CN111201235B - 劳拉替尼游离碱水合物的结晶形式 - Google Patents

劳拉替尼游离碱水合物的结晶形式 Download PDF

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CN111201235B
CN111201235B CN201880065709.6A CN201880065709A CN111201235B CN 111201235 B CN111201235 B CN 111201235B CN 201880065709 A CN201880065709 A CN 201880065709A CN 111201235 B CN111201235 B CN 111201235B
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ppm
free base
values
base hydrate
crystalline form
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CN111201235A (zh
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P·鲍尔斯
P·R·罗斯
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Pfizer Corp SRL
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Pfizer Corp SRL
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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)
  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CN201880065709.6A 2017-10-10 2018-10-04 劳拉替尼游离碱水合物的结晶形式 Active CN111201235B (zh)

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
CN111201235A CN111201235A (zh) 2020-05-26
CN111201235B true CN111201235B (zh) 2023-02-10

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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)
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RU (1) RU2022109286A (enExample)
SG (1) SG11202002445SA (enExample)
SI (1) SI3694863T1 (enExample)
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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2018101363A (ru) 2015-07-31 2019-08-29 Пфайзер Инк. Кристаллическая форма свободного основания лорлатиниба
EP3440086B1 (en) 2016-04-08 2020-08-12 Pfizer Inc. Crystalline forms of lorlatinib maleate
EP3784675A1 (en) * 2018-04-23 2021-03-03 Pliva Hrvatska D.O.O. Solid state forms of lorlatinib and their preparation
WO2021011345A1 (en) * 2019-07-18 2021-01-21 Pliva Hrvatska D.O.O 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
US20230117684A1 (en) 2020-03-05 2023-04-20 Pfizer Inc. Combination of an anaplastic lymphoma kinase inhibitor and a cyclin dependent kinase inhibitor
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 (4)

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CN104169286A (zh) * 2012-03-06 2014-11-26 辉瑞大药厂 用于治疗增殖性疾病的大环衍生物
WO2014207606A1 (en) * 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor
WO2016026423A1 (en) * 2014-08-20 2016-02-25 Teligene Ltd Substituted macrocycles useful as kinases inhibitors and methods of use thereof
WO2017021823A1 (en) * 2015-07-31 2017-02-09 Pfizer Inc. Crystalline form of lorlatinib free base

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Publication number Priority date Publication date Assignee Title
US8916593B2 (en) 2010-05-04 2014-12-23 Pfizer Inc. Alkoxy-substituted 2-aminopyridines 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
NZ618178A (en) * 2011-06-08 2016-03-31 Biogen Ma Inc Process for preparing high purity and crystalline dimethyl fumarate
JP6609308B2 (ja) * 2014-08-20 2019-11-20 テリジーン リミテッド キナーゼ阻害剤としての置換マクロサイクル
EP3440086B1 (en) 2016-04-08 2020-08-12 Pfizer Inc. Crystalline forms of lorlatinib maleate

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104169286A (zh) * 2012-03-06 2014-11-26 辉瑞大药厂 用于治疗增殖性疾病的大环衍生物
WO2014207606A1 (en) * 2013-06-28 2014-12-31 Pfizer Inc. Solid forms of a macrocyclic kinase inhibitor
WO2016026423A1 (en) * 2014-08-20 2016-02-25 Teligene Ltd Substituted macrocycles useful as kinases inhibitors and methods of use thereof
WO2017021823A1 (en) * 2015-07-31 2017-02-09 Pfizer Inc. Crystalline form of lorlatinib free base

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Discovery of (10R)‑7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H‑8,4-(metheno)pyrazolo[4,3‑h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and cros;Ted W. Johnson et al.;《J. Med. Chem.》;20140513;第57卷;第4720-4744页 *
Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations;Stephen Byrn et al.;《Pharmaceutical Research》;19951231;第12卷(第7期);第945-954页 *
Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F;Alice T. Shaw et al.;《The New England Journal of Medicine》;20151223;第374卷(第1期);第54-61页 *

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KR102424621B1 (ko) 2022-07-25
PL3694863T3 (pl) 2023-09-25
TW201922753A (zh) 2019-06-16
BR112020005989A2 (pt) 2020-09-29
KR20200051781A (ko) 2020-05-13
JP2020536893A (ja) 2020-12-17
US20200308191A1 (en) 2020-10-01
EP3694863B1 (en) 2023-06-21
TWI775960B (zh) 2022-09-01
CA3077508A1 (en) 2019-04-18
SG11202002445SA (en) 2020-04-29
HUE062926T2 (hu) 2023-12-28
CN111201235A (zh) 2020-05-26
AU2018349259B2 (en) 2021-02-18
CA3077508C (en) 2023-02-14
RU2022109286A (ru) 2022-05-06
ZA202001661B (en) 2023-11-29
SI3694863T1 (sl) 2023-10-30
PT3694863T (pt) 2023-08-23
AU2018349259A1 (en) 2020-04-09
EP3694863A1 (en) 2020-08-19
US11299500B2 (en) 2022-04-12
DK3694863T3 (da) 2023-07-03
JP7153069B2 (ja) 2022-10-13
ES2952985T3 (es) 2023-11-07
WO2019073347A1 (en) 2019-04-18
CY1126141T1 (el) 2023-11-15
RU2020113141A (ru) 2021-11-12
MX2020003373A (es) 2020-10-12
RU2020113141A3 (enExample) 2021-11-12
FI3694863T3 (fi) 2023-08-18

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