IL320269A - Method for the synthesis of thyroid hormone analogs and their polymorphs - Google Patents

Method for the synthesis of thyroid hormone analogs and their polymorphs

Info

Publication number
IL320269A
IL320269A IL320269A IL32026925A IL320269A IL 320269 A IL320269 A IL 320269A IL 320269 A IL320269 A IL 320269A IL 32026925 A IL32026925 A IL 32026925A IL 320269 A IL320269 A IL 320269A
Authority
IL
Israel
Prior art keywords
polymorphs
thyroid hormone
hormone analogs
synthesizing
synthesizing thyroid
Prior art date
Application number
IL320269A
Other languages
English (en)
Hebrew (he)
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 IL320269A publication Critical patent/IL320269A/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)
  • 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)
  • 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)
IL320269A 2012-09-17 2013-09-17 Method for the synthesis of thyroid hormone analogs and their polymorphs IL320269A (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 (1)

Publication Number Publication Date
IL320269A true IL320269A (en) 2025-06-01

Family

ID=50278769

Family Applications (7)

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
IL288133A IL288133B2 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
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
IL288133A IL288133B2 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof
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) EP4406594B1 (en:Method)
JP (7) JP6616688B2 (en:Method)
KR (4) KR20200023528A (en:Method)
CN (2) CN105008335B (en:Method)
AR (1) AR092872A1 (en:Method)
AU (1) AU2013315017C1 (en:Method)
BR (2) BR122021024202B1 (en:Method)
CA (3) CA3090070C (en:Method)
DK (2) DK2895466T3 (en:Method)
ES (2) ES2795450T3 (en:Method)
IL (7) IL320269A (en:Method)
IN (1) IN2015DN03133A (en:Method)
MX (2) MX364661B (en:Method)
MY (1) MY170520A (en:Method)
NZ (2) NZ705827A (en:Method)
RU (2) RU2018128393A (en:Method)
SG (3) SG10201705984XA (en:Method)
TW (4) TWI804870B (en:Method)
WO (1) WO2014043706A1 (en:Method)
ZA (1) ZA201501795B (en:Method)

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JP7181386B2 (ja) * 2018-06-12 2022-11-30 スーチョワン ハイスコ ファーマスーティカル カンパニー リミテッド 甲状腺ホルモン受容体アゴニスト及びその用途
CN110627773B (zh) * 2018-06-22 2021-03-19 海创药业股份有限公司 氘代mgl-3196化合物及其用途
AR115666A1 (es) * 2018-07-02 2021-02-10 Madrigal Pharmaceuticals Inc Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo
EP3864013A4 (en) * 2018-10-12 2022-09-28 InventisBio Co., Ltd. Thyroid hormone receptor agonists
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CN119431265A (zh) 2019-02-21 2025-02-14 南京瑞捷医药科技有限公司 一种作为甲状腺激素受体激动剂的化合物
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WO2020239076A1 (zh) * 2019-05-29 2020-12-03 南京明德新药研发有限公司 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用
CN112442013B (zh) * 2019-09-04 2022-07-26 广东东阳光药业有限公司 一种作为甲状腺激素β受体激动剂的化合物及其用途
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CN112707892A (zh) * 2019-10-24 2021-04-27 苏州泽璟生物制药股份有限公司 哒嗪酮或哒嗪类化合物及其衍生物和药物组合物
JP7574292B2 (ja) 2019-11-26 2024-10-28 昆薬集団股▲フン▼有限公司 1,2,4-トリアジン-3,5-ジオン系化合物およびその製造方法と応用
TW202128668A (zh) * 2019-12-16 2021-08-01 大陸商江蘇恆瑞醫藥股份有限公司 并環類衍生物、其製備方法及其在醫藥上的應用
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EP4406594B1 (en) 2025-09-10
US10376517B2 (en) 2019-08-13
IL314360A (en) 2024-09-01
IL288133B1 (en) 2024-08-01
EP2895466A1 (en) 2015-07-22
JP2020015739A (ja) 2020-01-30
NZ705827A (en) 2018-07-27
JP2015535817A (ja) 2015-12-17
RU2018128393A (ru) 2019-03-14
EP4406594A3 (en) 2024-11-06
TW201946917A (zh) 2019-12-16
TWI681957B (zh) 2020-01-11
CN108101851A (zh) 2018-06-01
MX2018014924A (es) 2020-09-02
US20180228807A1 (en) 2018-08-16
JP6616688B2 (ja) 2019-12-04
CA2884481A1 (en) 2014-03-20
KR102363776B1 (ko) 2022-02-15
ES2795450T3 (es) 2020-11-23
TWI804870B (zh) 2023-06-11
JP2018080188A (ja) 2018-05-24
IL237628B (en) 2019-07-31
JP6532931B2 (ja) 2019-06-19
SG10201705984XA (en) 2017-08-30
EP4023641A2 (en) 2022-07-06
IL314360B1 (en) 2025-05-01
TWI755628B (zh) 2022-02-21
KR102138750B1 (ko) 2020-07-29
EP3689853A1 (en) 2020-08-05
TW201425300A (zh) 2014-07-01
EP2895466B1 (en) 2020-03-25
IL288133B2 (en) 2024-12-01
BR112015005891A2 (pt) 2017-08-08
IL259610B (en) 2020-06-30
AR092872A1 (es) 2015-05-06
SG11201501907YA (en) 2015-04-29
US11564926B2 (en) 2023-01-31
CA3111317C (en) 2023-08-29
BR122021024202B1 (pt) 2022-05-17
MY170520A (en) 2019-08-08
CN105008335B (zh) 2018-12-21
JP6899413B2 (ja) 2021-07-07
US20210161904A1 (en) 2021-06-03
WO2014043706A1 (en) 2014-03-20
JP6765408B2 (ja) 2020-10-07
DK2895466T3 (da) 2020-06-08
MX395148B (es) 2025-03-24
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US10894050B2 (en) 2021-01-19
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KR101966490B1 (ko) 2019-08-14
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JP7038745B2 (ja) 2022-03-18
RU2015114327A (ru) 2016-11-10
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WO2014043706A8 (en) 2017-10-19
ES2907926T3 (es) 2022-04-27
TWI652260B (zh) 2019-03-01
KR20210083381A (ko) 2021-07-06
US20160243126A1 (en) 2016-08-25
CA3090070A1 (en) 2014-03-20
JP2024056793A (ja) 2024-04-23
EP3689853B1 (en) 2021-11-24
HK1212682A1 (en) 2016-06-17
IL288133A (en) 2022-01-01
KR20200023528A (ko) 2020-03-04
TW202134217A (zh) 2021-09-16
JP7436542B2 (ja) 2024-02-21
JP2019048856A (ja) 2019-03-28
KR20180131647A (ko) 2018-12-10
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CN105008335A (zh) 2015-10-28
IN2015DN03133A (en:Method) 2015-10-02

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