IN2015DN03133A - - Google Patents

Info

Publication number
IN2015DN03133A
IN2015DN03133A IN3133DEN2015A IN2015DN03133A IN 2015DN03133 A IN2015DN03133 A IN 2015DN03133A IN 3133DEN2015 A IN3133DEN2015 A IN 3133DEN2015A IN 2015DN03133 A IN2015DN03133 A IN 2015DN03133A
Authority
IN
India
Prior art keywords
compounds
pyridazinone
disclosure
thyroid hormone
allow
Prior art date
Application number
Inventor
D Keith Hester
Robert J Duguid
Martha Kelly
Anna Chasnoff
Gang Dong
Edwin L Crow
Rebecca Taub
Charles H Reynolds
Duk Soon Choi
Lianhe Shu
Ping Wang
Original Assignee
Madrigal Pharmaceuticals Inc
Hoffmann La Roche
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, Hoffmann La Roche filed Critical Madrigal Pharmaceuticals Inc
Publication of IN2015DN03133A publication Critical patent/IN2015DN03133A/en

Links

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
    • A61K31/53Heterocyclic 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
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (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)

Abstract

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large- scale preparation of pyridazinone compounds having high purity. In some embodiments , preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRP mutation.
IN3133DEN2015 2012-09-17 2013-09-17 IN2015DN03133A (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
IN2015DN03133A true IN2015DN03133A (en) 2015-10-02

Family

ID=50278769

Family Applications (1)

Application Number Title Priority Date Filing Date
IN3133DEN2015 IN2015DN03133A (en) 2012-09-17 2013-09-17

Country Status (22)

Country Link
US (8) US9266861B2 (en)
EP (3) EP4023641B1 (en)
JP (7) JP6616688B2 (en)
KR (4) KR102138750B1 (en)
CN (2) CN105008335B (en)
AR (1) AR092872A1 (en)
AU (1) AU2013315017C1 (en)
BR (2) BR112015005891A2 (en)
CA (3) CA3090070C (en)
DK (2) DK3689853T3 (en)
ES (2) ES2907926T3 (en)
HK (1) HK1212682A1 (en)
IL (5) IL237628B (en)
IN (1) IN2015DN03133A (en)
MX (2) MX364661B (en)
MY (1) MY170520A (en)
NZ (2) NZ705827A (en)
RU (2) RU2018128393A (en)
SG (3) SG10202006058QA (en)
TW (4) TWI755628B (en)
WO (1) WO2014043706A1 (en)
ZA (1) ZA201501795B (en)

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RU2018128393A (en) * 2012-09-17 2019-03-14 Мадригал Фармасьютикалз, Инк. METHOD FOR SYNTHESIS OF ANALOGUES OF THYROID HORMONES AND THEIR POLYMORPHES
IL266054B2 (en) 2016-10-18 2023-10-01 Madrigal Pharmaceuticals Inc Methods of treating liver disorders or lipid disorders with a thr-beta agonist
US11485729B2 (en) 2018-01-23 2022-11-01 Shenzhen Targetrx, Inc. Substituted pyridazinone compound
WO2019240938A1 (en) 2018-06-12 2019-12-19 Fronthera U.S. Pharmaceuticals Llc Thyroid hormone receptor agonists and uses thereof
WO2019242766A1 (en) * 2018-06-22 2019-12-26 成都海创药业有限公司 Deuterated mgl-3196 compound and use thereof
TW202019914A (en) * 2018-07-02 2020-06-01 美商瑪德瑞高製藥公司 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)- 3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
WO2020073974A1 (en) * 2018-10-12 2020-04-16 Inventisbio Shanghai Ltd. Thyroid hormone receptor agonists
JP7445996B2 (en) * 2019-02-21 2024-03-08 ナンジン・ルイジェ・ファーマ・カンパニー・リミテッド Novel compounds and their use as thyroid hormone receptor agonists
JP2022532706A (en) * 2019-05-08 2022-07-19 アリゴス セラピューティクス,インコーポレーテッド THR-β regulator and its usage
CN111909137B (en) * 2019-05-10 2023-05-30 深圳微芯生物科技股份有限公司 Pyridazinone derivative and application thereof
WO2020239076A1 (en) * 2019-05-29 2020-12-03 南京明德新药研发有限公司 Pyridazinone derivatives as thyroxine receptor-β agonists and application thereof
CN112442013B (en) * 2019-09-04 2022-07-26 广东东阳光药业有限公司 Compound serving as thyroid hormone beta receptor agonist and application thereof
WO2021063367A1 (en) * 2019-09-30 2021-04-08 苏州科睿思制药有限公司 Resmetirom crystal form and preparation method therefor and use thereof
CN112707892A (en) * 2019-10-24 2021-04-27 苏州泽璟生物制药股份有限公司 Pyridazinone or pyridazine compound and derivative and pharmaceutical composition thereof
EP4083024A4 (en) * 2019-11-26 2023-11-01 KPC Pharmaceuticals, Inc. 1,2,4-triazine-3,5-dione compound, preparation method therefor, and application thereof
WO2021121210A1 (en) * 2019-12-16 2021-06-24 江苏恒瑞医药股份有限公司 Fused-ring derivative, and preparation method therefor and medical use thereof
WO2021129465A1 (en) * 2019-12-26 2021-07-01 苏州科睿思制药有限公司 Resmetirom crystal, preparation method for same, and uses thereof
WO2022041026A1 (en) * 2020-08-27 2022-03-03 InventisBio Co., Ltd. Pyridazinone compounds
CN116171275A (en) * 2020-09-10 2023-05-26 苏州科睿思制药有限公司 Crystal form of Resmetirom and preparation method and application thereof
WO2022086894A1 (en) 2020-10-19 2022-04-28 Teva Pharmaceuticals International Gmbh Solid state forms of resmetirom
TW202245775A (en) 2021-02-01 2022-12-01 美商瑪德瑞高製藥公司 Therapeutic combinations of rosuvastatin and resmetirom for the treatment of liver disorders or lipid disorders
CN114907327A (en) * 2021-02-10 2022-08-16 杭州领业医药科技有限公司 Crystal form of Resmetirom and preparation method and application thereof
CN115073429A (en) * 2021-03-15 2022-09-20 昆药集团股份有限公司 Salt form and crystal form of 1,2, 4-triazine-3, 5-diketone compound and preparation method thereof
CA3233319A1 (en) 2021-09-27 2023-03-30 Rebecca Taub Resmetirom for reducing liver volume

