KR102088188B1 - 롤라티닙 유리 염기의 결정질 형태 - Google Patents

롤라티닙 유리 염기의 결정질 형태 Download PDF

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KR102088188B1
KR102088188B1 KR1020187002904A KR20187002904A KR102088188B1 KR 102088188 B1 KR102088188 B1 KR 102088188B1 KR 1020187002904 A KR1020187002904 A KR 1020187002904A KR 20187002904 A KR20187002904 A KR 20187002904A KR 102088188 B1 KR102088188 B1 KR 102088188B1
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KR20180022936A (ko
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멜리사 제이 버치
클리멘티나 디미트로바 펜체바
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화이자 인코포레이티드
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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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N21/00Investigating or analysing materials by the use of optical means, i.e. using sub-millimetre waves, infrared, visible or ultraviolet light
    • G01N21/62Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light
    • G01N21/63Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light optically excited
    • G01N21/65Raman scattering
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N23/00Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00 – G01N17/00, G01N21/00 or G01N22/00
    • G01N23/20Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00 – G01N17/00, G01N21/00 or G01N22/00 by using diffraction of the radiation by the materials, e.g. for investigating crystal structure; by using scattering of the radiation by the materials, e.g. for investigating non-crystalline materials; by using reflection of the radiation by the materials
    • G01N23/20075Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00 – G01N17/00, G01N21/00 or G01N22/00 by using diffraction of the radiation by the materials, e.g. for investigating crystal structure; by using scattering of the radiation by the materials, e.g. for investigating non-crystalline materials; by using reflection of the radiation by the materials by measuring interferences of X-rays, e.g. Borrmann effect
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N24/00Investigating or analyzing materials by the use of nuclear magnetic resonance, electron paramagnetic resonance or other spin effects
    • G01N24/08Investigating or analyzing materials by the use of nuclear magnetic resonance, electron paramagnetic resonance or other spin effects by using nuclear magnetic resonance
    • G01N24/087Structure determination of a chemical compound, e.g. of a biomolecule such as a protein

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020187002904A 2015-07-31 2016-07-27 롤라티닙 유리 염기의 결정질 형태 Active KR102088188B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562199418P 2015-07-31 2015-07-31
US62/199,418 2015-07-31
US201662352349P 2016-06-20 2016-06-20
US62/352,349 2016-06-20
PCT/IB2016/054483 WO2017021823A1 (en) 2015-07-31 2016-07-27 Crystalline form of lorlatinib free base

Publications (2)

Publication Number Publication Date
KR20180022936A KR20180022936A (ko) 2018-03-06
KR102088188B1 true KR102088188B1 (ko) 2020-03-12

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KR1020187002904A Active KR102088188B1 (ko) 2015-07-31 2016-07-27 롤라티닙 유리 염기의 결정질 형태

