DK3073999T3 - Krystalinsk form i af ibrutinib - Google Patents
Krystalinsk form i af ibrutinib Download PDFInfo
- Publication number
- DK3073999T3 DK3073999T3 DK14866302.4T DK14866302T DK3073999T3 DK 3073999 T3 DK3073999 T3 DK 3073999T3 DK 14866302 T DK14866302 T DK 14866302T DK 3073999 T3 DK3073999 T3 DK 3073999T3
- Authority
- DK
- Denmark
- Prior art keywords
- ibrutinib
- crystalline form
- alkane
- mixture
- ketone
- Prior art date
Links
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
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1. Krystallinsk form af ibrutinib, betegnet som Form 1, der udviser et røntgenpulverdiffraktionsmønster, der omfatter følgende 2Θ værdier, som er målt ved anvendelse af CuKa-stråling: 5,2° ± 0,2°, 17,6° ± 0,2° og 22,1° ± 0,2°.
2. Krystallinsk form ifølge krav 1, hvor røntgenpulver-diffraktionsmønsteret yderligere omfatter følgende 2Θ værdier, som er målt ved anvendelse af CuKa-stråling: 19,3° ± 0,2°, 20,8° ± 0,2° og 22,4° ± 0,2°.
3. Krystallinsk form ifølge krav 1 eller 2, hvor røntgenpulver-diffraktionsmønsteret yderligere omfatter følgende 2Θ værdier, som er målt ved anvendelse af CuKa-stråling: 16,2° ± 0,2°, 18,1° ± 0,2°, 18,9° ± 0,2° og 23,0° ± 0,2°.
4. Krystallinsk form ifølge krav 1, hvor røntgenpulver-diffraktionsmønsteret hovedsageligt er det samme som det, der er vist i Fig. 1:
5. Fremgangsmåde til tilvejebringelse af ibrutinib Form I ifølge krav 1, 2, 3 eller 4 omfattende: Opløsning af ibrutinib i et opløsnings-system udvalgt blandt gruppen omfattende: alkohol, æter, keton, en blanding af alkohol med alkan, en blanding af æter og alkan og en blanding af keton med alkan til dannelse af en opløsning; og krystallisering af den nævnte Form I ved køling af opløsningen under ambiente (omgivende) forhold eller på en kontrolleret måde.
6. Fremgangsmåde ifølge krav 5, hvor opløsnings-systemet er en blanding af en alkohol eller keton og en alkan.
7. Fremgangsmåde ifølge krav 6, hvor den nævnte alkan er en C4-C10-alkan.
8. Fremgangsmåde ifølge krav 6, hvor opløsnings-systemet er en blanding af 2-pro-panol og n-heptan.
9. Fremgangsmåde ifølge krav 6, hvor den nævnte keton er en C3-C6-keton, og den nævnte alkan er en C4-C10-alkan.
10. Fremgangsmåde ifølge krav 6, hvor opløsnings-systemet er en blanding af acetone og n-heptan.
11. Pharmaceutisk sammensætning omfattende en krystallinsk Form I af ibrutinib ifølge krav 1, 2, 3 eller 4.
12. Krystallinsk Form I af ibrutinib ifølge krav 1, 2, 3 eller 4 til anvendelse som et pharmaceutisk produkt.
13. Krystallinsk Form I af ibrutinib ifølge krav 1, 2, 3 eller 4 til anvendelse ved en fremgangsmåde til behandling af en sygdom eller lidelse udvalgt blandt gruppen omfattende kronisk lymfocytær leukæmi (CLL)/lille lymphocytær lymphom (SLL), kap-pecellelymphom (MCL) (engelsk: mantle cell lymphoma), diffus stor-B-celle -lymphom (DLBCL) og multipel myelom.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310616065.4A CN103694241A (zh) | 2013-11-27 | 2013-11-27 | Pci-32765的新晶型a及其制备方法 |
| CN201410542609.1A CN104327085B (zh) | 2013-11-27 | 2014-10-14 | Pci-32765的晶型a及其制备方法 |
| PCT/US2014/067586 WO2015081180A1 (en) | 2013-11-27 | 2014-11-26 | Crystalline form i of ibrutinib |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3073999T3 true DK3073999T3 (da) | 2018-09-03 |
Family
ID=50355928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14866302.4T DK3073999T3 (da) | 2013-11-27 | 2014-11-26 | Krystalinsk form i af ibrutinib |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9751889B2 (da) |
