HK1248231A1 - 取代的喹唑啉化合物和其使用方法 - Google Patents

取代的喹唑啉化合物和其使用方法 Download PDF

Info

Publication number
HK1248231A1
HK1248231A1 HK18107777.4A HK18107777A HK1248231A1 HK 1248231 A1 HK1248231 A1 HK 1248231A1 HK 18107777 A HK18107777 A HK 18107777A HK 1248231 A1 HK1248231 A1 HK 1248231A1
Authority
HK
Hong Kong
Prior art keywords
methods
compounds
quinazoline compounds
substituted quinazoline
activity
Prior art date
Application number
HK18107777.4A
Other languages
English (en)
Chinese (zh)
Inventor
Li Liansheng
Feng Jun
Oliver Long Yun
Liu Yuan
Wu Tao
Ren Pingda
Liu Yi
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 HK1248231A1 publication Critical patent/HK1248231A1/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • 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
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
HK18107777.4A 2015-04-10 2016-04-08 取代的喹唑啉化合物和其使用方法 HK1248231A1 (zh)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201562145705P 2015-04-10 2015-04-10
US201562145818P 2015-04-10 2015-04-10
US62/145,705 2015-04-10
US62/145,818 2015-04-10
US201562255891P 2015-11-16 2015-11-16
US62/255,891 2015-11-16
US201562265316P 2015-12-09 2015-12-09
US201562265320P 2015-12-09 2015-12-09
US62/265,316 2015-12-09
US62/265,320 2015-12-09
PCT/US2016/026573 WO2016164675A1 (en) 2015-04-10 2016-04-08 Substituted quinazoline compounds and methods of use thereof

Publications (1)

Publication Number Publication Date
HK1248231A1 true HK1248231A1 (zh) 2018-10-12

Family

ID=55754477

Family Applications (1)

Application Number Title Priority Date Filing Date
HK18107777.4A HK1248231A1 (zh) 2015-04-10 2016-04-08 取代的喹唑啉化合物和其使用方法

Country Status (15)

Country Link
US (3) US10246424B2 (OSRAM)
EP (1) EP3280708B1 (OSRAM)
JP (2) JP2018513853A (OSRAM)
KR (1) KR20180005178A (OSRAM)
CN (1) CN107849022A (OSRAM)
AU (1) AU2016245864C1 (OSRAM)
BR (1) BR112017021869A2 (OSRAM)
EA (1) EA201792214A1 (OSRAM)
ES (1) ES2898765T3 (OSRAM)
HK (1) HK1248231A1 (OSRAM)
JO (1) JO3707B1 (OSRAM)
MX (1) MX382355B (OSRAM)
TW (1) TW201702232A (OSRAM)
UY (1) UY36612A (OSRAM)
WO (1) WO2016164675A1 (OSRAM)

