AU2013274030B2 - Deuterated derivatives of ruxolitinib - Google Patents

Deuterated derivatives of ruxolitinib Download PDF

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Publication number
AU2013274030B2
AU2013274030B2 AU2013274030A AU2013274030A AU2013274030B2 AU 2013274030 B2 AU2013274030 B2 AU 2013274030B2 AU 2013274030 A AU2013274030 A AU 2013274030A AU 2013274030 A AU2013274030 A AU 2013274030A AU 2013274030 B2 AU2013274030 B2 AU 2013274030B2
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Prior art keywords
compound
deuterium
hydrogen
myelofibrosis
pharmaceutically acceptable
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AU2013274030A
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AU2013274030A1 (en
Inventor
Scott L. Harbeson
Julie F. Liu
Adam J. Morgan
Bhaumik PANDYA
I. Robert Silverman
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Sun Pharmaceutical Industries Inc
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Sun Pharmaceutical Industries Inc
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Application filed by Sun Pharmaceutical Industries Inc filed Critical Sun Pharmaceutical Industries Inc
Publication of AU2013274030A1 publication Critical patent/AU2013274030A1/en
Application granted granted Critical
Publication of AU2013274030B2 publication Critical patent/AU2013274030B2/en
Priority to AU2016238877A priority Critical patent/AU2016238877B2/en
Priority to AU2018271227A priority patent/AU2018271227B2/en
Assigned to SUN PHARMACEUTICAL INDUSTRIES, INC. reassignment SUN PHARMACEUTICAL INDUSTRIES, INC. Request to Amend Deed and Register Assignors: CONCERT PHARMACEUTICALS, INC.
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    • 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
    • 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
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/7068—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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2013274030A 2012-06-15 2013-06-14 Deuterated derivatives of ruxolitinib Active AU2013274030B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2016238877A AU2016238877B2 (en) 2012-06-15 2016-10-05 Deuterated derivatives of ruxolitinib
AU2018271227A AU2018271227B2 (en) 2012-06-15 2018-11-26 Deuterated derivatives of ruxolitinib

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261660428P 2012-06-15 2012-06-15
US61/660,428 2012-06-15
US201261678795P 2012-08-02 2012-08-02
US61/678,795 2012-08-02
PCT/US2013/045919 WO2013188783A1 (en) 2012-06-15 2013-06-14 Deuterated derivatives of ruxolitinib

Related Child Applications (1)

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AU2016238877A Division AU2016238877B2 (en) 2012-06-15 2016-10-05 Deuterated derivatives of ruxolitinib

Publications (2)

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AU2013274030A1 AU2013274030A1 (en) 2015-01-22
AU2013274030B2 true AU2013274030B2 (en) 2016-07-07

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AU2013274030A Active AU2013274030B2 (en) 2012-06-15 2013-06-14 Deuterated derivatives of ruxolitinib
AU2016238877A Active AU2016238877B2 (en) 2012-06-15 2016-10-05 Deuterated derivatives of ruxolitinib
AU2018271227A Active AU2018271227B2 (en) 2012-06-15 2018-11-26 Deuterated derivatives of ruxolitinib

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AU2018271227A Active AU2018271227B2 (en) 2012-06-15 2018-11-26 Deuterated derivatives of ruxolitinib

Country Status (17)

Country Link
US (7) US20150197525A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (4) EP3882249B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (3) AU2013274030B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR122023027277A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2876306C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (2) DK3450434T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EA (1) EA201492287A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2867048T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FI (1) FI3882249T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2014DN10670A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
LT (1) LT3882249T (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (2) MX360495B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (2) PL3882249T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT3882249T (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RS (1) RS67061B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SM (1) SMT202500302T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2013188783A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

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