BR112015005891A2 - método de sintetizar análogos do hormônio da tireoide e polimorfos destes - Google Patents

método de sintetizar análogos do hormônio da tireoide e polimorfos destes

Info

Publication number
BR112015005891A2
BR112015005891A2 BR112015005891A BR112015005891A BR112015005891A2 BR 112015005891 A2 BR112015005891 A2 BR 112015005891A2 BR 112015005891 A BR112015005891 A BR 112015005891A BR 112015005891 A BR112015005891 A BR 112015005891A BR 112015005891 A2 BR112015005891 A2 BR 112015005891A2
Authority
BR
Brazil
Prior art keywords
thyroid hormone
polymorphs
synthesizing
compounds
pyridazinone
Prior art date
Application number
BR112015005891A
Other languages
English (en)
Inventor
Chasnoff Anna
H Reynolds Charles
Keith Hester D
Soon Choi Duk
L Crow Edwin
Dong Gang
Shu Lianhe
Kelly Martha
Wang Ping
Taub Rebecca
J Duguid Robert
Original Assignee
F Hoffmann La Roche Ltd
Madrigal Pharmaceuticals Inc
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.)
Filing date
Publication date
Application filed by F Hoffmann La Roche Ltd, Madrigal Pharmaceuticals Inc filed Critical F Hoffmann La Roche Ltd
Priority to BR122021024202-0A priority Critical patent/BR122021024202B1/pt
Publication of BR112015005891A2 publication Critical patent/BR112015005891A2/pt

Links

Classifications

    • 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
    • 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
    • A61K31/53—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

Abstract

resumo “método de sintetizar análogos do hormônio da tireoide e polimorfos destes” a divulgação descreve métodos de síntese de compostos de piridazinona como análogos do hormônio da tireoide e seus pró-medicamentos. métodos preferidos de acordo com a divulgação levam em consideração preparação em grande escala de compostos de piridazinona tendo pureza alta. em algumas formas de realização, métodos preferidos de acordo com a divulgação também levam em consideração a preparação de compostos de piridazinona em melhor rendimento do que métodos previamente usados para preparar tais compostos. também divulgadas são formas mórficas de um composto de piridazinona. ainda divulgado é um método para tratar resistência ao hormônio da tireoide em um indivíduo tendo pelo menos uma mutação de trß.
BR112015005891A 2012-09-17 2013-09-17 método de sintetizar análogos do hormônio da tireoide e polimorfos destes BR112015005891A2 (pt)

Priority Applications (1)

Application Number Priority Date Filing Date Title
BR122021024202-0A BR122021024202B1 (pt) 2012-09-17 2013-09-17 Processo sintético compreendendo compostos de piridazinona bem como os ditos compostos

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
BR112015005891A2 true BR112015005891A2 (pt) 2017-08-08

Family

ID=50278769

Family Applications (2)

Application Number Title Priority Date Filing Date
BR122021024202-0A BR122021024202B1 (pt) 2012-09-17 2013-09-17 Processo sintético compreendendo compostos de piridazinona bem como os ditos compostos
BR112015005891A BR112015005891A2 (pt) 2012-09-17 2013-09-17 método de sintetizar análogos do hormônio da tireoide e polimorfos destes

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BR122021024202-0A BR122021024202B1 (pt) 2012-09-17 2013-09-17 Processo sintético compreendendo compostos de piridazinona bem como os ditos compostos

Country Status (22)

Country Link
US (8) US9266861B2 (pt)
EP (3) EP2895466B1 (pt)
JP (7) JP6616688B2 (pt)
KR (4) KR102138750B1 (pt)
CN (2) CN105008335B (pt)
AR (1) AR092872A1 (pt)
AU (1) AU2013315017C1 (pt)
BR (2) BR122021024202B1 (pt)
CA (3) CA3090070C (pt)
DK (2) DK3689853T3 (pt)
ES (2) ES2907926T3 (pt)
HK (1) HK1212682A1 (pt)
IL (5) IL237628B (pt)
IN (1) IN2015DN03133A (pt)
MX (2) MX364661B (pt)
MY (1) MY170520A (pt)
NZ (2) NZ739645A (pt)
RU (2) RU2668960C2 (pt)
SG (3) SG10202006058QA (pt)
TW (4) TWI804870B (pt)
WO (1) WO2014043706A1 (pt)
ZA (1) ZA201501795B (pt)

