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SMT202200053T1 - Inibitori di kras g12c e metodi di uso degli stessi - Google Patents

Inibitori di kras g12c e metodi di uso degli stessi

Info

Publication number
SMT202200053T1
SMT202200053T1 SM20220053T SMT202200053T SMT202200053T1 SM T202200053 T1 SMT202200053 T1 SM T202200053T1 SM 20220053 T SM20220053 T SM 20220053T SM T202200053 T SMT202200053 T SM T202200053T SM T202200053 T1 SMT202200053 T1 SM T202200053T1
Authority
SM
San Marino
Prior art keywords
kras
inhibitors
methods
same
Prior art date
Application number
SM20220053T
Other languages
English (en)
Inventor
David John Kopecky
Victor J Cee
Patricia Lopez
Youngsook Shin
Nobuko Nishimura
Brian Alan Lanman
Anthony B Reed
Shon Booker
Jian Chen
Longbin Liu
Ryan Paul Wurz
Thomas T Nguyen
Nuria A Tamayo
John Gordon Allen
Jennifer Rebecca Allen
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of SMT202200053T1 publication Critical patent/SMT202200053T1/it

Links

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/12—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 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
    • C07D475/00—Heterocyclic compounds containing pteridine ring 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
SM20220053T 2017-05-22 2018-05-21 Inibitori di kras g12c e metodi di uso degli stessi SMT202200053T1 (it)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762509629P 2017-05-22 2017-05-22
PCT/US2018/033714 WO2018217651A1 (en) 2017-05-22 2018-05-21 Kras g12c inhibitors and methods of using the same
EP18731624.5A EP3630761B1 (en) 2017-05-22 2018-05-21 Kras g12c inhibitors and methods of using the same

Publications (1)

Publication Number Publication Date
SMT202200053T1 true SMT202200053T1 (it) 2022-03-21

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SM20220053T SMT202200053T1 (it) 2017-05-22 2018-05-21 Inibitori di kras g12c e metodi di uso degli stessi

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US (4) US10519146B2 (it)
EP (2) EP3974429A1 (it)
JP (4) JP6785819B2 (it)
KR (4) KR102573230B1 (it)
CN (2) CN115626923B (it)
AR (9) AR111882A1 (it)
AU (3) AU2018273356B2 (it)
BR (1) BR112019024525B1 (it)
CA (1) CA3063469C (it)
CL (2) CL2019003394A1 (it)
CO (1) CO2019013010A2 (it)
CR (2) CR20190534A (it)
CY (1) CY1125289T1 (it)
DK (1) DK3630761T3 (it)
EA (1) EA201992781A1 (it)
ES (1) ES2905676T3 (it)
HR (1) HRP20212017T1 (it)
HU (1) HUE057632T2 (it)
IL (2) IL270490B (it)
JO (1) JOP20190272A1 (it)
LT (1) LT3630761T (it)
MA (1) MA48772B1 (it)
MX (2) MX386189B (it)
MY (1) MY199303A (it)
NZ (1) NZ758786A (it)
PE (1) PE20200733A1 (it)
PH (1) PH12019502579A1 (it)
PL (1) PL3630761T3 (it)
PT (1) PT3630761T (it)
RS (1) RS62800B1 (it)
SA (2) SA522432081B1 (it)
SG (1) SG10201913195RA (it)
SI (1) SI3630761T1 (it)
SM (1) SMT202200053T1 (it)
TW (2) TWI780154B (it)
UA (1) UA127968C2 (it)
UY (1) UY37744A (it)
WO (1) WO2018217651A1 (it)
ZA (3) ZA201907651B (it)

Families Citing this family (186)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201906223TA (en) * 2016-12-22 2019-08-27 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
JOP20190272A1 (ar) * 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
ES2985118T3 (es) 2017-09-08 2024-11-04 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
US11161841B2 (en) 2018-04-04 2021-11-02 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
US11045484B2 (en) 2018-05-04 2021-06-29 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020010836A (es) * 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
ES2986917T3 (es) 2018-05-10 2024-11-13 Amgen Inc Inhibidores de KRAS G12C para el tratamiento del cáncer
JP7360396B2 (ja) 2018-06-01 2023-10-12 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤及び同一物の使用方法
EP4268898A3 (en) * 2018-06-11 2024-01-17 Amgen Inc. Kras g12c inhibitors for treating cancer
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
EA202190137A1 (ru) 2018-06-27 2021-05-17 Бристол-Маерс Сквибб Компани Нафтиридиноновые соединения для применения в качестве активаторов t-клеток
CA3104654A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators
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
MX2021005700A (es) 2018-11-19 2021-07-07 Amgen Inc Inhibidores de kras g12c y metodos de uso de los mismos.
