WO2019099524A1 - Kras g12c inhibitors - Google Patents

Kras g12c inhibitors Download PDF

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Publication number
WO2019099524A1
WO2019099524A1 PCT/US2018/061060 US2018061060W WO2019099524A1 WO 2019099524 A1 WO2019099524 A1 WO 2019099524A1 US 2018061060 W US2018061060 W US 2018061060W WO 2019099524 A1 WO2019099524 A1 WO 2019099524A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
alkyl
mmol
optionally substituted
formula
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2018/061060
Other languages
English (en)
French (fr)
Inventor
James F. Blake
Laurence E. Burgess
Mark Joseph Chicarelli
James Gail CHRISTENSEN
Adam Cook
Jay Bradford Fell
John P. Fischer
Matthew Arnold Marx
Macedonio J. MEJIA
Pavel SAVECHENKOV
Guy P.A. VIGERS
Christopher Ronald Smith
Martha E. Rodriguez
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Array Biopharma Inc
Mirati Therapeutics Inc
Original Assignee
Array Biopharma Inc
Mirati Therapeutics 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
Priority to CA3082579A priority Critical patent/CA3082579A1/en
Priority to EA202091186A priority patent/EA202091186A1/ru
Priority to ES18879484T priority patent/ES2944547T3/es
Priority to RS20230345A priority patent/RS64182B1/sr
Priority to AU2018369759A priority patent/AU2018369759B2/en
Priority to JP2020526612A priority patent/JP7322019B2/ja
Priority to UAA202003509A priority patent/UA125802C2/uk
Priority to MX2020005063A priority patent/MX2020005063A/es
Priority to CN201880086849.1A priority patent/CN111989321B/zh
Priority to SI201830912T priority patent/SI3710439T1/sl
Priority to MYPI2020001151A priority patent/MY200356A/en
Priority to DK18879484.6T priority patent/DK3710439T3/da
Priority to LTEPPCT/US2018/061060T priority patent/LT3710439T/lt
Priority to FIEP18879484.6T priority patent/FI3710439T3/fi
Priority to BR112020009818-3A priority patent/BR112020009818A2/pt
Priority to IL274601A priority patent/IL274601B2/en
Priority to SG11202004427TA priority patent/SG11202004427TA/en
Priority to CN202410549759.9A priority patent/CN118459460A/zh
Application filed by Array Biopharma Inc, Mirati Therapeutics Inc filed Critical Array Biopharma Inc
Priority to KR1020207016494A priority patent/KR102861303B1/ko
Priority to EP18879484.6A priority patent/EP3710439B1/en
Priority to HRP20230377TT priority patent/HRP20230377T1/hr
Priority to PL18879484.6T priority patent/PL3710439T3/pl
Publication of WO2019099524A1 publication Critical patent/WO2019099524A1/en
Priority to ZA2020/02105A priority patent/ZA202002105B/en
Priority to PH12020550622A priority patent/PH12020550622A1/en
Anticipated expiration legal-status Critical
Priority to CONC2020/0007244A priority patent/CO2020007244A2/es
Priority to NL301279C priority patent/NL301279I2/nl
Priority to FIC20240021C priority patent/FIC20240021I1/fi
Priority to LTPA2024517C priority patent/LTC3710439I2/lt
Priority to FR24C1026C priority patent/FR24C1026I2/fr
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Definitions

