JP2022534788A - Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態 - Google Patents

Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態 Download PDF

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JP2022534788A
JP2022534788A JP2021571896A JP2021571896A JP2022534788A JP 2022534788 A JP2022534788 A JP 2022534788A JP 2021571896 A JP2021571896 A JP 2021571896A JP 2021571896 A JP2021571896 A JP 2021571896A JP 2022534788 A JP2022534788 A JP 2022534788A
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compound
pharmaceutically acceptable
acceptable salt
crystalline form
ray powder
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JP2022534788A5 (https=
JPWO2020247643A5 (https=
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シャオリン・リー
スティーブン・ジー・ボールマー
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Revolution Medicines Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D471/10—Spiro-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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further 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

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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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2021571896A 2019-06-07 2020-06-04 Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態 Pending JP2022534788A (ja)

Priority Applications (1)

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JP2025101917A JP2025138706A (ja) 2019-06-07 2025-06-18 Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態

Applications Claiming Priority (3)

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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

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JP2025101917A Division JP2025138706A (ja) 2019-06-07 2025-06-18 Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態

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JP2022534788A5 JP2022534788A5 (https=) 2023-06-07
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JP2021571896A Pending JP2022534788A (ja) 2019-06-07 2020-06-04 Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態
JP2025101917A Pending JP2025138706A (ja) 2019-06-07 2025-06-18 Ｓｈｐ２阻害物質である｛６－［（２－アミノ－３－クロロピリジン－４－イル）スルファニル］－３－［（３ｓ，４ｓ）－４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル］－５－メチルピラジン－２－イル｝メタノールの固体形態

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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
EP3980128A1 (en) 2019-06-07 2022-04-13 Revolution Medicines, Inc. 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
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
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers

Citations (5)

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Publication number Priority date Publication date Assignee Title
JP2008536950A (ja) * 2005-04-18 2008-09-11 ニューロジェン・コーポレーション 置換ヘテロアリールのｃｂ１拮抗薬
JP2013502424A (ja) * 2009-08-17 2013-01-24 メモリアル スローン−ケタリング キャンサー センター 熱ショックタンパク質結合化合物、組成物、およびそれらを製造するための方法
WO2015107495A1 (en) * 2014-01-17 2015-07-23 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
WO2015107493A1 (en) * 2014-01-17 2015-07-23 Novartis Ag 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
WO2018013597A1 (en) * 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors

Family Cites Families (4)

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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
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
SG11202009793TA (en) 2018-04-10 2020-10-29 Revolution Medicines Inc Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
EP3980128A1 (en) * 2019-06-07 2022-04-13 Revolution Medicines, Inc. 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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008536950A (ja) * 2005-04-18 2008-09-11 ニューロジェン・コーポレーション 置換ヘテロアリールのｃｂ１拮抗薬
JP2013502424A (ja) * 2009-08-17 2013-01-24 メモリアル スローン−ケタリング キャンサー センター 熱ショックタンパク質結合化合物、組成物、およびそれらを製造するための方法
WO2015107495A1 (en) * 2014-01-17 2015-07-23 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
WO2015107493A1 (en) * 2014-01-17 2015-07-23 Novartis Ag 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
WO2018013597A1 (en) * 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors

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厚生労働省医薬局審査管理課長: "安定性試験ガイドラインの改定について", 医薬審発第０６０３００１号, JPN6023001926, 3 June 2003 (2003-06-03), pages 1 - 24, ISSN: 0005645468 *
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Publication number Publication date
WO2020247643A1 (en) 2020-12-10
JP2025138706A (ja) 2025-09-25
SG11202112461QA (en) 2021-12-30
AU2020288631A1 (en) 2021-12-09
BR112021022635A2 (pt) 2022-01-04
CA3142430A1 (en) 2020-12-10
MX2021014855A (es) 2022-01-18
US12528807B2 (en) 2026-01-20
EP3980128A1 (en) 2022-04-13
MA56113A (fr) 2022-04-13
PH12021552902A1 (en) 2022-04-04
IL288568A (en) 2022-02-01
US11220501B2 (en) 2022-01-11
CN115141205A (zh) 2022-10-04
US20220298159A1 (en) 2022-09-22
KR20220019017A (ko) 2022-02-15
TW202112785A (zh) 2021-04-01
US20210253574A1 (en) 2021-08-19
CN114190090A (zh) 2022-03-15

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