Families Citing this family (210)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014143659A1 (en) 2013-03-15 2014-09-18 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
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
US10144724B2 (en) * 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058768A1 (en) 2015-09-28 2017-04-06 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
US10882847B2 (en) 2015-09-28 2021-01-05 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
WO2017058915A1 (en) 2015-09-28 2017-04-06 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
CA3005089A1 (en) * 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
CN109311868B (zh) 2015-12-22 2022-04-01 尚医治疗有限责任公司 用于治疗癌症和炎性疾病的化合物
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
AU2017266911B2 (en) 2016-05-18 2021-09-02 Array Biopharma, Inc. KRas G12C inhibitors
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
JP2019529484A (ja) * 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質の阻害剤
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
SI3558955T1 (sl) * 2016-12-22 2021-12-31 Amgen Inc., Derivati benzizotiazola, izotiazola(3,4-b)piridina, kinazolina, ftalazina, pirido(2,3-d)piridazina in pirido(2,3-D)pirimidina, kot zaviralci KRAS G12C za zdravljenje pljučnega raka, raka trebušne slinavke ali kolorektalnega raka
US11274093B2 (en) * 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (ja) * 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
JOP20190186A1 (ar) * 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
JP2020521740A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体kras、hrasまたはnrasの調節因子としてのキナゾリン誘導体
US10745385B2 (en) * 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
IL271230B2 (en) 2017-06-21 2024-06-01 SHY Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
EP3710439B1 (en) 2017-11-15 2023-02-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
ES2969284T3 (es) * 2018-01-19 2024-05-17 Medshine Discovery Inc Derivado de piridona-pirimidina que actúa como inhibidor de la muteína krasg12c
TW201942115A (zh) * 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
JP7266043B2 (ja) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド KRas G12C阻害剤及びそれを使用する方法
US11932633B2 (en) 2018-05-07 2024-03-19 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
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
MA52765A (fr) 2018-06-01 2021-04-14 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US20190375749A1 (en) * 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
MA51848A (fr) 2018-06-12 2021-04-21 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
SG11202012972YA (en) 2018-06-27 2021-01-28 Bristol Myers Squibb Co Substituted naphthyridinone compounds useful as t cell activators
US11866430B2 (en) 2018-06-27 2024-01-09 Bristol-Myers Squibb Company Naphthyridinone compounds useful as T cell activators
JP2021176820A (ja) * 2018-07-31 2021-11-11 アステラス製薬株式会社 キナゾリン化合物を有効成分とする医薬組成物
JP2021176819A (ja) * 2018-07-31 2021-11-11 アステラス製薬株式会社 キナゾリン化合物を有効成分とする医薬組成物
BR112021001709A2 (pt) * 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
US12336995B2 (en) 2018-09-10 2025-06-24 Mirati Therapeutics, Inc. Combination therapies
HRP20250059T1 (hr) 2018-09-10 2025-03-28 Mirati Therapeutics, Inc. Kombinirane terapije
CA3113234A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
TW202033518A (zh) 2018-10-15 2020-09-16 美商美國禮來大藥廠 Kras g12c 抑制劑
EP3870585A1 (en) * 2018-10-24 2021-09-01 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
WO2020085493A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
JP7186874B2 (ja) * 2018-10-26 2022-12-09 アーリーン ファーマシューティカルズ エルエルシー ピラゾリル化合物およびその使用方法
BR112021008986A2 (pt) 2018-11-09 2021-08-10 F. Hoffmann-La Roche Ag composto, composto da fórmula, composto ou sal farmaceuticamente aceitável, composição farmacêutica, métodos para tratar o câncer, para regular a atividade de uma proteína mutante g12c k-ras, para inibir a proliferação de uma população de células, para tratar um distúrbio mediado, para preparar uma proteína e para inibir metástase de tumor e uso
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
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
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
KR20210097715A (ko) * 2018-11-29 2021-08-09 아락세스 파마 엘엘씨 암 치료용 화합물 및 이의 사용 방법
JP2022509724A (ja) 2018-12-05 2022-01-24 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
JP7407461B2 (ja) 2018-12-19 2024-01-04 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ras病、及び線維性疾患の処置のためのrasスーパーファミリーと相互作用する化合物
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス, インコーポレイテッド Kras g12c阻害剤
KR102405055B1 (ko) * 2019-01-16 2022-06-07 상하이 잉리 파마슈티컬 컴퍼니 리미티드 모르폴리노퀴나졸린 화합물의 제조방법 및 이의 중간체
WO2020156285A1 (zh) * 2019-01-29 2020-08-06 博瑞生物医药(苏州)股份有限公司 一种苯并吡啶酮杂环化合物及其用途
CN111499634B (zh) * 2019-01-31 2023-05-12 贝达药业股份有限公司 一种喹唑啉化合物及其在医药上的应用
