TWI652260B - 用以合成甲狀腺激素類似物及其多形體之方法 - Google Patents

用以合成甲狀腺激素類似物及其多形體之方法 Download PDF

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TWI652260B
TWI652260B TW102133687A TW102133687A TWI652260B TW I652260 B TWI652260 B TW I652260B TW 102133687 A TW102133687 A TW 102133687A TW 102133687 A TW102133687 A TW 102133687A TW I652260 B TWI652260 B TW I652260B
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compound
formula
acid
item
batch
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TW102133687A
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TW201425300A (zh
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迪 海斯特二世
Ii D. Keith Hester
羅伯特 杜蓋德
Robert J. Duguid
瑪沙 凱利
Martha J. Kelly
安娜 加斯諾夫
Anna CHASNOFF
董剛
Gang Dong
愛德恩 克羅
Edwin L. Crow
雷貝卡 塔伯
Rebecca Taub
查理斯 雷諾
Charles H. Reynolds
崔德舜
Duk Soon Choi
聯合 舒
Lianhe Shu
王平
Ping Wang
Original Assignee
美商瑪德瑞高製藥公司
Madrigal Pharmaceuticals, Inc.
瑞士商赫夫曼羅氏股份有限公司
F. Hoffmann-La Roche Ltd
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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
    • A61K31/53Heterocyclic 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
    • 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
    • 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)
  • 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)
  • Medicinal Preparation (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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
TW102133687A 2012-09-17 2013-09-17 用以合成甲狀腺激素類似物及其多形體之方法 TWI652260B (zh)

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US201261702137P 2012-09-17 2012-09-17
US61/702,137 2012-09-17
US201361790432P 2013-03-15 2013-03-15
US61/790,432 2013-03-15

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TWI652260B true TWI652260B (zh) 2019-03-01

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TW110117935A TWI804870B (zh) 2012-09-17 2013-09-17 用以合成甲狀腺激素類似物及其多形體之方法
TW102133687A TWI652260B (zh) 2012-09-17 2013-09-17 用以合成甲狀腺激素類似物及其多形體之方法
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CN (2) CN108101851A (enExample)
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TW (4) TWI681957B (enExample)
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IL288133A (en) 2022-01-01
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JP2020109090A (ja) 2020-07-16
RU2015114327A (ru) 2016-11-10
FI4406594T3 (fi) 2025-11-26
JP2025179154A (ja) 2025-12-09
JP2024056793A (ja) 2024-04-23
EP2895466A4 (en) 2016-08-10
US9968612B2 (en) 2018-05-15
CN105008335A (zh) 2015-10-28
US20210161904A1 (en) 2021-06-03
US20150203473A1 (en) 2015-07-23
TW201906835A (zh) 2019-02-16
JP7038745B2 (ja) 2022-03-18
EP4406594A2 (en) 2024-07-31
IL275393B (en) 2022-01-01
IL259610B (en) 2020-06-30
US20240122936A1 (en) 2024-04-18
US10894050B2 (en) 2021-01-19
US20190381053A1 (en) 2019-12-19
RU2668960C2 (ru) 2018-10-05
IN2015DN03133A (enExample) 2015-10-02
JP2022078218A (ja) 2022-05-24
IL314360B1 (en) 2025-05-01
TWI804870B (zh) 2023-06-11
IL288133B1 (en) 2024-08-01
EP4023641B1 (en) 2024-05-01
CA3111317A1 (en) 2014-03-20
US20180228807A1 (en) 2018-08-16
IL288133B2 (en) 2024-12-01
NZ705827A (en) 2018-07-27
EP2895466A1 (en) 2015-07-22
SG11201501907YA (en) 2015-04-29
CA3111317C (en) 2023-08-29
JP7436542B2 (ja) 2024-02-21
IL314360A (en) 2024-09-01
EP4406594B1 (en) 2025-09-10
EP4023641A3 (en) 2022-09-14
JP6616688B2 (ja) 2019-12-04
JP2018080188A (ja) 2018-05-24
CN105008335B (zh) 2018-12-21
JP2015535817A (ja) 2015-12-17
NZ739645A (en) 2019-11-29
KR102138750B1 (ko) 2020-07-29
EP4023641A2 (en) 2022-07-06
US11986481B2 (en) 2024-05-21
MY170520A (en) 2019-08-08
KR20180131647A (ko) 2018-12-10
TW201946917A (zh) 2019-12-16
IL320269A (en) 2025-06-01
AU2013315017A1 (en) 2015-04-02
IL265030B (en) 2020-07-30
SG10201705984XA (en) 2017-08-30
IL237628A0 (en) 2015-04-30
IL275393A (en) 2020-07-30
BR112015005891A2 (pt) 2017-08-08
US11564926B2 (en) 2023-01-31
KR102363776B1 (ko) 2022-02-15
WO2014043706A8 (en) 2017-10-19
DK3689853T3 (da) 2022-03-07
US20230210856A1 (en) 2023-07-06
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BR122021024202B1 (pt) 2022-05-17
JP2020015739A (ja) 2020-01-30
CN108101851A (zh) 2018-06-01
MX2018014924A (es) 2020-09-02
CA3090070A1 (en) 2014-03-20
US9266861B2 (en) 2016-02-23
EP3689853B1 (en) 2021-11-24
JP2019048856A (ja) 2019-03-28
SG10202006058QA (en) 2020-08-28
CA2884481C (en) 2021-04-27
KR20210083381A (ko) 2021-07-06
ES2795450T3 (es) 2020-11-23
MX2015003418A (es) 2016-04-04
HK1212682A1 (en) 2016-06-17
IL237628B (en) 2019-07-31
CA3090070C (en) 2023-01-24
EP4406594A3 (en) 2024-11-06
DK2895466T3 (da) 2020-06-08
ES2907926T3 (es) 2022-04-27
JP6765408B2 (ja) 2020-10-07
MX364661B (es) 2019-05-03
KR20150056630A (ko) 2015-05-26
KR101966490B1 (ko) 2019-08-14
IL314360B2 (en) 2025-09-01
TW202134217A (zh) 2021-09-16
TWI681957B (zh) 2020-01-11
AU2013315017C1 (en) 2017-11-23
EP3689853A1 (en) 2020-08-05
CA2884481A1 (en) 2014-03-20
TWI755628B (zh) 2022-02-21
US20160243126A1 (en) 2016-08-25
MX395148B (es) 2025-03-24
AR092872A1 (es) 2015-05-06
EP2895466B1 (en) 2020-03-25
US10376517B2 (en) 2019-08-13
WO2014043706A1 (en) 2014-03-20
RU2018128393A (ru) 2019-03-14
JP6532931B2 (ja) 2019-06-19
JP6899413B2 (ja) 2021-07-07
US20240148742A1 (en) 2024-05-09
ZA201501795B (en) 2021-10-27
RU2018128393A3 (enExample) 2019-04-16
IL259610A (en) 2018-07-31

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