BR112017003421B1 - Formas sólidas cristalinas de 6-carbóxi-2-(3,5-dicloro-fenil)- benzoxazol e composição farmacêutica - Google Patents

Formas sólidas cristalinas de 6-carbóxi-2-(3,5-dicloro-fenil)- benzoxazol e composição farmacêutica Download PDF

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Publication number
BR112017003421B1
BR112017003421B1 BR112017003421-2A BR112017003421A BR112017003421B1 BR 112017003421 B1 BR112017003421 B1 BR 112017003421B1 BR 112017003421 A BR112017003421 A BR 112017003421A BR 112017003421 B1 BR112017003421 B1 BR 112017003421B1
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Brazil
Prior art keywords
solid
peaks
less
compound
raman
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BR112017003421-2A
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English (en)
Portuguese (pt)
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BR112017003421A2 (pt
Inventor
Kevin Paul Girard
Andrew J. Jensen
Kris Nicole Jones
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Pfizer Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54199901&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112017003421(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc filed Critical Pfizer Inc
Publication of BR112017003421A2 publication Critical patent/BR112017003421A2/pt
Publication of BR112017003421B1 publication Critical patent/BR112017003421B1/pt

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57Aryl or substituted aryl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Dermatology (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)
  • Medicinal Preparation (AREA)
BR112017003421-2A 2014-09-08 2015-08-31 Formas sólidas cristalinas de 6-carbóxi-2-(3,5-dicloro-fenil)- benzoxazol e composição farmacêutica BR112017003421B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462047614P 2014-09-08 2014-09-08
US62/047,614 2014-09-08
US201562203953P 2015-08-12 2015-08-12
US62/203,953 2015-08-12
PCT/IB2015/056597 WO2016038500A1 (en) 2014-09-08 2015-08-31 Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole

Publications (2)

Publication Number Publication Date
BR112017003421A2 BR112017003421A2 (pt) 2017-11-28
BR112017003421B1 true BR112017003421B1 (pt) 2023-10-10

Family

ID=54199901

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017003421-2A BR112017003421B1 (pt) 2014-09-08 2015-08-31 Formas sólidas cristalinas de 6-carbóxi-2-(3,5-dicloro-fenil)- benzoxazol e composição farmacêutica

Country Status (24)

Country Link
US (1) US9770441B1 (https=)
EP (3) EP4349406B1 (https=)
JP (5) JP2016065042A (https=)
KR (1) KR102004059B1 (https=)
CN (2) CN106715405A (https=)
AU (1) AU2015313875B2 (https=)
BR (1) BR112017003421B1 (https=)
CA (1) CA2903194A1 (https=)
CY (1) CY1124843T1 (https=)
DK (2) DK3977993T3 (https=)
ES (3) ES2901785T3 (https=)
FI (2) FI4349406T3 (https=)
HR (1) HRP20211834T1 (https=)
HU (2) HUE056583T2 (https=)
IL (1) IL251037B1 (https=)
LT (1) LT3191461T (https=)
MX (1) MX374012B (https=)
PL (3) PL3977993T3 (https=)
PT (3) PT4349406T (https=)
RS (1) RS62634B1 (https=)
SG (1) SG11201700958YA (https=)
SI (3) SI3977993T1 (https=)
TW (1) TWI644902B (https=)
WO (1) WO2016038500A1 (https=)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2021001858A1 (en) * 2019-07-04 2021-01-07 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid or its pharmaceutically acceptable salts and polymorphs thereof
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.
WO2021152623A1 (en) * 2020-01-27 2021-08-05 Dr. Reddy’S Laboratories Limited Improved processes for the preparation of tafamidis and its meglumine salt
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
WO2022084790A1 (en) * 2020-10-19 2022-04-28 Glenmark Life Sciences Limited Process for preparation of tafamidis and salts thereof
WO2022107166A1 (en) * 2020-11-20 2022-05-27 Natco Pharma Limited Novel crystalline form of tafamidis and its process thereof
WO2022112919A1 (en) 2020-11-25 2022-06-02 Pfizer Inc. (aza)benzothiazolyl substituted pyrazole compounds
CN114907283B (zh) * 2021-02-07 2025-01-28 南京正大天晴制药有限公司 一种2-(3,5-二氯苯基)-苯并噁唑-6-羧酸的制备方法
CN114989106A (zh) * 2021-02-09 2022-09-02 齐鲁制药有限公司 氯苯唑酸的新晶型及其制备方法
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
KR20250036933A (ko) 2022-07-28 2025-03-14 화이자 인코포레이티드 타파미디스 약학 조성물
EP4605382A1 (en) * 2022-10-17 2025-08-27 Biophore India Pharmaceuticals Pvt. Ltd. A process for the preparation of crystalline form of tafamidis
US11878081B1 (en) 2022-12-23 2024-01-23 Tap Pharmaceuticals Ag Pharmaceutical formulations of tafamidis
US11980685B1 (en) 2022-12-23 2024-05-14 Tap Pharmaceuticals, Ag Liquid pharmaceutical formulations of tafamidis
WO2026050334A1 (en) 2024-08-29 2026-03-05 Alexion Pharmaceuticals, Inc. Transthyretin stabilizers and methods of use thereof
EP4717261A1 (en) 2024-09-26 2026-04-01 Galenicum Health S.L.U. Pharmaceutical compositions of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid
EP4717262A1 (en) 2024-09-26 2026-04-01 Galenicum Health S.L.U. Pharmaceutical compositions of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid

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US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
ATE405840T1 (de) 2002-12-19 2008-09-15 Scripps Research Inst Zusammensetzungen und verfahren zur stabilisierung von transthyretin und zur hemmung von transthyretin-fehlfaltung
KR101125932B1 (ko) * 2006-12-06 2012-03-22 아이디유엔 파마슈티칼즈, 인코포레이티드 (3s)-3-[n-(n'-(2-tert-부틸페닐)옥사밀)알라니닐]아미노-5-(2',3',5',6'-테트라플루오로페녹시)-4-옥소펜탄산의 결정 형태
US8576985B2 (en) 2009-09-01 2013-11-05 Aptuit (West Lafayette) Llc Methods for indexing solid forms of compounds
RU2586330C2 (ru) 2011-09-16 2016-06-10 Пфайзер Инк. Твердые формы ингибитора диссоциации транстиретина
WO2013168014A1 (en) * 2012-05-10 2013-11-14 Mahesh Kandula Compositions and methods for the treatment of familial amyloid polyneuropathy
GB2571950A (en) 2018-03-13 2019-09-18 Azad Pharma Ag New polymorph and new path to synthesize tafamidis
EP3969443B1 (en) 2019-05-16 2024-11-20 Teva Pharmaceuticals International GmbH Solid state forms of tafamidis and salts thereof
WO2021001858A1 (en) 2019-07-04 2021-01-07 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid or its pharmaceutically acceptable salts and polymorphs thereof
WO2021152623A1 (en) 2020-01-27 2021-08-05 Dr. Reddy’S Laboratories Limited Improved processes for the preparation of tafamidis and its meglumine salt

Also Published As

Publication number Publication date
HRP20211834T1 (hr) 2022-03-04
PL4349406T3 (pl) 2026-03-23
MX374012B (es) 2020-07-22
RS62634B1 (sr) 2021-12-31
CN115368313A (zh) 2022-11-22
RU2692252C2 (ru) 2019-06-24
EP3977993A1 (en) 2022-04-06
JP7357525B2 (ja) 2023-10-06
TWI644902B (zh) 2018-12-21
JP2023134645A (ja) 2023-09-27
SI3977993T1 (sl) 2024-05-31
JP2016065042A (ja) 2016-04-28
PT3977993T (pt) 2024-04-01
HUE056583T2 (hu) 2022-02-28
EP4349406A2 (en) 2024-04-10
US20170273953A1 (en) 2017-09-28
KR102004059B1 (ko) 2019-07-25
EP3977993B1 (en) 2024-01-31
JP2020055832A (ja) 2020-04-09
SI4349406T1 (sl) 2026-02-27
SI3191461T1 (sl) 2022-01-31
CA2903194A1 (en) 2016-03-08
AU2015313875B2 (en) 2018-03-15
JP2022024014A (ja) 2022-02-08
BR112017003421A2 (pt) 2017-11-28
AU2015313875A1 (en) 2017-03-02
EP3191461B1 (en) 2021-11-03
EP4349406B1 (en) 2025-12-03
RU2017107235A3 (https=) 2018-10-11
FI3977993T3 (fi) 2024-03-25
RU2017107235A (ru) 2018-10-11
ES2975633T3 (es) 2024-07-10
EP4349406A3 (en) 2024-05-22
JP2025108584A (ja) 2025-07-23
ES2901785T3 (es) 2022-03-23
NZ729011A (en) 2023-10-27
TW201613880A (en) 2016-04-16
PL3977993T3 (pl) 2024-05-06
WO2016038500A1 (en) 2016-03-17
DK4349406T3 (da) 2026-02-02
DK3977993T3 (da) 2024-02-19
LT3191461T (lt) 2021-12-10
EP3191461A1 (en) 2017-07-19
KR20170040314A (ko) 2017-04-12
PL3191461T3 (pl) 2022-02-07
SG11201700958YA (en) 2017-03-30
IL251037A0 (en) 2017-04-30
NZ766084A (en) 2023-12-22
US9770441B1 (en) 2017-09-26
ES3061774T3 (en) 2026-04-07
CY1124843T1 (el) 2022-11-25
FI4349406T3 (fi) 2026-02-04
PT4349406T (pt) 2026-02-04
MX2017002954A (es) 2017-06-15
PT3191461T (pt) 2021-12-27
HUE065233T2 (hu) 2024-05-28
CN106715405A (zh) 2017-05-24
IL251037B1 (en) 2024-10-01

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Legal Events

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B25G Requested change of headquarter approved

Owner name: PFIZER INC. (US)

B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 31/08/2015, OBSERVADAS AS CONDICOES LEGAIS

B17A Notification of administrative nullity (patentee has 60 days time to reply to this notification)

Free format text: REQUERENTE DA NULIDADE: WILSON PINHEIRO JABUR - 870240027378 - 28/03/2024

B15G Petition not considered as such [chapter 15.7 patent gazette]
B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: REF. RPI 2753 DE 10/10/2023 QUANTO AO QUADRO REIVINDICATORIO.