CN110036003A - Ap26113的新晶型及其制备方法 - Google Patents
Ap26113的新晶型及其制备方法 Download PDFInfo
- Publication number
- CN110036003A CN110036003A CN201780061108.3A CN201780061108A CN110036003A CN 110036003 A CN110036003 A CN 110036003A CN 201780061108 A CN201780061108 A CN 201780061108A CN 110036003 A CN110036003 A CN 110036003A
- Authority
- CN
- China
- Prior art keywords
- crystal form
- preparation
- ray powder
- powder diffraction
- characteristic peak
- 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.)
- Granted
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明涉及AP26113的两种晶型及其制备方法。本发明提供的AP26113晶型CS1和晶型CS2在溶解度、稳定性等方面存在优势，适合于工艺开发，为含AP26113的药物制剂的制备提供了更好的选择，对于药物开发具有重要意义。
Description
PCT国内申请，说明书已公开。
Claims (13)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016109334967 | 2016-10-25 | ||
| CN201610933496 | 2016-10-25 | ||
| PCT/CN2017/107652 WO2018077187A1 (zh) | 2016-10-25 | 2017-10-25 | Ap26113的新晶型及其制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110036003A true CN110036003A (zh) | 2019-07-19 |
| CN110036003B CN110036003B (zh) | 2021-10-29 |
Family
ID=62024413
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780061108.3A Active CN110036003B (zh) | 2016-10-25 | 2017-10-25 | Ap26113的新晶型及其制备方法 |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US10544129B2 (zh) |
| CN (1) | CN110036003B (zh) |
| WO (1) | WO2018077187A1 (zh) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020099483A1 (en) | 2018-11-15 | 2020-05-22 | Sandoz Ag | Crystalline forms of brigatinib |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102105150A (zh) * | 2008-05-21 | 2011-06-22 | 阿里亚德医药股份有限公司 | 用作激酶抑制剂的磷衍生物 |
| WO2016065028A1 (en) * | 2014-10-21 | 2016-04-28 | Ariad Pharmaceuticals, Inc. | Crystalline forms of 5-chloro-n4-[-2-(dimethylphosphoryl) phenyl]-n2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] pyrimidine-2,4-diamine |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9611283B1 (en) * | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
-
2017
- 2017-10-25 WO PCT/CN2017/107652 patent/WO2018077187A1/zh active Application Filing
- 2017-10-25 CN CN201780061108.3A patent/CN110036003B/zh active Active
- 2017-10-25 US US16/344,443 patent/US10544129B2/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102105150A (zh) * | 2008-05-21 | 2011-06-22 | 阿里亚德医药股份有限公司 | 用作激酶抑制剂的磷衍生物 |
| WO2016065028A1 (en) * | 2014-10-21 | 2016-04-28 | Ariad Pharmaceuticals, Inc. | Crystalline forms of 5-chloro-n4-[-2-(dimethylphosphoryl) phenyl]-n2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] pyrimidine-2,4-diamine |
Non-Patent Citations (1)
| Title |
|---|
| WEI-SHENG HUANG等: "Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase", 《J. MED. CHEM.》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20190322646A1 (en) | 2019-10-24 |
| CN110036003B (zh) | 2021-10-29 |
| US10544129B2 (en) | 2020-01-28 |
| WO2018077187A1 (zh) | 2018-05-03 |
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