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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Canada
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 date
Application filed by Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of CA3142430A1 publication Critical patent/CA3142430A1/en
Pending legal-status Critical Current

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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
    • 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
    • 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
    • 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)
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
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

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
CA2606288A1 (en) * 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
KR101906146B1 (ko) * 2009-08-17 2018-10-10 메모리얼 슬로안-케터링 캔서 센터 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP6523303B2 (ja) * 2014-01-17 2019-05-29 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−ピリダジン／トリアジン−３−イル−ピペラジン／ピペリジン／ピロリジン誘導体およびその組成物
KR102598895B1 (ko) * 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
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

Also Published As

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
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
JP2022534788A (ja) 2022-08-03
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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