AR096759A1 - Formas sólidas de un inhibidor de quinasa macrocíclica - Google Patents
Formas sólidas de un inhibidor de quinasa macrocíclicaInfo
- Publication number
- AR096759A1 AR096759A1 ARP140102433A ARP140102433A AR096759A1 AR 096759 A1 AR096759 A1 AR 096759A1 AR P140102433 A ARP140102433 A AR P140102433A AR P140102433 A ARP140102433 A AR P140102433A AR 096759 A1 AR096759 A1 AR 096759A1
- Authority
- AR
- Argentina
- Prior art keywords
- crystalline
- benzoxadiazacyclotetradecin
- pyrazolo
- carbonitrile
- tetrahydro
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 239000007787 solid Substances 0.000 title 1
- 239000012453 solvate Substances 0.000 abstract 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 abstract 3
- 241000124008 Mammalia Species 0.000 abstract 2
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 230000010261 cell growth Effects 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Solvatos cristalinos de (10R)-7-amino-12-fluoro-2,10,16-trimetil-15-oxo-10,15,16,17-tetrahidro-2H-8,4-(meteno)pirazolo[4,3-h][2,5,11]-benzoxadiazaciclotetradecina-3-carbonitrilo, útiles en el tratamiento de crecimiento celular anormal, tal como cáncer, en mamíferos. También composiciones farmacéuticas que comprenden dichos solvatos cristalinos, y métodos de usar dichos solvatos y composiciones en el tratamiento de crecimiento celular anormal en mamíferos, en especial humanos. Reivindicación 1: Un solvato, caracterizado porque es un solvato de ácido acético cristalino de (10R)-7-amino-12-fluoro-2,10,16-trimetil-15-oxo-10,15,16,17-tetrahidro-2H-8,4-(meteno)pirazolo[4,3-h][2,5,11]-benzoxadiazaciclotetradecina-3-carbonitrilo. Reivindicación 6: El solvato cristalino de conformidad con la reivindicación 1, caracterizado porque tiene un patrón de difracción de rayos X en polvo que comprende picos a valores 2q de: 10.5, 11.4, 12.9, 14.5 y 15.3 º2q ± 0.2 º2q. Reivindicación 12: Un hidrato, caracterizado porque es un hidrato cristalino de (10R)-7-amino-12-fluoro-2,10,16-trimetil-15-oxo-10,15,16,17-tetrahidro-2H-8,4-(meteno)pirazolo[4,3-h][2,5,11]-benzoxadiazaciclotetradecina-3-carbonitrilo. Reivindicación 15: El hidrato cristalino de conformidad con la reivindicación 12, caracterizado porque tiene un patrón de difracción de rayos X en polvo que comprende picos a valores 2q de: 8.4, 8.9 y 10.4 º2q ± 0.2 º2q.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361840703P | 2013-06-28 | 2013-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR096759A1 true AR096759A1 (es) | 2016-02-03 |
Family
ID=51136530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140102433A AR096759A1 (es) | 2013-06-28 | 2014-06-26 | Formas sólidas de un inhibidor de quinasa macrocíclica |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9637500B2 (es) |
| EP (1) | EP3013835B1 (es) |
| JP (1) | JP6110817B2 (es) |
| AR (1) | AR096759A1 (es) |
| CA (1) | CA2916605C (es) |
| ES (1) | ES2656189T3 (es) |
| TW (1) | TW201504246A (es) |
| WO (1) | WO2014207606A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016026423A1 (en) * | 2014-08-20 | 2016-02-25 | Teligene Ltd | Substituted macrocycles useful as kinases inhibitors and methods of use thereof |