WO2020123395A1 (en) 2018-12-10 2020-06-18 Ideaya Biosciences, Inc. 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors
JP2022518591A (ja) * 2019-01-29 2022-03-15 博瑞生物医薬（蘇州）股▲分▼有限公司 複素環式化合物であるベンゾピリドンおよびその使用
WO2020165732A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
JP2022529523A (ja) * 2019-04-22 2022-06-22 ユニバーシティ オブ ピッツバーグ －オブ ザ コモンウェルス システム オブ ハイヤー エデュケイション 小児対象において神経膠腫を治療するためのｔｇ０２の使用
KR20220012255A (ko) * 2019-04-28 2022-02-03 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 옥사아자퀴나졸린-7(8h)-케톤 화합물, 이의 제조 방법 및 이의 약학적 응용
EP3738593A1 (en) * 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
JP2022532790A (ja) 2019-05-21 2022-07-19 アムジエン・インコーポレーテツド 固体形態
WO2020233592A1 (en) * 2019-05-21 2020-11-26 Inventisbio Shanghai Ltd. Heterocyclic compounds, preparation methods and uses thereof
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
CA3139769A1 (en) 2019-05-29 2020-12-03 Shiqiang Liu Nitrogen-containing heterocyclic derivative regulator, preparation method therefor and application thereof
CN112552294B (zh) * 2019-09-10 2023-12-19 上海翰森生物医药科技有限公司 含哌嗪杂环类衍生物抑制剂、其制备方法和应用
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
CA3144548A1 (en) * 2019-06-24 2020-12-30 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12c
US20220372036A1 (en) * 2019-06-25 2022-11-24 Medshine Discovery Inc. Seven-membered heterocyclic derivative acting as kras g12c mutant protein inhibitor
CN110256421A (zh) * 2019-06-26 2019-09-20 微境生物医药科技(上海)有限公司 Kras-g12c抑制剂
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
CN112300194B (zh) * 2019-07-30 2022-01-14 上海凌达生物医药有限公司 一类稠环吡啶酮类化合物、制备方法和用途
KR20220079521A (ko) * 2019-08-02 2022-06-13 상하이 제민케어 파마슈티칼스 컴퍼니 리미티드 테트라시클릭 화합물, 그의 제조 방법 및 용도
CN112341457A (zh) * 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CN112390788A (zh) * 2019-08-13 2021-02-23 苏州闻天医药科技有限公司 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途
CN112390797A (zh) * 2019-08-15 2021-02-23 微境生物医药科技(上海)有限公司 新型螺环类K-Ras G12C抑制剂
CN112390796B (zh) * 2019-08-19 2023-06-27 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
JP7607642B2 (ja) 2019-09-11 2024-12-27 キラル クエスト （スーチョウ） カンパニー、リミテッド Ｋｒａｓ阻害剤である複素環式中間体に適用される合成方法
CN119462689A (zh) 2019-09-20 2025-02-18 上海济煜医药科技有限公司 稠合吡啶酮类化合物及其制备方法和应用
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
KR20220091480A (ko) 2019-09-24 2022-06-30 미라티 테라퓨틱스, 인크. 병용 요법
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
US20240190862A1 (en) 2019-10-24 2024-06-13 Amgen Inc. Epoxyamides as kras g12c and kras g12d inhibitors and methods of using the same
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
JOP20220101A1 (ar) 2019-10-28 2023-01-30 Merck Sharp & Dohme مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS)
CN115057872B (zh) * 2019-10-30 2025-03-18 劲方医药科技(上海)股份有限公司 取代的杂环并环类化合物，其制法与医药上的用途
EP4054719A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
AU2020377925A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
AU2020379731A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
TW202132271A (zh) 2019-11-14 2021-09-01 美商安進公司 Ｋｒａｓ ｇ１２ｃ抑制劑化合物之改善的合成
IL292315A (en) * 2019-11-14 2022-06-01 Amgen Inc Improved synthesis of kras g12c inhibitor compound
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
TW202133855A (zh) 2019-11-27 2021-09-16 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CN111377918B (zh) * 2019-11-29 2021-03-02 苏州信诺维医药科技有限公司 一种kras抑制剂化合物
US20230061083A1 (en) * 2019-11-29 2023-03-02 Evopoint Biosciences Co., Ltd. Kras g12c inhibitor compound and use thereof
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
WO2021113595A1 (en) * 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
AU2020401223A1 (en) * 2019-12-10 2022-06-23 The Board Of Regents Of The University Of Texas System Compositions and methods for substituted 7-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine analogs as inhibitors of KRAS
