JP6616688B2 - 甲状腺ホルモンアナログ及びその多形体の合成方法 - Google Patents

甲状腺ホルモンアナログ及びその多形体の合成方法 Download PDF

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JP6616688B2
JP6616688B2 JP2015532148A JP2015532148A JP6616688B2 JP 6616688 B2 JP6616688 B2 JP 6616688B2 JP 2015532148 A JP2015532148 A JP 2015532148A JP 2015532148 A JP2015532148 A JP 2015532148A JP 6616688 B2 JP6616688 B2 JP 6616688B2
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formula
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JP2015535817A (ja
JP2015535817A5 (Direct
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ヘスター，ディー・キース
ダギッド，ロバート・ジェイ
ケリー，マーサ
シャスノフ，アンナ
ドン，ガン
クロウ，エドウィン・エル
タウブ，レベッカ
レイノルズ，チャールズ・エイチ
チェ，ドク・スン
シュウ，リエンホー
ワン，ピン
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F Hoffmann La Roche AG
Madrigal Pharmaceuticals Inc
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F Hoffmann La Roche AG
Madrigal Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic 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
    • C07D237/10—Heterocyclic 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
    • C07D237/14—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic 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
    • C07D237/10—Heterocyclic 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
    • C07D237/14—Oxygen atoms
    • C07D237/16—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
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  • 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)
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  • 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)
  • Medicinal Preparation (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)
JP2015532148A 2012-09-17 2013-09-17 甲状腺ホルモンアナログ及びその多形体の合成方法 Active JP6616688B2 (ja)

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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
PCT/US2013/060177 WO2014043706A1 (en) 2012-09-17 2013-09-17 Method of synthesizing thyroid hormone analogs and polymorphs thereof

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JP2019154299A Division JP6899413B2 (ja) 2012-09-17 2019-08-27 甲状腺ホルモンアナログ及びその多形体の合成方法

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JP2015535817A JP2015535817A (ja) 2015-12-17
JP2015535817A5 JP2015535817A5 (Direct) 2016-11-04
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JP2017249107A Active JP6532931B2 (ja) 2012-09-17 2017-12-26 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2018217045A Active JP6765408B2 (ja) 2012-09-17 2018-11-20 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2019154299A Active JP6899413B2 (ja) 2012-09-17 2019-08-27 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2020020343A Active JP7038745B2 (ja) 2012-09-17 2020-02-10 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2022034154A Active JP7436542B2 (ja) 2012-09-17 2022-03-07 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2024016915A Pending JP2024056793A (ja) 2012-09-17 2024-02-07 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2025145966A Pending JP2025179154A (ja) 2012-09-17 2025-09-03 甲状腺ホルモンアナログ及びその多形体の合成方法

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JP2018217045A Active JP6765408B2 (ja) 2012-09-17 2018-11-20 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2019154299A Active JP6899413B2 (ja) 2012-09-17 2019-08-27 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2020020343A Active JP7038745B2 (ja) 2012-09-17 2020-02-10 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2022034154A Active JP7436542B2 (ja) 2012-09-17 2022-03-07 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2024016915A Pending JP2024056793A (ja) 2012-09-17 2024-02-07 甲状腺ホルモンアナログ及びその多形体の合成方法
JP2025145966A Pending JP2025179154A (ja) 2012-09-17 2025-09-03 甲状腺ホルモンアナログ及びその多形体の合成方法

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US (8) US9266861B2 (Direct)
EP (4) EP4023641B1 (Direct)
JP (8) JP6616688B2 (Direct)
KR (4) KR20200023528A (Direct)
CN (2) CN108101851A (Direct)
AR (1) AR092872A1 (Direct)
AU (1) AU2013315017C1 (Direct)
BR (2) BR112015005891A2 (Direct)
CA (3) CA3090070C (Direct)
DK (3) DK4406594T3 (Direct)
ES (2) ES2795450T3 (Direct)
FI (1) FI4406594T3 (Direct)
IL (7) IL320269A (Direct)
IN (1) IN2015DN03133A (Direct)
LT (1) LT4406594T (Direct)
MX (2) MX395148B (Direct)
MY (1) MY170520A (Direct)
NZ (2) NZ739645A (Direct)
PT (1) PT4406594T (Direct)
RU (2) RU2668960C2 (Direct)
SG (3) SG10202006058QA (Direct)
TW (4) TWI755628B (Direct)
WO (1) WO2014043706A1 (Direct)
ZA (1) ZA201501795B (Direct)

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JP2020109090A (ja) * 2012-09-17 2020-07-16 マドリガル・ファーマシューティカルズ・インコーポレーテッドＭａｄｒｉｇａｌ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 甲状腺ホルモンアナログ及びその多形体の合成方法

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