RU2586330C2 - Твердые формы ингибитора диссоциации транстиретина - Google Patents
Твердые формы ингибитора диссоциации транстиретина Download PDFInfo
- Publication number
- RU2586330C2 RU2586330C2 RU2014109676/04A RU2014109676A RU2586330C2 RU 2586330 C2 RU2586330 C2 RU 2586330C2 RU 2014109676/04 A RU2014109676/04 A RU 2014109676/04A RU 2014109676 A RU2014109676 A RU 2014109676A RU 2586330 C2 RU2586330 C2 RU 2586330C2
- Authority
- RU
- Russia
- Prior art keywords
- crystalline form
- compound
- peaks
- solid
- raman
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D263/57—Aryl or substituted aryl radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H5/00—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
- C07H5/04—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to nitrogen
- C07H5/06—Aminosugars
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161535551P | 2011-09-16 | 2011-09-16 | |
| US61/535,551 | 2011-09-16 | ||
| PCT/IB2012/054748 WO2013038351A1 (en) | 2011-09-16 | 2012-09-12 | Solid forms of a transthyretin dissociation inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2014109676A RU2014109676A (ru) | 2015-10-27 |
| RU2586330C2 true RU2586330C2 (ru) | 2016-06-10 |
Family
ID=47116132
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014109676/04A RU2586330C2 (ru) | 2011-09-16 | 2012-09-12 | Твердые формы ингибитора диссоциации транстиретина |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9249112B2 (enExample) |
| EP (1) | EP2755961A1 (enExample) |
| JP (2) | JP5869677B2 (enExample) |
| KR (1) | KR20140054231A (enExample) |
| CN (1) | CN103781770B (enExample) |
| AR (1) | AR088755A1 (enExample) |
| AU (1) | AU2012310157B2 (enExample) |
| BR (1) | BR112014005810A2 (enExample) |
| CA (1) | CA2847293C (enExample) |
| IL (1) | IL231472A0 (enExample) |
| MX (1) | MX2014003043A (enExample) |
| RU (1) | RU2586330C2 (enExample) |
| SG (1) | SG2014013270A (enExample) |
| TW (2) | TWI538909B (enExample) |
| WO (1) | WO2013038351A1 (enExample) |
| ZA (1) | ZA201401202B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2810493C1 (ru) * | 2019-12-20 | 2023-12-27 | Пфайзер Айэленд Фармасьютикалс | Эффективный процесс получения производных 6-карбоксибензоксазола |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06105459B2 (ja) * | 1988-08-11 | 1994-12-21 | 日本電気株式会社 | ベクトル処理装置 |
| RU2586330C2 (ru) * | 2011-09-16 | 2016-06-10 | Пфайзер Инк. | Твердые формы ингибитора диссоциации транстиретина |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| SI4349406T1 (sl) * | 2014-09-08 | 2026-02-27 | Pfizer Inc. | Kristalne trdne oblike 6-karboksi-2-(3,5-diklorofenil)-benzoksazola za uporabo kot zdravilo |
| CN107344927A (zh) * | 2016-05-05 | 2017-11-14 | 苏州晶云药物科技有限公司 | Tafamidis葡甲胺盐的晶型E及其制备方法和用途 |
| GB2571950A (en) * | 2018-03-13 | 2019-09-18 | Azad Pharma Ag | New polymorph and new path to synthesize tafamidis |
| WO2020128816A2 (en) | 2018-12-20 | 2020-06-25 | Pfizer Inc. | Pharmaceutical compositions and methods comprising a combination of a benzoxazole transthyretin stabilizer and an additional therapeutic agent |
| US12116352B2 (en) | 2019-04-11 | 2024-10-15 | Inke, S.A. | Process for preparing 1-deoxy-1-methylamino-d-glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate |
| US12391656B2 (en) | 2019-05-16 | 2025-08-19 | Assia Chemical Industries Ltd. | Solid state forms of Tafamidis and salts thereof |
