial compounds
US20020123077A1 (en) * 2000-09-29 2002-09-05 O'toole George A. Novel compounds capable of modulating biofilms
US20020052396A1 (en) * 2001-04-23 2002-05-02 Bailey Thomas R. Compounds, compositions and methods for treating or preventing viral infections and associated diseases
AU2002336746A1 (en) * 2001-09-21 2003-04-01 Message Pharmaceuticals, Inc. Inhibitors of rnase p proteins as antibacterial compounds
US20050042674A9 (en) 2002-02-21 2005-02-24 Lin Yu Common ligand mimics: thiazolidinediones and rhodanines
GB2386892A (en) * 2002-03-28 2003-10-01 Pantherix Ltd Carboxy containing (phenyl-/heterocyclyl-)methylene substituted azole & azine derivatives and their therapeutic use as antibacterials
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US7718680B2 (en) * 2004-09-23 2010-05-18 Burnham Institute For Medical Research Inhibition of lethal factor protease activity from anthrax toxin
CN101267815B (zh) 2005-09-22 2013-11-06 明治制果药业株式会社 金属-β-内酰胺酶抑制剂
EP3243513B1 (en) 2011-01-26 2019-06-05 University Of Rochester Use of the rnase inhibitor rnpa-3000 for treating staphylococcus infections

Patent Citations (5)

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Publication number Priority date Publication date Assignee Title
JPH03182742A (ja) * 1989-12-12 1991-08-08 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料
US20040180889A1 (en) * 2002-03-01 2004-09-16 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
US20050187409A1 (en) * 2003-10-21 2005-08-25 Powers Gordon D. Inhibitors of RNase P proteins as antibacterial compounds
US20090163545A1 (en) * 2007-12-21 2009-06-25 University Of Rochester Method For Altering The Lifespan Of Eukaryotic Organisms
WO2010003533A2 (en) * 2008-06-17 2010-01-14 Institut Pasteur Korea Anti-infective compounds

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Also Published As

Publication number Publication date
AU2012211299A2 (en) 2013-11-14
CN103635191A (zh) 2014-03-12
US9089545B2 (en) 2015-07-28
WO2012103336A1 (en) 2012-08-02
CA2825907C (en) 2019-07-30
US20130296386A1 (en) 2013-11-07
EP2667872A2 (en) 2013-12-04
EP3243513B1 (en) 2019-06-05
EP2667873A1 (en) 2013-12-04
AU2012211253B2 (en) 2016-11-10
US9693999B2 (en) 2017-07-04
US9517230B2 (en) 2016-12-13
US20150283118A1 (en) 2015-10-08
WO2012103295A2 (en) 2012-08-02
CN103635193A (zh) 2014-03-12
CA2825907A1 (en) 2012-08-02
US20160115124A1 (en) 2016-04-28
US20130303585A1 (en) 2013-11-14
EP3243513A1 (en) 2017-11-15
CN103635193B (zh) 2017-02-08
EP2667872A4 (en) 2014-08-13
JP6010548B2 (ja) 2016-10-19
JP2017014246A (ja) 2017-01-19
US9233095B2 (en) 2016-01-12
EP2667873A4 (en) 2014-07-30
WO2012103295A3 (en) 2012-10-11
JP6248151B2 (ja) 2017-12-13
CA2825905A1 (en) 2012-08-02
EP2667872B1 (en) 2019-01-02
JP2014510717A (ja) 2014-05-01
JP2014511366A (ja) 2014-05-15
EP2667873B1 (en) 2017-05-31
CA2825905C (en) 2019-06-04

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