EP3924053A1 (en) 2019-02-12 2021-12-22 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
PT3927701T (pt) * 2019-02-18 2025-02-03 Pi Industries Ltd Um processo de preparação de diamidas antranílicas e seus intermediários
WO2020177629A1 (zh) * 2019-03-01 2020-09-10 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物,其制法与医药上的用途
SG11202109451TA (en) 2019-03-05 2021-09-29 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
WO2020198567A1 (en) * 2019-03-28 2020-10-01 Epizyme, Inc. Quinoline derivatives and their use for the treatment of cancer
KR20220012248A (ko) * 2019-04-22 2022-02-03 베타 파머수티컬 컴퍼니 리미티드 퀴나졸린 화합물 및 이의 의약품에서의 응용
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
WO2020236940A1 (en) * 2019-05-20 2020-11-26 California Institute Of Technology Kras g12c inhibitors and uses thereof
CA3140394A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
JP7092935B2 (ja) 2019-05-21 2022-06-28 アムジエン・インコーポレーテツド 固体形態
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
US12497396B2 (en) 2019-05-29 2025-12-16 Shanghai Hansoh Biomedical Co., Ltd. Nitrogen-containing heterocyclic derivatives, method therefor and application therefor as inhibitors of KRAS G12C for the treatment of cancers
CN112047948B (zh) * 2019-06-06 2022-08-16 山东轩竹医药科技有限公司 Kras突变体抑制剂
CN112110918B (zh) * 2019-06-21 2023-08-22 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物,其制法与医药上的用途
WO2021000885A1 (zh) * 2019-07-01 2021-01-07 江苏恒瑞医药股份有限公司 喹唑啉酮类衍生物、其制备方法及其在医药上的应用
CN114222743A (zh) * 2019-08-16 2022-03-22 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物,其制法与医药上的用途
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
JP7622043B2 (ja) 2019-08-29 2025-01-27 ミラティ セラピューティクス, インコーポレイテッド Kras g12d阻害剤
WO2021055728A1 (en) * 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
TWI761961B (zh) * 2019-09-20 2022-04-21 大陸商上海濟煜醫藥科技有限公司 稠合吡啶酮類化合物及其製備方法和應用
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
AU2020356455A1 (en) 2019-09-24 2022-04-14 Mirati Therapeutics, Inc. Combination therapies
CN112552295A (zh) * 2019-09-25 2021-03-26 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CN112574224A (zh) * 2019-09-30 2021-03-30 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
PE20221253A1 (es) 2019-10-28 2022-08-16 Merck Sharp & Dohme Inhibidores de pequenas moleculas de mutante g12c de kras
CN113286794B (zh) * 2019-11-04 2024-03-12 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CR20220241A (es) 2019-11-04 2022-08-03 Revolution Medicines Inc Inhibidores de ras
US11739074B2 (en) 2019-11-04 2023-08-29 Revolution Medicines, Inc. Ras inhibitors
BR112022008535A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras
WO2021093758A1 (zh) * 2019-11-15 2021-05-20 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
CN114980976A (zh) * 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
JP7480298B2 (ja) * 2019-12-02 2024-05-09 シャンハイ インリー ファーマシューティカル カンパニー リミテッド 酸素含有複素環化合物、その製造方法及び使用
CN113024544B (zh) * 2019-12-09 2024-07-02 武汉誉祥医药科技有限公司 一种含氰基并杂环化合物及其用途
NZ788613A (en) * 2019-12-11 2025-07-25 Lilly Co Eli Kras g12c inhibitors
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
CN115135315B (zh) 2019-12-20 2024-11-26 米拉蒂治疗股份有限公司 Sos1抑制剂
MX2022007130A (es) 2019-12-23 2022-07-11 Bristol Myers Squibb Co Derivados de piperazina sustituidos utiles como activadores de celulas t.
CA3162985A1 (en) 2019-12-23 2021-07-01 Upender Velaparthi Substituted quinazolinyl compounds useful as t cell activators
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
CA3162106A1 (en) * 2019-12-27 2021-07-01 Yuli Xie Spiro ring-containing quinazoline compound
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN113637005B (zh) * 2020-02-24 2024-05-24 泰励生物科技(上海)有限公司 用于癌症治疗的kras抑制剂
US12391692B2 (en) 2020-03-25 2025-08-19 Wigen Boimedicine Technology (Shanghai) Co., Ltd. Spiro ring-containing quinazoline compound
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
EP4168002A1 (en) 2020-06-18 2023-04-26 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2021259331A1 (zh) * 2020-06-24 2021-12-30 南京明德新药研发有限公司 八元含n杂环类化合物
CN116368130A (zh) 2020-08-28 2023-06-30 金橘生物科技公司 杂环化合物及其用途
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations
WO2022052895A1 (zh) 2020-09-11 2022-03-17 南京明德新药研发有限公司 氮杂环丁烷取代化合物的晶型
JP2023540809A (ja) 2020-09-11 2023-09-26 ミラティ セラピューティクス, インコーポレイテッド Kras g12c阻害剤の結晶形態
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
CN116323624A (zh) * 2020-09-30 2023-06-23 上海医药集团股份有限公司 一种喹唑啉类化合物及其应用
CA3199082A1 (en) * 2020-10-27 2022-05-05 Amgen Inc. Heterocyclic spiro compounds and methods of use
WO2022098625A1 (en) * 2020-11-03 2022-05-12 Mirati Therapeutics, Inc. Kras g12d inhibitors
CN120887884A (zh) * 2020-11-06 2025-11-04 泰励生物科技(上海)有限公司 用于癌症治疗的KRas抑制剂
TWI880049B (zh) 2020-12-04 2025-04-11 美商美國禮來大藥廠 Kras g12c抑制劑
CN112574127B (zh) * 2020-12-09 2022-11-01 深圳湾实验室 喹唑啉类化合物及其制备方法、药物组合物及其应用