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor
WO2021120045A1 (en) * 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
CN115192577B (zh) 2019-12-19 2024-03-29 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
WO2021139678A1 (zh) * 2020-01-07 2021-07-15 广州百霆医药科技有限公司 吡啶并嘧啶类kras g12c突变蛋白抑制剂
TWI770760B (zh) 2020-01-08 2022-07-11 大陸商蘇州亞盛藥業有限公司 螺環四氫喹唑啉
CN114671866A (zh) * 2020-12-25 2022-06-28 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
CN111205286B (zh) * 2020-01-13 2022-12-13 中科苏州药物研究院 作为kras g12c突变蛋白抑制剂的腈甲基哌嗪类衍生物及其应用
WO2021150613A1 (en) 2020-01-20 2021-07-29 Incyte Corporation Spiro compounds as inhibitors of kras
WO2021147965A1 (zh) * 2020-01-21 2021-07-29 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
CN112159405B (zh) * 2020-02-04 2021-09-14 广州必贝特医药技术有限公司 吡啶并嘧啶酮类化合物及其应用
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
CN113248521B (zh) * 2020-02-11 2023-07-18 上海和誉生物医药科技有限公司 一种k-ras g12c抑制剂及其制备方法和应用
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
JP7462985B2 (ja) * 2020-02-24 2024-04-08 上海▲テツ▼▲ギョウ▼生物科技有限公司 芳香族化合物および抗腫瘍薬物の調製におけるその使用
WO2021175199A1 (zh) * 2020-03-02 2021-09-10 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
WO2021185233A1 (en) * 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN115335372B (zh) * 2020-04-03 2024-01-12 南京明德新药研发有限公司 八氢吡嗪并二氮杂萘啶二酮类化生物
WO2021218939A1 (zh) * 2020-04-28 2021-11-04 贝达药业股份有限公司 稠环化合物及其在医药上的应用
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
US20230241073A1 (en) 2020-05-18 2023-08-03 Wellmarker Bio Co., Ltd. Pharmaceutical composition for preventing or treating non-small cell lung cancer associated with ron mutantation, and method using same
WO2021236920A1 (en) * 2020-05-20 2021-11-25 Teva Pharmaceuticals International Gmbh Solid state forms of amg-510 and process for preparation thereof
CN112574199B (zh) * 2020-05-20 2021-05-18 首药控股(北京)股份有限公司 Kras-G12C抑制剂杂环化合物
AU2021285032A1 (en) 2020-06-02 2022-12-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2021244555A1 (zh) * 2020-06-02 2021-12-09 上海喆邺生物科技有限公司 一种手性中间体及其制备方法
WO2021249563A1 (zh) * 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
EP4171570A1 (en) 2020-06-24 2023-05-03 Boehringer Ingelheim International GmbH Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
CN115996717A (zh) * 2020-06-25 2023-04-21 托雷莫治疗股份公司 用于治疗癌症的cbp/p300溴结构域抑制剂和kras抑制剂的组合
CN113929676A (zh) * 2020-07-14 2022-01-14 浙江海正药业股份有限公司 吡啶并杂环类衍生物及其制备方法和用途
CN113980032B (zh) * 2020-07-27 2023-06-16 江苏恒瑞医药股份有限公司 稠合四环类衍生物、其制备方法及其在医药上的应用
CN115052870B (zh) 2020-08-02 2024-02-20 上海喆邺生物科技有限公司 一种芳香类化合物及其在抗肿瘤药物中的应用
CN114075195A (zh) * 2020-08-21 2022-02-22 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
WO2022037630A1 (zh) * 2020-08-21 2022-02-24 浙江海正药业股份有限公司 四环类衍生物、其制备方法及其医药上的用途
WO2022047093A1 (en) * 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
KR20230081726A (ko) 2020-09-03 2023-06-07 레볼루션 메디슨즈, 인크. Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도
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
WO2022066805A1 (en) 2020-09-23 2022-03-31 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
CN116323611A (zh) 2020-10-07 2023-06-23 美国安进公司 使7-氯-6-氟-1-(2-异丙基-4-甲基吡啶-3-基)吡啶并[2,3-d]嘧啶-2,4(1h,3h)-二酮的阻转异构体外消旋和分离的方法
TW202233629A (zh) 2020-10-20 2022-09-01 美商安進公司 雜環螺環化合物及使用方法
JP2023549055A (ja) 2020-10-27 2023-11-22 アムジエン・インコーポレーテツド 複素環式スピロ化合物及びその使用方法
TW202224682A (zh) * 2020-11-13 2022-07-01 美商建南德克公司 用於治療實性瘤之方法與包含ｋｒａｓｇ１２ｃ抑制劑及ｖｅｇｆ抑制劑之組成物
CA3201663A1 (en) * 2020-11-20 2022-05-27 Amgen Inc. Process for preparing 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidine-2,4(1h,3h)-dione
CN116390919A (zh) * 2020-11-24 2023-07-04 杭州多域生物技术有限公司 一种芳香化合物、其制备方法及应用
WO2022111513A1 (zh) * 2020-11-24 2022-06-02 杭州多域生物技术有限公司 一种芳香化合物、其制备方法及应用
