MX364438B - Inhibidores covalentes de kras g12c. - Google Patents

Inhibidores covalentes de kras g12c.

Info

Publication number
MX364438B
MX364438B MX2015012054A MX2015012054A MX364438B MX 364438 B MX364438 B MX 364438B MX 2015012054 A MX2015012054 A MX 2015012054A MX 2015012054 A MX2015012054 A MX 2015012054A MX 364438 B MX364438 B MX 364438B
Authority
MX
Mexico
Prior art keywords
kras
covalent inhibitors
mutant
ras protein
methods
Prior art date
Application number
MX2015012054A
Other languages
English (en)
Spanish (es)
Other versions
MX2015012054A (es
Inventor
Ren Pingda
Liu Yi
Li Liansheng
Feng Jun
Wu Tao
Original Assignee
Araxes Pharma Llc
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 Araxes Pharma Llc filed Critical Araxes Pharma Llc
Publication of MX2015012054A publication Critical patent/MX2015012054A/es
Publication of MX364438B publication Critical patent/MX364438B/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen 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
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
MX2015012054A 2013-03-15 2014-03-14 Inhibidores covalentes de kras g12c. MX364438B (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361852123P 2013-03-15 2013-03-15
US201361889480P 2013-10-10 2013-10-10
JOP20140098 2014-03-13
PCT/US2014/027504 WO2014152588A1 (en) 2013-03-15 2014-03-14 Covalent inhibitors of kras g12c

Publications (2)

Publication Number Publication Date
MX2015012054A MX2015012054A (es) 2016-04-06
MX364438B true MX364438B (es) 2019-04-26

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Family Applications (1)

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MX2015012054A MX364438B (es) 2013-03-15 2014-03-14 Inhibidores covalentes de kras g12c.

Country Status (8)

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EP (2) EP3401314B1 (enExample)
JP (2) JP6473133B2 (enExample)
CN (1) CN105189456B (enExample)
AU (2) AU2014239542A1 (enExample)
CA (1) CA2904393A1 (enExample)
MX (1) MX364438B (enExample)
TW (1) TW201524952A (enExample)
WO (1) WO2014152588A1 (enExample)

