CN115368313A - 6-羧基-2-(3,5-二氯苯基)苯并噁唑的结晶固体形式 - Google Patents

6-羧基-2-(3,5-二氯苯基)苯并噁唑的结晶固体形式 Download PDF

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Publication number
CN115368313A
CN115368313A CN202211071641.7A CN202211071641A CN115368313A CN 115368313 A CN115368313 A CN 115368313A CN 202211071641 A CN202211071641 A CN 202211071641A CN 115368313 A CN115368313 A CN 115368313A
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Prior art keywords
dichlorophenyl
carboxy
solid
crystalline form
raman
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Pending
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CN202211071641.7A
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English (en)
Chinese (zh)
Inventor
K·P·吉拉德
A·J·詹森
K·N·琼斯
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Pfizer Corp SRL
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Pfizer Corp SRL
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Application filed by Pfizer Corp SRL filed Critical Pfizer Corp SRL
Publication of CN115368313A publication Critical patent/CN115368313A/zh
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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Cardiology (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)
CN202211071641.7A 2014-09-08 2015-08-31 6-羧基-2-(3,5-二氯苯基)苯并噁唑的结晶固体形式 Pending CN115368313A (zh)

Applications Claiming Priority (6)

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
CN201580048168.2A CN106715405A (zh) 2014-09-08 2015-08-31 6‑羧基‑2‑(3,5‑二氯苯基)苯并噁唑的结晶固体形式
PCT/IB2015/056597 WO2016038500A1 (en) 2014-09-08 2015-08-31 Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201580048168.2A Division CN106715405A (zh) 2014-09-08 2015-08-31 6‑羧基‑2‑(3,5‑二氯苯基)苯并噁唑的结晶固体形式

Publications (1)

Publication Number Publication Date
CN115368313A true CN115368313A (zh) 2022-11-22

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ID=54199901

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201580048168.2A Pending CN106715405A (zh) 2014-09-08 2015-08-31 6‑羧基‑2‑(3,5‑二氯苯基)苯并噁唑的结晶固体形式
CN202211071641.7A Pending CN115368313A (zh) 2014-09-08 2015-08-31 6-羧基-2-(3,5-二氯苯基)苯并噁唑的结晶固体形式

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CN201580048168.2A Pending CN106715405A (zh) 2014-09-08 2015-08-31 6‑羧基‑2‑(3,5‑二氯苯基)苯并噁唑的结晶固体形式

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EP (3) EP3977993B1 (enExample)
JP (5) JP2016065042A (enExample)
KR (1) KR102004059B1 (enExample)
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WO (1) WO2016038500A1 (enExample)

Families Citing this family (22)

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GB2571950A (en) * 2018-03-13 2019-09-18 Azad Pharma Ag New polymorph and new path to synthesize tafamidis
US12268669B2 (en) 2018-12-20 2025-04-08 Pfizer Inc. Pharmaceutical compositions and methods comprising a combination of a benzoxazole transthyretin stabilizer and an additional therapeutic agent
PL3953339T3 (pl) * 2019-04-11 2025-05-05 Inke, S.A. Proces otrzymania 1-deoksy-1-metyloamino-d-glucitolu 2-(3,5-dichlorofenylo)-6-benzoksazolokarboksylanu
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
WO2021093809A1 (zh) * 2019-11-15 2021-05-20 苏州科睿思制药有限公司 他发米帝司的晶型及其制备方法和用途
CA3165298A1 (en) * 2019-12-20 2021-06-24 Pfizer Ireland Pharmaceuticals Efficient process for making 6-carboxy benzoxazole derivatives
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
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
US20230391737A1 (en) * 2020-10-19 2023-12-07 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
JP2025524085A (ja) 2022-07-28 2025-07-25 ファイザー・インク タファミジス医薬組成物
EP4605382A1 (en) * 2022-10-17 2025-08-27 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

Citations (2)