JP2023551006A (ja) * 2020-11-26 2023-12-06 上▲海▼翰森生物医▲薬▼科技有限公司 窒素含有複素環誘導体の塩、結晶、並びにその調製方法、及び使用
CN116171155B (zh) * 2020-12-08 2024-09-17 上海和誉生物医药科技有限公司 吡啶并[2,3-d]嘧啶-2(1H)-酮衍生物及其制备方法和应用
JP2023553534A (ja) * 2020-12-11 2023-12-21 エラスカ，インク． 癌の処置のための併用療法
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
TWI795129B (zh) * 2020-12-18 2023-03-01 大陸商正大天晴藥業集團股份有限公司 吡啶并嘧啶酮類化合物
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
CN114685502A (zh) * 2020-12-25 2022-07-01 由理生物医药（上海）有限公司 作为kras-g12c抑制剂的螺环类化合物
US20240091230A1 (en) 2021-01-08 2024-03-21 Amgen Inc. Use of kras g12c inhibitor in treating cancers
EP4281457A4 (en) * 2021-03-10 2024-07-31 Beta Pharma, Inc. PYRIDOPYRIMIDINE DERIVATIVES AS KRAS INHIBITORS
US20240189313A1 (en) * 2021-03-11 2024-06-13 InventisBio Co., Ltd. Solid dispersions
CN113018415B (zh) * 2021-03-17 2022-07-01 遵义医科大学 一种药物组合及其应用
US12077539B2 (en) 2021-03-22 2024-09-03 Incyte Corporation Imidazole and triazole KRAS inhibitors
EP4319757A1 (en) 2021-04-09 2024-02-14 Boehringer Ingelheim International GmbH Anticancer therapy
WO2022232318A1 (en) * 2021-04-27 2022-11-03 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
AU2022265682A1 (en) 2021-04-29 2023-11-09 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
US20230106174A1 (en) 2021-05-05 2023-04-06 Revolution Medicines, Inc. Ras inhibitors
EP4334325A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
JP2024518845A (ja) 2021-05-19 2024-05-07 テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハー ソトラシブ及びその固体状態形態の調製のためのプロセス
EP4340883A1 (en) * 2021-05-19 2024-03-27 Genentech, Inc. Combination therapy
CA3221390A1 (en) * 2021-05-25 2022-12-01 Erasca, Inc. Sulfur-containing heteroaromatic tricyclic kras inhibitors
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022262797A1 (en) * 2021-06-18 2022-12-22 Shanghai Antengene Corporation Limited Combination of an erk inhibitor and a kras inhibitor and uses thereof
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
WO2022269008A1 (en) 2021-06-24 2022-12-29 Sandoz Ag Crystalline form of sotorasib
EP4227305A1 (en) 2022-02-10 2023-08-16 Sandoz AG Crystalline form of sotorasib
US20240417412A1 (en) * 2021-08-10 2024-12-19 Amgen Inc. Heterocyclic compounds and methods of use
AU2022336415A1 (en) 2021-09-01 2024-01-04 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
CN114605406B (zh) * 2021-09-18 2023-05-26 都创(上海)医药开发有限公司 Amg510化合物的晶型及其制备方法和用途
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
AU2022356286B2 (en) 2021-10-01 2024-10-10 Xinthera, Inc. Azetidine and pyrrolidine parp1 inhibitors and uses thereof
JP2024537824A (ja) 2021-10-01 2024-10-16 インサイト・コーポレイション ピラゾロキノリンｋｒａｓ阻害剤
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
EP4415824A1 (en) 2021-10-14 2024-08-21 Incyte Corporation Quinoline compounds as inhibitors of kras
WO2023066371A1 (zh) 2021-10-22 2023-04-27 江苏恒瑞医药股份有限公司 含氮的四环化合物、其制备方法及其在医药上的应用
TW202334089A (zh) 2021-11-02 2023-09-01 美商夫雷爾醫療公司 Ｐｐａｒｇ反向激動劑及其用途
CN118139861A (zh) * 2021-11-05 2024-06-04 苏州信诺维医药科技股份有限公司 Kras突变体抑制剂的晶型、其制备方法及其应用
WO2023097194A2 (en) 2021-11-24 2023-06-01 Genentech, Inc. Therapeutic compounds and methods of use
TW202332429A (zh) 2021-11-24 2023-08-16 美商建南德克公司 治療性化合物及其使用方法
AU2022402390A1 (en) 2021-12-01 2024-05-30 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4448526A1 (en) 2021-12-17 2024-10-23 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CN118339153A (zh) 2021-12-22 2024-07-12 勃林格殷格翰国际有限公司 用于治疗癌症的杂芳族化合物
CA3240772A1 (en) 2021-12-22 2023-06-29 Kevan M. Shokat Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
KR20240133756A (ko) 2022-01-21 2024-09-04 신테라, 인크. Parp1 저해제 및 이의 용도
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
MX2024010045A (es) 2022-02-16 2024-08-26 Amgen Inc Compuestos de quinazolina y uso de los mismos como inhibidores de proteinas mutantes kras.