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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
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CA3158379A1 (en) * 2019-11-26 2021-06-03 Hejun Lv 1,2,4-triazine-3,5-dione compound, preparation method therefor, and application thereof
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
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CN116847847A (zh) 2021-02-01 2023-10-03 马德里加尔制药公司 用于治疗肝紊乱或血脂紊乱的瑞舒伐他汀和resmetirom的治疗组合
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JP6532931B2 (ja) 2019-06-19
US20210161904A1 (en) 2021-06-03
CA2884481C (en) 2021-04-27
EP4023641A3 (en) 2022-09-14
WO2014043706A8 (en) 2017-10-19
DK2895466T3 (da) 2020-06-08
KR102363776B1 (ko) 2022-02-15
US10894050B2 (en) 2021-01-19
IL275393A (en) 2020-07-30
EP3689853A1 (en) 2020-08-05
CN105008335A (zh) 2015-10-28
JP2018080188A (ja) 2018-05-24
AR092872A1 (es) 2015-05-06
EP3689853B1 (en) 2021-11-24
TW201946917A (zh) 2019-12-16
CA3090070A1 (en) 2014-03-20
US10376517B2 (en) 2019-08-13
KR20150056630A (ko) 2015-05-26
TWI804870B (zh) 2023-06-11
JP2020109090A (ja) 2020-07-16
IL265030B (en) 2020-07-30
TW201425300A (zh) 2014-07-01
IL237628A0 (en) 2015-04-30
JP2022078218A (ja) 2022-05-24
IL288133A (en) 2022-01-01
DK3689853T3 (da) 2022-03-07
ES2907926T3 (es) 2022-04-27
SG11201501907YA (en) 2015-04-29
TWI681957B (zh) 2020-01-11
TW201906835A (zh) 2019-02-16
EP4023641B1 (en) 2024-05-01
JP2019048856A (ja) 2019-03-28
RU2018128393A (ru) 2019-03-14
KR101966490B1 (ko) 2019-08-14
US11564926B2 (en) 2023-01-31
US20190381053A1 (en) 2019-12-19
RU2668960C2 (ru) 2018-10-05
TWI755628B (zh) 2022-02-21
JP6899413B2 (ja) 2021-07-07
RU2018128393A3 (pt) 2019-04-16
HK1212682A1 (zh) 2016-06-17
US20240148742A1 (en) 2024-05-09
CA3111317C (en) 2023-08-29
ZA201501795B (en) 2021-10-27
MX2015003418A (es) 2016-04-04
KR102138750B1 (ko) 2020-07-29
WO2014043706A1 (en) 2014-03-20
MX2018014924A (es) 2020-09-02
IL275393B (en) 2022-01-01
JP2024056793A (ja) 2024-04-23
US9266861B2 (en) 2016-02-23
CA3090070C (en) 2023-01-24
JP2015535817A (ja) 2015-12-17
JP7038745B2 (ja) 2022-03-18
RU2015114327A (ru) 2016-11-10
US20240122936A1 (en) 2024-04-18
JP6616688B2 (ja) 2019-12-04
CN108101851A (zh) 2018-06-01
EP4023641A2 (en) 2022-07-06
AU2013315017A1 (en) 2015-04-02
CA3111317A1 (en) 2014-03-20
JP7436542B2 (ja) 2024-02-21
BR122021024202B1 (pt) 2022-05-17
US20150203473A1 (en) 2015-07-23
CA2884481A1 (en) 2014-03-20
KR20210083381A (ko) 2021-07-06
IL237628B (en) 2019-07-31
SG10202006058QA (en) 2020-08-28
CN105008335B (zh) 2018-12-21
KR20200023528A (ko) 2020-03-04
ES2795450T3 (es) 2020-11-23
TWI652260B (zh) 2019-03-01
IL259610A (en) 2018-07-31
JP2020015739A (ja) 2020-01-30
US20180228807A1 (en) 2018-08-16
TW202134217A (zh) 2021-09-16
JP6765408B2 (ja) 2020-10-07
NZ739645A (en) 2019-11-29
US20230210856A1 (en) 2023-07-06
EP2895466A4 (en) 2016-08-10
MY170520A (en) 2019-08-08
SG10201705984XA (en) 2017-08-30
NZ705827A (en) 2018-07-27
EP2895466A1 (en) 2015-07-22
US9968612B2 (en) 2018-05-15
AU2013315017C1 (en) 2017-11-23
MX364661B (es) 2019-05-03
AU2013315017B2 (en) 2017-07-27
EP2895466B1 (en) 2020-03-25
IL259610B (en) 2020-06-30
IN2015DN03133A (pt) 2015-10-02
US20160243126A1 (en) 2016-08-25
KR20180131647A (ko) 2018-12-10

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