Families Citing this family (159)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104379563B (zh) 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
BR112015022993B1 (pt) 2013-03-14 2021-12-14 Sumitomo Dainippon Pharma Oncology, Inc. Inibidores de jak2 e alk2, composição farmacêutica compreendendo os referidos inibidores e uso destes
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
MX387055B (es) 2014-06-06 2025-03-19 Res Triangle Inst Agonistas del receptor de apelina (apj) y usos de los mismos.
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
AR102094A1 (es) * 2014-09-25 2017-02-01 Araxes Pharma Llc Inhibidores de proteínas kras con una mutación g12c
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
AU2016240033B2 (en) 2015-03-30 2020-04-16 Mission Therapeutics Limited 1-cyano-pyrrolidine compounds as USP30 inhibitors
WO2016164675A1 (en) 2015-04-10 2016-10-13 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
CA2983927A1 (en) * 2015-05-06 2016-11-10 The Regents Of The University Of California K-ras modulators
WO2016200726A1 (en) * 2015-06-08 2016-12-15 Texas Tech University System Inhibitors of mci-1 as drugs to overcome resistance to braf inhibitors and mek inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
CN108779097A (zh) 2015-11-16 2018-11-09 亚瑞克西斯制药公司 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法
BR112018011784A2 (pt) 2015-12-09 2018-12-04 Res Triangle Inst agonistas aprimorados do receptor de apelina (apj) e usos dos mesmos
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
MX382339B (es) * 2016-05-18 2025-03-13 Mirati Therapeutics Inc Inhibidores g12c de kras.
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
US11260049B2 (en) 2016-09-20 2022-03-01 Glaxosmithkline Intellectual Property (No. 2) Limited TRPV4 antagonists
US10590077B2 (en) 2016-09-20 2020-03-17 Glaxosmithkline Intellectual Property Development Limited TRPV4 antagonists
TW201825458A (zh) 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產（第二）有限公司 Ｔｒｐｖ４拮抗劑
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
WO2018098352A2 (en) 2016-11-22 2018-05-31 Jun Oishi Targeting kras induced immune checkpoint expression
BR112019012263A2 (pt) * 2016-12-15 2020-01-28 The Regents Of The University Of California composições e métodos para tratar câncer
UA124474C2 (uk) * 2016-12-22 2021-09-22 Емджен Інк. БЕНЗІЗОТІАЗОЛЬНІ, ІЗОТІАЗОЛО[3,4-b]ПІРИДИНОВІ, ХІНАЗОЛІНОВІ, ФТАЛАЗИНОВІ, ПІРИДО[2,3-d]ПІРИДАЗИНОВІ Й ПІРИДО[2,3-d]ПІРИМІДИНОВІ ПОХІДНІ ЯК ІНГІБІТОРИ G12C KRAS ДЛЯ ЛІКУВАННЯ РАКУ ЛЕГЕНІ, РАКУ ПІДШЛУНКОВОЇ ЗАЛОЗИ АБО КОЛОРЕКТАЛЬНОГО РАКУ
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
JP7161760B2 (ja) 2017-02-03 2022-10-27 国立大学法人東北大学 複素環化合物
MD3448859T2 (ro) 2017-03-20 2020-03-31 Forma Therapeutics Inc Compoziții de pirolopirol în calitate de activatori ai piruvatkinazei (PKR)
TW201900638A (zh) 2017-04-20 2019-01-01 加州大學董事會 Ｋ－ｒａｓ調節劑
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
CN116003405A (zh) 2017-09-08 2023-04-25 美国安进公司 Kras g12c的抑制剂及其使用方法
EP3700901A1 (en) 2017-10-24 2020-09-02 Genentech, Inc. (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
AU2018369759B2 (en) 2017-11-15 2022-11-24 Array Biopharma Inc. KRas G12C inhibitors
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
KR102746913B1 (ko) 2017-12-21 2024-12-24 베링거 인겔하임 인터내셔날 게엠베하 Sos1 억제제로서의 신규 벤질아미노 치환 피리도피리미디논 및 유도체
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
EP3773591A4 (en) 2018-04-05 2021-12-22 Sumitomo Dainippon Pharma Oncology, Inc. AXL KINASE INHIBITORS AND THEIR USE
TW202012396A (zh) * 2018-04-18 2020-04-01 美商德洛斯股份有限公司 具乙烯磺醯胺部分之k-ras調節劑
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
EP3788038B1 (en) 2018-05-04 2023-10-11 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. Kras g12c inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
MX2020011907A (es) 2018-05-10 2021-01-29 Amgen Inc Inhibidores de kras g12c para el tratamiento de cancer.
MA52765A (fr) 2018-06-01 2021-04-14 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
EP3807276B1 (en) 2018-06-12 2025-12-10 Amgen Inc. Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
US11040038B2 (en) 2018-07-26 2021-06-22 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same
HUE070338T2 (hu) 2018-09-10 2025-05-28 Mirati Therapeutics Inc Kombinációs terápiák
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
EP3849538A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
EP3628664A1 (en) 2018-09-25 2020-04-01 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Irreversible inhibitors of kras g12c mutant
CA3117210A1 (en) * 2018-10-24 2020-04-30 Araxes Pharma Llc 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
WO2020085504A1 (ja) * 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
JP7516029B2 (ja) * 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
AU2019392683B2 (en) 2018-12-05 2025-08-14 Mirati Therapeutics, Inc. Combination therapies
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
CN109646680B (zh) * 2019-01-31 2020-02-11 四川大学华西医院 一种治疗kras突变型肠癌的联合用药物
JP7572958B2 (ja) 2019-02-12 2024-10-24 ノバルティス アーゲー Ｔｎｏ１５５及びｋｒａｓｇ１２ｃ阻害剤を含む医薬組合せ
