RU2668960C2 - Способ синтеза аналогов гормонов щитовидной железы и их полиморфов - Google Patents

Способ синтеза аналогов гормонов щитовидной железы и их полиморфов Download PDF

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RU2668960C2
RU2668960C2 RU2015114327A RU2015114327A RU2668960C2 RU 2668960 C2 RU2668960 C2 RU 2668960C2 RU 2015114327 A RU2015114327 A RU 2015114327A RU 2015114327 A RU2015114327 A RU 2015114327A RU 2668960 C2 RU2668960 C2 RU 2668960C2
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compound
temperature
morphological form
batch
filtered precipitate
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RU2015114327A
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II Д. Кит ХЕСТЕР
Роберт Дж. ДЬЮГИД
Марта КЕЛЛИ
Анна ЧАСНОФФ
Ган ДУН
Эдвин Л. КРОУ
Ребекка ТАУБ
Чарльз Х. РЕЙНОЛДС
Дук Соон ЧОЙ
Ляньхэ ШУ
Пин ВАН
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Мадригал Фармасьютикалз, Инк.
Ф.Хоффманн-Ля Рош Лтд.
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    • A—HUMAN NECESSITIES
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • 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
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    • 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
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    • Y02P20/00—Technologies relating to chemical industry
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    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • 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)
RU2015114327A 2012-09-17 2013-09-17 Способ синтеза аналогов гормонов щитовидной железы и их полиморфов RU2668960C2 (ru)

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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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RU2809040C2 (ru) * 2018-12-13 2023-12-06 Тернс, Инк. АГОНИСТ РЕЦЕПТОРОВ THRβ И СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ
US12338232B2 (en) 2018-12-13 2025-06-24 Terns, Inc. THRβ receptor agonist compound and preparation method and use thereof
US12398127B2 (en) 2019-09-12 2025-08-26 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
US12485118B2 (en) 2023-04-07 2025-12-02 Terns Pharmaceuticals, Inc. Combinations of GLP-1R and THRβ agonists and methods of use thereof
US12528791B2 (en) 2019-08-23 2026-01-20 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds

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CA2884481C (en) * 2012-09-17 2021-04-27 Madrigal Pharmaceuticals, Inc. Method of synthesizing thyroid hormone analogs and polymorphs thereof
CN110167557A (zh) * 2016-10-18 2019-08-23 马德里加尔制药公司 用thr-beta兴奋剂治疗肝脏疾病或脂质疾病的方法
JP7156722B2 (ja) 2018-01-23 2022-10-19 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピリダジノン化合物
PT3807267T (pt) 2018-06-12 2025-05-22 Xizang Haisco Pharmaceutical Co Ltd Agonistas do recetor da hormona da tiroide e usos dos mesmos
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CN114437034A (zh) * 2020-11-06 2022-05-06 深圳微芯生物科技股份有限公司 一种酞嗪类化合物的可药用盐、晶型及其制备方法
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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
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RU2809040C2 (ru) * 2018-12-13 2023-12-06 Тернс, Инк. АГОНИСТ РЕЦЕПТОРОВ THRβ И СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ
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US12365669B2 (en) 2018-12-13 2025-07-22 Terns, Inc. THRβ receptor agonist compound and preparation method and use thereof
US12459926B2 (en) 2018-12-13 2025-11-04 Terns, Inc. THRβ receptor agonist compound and preparation method and use thereof
RU2820475C2 (ru) * 2019-08-21 2024-06-04 Хинова Фармасьютикалс Инк. Галогензамещенное фенилатное соединение и его применения
US12528791B2 (en) 2019-08-23 2026-01-20 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
US12398127B2 (en) 2019-09-12 2025-08-26 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
US12485118B2 (en) 2023-04-07 2025-12-02 Terns Pharmaceuticals, Inc. Combinations of GLP-1R and THRβ agonists and methods of use thereof

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