IL324622A - Pyrazolo[3,4-f]quinazoline derivatives as modulators of the KRAS G12D mutation for cancer treatment - Google Patents

Pyrazolo[3,4-f]quinazoline derivatives as modulators of the KRAS G12D mutation for cancer treatment

Info

Publication number
IL324622A
IL324622A IL324622A IL32462225A IL324622A IL 324622 A IL324622 A IL 324622A IL 324622 A IL324622 A IL 324622A IL 32462225 A IL32462225 A IL 32462225A IL 324622 A IL324622 A IL 324622A
Authority
IL
Israel
Prior art keywords
alkyl
pct
compound
independently
groups
Prior art date
Application number
IL324622A
Other languages
English (en)
Hebrew (he)
Inventor
Paula Jackson
Helen Elizabeth Aylott
Clifford D Jones
Inder Bhamra
James Ryan
Daniel J Leng
Kelvin Ho
Original Assignee
Jazz Pharmaceuticals Ireland Ltd
Paula Jackson
Helen Elizabeth Aylott
Clifford D Jones
Inder Bhamra
James Ryan
Daniel J Leng
Kelvin Ho
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB2307077.4A external-priority patent/GB202307077D0/en
Priority claimed from GBGB2319678.5A external-priority patent/GB202319678D0/en
Application filed by Jazz Pharmaceuticals Ireland Ltd, Paula Jackson, Helen Elizabeth Aylott, Clifford D Jones, Inder Bhamra, James Ryan, Daniel J Leng, Kelvin Ho filed Critical Jazz Pharmaceuticals Ireland Ltd
Publication of IL324622A publication Critical patent/IL324622A/en

Links

Classifications

    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
IL324622A 2023-05-12 2024-05-11 Pyrazolo[3,4-f]quinazoline derivatives as modulators of the KRAS G12D mutation for cancer treatment IL324622A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB2307077.4A GB202307077D0 (en) 2023-05-12 2023-05-12 Compounds
GBGB2319678.5A GB202319678D0 (en) 2023-12-20 2023-12-20 Compounds
PCT/IB2024/054597 WO2024236452A1 (fr) 2023-05-12 2024-05-11 Dérivés de pyrazolo[4,3-f]quinazoline en tant que modulateurs de mutants kras g12d utiles pour le traitement du cancer

Publications (1)

Publication Number Publication Date
IL324622A true IL324622A (en) 2026-01-01

Family

ID=91276778

Family Applications (1)

Application Number Title Priority Date Filing Date
IL324622A IL324622A (en) 2023-05-12 2024-05-11 Pyrazolo[3,4-f]quinazoline derivatives as modulators of the KRAS G12D mutation for cancer treatment

Country Status (8)

Country Link
EP (1) EP4709729A1 (fr)
KR (1) KR20260015208A (fr)
CN (1) CN121511246A (fr)
AU (1) AU2024272361A1 (fr)
IL (1) IL324622A (fr)
MX (1) MX2025013539A (fr)
TW (1) TW202500142A (fr)
WO (1) WO2024236452A1 (fr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (fr) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Procédés de traitement d'une maladie ou d'un trouble lié à la protéine ras
WO2025265060A1 (fr) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Compositions thérapeutiques et procédés de gestion d'effets liés au traitement
WO2026006747A1 (fr) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Inhibiteurs de ras
WO2026015790A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras
WO2026015796A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras
WO2026015801A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble liés à ras
WO2026015825A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Utilisation d'un inhibiteur de ras pour traiter le cancer du pancréas
WO2026035945A1 (fr) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Conjugués médicamenteux induits par covalence ciblant kras et comprenant une charge utile de topoisomérase
WO2026035947A1 (fr) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Conjugués médicamenteux à induction par liaison covalente ciblant kras comprenant une charge utile de topo-isomérase
WO2026050446A1 (fr) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Inhibiteurs de ras
WO2026064520A1 (fr) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Conjugués médicamenteux à induction covalente ciblant kras et comprenant une charge utile inhibitrice de tubuline
WO2026064527A1 (fr) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Conjugués médicamenteux à induction covalente ciblant kras comprenant une charge utile d'inhibiteur de tubuline
WO2026072904A2 (fr) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions et méthodes de traitement du cancer du poumon