| EP (1) | EP3073999B1 (da) |
| JP (1) | JP6483126B2 (da) |
| CN (2) | CN103694241A (da) |
| AU (1) | AU2014354728B2 (da) |
| CA (1) | CA2932059C (da) |
| DK (1) | DK3073999T3 (da) |
| ES (1) | ES2684094T3 (da) |
| HU (1) | HUE039718T2 (da) |
| IL (1) | IL245865B (da) |
| MX (1) | MX363265B (da) |
| PL (1) | PL3073999T3 (da) |
| PT (1) | PT3073999T (da) |
| WO (1) | WO2015081180A1 (da) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104736178A (zh) | 2012-06-04 | 2015-06-24 | 药品循环公司 | 布鲁顿酪氨酸激酶抑制剂的晶形 |
| CA2941087A1 (en) | 2014-03-27 | 2015-10-01 | Perrigo Api Ltd | Ibrutinib solid forms and production process therefor |
| CN105085529A (zh) * | 2014-05-15 | 2015-11-25 | 广东东阳光药业有限公司 | 依鲁替尼新晶型及其制备方法 |
| SG11201700849XA (en) | 2014-08-07 | 2017-03-30 | Pharmacyclics Llc | Novel formulations of a bruton's tyrosine kinase inhibitor |
| CA2958139A1 (en) * | 2014-08-14 | 2016-02-18 | Assia Chemical Industries Ltd. | Solid state forms of ibrutinib |
| CZ201584A3 (cs) | 2015-02-09 | 2016-08-17 | Zentiva, K.S. | Sůl Ibrutinib sulfátu |
| US10477780B2 (en) * | 2015-02-13 | 2019-11-19 | Hgci, Inc. | Multiple cell tray with media plugs |
| JP7149076B2 (ja) | 2015-03-03 | 2022-10-06 | ファーマサイクリックス エルエルシー | ブルトン型チロシンキナーゼ阻害剤の薬学的製剤 |
| AU2016236578B2 (en) * | 2015-03-20 | 2019-04-04 | Crystal Pharmatech Co., Ltd. | Preparation method of crystalline form a of pci-32765 |
| CN106153797B (zh) * | 2015-04-20 | 2017-08-29 | 北京睿创康泰医药研究院有限公司 | 一种依鲁替尼及依鲁替尼制剂有关物质分析方法 |
| CN106153798B (zh) * | 2015-04-22 | 2017-08-29 | 北京睿创康泰医药研究院有限公司 | 一种用于分析依鲁替尼及依鲁替尼制剂有关物质的hplc方法以及这些杂质做参比标准的用途 |
| KR20180040694A (ko) | 2015-08-19 | 2018-04-20 | 썬 파마슈티칼 인더스트리스 리미티드 | 이브루티닙의 결정형 및 그 제조 방법 |
| ITUB20155616A1 (it) * | 2015-11-16 | 2017-05-16 | Laboratorio Chimico Int S P A | Procedimento per la preparazione della forma amorfa dell?ibrutinib e nuova forma cristallina. |
| CN105294696A (zh) * | 2015-11-19 | 2016-02-03 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
| CN106905320A (zh) * | 2015-12-23 | 2017-06-30 | 杭州容立医药科技有限公司 | 一种适合药用的依鲁替尼及其制剂 |
| CN106995445B (zh) * | 2016-01-22 | 2021-08-03 | 山东新时代药业有限公司 | 一种布鲁顿酪氨酸激酶抑制剂晶型及其制备方法 |
| CN107286163A (zh) * | 2016-03-30 | 2017-10-24 | 上海星泰医药科技有限公司 | 一种依鲁替尼的新晶型及其制备方法 |
| CZ2016196A3 (cs) | 2016-04-06 | 2017-10-18 | Zentiva, K.S. | Pevné formy Ibrutinibu |
| CZ2016276A3 (cs) | 2016-05-11 | 2017-11-22 | Zentiva, K.S. | Pevné formy volné báze ibrutinibu |
| CN106117214A (zh) * | 2016-06-29 | 2016-11-16 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
| CN106008529A (zh) * | 2016-08-08 | 2016-10-12 | 上海工程技术大学 | 一种依鲁替尼溶剂化物及其制备方法 |
| US10183024B2 (en) | 2016-12-02 | 2019-01-22 | Apotex Inc. | Crystalline forms of ibrutinib |
| WO2019070698A1 (en) | 2017-10-02 | 2019-04-11 | Johnson Matthey Public Limited Company | NEW FORMS OF IBRUTINIB |
| CZ2017787A3 (cs) | 2017-12-08 | 2019-06-19 | Zentiva, K.S. | Farmaceutické kompozice obsahující ibrutinib |
| WO2019195827A1 (en) | 2018-04-06 | 2019-10-10 | Johnson Matthey Public Limited Company | Novel form of ibrutinib |
| WO2019211870A1 (en) | 2018-05-02 | 2019-11-07 | Cipla Limited | Polymorphic forms of ibrutinib |
| SG11202010642TA (en) | 2018-05-03 | 2020-11-27 | Juno Therapeutics Inc | Combination therapy of a chimeric antigen receptor (car) t cell therapy and a kinase inhibitor |
| EP3575300A1 (en) | 2018-05-31 | 2019-12-04 | Apotex Inc. | Novel crystalline forms of ibrutinib |
| SG11202012595PA (en) * | 2018-06-19 | 2021-01-28 | Merck Patent Gmbh | Novel crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain |
