JP2014526498A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014526498A5 JP2014526498A5 JP2014530354A JP2014530354A JP2014526498A5 JP 2014526498 A5 JP2014526498 A5 JP 2014526498A5 JP 2014530354 A JP2014530354 A JP 2014530354A JP 2014530354 A JP2014530354 A JP 2014530354A JP 2014526498 A5 JP2014526498 A5 JP 2014526498A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline form
- dichlorophenyl
- carboxy
- benzoxazole meglumine
- crystal
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 9
- 229960003194 meglumine Drugs 0.000 claims 9
- TXEIIPDJKFWEEC-UHFFFAOYSA-N tafamidis Chemical compound O1C2=CC(C(=O)O)=CC=C2N=C1C1=CC(Cl)=CC(Cl)=C1 TXEIIPDJKFWEEC-UHFFFAOYSA-N 0.000 claims 9
- 239000013078 crystal Substances 0.000 claims 8
- 238000001069 Raman spectroscopy Methods 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 claims 3
- 238000001228 spectrum Methods 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 108010071690 Prealbumin Proteins 0.000 claims 1
- 238000001237 Raman spectrum Methods 0.000 claims 1
- 102000009190 Transthyretin Human genes 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 238000002329 infrared spectrum Methods 0.000 claims 1
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016001888A Division JP2016128444A (ja) | 2011-09-16 | 2016-01-07 | トランスサイレチン解離阻害剤の固体形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014526498A JP2014526498A (ja) | 2014-10-06 |
| JP2014526498A5 true JP2014526498A5 (https=) | 2015-07-30 |
| JP5869677B2 JP5869677B2 (ja) | 2016-02-24 |
Family
ID=47116132
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014530354A Expired - Fee Related JP5869677B2 (ja) | 2011-09-16 | 2012-09-12 | トランスサイレチン解離阻害剤の固体形態 |
| JP2016001888A Pending JP2016128444A (ja) | 2011-09-16 | 2016-01-07 | トランスサイレチン解離阻害剤の固体形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016001888A Pending JP2016128444A (ja) | 2011-09-16 | 2016-01-07 | トランスサイレチン解離阻害剤の固体形態 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9249112B2 (https=) |
| EP (1) | EP2755961A1 (https=) |
| JP (2) | JP5869677B2 (https=) |
| KR (1) | KR20140054231A (https=) |
| CN (1) | CN103781770B (https=) |
| AR (1) | AR088755A1 (https=) |
| AU (1) | AU2012310157B2 (https=) |
| BR (1) | BR112014005810A2 (https=) |
| CA (1) | CA2847293C (https=) |
| IL (1) | IL231472A0 (https=) |
| MX (1) | MX2014003043A (https=) |
| RU (1) | RU2586330C2 (https=) |
| SG (1) | SG2014013270A (https=) |
| TW (2) | TWI476185B (https=) |
| WO (1) | WO2013038351A1 (https=) |
| ZA (1) | ZA201401202B (https=) |
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 |
| SI3977993T1 (sl) | 2014-09-08 | 2024-05-31 | 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 |
| ES2991081T3 (es) * | 2019-04-11 | 2024-12-02 | Inke Sa | Procedimiento para preparar 2-(3,5-diclorofenil)-6-benzoxazolcarboxilato de 1-desoxi-1-metilamino-D-glucitol |
| EP3969443B1 (en) | 2019-05-16 | 2024-11-20 | Teva Pharmaceuticals International GmbH | Solid state forms of tafamidis and salts thereof |
| EP3976017A4 (en) * | 2019-05-31 | 2023-06-14 | Plex Pharmaceuticals, Inc. | PHARMACOLOGICAL SUBSTANCES FOR THE TREATMENT OF 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 |
| MX2022007787A (es) * | 2019-12-20 | 2022-07-19 | Pfizer Ireland Pharmaceuticals | Proceso eficiente para elaborar derivados de 6-carboxi-benzoxazol. |
