ECSP22046699A - Inhibidores de kras g12c - Google Patents

Inhibidores de kras g12c

Info

Publication number
ECSP22046699A
ECSP22046699A ECSENADI202246699A ECDI202246699A ECSP22046699A EC SP22046699 A ECSP22046699 A EC SP22046699A EC SENADI202246699 A ECSENADI202246699 A EC SENADI202246699A EC DI202246699 A ECDI202246699 A EC DI202246699A EC SP22046699 A ECSP22046699 A EC SP22046699A
Authority
EC
Ecuador
Prior art keywords
kras
inhibitors
compounds
salts
formula
Prior art date
Application number
ECSENADI202246699A
Other languages
English (en)
Inventor
Chong Si
Kevin Charles Fortner
Sheng-Bin Peng
Deqi Guo
David Michael Hyman
Serge Louis Boulet
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 ECSP22046699A publication Critical patent/ECSP22046699A/es

Links

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

Abstract

La presente invenci?n proporciona compuestos de la f?rmula: en donde R1, R2, R3, R4, R5, A, B, e Y son como se describen en la presente, las sales aceptables desde el punto de vista farmac?utico de estos, y los m?todos de uso de estos compuestos y sales para tratar pacientes con c?ncer.
ECSENADI202246699A 2019-12-11 2022-06-10 Inhibidores de kras g12c ECSP22046699A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201962946586P 2019-12-11 2019-12-11

Publications (1)

Publication Number Publication Date
ECSP22046699A true ECSP22046699A (es) 2022-07-29

Family

ID=74106135

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202246699A ECSP22046699A (es) 2019-12-11 2022-06-10 Inhibidores de kras g12c

Country Status (31)

Country Link
US (2) US11731984B2 (es)
EP (1) EP3886991B1 (es)
JP (1) JP7023421B2 (es)
KR (1) KR102546592B1 (es)
CN (2) CN117820333A (es)
AR (1) AR120700A1 (es)
AU (2) AU2020402701B2 (es)
BR (1) BR112022009557A2 (es)
CA (1) CA3161162A1 (es)
CL (1) CL2022001513A1 (es)
CO (1) CO2022008091A2 (es)
CR (1) CR20220258A (es)
DK (1) DK3886991T3 (es)
DO (1) DOP2022000117A (es)
EC (1) ECSP22046699A (es)
ES (1) ES2929700T3 (es)
HR (1) HRP20221301T1 (es)
HU (1) HUE060684T2 (es)
IL (2) IL293394B2 (es)
JO (1) JOP20220142A1 (es)
LT (1) LT3886991T (es)
MA (1) MA54327B1 (es)
MD (1) MD3886991T2 (es)
MX (1) MX2022006986A (es)
PE (1) PE20230238A1 (es)
PL (1) PL3886991T3 (es)
PT (1) PT3886991T (es)
RS (1) RS63719B1 (es)
SI (1) SI3886991T1 (es)
TW (1) TWI765448B (es)
WO (1) WO2021118877A1 (es)

Families Citing this family (25)

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MX2022005053A (es) 2019-10-28 2022-05-18 Merck Sharp & Dohme Llc Inhibidores de peque?as moleculas de mutante g12c de kras.
TWI799871B (zh) * 2020-05-27 2023-04-21 大陸商勁方醫藥科技(上海)有限公司 三環并環類化合物,其製法與醫藥上的用途
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
KR20240041917A (ko) 2021-07-27 2024-04-01 도레이 카부시키가이샤 암의 치료 및/또는 예방을 위한 의약품
TW202322819A (zh) 2021-10-22 2023-06-16 大陸商江蘇恆瑞醫藥股份有限公司 含氮的四環化合物、其製備方法及其在醫藥上的應用
WO2023099592A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099623A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099620A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
TW202340209A (zh) * 2021-12-01 2023-10-16 德商百靈佳殷格翰國際股份有限公司 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
CA3240980A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
AU2022421224A1 (en) 2021-12-22 2024-06-20 The Regents Of The University Of California Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
TW202333800A (zh) 2021-12-28 2023-09-01 英商阿斯特捷利康英國股份有限公司 抗體-藥物結合物及rasg12c抑制劑之組合
WO2023168036A1 (en) * 2022-03-04 2023-09-07 Eli Lilly And Company Method of treatment including kras g12c inhibitors and shp2 inhibitors
US20240043451A1 (en) 2022-03-25 2024-02-08 Eli Lilly And Company Kras inhibitors
WO2023196959A1 (en) 2022-04-07 2023-10-12 Eli Lilly And Company Process for making a kras g12c inhibitor
WO2023196887A1 (en) 2022-04-08 2023-10-12 Eli Lilly And Company Method of treatment including kras g12c inhibitors and aurora a inhibitors
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2024006424A1 (en) 2022-06-30 2024-01-04 Eli Lilly And Company Kras g12c inhibitor for treating cancer
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors

Family Cites Families (13)

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US20090318412A1 (en) * 2006-07-11 2009-12-24 Takahiro Matsumoto Tricyclic heterocyclic compound and use thereof
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
BR112017021869A2 (pt) 2015-04-10 2018-12-11 Araxes Pharma Llc compostos quinazolina substituídos e métodos de uso dos mesmos
CN110603258A (zh) 2017-05-11 2019-12-20 阿斯利康(瑞典)有限公司 抑制g12c突变型ras蛋白的杂芳基化合物
BR112020004246A2 (pt) 2017-09-07 2020-09-01 Revolution Medicines, Inc. composições inibidoras de shp2 e métodos para o tratamento de câncer
EP4141005B1 (en) 2017-09-08 2024-04-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
CN111989321B (zh) 2017-11-15 2024-05-14 米拉蒂治疗股份有限公司 Kras g12c抑制剂
TW202012415A (zh) * 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
AR116604A1 (es) 2018-10-15 2021-05-26 Lilly Co Eli Inhibidores de kras g12c
US20220204527A1 (en) * 2019-03-05 2022-06-30 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
CN112390818B (zh) 2019-08-12 2023-08-22 劲方医药科技(上海)有限公司 取代的杂芳环并二氢嘧啶酮衍生物,其制法与医药上的用途

Also Published As

Publication number Publication date
TWI765448B (zh) 2022-05-21
DOP2022000117A (es) 2022-07-15
MX2022006986A (es) 2022-07-13
JP7023421B2 (ja) 2022-02-21
IL293394B1 (en) 2023-08-01
HRP20221301T1 (hr) 2022-12-23
AU2024202573A1 (en) 2024-05-09
TW202136274A (zh) 2021-10-01
IL304534A (en) 2023-09-01
US20230339968A1 (en) 2023-10-26
PE20230238A1 (es) 2023-02-07
US20210179633A1 (en) 2021-06-17
DK3886991T3 (da) 2022-10-03
PT3886991T (pt) 2022-10-17
US11731984B2 (en) 2023-08-22
IL293394A (en) 2022-07-01
AU2020402701A1 (en) 2022-06-02
KR20220087566A (ko) 2022-06-24
PL3886991T3 (pl) 2022-11-21
EP3886991B1 (en) 2022-09-21
WO2021118877A1 (en) 2021-06-17
CA3161162A1 (en) 2021-06-17
CN114828964A (zh) 2022-07-29
EP3886991A1 (en) 2021-10-06
MA54327A (fr) 2022-04-13
ES2929700T3 (es) 2022-12-01
HUE060684T2 (hu) 2023-04-28
BR112022009557A2 (pt) 2022-08-02
LT3886991T (lt) 2022-11-10
RS63719B1 (sr) 2022-11-30
AR120700A1 (es) 2022-03-09
CR20220258A (es) 2022-07-03
AU2020402701B2 (en) 2024-03-14
JP2022508469A (ja) 2022-01-19
CN117820333A (zh) 2024-04-05
CN114828964B (zh) 2023-11-24
MA54327B1 (fr) 2022-12-30
CL2022001513A1 (es) 2023-03-03
IL293394B2 (en) 2023-12-01
MD3886991T2 (ro) 2023-03-31
CO2022008091A2 (es) 2022-06-10
KR102546592B1 (ko) 2023-06-23
JOP20220142A1 (ar) 2023-01-30
SI3886991T1 (sl) 2022-11-30

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