WO2023159087A1 (en) 2022-02-16 2023-08-24 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
AU2023230882A1 (en) 2022-03-07 2024-08-22 Amgen Inc. A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile.
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
KR20240163107A (ko) 2022-03-11 2024-11-18 컴쿼트 바이오사이언시즈 인크. 헤테로환 화합물 및 이의 용도
MX2024010728A (es) 2022-03-31 2024-09-10 Eisai R&D Man Co Ltd Composicion farmaceutica para tratar tumores.
WO2023194310A1 (en) 2022-04-04 2023-10-12 Sanofi Therapeutic combination of kras g12c inhibitor and tead inhibitor
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
TW202400596A (zh) 2022-04-28 2024-01-01 美商辛瑟拉股份有限公司 三環parp1抑制劑及其用途
KR20250022133A (ko) 2022-06-10 2025-02-14 레볼루션 메디슨즈, 인크. 거대고리 ras 억제제
WO2024031088A1 (en) 2022-08-05 2024-02-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
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
CN115368358A (zh) * 2022-09-01 2022-11-22 浙江九洲药业股份有限公司 一种Sotorasib新晶型及其制备方法与应用
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
TW202430179A (zh) 2022-11-21 2024-08-01 美商樹線生物科學公司 螺環二氫哌喃并嘧啶ＫＲａｓ抑制劑
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
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
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
TW202500126A (zh) 2023-05-24 2025-01-01 美商金橘生物科技公司 雜環化合物及其用途
WO2024246114A1 (en) 2023-05-31 2024-12-05 Boehringer Ingelheim International Gmbh Survivin as a biomarker for predicting the responsiveness of cancer treatment
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
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025034849A1 (en) * 2023-08-08 2025-02-13 Theras, Inc. Fused pyridazines for the treatment of cancer and other indications
WO2025064848A1 (en) 2023-09-21 2025-03-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyridine kras inhibitors
WO2025067459A2 (en) 2023-09-29 2025-04-03 D3 Bio (Wuxi) Co., Ltd. Therapies for the treatment of cancer

Family Cites Families (235)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4232027A (en) 1979-01-29 1980-11-04 E. R. Squibb & Sons, Inc. 1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives
GB2116183B (en) 1982-03-03 1985-06-05 Genentech Inc Human antithrombin iii dna sequences therefore expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby a process for expressing human antithrombin iii and pharmaceutical compositions comprising it
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
GB8912336D0 (en) 1989-05-30 1989-07-12 Smithkline Beckman Intercredit Compounds
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
CA2066898A1 (en) 1991-04-29 1992-10-30 Chuan Shih Pharmaceutical compounds
ES2108120T3 (es) 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
JP3560609B2 (ja) 1992-11-13 2004-09-02 イミュネックス・コーポレーション Ｅｌｋリガンドと呼ばれる新規なサイトカイン
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
US5612340A (en) 1993-10-01 1997-03-18 Ciba-Geigy Corporation Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
HUT74686A (en) 1993-12-17 1997-01-28 Sandoz Ag Rapamycin derivatives, their pharmaceutical use, process for producing them and pharmaceutical composition containing them as active agents
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
WO1995028484A1 (en) 1994-04-15 1995-10-26 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
DK0682027T3 (da) 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
ES2161290T3 (es) 1995-03-30 2001-12-01 Pfizer Derivados de quinazolina.
ES2150113T3 (es) 1995-04-03 2000-11-16 Novartis Ag Derivados de pirazol y procedimientos para la preparacion de los mismos.
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
TR199701567T1 (xx) 1995-06-09 1998-04-21 Novartis Ag Rapamisin t�revleri.