| CN111138436A (zh) * | 2018-11-04 | 2020-05-12 | 鲁南制药集团股份有限公司 | 伊布替尼晶型a单晶及其制备方法 |
| EP3669867A1 (en) | 2018-12-21 | 2020-06-24 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
| US10688050B1 (en) | 2018-12-21 | 2020-06-23 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
| CN113214261A (zh) * | 2020-01-21 | 2021-08-06 | 尚科生物医药（上海）有限公司 | 一种依鲁替尼晶型a的纯化方法 |
| WO2022260667A1 (en) | 2021-06-10 | 2022-12-15 | Hikma Pharmaceuticals Usa Inc. | Oral dosage forms of ibrutinib |
| US11433072B1 (en) * | 2021-06-10 | 2022-09-06 | Hikma Pharmaceuticals USA, Inc. | Oral dosage forms of ibrutinib |
| WO2023220655A1 (en) | 2022-05-11 | 2023-11-16 | Celgene Corporation | Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy |
| WO2023242384A1 (en) | 2022-06-17 | 2023-12-21 | Krka, D.D., Novo Mesto | Crystalline form of ibrutinib |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2645583A1 (en) * | 2006-03-20 | 2007-09-27 | F. Hoffman-La Roche Ag | Methods of inhibiting btk and syk protein kinases |
| EP2081435B1 (en) * | 2006-09-22 | 2016-05-04 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| CN103096716B (zh) * | 2010-08-10 | 2016-03-02 | 西建阿维拉米斯研究公司 | Btk抑制剂的苯磺酸盐 |
| US9522917B2 (en) | 2012-04-11 | 2016-12-20 | Acerta Pharma B.V. | Bruton's tyrosine kinase inhibitors for hematopoietic mobilization |
| WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| CN104736178A (zh) * | 2012-06-04 | 2015-06-24 | 药品循环公司 | 布鲁顿酪氨酸激酶抑制剂的晶形 |
| CN103121999A (zh) * | 2012-08-29 | 2013-05-29 | 苏州迪飞医药科技有限公司 | 一种酪氨酸激酶抑制剂pci-32765的合成方法 |
| CN103142601A (zh) * | 2013-03-13 | 2013-06-12 | 杭州雷索药业有限公司 | Pci-32765在制备抗血管生成类药物中的应用 |
-
2013
- 2013-11-27 CN CN201310616065.4A patent/CN103694241A/zh active Pending
-
2014
- 2014-10-14 CN CN201410542609.1A patent/CN104327085B/zh active Active
- 2014-11-26 EP EP14866302.4A patent/EP3073999B1/en active Active
- 2014-11-26 AU AU2014354728A patent/AU2014354728B2/en active Active
- 2014-11-26 PT PT14866302T patent/PT3073999T/pt unknown
- 2014-11-26 ES ES14866302.4T patent/ES2684094T3/es active Active
- 2014-11-26 JP JP2016535162A patent/JP6483126B2/ja active Active
- 2014-11-26 WO PCT/US2014/067586 patent/WO2015081180A1/en active Application Filing
- 2014-11-26 PL PL14866302T patent/PL3073999T3/pl unknown
- 2014-11-26 US US15/100,247 patent/US9751889B2/en active Active
- 2014-11-26 HU HUE14866302A patent/HUE039718T2/hu unknown
- 2014-11-26 MX MX2016006901A patent/MX363265B/es unknown
- 2014-11-26 CA CA2932059A patent/CA2932059C/en active Active
- 2014-11-26 DK DK14866302.4T patent/DK3073999T3/da active
-
2016
- 2016-05-26 IL IL245865A patent/IL245865B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| IL245865B (en) | 2019-05-30 |
| ES2684094T3 (es) | 2018-10-01 |
| CN104327085A (zh) | 2015-02-04 |
| CN103694241A (zh) | 2014-04-02 |
| EP3073999A1 (en) | 2016-10-05 |
| EP3073999A4 (en) | 2017-03-22 |
| AU2014354728B2 (en) | 2019-02-28 |
| PL3073999T3 (pl) | 2018-10-31 |
| MX2016006901A (es) | 2016-10-28 |
| PT3073999T (pt) | 2018-10-16 |
| IL245865A0 (en) | 2016-07-31 |
| JP2016538314A (ja) | 2016-12-08 |
| AU2014354728A1 (en) | 2016-06-16 |
| US9751889B2 (en) | 2017-09-05 |
| US20170002009A1 (en) | 2017-01-05 |
| JP6483126B2 (ja) | 2019-03-13 |
| HUE039718T2 (hu) | 2019-02-28 |
| CN104327085B (zh) | 2016-08-24 |
| EP3073999B1 (en) | 2018-05-30 |
| MX363265B (es) | 2019-03-19 |
| CA2932059A1 (en) | 2015-06-04 |
| CA2932059C (en) | 2019-07-02 |
| WO2015081180A1 (en) | 2015-06-04 |
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