| 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 |
| WO2022009221A1 (en) * | 2020-07-04 | 2022-01-13 | 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 |
| WO2022084790A1 (en) * | 2020-10-19 | 2022-04-28 | Glenmark Life Sciences Limited | Process for preparation of 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 |
| US20250042864A1 (en) | 2021-11-17 | 2025-02-06 | Teva Pharmaceuticals International Gmbh | Solid state form of tafamidis |
Family Cites Families (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602336C (de) | 1933-03-09 | 1934-09-06 | I G Farbenindustrie Akt Ges | Verfahren zur Herstellung von Kuepenfarbstoffen der Anthrachinonreihe |
| US3551433A (en) | 1967-06-21 | 1970-12-29 | Us Army | Preparation of 4-phenyl-4-acyloxypiperidine |
| US3551443A (en) | 1968-10-30 | 1970-12-29 | Ciba Ltd | 2-phenylbenzoxazole derivatives |
| USRE29608E (en) | 1972-05-18 | 1978-04-11 | Lilly Industries Limited | Benzoxazole derivatives |
| DE2314238A1 (de) | 1973-03-22 | 1974-09-26 | Henkel & Cie Gmbh | Neue 2-(tetrazol-5'-yl)-benzoxazole, deren herstellung sowie verwendung als entzuendungshemmer in kosmetischen praeparationen |
| US4025636A (en) | 1973-10-23 | 1977-05-24 | Lilly Industries, Ltd. | 2-(Optionally substituted)phenyl-5 or 6-substituted benzoxazoles |
| GB1488003A (en) * | 1973-10-23 | 1977-10-05 | Lilly Industries Ltd | 1,2-benzisoxazole derivatives processes for their preparation and their use as pharmaceuticals |
| US4025637A (en) | 1973-10-23 | 1977-05-24 | Lilly Industries, Ltd. | 2,5 OR 2,6 Disubstituted benzoxazoles |
| DE2619547A1 (de) | 1976-05-04 | 1977-11-24 | Dynamit Nobel Ag | Verfahren zur herstellung von 2-aryl- benzoxazolen und 2-aryl-benzthiazolen |
| US4416892A (en) | 1981-04-23 | 1983-11-22 | Lilly Industries Limited | Method of treating hypersensitivity disease with benzoxazole derivatives |
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| DE4011106A1 (de) | 1990-04-06 | 1991-10-10 | Bayer Ag | Neue heterocyclisch substituierte dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
| US5254692A (en) | 1990-04-06 | 1993-10-19 | Bayer Aktiengesellschaft | 2,6-dialkyl-4-(benzothiazol- or benzoxazol-7-yl)-1,4-dihydropyridines |
| US5037842A (en) | 1990-06-05 | 1991-08-06 | Pfizer Inc. | Oxa- and thiazolidinedione hypoglycemic and hypocholesterolemic agents |
| CA2051518A1 (en) | 1990-10-01 | 1992-04-02 | Robert J. Perry | Synthesis of heterocyclic compounds |
| CH681806A5 (https=) | 1991-03-19 | 1993-05-28 | Ciba Geigy Ag | |
| US5354759A (en) | 1991-09-12 | 1994-10-11 | Fujisawa Pharmaceutical Co., Ltd. | Angiotenin II antagonizing heterocyclic compounds |
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| GB9218334D0 (en) | 1992-08-28 | 1992-10-14 | Ici Plc | Heterocyclic compounds |
| DE4304650A1 (de) | 1993-02-16 | 1994-08-18 | Thomae Gmbh Dr K | Kondensierte 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US5441946A (en) | 1994-04-14 | 1995-08-15 | Rhone-Poulenc-Rorer Pharmaceuticals, Inc. | Phosphonate derivatives of lipophilic amines |
| US5552426A (en) | 1994-04-29 | 1996-09-03 | Eli Lilly And Company | Methods for treating a physiological disorder associated with β-amyloid peptide |
| US5837390A (en) | 1995-05-10 | 1998-11-17 | Sony Corporation | Metal complex, method for producing the same and optical device |
| WO1998027972A2 (en) | 1996-12-23 | 1998-07-02 | Texas A & M University | Anti-amyloidogenic agents |
| FR2767527B1 (fr) | 1997-08-25 | 1999-11-12 | Pf Medicament | Derives de piperazines indoliques, utiles comme medicaments et procede de preparation |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| ATE244241T1 (de) | 1998-02-04 | 2003-07-15 | Univ Texas | Hemmung der menschlichen telomerase durch g- quadruplex interaktionverbindung |
| US6107491A (en) | 1998-07-20 | 2000-08-22 | Ciba Specialty Chemicals Corporation | Polymerizable diketopyrrolopyrroles |
| GB9816654D0 (en) | 1998-07-30 | 1998-09-30 | Zeneca Ltd | Chemical compounds |
| PL352285A1 (en) | 1999-06-18 | 2003-08-11 | Bayer Ag | Phenoxy fluoropyrimidines |
| WO2001012183A1 (en) | 1999-08-16 | 2001-02-22 | Merck & Co., Inc. | Heterocycle amides as cell adhesion inhibitors |
| GB9919673D0 (en) | 1999-08-20 | 1999-10-20 | Cancer Res Campaign Tech | 2-Arlybenzazole compounds |
| JP2001226358A (ja) | 1999-10-12 | 2001-08-21 | Japan Tobacco Inc | Ｌｐｌ活性増強剤 |
| YU68102A (sh) | 2000-03-16 | 2006-01-16 | F. Hoffmann-La Roche Ag. | Derivati karboksilne kiseline kao ip antagonisti |
| GB0007934D0 (en) | 2000-03-31 | 2000-05-17 | Darwin Discovery Ltd | Chemical compounds |
| PT1334091E (pt) | 2000-08-24 | 2013-01-07 | Univ Pittsburgh | Derivados de tioflavina e seu uso no diagnóstico e terapia da doença de alzheimer |
| EP1330432A2 (en) | 2000-11-04 | 2003-07-30 | Aventis Pharma Limited | Substituted alkanoic acids |
| US20070004713A1 (en) | 2000-12-07 | 2007-01-04 | Bernard Barlaam | Therapeutic benimidazole compounds |
| EP1345914A1 (en) | 2000-12-22 | 2003-09-24 | AstraZeneca AB | Therapeutic compounds |
| GB0118357D0 (en) | 2001-07-27 | 2001-09-19 | Syngenta Ltd | Chemical compounds |
| WO2003020698A2 (en) | 2001-09-06 | 2003-03-13 | Prochon Biotech Ltd. | Protein tyrosine kinase inhibitors |
| US6602619B2 (en) | 2001-10-19 | 2003-08-05 | Lightronik Technology Inc. | Organic EL device |
| US7253154B2 (en) | 2001-11-16 | 2007-08-07 | Nippon Chemiphar Co., Ltd. | Substituted thiazolopyrimidines as xanthine oxidase inhibitors |
| WO2003045930A1 (en) | 2001-11-28 | 2003-06-05 | Astrazeneca Ab | Therapeutic compounds |
| UA83620C2 (ru) | 2001-12-05 | 2008-08-11 | Уайт | Замещенные бензоксазолы и их аналоги как эстрогенные агенты |
| AU2002361811A1 (en) | 2001-12-19 | 2003-07-09 | Atherogenics, Inc. | 1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders |
| CN1596240A (zh) | 2001-12-19 | 2005-03-16 | 阿特罗吉尼克斯公司 | 查耳酮衍生物及其治疗疾病的用途 |
| GB0205256D0 (en) | 2002-03-06 | 2002-04-17 | Oxford Glycosciences Uk Ltd | Novel compounds |
| CA2479338A1 (en) | 2002-03-20 | 2003-10-02 | Metabolex, Inc. | Substituted phenylacetic acids |
| UA79755C2 (en) | 2002-04-16 | 2007-07-25 | Bayer Pharmaceuticals Corp | Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation |
| GB0226822D0 (en) | 2002-11-16 | 2002-12-24 | Oxford Glycosciences Uk Ltd | Novel compounds |
| ATE405840T1 (de) * | 2002-12-19 | 2008-09-15 | Scripps Research Inst | Zusammensetzungen und verfahren zur stabilisierung von transthyretin und zur hemmung von transthyretin-fehlfaltung |
| EP1587798A4 (en) | 2003-01-14 | 2007-06-27 | Merck & Co Inc | GEMINAL DISUBSTITUTED SODIUM DERIVATIVES AS ABETA 42 SUBSTITUTING AGENTS |