DE69619114T2 (de) 1995-07-06 2002-10-02 Novartis Ag, Basel Pyrolopyrimidine und verfahren zu ihrer herstellung
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
EP0888349B1 (en) 1996-01-23 2002-05-22 Novartis AG Pyrrolopyrimidines and processes for their preparation
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU716383B2 (en) 1996-03-15 2000-02-24 Novartis Ag Novel N-7-heterocyclyl pyrrolo(2,3-d)pyrimidines and the use thereof
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
ES2249800T3 (es) 1996-06-24 2006-04-01 Pfizer Inc. Derivados triciclicos sustituidos con fenilamino para el tratamento de enfermedades hiperproliferativas.
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
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
WO1998002437A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
JP3299975B2 (ja) 1996-07-18 2002-07-08 ファイザー・インク マトリックスメタロプロテアーゼのホスフィン酸塩ベース阻害薬
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
EP0920505B1 (en) 1996-08-16 2008-06-04 Schering Corporation Mammalian cell surface antigens; related reagents
BR9711223A (pt) 1996-08-23 1999-08-17 Pfizer Derivados de cido arilsulfonilamino-hidrox mico
AU720429B2 (en) 1996-08-23 2000-06-01 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
ATE291022T1 (de) 1996-10-02 2005-04-15 Novartis Pharma Gmbh Pyrimiderivate und verfahren zu ihrer herstellung
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
JP3338064B2 (ja) 1997-01-06 2002-10-28 ファイザー・インク 環状スルホン誘導体
ATE248812T1 (de) 1997-02-03 2003-09-15 Pfizer Prod Inc Arylsulfonylhydroxamsäurederivate
AU749750B2 (en) 1997-02-05 2002-07-04 Warner-Lambert Company Pyrido {2,3-d} pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク Ｎ−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
HUP0000657A3 (en) 1997-02-11 2000-10-30 Pfizer N-arylsulfonyl-piperidine, -morpholine hydroxamic acid derivatives and pharmaceutical compositions containing them
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
AU8689298A (en) 1997-08-05 1999-03-01 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
CN1171866C (zh) 1997-08-08 2004-10-20 辉瑞产品公司 芳氧基芳基磺酰氨基异羟肟酸衍生物
JP2001520039A (ja) 1997-10-21 2001-10-30 ヒューマン ジノーム サイエンシーズ， インコーポレイテッド ヒト腫瘍壊死因子レセプター様タンパク質、ｔｒ１１，ｔｒ１１ｓｖ１およびｔｒ１１ｓｖ２
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
CA2319236A1 (en) 1998-02-09 1999-08-12 Genentech, Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
JP2002505330A (ja) 1998-03-04 2002-02-19 ブリストル−マイヤーズ スクイブ カンパニー ヘテロシクロ−置換イミダゾピラジン・たんぱくチロシンキナーゼ抑制剤
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
KR100743287B1 (ko) 1998-05-29 2007-07-26 수젠, 인크. 피롤기로 치환된 2-인돌리논 단백질 인산화 효소 억제제
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
EP1109555A4 (en) 1998-08-31 2001-11-21 Merck & Co Inc NEW ANGIOGENIC INHIBITORS
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
WO2000041698A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
ATE324444T1 (de) 1999-06-07 2006-05-15 Immunex Corp Tek-antagonisten
EP1196186B1 (en) 1999-07-12 2007-10-31 Genentech, Inc. Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs
ATE264863T1 (de) 1999-08-24 2004-05-15 Ariad Gene Therapeutics Inc 28-epirapaloge
PL203782B1 (pl) 1999-11-05 2009-11-30 Astrazeneca Ab Pochodne chinazoliny,sposoby ich wytwarzania,ich kompozycje farmaceutyczne oraz ich zastosowania
JP5336686B2 (ja) 1999-11-24 2013-11-06 スージェン， インク． 遊離酸または遊離塩基としてイオン化可能な医薬品のための処方
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
ATE358718T1 (de) 2000-02-25 2007-04-15 Immunex Corp Integrin antagonisten
KR100773621B1 (ko) 2000-07-19 2007-11-05 워너-램버트 캄파니 엘엘씨 4-요오도 페닐아미노 벤즈히드록삼산의 산소화 에스테르
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
MXPA03005696A (es) 2000-12-21 2003-10-06 Glaxo Group Ltd Pirimidinaminas como moduladores de angiogenesis.