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US20040152140A1 (en) * 2002-12-19 2004-08-05 Kelly Jeffery W. Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
WO2013168014A1 (en) * 2012-05-10 2013-11-14 Mahesh Kandula Compositions and methods for the treatment of familial amyloid polyneuropathy

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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
PL2091910T3 (pl) * 2006-12-06 2015-02-27 Conatus Pharmaceuticals Inc Postacie krystaliczne kwasu (3S)-3-[N-(N’-(2-tert-butylofenylo)oksamylo)alaninylo]amino-5-(2’,3’,5’,6’-tetrafluorofenoksy)-4-oksopentanowego
US8576985B2 (en) 2009-09-01 2013-11-05 Aptuit (West Lafayette) Llc Methods for indexing solid forms of compounds
MX2014003043A (es) * 2011-09-16 2015-02-05 Pfizer Formas solidas de un inhibidor de disociacion transtiretina.
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 (2)

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US20040152140A1 (en) * 2002-12-19 2004-08-05 Kelly Jeffery W. Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
WO2013168014A1 (en) * 2012-05-10 2013-11-14 Mahesh Kandula Compositions and methods for the treatment of familial amyloid polyneuropathy

Non-Patent Citations (2)

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TAKUYA YAMAMOTO等: "Nickel-Catalyzed C H Arylation of Azoles with Haloarenes: Scope, Mechanism, and Applications to the Synthesis of Bioactive Molecules", 《CHEM. EUR. J.》, vol. 17, no. 36, pages 10113 - 10122, XP055023323, DOI: 10.1002/chem.201101091 *

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DK3977993T3 (da) 2024-02-19
JP2025108584A (ja) 2025-07-23
JP2016065042A (ja) 2016-04-28
EP3191461A1 (en) 2017-07-19
JP2022024014A (ja) 2022-02-08
TW201613880A (en) 2016-04-16
EP3977993B1 (en) 2024-01-31
PL3191461T3 (pl) 2022-02-07
EP4349406A3 (en) 2024-05-22
CN106715405A (zh) 2017-05-24
CY1124843T1 (el) 2022-11-25
PT3191461T (pt) 2021-12-27
BR112017003421A2 (pt) 2017-11-28
CA2903194A1 (en) 2016-03-08
FI3977993T3 (fi) 2024-03-25
HUE065233T2 (hu) 2024-05-28
MX2017002954A (es) 2017-06-15
MX374012B (es) 2020-07-22
HUE056583T2 (hu) 2022-02-28
JP2023134645A (ja) 2023-09-27
EP3977993A1 (en) 2022-04-06
EP4349406A2 (en) 2024-04-10
US20170273953A1 (en) 2017-09-28
TWI644902B (zh) 2018-12-21
EP3191461B1 (en) 2021-11-03
JP7357525B2 (ja) 2023-10-06
JP2020055832A (ja) 2020-04-09
NZ766084A (en) 2023-12-22
US9770441B1 (en) 2017-09-26
AU2015313875B2 (en) 2018-03-15
KR20170040314A (ko) 2017-04-12
HRP20211834T1 (hr) 2022-03-04
SI3191461T1 (sl) 2022-01-31
EP4349406B1 (en) 2025-12-03
RS62634B1 (sr) 2021-12-31
PT3977993T (pt) 2024-04-01
PL3977993T3 (pl) 2024-05-06
AU2015313875A1 (en) 2017-03-02
BR112017003421B1 (pt) 2023-10-10
RU2692252C2 (ru) 2019-06-24
NZ729011A (en) 2023-10-27
IL251037A0 (en) 2017-04-30
WO2016038500A1 (en) 2016-03-17
ES2975633T3 (es) 2024-07-10
SI3977993T1 (sl) 2024-05-31
RU2017107235A (ru) 2018-10-11
SG11201700958YA (en) 2017-03-30
IL251037B1 (en) 2024-10-01
ES2901785T3 (es) 2022-03-23
RU2017107235A3 (enExample) 2018-10-11
KR102004059B1 (ko) 2019-07-25
LT3191461T (lt) 2021-12-10

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