| US20220241247A1 (en) * | 2019-05-31 | 2022-08-04 | Plex Pharmaceuticals, Inc. | Pharmacological agents for treating protein aggregation diseases of the eye |
| WO2021019448A1 (en) * | 2019-08-01 | 2021-02-04 | Honour (R&D) | Process for the preparation of transthyretin dissociation inhibitor |
| JP2023503833A (ja) | 2019-11-15 | 2023-02-01 | ▲蘇▼州科睿思制▲葯▼有限公司 | タファミジスの結晶形及びその調製方法及びその使用 |
| EP4077287B1 (en) * | 2019-12-20 | 2025-11-19 | Pfizer Ireland Pharmaceuticals Unlimited Company | Efficient process for making 6-carboxy benzoxazole derivatives |
| WO2021232619A1 (zh) * | 2020-05-19 | 2021-11-25 | 苏州科睿思制药有限公司 | 一种他发米帝司游离酸的晶型及其制备方法和用途 |
| US20230265059A1 (en) * | 2020-07-04 | 2023-08-24 | Nuray Chemicals Private Limited | Solid state forms of 6-carboxy-2-(3, 5-dichlorophenyl)-benzoxazole of formula-i and pharmaceutically acceptable salts thereof |
| FR3114230B1 (fr) | 2020-09-23 | 2022-12-23 | Pierre Berger | Dispositif de connexion entre une toile et un rail |
| EP4228629A4 (en) * | 2020-10-19 | 2024-12-25 | Glenmark Life Sciences Limited | PROCESS FOR PREPARING TAFAMIDIS AND SALTS THEREOF |
| WO2022112919A1 (en) | 2020-11-25 | 2022-06-02 | Pfizer Inc. | (aza)benzothiazolyl substituted pyrazole compounds |
| EP4083027A1 (en) | 2021-04-26 | 2022-11-02 | Química Sintética, S.A. | A solid state form of tafamidis and a process for its preparation |
| WO2023020762A1 (en) | 2021-08-16 | 2023-02-23 | Synthon B.V. | Crystalline forms of tafamidis nicotinamide adduct |
| WO2023091534A1 (en) | 2021-11-17 | 2023-05-25 | Teva Pharmaceuticals International Gmbh | Solid state form of tafamidis |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU608476A3 (ru) * | 1973-10-23 | 1978-05-25 | Лилли Индастриз Лимитед, (Фирма) | Способ получени 5-или-6замещенных бензоксазолкарбоновых кислот |
| US7214695B2 (en) * | 2002-12-19 | 2007-05-08 | The Scripps Research Institute | Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding |
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| US3551433A (en) | 1967-06-21 | 1970-12-29 | Us Army | Preparation of 4-phenyl-4-acyloxypiperidine |
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| RU2586330C2 (ru) * | 2011-09-16 | 2016-06-10 | Пфайзер Инк. | Твердые формы ингибитора диссоциации транстиретина |
| WO2013166041A1 (en) | 2012-05-01 | 2013-11-07 | The Trustees Of Columbia University In The City Of New York | Transthyretin ligands capable of inhibiting retinol-dependent rbp4-ttr interaction for treatment of age-related macular |
| WO2013168014A1 (en) | 2012-05-10 | 2013-11-14 | Mahesh Kandula | Compositions and methods for the treatment of familial amyloid polyneuropathy |
-
2012
- 2012-09-12 RU RU2014109676/04A patent/RU2586330C2/ru not_active Application Discontinuation
- 2012-09-12 EP EP12780287.4A patent/EP2755961A1/en not_active Withdrawn
- 2012-09-12 AU AU2012310157A patent/AU2012310157B2/en active Active
- 2012-09-12 SG SG2014013270A patent/SG2014013270A/en unknown
- 2012-09-12 US US14/345,111 patent/US9249112B2/en not_active Expired - Fee Related
- 2012-09-12 KR KR1020147006603A patent/KR20140054231A/ko not_active Ceased
- 2012-09-12 CA CA2847293A patent/CA2847293C/en not_active Expired - Fee Related
- 2012-09-12 CN CN201280043084.6A patent/CN103781770B/zh not_active Expired - Fee Related