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
JP2002233610A (ja) 2002-02-18 2002-08-20 Olympia:Kk スロットマシン
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
RU2369636C2 (ru) 2003-05-23 2009-10-10 Уайт Лиганд gitr и связанные с лигандом gitr молекулы и антитела и варианты их применения
PT1646634E (pt) 2003-07-08 2009-02-16 Novartis Ag Utilização de rapamicina e derivados de rapamicina para o tratamento de perda óssea
EP1648900A4 (en) 2003-07-11 2010-02-10 Ariad Pharma Inc PHOSPHORUS MACROCYCLES
US20050048054A1 (en) 2003-07-11 2005-03-03 Shino Hanabuchi Lymphocytes; methods
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
CA2531506A1 (en) 2003-08-22 2005-03-10 Avanir Pharmaceuticals Substituted naphthyridine derivatives as inhibitors of macrophage migration inhibitory factor and their use in the treatment of human diseases
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
MX2007002312A (es) 2004-08-26 2007-04-16 Pfizer Compuestos de aminoheteroarilo enantiomericamente puros como inhibidores de proteina quinasa.
MX2007004489A (es) 2004-10-13 2007-09-21 Wyeth Corp Analogos de 17-hidroxiwortamina como inhibidores pi3k.
CA2583217C (en) 2004-10-18 2011-05-31 Amgen Inc. 1,3,4-thiadiazole compounds as protein kinase inhibitors
WO2006105021A2 (en) 2005-03-25 2006-10-05 Tolerrx, Inc. Gitr binding molecules and uses therefor
RU2406760C3 (ru) 2005-05-09 2017-11-28 Оно Фармасьютикал Ко., Лтд. Моноклональные антитела человека к белку программируемой смерти 1 (pd-1) и способы лечения рака с использованием анти-pd-1-антител самостоятельно или в комбинации с другими иммунотерапевтическими средствами
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007034327A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
KR20080091369A (ko) 2006-01-18 2008-10-10 암젠 인크 단백질 키나제 ｂ （ｐｋｂ） 억제제로서 티아졸 화합물
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
ES2544082T3 (es) 2006-12-07 2015-08-27 F. Hoffmann-La Roche Ag Compuestos inhibidores de fosfoinosítido 3-quinasa y métodos de uso
WO2008118468A1 (en) 2007-03-23 2008-10-02 Amgen Inc. Heterocyclic compounds and their uses
SI2139882T1 (sl) 2007-03-23 2014-03-31 Amgen Inc. 3-substituirani kinolinski ali kinoksalinski derivati in njihoba uporaba kot inhibitorji fosfatidilinozitol 3-kinaze (pi3k)
EP2132207A2 (en) 2007-03-23 2009-12-16 Amgen Inc. Heterocyclic compounds and their uses
EP2170887A2 (en) 2007-06-07 2010-04-07 Amgen Inc. Heterocyclic compounds as raf kinase modulators
DK2175884T3 (en) 2007-07-12 2016-09-26 Gitr Inc Combination USING GITR BINDING MOLECULES
US7919504B2 (en) 2007-07-17 2011-04-05 Amgen Inc. Thiadiazole modulators of PKB
AU2008276521B2 (en) 2007-07-17 2011-11-03 Amgen Inc. Heterocyclic modulators of PKB
EP2183232B1 (en) 2007-08-02 2013-03-06 Amgen, Inc Pi3 kinase modulators and methods of use
WO2009036082A2 (en) 2007-09-12 2009-03-19 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
EP2231656A1 (en) 2007-12-19 2010-09-29 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
CA2710194C (en) 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
MX2010010975A (es) 2008-04-07 2010-11-01 Amgen Inc Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular.
ES2474147T3 (es) 2008-05-30 2014-07-08 Amgen, Inc Inhibidores de PI3 cinasa
EA201170031A1 (ru) 2008-07-02 2011-08-30 Эмерджент Продакт Дивелопмент Сиэтл, Ллс СВЯЗЫВАЮЩИЕ НЕСКОЛЬКО МИШЕНЕЙ БЕЛКИ, ОБЛАДАЮЩИЕ АНТАГОНИСТИЧЕСКИМ ДЕЙСТВИЕМ ПО ОТНОШЕНИЮ К TGF-β
JPWO2010030002A1 (ja) 2008-09-12 2012-02-02 国立大学法人三重大学 外来性ｇｉｔｒリガンド発現細胞
US20110263647A1 (en) 2009-01-15 2011-10-27 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
CA2752527C (en) 2009-02-18 2014-09-23 Amgen Inc. Indole/benzimidazole compounds as mtor kinase inhibitors
JP2012521354A (ja) 2009-03-20 2012-09-13 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
EP2430013B1 (en) 2009-05-13 2014-10-15 Amgen Inc. Heteroaryl compounds as pikk inhibitors
US8754089B2 (en) 2009-06-25 2014-06-17 Amgen Inc. Heterocyclic compounds and their uses
MX2011013510A (es) 2009-06-25 2012-03-07 Amgen Inc Compuestos heterociclicos y sus usos.
