DK2895466T3 - Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf - Google Patents

Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf Download PDF

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Publication number
DK2895466T3
DK2895466T3 DK13837402.0T DK13837402T DK2895466T3 DK 2895466 T3 DK2895466 T3 DK 2895466T3 DK 13837402 T DK13837402 T DK 13837402T DK 2895466 T3 DK2895466 T3 DK 2895466T3
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Denmark
Prior art keywords
thyreoida
polymorphs
synthesis
procedure
hormone analogs
Prior art date
Application number
DK13837402.0T
Other languages
English (en)
Inventor
D Keith Hester
Robert J Duguid
Martha Kelly
Gang Dong
Edwin L Crow
Rebecca Taub
Charles H Reynolds
Duk Soon Choi
Lianhe Shu
Ping Wang
Anna Chasnoff
Original Assignee
Madrigal Pharmaceuticals Inc
F Hoffmann La Roche Ltd
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Application filed by Madrigal Pharmaceuticals Inc, F Hoffmann La Roche Ltd filed Critical Madrigal Pharmaceuticals Inc
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Publication of DK2895466T3 publication Critical patent/DK2895466T3/da

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    • 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

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  • 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)
  • 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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
DK13837402.0T 2012-09-17 2013-09-17 Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf DK2895466T3 (da)

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
DK2895466T3 true DK2895466T3 (da) 2020-06-08

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Application Number Title Priority Date Filing Date
DK20157696.4T DK3689853T3 (da) 2012-09-17 2013-09-17 Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf
DK13837402.0T DK2895466T3 (da) 2012-09-17 2013-09-17 Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf

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US (8) US9266861B2 (da)
EP (4) EP4023641B1 (da)
JP (7) JP6616688B2 (da)
KR (4) KR102363776B1 (da)
CN (2) CN105008335B (da)
AR (1) AR092872A1 (da)
AU (1) AU2013315017C1 (da)
BR (2) BR112015005891A2 (da)
CA (3) CA2884481C (da)
DK (2) DK3689853T3 (da)
ES (2) ES2795450T3 (da)
HK (1) HK1212682A1 (da)
IL (6) IL288133B1 (da)
IN (1) IN2015DN03133A (da)
MX (2) MX364661B (da)
MY (1) MY170520A (da)
NZ (2) NZ739645A (da)
RU (2) RU2018128393A (da)
SG (3) SG10202006058QA (da)
TW (4) TWI681957B (da)
WO (1) WO2014043706A1 (da)
ZA (1) ZA201501795B (da)

