PE20230388A1 - CRYSTALLINE RET INHIBITOR - Google Patents

CRYSTALLINE RET INHIBITOR

Info

Publication number
PE20230388A1
PE20230388A1 PE2022002417A PE2022002417A PE20230388A1 PE 20230388 A1 PE20230388 A1 PE 20230388A1 PE 2022002417 A PE2022002417 A PE 2022002417A PE 2022002417 A PE2022002417 A PE 2022002417A PE 20230388 A1 PE20230388 A1 PE 20230388A1
Authority
PE
Peru
Prior art keywords
crystalline
ret inhibitor
ppm
peaks
selpercatinib
Prior art date
Application number
PE2022002417A
Other languages
Spanish (es)
Inventor
Rajni Miglani Bhardwaj
Mark Steven Kerr
Douglas Patton Kjell
Jeremy Miles Merritt
Jon Gordon Selbo
Shekhar Krishna Viswanath
Original Assignee
Loxo Oncology Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Loxo Oncology Inc filed Critical Loxo Oncology Inc
Publication of PE20230388A1 publication Critical patent/PE20230388A1/en

Links

Classifications

    • 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Semiconductor Lasers (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Una forma cristalina de selpercatinib, que se caracteriza por al menos uno de: (a) un patron de difraccion de rayos X en polvo (XRPD) que comprende un pico a 21,1 y uno o mas picos a 17,1 , 17,7 y 19,8 0,2 2? medidos utilizando una longitud de onda de rayos X de 1,5418 ; o (b) un espectro de NMR de 13C en estado solido que comprende picos referidos a la resonancia de campo alto de adamantano (? = 29,5 ppm) a: 28,0, 48,0, 80,4, 106,8, 130,2 y 134,9ppm ( 0,2 ppm, respectivamente).A crystalline form of selpercatinib, characterized by at least one of: (a) an X-ray powder diffraction (XRPD) pattern comprising a peak at 21.1 and one or more peaks at 17.1, 17, 7 and 19.8 0.2 2? measured using an X-ray wavelength of 1.5418; or (b) a solid state 13C NMR spectrum comprising peaks referred to the high field resonance of adamantane (? = 29.5 ppm) at: 28.0, 48.0, 80.4, 106.8 , 130.2 and 134.9ppm (0.2 ppm, respectively).

PE2022002417A 2020-04-17 2021-04-09 CRYSTALLINE RET INHIBITOR PE20230388A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063011701P 2020-04-17 2020-04-17
US202163151354P 2021-02-19 2021-02-19
PCT/US2021/026611 WO2021211380A1 (en) 2020-04-17 2021-04-09 Crystalline ret inhibitor

Publications (1)

Publication Number Publication Date
PE20230388A1 true PE20230388A1 (en) 2023-03-06

Family

ID=75747118

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002417A PE20230388A1 (en) 2020-04-17 2021-04-09 CRYSTALLINE RET INHIBITOR

Country Status (17)

Country Link
EP (1) EP4136090A1 (en)
JP (1) JP2023522012A (en)
KR (1) KR20230002706A (en)
CN (1) CN115916791A (en)
AU (1) AU2021255488B2 (en)
BR (1) BR112022020446A2 (en)
CA (1) CA3174316A1 (en)
CL (1) CL2022002849A1 (en)
CO (1) CO2022014882A2 (en)
CR (1) CR20220520A (en)
DO (1) DOP2022000221A (en)
EC (1) ECSP22080982A (en)
IL (1) IL297212A (en)
MX (1) MX2022012952A (en)
PE (1) PE20230388A1 (en)
TW (1) TW202202501A (en)
WO (1) WO2021211380A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022069357A1 (en) * 2020-10-01 2022-04-07 Sandoz Ag Crystalline form of selpercatinib
MX2024007017A (en) 2021-12-13 2024-06-19 Loxo Oncology Inc Processes for the preparation of the crystalline form a of selpercatinib. a ret inhibitor.
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI704148B (en) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TWI783057B (en) * 2017-10-10 2022-11-11 美商絡速藥業公司 Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
TWI791053B (en) * 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 Crystalline forms of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and pharmaceutical composition thereof
TW202410896A (en) * 2017-10-10 2024-03-16 美商絡速藥業公司 Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
CN114380825B (en) * 2018-09-30 2024-02-13 北京志健金瑞生物医药科技有限公司 Substituted pyrazole condensed ring derivative and preparation method and application thereof
CN111004257B (en) * 2019-12-24 2021-06-29 武汉九州钰民医药科技有限公司 Method for preparing RET inhibitor Selpercatinib

Also Published As

Publication number Publication date
TW202202501A (en) 2022-01-16
CA3174316A1 (en) 2021-10-21
EP4136090A1 (en) 2023-02-22
BR112022020446A2 (en) 2022-11-29
AU2021255488A1 (en) 2022-11-10
ECSP22080982A (en) 2023-01-31
DOP2022000221A (en) 2023-01-15
MX2022012952A (en) 2023-01-11
JP2023522012A (en) 2023-05-26
AU2021255488B2 (en) 2024-05-30
CR20220520A (en) 2022-11-15
WO2021211380A1 (en) 2021-10-21
CL2022002849A1 (en) 2023-06-16
CN115916791A (en) 2023-04-04
CO2022014882A2 (en) 2022-10-31
KR20230002706A (en) 2023-01-05
IL297212A (en) 2022-12-01

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