TWI644902B - ６－羧基－２－（３，５－二氯苯基）－苯并唑之結晶固體型式 - Google Patents

６－羧基－２－（３，５－二氯苯基）－苯并唑之結晶固體型式 Download PDF

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Publication number
TWI644902B
TWI644902B TW104129562A TW104129562A TWI644902B TW I644902 B TWI644902 B TW I644902B TW 104129562 A TW104129562 A TW 104129562A TW 104129562 A TW104129562 A TW 104129562A TW I644902 B TWI644902 B TW I644902B
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Taiwan
Prior art keywords
crystalline form
type
dichlorophenyl
carboxy
peaks
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TW104129562A
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English (en)
Chinese (zh)
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TW201613880A (en
Inventor
凱文 保羅 吉拉德
安德魯Ｊ 詹森
克里斯 尼可 瓊斯
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輝瑞大藥廠
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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=TWI644902(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 輝瑞大藥廠 filed Critical 輝瑞大藥廠
Publication of TW201613880A publication Critical patent/TW201613880A/zh
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    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (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)
TW104129562A 2014-09-08 2015-09-07 ６－羧基－２－（３，５－二氯苯基）－苯并唑之結晶固體型式 TWI644902B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW201613880A TW201613880A (en) 2016-04-16
TWI644902B true TWI644902B (zh) 2018-12-21

Family

ID=54199901

Family Applications (1)

Application Number Title Priority Date Filing Date
TW104129562A TWI644902B (zh) 2014-09-08 2015-09-07 ６－羧基－２－（３，５－二氯苯基）－苯并唑之結晶固體型式

Country Status (24)

Country Link
US (1) US9770441B1 (enExample)
EP (3) EP3191461B1 (enExample)
JP (5) JP2016065042A (enExample)
KR (1) KR102004059B1 (enExample)
CN (2) CN115368313A (enExample)
AU (1) AU2015313875B2 (enExample)
BR (1) BR112017003421B1 (enExample)
CA (1) CA2903194A1 (enExample)
CY (1) CY1124843T1 (enExample)
DK (2) DK4349406T3 (enExample)
ES (3) ES2975633T3 (enExample)
FI (2) FI3977993T3 (enExample)
HR (1) HRP20211834T1 (enExample)
HU (2) HUE056583T2 (enExample)
IL (1) IL251037B1 (enExample)
LT (1) LT3191461T (enExample)
MX (1) MX374012B (enExample)
PL (3) PL3191461T3 (enExample)
PT (3) PT3191461T (enExample)
RS (1) RS62634B1 (enExample)
SG (1) SG11201700958YA (enExample)
SI (3) SI4349406T1 (enExample)
TW (1) TWI644902B (enExample)
WO (1) WO2016038500A1 (enExample)

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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
HRP20250159T1 (hr) * 2019-05-16 2025-03-28 Assia Chemical Industries Ltd. Kruti oblici tafamidisa i njegovih soli
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
EP4059926A4 (en) 2019-11-15 2022-12-14 Crystal Pharmaceutical (Suzhou) Co., Ltd. CRYSTALLINE FORM OF TAFAMIDIS AND PROCESS FOR PRODUCTION AND USE THEREOF
HRP20251570T1 (hr) * 2019-12-20 2026-01-30 Pfizer Ireland Pharmaceuticals Unlimited Company Djelotvoran postupak dobivanja derivata 6-karboksibenzoksazola
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
WO2023091534A1 (en) 2021-11-17 2023-05-25 Teva Pharmaceuticals International Gmbh Solid state form of tafamidis
CN119604278A (zh) 2022-07-28 2025-03-11 辉瑞大药厂 氯苯唑酸药物组合物
US20260138960A1 (en) * 2022-10-17 2026-05-21 Biophore India Pharmaceuticals Pvt. Ltd A process for the preparation of crystalline form of tafamidis
US11980685B1 (en) 2022-12-23 2024-05-14 Tap Pharmaceuticals, Ag Liquid pharmaceutical formulations of tafamidis
US11878081B1 (en) 2022-12-23 2024-01-23 Tap Pharmaceuticals Ag Pharmaceutical formulations of tafamidis
WO2026050334A1 (en) 2024-08-29 2026-03-05 Alexion Pharmaceuticals, Inc. Transthyretin stabilizers and methods of use thereof
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
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
WO2026159144A1 (en) 2025-01-22 2026-07-30 Inke, S.A. Solid forms of tafamidis methyl ethyl ketone solvate and processes for their manufacture