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021063346A1 (fr) * 2019-09-30 2021-04-08 上海迪诺医药科技有限公司 Inhibiteur de kras g12c et application associée
WO2022184178A1 (fr) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Inhibiteurs de kras g12d
US20240300980A1 (en) * 2021-05-22 2024-09-12 Shanghai Kechow Pharma, Inc. Heterocyclic compounds as kras inhibitor, and preparation therefor and use thereof in treatment
BR112023024906A2 (pt) 2021-05-28 2024-02-15 Redx Pharma Plc Compostos
BR112023025869A2 (pt) 2021-06-10 2024-02-27 Redx Pharma Plc Derivados de quinazolina úteis como inibidores de ras
WO2024123102A1 (fr) * 2022-12-07 2024-06-13 에스케이바이오팜 주식회사 Nouveau composé tricyclique en tant qu'inhibiteur de kras g12d, et son utilisation

Also Published As

Publication number Publication date
MX2025013539A (es) 2026-03-02
AU2024272361A1 (en) 2025-12-18
EP4709729A1 (fr) 2026-03-18
CN121511246A (zh) 2026-02-10
WO2024236452A1 (fr) 2024-11-21
TW202500142A (zh) 2025-01-01
KR20260015208A (ko) 2026-02-02

Similar Documents

Publication Publication Date Title
IL324622A (en) Pyrazolo[3,4-f]quinazoline derivatives as modulators of the KRAS G12D mutation for cancer treatment
EP4347589A2 (fr) Composés pyrido[4,3-d]pyrimidine capables d'inhiber des protéines mutantes kras
AU2022288151A1 (en) Quinazoline derivatives useful as ras inhibitiors
EP4626888A1 (fr) Composés
KR20250024842A (ko) 아자퀴나졸린 범-kras 억제제
CN105732636B (zh) 杂芳化合物及其在药物中的应用
TWI675833B (zh) 布魯頓氏(bruton’s)酪胺酸激酶之聯芳基抑制劑
KR20240128852A (ko) 암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체
CN117263942A (zh) Shp2磷酸酶抑制剂及其使用方法
WO2014188173A1 (fr) Dérivés pyrazolopyrimidine utiles comme inhibiteurs de la tyrosine kinase de bruton
CN102803265A (zh) 吡咯并吡嗪激酶抑制剂
JP2009514882A (ja) がんおよび他の過剰増殖性疾患の処置のためのピロロ[2,1−f][1,2,4]トリアジン−4−イルアミンIGF−1Rキナーゼ阻害剤
CN111527090B (zh) 作为p2x3抑制剂的吡唑并-吡咯并-嘧啶-二酮衍生物
CA2873975A1 (fr) Thienopyrimidines substituees
CN112135818A (zh) 4-羟基哌啶衍生物及其作为泛素特异性蛋白酶19(usp19)的抑制剂的用途
WO2025163494A1 (fr) Azines condensées pour le traitement du cancer
CN113365696A (zh) 药物化合物和其作为泛素特异性蛋白酶19(usp19)抑制剂的用途
CN116829151A (zh) 氮杂喹唑啉泛KRas抑制剂
CN117460730A (zh) 能够抑制kras突变蛋白的吡啶并[4,3-d]嘧啶化合物
CN117425658A (zh) 用作ras抑制剂的喹唑啉衍生物
JP2026059772A (ja) ピリド[4,3-d]ピリミジン化合物
US20250235456A1 (en) Methods of use for aza-quinazoline compounds
TW202545531A (zh) 氮—喹唑啉化合物之使用方法
HK40030438A (en) Novel pyrazolo-pyrrolo-pyrimidine-dione derivatives as p2x3 inhibitors
HK1178536A (en) Pyrrolopyrazine kinase inhibitors