KR102004059B1 - 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 - Google Patents

6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 Download PDF

Info

Publication number
KR102004059B1
KR102004059B1 KR1020177006011A KR20177006011A KR102004059B1 KR 102004059 B1 KR102004059 B1 KR 102004059B1 KR 1020177006011 A KR1020177006011 A KR 1020177006011A KR 20177006011 A KR20177006011 A KR 20177006011A KR 102004059 B1 KR102004059 B1 KR 102004059B1
Authority
KR
South Korea
Prior art keywords
crystalline form
peak
benzoxazole
crystalline
dichlorophenyl
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.)
Active
Application number
KR1020177006011A
Other languages
English (en)
Korean (ko)
Other versions
KR20170040314A (ko
Inventor
케빈 폴 지라드
앤드류 제이. 젠센
크리스 니콜 존스
Original Assignee
화이자 인코포레이티드
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
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=KR102004059(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 화이자 인코포레이티드 filed Critical 화이자 인코포레이티드
Publication of KR20170040314A publication Critical patent/KR20170040314A/ko
Application granted granted Critical
Publication of KR102004059B1 publication Critical patent/KR102004059B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • 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)
KR1020177006011A 2014-09-08 2015-08-31 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 Active KR102004059B1 (ko)

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
KR20170040314A KR20170040314A (ko) 2017-04-12
KR102004059B1 true KR102004059B1 (ko) 2019-07-25

Family

ID=54199901

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177006011A Active KR102004059B1 (ko) 2014-09-08 2015-08-31 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형

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

Citations (2)

* 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
WO2013038351A1 (en) * 2011-09-16 2013-03-21 Pfizer Inc. Solid forms of a transthyretin dissociation inhibitor

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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

Patent Citations (2)

* 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
WO2013038351A1 (en) * 2011-09-16 2013-03-21 Pfizer Inc. Solid forms of a transthyretin dissociation inhibitor

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
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
BR112017003421B1 (pt) 2023-10-10
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

Similar Documents

Publication Publication Date Title
KR102004059B1 (ko) 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형
CN103781770B (zh) 转甲状腺素蛋白解离抑制剂的固体形式
HK40083489A (en) Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole
NZ729011B2 (en) Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole
HK1237336A1 (en) Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole
HK1197239B (en) Solid forms of a transthyretin dissociation inhibitor
NZ621194B2 (en) Solid forms of a transthyretin dissociation inhibitor

Legal Events

Date Code Title Description
A201 Request for examination
AMND Amendment
PA0105 International application

Patent event date: 20170303

Patent event code: PA01051R01D

Comment text: International Patent Application

PA0201 Request for examination
PG1501 Laying open of application
E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20180501

Patent event code: PE09021S01D

AMND Amendment
E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20190401

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20180501

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I

X091 Application refused [patent]
AMND Amendment
PX0901 Re-examination

Patent event code: PX09011S01I

Patent event date: 20190401

Comment text: Decision to Refuse Application

Patent event code: PX09012R01I

Patent event date: 20190201

Comment text: Amendment to Specification, etc.

Patent event code: PX09012R01I

Patent event date: 20170303

Comment text: Amendment to Specification, etc.

PX0701 Decision of registration after re-examination

Patent event date: 20190704

Comment text: Decision to Grant Registration

Patent event code: PX07013S01D

Patent event date: 20190628

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

Patent event date: 20190401

Comment text: Decision to Refuse Application

Patent event code: PX07011S01I

Patent event date: 20190201

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

Patent event date: 20170303

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

X701 Decision to grant (after re-examination)
GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20190719

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20190719

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
FPAY Annual fee payment

Payment date: 20220622

Year of fee payment: 4

PR1001 Payment of annual fee

Payment date: 20220622

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20230626

Start annual number: 5

End annual number: 5

PR1001 Payment of annual fee

Payment date: 20240624

Start annual number: 6

End annual number: 6