Citations (1)

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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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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
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
CN103951583B (zh) * 2006-12-06 2016-01-06 科内图斯医药公司 一种抑制剂的结晶形式
US8576985B2 (en) 2009-09-01 2013-11-05 Aptuit (West Lafayette) Llc Methods for indexing solid forms of compounds
WO2013038351A1 (en) * 2011-09-16 2013-03-21 Pfizer Inc. Solid forms of a transthyretin dissociation inhibitor
US9499527B2 (en) * 2012-05-10 2016-11-22 Cellix Bio Private Limited 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
HRP20250159T1 (hr) 2019-05-16 2025-03-28 Assia Chemical Industries Ltd. Kruti oblici tafamidisa i njegovih soli
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7214695B2 (en) * 2002-12-19 2007-05-08 The Scripps Research Institute Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding

Also Published As

Publication number Publication date
CA2903194A1 (en) 2016-03-08
US9770441B1 (en) 2017-09-26
CY1124843T1 (el) 2022-11-25
EP4349406A2 (en) 2024-04-10
HUE065233T2 (hu) 2024-05-28
CN106715405A (zh) 2017-05-24
SI3191461T1 (sl) 2022-01-31
JP2025108584A (ja) 2025-07-23
PL3191461T3 (pl) 2022-02-07
RU2017107235A (ru) 2018-10-11
RS62634B1 (sr) 2021-12-31
HUE056583T2 (hu) 2022-02-28
FI4349406T3 (fi) 2026-02-04
SG11201700958YA (en) 2017-03-30
DK3977993T3 (da) 2024-02-19
JP2023134645A (ja) 2023-09-27
EP4349406B1 (en) 2025-12-03
IL251037B1 (en) 2024-10-01
AU2015313875B2 (en) 2018-03-15
BR112017003421A2 (pt) 2017-11-28
PT4349406T (pt) 2026-02-04
MX2017002954A (es) 2017-06-15
PL4349406T3 (pl) 2026-03-23
RU2017107235A3 (enExample) 2018-10-11
JP7357525B2 (ja) 2023-10-06
FI3977993T3 (fi) 2024-03-25
EP3191461A1 (en) 2017-07-19
JP2020055832A (ja) 2020-04-09
TW201613880A (en) 2016-04-16
NZ766084A (en) 2023-12-22
ES2901785T3 (es) 2022-03-23
EP3977993B1 (en) 2024-01-31
KR102004059B1 (ko) 2019-07-25
LT3191461T (lt) 2021-12-10
JP2022024014A (ja) 2022-02-08
HRP20211834T1 (hr) 2022-03-04
EP4349406A3 (en) 2024-05-22
SI4349406T1 (sl) 2026-02-27
EP3977993A1 (en) 2022-04-06
SI3977993T1 (sl) 2024-05-31
NZ729011A (en) 2023-10-27
PT3191461T (pt) 2021-12-27
MX374012B (es) 2020-07-22
WO2016038500A1 (en) 2016-03-17
CN115368313A (zh) 2022-11-22
PT3977993T (pt) 2024-04-01
RU2692252C2 (ru) 2019-06-24
EP3191461B1 (en) 2021-11-03
BR112017003421B1 (pt) 2023-10-10
AU2015313875A1 (en) 2017-03-02
JP2016065042A (ja) 2016-04-28
ES2975633T3 (es) 2024-07-10
PL3977993T3 (pl) 2024-05-06
US20170273953A1 (en) 2017-09-28
DK4349406T3 (da) 2026-02-02
ES3061774T3 (en) 2026-04-07
IL251037A0 (en) 2017-04-30
KR20170040314A (ko) 2017-04-12

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