US12281099B2 (en) 2019-02-26 2025-04-22 Boehringer Ingelheim International Gmbh Isoindolinone substituted indoles and derivatives as RAS inhibitors
SG11202109451TA (en) 2019-03-05 2021-09-29 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
CN111662232B (zh) * 2019-03-06 2022-08-02 中国科学院上海药物研究所 具有2h-吲唑结构的小分子化合物及其合成和应用
WO2020205867A1 (en) 2019-04-02 2020-10-08 Aligos Therapeutics, Inc. Compounds targeting prmt5
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
KR20220011670A (ko) 2019-05-21 2022-01-28 암젠 인크 고체 상태 형태
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN113396147B (zh) * 2019-05-31 2024-06-18 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
US12421236B2 (en) 2019-06-25 2025-09-23 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Seven-membered heterocyclic derivative acting as KRAS G12C mutant protein inhibitor
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
AU2020350763A1 (en) 2019-09-19 2022-04-07 Novo Nordisk Health Care Ag Pyruvate kinase R (PKR) activating compositions
US11890285B2 (en) 2019-09-24 2024-02-06 Mirati Therapeutics, Inc. Combination therapies
CN112225734B (zh) * 2019-10-25 2021-12-07 南京瑞捷医药科技有限公司 Kras g12c抑制剂及其用途
GEP20247710B (en) 2019-10-28 2024-12-25 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12c mutant
EP4051266A1 (en) 2019-10-31 2022-09-07 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
CN120699039A (zh) 2019-11-04 2025-09-26 锐新医药公司 Ras抑制剂
EP4054719A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CN110698378B (zh) * 2019-11-19 2021-03-19 上海皓元生物医药科技有限公司 2-(羟基-(甲基环丙基)苯基氨基)-1-哌嗪基乙酮衍生物的制备方法
EP4061341A4 (en) * 2019-11-22 2024-04-10 The Regents of the University of California CASPASE 6 INHIBITORS AND THEIR USES
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
EP4076418A4 (en) 2019-12-20 2024-01-24 Mirati Therapeutics, Inc. Sos1 inhibitors
CN113045565A (zh) * 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021215545A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
EP4139299B1 (en) * 2020-04-24 2025-12-17 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
WO2021219090A1 (zh) * 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
TW202210633A (zh) 2020-06-05 2022-03-16 法商昂席歐公司 用於治療癌症之dbait分子與kras抑制劑的組合
BR112022025550A2 (pt) 2020-06-18 2023-03-07 Revolution Medicines Inc Métodos para retardar, prevenir e tratar resistência adquirida aos inibidores de ras
JP2023541236A (ja) 2020-09-03 2023-09-29 レボリューション メディシンズ インコーポレイテッド Ｓｈｐ２変異を有する悪性腫瘍を治療するためのｓｏｓ１阻害剤の使用
MX2023002942A (es) 2020-09-11 2023-05-22 Mirati Therapeutics Inc Formas cristalinas de un inhibidor de kras g12c.
CN117683049A (zh) 2020-09-15 2024-03-12 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物
JP2023544450A (ja) 2020-09-23 2023-10-23 エラスカ・インコーポレイテッド 三環式ピリドン及びピリミドン
CN114249703B (zh) * 2020-09-25 2023-10-13 四川科瑞德制药股份有限公司 适合工业放大的医药中间体的制备方法
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
US11999753B2 (en) 2020-12-16 2024-06-04 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
AR124449A1 (es) 2020-12-22 2023-03-29 Qilu Regor Therapeutics Inc Inhibidores de sos1 y usos de los mismos
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
WO2022232320A1 (en) 2021-04-27 2022-11-03 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
PE20240088A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras
JP2024517845A (ja) 2021-05-05 2024-04-23 レボリューション メディシンズ インコーポレイテッド がん治療のためのｒａｓ阻害剤
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
WO2022269508A1 (en) 2021-06-23 2022-12-29 Novartis Ag Pyrazolyl derivatives as inhibitors of the kras mutant protein
TW202327569A (zh) 2021-09-01 2023-07-16 瑞士商諾華公司 包含ｔｅａｄ抑制劑的藥物組合及其用於癌症治療之用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
MX2024004846A (es) 2021-10-22 2024-05-03 Jiangsu Hengrui Pharmaceuticals Co Ltd Compuesto tetraciclico que contiene nitrogeno, metodo de preparacion del mismo y uso medico del mismo.
CN113956233B (zh) * 2021-10-22 2023-06-06 南方医科大学 一种酰胺类化合物或其药学上可接受的盐及其制备方法和应用
CN114380682A (zh) * 2021-10-27 2022-04-22 上海毕得医药科技股份有限公司 一种2,3-二氟-4-甲氧基苯乙酸合成方法
US20250282782A1 (en) 2021-12-17 2025-09-11 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CN118696046A (zh) 2022-02-10 2024-09-24 拜耳公司 作为kras抑制剂的稠合嘧啶
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
IL320639A (en) 2022-11-09 2025-07-01 Revolution Medicines Inc Compounds, complexes and methods for their preparation and use
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AU2024243852A1 (en) 2023-04-07 2025-11-06 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
TW202446388A (zh) 2023-04-14 2024-12-01 美商銳新醫藥公司 Ｒａｓ抑制劑之結晶形式、含有其之組合物及其使用方法
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024248123A1 (ja) 2023-06-02 2024-12-05 第一三共株式会社 抗ｈｅｒ３抗体－薬物コンジュゲートとｒａｓｇ１２ｃ阻害剤の組み合わせ
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025016899A1 (en) 2023-07-19 2025-01-23 Bayer Aktiengesellschaft Spirocyclic compounds for the treatment of cancer
WO2025026903A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft Imidazo pyrimidine compounds for the treatment of cancer
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
CN119039303A (zh) * 2024-09-20 2024-11-29 上海信诺维生物医药有限公司 一种螺环化合物