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Country Link
US (2) US10420749B2 (https=)
EP (2) EP3798222B1 (https=)
JP (1) JP6218253B2 (https=)
KR (1) KR102088188B1 (https=)
CN (3) CN116063322A (https=)
AU (1) AU2016304420B2 (https=)
BR (1) BR112017028604A2 (https=)
CA (1) CA2937257C (https=)
CY (1) CY1123689T1 (https=)
DK (2) DK3798222T3 (https=)
ES (2) ES2842302T3 (https=)
FI (1) FI3798222T3 (https=)
HK (1) HK1252845A1 (https=)
HU (2) HUE065536T2 (https=)
MX (2) MX382600B (https=)
PL (2) PL3798222T3 (https=)
PT (2) PT3798222T (https=)
RU (1) RU2018101363A (https=)
SG (1) SG10201913200XA (https=)
SI (2) SI3798222T1 (https=)
TW (1) TWI616449B (https=)
WO (1) WO2017021823A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6783311B2 (ja) 2015-09-24 2020-11-11 サイクレニウム ファーマ インコーポレーテッド ヘテロアリール含有大環状化合物のライブラリならびにその製造方法および使用方法
EP3440086B1 (en) 2016-04-08 2020-08-12 Pfizer Inc. Crystalline forms of lorlatinib maleate
JP2020524701A (ja) * 2017-06-22 2020-08-20 サイクルニウム ファーマ インコーポレイテッド ピリジン含有大環状化合物ライブラリーならびにその製造および使用方法
JP7153069B2 (ja) 2017-10-10 2022-10-13 ファイザー・インク ロルラチニブ遊離塩基水和物の結晶形態
US11179412B2 (en) 2017-12-04 2021-11-23 University of Pittsburgh—of the Commonwealth System of Higher Education Methods of treating conditions involving elevated inflammatory response
US20210163498A1 (en) 2018-04-23 2021-06-03 Pliva Hrvatska D.O.O. Solid state forms of lorlatinib and their preparation
CN109232607A (zh) * 2018-09-20 2019-01-18 沈阳药科大学 劳拉替尼的合成方法
WO2020148635A1 (en) * 2019-01-17 2020-07-23 Pfizer Inc. Crystalline form of a cdk inhibitor
EP3999514A1 (en) 2019-07-18 2022-05-25 Pliva Hrvatska D.O.O. Crystalline lorlatinib : fumaric acid and solid state form thereof
CN110483551B (zh) * 2019-08-30 2021-10-22 北京赛思源生物医药技术有限公司 一种劳拉替尼游离碱的晶体
CN110530998A (zh) * 2019-09-16 2019-12-03 山东省药学科学院 一种劳拉替尼及含劳拉替尼的制剂中有关物质的检测方法
WO2021069571A1 (en) 2019-10-10 2021-04-15 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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8680111B2 (en) 2012-03-06 2014-03-25 Pfizer Inc. Macrocyclic derivatives for the treatment of diseases
WO2014207606A1 (en) 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2566858A2 (en) 2010-05-04 2013-03-13 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
CN103476770B (zh) * 2010-11-25 2017-02-15 拉蒂欧制药有限责任公司 阿法替尼盐和多晶型物
CN104513253A (zh) * 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
EP3440086B1 (en) 2016-04-08 2020-08-12 Pfizer Inc. Crystalline forms of lorlatinib maleate
JP7153069B2 (ja) 2017-10-10 2022-10-13 ファイザー・インク ロルラチニブ遊離塩基水和物の結晶形態

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8680111B2 (en) 2012-03-06 2014-03-25 Pfizer Inc. Macrocyclic derivatives for the treatment of diseases
WO2014207606A1 (en) 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor

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Publication number Publication date
EP3798222B1 (en) 2023-11-22
US20180235933A1 (en) 2018-08-23
AU2016304420B2 (en) 2019-09-19
BR112017028604A2 (pt) 2018-09-04
SI3798222T1 (sl) 2024-02-29
TWI616449B (zh) 2018-03-01
FI3798222T3 (fi) 2023-11-28
RU2018101363A3 (https=) 2019-08-29
RU2018101363A (ru) 2019-08-29
EP3798222A1 (en) 2021-03-31
US10420749B2 (en) 2019-09-24
PL3328867T3 (pl) 2021-04-19
US20190365712A1 (en) 2019-12-05
TW201718600A (zh) 2017-06-01
PT3798222T (pt) 2024-01-22
CN107849060A (zh) 2018-03-27
MX382600B (es) 2025-03-13
AU2016304420A1 (en) 2018-02-01
CA2937257C (en) 2022-06-14
SG10201913200XA (en) 2020-03-30
MX2018001324A (es) 2018-04-30
CN116063322A (zh) 2023-05-05
HUE052790T2 (hu) 2021-05-28
WO2017021823A1 (en) 2017-02-09
JP6218253B2 (ja) 2017-10-25
DK3798222T3 (da) 2023-12-11
EP3328867B9 (en) 2021-04-14
PL3798222T3 (pl) 2024-03-25
DK3328867T3 (da) 2020-11-16
MX395263B (es) 2025-03-25
NZ739304A (en) 2024-11-29
HUE065536T2 (hu) 2024-05-28
ES2842302T3 (es) 2021-07-13
CY1123689T1 (el) 2022-03-24
EP3328867B1 (en) 2020-11-11
CN116063323A (zh) 2023-05-05
US11020376B2 (en) 2021-06-01
ES2972010T3 (es) 2024-06-10
MX2021002220A (es) 2022-09-01
CA2937257A1 (en) 2017-01-31
JP2017039702A (ja) 2017-02-23
EP3328867A1 (en) 2018-06-06
KR20180022936A (ko) 2018-03-06
SI3328867T1 (sl) 2021-04-30
PT3328867T (pt) 2021-01-13
HK1252845A1 (zh) 2019-06-06

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