DK2895466T3 - Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf - Google Patents

Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf Download PDF

Info

Publication number: DK2895466T3
Authority: DK; Denmark
Prior art keywords: thyreoida; polymorphs; synthesis; procedure; hormone analogs
Prior art date: 2012-09-17

Application number

DK13837402.0T

Other languages

English (en)

Inventor

D Keith Hester

Robert J Duguid

Martha Kelly

Gang Dong

Edwin L Crow

Rebecca Taub

Charles H Reynolds

Duk Soon Choi

Lianhe Shu

Ping Wang

Anna Chasnoff

Original Assignee

Madrigal Pharmaceuticals Inc

F Hoffmann La Roche Ltd

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.)

2012-09-17

Filing date

2013-09-17

Publication date

2020-06-08

2013-09-17 Application filed by Madrigal Pharmaceuticals Inc, F Hoffmann La Roche Ltd filed Critical Madrigal Pharmaceuticals Inc

2020-06-08 Application granted granted Critical

2020-06-08 Publication of DK2895466T3 publication Critical patent/DK2895466T3/da

Links

230000015572 biosynthetic process Effects 0.000 title 1
239000003668 hormone analog Substances 0.000 title 1
238000000034 method Methods 0.000 title 1
238000003786 synthesis reaction Methods 0.000 title 1

Classifications

- 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
- 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
- A61K31/495—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
- A61K31/53—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

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)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (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)
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)
Steroid Compounds (AREA)

DK13837402.0T 2012-09-17 2013-09-17 Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf DK2895466T3 (da)

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
DK2895466T3 true DK2895466T3 (da)	2020-06-08

Family

ID=50278769

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
DK13837402.0T DK2895466T3 (da)	2012-09-17	2013-09-17	Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf
DK20157696.4T DK3689853T3 (da)	2012-09-17	2013-09-17	Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
DK20157696.4T DK3689853T3 (da)	2012-09-17	2013-09-17	Fremgangsmåde til syntese af thyreoideahormonanaloger og polymorfer deraf

Country Status (22)

Country	Link
US (8)	US9266861B2 (da)
EP (4)	EP3689853B1 (da)
JP (7)	JP6616688B2 (da)
KR (4)	KR20200023528A (da)
CN (2)	CN105008335B (da)
AR (1)	AR092872A1 (da)
AU (1)	AU2013315017C1 (da)
BR (2)	BR112015005891A2 (da)
CA (3)	CA3111317C (da)
DK (2)	DK2895466T3 (da)
ES (2)	ES2795450T3 (da)
HK (1)	HK1212682A1 (da)
IL (5)	IL237628B (da)
IN (1)	IN2015DN03133A (da)
MX (2)	MX364661B (da)
MY (1)	MY170520A (da)
NZ (2)	NZ705827A (da)
RU (2)	RU2018128393A (da)
SG (3)	SG10201705984XA (da)
TW (4)	TWI681957B (da)
WO (1)	WO2014043706A1 (da)
ZA (1)	ZA201501795B (da)

