RU2018101363A - Кристаллическая форма свободного основания лорлатиниба - Google Patents
Кристаллическая форма свободного основания лорлатиниба Download PDFInfo
- Publication number
- RU2018101363A RU2018101363A RU2018101363A RU2018101363A RU2018101363A RU 2018101363 A RU2018101363 A RU 2018101363A RU 2018101363 A RU2018101363 A RU 2018101363A RU 2018101363 A RU2018101363 A RU 2018101363A RU 2018101363 A RU2018101363 A RU 2018101363A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline form
- nmr
- solid
- range
- state
- Prior art date
Links
- 239000012458 free base Substances 0.000 title claims 8
- IIXWYSCJSQVBQM-LLVKDONJSA-N lorlatinib Chemical compound N=1N(C)C(C#N)=C2C=1CN(C)C(=O)C1=CC=C(F)C=C1[C@@H](C)OC1=CC2=CN=C1N IIXWYSCJSQVBQM-LLVKDONJSA-N 0.000 title claims 7
- 229950001290 lorlatinib Drugs 0.000 title claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 238000001237 Raman spectrum Methods 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 230000002159 abnormal effect Effects 0.000 claims 4
- 230000010261 cell growth Effects 0.000 claims 4
- 238000001144 powder X-ray diffraction data Methods 0.000 claims 4
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims 3
- 101710168331 ALK tyrosine kinase receptor Proteins 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 102000027452 oncogenic receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008822 oncogenic receptor tyrosine kinases Proteins 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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)
- 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)
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2020136860A Division RU2852836C1 (ru) | 2015-07-31 | 2016-07-27 | Кристаллическая форма свободного основания лорлатиниба |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018101363A3 RU2018101363A3 (https=) | 2019-08-29 |
| RU2018101363A true RU2018101363A (ru) | 2019-08-29 |
Family
ID=56686850
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018101363A RU2018101363A (ru) | 2015-07-31 | 2016-07-27 | Кристаллическая форма свободного основания лорлатиниба |
Country Status (22)
| 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)
| 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 |
Family Cites Families (7)
| 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 |
| HUE034118T2 (en) * | 2012-03-06 | 2018-01-29 | Pfizer | Macrocyclic derivatives for the treatment of proliferative diseases |
| CA2916605C (en) * | 2013-06-28 | 2018-04-24 | 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 |
| 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 |
-
2016
- 2016-07-27 EP EP20202336.2A patent/EP3798222B1/en active Active
- 2016-07-27 HU HUE20202336A patent/HUE065536T2/hu unknown
- 2016-07-27 PL PL20202336.2T patent/PL3798222T3/pl unknown
- 2016-07-27 ES ES16751665T patent/ES2842302T3/es active Active
- 2016-07-27 WO PCT/IB2016/054483 patent/WO2017021823A1/en not_active Ceased
- 2016-07-27 RU RU2018101363A patent/RU2018101363A/ru unknown
- 2016-07-27 CN CN202310197825.6A patent/CN116063322A/zh active Pending
- 2016-07-27 US US15/743,894 patent/US10420749B2/en active Active
- 2016-07-27 MX MX2018001324A patent/MX382600B/es unknown
- 2016-07-27 HU HUE16751665A patent/HUE052790T2/hu unknown
- 2016-07-27 ES ES20202336T patent/ES2972010T3/es active Active
- 2016-07-27 KR KR1020187002904A patent/KR102088188B1/ko active Active
- 2016-07-27 CN CN201680042321.5A patent/CN107849060A/zh active Pending
- 2016-07-27 HK HK18112176.1A patent/HK1252845A1/zh unknown
- 2016-07-27 MX MX2021002220A patent/MX395263B/es unknown
- 2016-07-27 SI SI201631780T patent/SI3798222T1/sl unknown
- 2016-07-27 TW TW105123769A patent/TWI616449B/zh active
- 2016-07-27 PT PT202023362T patent/PT3798222T/pt unknown
- 2016-07-27 PL PL16751665T patent/PL3328867T3/pl unknown
- 2016-07-27 SI SI201631027T patent/SI3328867T1/sl unknown
- 2016-07-27 CN CN202310214099.4A patent/CN116063323A/zh active Pending
- 2016-07-27 PT PT167516657T patent/PT3328867T/pt unknown
- 2016-07-27 FI FIEP20202336.2T patent/FI3798222T3/fi active
- 2016-07-27 DK DK20202336.2T patent/DK3798222T3/da active
- 2016-07-27 CA CA2937257A patent/CA2937257C/en active Active
- 2016-07-27 DK DK16751665.7T patent/DK3328867T3/da active
- 2016-07-27 SG SG10201913200XA patent/SG10201913200XA/en unknown
- 2016-07-27 AU AU2016304420A patent/AU2016304420B2/en active Active
- 2016-07-27 BR BR112017028604A patent/BR112017028604A2/pt not_active Application Discontinuation
- 2016-07-27 EP EP16751665.7A patent/EP3328867B9/en active Active
- 2016-07-27 JP JP2016146928A patent/JP6218253B2/ja active Active
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2019
- 2019-08-08 US US16/535,747 patent/US11020376B2/en active Active
-
2020
- 2020-12-30 CY CY20201101227T patent/CY1123689T1/el unknown
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| HE9A | Changing address for correspondence with an applicant |