TW202334136A - PI3Kα抑制劑及其製造與使用方法 - Google Patents

PI3Kα抑制劑及其製造與使用方法 Download PDF

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Publication number
TW202334136A
TW202334136A TW111141786A TW111141786A TW202334136A TW 202334136 A TW202334136 A TW 202334136A TW 111141786 A TW111141786 A TW 111141786A TW 111141786 A TW111141786 A TW 111141786A TW 202334136 A TW202334136 A TW 202334136A
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TW
Taiwan
Prior art keywords
compound
iii
formula
solid
crystalline
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TW111141786A
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English (en)
Chinese (zh)
Inventor
安德烈 蘭斯卡比
亞歷山卓 波席歐
蘇藍卓 P 辛
慶林 車
蔣思懿
何紅燕
周秋湘
周加加
林沅
古偉
呂敏
周雲飛
龔熙見
陳佳輝
王曉紅
殷昌波
Original Assignee
美商傳達治療有限公司
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Application filed by 美商傳達治療有限公司 filed Critical 美商傳達治療有限公司
Publication of TW202334136A publication Critical patent/TW202334136A/zh

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    • 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
    • C07D471/04—Ortho-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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW111141786A 2021-11-03 2022-11-02 PI3Kα抑制劑及其製造與使用方法 TW202334136A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202163263474P 2021-11-03 2021-11-03
US63/263,474 2021-11-03
CN2021128533 2021-11-03
WOPCT/CN2021/128533 2021-11-03

Publications (1)

Publication Number Publication Date
TW202334136A true TW202334136A (zh) 2023-09-01

Family

ID=86242193

Family Applications (1)

Application Number Title Priority Date Filing Date
TW111141786A TW202334136A (zh) 2021-11-03 2022-11-02 PI3Kα抑制劑及其製造與使用方法

Country Status (13)

Country Link
US (1) US20260125374A1 (enExample)
EP (1) EP4426314A4 (enExample)
JP (1) JP2024540303A (enExample)
KR (1) KR20240112283A (enExample)
CN (1) CN118401245A (enExample)
AU (1) AU2022381187A1 (enExample)
CA (1) CA3236861A1 (enExample)
CL (1) CL2024001364A1 (enExample)
IL (1) IL312466A (enExample)
MX (1) MX2024005429A (enExample)
PE (1) PE20250676A1 (enExample)
TW (1) TW202334136A (enExample)
WO (1) WO2023081757A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021263914B2 (en) 2020-04-29 2026-07-23 D.E. Shaw Research, Llc PI3K-α inhibitors and methods of use thereof
WO2024055992A1 (zh) * 2022-09-14 2024-03-21 南京再明医药有限公司 三环化合物及其应用
JP2025538147A (ja) 2022-11-02 2025-11-26 ペトラ・ファーマ・コーポレイション 疾患の治療のためのホスホイノシチド3-キナーゼ(pi3k)のアロステリックポケット及びオルソステリックポケットの標的化
WO2024233256A1 (en) 2023-05-05 2024-11-14 Eli Lilly And Company Imlunestrant or salts thereof for use in treating and preventing central nervous system (cns) metastases in subjects having er+ breast cancer

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010007100A1 (en) * 2008-07-15 2010-01-21 Cellzome Ltd 7-substituted amino triazoles as pi3k inhibitors
JP6472803B2 (ja) * 2013-09-05 2019-02-20 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft トリアゾロピリジン化合物、その組成物及び使用方法
WO2017000277A1 (en) * 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
EP3931188B1 (en) * 2019-02-26 2023-08-30 Boehringer Ingelheim International GmbH New isoindolinone substituted indoles and derivatives as ras inhibitors
AU2021263914B2 (en) * 2020-04-29 2026-07-23 D.E. Shaw Research, Llc PI3K-α inhibitors and methods of use thereof

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Publication number Publication date
CL2024001364A1 (es) 2024-10-25
KR20240112283A (ko) 2024-07-18
EP4426314A1 (en) 2024-09-11
IL312466A (en) 2024-06-01
MX2024005429A (es) 2024-05-21
CN118401245A (zh) 2024-07-26
JP2024540303A (ja) 2024-10-31
EP4426314A4 (en) 2025-10-01
US20260125374A1 (en) 2026-05-07
PE20250676A1 (es) 2025-03-04
CA3236861A1 (en) 2023-05-11
AU2022381187A1 (en) 2024-05-16
WO2023081757A1 (en) 2023-05-11

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