KR20230142465A (ko) 2020-12-15 2023-10-11 미라티 테라퓨틱스, 인크. 아자퀴나졸린 범-KRas 저해제
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
CN114644628A (zh) * 2020-12-17 2022-06-21 广东东阳光药业有限公司 嘧啶酮衍生物及其在药物中的应用
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
WO2022152233A1 (en) * 2021-01-15 2022-07-21 Beigene, Ltd. Kras g12c inhibitors
WO2022152313A1 (zh) * 2021-01-18 2022-07-21 成都百裕制药股份有限公司 嘧啶衍生物及其在医药上的应用
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
CN115490689B (zh) * 2021-06-17 2024-04-09 药雅科技(上海)有限公司 不可逆krasg12c抑制剂的制备及其应用
CN115304603B (zh) * 2021-05-07 2024-04-09 药雅科技(上海)有限公司 喹唑啉类抑制剂的制备及其应用
TWI814234B (zh) * 2021-03-15 2023-09-01 大陸商藥雅科技(上海)有限公司 突變蛋白抑制劑的製備及其應用
CN115073450A (zh) * 2021-03-15 2022-09-20 药雅科技(上海)有限公司 Krasg12c突变蛋白抑制剂的制备及其应用
CN117659051A (zh) * 2021-03-30 2024-03-08 上海德琪医药科技有限公司 Kras g12d蛋白抑制剂和其用途
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
EP4334325A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
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
CN117980310A (zh) 2021-07-14 2024-05-03 尼坎治疗公司 作为kras抑制剂的亚烷基衍生物
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
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US20250145589A1 (en) 2021-09-22 2025-05-08 Sichuan Huiyu Pharmaceutical Co., Ltd. Pyridine derivative and use thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
JP2024539228A (ja) 2021-10-22 2024-10-28 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 含窒素四環式化合物、その調製方法及びその医薬的使用
US20250282782A1 (en) 2021-12-17 2025-09-11 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023125989A1 (zh) * 2021-12-31 2023-07-06 上海医药集团股份有限公司 一种喹唑啉类化合物及其应用
JP2025506408A (ja) * 2022-02-03 2025-03-11 ミラティ セラピューティクス, インコーポレイテッド キナゾリンpan-KRas阻害剤
EP4476221A1 (en) 2022-02-10 2024-12-18 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4486345A1 (en) 2022-03-04 2025-01-08 Eli Lilly and Company Method of treatment including kras g12c inhibitors and shp2 inhibitors
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
EP4499634A1 (en) 2022-03-28 2025-02-05 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
CA3247183A1 (en) 2022-04-08 2023-10-12 Eli Lilly And Company TREATMENT METHOD INCLUDING KRAS G12C INHIBITORS AND AURORA A INHIBITORS
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
CN119731195A (zh) 2022-05-06 2025-03-28 中外制药株式会社 相对于hras和nras对kras具有选择性抑制作用的环状化合物
EP4536363A1 (en) 2022-06-08 2025-04-16 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4545536A1 (en) * 2022-06-24 2025-04-30 Medshine Discovery Inc. Heterocyclic substituted pyrimidopyran compound and use thereof
JP2025525946A (ja) 2022-08-05 2025-08-07 カムクワット バイオサイエンシーズ インコーポレイテッド 複素環式化合物およびその使用
EP4565579A1 (en) * 2022-08-05 2025-06-11 Theras, Inc. Compositions and methods for inhibition of kras
WO2024030647A1 (en) * 2022-08-05 2024-02-08 Theras, Inc. Compositions and methods for inhibition of ras
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
WO2024051763A1 (zh) * 2022-09-08 2024-03-14 深圳福沃药业有限公司 用于治疗癌症的kras突变抑制剂的喹唑啉杂环类衍生物
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
JP2025537123A (ja) 2022-11-11 2025-11-14 ニカング セラピューティクス, インコーポレイテッド ユビキチンプロテアソーム経路を介してサイクリン依存性キナーゼ2を分解するための2,5-置換ピリミジン誘導体を含有する二官能性化合物
IL320913A (en) 2022-11-21 2025-07-01 Treeline Biosciences Inc Spirocyclic dihydropyranopyrimidine KRAS inhibitors
WO2024109233A1 (zh) * 2022-11-22 2024-05-30 四川汇宇制药股份有限公司 一种嘧啶并芳环化合物及其制备方法和用途
EP4655298A1 (en) * 2023-01-24 2025-12-03 Theras Inc. Compositions and methods for inhibition of ras
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ras gtp水解之組合物及其用途
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
AU2024243852A1 (en) 2023-04-07 2025-11-06 Revolution Medicines, Inc. Macrocyclic ras inhibitors
TW202448897A (zh) 2023-04-14 2024-12-16 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
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
AU2024276994A1 (en) 2023-05-24 2025-10-23 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
TW202502779A (zh) 2023-06-30 2025-01-16 美商金橘生物科技公司 取代的雜芳族胺及其用途
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
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
TW202535891A (zh) 2023-10-20 2025-09-16 美商默沙東有限責任公司 Kras蛋白之小分子抑制劑
WO2025117616A1 (en) 2023-11-27 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025117981A1 (en) 2023-12-02 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025212828A1 (en) 2024-04-03 2025-10-09 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025240536A1 (en) 2024-05-15 2025-11-20 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (213)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB939516A (en) 1961-05-29 1963-10-16 British Drug Houses Ltd Sulphonyl ureas
US3702849A (en) 1967-10-26 1972-11-14 Pfizer 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters
US3752660A (en) 1971-03-15 1973-08-14 Allied Chem Chlorophenoxyacetyloxazolidone herbicides and preparation thereof
US4439606A (en) 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
EP0094498A3 (en) 1982-05-06 1985-04-03 American Cyanamid Company Antiatherosclerotic 1-piperazine derivatives
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
JPS59163372A (ja) 1983-03-09 1984-09-14 Showa Denko Kk ピラゾ−ル誘導体とその製造法及び除草剤
JPS60193955A (ja) 1984-03-13 1985-10-02 Mitsui Toatsu Chem Inc 環式不飽和アミド置換エ−テル化合物及びその製造方法
JPS6143190A (ja) 1984-08-06 1986-03-01 Mitsui Petrochem Ind Ltd ピリドピリミジン誘導体およびその製法
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5925525A (en) 1989-06-07 1999-07-20 Affymetrix, Inc. Method of identifying nucleotide differences
IE66205B1 (en) 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5650489A (en) 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6051380A (en) 1993-11-01 2000-04-18 Nanogen, Inc. Methods and procedures for molecular biological analysis and diagnostics
US6017696A (en) 1993-11-01 2000-01-25 Nanogen, Inc. Methods for electronic stringency control for molecular biological analysis and diagnostics
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5605798A (en) 1993-01-07 1997-02-25 Sequenom, Inc. DNA diagnostic based on mass spectrometry
US5858659A (en) 1995-11-29 1999-01-12 Affymetrix, Inc. Polymorphism detection
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US6068818A (en) 1993-11-01 2000-05-30 Nanogen, Inc. Multicomponent devices for molecular biological analysis and diagnostics
US5538848A (en) 1994-11-16 1996-07-23 Applied Biosystems Division, Perkin-Elmer Corp. Method for detecting nucleic acid amplification using self-quenching fluorescence probe
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
JP3175110B2 (ja) 1994-02-07 2001-06-11 オーキッド・バイオサイエンシーズ・インコーポレイテッド リガーゼ/ポリメラーゼ媒体された単一ヌクレオチド多型のジェネティックビットアナリシスおよび遺伝子解析におけるその使用
US5593853A (en) 1994-02-09 1997-01-14 Martek Corporation Generation and screening of synthetic drug libraries
US5539083A (en) 1994-02-23 1996-07-23 Isis Pharmaceuticals, Inc. Peptide nucleic acid combinatorial libraries and improved methods of synthesis
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
JP2002515008A (ja) 1994-10-27 2002-05-21 メルク エンド カンパニー インコーポレーテッド ムスカリン・アンタゴニスト
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
MX9708026A (es) 1995-04-20 1997-11-29 Pfizer Derivados del acido arislfulfonil hidroxamico, composiciones que los contienen y uso de los mismos.
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5977322A (en) 1995-06-14 1999-11-02 The Regents Of The University Of California High affinity human antibodies to tumor antigens
ES2183905T3 (es) 1995-12-20 2003-04-01 Hoffmann La Roche Inhibidores de metaloproteasa de matriz.
US6011029A (en) 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
IL127567A0 (en) 1996-07-18 1999-10-28 Pfizer Phosphinate based inhibitors of matrix metalloproteases
JP2000501423A (ja) 1996-08-23 2000-02-08 ファイザー インク. アリールスルホニルアミノヒドロキサム酸誘導体
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
ES2202796T3 (es) 1997-02-03 2004-04-01 Pfizer Products Inc. Derivados de acidos arilsulfonilaminohidroxamicos.
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
EP0966438A1 (en) 1997-02-07 1999-12-29 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
US6291464B1 (en) 1997-02-17 2001-09-18 Fujisawa Pharmaceutical Co., Ltd. Aminopiperazine derivatives
UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6002008A (en) * 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US5919626A (en) 1997-06-06 1999-07-06 Orchid Bio Computer, Inc. Attachment of unmodified nucleic acids to silanized solid phase surfaces
CN1267291A (zh) 1997-06-17 2000-09-20 先灵公司 新的n-取代的脲的法呢基蛋白转移酶抑制剂
EA002490B1 (ru) 1997-08-08 2002-06-27 Пфайзер Продактс Инк. Производные арилоксиарилсульфониламиногидроксамовой кислоты
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
DE19756236A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
BR9813835A (pt) 1997-12-22 2000-10-10 Du Pont Pharm Co Composto, composição farmacêutica e método de tratamento ou prevenção de uma desordem tromboembólica
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
DE69940430D1 (de) 1998-06-24 2009-04-02 Illumina Inc Dekodierung von matrixartig-angeordneten Sensoren durch Mikropartikel
DE69915004T2 (de) 1998-11-05 2004-09-09 Pfizer Products Inc., Groton 5-Oxo-pyrrolidine-2-Carbonsäure-Hydroxamidderivate
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6511993B1 (en) 1999-06-03 2003-01-28 Kevin Neil Dack Metalloprotease inhibitors
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
CN102586228A (zh) 1999-09-13 2012-07-18 纽亘技术公司 用于多核苷酸序列线性等温扩增的方法及组合物
KR100817423B1 (ko) * 2000-03-13 2008-03-27 와이어쓰 홀딩스 코포레이션 시아노퀴놀린을 포함하는 결장 폴립의 치료 또는 억제를 위한 약제학적 조성물
RU2230736C2 (ru) 2000-03-21 2004-06-20 Дзе Проктер Энд Гэмбл Компани Содержащие гетероциклическую боковую цепь ингибиторы металлопротеиназы и фармацевтическая композиция
