AU2016304420B2 - Crystalline form of lorlatinib free base - Google Patents
Crystalline form of lorlatinib free base Download PDFInfo
- Publication number
- AU2016304420B2 AU2016304420B2 AU2016304420A AU2016304420A AU2016304420B2 AU 2016304420 B2 AU2016304420 B2 AU 2016304420B2 AU 2016304420 A AU2016304420 A AU 2016304420A AU 2016304420 A AU2016304420 A AU 2016304420A AU 2016304420 B2 AU2016304420 B2 AU 2016304420B2
- Authority
- AU
- Australia
- Prior art keywords
- tablet
- ppm
- free base
- crystalline form
- lorlatinib
- 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
Links
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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
- 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
-
- 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
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N21/00—Investigating or analysing materials by the use of optical means, i.e. using sub-millimetre waves, infrared, visible or ultraviolet light
- G01N21/62—Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light
- G01N21/63—Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light optically excited
- G01N21/65—Raman scattering
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N23/00—Investigating 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
- G01N23/20—Investigating 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
- G01N23/20075—Investigating 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
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N24/00—Investigating or analyzing materials by the use of nuclear magnetic resonance, electron paramagnetic resonance or other spin effects
- G01N24/08—Investigating or analyzing materials by the use of nuclear magnetic resonance, electron paramagnetic resonance or other spin effects by using nuclear magnetic resonance
- G01N24/087—Structure determination of a chemical compound, e.g. of a biomolecule such as a protein
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
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 |
|---|---|
| AU2016304420A1 AU2016304420A1 (en) | 2018-02-01 |
| AU2016304420B2 true AU2016304420B2 (en) | 2019-09-19 |
Family
ID=56686850
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016304420A Active AU2016304420B2 (en) | 2015-07-31 | 2016-07-27 | Crystalline form of lorlatinib free base |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US10420749B2 (enExample) |
| EP (2) | EP3798222B1 (enExample) |
| JP (1) | JP6218253B2 (enExample) |
| KR (1) | KR102088188B1 (enExample) |
| CN (3) | CN116063322A (enExample) |
| AU (1) | AU2016304420B2 (enExample) |
| BR (1) | BR112017028604A2 (enExample) |
| CA (1) | CA2937257C (enExample) |
| CY (1) | CY1123689T1 (enExample) |
| DK (2) | DK3798222T3 (enExample) |
| ES (2) | ES2972010T3 (enExample) |
| FI (1) | FI3798222T3 (enExample) |
| HK (1) | HK1252845A1 (enExample) |
| HU (2) | HUE052790T2 (enExample) |
| MX (2) | MX382600B (enExample) |
| PL (2) | PL3798222T3 (enExample) |
| PT (2) | PT3798222T (enExample) |
| RU (1) | RU2018101363A (enExample) |
| SG (1) | SG10201913200XA (enExample) |
| SI (2) | SI3328867T1 (enExample) |
| TW (1) | TWI616449B (enExample) |
| WO (1) | WO2017021823A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3353341A4 (en) | 2015-09-24 | 2018-10-31 | Cyclenium Pharma Inc. | Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same |
| US11078215B2 (en) * | 2016-04-08 | 2021-08-03 | 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 |
| SG11202002445SA (en) * | 2017-10-10 | 2020-04-29 | Pfizer | Crystalline form of lorlatinib free base hydrate |
| 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 |
| WO2019209633A1 (en) | 2018-04-23 | 2019-10-31 | 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 |
| MX2021008645A (es) * | 2019-01-17 | 2021-08-19 | Pfizer | Forma cristalina de un inhibidor de cinasa ciclinodependiente (cdk). |
| 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 (1)
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011138751A2 (en) | 2010-05-04 | 2011-11-10 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
| EA024026B1 (ru) * | 2010-11-25 | 2016-08-31 | Рациофарм Гмбх | Новые соли и полиморфные формы афатиниба |
| WO2014207606A1 (en) * | 2013-06-28 | 2014-12-31 | Pfizer Inc. | Solid forms of a macrocyclic kinase inhibitor |
| 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 |
| US11078215B2 (en) | 2016-04-08 | 2021-08-03 | Pfizer Inc. | Crystalline forms of lorlatinib maleate |
| SG11202002445SA (en) | 2017-10-10 | 2020-04-29 | Pfizer | Crystalline form of lorlatinib free base hydrate |
-
2016
- 2016-07-27 EP EP20202336.2A patent/EP3798222B1/en active Active
- 2016-07-27 PL PL20202336.2T patent/PL3798222T3/pl unknown
- 2016-07-27 RU RU2018101363A patent/RU2018101363A/ru unknown
- 2016-07-27 SI SI201631027T patent/SI3328867T1/sl unknown
- 2016-07-27 EP EP16751665.7A patent/EP3328867B9/en active Active
- 2016-07-27 CN CN202310197825.6A patent/CN116063322A/zh active Pending
- 2016-07-27 CA CA2937257A patent/CA2937257C/en active Active
- 2016-07-27 HU HUE16751665A patent/HUE052790T2/hu unknown
- 2016-07-27 DK DK20202336.2T patent/DK3798222T3/da active
- 2016-07-27 CN CN201680042321.5A patent/CN107849060A/zh active Pending
- 2016-07-27 TW TW105123769A patent/TWI616449B/zh active
- 2016-07-27 US US15/743,894 patent/US10420749B2/en active Active
- 2016-07-27 SI SI201631780T patent/SI3798222T1/sl unknown
- 2016-07-27 CN CN202310214099.4A patent/CN116063323A/zh active Pending
- 2016-07-27 JP JP2016146928A patent/JP6218253B2/ja active Active
- 2016-07-27 ES ES20202336T patent/ES2972010T3/es active Active
- 2016-07-27 WO PCT/IB2016/054483 patent/WO2017021823A1/en not_active Ceased
- 2016-07-27 PL PL16751665T patent/PL3328867T3/pl unknown
- 2016-07-27 HK HK18112176.1A patent/HK1252845A1/zh unknown
- 2016-07-27 HU HUE20202336A patent/HUE065536T2/hu unknown
- 2016-07-27 MX MX2018001324A patent/MX382600B/es unknown
- 2016-07-27 PT PT202023362T patent/PT3798222T/pt unknown
- 2016-07-27 BR BR112017028604A patent/BR112017028604A2/pt not_active Application Discontinuation
- 2016-07-27 DK DK16751665.7T patent/DK3328867T3/da active
- 2016-07-27 ES ES16751665T patent/ES2842302T3/es active Active
- 2016-07-27 PT PT167516657T patent/PT3328867T/pt unknown
- 2016-07-27 MX MX2021002220A patent/MX395263B/es unknown
- 2016-07-27 SG SG10201913200XA patent/SG10201913200XA/en unknown
- 2016-07-27 FI FIEP20202336.2T patent/FI3798222T3/fi active
- 2016-07-27 AU AU2016304420A patent/AU2016304420B2/en active Active
- 2016-07-27 KR KR1020187002904A patent/KR102088188B1/ko active Active
-
2019
- 2019-08-08 US US16/535,747 patent/US11020376B2/en active Active
-
2020
- 2020-12-30 CY CY20201101227T patent/CY1123689T1/el unknown
Patent Citations (1)
| 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 |
Also Published As
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| US11299500B2 (en) | Crystalline form of lorlatinib free base hydrate | |
| RU2852836C1 (ru) | Кристаллическая форма свободного основания лорлатиниба | |
| HK40093795A (zh) | 劳拉替尼游离碱的结晶形式 | |
| HK40092368A (zh) | 劳拉替尼游离碱的结晶形式 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |