HRP20240026T1 - Kruti oblik ribociklib sukcinata - Google Patents
Kruti oblik ribociklib sukcinata Download PDFInfo
- Publication number
- HRP20240026T1 HRP20240026T1 HRP20240026TT HRP20240026T HRP20240026T1 HR P20240026 T1 HRP20240026 T1 HR P20240026T1 HR P20240026T T HRP20240026T T HR P20240026TT HR P20240026 T HRP20240026 T HR P20240026T HR P20240026 T1 HRP20240026 T1 HR P20240026T1
- Authority
- HR
- Croatia
- Prior art keywords
- ribociclib
- crystalline form
- ribociclib succinate
- ppm
- preparation
- Prior art date
Links
- NHANOMFABJQAAH-UHFFFAOYSA-N butanedioic acid;7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound OC(=O)CCC(O)=O.N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 NHANOMFABJQAAH-UHFFFAOYSA-N 0.000 title claims 13
- 229950010518 ribociclib succinate Drugs 0.000 title claims 12
- 239000007787 solid Substances 0.000 title claims 7
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims 4
- 229950003687 ribociclib Drugs 0.000 claims 4
- 239000013078 crystal Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 238000004922 13C solid-state nuclear magnetic resonance spectroscopy Methods 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 238000001157 Fourier transform infrared spectrum Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 238000001228 spectrum Methods 0.000 claims 2
- 230000009102 absorption Effects 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
-
- 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)
- 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)
- 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)
- Medicinal Preparation (AREA)
Claims (13)
1. Kristalni oblik ribociklib sukcinata označen kao oblik B, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu koji ima maksimume na 6.5, 7.5, 10.2, 10.9 i 12.0 stupnjeva dva theta ± 0.2 stupnja dva theta.
2. Kristalni oblik prema zahtjevu 1, koji je nadalje naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu koji ima bilo koji jedan, dva, tri, četiri ili pet dodatnih maksimuma odabranih između 14.6, 20.2, 20.7, 25.4 i 26.6 stupnjeva dva theta ± 0.2 stupnja dva theta.
3. Kristalni oblik prema zahtjevu 1 ili zahtjevu 2, koji je nadalje naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu kao što je prikazano na slici 2.
4. Kristalni oblik prema bilo kojem od zahtjeva 1-3, koji je nadalje naznačen time što ima podatke odabrane između jednog ili više od sljedećeg:
(iv) 13C NMR spektar krutog stanja koji ima maksimume na 183.0, 165.5, 156.5, 138.3 i 103.1 ppm ± 0.2 ppm;
(v) 13C NMR spektar krutog stanja koji ima sljedeće apsolutne razlike kemijskog pomaka između navedenih karakterističnih maksimuma na 183.0, 165.5, 156.5, 138.3 i 103.1 ppm ± 0.2 ppm i referentnog maksimuma na 122.3 ppm ± 1 ppm od 60.7, 43.2, 34.1, 15.9 i (-19.2) ± 0.1 ppm;
(vi) 13C NMR spektar krutog stanja uglavnom kao što je prikazano na slici 12 ili uglavnom kao što je prikazano na slici 13;
(vii) FT-IR spektar koji ima apsorpcije na 1605, 1525, 1399, 1261 i 786 cm-1 ± 4 cm-1; ili
(viii) FT-IR spektar uglavnom kao što je prikazano na slici 8 ili uglavnom kao što je prikazano na slici 9.
5. Kristalni oblik B prema bilo kojem od zahtjeva 1-4, naznačen time što je kristalni oblik izoliran, ili pri čemu je kristalni oblik uglavnom bez bilo kojeg drugog oblika krutog stanja, pri čemu izraz "uglavnom bez bilo kojeg drugog oblika krutog stanja" znači da kruti oblik sadrži 20% (m/m) ili manje bilo kojeg drugog oblika predmetnog spoja.