BR0111280A (pt) 2000-06-05 2003-06-10 Dong A Pharm Co Ltd Novos derivados de oxazolidinona e um processo para a preparação dos mesmos
TWI227231B (en) 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
CA2426440C (en) 2000-08-18 2011-03-15 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as kinase inhibitors
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
US20020169300A1 (en) 2001-01-30 2002-11-14 Waterman Marian L. Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1
CA2443108A1 (en) 2001-04-03 2002-10-17 Merck & Co. Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
DE60227794D1 (de) 2001-04-26 2008-09-04 Eisai R&D Man Co Ltd Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon
ATE449090T1 (de) 2001-07-02 2009-12-15 High Point Pharmaceuticals Llc Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
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).
JP4608852B2 (ja) 2002-10-15 2011-01-12 チッソ株式会社 液晶性ビニルケトン誘導体およびその重合体
EP1597256A1 (en) 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
KR101146806B1 (ko) 2003-03-12 2012-05-22 메이브릿지 리미티드 프탈라지논 유도체
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
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
EP1713484A2 (en) 2004-01-23 2006-10-25 Amgen Inc. Compounds and methods of use
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
EP1736465A4 (en) 2004-03-31 2009-06-17 Ajinomoto Kk ANILINE DERIVATIVES
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
US7579368B2 (en) 2005-03-16 2009-08-25 Hoffman-La Roche Inc. Cis-imidazolines
JP2007016011A (ja) 2005-06-10 2007-01-25 Nippon Soda Co Ltd 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬
WO2006135993A1 (en) 2005-06-24 2006-12-28 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c.
BRPI0617271A2 (pt) 2005-10-11 2011-07-19 Intermune Inc inibidores de replicação viral
EP1966132A2 (en) 2005-12-15 2008-09-10 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
CA2644963A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
CA2655282A1 (en) 2006-06-16 2007-12-21 High Point Pharmaceuticals, Llc Pharmaceutical use of substituted piperidine carboxamides
JP2009541268A (ja) 2006-06-22 2009-11-26 ビオヴィトルム・アクチボラゲット(プブリクト) Mnkキナーゼ阻害剤としてのピリジンおよびピラジン誘導体
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US9259426B2 (en) 2006-07-20 2016-02-16 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
EP1903038A1 (de) * 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
JP2010503676A (ja) 2006-09-15 2010-02-04 シェーリング コーポレイション 疼痛、糖尿病および脂質代謝の障害の治療
CN101679261A (zh) 2007-03-09 2010-03-24 阿斯利康(瑞典)有限公司 哌嗪和哌啶mGluR5增效剂
JP5496877B2 (ja) 2007-04-16 2014-05-21 アッヴィ・インコーポレイテッド 7−置換インドールMcl−1阻害薬
CA2719747C (en) 2008-03-28 2018-02-20 Pacific Biosciences Of California, Inc. Compositions and methods for nucleic acid sequencing
EP2133334A1 (en) 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
MX2011002060A (es) 2008-08-25 2011-04-05 Irm Llc Moduladores de la senda de hedgehog.
WO2010087399A1 (ja) 2009-01-30 2010-08-05 第一三共株式会社 ウロテンシンii受容体拮抗薬
CA2758210C (en) 2009-04-20 2017-08-29 F. Hoffmann-La Roche Ag Proline derivatives as cathepsin inhibitors
TW201105665A (en) 2009-04-22 2011-02-16 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
SE533816C2 (sv) 2009-05-06 2011-01-25 Tetra Laval Holdings & Finance Förfarande för framställning av kartongflaskor
WO2010141817A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
EP2270002A1 (en) 2009-06-18 2011-01-05 Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011016559A1 (ja) 2009-08-07 2011-02-10 武田薬品工業株式会社 複素環化合物およびその用途
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
CN102625708A (zh) 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
AU2010341573B2 (en) 2009-12-22 2016-10-13 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
RS53705B1 (sr) 2010-01-29 2015-04-30 Otsuka Pharmaceutical Co., Ltd. Di-supstituisani piridinski derivati kao antikancerska sredstva
AU2011223655A1 (en) 2010-03-03 2012-06-28 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
AU2011229542A1 (en) 2010-03-16 2012-11-08 Merck Patent Gmbh Morpholinylquinazolines
SG183426A1 (en) 2010-04-28 2012-09-27 Daiichi Sankyo Co Ltd [5,6] heterocyclic compound
TW201202230A (en) 2010-05-24 2012-01-16 Mitsubishi Tanabe Pharma Corp Novel quinazoline compound
WO2011153553A2 (en) * 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
WO2011156529A2 (en) 2010-06-08 2011-12-15 Nugen Technologies, Inc. Methods and composition for multiplex sequencing
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
CN103153063B (zh) 2010-07-30 2016-02-17 肿瘤疗法科学股份有限公司 喹啉衍生物及含有其的melk抑制剂
RU2013114771A (ru) 2010-09-03 2014-10-10 Янссен Фармацевтика Нв Диамиды азетидинила как ингибиторы моноацилглицерол липазы
ES2624845T3 (es) 2010-09-29 2017-07-17 Intervet International B.V. Compuestos de N-heteroarilo con unidad de puente cíclico para el tratamiento de enfermedades parasitarias
CA2815350A1 (en) 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