  • Y is a bond, O, S or NR 5 ;
  • heteroarylalkyl wherein each of the Z, heterocyclyl, heterocyclylalkyl, aryl, heteroaryl, and heteroarylalkyl may be optionally substituted with one or more R 9 ;
  • m is zero or an integer between 1 and 2;
  • each R 10 is independently hydrogen, acyl, Cl - C3 alkyl, heteroalkyl or hydroxyalkyl;
  • R 11 is haloalkyl
  • methods for inhibiting KRas G12C activity in a in a cell comprising contacting the cell with a compound of Formula I, Formula I-A, Formula 1- B, Formula II, Formula II-A or Formula II-B.
  • the contacting is in vitro. In one embodiment, the contacting is in vivo.
  • the present invention relates to inhibitors of KRas G12C.
  • the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C,
  • regulatory agency is a country’s agency for the approval of the medical use of pharmaceutical agents with the country.
  • a regulatory agency is the U.S. Food and Drug Administration (FDA).
  • a "therapeutically effective amount" of a compound is an amount that is sufficient to ameliorate, or in some manner reduce a symptom or stop or reverse progression of a condition, or negatively modulate or inhibit the activity of KRas G12C. Such amount may be administered as a single dosage or may be administered according to a regimen, whereby it is effective.
  • the aryl is phenyl substituted with one or more R 7 groups independently selected from halogen, hydroxyl, Cl - C3 alkyl, haloalkyl, Q-haloalkyl, and alkoxy. In one embodiment, the aryl is phenyl substituted with one or more R 7 groups independently selected from halogen, haloalkyl, methyl, isopropyl, methoxy, Q-haloalkyl and hydroxyl. In one embodiment, the aryl is phenyl substituted with one or more R 7 groups independently selected from methyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxyl,
  • Formula I includes compounds having the Formula I-A:
  • R 1 is -C(0)C(R A ) . C(R B ) P , wherein— . is a double bond and p is two, one R B is hydrogen and R A and one R B and the carbon atoms to which they are attached form a 5-8 membered partially saturated cycloalkyl substituted with oxo.
  • hydroxypyrrolindinyl fluoropyrrolidinyl, difluoropyrrolidinyl, (N-methyl)fluoropyrrolidinyl, (N-methyl)difluoropyrrolidinyl, methoxyethylpyrrolidinyl, alkoxy-substituted N- methylpyrrolidinyl (e.g., (N-methyl)methoxypyrrolidinyl), piperazinyl,
  • liver nephroblastoma
  • lymphoma lymphoma
  • leukemia bladder and urethra
  • squamous cell carcinoma transitional cell carcinoma, adenocarcinoma
  • prostate adenocarcinoma, sarcoma
  • testis seminoma, teratoma, embryonal carcinoma, teratocarcinoma, choriocarcinoma, sarcoma, interstitial cell carcinoma, fibroma, fibroadenoma, adenomatoid tumors, lipoma
  • Liver Liver:
  • compositions comprising such compounds and salts also may be co-reacted
  • R 1 is introduced to provide a compound of Formula I, for example by treating with an acid chloride having the formula C1-C(0)C(R A ) C(R B ) P or Cl-S0 2 C(R A ) — .
  • C(R B ) P or an anhydride having the formula C(R B ) p ⁇ C(R A )C(0)0C(0)C(R A ) C(R B ) P , where R A , R B and p are as defined for Formula I.
  • Step A ethyl 2-methyl-3-oxo-4-phenyl-butanoate.
  • ethyl 3-oxo-4-phenyl-butanoate 4.00 g, 19.4 mmol.
  • THF 50.0 mL
  • sodium hydride 931 mg, 23.3 mmol
  • a solution of methyl iodide (3.03 g, 21.3) was next added drop-wise. After addition was completed, the reaction mixture was warmed to 20 °C and stirred for two hours at 20°C.
  • Step B 2-methylnaphthalene-l ,3-diol.
  • a solution of ethyl 2-methyl-3-oxo-4-phenyl- butanoate (3.60 g, 16.3 mmol) in concentrated sulfuric acid (19.9 g, 203 mmol) was stirred at 15 °C for 12 hours.
  • the reaction mixture was poured into ice-water (30.0 mL) and the resulting solid collected by filtration and dried under vacuum to afford 2-methylnaphthalene-l,3-diol (1.80 g, 10.3 mmol, 63.2% yield) as a red solid.
  • Step B /eH-butyl (2y)-2-(cvanomethyl)-4-[7-(2,3-dimethylphenyl)-2-methylsulfinyl-6,8- dihvdro-5//-pyrido[3,4- ⁇ /lpyrimidin-4-ynpiperazine-l-carboxylate.
  • Step C fe/7-butyl (2S , )-2-(cvanomethyl)-4-[7-(2,3-dimethylphenyl)-2-[[(2S r )-l- methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-57/-pyrido[3,4- ⁇ i]pyrimidin-4-yllpiperazine-l- carboxylate.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
PCT/US2018/061060 2017-11-15 2018-11-14 Kras g12c inhibitors Ceased WO2019099524A1 (en)

Priority Applications (29)

Application Number Priority Date Filing Date Title
SG11202004427TA SG11202004427TA (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
ES18879484T ES2944547T3 (es) 2017-11-15 2018-11-14 Inhibidores de KRas G12C
RS20230345A RS64182B1 (sr) 2017-11-15 2018-11-14 Inhibitori kras g12c
AU2018369759A AU2018369759B2 (en) 2017-11-15 2018-11-14 KRas G12C inhibitors
JP2020526612A JP7322019B2 (ja) 2017-11-15 2018-11-14 Ｋｒａｓ ｇ１２ｃ阻害剤
UAA202003509A UA125802C2 (uk) 2017-11-15 2018-11-14 Інгібітори kras g12c
MX2020005063A MX2020005063A (es) 2017-11-15 2018-11-14 Inhibidores de kras g12c.
CN201880086849.1A CN111989321B (zh) 2017-11-15 2018-11-14 Kras g12c抑制剂
SI201830912T SI3710439T1 (sl) 2017-11-15 2018-11-14 Zaviralci mutacije kras g12c
MYPI2020001151A MY200356A (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
DK18879484.6T DK3710439T3 (da) 2017-11-15 2018-11-14 Kras g12c-hæmmere
LTEPPCT/US2018/061060T LT3710439T (lt) 2017-11-15 2018-11-14 Kras g12c inhibitoriai
FIEP18879484.6T FI3710439T3 (fi) 2017-11-15 2018-11-14 Kras g12c:n estäjiä
BR112020009818-3A BR112020009818A2 (pt) 2017-11-15 2018-11-14 inibidores kras g12c
IL274601A IL274601B2 (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
CA3082579A CA3082579A1 (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
EA202091186A EA202091186A1 (ru) 2017-11-15 2018-11-14 ИНГИБИТОРЫ KRas G12C
CN202410549759.9A CN118459460A (zh) 2017-11-15 2018-11-14 Kras g12c抑制剂
KR1020207016494A KR102861303B1 (ko) 2017-11-15 2018-11-14 Ｋｒａｓ ｇ12ｃ 억제제
EP18879484.6A EP3710439B1 (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
HRP20230377TT HRP20230377T1 (hr) 2017-11-15 2018-11-14 Inhibitori mutacije kras g12c
PL18879484.6T PL3710439T3 (pl) 2017-11-15 2018-11-14 Inhibitory kras g12c
ZA2020/02105A ZA202002105B (en) 2017-11-15 2020-05-04 Kras g12c inhibitors
PH12020550622A PH12020550622A1 (en) 2017-11-15 2020-05-13 Kras g12c inhibitors
CONC2020/0007244A CO2020007244A2 (es) 2017-11-15 2020-06-12 Inhibidores de kras g12c
NL301279C NL301279I2 (nl) 2017-11-15 2024-06-10 Adagrasib, desgewenst in de vorm van een farmaceutisch aanvaardbaar zout
FIC20240021C FIC20240021I1 (fi) 2017-11-15 2024-06-10 Adagrasibi tai sen farmaseuttisesti hyväksyttävä suola
LTPA2024517C LTC3710439I2 (https=) 2017-11-15 2024-06-11
FR24C1026C FR24C1026I2 (fr) 2017-11-15 2024-06-13 Inhibiteurs de kras g12c

