MX2018000777A - Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins. - Google Patents
Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins.Info
- Publication number
- MX2018000777A MX2018000777A MX2018000777A MX2018000777A MX2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A
- Authority
- MX
- Mexico
- Prior art keywords
- inhibitors
- mutant kras
- hras
- compounds
- quinazoline compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
Abstract
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562195636P | 2015-07-22 | 2015-07-22 | |
US201662342078P | 2016-05-26 | 2016-05-26 | |
GC201631750 | 2016-07-21 | ||
JOP/2016/0150A JOP20160150B1 (en) | 2015-07-22 | 2016-07-21 | Substituted quinazoline compounds and methods of use thereof |
PCT/US2016/043568 WO2017015562A1 (en) | 2015-07-22 | 2016-07-22 | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2018000777A true MX2018000777A (en) | 2018-03-23 |
Family
ID=57821530
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2018000777A MX2018000777A (en) | 2015-07-22 | 2016-07-22 | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins. |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP3325447A1 (en) |
JP (1) | JP6869947B2 (en) |
CA (1) | CA2993013A1 (en) |
MX (1) | MX2018000777A (en) |
WO (1) | WO2017015562A1 (en) |
Families Citing this family (80)
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US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
JO3805B1 (en) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | Inhibitors of kras g12c |
JO3556B1 (en) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | Combination therapies for treatment of cancer |
WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
WO2016049524A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
BR112017021869A2 (en) | 2015-04-10 | 2018-12-11 | Araxes Pharma Llc | substituted quinazoline compounds and methods of use thereof |
EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
JP2018533939A (en) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Method for screening for inhibitors of RAS |
CN108779097A (en) | 2015-11-16 | 2018-11-09 | 亚瑞克西斯制药公司 | Include the quinazoline compound and its application method of the 2- substitutions of substituted heterocycle |
US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
SG11201804901WA (en) | 2015-12-22 | 2018-07-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
CN110036010A (en) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | The inhibitor of KRAS G12C mutain |
JP2019534260A (en) | 2016-10-07 | 2019-11-28 | アラクセス ファーマ エルエルシー | Heterocyclic compounds as inhibitors of RAS and methods of use thereof |
JOP20190154B1 (en) | 2016-12-22 | 2022-09-15 | Amgen Inc | Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
JOP20190272A1 (en) | 2017-05-22 | 2019-11-21 | Amgen Inc | Kras g12c inhibitors and methods of using the same |
EP3630745A2 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Covalent inhibitors of kras |
EP3630746A1 (en) * | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
US10588894B2 (en) | 2017-06-21 | 2020-03-17 | SHY Therapeutics LLC | Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
EP4141005B1 (en) | 2017-09-08 | 2024-04-03 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
SG11202002425PA (en) * | 2017-09-20 | 2020-04-29 | The United States Of America As Represented By The Secretary | Hla class ii-restricted t cell receptors against mutated ras |
WO2019110751A1 (en) * | 2017-12-08 | 2019-06-13 | Astrazeneca Ab | Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents |
TW201942115A (en) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | Substituted quinazoline and pyridopyrimidine derivatives useful as anticancer agents |
WO2019213526A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
MX2020010836A (en) | 2018-05-04 | 2021-01-08 | Amgen Inc | Kras g12c inhibitors and methods of using the same. |
US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
TW202012415A (en) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | Chemical compounds |
MA52564A (en) | 2018-05-10 | 2021-03-17 | Amgen Inc | KRAS G12C INHIBITORS FOR CANCER TREATMENT |
MA52765A (en) | 2018-06-01 | 2021-04-14 | Amgen Inc | KRAS G12C INHIBITORS AND THEIR PROCEDURES FOR USE |
MA51848A (en) | 2018-06-12 | 2021-04-21 | Amgen Inc | KRAS G12C INHIBITORS AND THEIR PROCEDURES FOR USE |
WO2020004594A1 (en) * | 2018-06-27 | 2020-01-02 | 株式会社リボルナバイオサイエンス | Prophylactic or therapeutic agent for spinal muscular atrophy |