JP2014504269A (ja) * 2010-11-05 2014-02-20 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー2、リミテッド 化学化合物
US9260484B2 (en) 2011-06-15 2016-02-16 Ohio State Innovation Foundation Small molecule composite surfaces as inhibitors of protein-protein interactions
CA2840627A1 (en) 2011-06-29 2013-01-03 Otsuka Pharmaceutical Co., Ltd. Quinazolines as therapeutic compounds and related methods of use
CN103087077B (zh) 2011-11-03 2016-05-18 上海希迈医药科技有限公司 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用
JP2013107855A (ja) 2011-11-22 2013-06-06 Mitsubishi Tanabe Pharma Corp 医薬組成物
US9745631B2 (en) 2011-12-20 2017-08-29 Dana-Farber Cancer Institute, Inc. Methods for diagnosing and treating oncogenic kras-associated cancer
WO2013096151A1 (en) * 2011-12-22 2013-06-27 Glaxosmithkline Llc Chemical compounds
WO2013106641A1 (en) 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
US9932317B2 (en) 2012-03-19 2018-04-03 Imperial Innovations Limited Quinazoline compounds and their use in therapy
WO2013155077A1 (en) 2012-04-09 2013-10-17 Board Of Regents,The University Of Texas System Response markers for src inhibitor therapies
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
KR20150006477A (ko) 2012-05-09 2015-01-16 그래댈리스, 인코포레이티드 단일-뉴클레오타이드 kras 돌연변이에 특이적인 이-기능성 짧은-헤어핀 rna (bi-shrna)
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
RU2679130C2 (ru) 2012-07-11 2019-02-06 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
TW201414737A (zh) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
WO2014030743A1 (ja) 2012-08-24 2014-02-27 武田薬品工業株式会社 複素環化合物
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
KR20150135359A (ko) 2013-03-14 2015-12-02 컨버진 엘엘씨 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물
WO2014143659A1 (en) 2013-03-15 2014-09-18 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.
MX364438B (es) * 2013-03-15 2019-04-26 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
EP3008465B1 (en) 2013-06-13 2019-08-07 Biodesy, Inc. Method of screening candidate biochemical entities targeting a target biochemical entity
BR112015032921B1 (pt) 2013-07-03 2022-06-14 Karyopharm Therapeutics, Inc Compostos de benzofuranila e benzoxazolila substituídos e utilizações dos mesmos
KR20160036053A (ko) 2013-07-31 2016-04-01 메르크 파텐트 게엠베하 Btk 저해제로서 피리딘, 피리미딘, 및 피라진, 및 이들의 용도
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
UA119971C2 (uk) * 2013-10-10 2019-09-10 Араксіс Фарма Ллк Інгібітори g12c kras
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
MX2016009403A (es) 2014-02-03 2016-09-16 Cadila Healthcare Ltd Compuestos heterociclicos.
EP3922630A1 (en) 2014-03-20 2021-12-15 Capella Therapeutics, Inc. Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer
WO2015144001A1 (zh) 2014-03-24 2015-10-01 南京明德新药研发股份有限公司 作为smo抑制剂的喹啉衍生物
MA40074A (fr) 2014-05-30 2015-12-03 Univ Columbia Composés liant ras multivalents
US10092555B2 (en) 2014-06-27 2018-10-09 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon and other E3 ubiquitin ligases
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
KR20170103838A (ko) 2015-01-23 2017-09-13 컨플루언스 라이프 사이언시스, 인코포레이티드 염증 및 암의 치료를 위한 헤테로시클릭 itk 저해제
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
MX388781B (es) 2015-07-22 2025-03-20 Araxes Pharma Llc Compuestos de quinazolina sustituido y su uso como inhibidores de proteínas kras, hras y/o nras mutantes g12c.
US10689356B2 (en) 2015-09-28 2020-06-23 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
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
US10882847B2 (en) 2015-09-28 2021-01-05 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
EP3356347A1 (en) 2015-09-28 2018-08-08 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
PL3365334T3 (pl) 2015-10-21 2024-11-25 Otsuka Pharmaceutical Co., Ltd. Związki benzolaktamu jako inhibitory kinazy białkowej
CA3005089A1 (en) 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
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
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
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質の阻害剤
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
MX392031B (es) 2016-11-03 2025-03-21 Corvus Pharmaceuticals Inc Compuestos y métodos para modular la cinasa de linfocitos t inducible por interleucina 2
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
JP2020521740A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体kras、hrasまたはnrasの調節因子としてのキナゾリン誘導体
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
JP7266043B2 (ja) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド KRas G12C阻害剤及びそれを使用する方法
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
EP3870585A1 (en) 2018-10-24 2021-09-01 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
JP2020203966A (ja) 2019-06-14 2020-12-24 大塚化学株式会社 摩擦材組成物、摩擦材、及び摩擦部材
JP2024163372A (ja) 2023-05-11 2024-11-22 株式会社大一商会 遊技機

