IL288133B2 - Method of synthesizing thyroid hormone analogs and polymorphs thereof - Google Patents

Method of synthesizing thyroid hormone analogs and polymorphs thereof

Info

Publication number
IL288133B2
IL288133B2 IL288133A IL28813321A IL288133B2 IL 288133 B2 IL288133 B2 IL 288133B2 IL 288133 A IL288133 A IL 288133A IL 28813321 A IL28813321 A IL 28813321A IL 288133 B2 IL288133 B2 IL 288133B2
Authority
IL
Israel
Prior art keywords
compound
morphic form
batch
vol
less
Prior art date
Application number
IL288133A
Other languages
English (en)
Hebrew (he)
Other versions
IL288133A (en
IL288133B1 (en
Original Assignee
F Hoffmann La Roche Ltd
Madrigal Pharmaceuticals Inc
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
Application filed by F Hoffmann La Roche Ltd, Madrigal Pharmaceuticals Inc filed Critical F Hoffmann La Roche Ltd
Publication of IL288133A publication Critical patent/IL288133A/en
Publication of IL288133B1 publication Critical patent/IL288133B1/en
Publication of IL288133B2 publication Critical patent/IL288133B2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D237/14Oxygen atoms
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D237/14Oxygen atoms
    • C07D237/16Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • 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
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
IL288133A 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof IL288133B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261702137P 2012-09-17 2012-09-17
US201361790432P 2013-03-15 2013-03-15
PCT/US2013/060177 WO2014043706A1 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

Publications (3)

Publication Number Publication Date
IL288133A IL288133A (en) 2022-01-01
IL288133B1 IL288133B1 (en) 2024-08-01
IL288133B2 true IL288133B2 (en) 2024-12-01

Family

ID=50278769

Family Applications (7)

Application Number Title Priority Date Filing Date
IL288133A IL288133B2 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
IL320269A IL320269A (en) 2012-09-17 2013-09-17 Method for the synthesis of thyroid hormone analogs and their polymorphs
IL237628A IL237628B (en) 2012-09-17 2015-03-09 A method for synthesizing thyroid hormone analogs and their polymorphs
IL259610A IL259610B (en) 2012-09-17 2018-05-27 A method for synthesizing thyroid hormone analogs and their polymorphs
IL265030A IL265030B (en) 2012-09-17 2019-02-25 Method of synthesizing thyroid hormone analogs and polymorphs thereof
IL275393A IL275393B (en) 2012-09-17 2020-06-15 A method for synthesizing thyroid hormone analogs and their polymorphs
IL314360A IL314360B2 (en) 2012-09-17 2024-07-17 Method for the synthesis of thyroid hormone analogs and their polymorphs

Family Applications After (6)

Application Number Title Priority Date Filing Date
IL320269A IL320269A (en) 2012-09-17 2013-09-17 Method for the synthesis of thyroid hormone analogs and their polymorphs
IL237628A IL237628B (en) 2012-09-17 2015-03-09 A method for synthesizing thyroid hormone analogs and their polymorphs
IL259610A IL259610B (en) 2012-09-17 2018-05-27 A method for synthesizing thyroid hormone analogs and their polymorphs
IL265030A IL265030B (en) 2012-09-17 2019-02-25 Method of synthesizing thyroid hormone analogs and polymorphs thereof
IL275393A IL275393B (en) 2012-09-17 2020-06-15 A method for synthesizing thyroid hormone analogs and their polymorphs
IL314360A IL314360B2 (en) 2012-09-17 2024-07-17 Method for the synthesis of thyroid hormone analogs and their polymorphs

Country Status (21)

Country Link
US (8) US9266861B2 (en:Method)
EP (4) EP2895466B1 (en:Method)
JP (7) JP6616688B2 (en:Method)
KR (4) KR20200023528A (en:Method)
CN (2) CN108101851A (en:Method)
AR (1) AR092872A1 (en:Method)
AU (1) AU2013315017C1 (en:Method)
BR (2) BR112015005891A2 (en:Method)
CA (3) CA2884481C (en:Method)
DK (2) DK2895466T3 (en:Method)
ES (2) ES2795450T3 (en:Method)
IL (7) IL288133B2 (en:Method)
IN (1) IN2015DN03133A (en:Method)
MX (2) MX395148B (en:Method)
MY (1) MY170520A (en:Method)
NZ (2) NZ739645A (en:Method)
RU (2) RU2668960C2 (en:Method)
SG (3) SG11201501907YA (en:Method)
TW (4) TWI804870B (en:Method)
WO (1) WO2014043706A1 (en:Method)
ZA (1) ZA201501795B (en:Method)

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Also Published As

Publication number Publication date
AU2013315017B2 (en) 2017-07-27
KR102138750B1 (ko) 2020-07-29
IL275393A (en) 2020-07-30
US11986481B2 (en) 2024-05-21
JP2020015739A (ja) 2020-01-30
CA3111317C (en) 2023-08-29
IL275393B (en) 2022-01-01
IL314360A (en) 2024-09-01
US10376517B2 (en) 2019-08-13
EP4406594A3 (en) 2024-11-06
CN108101851A (zh) 2018-06-01
AU2013315017C1 (en) 2017-11-23
US20240148742A1 (en) 2024-05-09
RU2015114327A (ru) 2016-11-10
IL314360B2 (en) 2025-09-01
EP2895466B1 (en) 2020-03-25
RU2668960C2 (ru) 2018-10-05
ES2907926T3 (es) 2022-04-27
CN105008335B (zh) 2018-12-21
US20190381053A1 (en) 2019-12-19
TW201425300A (zh) 2014-07-01
DK3689853T3 (da) 2022-03-07
IL288133A (en) 2022-01-01
ZA201501795B (en) 2021-10-27
JP6532931B2 (ja) 2019-06-19
SG10201705984XA (en) 2017-08-30
JP6899413B2 (ja) 2021-07-07
IL237628A0 (en) 2015-04-30
EP2895466A4 (en) 2016-08-10
SG11201501907YA (en) 2015-04-29
JP6765408B2 (ja) 2020-10-07
EP4406594A2 (en) 2024-07-31
US11564926B2 (en) 2023-01-31
KR102363776B1 (ko) 2022-02-15
KR20210083381A (ko) 2021-07-06
MY170520A (en) 2019-08-08
RU2018128393A3 (en:Method) 2019-04-16
TWI755628B (zh) 2022-02-21
US9968612B2 (en) 2018-05-15
EP4023641B1 (en) 2024-05-01
US20150203473A1 (en) 2015-07-23
IL288133B1 (en) 2024-08-01
MX2018014924A (es) 2020-09-02
EP3689853B1 (en) 2021-11-24
EP3689853A1 (en) 2020-08-05
EP2895466A1 (en) 2015-07-22
US20240122936A1 (en) 2024-04-18
US20180228807A1 (en) 2018-08-16
SG10202006058QA (en) 2020-08-28
WO2014043706A8 (en) 2017-10-19
IL320269A (en) 2025-06-01
NZ705827A (en) 2018-07-27
EP4023641A2 (en) 2022-07-06
TW201946917A (zh) 2019-12-16
MX395148B (es) 2025-03-24
JP6616688B2 (ja) 2019-12-04
TW202134217A (zh) 2021-09-16
US10894050B2 (en) 2021-01-19
JP2019048856A (ja) 2019-03-28
JP2022078218A (ja) 2022-05-24
ES2795450T3 (es) 2020-11-23
AR092872A1 (es) 2015-05-06
US9266861B2 (en) 2016-02-23
BR112015005891A2 (pt) 2017-08-08
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