KR102424621B1 - 로라티닙 유리 염기 수화물의 결정질 형태 - Google Patents

로라티닙 유리 염기 수화물의 결정질 형태 Download PDF

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Publication number
KR102424621B1
KR102424621B1 KR1020207010512A KR20207010512A KR102424621B1 KR 102424621 B1 KR102424621 B1 KR 102424621B1 KR 1020207010512 A KR1020207010512 A KR 1020207010512A KR 20207010512 A KR20207010512 A KR 20207010512A KR 102424621 B1 KR102424621 B1 KR 102424621B1
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South Korea
Prior art keywords
ppm
loratinib
free base
crystalline form
base hydrate
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English (en)
Korean (ko)
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KR20200051781A (ko
Inventor
폴 볼스
피터 로버트 로즈
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화이자 인코포레이티드
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=64049474&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR102424621(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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Publication of KR20200051781A publication Critical patent/KR20200051781A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020207010512A 2017-10-10 2018-10-04 로라티닙 유리 염기 수화물의 결정질 형태 Active KR102424621B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762570326P 2017-10-10 2017-10-10
US62/570,326 2017-10-10
US201862727734P 2018-09-06 2018-09-06
US62/727,734 2018-09-06
PCT/IB2018/057735 WO2019073347A1 (en) 2017-10-10 2018-10-04 CRYSTALLINE BASE FREE HYDRATE SHAPE OF LORLATINIB

Publications (2)

Publication Number Publication Date
KR20200051781A KR20200051781A (ko) 2020-05-13
KR102424621B1 true KR102424621B1 (ko) 2022-07-25

Family

ID=64049474

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KR1020207010512A Active KR102424621B1 (ko) 2017-10-10 2018-10-04 로라티닙 유리 염기 수화물의 결정질 형태

Country Status (21)

Country Link
US (1) US11299500B2 (enExample)
EP (1) EP3694863B1 (enExample)
JP (1) JP7153069B2 (enExample)
KR (1) KR102424621B1 (enExample)
CN (1) CN111201235B (enExample)
AU (1) AU2018349259B2 (enExample)
CA (1) CA3077508C (enExample)
CY (1) CY1126141T1 (enExample)
DK (1) DK3694863T3 (enExample)
ES (1) ES2952985T3 (enExample)
FI (1) FI3694863T3 (enExample)
HU (1) HUE062926T2 (enExample)
MX (1) MX2020003373A (enExample)
PL (1) PL3694863T3 (enExample)
PT (1) PT3694863T (enExample)
RU (1) RU2022109286A (enExample)
SG (1) SG11202002445SA (enExample)
SI (1) SI3694863T1 (enExample)
TW (1) TWI775960B (enExample)
WO (1) WO2019073347A1 (enExample)
ZA (1) ZA202001661B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201913200XA (en) 2015-07-31 2020-03-30 Pfizer Crystalline form of lorlatinib free base
CA3019905C (en) 2016-04-08 2022-08-23 Pfizer Inc. Crystalline forms of lorlatinib maleate
WO2019209633A1 (en) * 2018-04-23 2019-10-31 Pliva Hrvatska D.O.O. Solid state forms of lorlatinib and their preparation
US12391708B2 (en) 2019-07-18 2025-08-19 Tapi Croatia Industries Ltd Crystalline Lorlatinib : fumaric acid and solid state form thereof
CN112321604A (zh) * 2019-08-05 2021-02-05 华东理工大学 大环类jak2抑制剂及其应用
EP4041396A1 (en) 2019-10-10 2022-08-17 Sandoz AG Polymorph of lorlatinib
CN112824417A (zh) * 2019-11-21 2021-05-21 上海天慈国际药业有限公司 一种劳拉替尼的制备方法
TW202146017A (zh) 2020-03-05 2021-12-16 美商輝瑞股份有限公司 間變性淋巴瘤激酶抑制劑及周期蛋白依賴型激酶抑制劑之組合
CN111362967B (zh) * 2020-04-28 2021-09-07 南京雷正医药科技有限公司 苯并氧杂二氮杂十四碳烯衍生物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014207606A1 (en) * 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor
WO2017021823A1 (en) 2015-07-31 2017-02-09 Pfizer Inc. Crystalline form of lorlatinib free base

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2796967C (en) 2010-05-04 2015-12-01 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
JP5808818B2 (ja) 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー アファチニブの新規塩及び多形形態
PE20141639A1 (es) * 2011-06-08 2014-11-08 Biogen Idec Inc Proceso para preparar fumarato de dimetilo de alta pureza y cristalino
CA2863892C (en) * 2012-03-06 2016-08-30 Pfizer Inc. Macrocyclic derivatives for the treatment of proliferative diseases
EP3183256A4 (en) * 2014-08-20 2018-05-30 Teligene Ltd. Substituted macrocycles useful as kinases inhibitors and methods of use thereof
WO2016026423A1 (en) * 2014-08-20 2016-02-25 Teligene Ltd Substituted macrocycles useful as kinases inhibitors and methods of use thereof
CA3019905C (en) 2016-04-08 2022-08-23 Pfizer Inc. Crystalline forms of lorlatinib maleate

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014207606A1 (en) * 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor
WO2017021823A1 (en) 2015-07-31 2017-02-09 Pfizer Inc. Crystalline form of lorlatinib free base

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Journal of Medicinal Chemistry. Vol. 57(11), pp.4720-4744 (2014)
Pharmaceutical Research. Vol. 12(7), pp.945-954 (1995)

Also Published As

Publication number Publication date
AU2018349259B2 (en) 2021-02-18
PL3694863T3 (pl) 2023-09-25
TWI775960B (zh) 2022-09-01
AU2018349259A1 (en) 2020-04-09
JP7153069B2 (ja) 2022-10-13
DK3694863T3 (da) 2023-07-03
EP3694863A1 (en) 2020-08-19
TW201922753A (zh) 2019-06-16
CN111201235B (zh) 2023-02-10
WO2019073347A1 (en) 2019-04-18
US11299500B2 (en) 2022-04-12
HUE062926T2 (hu) 2023-12-28
SG11202002445SA (en) 2020-04-29
RU2020113141A (ru) 2021-11-12
PT3694863T (pt) 2023-08-23
EP3694863B1 (en) 2023-06-21
JP2020536893A (ja) 2020-12-17
ES2952985T3 (es) 2023-11-07
KR20200051781A (ko) 2020-05-13
ZA202001661B (en) 2023-11-29
MX2020003373A (es) 2020-10-12
US20200308191A1 (en) 2020-10-01
CA3077508A1 (en) 2019-04-18
BR112020005989A2 (pt) 2020-09-29
CA3077508C (en) 2023-02-14
CY1126141T1 (el) 2023-11-15
RU2020113141A3 (enExample) 2021-11-12
CN111201235A (zh) 2020-05-26
FI3694863T3 (fi) 2023-08-18
RU2022109286A (ru) 2022-05-06
SI3694863T1 (sl) 2023-10-30

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