JOP20220142A1 - مثبطات kras g12c - Google Patents

مثبطات kras g12c

Info

Publication number
JOP20220142A1
JOP20220142A1 JOP/2022/0142A JOP20220142A JOP20220142A1 JO P20220142 A1 JOP20220142 A1 JO P20220142A1 JO P20220142 A JOP20220142 A JO P20220142A JO P20220142 A1 JOP20220142 A1 JO P20220142A1
Authority
JO
Jordan
Prior art keywords
kras
inhibitors
compounds
salts
cancer
Prior art date
Application number
JOP/2022/0142A
Other languages
English (en)
Inventor
Serge Louis Boulet
Sheng-Bin Peng
Chong Si
Deqi Guo
Kevin Charles Fortner
David Michael Hyman
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of JOP20220142A1 publication Critical patent/JOP20220142A1/ar
Application granted granted Critical
Publication of JOP20220142B1 publication Critical patent/JOP20220142B1/ar

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Classifications

    • 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
    • C07D498/04Ortho-condensed systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/495Heterocyclic 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/243Platinum; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Inorganic Chemistry (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

يتعلق الاختراع الحالي بتوفير مركبات لها الصيغة: حيث R1، R2، R3، R4، R5، A، B، وY تعد كما هي موصوفة هنا، أملاح مقبولة صيدليًا منها، وطرق استخدام هذه المركبات وأملاح لمعالجة مرضى السرطان.
JOJO/P/2022/0142A 2019-12-11 2022-06-09 مثبطات kras g12c JOP20220142B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962946586P 2019-12-11 2019-12-11
PCT/US2020/063272 WO2021118877A1 (en) 2019-12-11 2020-12-04 Kras g12c inhibitors

Publications (2)

Publication Number Publication Date
JOP20220142A1 true JOP20220142A1 (ar) 2023-01-30
JOP20220142B1 JOP20220142B1 (ar) 2025-10-01

Family

ID=74106135

Family Applications (2)

Application Number Title Priority Date Filing Date
JOJO/P/2022/0142A JOP20220142B1 (ar) 2019-12-11 2022-06-09 مثبطات kras g12c
JOJO/P/2024/0216A JOP20240216A1 (ar) 2019-12-11 2024-09-30 مثبطات kras g12c

Family Applications After (1)

Application Number Title Priority Date Filing Date
JOJO/P/2024/0216A JOP20240216A1 (ar) 2019-12-11 2024-09-30 مثبطات kras g12c

Country Status (34)

Country Link
US (2) US11731984B2 (ar)
EP (1) EP3886991B1 (ar)
JP (1) JP7023421B2 (ar)
KR (1) KR102546592B1 (ar)
CN (2) CN117820333A (ar)
AR (1) AR120700A1 (ar)
AU (2) AU2020402701B2 (ar)
CA (1) CA3161162A1 (ar)
CL (1) CL2022001513A1 (ar)
CO (1) CO2022008091A2 (ar)
CR (1) CR20220258A (ar)
DK (1) DK3886991T3 (ar)
DO (1) DOP2022000117A (ar)
EC (1) ECSP22046699A (ar)
ES (1) ES2929700T3 (ar)
HR (1) HRP20221301T1 (ar)
HU (1) HUE060684T2 (ar)
IL (2) IL293394B2 (ar)
JO (2) JOP20220142B1 (ar)
LT (1) LT3886991T (ar)
MA (1) MA54327B1 (ar)
MD (1) MD3886991T2 (ar)
MX (2) MX2022006986A (ar)
PE (1) PE20230238A1 (ar)
PH (1) PH12022551424A1 (ar)
PL (1) PL3886991T3 (ar)
PT (1) PT3886991T (ar)
RS (1) RS63719B1 (ar)
SA (1) SA522432955B1 (ar)
SI (1) SI3886991T1 (ar)
TW (1) TWI765448B (ar)
UA (1) UA128806C2 (ar)
WO (1) WO2021118877A1 (ar)
ZA (1) ZA202205218B (ar)

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LT3886991T (lt) 2022-11-10
JP2022508469A (ja) 2022-01-19
CN114828964B (zh) 2023-11-24
PT3886991T (pt) 2022-10-17
IL304534A (en) 2023-09-01
UA128806C2 (uk) 2024-10-23
CR20220258A (es) 2022-07-03
DK3886991T3 (da) 2022-10-03
PE20230238A1 (es) 2023-02-07
HRP20221301T1 (hr) 2022-12-23
CN114828964A (zh) 2022-07-29
SA522432955B1 (ar) 2024-07-31
WO2021118877A1 (en) 2021-06-17
BR112022009557A2 (pt) 2022-08-02
JOP20240216A1 (ar) 2024-09-30
IL293394B2 (en) 2023-12-01
TWI765448B (zh) 2022-05-21
AU2024202573A1 (en) 2024-05-09
US20210179633A1 (en) 2021-06-17
CO2022008091A2 (es) 2022-06-10
CA3161162A1 (en) 2021-06-17
ES2929700T3 (es) 2022-12-01
CL2022001513A1 (es) 2023-03-03
AU2024202573B2 (en) 2026-02-12
MA54327A (fr) 2022-04-13
AU2020402701B2 (en) 2024-03-14
NZ788613A (en) 2025-07-25
JOP20220142B1 (ar) 2025-10-01
IL293394A (en) 2022-07-01
ECSP22046699A (es) 2022-07-29
IL293394B1 (en) 2023-08-01
AR120700A1 (es) 2022-03-09
RS63719B1 (sr) 2022-11-30
MX2025002170A (es) 2025-04-02
SI3886991T1 (sl) 2022-11-30
MD3886991T2 (ro) 2023-03-31
CN117820333A (zh) 2024-04-05
KR102546592B1 (ko) 2023-06-23
JP7023421B2 (ja) 2022-02-21
MA54327B1 (fr) 2022-12-30
HUE060684T2 (hu) 2023-04-28
US20230339968A1 (en) 2023-10-26
KR20220087566A (ko) 2022-06-24
DOP2022000117A (es) 2022-07-15
PH12022551424A1 (en) 2023-11-20
EP3886991B1 (en) 2022-09-21
PL3886991T3 (pl) 2022-11-21
IL304534B1 (en) 2026-04-01
EP3886991A1 (en) 2021-10-06
MX2022006986A (es) 2022-07-13
US11731984B2 (en) 2023-08-22
ZA202205218B (en) 2024-11-27
TW202136274A (zh) 2021-10-01
AU2020402701A1 (en) 2022-06-02

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