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762586775P 2017-11-15 2017-11-15
US62/586,775 2017-11-15

Publications (1)

Publication Number Publication Date
WO2019099524A1 true WO2019099524A1 (en) 2019-05-23

Family

ID=66431793

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2018/061060 Ceased WO2019099524A1 (en) 2017-11-15 2018-11-14 Kras g12c inhibitors
PCT/US2019/032249 Ceased WO2020101736A1 (en) 2017-11-15 2019-05-14 Kras g12c inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2019/032249 Ceased WO2020101736A1 (en) 2017-11-15 2019-05-14 Kras g12c inhibitors

Country Status (34)

Country Link
US (4) US10689377B2 (https=)
EP (3) EP3710439B1 (https=)
JP (2) JP7322019B2 (https=)
KR (1) KR102861303B1 (https=)
CN (2) CN111989321B (https=)
AU (1) AU2018369759B2 (https=)
BR (1) BR112020009818A2 (https=)
CA (1) CA3082579A1 (https=)
CL (1) CL2020001271A1 (https=)
CO (1) CO2020007244A2 (https=)
CY (2) CY1125974T1 (https=)
DK (1) DK3710439T3 (https=)
EA (1) EA202091186A1 (https=)
ES (2) ES2944547T3 (https=)
FI (2) FI3710439T3 (https=)
FR (1) FR24C1026I2 (https=)
HR (1) HRP20230377T1 (https=)
HU (2) HUE061599T2 (https=)
IL (1) IL274601B2 (https=)
LT (2) LT3710439T (https=)
MX (1) MX2020005063A (https=)
MY (1) MY200356A (https=)
NL (1) NL301279I2 (https=)
PH (1) PH12020550622A1 (https=)
PL (1) PL3710439T3 (https=)
PT (1) PT3710439T (https=)
RS (1) RS64182B1 (https=)
SA (1) SA520411982B1 (https=)
SG (1) SG11202004427TA (https=)
SI (1) SI3710439T1 (https=)
TW (1) TWI809005B (https=)
UA (1) UA125802C2 (https=)
WO (2) WO2019099524A1 (https=)
ZA (1) ZA202002105B (https=)

