JOP20220101A1 - مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS) - Google Patents

مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS)

Info

Publication number
JOP20220101A1
JOP20220101A1 JOP/2022/0101A JOP20220101A JOP20220101A1 JO P20220101 A1 JOP20220101 A1 JO P20220101A1 JO P20220101 A JOP20220101 A JO P20220101A JO P20220101 A1 JOP20220101 A1 JO P20220101A1
Authority
JO
Jordan
Prior art keywords
kras
mutant
pharmaceutically acceptable
kirsten
compounds
Prior art date
Application number
JOP/2022/0101A
Other languages
English (en)
Inventor
Palani Anandan
Hennessy Elisabeth
Bharathan Indu
H Graham Thomas
Henderson Timothy
L Sloman David
Otte Ryan
Gathiaka Symon
Ma Xiaoshen
Han Yongxin
Original Assignee
Merck Sharp & Dohme
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
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of JOP20220101A1 publication Critical patent/JOP20220101A1/ar

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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic 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 four or more hetero rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • 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)
  • 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

يتعلق الكشف الحالي بتوفير مركبات الصيغة (I) صورة الصيغة (I) ، أو ملح منها مقبول صيدلانياً، حيث تكون W1، W2، Y، Z، M، L، Cy، Cz، R1، R2، R3، R4، R2a، Ry، Rz، والرموز السفلية m، n، q، وr كما هو موصوف في الطلب الحالي. يمكن للمركبات أو أملاحها المقبولة صيدلانياً تثبيط الطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS) ومن المتوقع أن يكون لها فائدة كعوامل علاجية، على سبيل المثال، لعلاج السرطان. يوفر الكشف أيضاً تركيبات صيدلانية والتي تشتمل على مركبات الصيغة (I) أو أملاحها المقبولة صيدلانياً. يتعلق الكشف أيضاً بطرق لاستخدام المركبات أو أملاحها المقبولة صيدلانياً في علاج السرطان والوقاية منه ولتحضير مركبات صيدلانية لهذا الغرض.
JOP/2022/0101A 2019-10-28 2020-10-27 مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS) JOP20220101A1 (ar)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US202063030014P 2020-05-26 2020-05-26
PCT/US2020/057496 WO2021086833A1 (en) 2019-10-28 2020-10-27 Small molecule inhibitors of kras g12c mutant

Publications (1)

Publication Number Publication Date
JOP20220101A1 true JOP20220101A1 (ar) 2023-01-30

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2022/0101A JOP20220101A1 (ar) 2019-10-28 2020-10-27 مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS)

Country Status (21)

Country Link
US (3) US11697657B2 (ar)
EP (1) EP4051678B1 (ar)
JP (2) JP7340100B2 (ar)
KR (1) KR20220106980A (ar)
CN (1) CN114867726B (ar)
AU (1) AU2020372881A1 (ar)
BR (1) BR112022007783A8 (ar)
CA (1) CA3158793A1 (ar)
CO (1) CO2022006858A2 (ar)
CR (1) CR20220230A (ar)
DO (1) DOP2022000090A (ar)
EC (1) ECSP22033597A (ar)
GE (2) GEP20247710B (ar)
IL (1) IL292438B2 (ar)
JO (1) JOP20220101A1 (ar)
MX (1) MX2022005053A (ar)
PE (1) PE20221253A1 (ar)
PH (1) PH12022551027A1 (ar)
UA (1) UA129778C2 (ar)
WO (1) WO2021086833A1 (ar)
ZA (1) ZA202205938B (ar)

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