ECSP22046699A - Inhibidores de kras g12c - Google Patents
Inhibidores de kras g12cInfo
- 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
Links
Classifications
-
- 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic 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
-
- 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
- A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
-
2020
- 2020-12-04 PL PL20834024.0T patent/PL3886991T3/pl unknown
- 2020-12-04 ES ES20834024T patent/ES2929700T3/es active Active
- 2020-12-04 EP EP20834024.0A patent/EP3886991B1/en active Active
- 2020-12-04 JO JOP/2022/0142A patent/JOP20220142A1/ar unknown
- 2020-12-04 MX MX2022006986A patent/MX2022006986A/es unknown
- 2020-12-04 AU AU2020402701A patent/AU2020402701B2/en active Active
- 2020-12-04 DK DK20834024.0T patent/DK3886991T3/da active
- 2020-12-04 RS RS20220956A patent/RS63719B1/sr unknown
- 2020-12-04 MA MA54327A patent/MA54327B1/fr unknown
- 2020-12-04 JP JP2021539866A patent/JP7023421B2/ja active Active
- 2020-12-04 SI SI202030102T patent/SI3886991T1/sl unknown
- 2020-12-04 US US17/111,676 patent/US11731984B2/en active Active
- 2020-12-04 HR HRP20221301TT patent/HRP20221301T1/hr unknown
- 2020-12-04 IL IL293394A patent/IL293394B2/en unknown
- 2020-12-04 BR BR112022009557A patent/BR112022009557A2/pt unknown
- 2020-12-04 KR KR1020227019240A patent/KR102546592B1/ko active IP Right Grant
- 2020-12-04 TW TW109142894A patent/TWI765448B/zh active
- 2020-12-04 PT PT208340240T patent/PT3886991T/pt unknown
- 2020-12-04 CA CA3161162A patent/CA3161162A1/en active Pending
- 2020-12-04 HU HUE20834024A patent/HUE060684T2/hu unknown
- 2020-12-04 LT LTEPPCT/US2020/063272T patent/LT3886991T/lt unknown
- 2020-12-04 WO PCT/US2020/063272 patent/WO2021118877A1/en active Application Filing
- 2020-12-04 CN CN202311816497.XA patent/CN117820333A/zh active Pending
- 2020-12-04 CN CN202080085553.5A patent/CN114828964B/zh active Active
- 2020-12-04 PE PE2022001047A patent/PE20230238A1/es unknown
- 2020-12-04 CR CR20220258A patent/CR20220258A/es unknown
- 2020-12-04 MD MDE20210978T patent/MD3886991T2/ro unknown
- 2020-12-09 AR ARP200103420A patent/AR120700A1/es unknown
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2022
- 2022-06-07 DO DO2022000117A patent/DOP2022000117A/es unknown
- 2022-06-07 CO CONC2022/0008091A patent/CO2022008091A2/es unknown
- 2022-06-08 CL CL2022001513A patent/CL2022001513A1/es unknown
- 2022-06-10 EC ECSENADI202246699A patent/ECSP22046699A/es unknown
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2023
- 2023-06-28 US US18/343,326 patent/US20230339968A1/en active Pending
- 2023-07-17 IL IL304534A patent/IL304534A/en unknown
-
2024
- 2024-04-18 AU AU2024202573A patent/AU2024202573A1/en active Pending
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