Cited By (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055755A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055756A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055758A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020118066A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
WO2020165732A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
CN112300153A (zh) * 2019-07-26 2021-02-02 博瑞生物医药（苏州）股份有限公司 一种杂环化合物、药物组合物和用途
CN112300195A (zh) * 2019-08-02 2021-02-02 上海济煜医药科技有限公司 四并环类化合物及其制备方法和应用
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
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
WO2021068898A1 (zh) * 2019-10-10 2021-04-15 信达生物制药(苏州)有限公司 新颖的kras g12c蛋白抑制剂及其制备方法和用途
CN112694475A (zh) * 2019-10-23 2021-04-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
WO2021091967A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CN112824410A (zh) * 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021124222A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
WO2021129824A1 (zh) * 2019-12-27 2021-07-01 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021152149A1 (en) 2020-01-31 2021-08-05 Jazz Pharmaceuticals Ireland Limited Ras inhibitors and methods of using the same
WO2021169990A1 (zh) * 2020-02-24 2021-09-02 泰励生物科技（上海）有限公司 用于癌症治疗的kras抑制剂
CN113423703A (zh) * 2019-05-29 2021-09-21 上海翰森生物医药科技有限公司 含氮杂环类衍生物调节剂、其制备方法和应用
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
WO2021219072A1 (zh) * 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
CN113651814A (zh) * 2019-12-19 2021-11-16 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
WO2021245051A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2021257736A1 (en) 2020-06-18 2021-12-23 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2021259972A1 (en) 2020-06-24 2021-12-30 Boehringer Ingelheim International Gmbh Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
CN113912608A (zh) * 2020-07-10 2022-01-11 江苏恒瑞医药股份有限公司 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用
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
WO2022056307A1 (en) * 2020-09-11 2022-03-17 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
WO2022060836A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
US11312724B2 (en) 2020-01-08 2022-04-26 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
WO2022087270A1 (en) 2020-10-23 2022-04-28 Mirati Therapeutics, Inc. Methods for treatment of lung cancers
WO2022089604A1 (en) * 2020-10-30 2022-05-05 Novartis Ag New crystalline forms of a kras g12c inhibitor compound
WO2022129925A1 (en) 2020-12-18 2022-06-23 Amphista Therapeutics Limited Novel bifunctional molecules for targeted protein degradation
WO2022135346A1 (en) * 2020-12-22 2022-06-30 Novartis Ag Pharmaceutical combinations comprising a kras g12c inhibitor and uses of a kras g12c inhibitor for the treatment of cancers
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022161443A1 (zh) * 2021-02-01 2022-08-04 南京明德新药研发有限公司 嘧啶并吡喃类化合物
US11407765B2 (en) 2018-05-08 2022-08-09 Astrazeneca, Ab Tetracyclic heteroaryl compounds
EP3880208A4 (en) * 2017-11-15 2022-08-17 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2022187527A1 (en) * 2021-03-05 2022-09-09 Nikang Therapeutics, Inc Quinazoline nitrile derivatives as kras inhibitors
WO2022214594A1 (en) 2021-04-09 2022-10-13 Boehringer Ingelheim International Gmbh Anticancer therapy
WO2022216648A1 (en) 2021-04-08 2022-10-13 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
WO2022235864A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
US20220395507A1 (en) * 2021-05-27 2022-12-15 Mirati Therapeutics, Inc. Combination therapies
WO2022261154A1 (en) 2021-06-09 2022-12-15 Eli Lilly And Company Substituted fused azines as kras g12d inhibitors
WO2022262797A1 (en) * 2021-06-18 2022-12-22 Shanghai Antengene Corporation Limited Combination of an erk inhibitor and a kras inhibitor and uses thereof
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022269525A1 (en) 2021-06-23 2022-12-29 Novartis Ag Pharmaceutical combinations comprising a kras g12c inhibitor and uses thereof for the treatment of cancers
WO2023280280A1 (zh) * 2021-07-07 2023-01-12 微境生物医药科技(上海)有限公司 作为KRas G12D抑制剂的稠环化合物
WO2023284730A1 (en) 2021-07-14 2023-01-19 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
WO2023283933A1 (en) * 2021-07-16 2023-01-19 Silexon Biotech Co., Ltd. Compounds useful as kras g12d inhibitors
JP2023504178A (ja) * 2019-12-02 2023-02-01 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
WO2023008462A1 (ja) 2021-07-27 2023-02-02 東レ株式会社 癌の治療及び／又は予防のための医薬品
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
WO2023039020A1 (en) 2021-09-09 2023-03-16 Mirati Therapeutics, Inc. Processes and intermediates for synthesis of adagrasib
CN115836072A (zh) * 2020-06-04 2023-03-21 上海德琪医药科技有限公司 Kras g12c蛋白的抑制剂和其用途
WO2023060253A1 (en) 2021-10-08 2023-04-13 Revolution Medicines, Inc. Ras inhibitors
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
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023117681A1 (en) 2021-12-22 2023-06-29 Boehringer Ingelheim International Gmbh Heteroaromatic compounds for the treatment of cancer
WO2023126822A1 (en) 2021-12-28 2023-07-06 Astrazeneca Uk Limited Combination of antibody-drug conjugate and rasg12c inhibitor
US11697657B2 (en) 2019-10-28 2023-07-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
CN116601151A (zh) * 2020-09-11 2023-08-15 米拉蒂治疗股份有限公司 Kras g12c抑制剂的晶型
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023183585A1 (en) 2022-03-25 2023-09-28 Eli Lilly And Company Kras inhibitors
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
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2023240189A1 (en) * 2022-06-10 2023-12-14 Bristol-Myers Squibb Company Tetrahydropyrido 3,4-d pyrimidine derivatives as kras inhibitors
US11845761B2 (en) 2020-12-18 2023-12-19 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2024047135A1 (en) 2022-08-31 2024-03-07 Jazz Pharmaceuticals Ireland Limited Substituted heterocycles as ras inhibitors
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
US12060367B2 (en) 2021-12-01 2024-08-13 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
US12059425B2 (en) 2022-08-05 2024-08-13 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US12065430B2 (en) 2018-10-26 2024-08-20 Taiho Pharmaceutical Co., Ltd. Indazole compound or salt thereof
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024206766A1 (en) 2023-03-31 2024-10-03 Eli Lilly And Company Kras inhibitors
WO2024206747A1 (en) 2023-03-30 2024-10-03 Eli Lilly And Company Kras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
EP4247807A4 (en) * 2020-11-23 2024-10-16 Merck Sharp & Dohme LLC 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
RU2829553C2 (ru) * 2019-05-29 2024-10-31 Шанхай Ханьсох Байомедикал Ко., Лтд. Регулятор на основе азотсодержащего гетероциклического производного, способ его получения и его применение
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024246114A1 (en) 2023-05-31 2024-12-05 Boehringer Ingelheim International Gmbh Survivin as a biomarker for predicting the responsiveness of cancer treatment
WO2024248123A1 (ja) 2023-06-02 2024-12-05 第一三共株式会社 抗ｈｅｒ３抗体－薬物コンジュゲートとｒａｓｇ１２ｃ阻害剤の組み合わせ
US12162893B2 (en) 2020-09-23 2024-12-10 Erasca, Inc. Tricyclic pyridones and pyrimidones
EP4284370A4 (en) * 2021-01-29 2024-12-11 Mirati Therapeutics, Inc. POLYTHERAPIES
US12209102B2 (en) 2022-03-11 2025-01-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025072457A1 (en) 2023-09-27 2025-04-03 Eli Lilly And Company Kras inhibitors
WO2025019688A3 (en) * 2023-07-20 2025-04-10 Mirati Therapeutics, Inc. Crystalline forms of salts of adagrasib
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
US12286427B2 (en) 2020-08-28 2025-04-29 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US12291539B2 (en) 2021-11-05 2025-05-06 Frontier Medicines Corporation KRAS G12C inhibitors
WO2025132549A1 (en) 2023-12-20 2025-06-26 Boehringer Ingelheim International Gmbh Cancer combination therapy using zongertinib and a kras g12c inhibitor
WO2025145207A1 (en) 2023-12-29 2025-07-03 Bristol-Myers Squibb Company Combination therapy of kras inhibitor and treg-depleting agent
US12383503B2 (en) 2022-08-19 2025-08-12 Mirati Therapeutics, Inc. Adagrasib solid pharmaceutical compositions
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
US12410212B2 (en) 2022-05-06 2025-09-09 Chugai Seiyaku Kabushiki Kaisha Cyclic compound having selective KRAS inhibitory effect on HRAS and NRAS
US12410187B2 (en) 2019-03-05 2025-09-09 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
US12421253B2 (en) 2020-12-16 2025-09-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
US12466840B2 (en) 2023-10-20 2025-11-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS proteins
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
WO2025242126A1 (zh) * 2024-05-22 2025-11-27 上海正大天晴医药科技开发有限公司 一种药物组合及其应用
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026003808A1 (en) 2024-06-28 2026-01-02 Assia Chemical Industries Ltd. Solid state form of adagrasib and process for preparation
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026059955A1 (en) 2024-09-11 2026-03-19 Eli Lilly And Company (3-((6-(2-amino-benzo[d]thiazol-4-yl)-3-(pyrrolidin-1-yl)-7,9-dihydrofuro[3,4-f]quinazolin-1-yl)amino)- piperidin-2-one derivatives as kras inhibitors for the treatment of cancer
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
EP4511372A4 (en) * 2022-04-18 2026-04-01 Mirati Therapeutics Inc PROCESSES AND INTERMEDIARIES FOR ADAGRASIB SYNTHESIS
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026075942A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
WO2026075945A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
US12606572B2 (en) 2023-06-06 2026-04-21 Kumquat Biosciences Inc. Substituted heterocycles and uses thereof

Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7039489B2 (ja) * 2016-05-18 2022-03-22 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
WO2019213516A1 (en) * 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
US20210230170A1 (en) * 2018-08-31 2021-07-29 Mirati Therapeutics, Inc. Kras g12c inhibitors
PT3735299T (pt) 2018-11-09 2024-11-25 Hoffmann La Roche Compostos de anéis fundidos
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2020238791A1 (zh) * 2019-05-24 2020-12-03 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
CN112047939B (zh) * 2019-06-06 2023-05-02 江苏先声药业有限公司 一种具有抗肿瘤活性的四氢吡啶并嘧啶类化合物
TWI752580B (zh) * 2019-08-07 2022-01-11 大陸商北京加科思新藥研發有限公司 Kras突變蛋白抑制劑
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
WO2021043322A1 (zh) * 2019-09-06 2021-03-11 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
US20210094919A1 (en) * 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
US12478624B2 (en) 2019-10-02 2025-11-25 Tolremo Therapeutics Ag Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer
PT4053118T (pt) * 2019-10-30 2024-12-05 Genfleet Therapeutics Shanghai Inc Composto cíclico fundido heterocíclico substituído, método de preparação deste e utilização farmacêutica deste
WO2021088458A1 (en) * 2019-11-04 2021-05-14 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
CN112778301A (zh) * 2019-11-07 2021-05-11 苏州泽璟生物制药股份有限公司 四氢吡啶并嘧啶类抑制剂及其制备方法和应用
CN114901286B (zh) 2019-11-27 2024-05-10 特普医药公司 涉及二芳基巨环化合物的组合疗法
ES2929700T3 (es) 2019-12-11 2022-12-01 Lilly Co Eli Inhibidores de KRas g12c
CN113004269B (zh) * 2019-12-19 2024-11-05 首药控股(北京)股份有限公司 Kras-G12C抑制剂杂环化合物
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
CN112094269B (zh) * 2020-01-01 2021-12-07 上海凌达生物医药有限公司 一类饱和六元环并杂环类化合物、制备方法和用途
EP4077328A4 (en) * 2020-02-20 2023-11-29 Beta Pharma, Inc. PYRIDOPYRIMIDE DERIVATIVES AS KRAS INHIBITORS
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
KR102822517B1 (ko) * 2020-03-12 2025-06-19 디3 바이오 (우씨) 컴퍼니, 리미티드 피리미도헤테로사이클릭 화합물 및 이의 응용
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
CN113666923A (zh) * 2020-05-15 2021-11-19 苏州泽璟生物制药股份有限公司 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用
IL299344A (en) 2020-06-25 2023-02-01 Tolremo Therapeutics Ag Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer
CN113980014B (zh) * 2020-07-27 2023-05-12 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
CN115956080B (zh) * 2020-08-17 2025-07-11 贝达药业股份有限公司 双环化合物，包含其的组合物及其应用
US20220112204A1 (en) * 2020-10-14 2022-04-14 Accutar Biotechnology Inc. Substituted dihydropyranopyrimidine compounds as kras 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
CN114591319B (zh) * 2020-12-04 2024-06-28 江苏先声药业有限公司 四氢吡啶并嘧啶类衍生物及其用途
CN116829151A (zh) * 2020-12-15 2023-09-29 米拉蒂治疗股份有限公司 氮杂喹唑啉泛KRas抑制剂
CN116529249A (zh) * 2020-12-18 2023-08-01 正大天晴药业集团股份有限公司 吡啶并嘧啶酮类化合物
CN114716436A (zh) * 2021-01-04 2022-07-08 广州百霆医药科技有限公司 Kras g12c突变抑制剂及其用途
WO2022148421A1 (en) * 2021-01-08 2022-07-14 Beigene, Ltd. Bridged compounds as kras g12d inhibitor and degrader and the use thereof
WO2022171143A1 (zh) * 2021-02-09 2022-08-18 南京明德新药研发有限公司 5,6,7,8-四氢吡啶[3,4-d]嘧啶化合物
EP4308559A1 (en) 2021-03-15 2024-01-24 Novartis AG Benzisoxazole derivatives and uses thereof
WO2022194192A1 (zh) * 2021-03-18 2022-09-22 四川科伦博泰生物医药股份有限公司 一类杂芳环化合物、其制备方法及用途
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
CN115124524A (zh) * 2021-03-26 2022-09-30 浙江海正药业股份有限公司 三环类衍生物及其制备方法和用途
WO2022206724A1 (zh) * 2021-03-30 2022-10-06 浙江海正药业股份有限公司 杂环类衍生物及其制备方法和用途
BR112023020538A2 (pt) 2021-04-07 2024-01-23 Tolremo Therapeutics Ag Derivados heterocíclicos, composições farmacêuticas e seus usos no tratamento ou na melhoria de câncer
WO2022217042A1 (en) * 2021-04-09 2022-10-13 Ikena Oncology, Inc. Naphthyl-substituted quinoline-4(1h)-ones and related compounds and their use in treating medical conditions
CN117203208A (zh) * 2021-04-23 2023-12-08 清华大学 靶向活化与失活态kras g12d的抑制剂
CN117337193A (zh) * 2021-05-19 2024-01-02 基因泰克公司 组合疗法
WO2022247760A1 (zh) * 2021-05-22 2022-12-01 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物，及其制备和治疗用途
WO2022250170A1 (en) * 2021-05-28 2022-12-01 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
US20240417408A1 (en) * 2021-05-28 2024-12-19 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN113429405A (zh) * 2021-06-10 2021-09-24 都创(上海)医药开发有限公司 Mrtx849化合物的晶型及其制备方法和用途
CN115521312A (zh) * 2021-06-24 2022-12-27 上海希迈医药科技有限公司 Adagrasib的固体形式及其制备方法
MX2024000357A (es) 2021-07-07 2024-02-12 Incyte Corp Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras).
US12600717B2 (en) 2021-07-14 2026-04-14 Incyte Corporation Tricyclic compounds as inhibitors of KRAS
CN113527294A (zh) * 2021-08-25 2021-10-22 都创(上海)医药开发有限公司 Mrtx849化合物的晶型及其制备方法和用途
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
CN118043330A (zh) * 2021-09-29 2024-05-14 海南先声再明医药股份有限公司 Kras g12d抑制剂化合物及其制备方法和应用
EP4436957A1 (en) 2021-11-24 2024-10-02 Genentech, Inc. Therapeutic indazole compounds and methods of use in the treatment of cancer
TW202340212A (zh) 2021-11-24 2023-10-16 美商建南德克公司 治療性化合物及其使用方法
JP7779584B2 (ja) * 2021-12-02 2025-12-03 上海和誉生物医薬科技有限公司 Ｋｒａｓ阻害剤とその製造及び薬学における応用
CN114409653A (zh) * 2021-12-31 2022-04-29 苏州闻天医药科技有限公司 一种桥环并嘧啶并环类化合物及其用途
CN118556063A (zh) * 2022-01-21 2024-08-27 上海湃隆生物科技有限公司 杂环类化合物、药物组合物及其应用
EP4476202A1 (en) * 2022-02-11 2024-12-18 Wave Life Sciences Ltd. Stereoselective technologies for chiral compounds
CN116854642A (zh) * 2022-03-26 2023-10-10 重庆博腾制药科技股份有限公司 一种（s）-2-哌嗪乙腈及其盐酸盐的制备方法
US20250177406A1 (en) 2022-03-31 2025-06-05 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating tumors
CN114907387B (zh) * 2022-05-26 2023-11-10 中山大学 嘧啶并吡咯类kras抑制剂及其制备方法与应用
CN117164580A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 一种kras g12c抑制剂的制备方法及其中间体
CN117164526A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 2-(哌嗪-2-基)乙腈类衍生物及其制备方法和应用
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
CN116789609A (zh) * 2023-03-03 2023-09-22 南京优氟医药科技有限公司 一种(r)-2-(哌嗪-2-基)乙腈盐酸盐的制备方法
CN116768804A (zh) * 2023-03-15 2023-09-19 南京优氟医药科技有限公司 一种(s)-2-(哌嗪-2-基)乙腈盐酸盐的制备方法
JPWO2024209717A1 (https=) 2023-04-06 2024-10-10
CN121399123A (zh) * 2023-05-04 2026-01-23 前沿药品公司 作为突变型kras g12c抑制剂用于治疗癌症的吡啶并[4,3-d]嘧啶衍生物
CN120981456A (zh) 2023-05-24 2025-11-18 金橘生物科技公司 杂环化合物及其用途
CN116675690B (zh) * 2023-06-02 2026-03-27 北京康立生医药技术开发有限公司 一种肺癌治疗药物的制备方法
CN116478141B (zh) * 2023-06-20 2023-10-24 药康众拓(江苏)医药科技有限公司 氘代kras抑制剂药物及用途
AU2024307234A1 (en) 2023-06-30 2026-01-29 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
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
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030191143A1 (en) 2001-05-01 2003-10-09 Pitts William J. Fused heterocyclic compounds and use thereof
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
US20160166571A1 (en) 2014-09-18 2016-06-16 Araxes Pharma Llc Combination therapies for treatment of cancer
WO2017201161A1 (en) 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2432578C (en) 2001-01-02 2008-04-01 F. Hoffmann-La Roche Ag Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
US20080051387A1 (en) 2006-06-09 2008-02-28 Yuelian Xu Tetrahydropyrido[3,4-d]pyrimidines and related analogues
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
CA2673299C (en) 2006-12-21 2016-04-12 Sloan-Kettering Institute For Cancer Research Pyridazinone compounds for the treatment of proliferative diseases
WO2008103470A2 (en) 2007-02-21 2008-08-28 Trustees Of Columbia University In The City Of New York Oncogenic-ras-signal dependent lethal compounds
CN101679308B (zh) 2007-03-14 2014-05-07 埃克塞里艾克西斯公司 Hedgehog途径抑制剂
EP2209775A1 (en) 2007-10-09 2010-07-28 UCB Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
EP2278976A1 (en) 2008-04-07 2011-02-02 Gilead Sciences, Inc. 2h-benzo[b][1,4]oxazin-3(4h)-one derivatives for use as stearoyl coa desaturase inhibitors
AR073354A1 (es) 2008-07-31 2010-11-03 Genentech Inc Compuestos de pirimidina, composiciones farmaceuticas y su uso en el tratamiento del cancer.
WO2010120996A1 (en) 2009-04-17 2010-10-21 Wyeth Llc 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2518064A1 (en) 2009-12-25 2012-10-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
WO2014011973A2 (en) 2012-07-13 2014-01-16 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-ras-selective lethal compounds and their use
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの共有結合性阻害剤
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
MA40074A (fr) 2014-05-30 2015-12-03 Univ Columbia Composés liant ras multivalents
WO2016025650A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods
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
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
JP2018513853A (ja) 2015-04-10 2018-05-31 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およびその使用方法
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
WO2016172692A1 (en) 2015-04-24 2016-10-27 H. Lee Moffitt Cancer Center And Research Institute, Inc. Mutant kras inhibitors
BR112017023821A2 (pt) 2015-05-06 2018-07-31 Leidos Biomedical Res Inc moduladores de k-ras
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
JP6877414B2 (ja) 2015-09-24 2021-05-26 アイオニス・ファーマシューティカルズ・インコーポレイテッドＩｏｎｉｓ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． Ｋｒａｓ発現のモジュレーター
US10647703B2 (en) 2015-09-28 2020-05-12 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
WO2017058807A1 (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
WO2017058902A1 (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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤をスクリーニングするための方法
JP6953400B2 (ja) 2015-10-22 2021-10-27 ザ スクリプス リサーチ インスティテュート システイン反応性プローブとその使用
WO2017080980A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
WO2017079864A1 (en) 2015-11-12 2017-05-18 Hangzhou Yier Biotech Co., Ltd. Treatment of cancers related to chronically active ras
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
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
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
MX2019006296A (es) 2016-11-30 2019-11-12 Bantam Pharmaceutical Llc Métodos de uso de compuestos de pirazol y pirazol sustituido y para el tratamiento de enfermedades hiperproliferativas.
AU2017366901B2 (en) 2016-11-30 2022-09-29 Bantam Pharmaceutical, Llc Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases
BR112019012263A2 (pt) 2016-12-15 2020-01-28 The Regents Of The University Of California composições e métodos para tratar câncer
WO2018119183A2 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7219218B2 (ja) 2016-12-22 2023-02-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 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
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
BR112019021899A2 (pt) 2017-04-20 2020-08-18 The Regents Of The University Of California moduladores de k-ras
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US10647715B2 (en) * 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
HRP20230377T1 (hr) * 2017-11-15 2023-06-23 Mirati Therapeutics, Inc. Inhibitori mutacije kras g12c
WO2019110751A1 (en) 2017-12-08 2019-06-13 Astrazeneca Ab Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents
TW201942115A (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
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030191143A1 (en) 2001-05-01 2003-10-09 Pitts William J. Fused heterocyclic compounds and use thereof
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
US20160166571A1 (en) 2014-09-18 2016-06-16 Araxes Pharma Llc Combination therapies for treatment of cancer
WO2017201161A1 (en) 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
FELL ET AL.: "Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity", ACS MEDICINAL CHEMISTRY LETTERS, vol. 9, 7 November 2018 (2018-11-07), pages 1230 - 1234, XP055680197 *
MCCORMICK, CLIN CANCER RES, vol. 21, no. 8, 2015, pages 1797 - 1801
OSTREM ET AL., NATURE, vol. 503, 2013, pages 548 - 551
SUN ET AL., AGNEW CHEM INT ED ENGL, vol. 51, no. 25, 2012, pages 6140 - 6143