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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
AU2019359141A1 (en) * 2018-10-12 2021-04-22 InventisBio Co., Ltd. Thyroid hormone receptor agonists
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CA3158379A1 (en) 2019-11-26 2021-06-03 Hejun Lv 1,2,4-triazine-3,5-dione compound, preparation method therefor, and application thereof
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
WO2021129465A1 (zh) * 2019-12-26 2021-07-01 苏州科睿思制药有限公司 一种Resmetirom晶型及其制备方法和用途
US20230339911A1 (en) * 2020-08-27 2023-10-26 InventisBio Co., Ltd. Pyridazinone compounds
KR20230066408A (ko) * 2020-09-10 2023-05-15 크리스탈 파마슈티컬 (쑤저우) 씨오., 엘티디. 레스메티롬의 결정형, 이의 제조 방법 및 이의 용도
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TW202245775A (zh) 2021-02-01 2022-12-01 美商瑪德瑞高製藥公司 用於治療肝病症或脂質病症之瑞舒伐他汀(Rosuvastatin)和瑞司美替隆(Resmetirom)的治療組合
CN114907327A (zh) * 2021-02-10 2022-08-16 杭州领业医药科技有限公司 Resmetirom的晶型及其制备方法和用途
CN115073429A (zh) * 2021-03-15 2022-09-20 昆药集团股份有限公司 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法
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CA3099752C (en) 2018-06-12 2023-12-19 Fronthera U.S. Pharmaceuticals Llc Thyroid hormone receptor agonists and uses thereof
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
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HK1212682A1 (zh) 2016-06-17
WO2014043706A1 (en) 2014-03-20
TWI652260B (zh) 2019-03-01
AU2013315017C1 (en) 2017-11-23
CN105008335A (zh) 2015-10-28
TWI804870B (zh) 2023-06-11
JP2018080188A (ja) 2018-05-24
JP7436542B2 (ja) 2024-02-21
TWI755628B (zh) 2022-02-21
JP2015535817A (ja) 2015-12-17
EP2895466A4 (en) 2016-08-10
EP3689853A1 (en) 2020-08-05
IL237628B (en) 2019-07-31
KR20200023528A (ko) 2020-03-04
CN105008335B (zh) 2018-12-21
JP6532931B2 (ja) 2019-06-19
RU2018128393A3 (da) 2019-04-16
ZA201501795B (en) 2021-10-27
US10376517B2 (en) 2019-08-13
US20180228807A1 (en) 2018-08-16
JP2020015739A (ja) 2020-01-30
SG10201705984XA (en) 2017-08-30
EP4406594A2 (en) 2024-07-31
KR102138750B1 (ko) 2020-07-29
CN108101851A (zh) 2018-06-01
SG11201501907YA (en) 2015-04-29
AU2013315017B2 (en) 2017-07-27
US9968612B2 (en) 2018-05-15
US20240122936A1 (en) 2024-04-18
JP2022078218A (ja) 2022-05-24
US10894050B2 (en) 2021-01-19
IL237628A0 (en) 2015-04-30
CA2884481C (en) 2021-04-27
JP6616688B2 (ja) 2019-12-04
EP2895466A1 (en) 2015-07-22
TW202134217A (zh) 2021-09-16
IN2015DN03133A (da) 2015-10-02
US11986481B2 (en) 2024-05-21
IL265030B (en) 2020-07-30
IL259610B (en) 2020-06-30
KR20210083381A (ko) 2021-07-06
JP6899413B2 (ja) 2021-07-07
EP2895466B1 (en) 2020-03-25
IL259610A (en) 2018-07-31
MY170520A (en) 2019-08-08
EP4023641A3 (en) 2022-09-14
DK3689853T3 (da) 2022-03-07
ES2907926T3 (es) 2022-04-27
MX2015003418A (es) 2016-04-04
CA3090070C (en) 2023-01-24
US20160243126A1 (en) 2016-08-25
US20150203473A1 (en) 2015-07-23
CA3111317C (en) 2023-08-29
US11564926B2 (en) 2023-01-31
US9266861B2 (en) 2016-02-23
AR092872A1 (es) 2015-05-06
IL288133A (en) 2022-01-01
TW201906835A (zh) 2019-02-16
KR101966490B1 (ko) 2019-08-14
MX2018014924A (es) 2020-09-02
JP7038745B2 (ja) 2022-03-18
IL314360A (en) 2024-09-01
BR112015005891A2 (pt) 2017-08-08
SG10202006058QA (en) 2020-08-28
EP4023641B1 (en) 2024-05-01
EP3689853B1 (en) 2021-11-24
KR20150056630A (ko) 2015-05-26
CA2884481A1 (en) 2014-03-20
US20230210856A1 (en) 2023-07-06
US20210161904A1 (en) 2021-06-03
IL275393B (en) 2022-01-01
ES2795450T3 (es) 2020-11-23
IL275393A (en) 2020-07-30
JP6765408B2 (ja) 2020-10-07
JP2020109090A (ja) 2020-07-16
TW201425300A (zh) 2014-07-01
NZ739645A (en) 2019-11-29
NZ705827A (en) 2018-07-27
BR122021024202B1 (pt) 2022-05-17
AU2013315017A1 (en) 2015-04-02
KR20180131647A (ko) 2018-12-10
RU2018128393A (ru) 2019-03-14
JP2024056793A (ja) 2024-04-23
CA3090070A1 (en) 2014-03-20
RU2015114327A (ru) 2016-11-10
IL288133B1 (en) 2024-08-01
MX364661B (es) 2019-05-03
US20190381053A1 (en) 2019-12-19
US20240148742A1 (en) 2024-05-09
KR102363776B1 (ko) 2022-02-15
RU2668960C2 (ru) 2018-10-05
TWI681957B (zh) 2020-01-11
EP4023641A2 (en) 2022-07-06
JP2019048856A (ja) 2019-03-28
WO2014043706A8 (en) 2017-10-19
TW201946917A (zh) 2019-12-16
CA3111317A1 (en) 2014-03-20

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