- 2012-09-12 BR BR112014005810A patent/BR112014005810A2/pt active Search and Examination
- 2012-09-12 JP JP2014530354A patent/JP5869677B2/ja not_active Expired - Fee Related
- 2012-09-12 MX MX2014003043A patent/MX2014003043A/es unknown
- 2012-09-12 WO PCT/IB2012/054748 patent/WO2013038351A1/en not_active Ceased
- 2012-09-14 TW TW104101710A patent/TWI538909B/zh not_active IP Right Cessation
- 2012-09-14 AR ARP120103410A patent/AR088755A1/es unknown
- 2012-09-14 TW TW101133893A patent/TWI476185B/zh not_active IP Right Cessation
-
2014
- 2014-02-18 ZA ZA2014/01202A patent/ZA201401202B/en unknown
- 2014-03-12 IL IL231472A patent/IL231472A0/en unknown
-
2015
- 2015-12-22 US US14/979,021 patent/US20160185739A1/en not_active Abandoned
-
2016
- 2016-01-07 JP JP2016001888A patent/JP2016128444A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU608476A3 (ru) * | 1973-10-23 | 1978-05-25 | Лилли Индастриз Лимитед, (Фирма) | Способ получени 5-или-6замещенных бензоксазолкарбоновых кислот |
| US7214695B2 (en) * | 2002-12-19 | 2007-05-08 | The Scripps Research Institute | Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding |
Non-Patent Citations (2)
| Title |
|---|
| CAIRA M. R., "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY, SPRINGER, 1998, vol.198, p.163-208. HARWOOD L. M. et al., "Experimental organic chemistry - Principles and practice", EXPERIMENTAL CHEMISTRY - ORGANIC CHEMISTRY AND REACTION, 1989, p.127-132. ANDERSON N. G. et al., "TOOLS FOR PURIFYING THE PRODUCT: COLUMN CHROMATOGRAPHY, CRYSTALLIZATION AND RESLURRYING", PRACTICAL PROCESS RESEARCH AND DEVELOPMENT, 2000, p.223-247. BYRN S. et al., "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", Pharmaceutical Research, 1995, vol.12, no.7, p.945-954. * |
| MARK RATNER, "Spotlight focuses on protein-misfolding therapies", NATURE BIOTECHNOLOGY, 2009, vol. 27, no. 10, p. 874. S. E. KOLSTOE et al., "Trapping of palindromic ligands within native transthyretin prevents amyloid formation", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, 2010, vol. 107, no. 47, p. 20483-20488. * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2810493C1 (ru) * | 2019-12-20 | 2023-12-27 | Пфайзер Айэленд Фармасьютикалс | Эффективный процесс получения производных 6-карбоксибензоксазола |
Also Published As
| Publication number | Publication date |
|---|---|
| TW201516039A (zh) | 2015-05-01 |
| US20150031735A1 (en) | 2015-01-29 |
| CA2847293C (en) | 2017-03-28 |
| BR112014005810A2 (pt) | 2017-03-28 |
| IL231472A0 (en) | 2014-04-30 |
| TW201315720A (zh) | 2013-04-16 |
| TWI476185B (zh) | 2015-03-11 |
| CN103781770A (zh) | 2014-05-07 |
| SG2014013270A (en) | 2014-05-29 |
| CA2847293A1 (en) | 2013-03-21 |
| HK1197239A1 (zh) | 2015-01-09 |
| CN103781770B (zh) | 2016-04-13 |
| NZ621194A (en) | 2016-02-26 |
| ZA201401202B (en) | 2016-01-27 |
| AU2012310157A1 (en) | 2014-04-03 |
| RU2014109676A (ru) | 2015-10-27 |
| JP5869677B2 (ja) | 2016-02-24 |
| EP2755961A1 (en) | 2014-07-23 |
| US9249112B2 (en) | 2016-02-02 |
| AR088755A1 (es) | 2014-07-02 |
| JP2016128444A (ja) | 2016-07-14 |
| JP2014526498A (ja) | 2014-10-06 |
| US20160185739A1 (en) | 2016-06-30 |
| WO2013038351A1 (en) | 2013-03-21 |
| AU2012310157B2 (en) | 2015-11-12 |
| TWI538909B (zh) | 2016-06-21 |
| KR20140054231A (ko) | 2014-05-08 |
| MX2014003043A (es) | 2015-02-05 |
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