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IL266054B2 (en) 2016-10-18 2023-10-01 Madrigal Pharmaceuticals Inc Methods of treating liver disorders or lipid disorders with a thr-beta agonist
WO2019240938A1 (en) 2018-06-12 2019-12-19 Fronthera U.S. Pharmaceuticals Llc Thyroid hormone receptor agonists and uses thereof
TW202019914A (en) 2018-07-02 2020-06-01 美商瑪德瑞高製藥公司 Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)- 3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
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Publication number Publication date
TW201906835A (en) 2019-02-16
HK1212682A1 (en) 2016-06-17
IL259610A (en) 2018-07-31
US11564926B2 (en) 2023-01-31
IL237628B (en) 2019-07-31
TWI652260B (en) 2019-03-01
US9968612B2 (en) 2018-05-15
CN105008335A (en) 2015-10-28
EP2895466A4 (en) 2016-08-10
CA3090070A1 (en) 2014-03-20
AU2013315017C1 (en) 2017-11-23
NZ739645A (en) 2019-11-29
EP4023641A3 (en) 2022-09-14
TW202134217A (en) 2021-09-16
AR092872A1 (en) 2015-05-06
IL288133A (en) 2022-01-01
EP2895466B1 (en) 2020-03-25
US9266861B2 (en) 2016-02-23
AU2013315017B2 (en) 2017-07-27
IL265030B (en) 2020-07-30
JP2018080188A (en) 2018-05-24
JP6899413B2 (en) 2021-07-07
KR20200023528A (en) 2020-03-04
US11986481B2 (en) 2024-05-21
US20180228807A1 (en) 2018-08-16
JP2022078218A (en) 2022-05-24
EP2895466A1 (en) 2015-07-22
KR20180131647A (en) 2018-12-10
CA3111317A1 (en) 2014-03-20
CA2884481A1 (en) 2014-03-20
RU2668960C2 (en) 2018-10-05
BR112015005891A2 (en) 2017-08-08
MX2015003418A (en) 2016-04-04
JP2024056793A (en) 2024-04-23
JP7436542B2 (en) 2024-02-21
IL275393A (en) 2020-07-30
KR20210083381A (en) 2021-07-06
JP2020015739A (en) 2020-01-30
US20240148742A1 (en) 2024-05-09
US10894050B2 (en) 2021-01-19
IL237628A0 (en) 2015-04-30
DK2895466T3 (en) 2020-06-08
US10376517B2 (en) 2019-08-13
US20230210856A1 (en) 2023-07-06
SG10201705984XA (en) 2017-08-30
TWI681957B (en) 2020-01-11
MY170520A (en) 2019-08-08
KR102363776B1 (en) 2022-02-15
IL259610B (en) 2020-06-30
US20210161904A1 (en) 2021-06-03
US20160243126A1 (en) 2016-08-25
AU2013315017A1 (en) 2015-04-02
SG10202006058QA (en) 2020-08-28
JP7038745B2 (en) 2022-03-18
EP4023641B1 (en) 2024-05-01
CA2884481C (en) 2021-04-27
JP6616688B2 (en) 2019-12-04
SG11201501907YA (en) 2015-04-29
JP2019048856A (en) 2019-03-28
KR101966490B1 (en) 2019-08-14
JP2020109090A (en) 2020-07-16
EP4023641A2 (en) 2022-07-06
TW201946917A (en) 2019-12-16
TWI755628B (en) 2022-02-21
US20190381053A1 (en) 2019-12-19
IL275393B (en) 2022-01-01
ZA201501795B (en) 2021-10-27
WO2014043706A1 (en) 2014-03-20
EP3689853B1 (en) 2021-11-24
KR20150056630A (en) 2015-05-26
JP6765408B2 (en) 2020-10-07
CN105008335B (en) 2018-12-21
JP2015535817A (en) 2015-12-17
US20150203473A1 (en) 2015-07-23
RU2018128393A (en) 2019-03-14
TW201425300A (en) 2014-07-01
TWI804870B (en) 2023-06-11
ES2795450T3 (en) 2020-11-23
ES2907926T3 (en) 2022-04-27
CN108101851A (en) 2018-06-01
DK3689853T3 (en) 2022-03-07
RU2018128393A3 (en) 2019-04-16
JP6532931B2 (en) 2019-06-19
MX2018014924A (en) 2020-09-02
US20240122936A1 (en) 2024-04-18
WO2014043706A8 (en) 2017-10-19
EP3689853A1 (en) 2020-08-05
BR122021024202B1 (en) 2022-05-17
NZ705827A (en) 2018-07-27
CA3090070C (en) 2023-01-24
KR102138750B1 (en) 2020-07-29
MX364661B (en) 2019-05-03
CA3111317C (en) 2023-08-29
RU2015114327A (en) 2016-11-10

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