Also Published As

Publication number Publication date
AU2016245864A1 (en) 2017-10-26
MX2017012979A (es) 2017-11-28
TW201702232A (zh) 2017-01-16
EA201792214A1 (ru) 2018-01-31
EP3280708B1 (en) 2021-09-01
BR112017021869A2 (pt) 2018-12-11
CN107849022A (zh) 2018-03-27
US20190284144A1 (en) 2019-09-19
WO2016164675A1 (en) 2016-10-13
UY36612A (es) 2016-11-30
WO2016164675A8 (en) 2017-05-11
ES2898765T3 (es) 2022-03-08
JP2018513853A (ja) 2018-05-31
KR20180005178A (ko) 2018-01-15
JP2021098721A (ja) 2021-07-01
US10829458B2 (en) 2020-11-10
EP3280708A1 (en) 2018-02-14
US10246424B2 (en) 2019-04-02
AU2016245864C1 (en) 2021-09-09
AU2016245864B2 (en) 2020-10-22
US20160297774A1 (en) 2016-10-13
USRE50490E1 (en) 2025-07-15
MX382355B (es) 2025-03-13
JO3707B1 (ar) 2021-01-31
CA2981530A1 (en) 2016-10-13

Similar Documents

Publication Publication Date Title
HK1248231A1 (zh) 取代的喹唑啉化合物和其使用方法
MX2018005967A (es) Compuestos de quinazolina 2-sustituida que comprenden un grupo heterociclico sustituido y metodos de uso de los mismos.
PH12019550248A1 (en) Covalent inhibitors of kras
PH12016500538A1 (en) Inhibitors of kras g12c
JO3805B1 (ar) مثبطات كراس جي12سي
MX2017013275A (es) Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos.
MX2021005924A (es) Compuestos y metodos de uso de los mismos para el tratamiento del cancer.
MX388781B (es) Compuestos de quinazolina sustituido y su uso como inhibidores de proteínas kras, hras y/o nras mutantes g12c.
CA2983481A1 (en) Janus kinase inhibitor
MX2015017215A (es) Compuestos de sulfonamida biciclicos como inhibidores de los canales de sodio.
WO2016044556A3 (en) Arginine methyltransferase inhibitors and uses thereof
MX2017007607A (es) Inhibidores de necrosis celular y metodos relacionados.
IL292657A (en) Therapeutic history of interleukin-22
PH12018501285A1 (en) Alkyl dihydroquinoline sulfonamide compounds
TW201713630A (en) Substituted quinazoline compounds and methods of use thereof
MY188058A (en) Inhibitors of kras g12c
JOP20160150B1 (ar) مركبات كينازولين مستبدلة وطرق استعمالها
HK40108760A (zh) 白细胞介素-22的治疗性衍生物
HK40079539A (en) Therapeutic derivatives of interleukin-22
WO2018067638A3 (en) High mobility group b1 protein inhibitors
HK40119663A (zh) Tyk2抑制剂的剂型
HK40105168A (zh) 药学化合物、其盐类、其制剂和其制备和使用方法
HK40078214A (en) Pharmaceutical compounds and methods of use
HK40062425A (en) Pharmaceutical formulations of fcrn inhibitors suitable for subcutaneous administration
HK40037688A (en) Pharmaceutically active pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives