SG10201705984XA - Method of synthesizing thyroid hormone analogs and polymorphs thereof - Google Patents

Method of synthesizing thyroid hormone analogs and polymorphs thereof

Info

Publication number
SG10201705984XA
SG10201705984XA SG10201705984XA SG10201705984XA SG10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA SG 10201705984X A SG10201705984X A SG 10201705984XA
Authority
SG
Singapore
Prior art keywords
polymorphs
thyroid hormone
hormone analogs
synthesizing
synthesizing thyroid
Prior art date
Application number
SG10201705984XA
Other languages
English (en)
Original Assignee
Madrigal Pharmaceuticals Inc
F Hoffmann-La Roche Ltd
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 Madrigal Pharmaceuticals Inc, F Hoffmann-La Roche Ltd filed Critical Madrigal Pharmaceuticals Inc
Publication of SG10201705984XA publication Critical patent/SG10201705984XA/en

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Classifications

    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (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)
  • Steroid Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
SG10201705984XA 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof SG10201705984XA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261702137P 2012-09-17 2012-09-17
US201361790432P 2013-03-15 2013-03-15

Publications (1)

Publication Number Publication Date
SG10201705984XA true SG10201705984XA (en) 2017-08-30

Family

ID=50278769

Family Applications (3)

Application Number Title Priority Date Filing Date
SG11201501907YA SG11201501907YA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
SG10201705984XA SG10201705984XA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
SG10202006058QA SG10202006058QA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG11201501907YA SG11201501907YA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG10202006058QA SG10202006058QA (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

Country Status (21)

Country Link
US (8) US9266861B2 (en:Method)
EP (4) EP3689853B1 (en:Method)
JP (7) JP6616688B2 (en:Method)
KR (4) KR102138750B1 (en:Method)
CN (2) CN105008335B (en:Method)
AR (1) AR092872A1 (en:Method)
AU (1) AU2013315017C1 (en:Method)
BR (2) BR112015005891A2 (en:Method)
CA (3) CA3090070C (en:Method)
DK (2) DK3689853T3 (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) RU2018128393A (en:Method)
SG (3) SG11201501907YA (en:Method)
TW (4) TWI755628B (en:Method)
WO (1) WO2014043706A1 (en:Method)
ZA (1) ZA201501795B (en:Method)

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KR101966490B1 (ko) 2019-08-14
CA3111317C (en) 2023-08-29
US20180228807A1 (en) 2018-08-16
CN105008335B (zh) 2018-12-21
EP4406594B1 (en) 2025-09-10
EP3689853B1 (en) 2021-11-24
RU2018128393A (ru) 2019-03-14
TWI652260B (zh) 2019-03-01
AU2013315017B2 (en) 2017-07-27
US11986481B2 (en) 2024-05-21
KR102363776B1 (ko) 2022-02-15
MY170520A (en) 2019-08-08
HK1212682A1 (en) 2016-06-17
NZ705827A (en) 2018-07-27
SG10202006058QA (en) 2020-08-28
EP4023641A3 (en) 2022-09-14
JP6765408B2 (ja) 2020-10-07
AR092872A1 (es) 2015-05-06
KR20150056630A (ko) 2015-05-26
JP2018080188A (ja) 2018-05-24
DK3689853T3 (da) 2022-03-07
TWI681957B (zh) 2020-01-11
IL314360B2 (en) 2025-09-01
IL237628B (en) 2019-07-31
ZA201501795B (en) 2021-10-27
RU2018128393A3 (en:Method) 2019-04-16
US20240122936A1 (en) 2024-04-18
IL259610B (en) 2020-06-30
JP2019048856A (ja) 2019-03-28
KR20180131647A (ko) 2018-12-10
IL320269A (en) 2025-06-01
EP4406594A3 (en) 2024-11-06
RU2668960C2 (ru) 2018-10-05
JP2022078218A (ja) 2022-05-24
TWI804870B (zh) 2023-06-11
MX2018014924A (es) 2020-09-02
US20210161904A1 (en) 2021-06-03
IL288133B2 (en) 2024-12-01
EP2895466B1 (en) 2020-03-25
US20150203473A1 (en) 2015-07-23
CN108101851A (zh) 2018-06-01
IL275393A (en) 2020-07-30
US20160243126A1 (en) 2016-08-25
KR20200023528A (ko) 2020-03-04
JP7436542B2 (ja) 2024-02-21
DK2895466T3 (da) 2020-06-08
US11564926B2 (en) 2023-01-31
EP2895466A1 (en) 2015-07-22
EP4023641A2 (en) 2022-07-06
ES2907926T3 (es) 2022-04-27
US10894050B2 (en) 2021-01-19
TW201425300A (zh) 2014-07-01
US20240148742A1 (en) 2024-05-09
US20230210856A1 (en) 2023-07-06
IL265030B (en) 2020-07-30
CA3090070A1 (en) 2014-03-20
EP4406594A2 (en) 2024-07-31
IL237628A0 (en) 2015-04-30
IL259610A (en) 2018-07-31
MX364661B (es) 2019-05-03
TW201906835A (zh) 2019-02-16
MX2015003418A (es) 2016-04-04
US9266861B2 (en) 2016-02-23
JP6616688B2 (ja) 2019-12-04
JP2015535817A (ja) 2015-12-17
IL288133A (en) 2022-01-01
JP2024056793A (ja) 2024-04-23
JP2020015739A (ja) 2020-01-30
BR112015005891A2 (pt) 2017-08-08
ES2795450T3 (es) 2020-11-23
US20190381053A1 (en) 2019-12-19
WO2014043706A1 (en) 2014-03-20
JP6899413B2 (ja) 2021-07-07
TW202134217A (zh) 2021-09-16
CA3090070C (en) 2023-01-24
IL288133B1 (en) 2024-08-01
EP4023641B1 (en) 2024-05-01
IL314360A (en) 2024-09-01
US10376517B2 (en) 2019-08-13
WO2014043706A8 (en) 2017-10-19
SG11201501907YA (en) 2015-04-29
JP2020109090A (ja) 2020-07-16
NZ739645A (en) 2019-11-29
MX395148B (es) 2025-03-24
EP2895466A4 (en) 2016-08-10
BR122021024202B1 (pt) 2022-05-17
TWI755628B (zh) 2022-02-21
IL275393B (en) 2022-01-01
CA3111317A1 (en) 2014-03-20
CA2884481C (en) 2021-04-27
RU2015114327A (ru) 2016-11-10
AU2013315017A1 (en) 2015-04-02
US9968612B2 (en) 2018-05-15
JP6532931B2 (ja) 2019-06-19
KR20210083381A (ko) 2021-07-06
EP3689853A1 (en) 2020-08-05
IN2015DN03133A (en:Method) 2015-10-02
JP7038745B2 (ja) 2022-03-18
TW201946917A (zh) 2019-12-16
CN105008335A (zh) 2015-10-28
AU2013315017C1 (en) 2017-11-23
KR102138750B1 (ko) 2020-07-29
CA2884481A1 (en) 2014-03-20
IL314360B1 (en) 2025-05-01

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