6. Upotreba kristalnog oblika B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5 u pripravi drugih krutih oblika ribociklib sukcinata, ribocikliba i/ili drugih soli ribocikliba.
7. Upotreba kristalnog oblika B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5 u pripravi farmaceutskog pripravka ili formulacije koja sadrži ribociklib sukcinat.
8. Kristalni oblik B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5 naznačen time što je za upotrebu u pripravi drugih krutih oblika ribociklib sukcinata, ribocikliba i/ili drugih soli ili ribocikliba.
9. Kristalni oblik B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5 naznačen time što je za upotrebu u pripravi farmaceutskog pripravka ili formulacije koja sadrži ribociklib sukcinat.
10. Farmaceutski pripravak naznačen time što sadrži kristalni oblik B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5.
11. Postupak za pripremu farmaceutskog pripravka prema zahtjevu 10 naznačen time što obuhvaća kombiniranje kristalnog oblika B ribociklib sukcinata i najmanje jedne farmaceutski prihvatljive pomoćne tvari.
12. Farmaceutski pripravak prema zahtjevu 10, naznačen time što se koristi kao lijek, poželjno za upotrebu u liječenju raka dojke.
13. Oblik B ribociklib sukcinata prema bilo kojem od zahtjeva 1-5, ili njegova farmaceutska formulacija, za upotrebu kao lijek, po izboru za upotrebu u liječenju raka dojke.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762550208P | 2017-08-25 | 2017-08-25 | |
| US201762555170P | 2017-09-07 | 2017-09-07 | |
| US201762577446P | 2017-10-26 | 2017-10-26 | |
| US201762593319P | 2017-12-01 | 2017-12-01 | |
| PCT/US2018/047434 WO2019040567A1 (en) | 2017-08-25 | 2018-08-22 | RIBOCICLIB SALTS AND SOLID STATE FORMS THEREOF |
| EP18762743.5A EP3672968B1 (en) | 2017-08-25 | 2018-08-22 | Solid state form of ribociclib succinate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20240026T1 true HRP20240026T1 (hr) | 2024-03-29 |
Family
ID=63449728
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20240026TT HRP20240026T1 (hr) | 2017-08-25 | 2018-08-22 | Kruti oblik ribociklib sukcinata |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US11155545B2 (hr) |
| EP (2) | EP4327880A3 (hr) |
| KR (1) | KR20200074942A (hr) |
| CA (1) | CA3073936A1 (hr) |
| ES (1) | ES2968174T3 (hr) |
| HR (1) | HRP20240026T1 (hr) |
| IL (1) | IL272859A (hr) |
| MX (1) | MX2020002123A (hr) |
| SI (1) | SI3672968T1 (hr) |
| WO (1) | WO2019040567A1 (hr) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9994579B2 (en) | 2014-12-12 | 2018-06-12 | Crystal Pharmatech Co., Ltd. | Salt of pyrrolo[2,3-D]pyrimidine compound and novel polymorph of salt |
| CA3048036A1 (en) | 2018-07-02 | 2020-01-02 | Apotex Inc | Novel crystalline form of ribociclib succinate |
| WO2020225827A1 (en) * | 2019-05-08 | 2020-11-12 | Mylan Laboratories Limited | Novel polymorphs of ribociclib succinate |
| CN112010857B (zh) * | 2019-05-30 | 2021-11-05 | 常州制药厂有限公司 | 一种瑞博西尼单丁二酸盐的晶型 |
| CN112375081B (zh) * | 2020-11-23 | 2022-04-12 | 中国医学科学院医药生物技术研究所 | 具有抑制CDK4、6或9活性的吡咯[2,3-d]嘧啶衍生物及其制备方法和应用 |
| WO2022207788A2 (en) | 2021-04-01 | 2022-10-06 | Krka, D.D., Novo Mesto | Process for the preparation of ribociclib and pharmaceutically acceptable salts thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2734802C (en) | 2008-08-22 | 2016-05-31 | Novartis Ag | Pyrrolopyrimidine compounds as cdk inhibitors |
| AR083797A1 (es) | 2010-11-10 | 2013-03-20 | Novartis Ag | Succinato de dimetil-amida del acido 7-ciclopentil-2-(5-piperazin-1-il-piridin-2-il-amino)-7h-pirrolo-[2,3-d]pirimidin-6-carboxilico, proceso para prepararla, intermediarios de dicha sintesis y proceso de preparacion de los mismos |
| US9994579B2 (en) * | 2014-12-12 | 2018-06-12 | Crystal Pharmatech Co., Ltd. | Salt of pyrrolo[2,3-D]pyrimidine compound and novel polymorph of salt |
| EP3156406A1 (en) | 2015-10-14 | 2017-04-19 | ratiopharm GmbH | Crystalline forms of ribociclib free base |
| WO2019150181A1 (en) * | 2018-02-05 | 2019-08-08 | Biophore India Pharmaceuticals Pvt Ltd | Improved process for the preparation of 7-cyclopentyl-n, n-dimethyl-2-(5-(piperazin-1-yl) pyridin-2-ylaminuteso)-7h-pyrrolo[2,3-d] pyrimidine-6-carboxamide succinate (ribociclib succinate) and its crystalline forms thereof |
| TWI675662B (zh) * | 2018-05-17 | 2019-11-01 | 中化合成生技股份有限公司 | 瑞博西尼琥珀酸鹽（Ｒｉｂｏｃｉｃｌｉｂ ｓｕｃｃｉｎａｔｅ ｓａｌｔ）晶型Ｂ、Ｃ及Ｄ與其衍生物，以及其等之製造方法與藥物組合物 |
| CN113316471A (zh) | 2019-01-23 | 2021-08-27 | 诺华股份有限公司 | 7-环戊基-2-(5-哌嗪-1-基-吡啶-2-基氨基)-7H-吡咯并[2,3-d]嘧啶-6-羧酸二甲基酰胺的琥珀酸盐的新的结晶形式 |
-
2018
- 2018-08-22 EP EP23205642.4A patent/EP4327880A3/en active Pending
- 2018-08-22 US US16/641,390 patent/US11155545B2/en active Active
- 2018-08-22 SI SI201831040T patent/SI3672968T1/sl unknown
- 2018-08-22 KR KR1020207008143A patent/KR20200074942A/ko not_active Application Discontinuation
- 2018-08-22 MX MX2020002123A patent/MX2020002123A/es unknown
- 2018-08-22 HR HRP20240026TT patent/HRP20240026T1/hr unknown
- 2018-08-22 WO PCT/US2018/047434 patent/WO2019040567A1/en unknown
- 2018-08-22 EP EP18762743.5A patent/EP3672968B1/en active Active
- 2018-08-22 ES ES18762743T patent/ES2968174T3/es active Active
- 2018-08-22 CA CA3073936A patent/CA3073936A1/en active Pending
-
2020
- 2020-02-23 IL IL272859A patent/IL272859A/en unknown
-
2021
- 2021-10-25 US US17/509,140 patent/US20220041598A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20200074942A (ko) | 2020-06-25 |
| US20220041598A1 (en) | 2022-02-10 |
| IL272859A (en) | 2020-04-30 |
| EP4327880A2 (en) | 2024-02-28 |
| MX2020002123A (es) | 2020-09-18 |
| EP4327880A3 (en) | 2024-05-22 |
| US20200190084A1 (en) | 2020-06-18 |
| CA3073936A1 (en) | 2019-02-28 |
| SI3672968T1 (sl) | 2024-03-29 |
| EP3672968A1 (en) | 2020-07-01 |
| WO2019040567A1 (en) | 2019-02-28 |
| US11155545B2 (en) | 2021-10-26 |
| ES2968174T3 (es) | 2024-05-08 |
| EP3672968B1 (en) | 2023-11-01 |
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