CN102625799A (zh) 2009-06-25 2012-08-01 安姆根有限公司 杂环化合物及其用途
MX2011013667A (es) 2009-06-25 2012-03-06 Amgen Inc Compuestos heterociclicos y sus usos.
EP2266984A1 (en) * 2009-06-26 2010-12-29 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Pyrido[2,3-d]pyrimidines as Wnt antagonists for treatment of cancer and arthritis
LT3023438T (lt) 2009-09-03 2020-05-11 Merck Sharp & Dohme Corp. Anti-gitr antikūnai
SG179102A1 (en) 2009-09-11 2012-04-27 Amgen Inc N-4 ( - ( ( 3- ( 2 -amino-4 pyrimidinyl) -2 -pyridinyl) oxy) phenyl) -4- (4-methyl-2-thienyl) -1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
WO2011075747A1 (en) * 2009-12-18 2011-06-23 Glaxosmithkline Llc Therapeutic compounds
AU2010343056A1 (en) 2009-12-29 2012-08-02 Emergent Product Development Seattle, Llc Ron binding constructs and methods of use thereof
US9133164B2 (en) 2011-04-13 2015-09-15 Innov88 Llc MIF inhibitors and their uses
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
US20150087628A1 (en) 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
ES2618004T3 (es) 2012-08-07 2017-06-20 Merck Patent Gmbh Derivados de piridopirimidina como inhibidores de proteínas quinasas
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
WO2014152588A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
GB201312059D0 (en) 2013-07-05 2013-08-21 Univ Leuven Kath Novel GAK modulators
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
CA2926328C (en) * 2013-10-10 2022-11-29 Araxes Pharma Llc Substituted quinazolinyl and quinolinyl derivatives and pharmaceutical compositions thereof useful as inhibitors of kras g12c
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
MX374379B (es) 2014-01-20 2025-03-06 Cleave Biosciences Inc PIRIMIDINAS FUSIONADAS QUE TIENEN UN ANILLO HETEROCÍCLICO 5:6 COMO INHIBIDORES DEL COMPLEJO p97 Y EL USO DE LAS MISMAS EN EL TRATAMIENTO DE AFECCIONES NEOPLÁSICAS.
WO2016035008A1 (en) 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
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
CA2981677A1 (en) 2015-04-03 2016-10-06 Nantbioscience, Inc. Compositions and methods of targeting mutant k-ras
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
JP6869947B2 (ja) 2015-07-22 2021-05-12 アラクセス ファーマ エルエルシー 置換キナゾリン化合物ならびにそのｇ１２ｃ変異ｋｒａｓ、ｈｒａｓおよび／またはｎｒａｓタンパク質の阻害剤としての使用
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356339A1 (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
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017087528A1 (en) 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
SG11201810171SA (en) 2016-05-18 2018-12-28 Mirati Therapeutics 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
WO2018068017A1 (en) 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
SG11201906223TA (en) * 2016-12-22 2019-08-27 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
JP2020505395A (ja) 2017-01-26 2020-02-20 アラクセス ファーマ エルエルシー 縮合ｎ−複素環式化合物およびその使用方法
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
ES2985118T3 (es) 2017-09-08 2024-11-04 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
US11045484B2 (en) 2018-05-04 2021-06-29 Amgen Inc. KRAS G12C inhibitors and methods of using the same
ES2986917T3 (es) 2018-05-10 2024-11-13 Amgen Inc Inhibidores de KRAS G12C para el tratamiento del cáncer
JP7360396B2 (ja) 2018-06-01 2023-10-12 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤及び同一物の使用方法
EP4268898A3 (en) 2018-06-11 2024-01-17 Amgen Inc. Kras g12c inhibitors for treating cancer
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
CA3103048A1 (en) 2018-06-21 2019-12-26 Janssen Pharmaceutica Nv Oga inhibitor compounds
WO2019243535A1 (en) 2018-06-21 2019-12-26 Janssen Pharmaceutica Nv Oga inhibitor compounds
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
MX2021005700A (es) 2018-11-19 2021-07-07 Amgen Inc Inhibidores de kras g12c y metodos de uso de los mismos.
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
JP2022532790A (ja) 2019-05-21 2022-07-19 アムジエン・インコーポレーテツド 固体形態
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
US20240190862A1 (en) 2019-10-24 2024-06-13 Amgen Inc. Epoxyamides as kras g12c and kras g12d inhibitors and methods of using the same
TW202132271A (zh) 2019-11-14 2021-09-01 美商安進公司 Ｋｒａｓ ｇ１２ｃ抑制劑化合物之改善的合成
IL292315A (en) 2019-11-14 2022-06-01 Amgen Inc Improved synthesis of kras g12c inhibitor compound
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor

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