| US10159663B2 (en) * | 2014-08-20 | 2018-12-25 | Teligene Ltd. | Substituted macrocycles useful as kinases inhibitors and methods of use thereof |
| MX382600B (es) | 2015-07-31 | 2025-03-13 | Pfizer | Forma cristalina de base libre de lorlatinib. |
| CA3000386A1 (en) | 2015-09-30 | 2017-04-06 | Merck Patent Gmbh | Combination of a pd-1 axis binding antagonist and an alk inhibitor for treating alk-negative cancer |
| EP3763693A1 (en) | 2016-03-03 | 2021-01-13 | Shenzhen TargetRx, Inc. | Macrocycle and composition comprising thereof |
| EP3440086B1 (en) | 2016-04-08 | 2020-08-12 | Pfizer Inc. | Crystalline forms of lorlatinib maleate |
| WO2019073347A1 (en) * | 2017-10-10 | 2019-04-18 | Pfizer Inc. | CRYSTALLINE BASE FREE HYDRATE SHAPE OF LORLATINIB |
| 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 |
| EP3784675A1 (en) | 2018-04-23 | 2021-03-03 | Pliva Hrvatska D.O.O. | Solid state forms of lorlatinib and their preparation |
| WO2020108522A1 (zh) * | 2018-11-28 | 2020-06-04 | 深圳市塔吉瑞生物医药有限公司 | 一种氘代大环化合物的制备方法 |
| CN109651398B (zh) * | 2019-01-25 | 2021-07-30 | 安庆多辉生物科技有限公司 | 一种合成劳拉替尼的溴代物中间体及催化合成劳拉替尼的方法 |
| EP3999514A1 (en) * | 2019-07-18 | 2022-05-25 | 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 |
| 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 |
| 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 |
| AU2021268345A1 (en) | 2020-05-05 | 2022-11-10 | Nuvalent, Inc. | Heteroaromatic macrocyclic ether chemotherapeutic agents |
| WO2021226208A2 (en) | 2020-05-05 | 2021-11-11 | Nuvalent, Inc. | Heteroaromatic macrocyclic ether chemotherapeutic agents |
| CN112724077B (zh) * | 2020-12-29 | 2023-07-11 | 武汉利昌医药科技有限公司 | 一种劳拉替尼中间体的合成方法 |
| CN113292496B (zh) * | 2021-05-17 | 2023-03-10 | 安徽联创生物医药股份有限公司 | 一种劳拉替尼中间体的合成方法 |
| KR20240087788A (ko) | 2021-10-01 | 2024-06-19 | 뉴베일런트, 아이엔씨. | 헤테로방향족 매크로사이클릭 에테르 화합물의 고체 형태, 약학 조성물 및 제조 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011138751A2 (en) * | 2010-05-04 | 2011-11-10 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
| EP2822953B9 (en) | 2012-03-06 | 2017-06-21 | Pfizer Inc | Macrocyclic derivatives for the treatment of proliferative diseases |
-
2014
- 2014-06-17 US US14/898,582 patent/US9637500B2/en active Active
- 2014-06-17 ES ES14736454.1T patent/ES2656189T3/es active Active
- 2014-06-17 WO PCT/IB2014/062296 patent/WO2014207606A1/en not_active Ceased
- 2014-06-17 CA CA2916605A patent/CA2916605C/en active Active
- 2014-06-17 EP EP14736454.1A patent/EP3013835B1/en not_active Not-in-force
- 2014-06-18 JP JP2014124999A patent/JP6110817B2/ja active Active
- 2014-06-26 AR ARP140102433A patent/AR096759A1/es unknown
- 2014-06-27 TW TW103122400A patent/TW201504246A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2916605A1 (en) | 2014-12-31 |
| US20160115178A1 (en) | 2016-04-28 |
| CA2916605C (en) | 2018-04-24 |
| EP3013835B1 (en) | 2017-12-13 |
| ES2656189T3 (es) | 2018-02-26 |
| EP3013835A1 (en) | 2016-05-04 |
| US9637500B2 (en) | 2017-05-02 |
| TW201504246A (zh) | 2015-02-01 |
| WO2014207606A1 (en) | 2014-12-31 |
| JP6110817B2 (ja) | 2017-04-05 |
| JP2015010091A (ja) | 2015-01-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |