MX2018014924A - Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos. - Google Patents
Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos.Info
- Publication number
- MX2018014924A MX2018014924A MX2018014924A MX2018014924A MX2018014924A MX 2018014924 A MX2018014924 A MX 2018014924A MX 2018014924 A MX2018014924 A MX 2018014924A MX 2018014924 A MX2018014924 A MX 2018014924A MX 2018014924 A MX2018014924 A MX 2018014924A
- Authority
- MX
- Mexico
- Prior art keywords
- thyroid hormone
- compounds
- hormone analogs
- polymorphs
- pyridazinone
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 6
- AUYYCJSJGJYCDS-LBPRGKRZSA-N Thyrolar Chemical class IC1=CC(C[C@H](N)C(O)=O)=CC(I)=C1OC1=CC=C(O)C(I)=C1 AUYYCJSJGJYCDS-LBPRGKRZSA-N 0.000 title abstract 3
- 230000002194 synthesizing effect Effects 0.000 title 1
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 abstract 3
- 238000002360 preparation method Methods 0.000 abstract 2
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- -1 pyridazinone compound Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 239000005495 thyroid hormone Substances 0.000 abstract 1
- 229940036555 thyroid hormone Drugs 0.000 abstract 1
Classifications
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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
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- 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
Landscapes
- 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)
- 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)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente invención se refiere a los métodos de síntesis de los compuestos de piridazinona como análogos de hormona tiroidea y sus profármacos. Los métodos preferidos de acuerdo con la divulgación permiten la preparación a gran escala de los compuestos de piridazinona que tienen pureza elevada. En algunas modalidades, los métodos preferidos de acuerdo con la divulgación también permiten la preparación de los compuestos de piridazinona en mejor rendimiento que los métodos previamente usados para preparar tales compuestos. También se divulgan las formas morfonucleares de un compuesto de piridazinona. Además se divulga un método para tratar la resistencia a la hormona tiroidea en un sujeto que tiene por lo menos una mutación de TRP.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702137P | 2012-09-17 | 2012-09-17 | |
| US201361790432P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2018014924A true MX2018014924A (es) | 2020-09-02 |
Family
ID=50278769
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015003418A MX364661B (es) | 2012-09-17 | 2013-09-17 | Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos. |
| MX2018014924A MX2018014924A (es) | 2012-09-17 | 2015-03-17 | Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015003418A MX364661B (es) | 2012-09-17 | 2013-09-17 | Metodo para sintetizar los analogos de hormona tiroidea y leucocitos polimorfonucleares de los mismos. |
Country Status (22)
| Country | Link |
|---|---|
| US (8) | US9266861B2 (es) |
| EP (4) | EP3689853B1 (es) |
| JP (7) | JP6616688B2 (es) |
| KR (4) | KR102363776B1 (es) |
| CN (2) | CN105008335B (es) |
| AR (1) | AR092872A1 (es) |
| AU (1) | AU2013315017C1 (es) |
| BR (2) | BR122021024202B1 (es) |
| CA (3) | CA2884481C (es) |
| DK (2) | DK3689853T3 (es) |
| ES (2) | ES2795450T3 (es) |
| HK (1) | HK1212682A1 (es) |
| IL (6) | IL288133B2 (es) |
| IN (1) | IN2015DN03133A (es) |
| MX (2) | MX364661B (es) |
| MY (1) | MY170520A (es) |
| NZ (2) | NZ739645A (es) |
| RU (2) | RU2018128393A (es) |
| SG (3) | SG10201705984XA (es) |
| TW (4) | TWI755628B (es) |
| WO (1) | WO2014043706A1 (es) |
| ZA (1) | ZA201501795B (es) |