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BR112015005891A2 (pt)	2012-09-17	2017-08-08	F Hoffmann La Roche Ltd	método de sintetizar análogos do hormônio da tireoide e polimorfos destes
KR20190109387A (ko) *	2016-10-18	2019-09-25	마드리갈 파마슈티칼스, 인크.	Thr-베타 아고니스트로 간 질환 또는 지질 질환을 치료하는 방법
CN111646979B (zh) *	2018-01-23	2021-08-31	深圳市塔吉瑞生物医药有限公司	取代的哒嗪酮化合物
BR112020022146A2 (pt)	2018-06-12	2021-01-26	Fronthera U.S. Pharmaceuticals Llc	compostos da fórmula e composição farmacêutica
US20210292304A1 (en) *	2018-06-22	2021-09-23	Hinova Pharmaceuticals Inc.	Deuterated mgl-3196 compound and use thereof
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
JP2022504706A (ja) *	2018-10-12	2022-01-13	インベンティスバイオカンパニーリミテッド	甲状腺ホルモン受容体作動薬
WO2020169069A1 (en)	2019-02-21	2020-08-27	Nanjing Ruijie Pharma Co., Ltd.	Novel compounds and their uses as thyroid hormone receptor agonists
BR112021021718A2 (pt) *	2019-05-08	2022-01-18	Aligos Therapeutics Inc	Moduladores de thr-ss e métodos de uso dos mesmos
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
WO2021043185A1 (en) *	2019-09-04	2021-03-11	Sunshine Lake Pharma Co., Ltd.	A compound as a thyroid hormone beta receptor agonist and use thereof
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
JP2023503154A (ja) *	2019-11-26	2023-01-26	昆薬集団股▲フン▼有限公司	１，２，４－トリアジン－３，５－ジオン系化合物およびその製造方法と応用
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
WO2021129465A1 (zh) *	2019-12-26	2021-07-01	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
US20230339911A1 (en) *	2020-08-27	2023-10-26	InventisBio Co., Ltd.	Pyridazinone compounds
US20230416234A1 (en) *	2020-09-10	2023-12-28	Crystal Pharmaceutical (Suzhou) Co., Ltd.	Crystal form of resmetirom, preparation method therefor, and use thereof
EP4204419A1 (en)	2020-10-19	2023-07-05	Teva Pharmaceuticals International GmbH	Solid state forms of resmetirom
CA3206392A1 (en)	2021-02-01	2022-08-04	Rebecca Taub	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
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BR112020022146A2 (pt)	2018-06-12	2021-01-26	Fronthera U.S. Pharmaceuticals Llc	compostos da fórmula e composição farmacêutica
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
JP2022504706A (ja)	2018-10-12	2022-01-13	インベンティスバイオカンパニーリミテッド	甲状腺ホルモン受容体作動薬
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2013
- 2013-09-17 BR BR112015005891A patent/BR112015005891A2/pt not_active Application Discontinuation
- 2013-09-17 EP EP20157696.4A patent/EP3689853B1/en active Active
- 2013-09-17 EP EP24173563.8A patent/EP4406594A2/en active Pending
- 2013-09-17 TW TW107137798A patent/TWI681957B/zh active
- 2013-09-17 CA CA3111317A patent/CA3111317C/en active Active
- 2013-09-17 NZ NZ705827A patent/NZ705827A/en unknown
- 2013-09-17 JP JP2015532148A patent/JP6616688B2/ja active Active
- 2013-09-17 EP EP13837402.0A patent/EP2895466B1/en active Active
- 2013-09-17 ES ES13837402T patent/ES2795450T3/es active Active
- 2013-09-17 KR KR1020207005528A patent/KR20200023528A/ko not_active IP Right Cessation
- 2013-09-17 RU RU2018128393A patent/RU2018128393A/ru unknown
- 2013-09-17 BR BR122021024202-0A patent/BR122021024202B1/pt active IP Right Grant
- 2013-09-17 WO PCT/US2013/060177 patent/WO2014043706A1/en active Application Filing
- 2013-09-17 DK DK13837402.0T patent/DK2895466T3/da active
- 2013-09-17 TW TW108132827A patent/TWI755628B/zh active
- 2013-09-17 AU AU2013315017A patent/AU2013315017C1/en active Active
- 2013-09-17 MX MX2015003418A patent/MX364661B/es active IP Right Grant
- 2013-09-17 CN CN201380059943.5A patent/CN105008335B/zh active Active
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- 2013-09-17 MY MYPI2015000591A patent/MY170520A/en unknown
- 2013-09-17 CN CN201810077707.0A patent/CN108101851A/zh active Pending
- 2013-09-17 CA CA3090070A patent/CA3090070C/en active Active
- 2013-09-17 TW TW110117935A patent/TWI804870B/zh active
- 2013-09-17 NZ NZ73964513A patent/NZ739645A/en unknown
- 2013-09-17 IN IN3133DEN2015 patent/IN2015DN03133A/en unknown
- 2013-09-17 SG SG11201501907YA patent/SG11201501907YA/en unknown
- 2013-09-17 SG SG10202006058QA patent/SG10202006058QA/en unknown
- 2013-09-17 KR KR1020187034908A patent/KR102138750B1/ko active IP Right Grant
- 2013-09-17 RU RU2015114327A patent/RU2668960C2/ru active
- 2013-09-17 EP EP21209827.1A patent/EP4023641B1/en active Active
- 2013-09-17 TW TW102133687A patent/TWI652260B/zh active
- 2013-09-17 AR ARP130103332A patent/AR092872A1/es unknown
- 2013-09-17 DK DK20157696.4T patent/DK3689853T3/da active
- 2013-09-17 KR KR1020217019940A patent/KR102363776B1/ko active IP Right Grant
- 2013-09-17 KR KR1020157009807A patent/KR101966490B1/ko active IP Right Grant
- 2013-09-17 CA CA2884481A patent/CA2884481C/en active Active
- 2013-09-17 ES ES20157696T patent/ES2907926T3/es active Active
2015
- 2015-03-09 IL IL237628A patent/IL237628B/en active IP Right Grant
- 2015-03-16 ZA ZA2015/01795A patent/ZA201501795B/en unknown
- 2015-03-17 US US14/660,720 patent/US9266861B2/en active Active
- 2015-03-17 MX MX2018014924A patent/MX2018014924A/es unknown
2016
- 2016-01-18 HK HK16100496.1A patent/HK1212682A1/zh unknown
- 2016-02-17 US US15/046,213 patent/US9968612B2/en active Active
2017
- 2017-12-26 JP JP2017249107A patent/JP6532931B2/ja active Active
2018
- 2018-04-10 US US15/949,389 patent/US10376517B2/en active Active
- 2018-05-27 IL IL259610A patent/IL259610B/en active IP Right Grant
- 2018-11-20 JP JP2018217045A patent/JP6765408B2/ja active Active
2019
- 2019-02-25 IL IL265030A patent/IL265030B/en active IP Right Grant
- 2019-07-01 US US16/458,546 patent/US10894050B2/en active Active
- 2019-08-27 JP JP2019154299A patent/JP6899413B2/ja active Active
2020
- 2020-02-10 JP JP2020020343A patent/JP7038745B2/ja active Active
- 2020-06-15 IL IL275393A patent/IL275393B/en unknown
- 2020-12-11 US US17/118,706 patent/US11564926B2/en active Active
2021
- 2021-11-15 IL IL288133A patent/IL288133A/en unknown
2022
- 2022-03-07 JP JP2022034154A patent/JP7436542B2/ja active Active
- 2022-12-15 US US18/066,677 patent/US20230210856A1/en active Pending
2023
- 2023-12-22 US US18/393,813 patent/US11986481B2/en active Active
- 2023-12-22 US US18/393,818 patent/US20240148742A1/en active Pending
2024
- 2024-02-07 JP JP2024016915A patent/JP2024056793A/ja active Pending

Also Published As

Publication number	Publication date
IL275393B (en)	2022-01-01
KR20200023528A (ko)	2020-03-04
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TWI652260B (zh)	2019-03-01

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