CN115141205A - Shp2抑制剂的固体形式 - Google Patents

Shp2抑制剂的固体形式 Download PDF

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Publication number
CN115141205A
CN115141205A CN202210564150.XA CN202210564150A CN115141205A CN 115141205 A CN115141205 A CN 115141205A CN 202210564150 A CN202210564150 A CN 202210564150A CN 115141205 A CN115141205 A CN 115141205A
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China
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compound
pharmaceutically acceptable
acceptable salt
present disclosure
crystalline form
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Pending
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CN202210564150.XA
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English (en)
Chinese (zh)
Inventor
李少玲
S·G·鲍尔默
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Ruixin Pharmaceutical Co
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Ruixin Pharmaceutical Co
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Publication of CN115141205A publication Critical patent/CN115141205A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202210564150.XA 2019-06-07 2020-06-04 Shp2抑制剂的固体形式 Pending CN115141205A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962858837P 2019-06-07 2019-06-07
US62/858,837 2019-06-07
CN202080054905.0A CN114190090A (zh) 2019-06-07 2020-06-04 Shp2抑制剂{6-[(2-氨基-3-氯吡啶-4-基)硫烷基]-3-[(3s,4s)-4-氨基-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-8-基]-5-甲基吡嗪-2-基}甲醇的固体形式
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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN202080054905.0A Division CN114190090A (zh) 2019-06-07 2020-06-04 Shp2抑制剂{6-[(2-氨基-3-氯吡啶-4-基)硫烷基]-3-[(3s,4s)-4-氨基-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-8-基]-5-甲基吡嗪-2-基}甲醇的固体形式

Publications (1)

Publication Number Publication Date
CN115141205A true CN115141205A (zh) 2022-10-04

Family

ID=71787182

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202210564150.XA Pending CN115141205A (zh) 2019-06-07 2020-06-04 Shp2抑制剂的固体形式
CN202080054905.0A Pending CN114190090A (zh) 2019-06-07 2020-06-04 Shp2抑制剂{6-[(2-氨基-3-氯吡啶-4-基)硫烷基]-3-[(3s,4s)-4-氨基-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-8-基]-5-甲基吡嗪-2-基}甲醇的固体形式

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202080054905.0A Pending CN114190090A (zh) 2019-06-07 2020-06-04 Shp2抑制剂{6-[(2-氨基-3-氯吡啶-4-基)硫烷基]-3-[(3s,4s)-4-氨基-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-8-基]-5-甲基吡嗪-2-基}甲醇的固体形式

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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (8)

* 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
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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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
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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