MX2021003158A (en) | 2018-09-18 | 2021-07-16 | Nikang Therapeutics Inc | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors. |
CA3117221A1 (en) | 2018-11-16 | 2020-05-22 | Amgen Inc. | Improved synthesis of key intermediate of kras g12c inhibitor compound |
AU2019384118A1 (en) | 2018-11-19 | 2021-05-27 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
JP7377679B2 (en) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | Combination therapy comprising a KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancer |
JP2022520079A (en) | 2019-02-12 | 2022-03-28 | ノバルティス アーゲー | Pharmaceutical combination containing TNO155 and KRASG12C inhibitor |
JP7426398B2 (en) | 2019-02-26 | 2024-02-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Novel isoindolinone substituted indoles and derivatives as RAS inhibitors |
EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
CN114144414A (en) | 2019-05-21 | 2022-03-04 | 美国安进公司 | Solid state form |
MX2022005053A (en) | 2019-10-28 | 2022-05-18 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant. |
CN115873020A (en) | 2019-11-04 | 2023-03-31 | 锐新医药公司 | RAS inhibitors |
BR112022008565A2 (en) | 2019-11-04 | 2022-08-09 | Revolution Medicines Inc | COMPOUND, PHARMACEUTICAL COMPOSITION, CONJUGATE, METHODS TO TREAT CANCER AND A RAS PROTEIN-RELATED DISORDER |
TW202132314A (en) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ras inhibitors |
CN114980976A (en) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | Covalent RAS inhibitors and uses thereof |
GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
TW202210633A (en) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | A dbait molecule in combination with kras inhibitor for the treatment of cancer |
JP2023530351A (en) | 2020-06-18 | 2023-07-14 | レヴォリューション・メディスンズ,インコーポレイテッド | Methods of delaying, preventing and treating acquired resistance to RAS inhibitors |
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WO2023114954A1 (en) | 2021-12-17 | 2023-06-22 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
WO2023152255A1 (en) | 2022-02-10 | 2023-08-17 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
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WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
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GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
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WO2024102849A1 (en) | 2022-11-11 | 2024-05-16 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
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TWI271406B (en) * | 1999-12-13 | 2007-01-21 | Eisai Co Ltd | Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same |
JP2002371078A (en) * | 2001-06-12 | 2002-12-26 | Sankyo Co Ltd | Quinoline derivative and quinolone derivative |
WO2003053958A1 (en) * | 2001-12-20 | 2003-07-03 | Celltech R & D Limited | Quinazolinedione derivatives |
WO2005092894A1 (en) * | 2004-03-01 | 2005-10-06 | Eli Lilly And Company | Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms |
TW200643015A (en) * | 2005-03-11 | 2006-12-16 | Akzo Nobel Nv | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives |
BR112013002182B8 (en) * | 2010-07-30 | 2023-02-28 | Oncotherapy Science Inc | QUINOLINE DERIVATIVE COMPOUNDS, PHARMACEUTICAL COMPOSITION, MELK INHIBITOR, MELK EXPRESSION MODULATING AGENT, ANTI-TUMOR AGENT, THERAPEUTIC AND/OR PREVENTIVE AGENT FOR A DISEASE INVOLVING MELK OVEREXPRESSION CONTAINING THE SAME AND USE OF SAID COMPOUNDS |
EP2968360B1 (en) * | 2013-03-14 | 2021-01-20 | ConverGene LLC | Quinolinone derivatives for the inhibition of bromodomain-containing proteins |
EP3055290B1 (en) * | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
MX370438B (en) * | 2014-03-24 | 2019-12-13 | Guangdong Zhongsheng Pharmaceutical Co Ltd | Quinoline derivatives as smo inhibitors. |
-
2016
- 2016-07-22 EP EP16747678.7A patent/EP3325447A1/en not_active Withdrawn
- 2016-07-22 JP JP2018502355A patent/JP6869947B2/en active Active
- 2016-07-22 CA CA2993013A patent/CA2993013A1/en not_active Abandoned
- 2016-07-22 MX MX2018000777A patent/MX2018000777A/en unknown
- 2016-07-22 WO PCT/US2016/043568 patent/WO2017015562A1/en active Application Filing
Also Published As
Publication number | Publication date |
---|---|
WO2017015562A1 (en) | 2017-01-26 |
JP2018520195A (en) | 2018-07-26 |
JP6869947B2 (en) | 2021-05-12 |
CA2993013A1 (en) | 2017-01-26 |
EP3325447A1 (en) | 2018-05-30 |
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