| CA2438032C (en) | 2003-03-14 | 2013-05-07 | University Of Pittsburgh | Benzothiazole derivative compounds, compositions and uses |
| MY142651A (en) | 2003-03-18 | 2010-12-15 | Merck Sharp & Dohme | Biaryl substituted triazoles as sodium channel blockers |
| WO2004084824A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
| JP2006522130A (ja) | 2003-04-03 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換ピラゾール |
| EP1618099A4 (en) | 2003-04-18 | 2008-07-16 | Merck & Co Inc | BIARYLSUBSTITUTED DIAZOLE, OXAZOLE AND IMIDAZOLE AS SODIUM CHANNEL BLOCKERS |
| WO2004098494A2 (en) | 2003-04-30 | 2004-11-18 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| KR20070032700A (ko) | 2004-05-20 | 2007-03-22 | 폴드알엑스 파마슈티칼스, 인크. | 트랜스티레틴을 안정화하고 트랜스티레틴 미스폴딩을억제하기 위한, ２-((헤테로)아릴)-벤즈옥사졸 화합물 및유도체, 그리고 조성물 및 방법 |
| WO2011116123A1 (en) | 2010-03-19 | 2011-09-22 | Irm Llc | Tafamidis for the treatment of ophthalmic diseases |
| 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 BR BR112014005810A patent/BR112014005810A2/pt active Search and Examination
- 2012-09-12 WO PCT/IB2012/054748 patent/WO2013038351A1/en not_active Ceased
- 2012-09-12 KR KR1020147006603A patent/KR20140054231A/ko not_active Ceased
- 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 US US14/345,111 patent/US9249112B2/en not_active Expired - Fee Related
- 2012-09-12 SG SG2014013270A patent/SG2014013270A/en unknown
- 2012-09-12 CN CN201280043084.6A patent/CN103781770B/zh not_active Expired - Fee Related
- 2012-09-12 EP EP12780287.4A patent/EP2755961A1/en not_active Withdrawn
- 2012-09-12 CA CA2847293A patent/CA2847293C/en not_active Expired - Fee Related
- 2012-09-12 AU AU2012310157A patent/AU2012310157B2/en active Active
- 2012-09-14 AR ARP120103410A patent/AR088755A1/es unknown
- 2012-09-14 TW TW101133893A patent/TWI476185B/zh not_active IP Right Cessation
- 2012-09-14 TW TW104101710A patent/TWI538909B/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
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014526498A5 (https=) | ||
| JP2016065042A5 (https=) | ||
| JP2015010091A5 (https=) | ||
| HRP20211834T1 (hr) | Kristalni čvrsti oblici 6-karboksi-2-(3,5-diklorfenil)benzoksazola | |
| RU2014109676A (ru) | Твердые формы ингибитора диссоциации транстиретина | |
| HRP20210748T1 (hr) | Postupak priprave spojeva s aktivnošću inhibitora hiv integraze | |
| JP2011168587A5 (https=) | ||
| JP2015525757A5 (https=) | ||
| RU2016146119A (ru) | Новый кристалл тетрациклического соединения | |
| JP2018024682A5 (https=) | ||
| HRP20161742T1 (hr) | Soli i polimorfi od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6h-azepino[5,4,3-cd]indol-6-ona | |
| JP2013534511A5 (https=) | ||
| JP2013521273A5 (https=) | ||
| CN103717571B8 (zh) | 9‑氨基甲基取代的四环素类化合物 | |
| JP2012176975A5 (https=) | ||
| HRP20170540T1 (hr) | Spojevi dimetilbenzojeve kiseline, korisni u liječenju upalnih stanja | |
| JP2012036197A5 (https=) | ||
| JP2015522037A5 (https=) | ||
| JP2011242375A5 (https=) | ||
| JP2016510767A5 (https=) | ||
| WO2016016774A8 (en) | Crystalline forms of canagliflozin | |
| JP2009541344A5 (https=) | ||
| JP2014015489A5 (https=) | ||
| RU2016132469A (ru) | S-кристаллическая форма хлористоводородного ивабрадина, способ ее получения и фармацевтическая композиция на основе этой формы | |
| JP2012533539A5 (https=) |