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| SG10201705984XA (en) | 2012-09-17 | 2017-08-30 | Madrigal Pharmaceuticals Inc | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| JP2019533019A (ja) * | 2016-10-18 | 2019-11-14 | マドリガル ファーマシューティカルズ インコーポレイテッドＭａｄｒｉｇａｌ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | Ｔｈｒ−ベータアゴニストで肝臓障害又は脂質障害を治療する方法 |
| WO2019144835A1 (zh) * | 2018-01-23 | 2019-08-01 | 深圳市塔吉瑞生物医药有限公司 | 取代的哒嗪酮化合物 |
| JP7181386B2 (ja) * | 2018-06-12 | 2022-11-30 | スーチョワン ハイスコ ファーマスーティカル カンパニー リミテッド | 甲状腺ホルモン受容体アゴニスト及びその用途 |
| CN110627773B (zh) * | 2018-06-22 | 2021-03-19 | 海创药业股份有限公司 | 氘代mgl-3196化合物及其用途 |
| 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 |
| CN119552152A (zh) * | 2018-10-12 | 2025-03-04 | 益方生物科技(上海)股份有限公司 | 甲状腺激素受体激动剂 |
| CN113474335B (zh) * | 2019-02-21 | 2024-12-03 | 南京瑞捷医药科技有限公司 | 化合物及其作为甲状腺激素受体激动剂的用途 |
| WO2020227549A1 (en) * | 2019-05-08 | 2020-11-12 | Aligos Therapeutics, Inc. | MODULATORS OF THR-β AND METHODS OF USE THEREOF |
| TW202108556A (zh) * | 2019-05-10 | 2021-03-01 | 大陸商深圳微芯生物科技股份有限公司 | 一種噠嗪酮衍生物及其應用 |
| WO2020239076A1 (zh) * | 2019-05-29 | 2020-12-03 | 南京明德新药研发有限公司 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
| CN112442013B (zh) * | 2019-09-04 | 2022-07-26 | 广东东阳光药业有限公司 | 一种作为甲状腺激素β受体激动剂的化合物及其用途 |
| WO2021063367A1 (zh) * | 2019-09-30 | 2021-04-08 | 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 |
| CN112707892A (zh) * | 2019-10-24 | 2021-04-27 | 苏州泽璟生物制药股份有限公司 | 哒嗪酮或哒嗪类化合物及其衍生物和药物组合物 |
| CN113454069B (zh) * | 2019-11-26 | 2025-03-14 | 昆药集团股份有限公司 | 1，2，4-三嗪-3，5-二酮类化合物及其制备方法和应用 |
| 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 |
| CN114787153A (zh) * | 2019-12-26 | 2022-07-22 | 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 |
| CN116056709A (zh) * | 2020-08-27 | 2023-05-02 | 益方生物科技(上海)股份有限公司 | 哒嗪酮化合物 |
| CN116171275A (zh) * | 2020-09-10 | 2023-05-26 | 苏州科睿思制药有限公司 | Resmetirom的晶型及其制备方法和用途 |
| US20230364099A1 (en) | 2020-10-19 | 2023-11-16 | Teva Pharmaceuticals International Gmbh | Solid state forms of resmetirom |
| US20240307405A1 (en) | 2021-02-01 | 2024-09-19 | Madrigal Pharmaceuticals, Inc. | Therapeutic combinations of rosuvastatin and resmetirom for the treatment of liver disorders or lipid disorders |
| 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 |
| AR127165A1 (es) | 2021-09-27 | 2023-12-27 | Madrigal Pharmaceuticals Inc | Resmetirom para reducir el volumen del hígado |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| WO2024263714A1 (en) | 2023-06-22 | 2024-12-26 | Madrigal Pharmaceuticals, Inc. | BIOMARKERS FOR TREATING LIVER DISORDERS WITH THR-β AGONISTS AND RELATED USES |
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| RS51639B (en) * | 2005-07-21 | 2011-10-31 | F.Hoffmann-La Roche Ag. | Pyridazinone Derivatives As Receptors of Thyroid Hormone Receptors |
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| US8858502B2 (en) | 2012-10-10 | 2014-10-14 | Alcon Research, Ltd. | Systems and methods for external pressure sensing |
| WO2015123256A1 (en) | 2014-02-14 | 2015-08-20 | Cempra Pharmaceuticals, Inc. | Compositions and methods for treating diabetes and liver diseases |
| JP2019533019A (ja) | 2016-10-18 | 2019-11-14 | マドリガル ファーマシューティカルズ インコーポレイテッドＭａｄｒｉｇａｌ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | Ｔｈｒ−ベータアゴニストで肝臓障害又は脂質障害を治療する方法 |
| JP7181386B2 (ja) | 2018-06-12 | 2022-11-30 | スーチョワン ハイスコ ファーマスーティカル カンパニー リミテッド | 甲状腺ホルモン受容体アゴニスト及びその用途 |
| 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 |
| CN119552152A (zh) | 2018-10-12 | 2025-03-04 | 益方生物科技(上海)股份有限公司 | 甲状腺激素受体激动剂 |
| CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
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2013
- 2013-09-17 SG SG10201705984XA patent/SG10201705984XA/en unknown
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