CA3142430A1 - Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor - Google Patents

Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor Download PDF

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Publication number
CA3142430A1
CA3142430A1 CA3142430A CA3142430A CA3142430A1 CA 3142430 A1 CA3142430 A1 CA 3142430A1 CA 3142430 A CA3142430 A CA 3142430A CA 3142430 A CA3142430 A CA 3142430A CA 3142430 A1 CA3142430 A1 CA 3142430A1
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Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
crystalline form
pharmaceutical composition
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Pending
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CA3142430A
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English (en)
French (fr)
Inventor
Shaoling Li
Steven G. Ballmer
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Revolution Medicines Inc
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Revolution Medicines Inc
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Publication of CA3142430A1 publication Critical patent/CA3142430A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • 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)
  • 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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA3142430A 2019-06-07 2020-06-04 Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor Pending CA3142430A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962858837P 2019-06-07 2019-06-07
US62/858,837 2019-06-07
PCT/US2020/036137 WO2020247643A1 (en) 2019-06-07 2020-06-04 Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor

Publications (1)

Publication Number Publication Date
CA3142430A1 true CA3142430A1 (en) 2020-12-10

Family

ID=71787182

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3142430A Pending CA3142430A1 (en) 2019-06-07 2020-06-04 Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor

Country Status (15)

Country Link
US (2) US11220501B2 (https=)
EP (1) EP3980128A1 (https=)
JP (2) JP2022534788A (https=)
KR (1) KR20220019017A (https=)
CN (2) CN115141205A (https=)
AU (1) AU2020288631A1 (https=)
BR (1) BR112021022635A2 (https=)
CA (1) CA3142430A1 (https=)
IL (1) IL288568A (https=)
MA (1) MA56113A (https=)
MX (1) MX2021014855A (https=)
PH (1) PH12021552902A1 (https=)
SG (1) SG11202112461QA (https=)
TW (1) TW202112785A (https=)
WO (1) WO2020247643A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
CN115141205A (zh) 2019-06-07 2022-10-04 锐新医药公司 Shp2抑制剂的固体形式
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
TW200716594A (en) * 2005-04-18 2007-05-01 Neurogen Corp Substituted heteroaryl CB1 antagonists
NZ713361A (en) * 2009-08-17 2017-06-30 Memorial Sloan Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
ES2699351T3 (es) * 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EP4302834A3 (en) * 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
MX2020010719A (es) 2018-04-10 2020-11-06 Revolution Medicines Inc Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2.
CN115141205A (zh) 2019-06-07 2022-10-04 锐新医药公司 Shp2抑制剂的固体形式

Also Published As

Publication number Publication date
SG11202112461QA (en) 2021-12-30
US12528807B2 (en) 2026-01-20
WO2020247643A1 (en) 2020-12-10
CN114190090A (zh) 2022-03-15
JP2025138706A (ja) 2025-09-25
US11220501B2 (en) 2022-01-11
AU2020288631A1 (en) 2021-12-09
BR112021022635A2 (pt) 2022-01-04
TW202112785A (zh) 2021-04-01
CN115141205A (zh) 2022-10-04
PH12021552902A1 (en) 2022-04-04
MA56113A (fr) 2022-04-13
IL288568A (en) 2022-02-01
EP3980128A1 (en) 2022-04-13
JP2022534788A (ja) 2022-08-03
KR20220019017A (ko) 2022-02-15
MX2021014855A (es) 2022-01-18
US20210253574A1 (en) 2021-08-19
US20220298159A1 (en) 2022-09-22

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