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4656181A (en) * 1982-11-24 1987-04-07 Cermol S.A. Esters of 1,4-dihydropyridines, processes for the preparation of the new esters, and medicaments containing the same
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
IL111730A (en) * 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
EP0821671B1 (en) 1995-04-20 2000-12-27 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives as mmp and tnf inhibitors
DK0780386T3 (da) 1995-12-20 2003-02-03 Hoffmann La Roche Matrixmetalloproteaseinhibitorer
US6011029A (en) * 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
ES2175415T3 (es) 1996-07-18 2002-11-16 Pfizer Inhibidores de metaloproteasas matriciales basados en fosfinato.
IL128189A0 (en) 1996-08-23 1999-11-30 Pfizer Arylsulfonylamino hydroxamic acid derivatives
US6077864A (en) 1997-01-06 2000-06-20 Pfizer Inc. Cyclic sulfone derivatives
TR199901849T2 (xx) 1997-02-03 2000-02-21 Pfizer Products Inc. Arils�lfonilamino hidroksamik asit t�revleri.
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
CA2280151C (en) 1997-02-11 2005-12-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
WO1998035951A2 (en) * 1997-02-17 1998-08-20 Fujisawa Pharmaceutical Co., Ltd. New aminopiperazine derivatives
CA2293706C (en) * 1997-06-17 2008-11-18 Schering Corporation N-substituted urea inhibitors of farnesyl-protein transferase
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
EP1042299A1 (en) * 1997-12-22 2000-10-11 Du Pont Pharmaceuticals Company Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
TWI227231B (en) * 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
US7429599B2 (en) * 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
CA2443108A1 (en) * 2001-04-03 2002-10-17 Merck & Co. Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
EP1348434A1 (en) * 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
MXPA05003632A (es) * 2002-10-11 2005-06-03 Astrazeneca Ab Derivados de piperidina 1, 4-disustituidos y su uso como inhibidores de 11-beta-hidroesteroide deshidrogenasa humana de tipo 1 (11betahsd1).
HRP20050895B1 (hr) * 2003-03-12 2014-06-06 Kudos Pharmaceuticals Limited Ftalazinon derivati
US20050119266A1 (en) * 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
JP4923380B2 (ja) * 2003-12-22 2012-04-25 Ｊｎｃ株式会社 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物
EP1861376A1 (en) * 2005-03-16 2007-12-05 F. Hoffmann-Roche AG Cis-2,4,5-triaryl-imidazolines and their use as anti-cancer medicaments
WO2007047146A2 (en) * 2005-10-11 2007-04-26 Intermune, Inc. Inhibitors of viral replication
EP2133334A1 (en) * 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
AR076382A1 (es) * 2009-04-22 2011-06-08 Janssen Pharmaceutica Nv Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.
KR20120063515A (ko) * 2009-09-09 2012-06-15 아빌라 테라퓨틱스, 인크. Ｐｉ３ 키나제 억제제 및 이들의 용도
US8658131B2 (en) * 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
CA2815350A1 (en) * 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
AP2014007400A0 (en) * 2011-07-13 2014-01-31 Novartis Ag 4-Piperidinyl compounds for use as tankyrase inhibitors
ES2575604T3 (es) * 2012-01-13 2016-06-29 Bristol-Myers Squibb Company Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa
CN104379563B (zh) * 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法

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TW201524952A (zh) 2015-07-01
JP6849711B2 (ja) 2021-03-24
JP6473133B2 (ja) 2019-02-20
AU2018214014B2 (en) 2020-08-20
AU2018214014A1 (en) 2018-08-23
AU2018214014C1 (en) 2021-04-29
JP2016519072A (ja) 2016-06-30
HK1215029A1 (en) 2016-08-12
CN105189456B (zh) 2017-12-19
WO2014152588A1 (en) 2014-09-25
CA2904393A1 (en) 2014-09-25
EP3401314A1 (en) 2018-11-14
JP2019085414A (ja) 2019-06-06
MX2015012054A (es) 2016-04-06
CN105189456A (zh) 2015-12-23
AU2014239542A1 (en) 2015-10-01
EP2970121A1 (en) 2016-01-20
EP2970121B1 (en) 2017-12-13

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