AU2020211071A1 - New crystalline forms of a succinate salt of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide - Google Patents

New crystalline forms of a succinate salt of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide Download PDF

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AU2020211071A1
AU2020211071A1 AU2020211071A AU2020211071A AU2020211071A1 AU 2020211071 A1 AU2020211071 A1 AU 2020211071A1 AU 2020211071 A AU2020211071 A AU 2020211071A AU 2020211071 A AU2020211071 A AU 2020211071A AU 2020211071 A1 AU2020211071 A1 AU 2020211071A1
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Prior art keywords
modification
ribociclib
crystalline form
salt
diffraction pattern
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Arnaud Grandeury
Nilesh Patel
Frank Schaefer
Daniel Zimmermann
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Novartis AG
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Novartis AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2020211071A 2019-01-23 2020-01-23 New crystalline forms of a succinate salt of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide Abandoned AU2020211071A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023200724A AU2023200724B2 (en) 2019-01-23 2023-02-10 New crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962795799P 2019-01-23 2019-01-23
US62/795,799 2019-01-23
PCT/IB2020/050544 WO2020152629A1 (en) 2019-01-23 2020-01-23 New crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide

Related Child Applications (1)

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AU2023200724A Division AU2023200724B2 (en) 2019-01-23 2023-02-10 New crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide

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AU2020211071A Abandoned AU2020211071A1 (en) 2019-01-23 2020-01-23 New crystalline forms of a succinate salt of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide
AU2023200724A Active AU2023200724B2 (en) 2019-01-23 2023-02-10 New crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine -6-carboxylic acid dimethylamide

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Country Status (9)

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US (2) US12390468B2 (https=)
EP (1) EP3914353A1 (https=)
JP (2) JP2022517842A (https=)
KR (1) KR20210119444A (https=)
CN (1) CN113316471A (https=)
AU (2) AU2020211071A1 (https=)
CA (1) CA3124015A1 (https=)
IL (1) IL284510B2 (https=)
WO (1) WO2020152629A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20240026T1 (hr) 2017-08-25 2024-03-29 Assia Chemical Industries Ltd Kruti oblik ribociklib sukcinata
US12390468B2 (en) 2019-01-23 2025-08-19 Novartis Ag Crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide
EP4626890A1 (en) 2022-12-01 2025-10-08 KRKA, d.d., Novo mesto Ribociclib salts and formulations thereof
WO2025041004A1 (en) * 2023-08-18 2025-02-27 Alembic Pharmaceuticals Limited Polymorph of ribociclib salt
WO2025144118A1 (en) * 2023-12-27 2025-07-03 Deva Holding Novel polymorph of ribociclib dihydrochloride dihydrate and method of preparation
TW202602868A (zh) 2024-04-15 2026-01-16 瑞士商諾華公司 瑞波西利的藥物組成物

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ITMI992711A1 (it) 1999-12-27 2001-06-27 Novartis Ag Composti organici
EA012926B1 (ru) 2001-12-20 2010-02-26 Оси Фармасьютикалз, Инк. Пирролопиримидиновые соединения, относящиеся к a-селективным антагонистам, их синтез и применение
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
EP1781647A2 (en) 2004-07-22 2007-05-09 Astex Therapeutics Limited Thiazole and isothiazole derivatives as protein kinase inhibitors
RU2468988C2 (ru) 2005-07-22 2012-12-10 Квалкомм Инкорпорэйтэд Устройства мэмс, имеющие поддерживающие структуры, и способы их изготовления
AU2006331765A1 (en) 2005-12-22 2007-07-05 Wyeth Substituted isoquinoline-1,3(2H,4H)-diones, 1-thioxo-1,4-dihydro-2H-isoquinoline-3-ones and 1,4-dihydro-3(2H)-isoquinolones and use thereof as kinase inhibitor
TWI398252B (zh) 2006-05-26 2013-06-11 諾華公司 吡咯并嘧啶化合物及其用途
ES2522346T3 (es) 2008-08-22 2014-11-14 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de CDK
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
US20120115878A1 (en) 2010-11-10 2012-05-10 John Vincent Calienni Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺
EP2818007B1 (en) 2012-02-24 2022-02-23 Nokia Technologies Oy Method and apparatus for establishing a connection with an access network based upon access network interworking information
CN105111215B (zh) * 2014-12-12 2019-06-18 苏州晶云药物科技股份有限公司 一种周期蛋白依赖性激酶抑制剂的晶型及其制备方法
US10138250B2 (en) * 2014-12-12 2018-11-27 Crystal Pharmatech Co., Ltd. Salt of pyrrolo[2,3-D]pyrimidine compound and novel polymorph of salt
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
EP3279201B1 (en) 2015-04-01 2019-10-23 Crystal Pharmatech Co., Ltd. Cdk inhibitor, eutectic crystal of mek inhibitor, and preparation method therefor
HRP20240026T1 (hr) 2017-08-25 2024-03-29 Assia Chemical Industries Ltd Kruti oblik ribociklib sukcinata
WO2019111160A1 (en) * 2017-12-04 2019-06-13 Sun Pharmaceutical Industries Limited Crystalline forms of ribociclib succinate
US11111250B2 (en) * 2017-12-22 2021-09-07 Shilpa Meicare Limited Polymorphs of Ribociclib mono succinate
US11414421B2 (en) 2018-01-20 2022-08-16 Natco Pharma Ltd Process for the preparation of ribociclib succinate and its novel 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
US12390468B2 (en) 2019-01-23 2025-08-19 Novartis Ag Crystalline forms of a succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide

Also Published As

Publication number Publication date
US20250281492A1 (en) 2025-09-11
AU2023200724B2 (en) 2025-01-23
WO2020152629A1 (en) 2020-07-30
IL284510B2 (en) 2025-10-01
IL284510A (en) 2021-08-31
JP2022517842A (ja) 2022-03-10
IL284510B1 (en) 2025-06-01
JP2024099797A (ja) 2024-07-25
AU2023200724A1 (en) 2023-03-09
EP3914353A1 (en) 2021-12-01
CN113316471A (zh) 2021-08-27
US12390468B2 (en) 2025-08-19
KR20210119444A (ko) 2021-10-05
CA3124015A1 (en) 2020-07-30
US20230042479A1 (en) 2023-02-09

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