CN111542527A - 芦卡帕利樟脑磺酸盐的新晶型和制备方法及其用途 - Google Patents
芦卡帕利樟脑磺酸盐的新晶型和制备方法及其用途 Download PDFInfo
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- CN111542527A CN111542527A CN201880002900.6A CN201880002900A CN111542527A CN 111542527 A CN111542527 A CN 111542527A CN 201880002900 A CN201880002900 A CN 201880002900A CN 111542527 A CN111542527 A CN 111542527A
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- camphorsulfonate
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- ZBBHBTPTTSWHBA-UHFFFAOYSA-N Nicardipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZBBHBTPTTSWHBA-UHFFFAOYSA-N 0.000 description 7
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- IWEDIXLBFLAXBO-UHFFFAOYSA-N dicamba Chemical compound COC1=C(Cl)C=CC(Cl)=C1C(O)=O IWEDIXLBFLAXBO-UHFFFAOYSA-N 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
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- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- UKHWDRMMMYWSFL-UHFFFAOYSA-N Nicarbazin Chemical compound CC=1C=C(C)NC(=O)N=1.C1=CC([N+](=O)[O-])=CC=C1NC(=O)NC1=CC=C([N+]([O-])=O)C=C1 UKHWDRMMMYWSFL-UHFFFAOYSA-N 0.000 description 4
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- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 description 3
- WYACBZDAHNBPPB-UHFFFAOYSA-N diethyl oxalate Chemical compound CCOC(=O)C(=O)OCC WYACBZDAHNBPPB-UHFFFAOYSA-N 0.000 description 3
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- HMABYWSNWIZPAG-UHFFFAOYSA-N rucaparib Chemical compound C1=CC(CNC)=CC=C1C(N1)=C2CCNC(=O)C3=C2C1=CC(F)=C3 HMABYWSNWIZPAG-UHFFFAOYSA-N 0.000 description 2
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- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 1
- -1 4-methylaminomethylphenyl Chemical group 0.000 description 1
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- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 239000012661 PARP inhibitor Substances 0.000 description 1
- 208000000450 Pelvic Pain Diseases 0.000 description 1
- 102000057297 Pepsin A Human genes 0.000 description 1
- 108090000284 Pepsin A Proteins 0.000 description 1
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 description 1
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- JBXRLVPILRXPNH-UHFFFAOYSA-N indol-6-one Chemical compound O=C1C=CC2=CC=NC2=C1 JBXRLVPILRXPNH-UHFFFAOYSA-N 0.000 description 1
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Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明公开了芦卡帕利樟脑磺酸盐的新多晶型D及其制备方法和药用用途。与现有晶型相比，新晶型在溶解度、稳定性和制备工艺方面具有明显优势。
Description
PCT国内申请，说明书已公开。
Claims (5)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2018/119486 WO2020113500A1 (zh) | 2018-12-06 | 2018-12-06 | 芦卡帕利樟脑磺酸盐的新晶型和制备方法及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111542527A true CN111542527A (zh) | 2020-08-14 |
Family
ID=70975258
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880002900.6A Pending CN111542527A (zh) | 2018-12-06 | 2018-12-06 | 芦卡帕利樟脑磺酸盐的新晶型和制备方法及其用途 |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US11352362B2 (zh) |
| CN (1) | CN111542527A (zh) |
| WO (1) | WO2020113500A1 (zh) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102884066A (zh) * | 2010-02-12 | 2013-01-16 | 辉瑞公司 | 8-氟-2-{4-[(甲氨基)甲基]苯基}-1,3,4,5-四氢-6H-氮杂*并[5,4,3-cd]吲哚-6-酮的盐和多晶型物 |
| WO2018140377A1 (en) * | 2017-01-24 | 2018-08-02 | Assia Chemical Industries Ltd. | Solid state forms of rucaparib and of rucaparib salts |
| CN109111454A (zh) * | 2018-08-01 | 2019-01-01 | 宁波金未生物科技有限公司 | 一种瑞卡帕布s-樟脑磺酸盐 |
| CN111217818A (zh) * | 2018-11-27 | 2020-06-02 | 台耀化学股份有限公司 | 芦卡帕尼樟脑磺酸盐的结晶、及制备三环化合物、芦卡帕尼及其樟脑磺酸盐结晶的方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170043597A (ko) * | 2014-08-22 | 2017-04-21 | 클로비스 온콜로지 인코포레이티드 | 루카파립의 고 용량 강도 정제 |
| CN108201534A (zh) * | 2016-12-16 | 2018-06-26 | 苏州苏融生物医药有限公司 | 一种瑞卡帕布口服缓控释药物组合物及其用途 |
-
2018
- 2018-12-06 CN CN201880002900.6A patent/CN111542527A/zh active Pending
- 2018-12-06 WO PCT/CN2018/119486 patent/WO2020113500A1/zh active Application Filing
-
2020
- 2020-04-22 US US16/854,935 patent/US11352362B2/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102884066A (zh) * | 2010-02-12 | 2013-01-16 | 辉瑞公司 | 8-氟-2-{4-[(甲氨基)甲基]苯基}-1,3,4,5-四氢-6H-氮杂*并[5,4,3-cd]吲哚-6-酮的盐和多晶型物 |
| WO2018140377A1 (en) * | 2017-01-24 | 2018-08-02 | Assia Chemical Industries Ltd. | Solid state forms of rucaparib and of rucaparib salts |
| CN109111454A (zh) * | 2018-08-01 | 2019-01-01 | 宁波金未生物科技有限公司 | 一种瑞卡帕布s-樟脑磺酸盐 |
| CN111217818A (zh) * | 2018-11-27 | 2020-06-02 | 台耀化学股份有限公司 | 芦卡帕尼樟脑磺酸盐的结晶、及制备三环化合物、芦卡帕尼及其樟脑磺酸盐结晶的方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| US11352362B2 (en) | 2022-06-07 |
| US20200291036A1 (en) | 2020-09-17 |
| WO2020113500A1 (zh) | 2020-06-11 |
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| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20200814 |