Cited By (193)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4501932A3 (en) * 2017-11-15 2025-04-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3880208A4 (en) * 2017-11-15 2022-08-17 Mirati Therapeutics, Inc. Kras g12c inhibitors
US11407765B2 (en) 2018-05-08 2022-08-09 Astrazeneca, Ab Tetracyclic heteroaryl compounds
EP4552631A3 (en) * 2018-09-10 2025-07-02 Mirati Therapeutics, Inc. Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer
WO2020055758A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055755A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055756A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020055761A1 (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
EP4552631A2 (en) 2018-09-10 2025-05-14 Mirati Therapeutics, Inc. Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer
US12065430B2 (en) 2018-10-26 2024-08-20 Taiho Pharmaceutical Co., Ltd. Indazole compound or salt thereof
WO2020118066A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
EP4249000A2 (en) 2019-02-12 2023-09-27 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
EP3924053A1 (en) * 2019-02-12 2021-12-22 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
WO2020165732A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
US12410187B2 (en) 2019-03-05 2025-09-09 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
JP7584451B2 (ja) 2019-05-29 2024-11-15 上▲海▼翰森生物医▲薬▼科技有限公司 窒素含有複素環系誘導物レギュレーター、その製造方法及び使用
CN113423703A (zh) * 2019-05-29 2021-09-21 上海翰森生物医药科技有限公司 含氮杂环类衍生物调节剂、其制备方法和应用
JP2022534765A (ja) * 2019-05-29 2022-08-03 上▲海▼翰森生物医▲薬▼科技有限公司 窒素含有複素環系誘導物レギュレーター、その製造方法及び使用
EP3978490A4 (en) * 2019-05-29 2023-04-19 Shanghai Hansoh Biomedical Co., Ltd. HETEROCYCLIC DERIVATIVE REGULATOR CONTAINING NITROGEN, METHOD FOR PREPARATION AND APPLICATION
AU2020282473B2 (en) * 2019-05-29 2025-09-04 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Nitrogen-containing heterocyclic derivative regulator, preparation method therefor and application thereof
RU2829553C2 (ru) * 2019-05-29 2024-10-31 Шанхай Ханьсох Байомедикал Ко., Лтд. Регулятор на основе азотсодержащего гетероциклического производного, способ его получения и его применение
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
CN113423703B (zh) * 2019-05-29 2024-08-02 上海翰森生物医药科技有限公司 含氮杂环类衍生物调节剂、其制备方法和应用
CN112300153B (zh) * 2019-07-26 2023-06-13 博瑞生物医药（苏州）股份有限公司 一种杂环化合物、药物组合物和用途
CN112300153A (zh) * 2019-07-26 2021-02-02 博瑞生物医药（苏州）股份有限公司 一种杂环化合物、药物组合物和用途
JP7756069B2 (ja) 2019-08-02 2025-10-17 シャンハイ ジェミンケア ファーマシューティカル カンパニー，リミティド 四環式化合物、その調製と使用の方法
JP7756069B6 (ja) 2019-08-02 2025-11-27 上海済▲ユウ▼医薬科技股▲フン▼有限公司 四環式化合物、その調製と使用の方法
WO2021023154A1 (zh) * 2019-08-02 2021-02-11 上海济煜医药科技有限公司 四并环类化合物及其制备方法和应用
CN112300195A (zh) * 2019-08-02 2021-02-02 上海济煜医药科技有限公司 四并环类化合物及其制备方法和应用
CN112300195B (zh) * 2019-08-02 2021-12-24 上海济煜医药科技有限公司 四并环类化合物及其制备方法和应用
JP2022543767A (ja) * 2019-08-02 2022-10-14 シャンハイ ジェミンケア ファーマシューティカルズ カンパニー、リミテッド 四環式化合物、その調製と使用の方法
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
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
EP4031542A4 (en) * 2019-09-18 2023-10-25 Merck Sharp & Dohme LLC KRAS G12C MUTANT SMALL MOLECULE INHIBITORS
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
JP2022548791A (ja) * 2019-09-24 2022-11-21 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
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
CN114555586B (zh) * 2019-10-10 2023-06-23 信达生物制药(苏州)有限公司 Krasg12c蛋白抑制剂及其制备方法和用途
WO2021068898A1 (zh) * 2019-10-10 2021-04-15 信达生物制药(苏州)有限公司 新颖的kras g12c蛋白抑制剂及其制备方法和用途
CN114555586A (zh) * 2019-10-10 2022-05-27 信达生物制药(苏州)有限公司 新颖的krasg12c蛋白抑制剂及其制备方法和用途
US11459327B1 (en) 2019-10-23 2022-10-04 Suzhou Zelgen Biopharmaceuticals Co., Ltd. Cycloalkyl and hetero-cycloalkyl inhibitors, preparation methods therefor, and use thereof
CN112694475B (zh) * 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
WO2021078312A1 (zh) * 2019-10-23 2021-04-29 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
CN112694475A (zh) * 2019-10-23 2021-04-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
US12297208B2 (en) 2019-10-28 2025-05-13 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
US12291538B2 (en) 2019-10-28 2025-05-06 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
US11697657B2 (en) 2019-10-28 2023-07-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
WO2021091967A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
EP4656201A2 (en) 2019-11-04 2025-12-03 Revolution Medicines, Inc. Ras inhibitors
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
EP4696316A2 (en) 2019-11-04 2026-02-18 Revolution Medicines, Inc. Ras inhibitors
CN112824410A (zh) * 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
WO2021098859A1 (zh) * 2019-11-21 2021-05-27 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
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
CN115003677A (zh) * 2019-11-29 2022-09-02 大鹏药品工业株式会社 对kras g12d突变具有抑制活性的化合物
CN115003677B (zh) * 2019-11-29 2024-08-27 大鹏药品工业株式会社 对kras g12d突变具有抑制活性的化合物
EP4015520A4 (en) * 2019-12-02 2023-08-23 Shanghai Yingli Pharmaceutical Co. Ltd. OXYGEN-CONTAINING HETEROCYCLIC COMPOUND, PROCESS FOR THEIR PRODUCTION AND ITS USE
JP2023504178A (ja) * 2019-12-02 2023-02-01 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
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
US12195473B2 (en) 2019-12-19 2025-01-14 Jacobio Pharmaceuticals Co., Ltd KRAS mutant protein inhibitors
TWI871397B (zh) * 2019-12-19 2025-02-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ突變蛋白抑制劑
CN113651814B (zh) * 2019-12-19 2022-06-17 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CN113651814A (zh) * 2019-12-19 2021-11-16 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
EP4344702A3 (en) * 2019-12-20 2024-04-10 Novartis AG Pyrazolyl derivatives useful as anti-cancer agents
WO2021124222A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
US11702409B2 (en) 2019-12-20 2023-07-18 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
WO2021129824A1 (zh) * 2019-12-27 2021-07-01 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
CN114901661A (zh) * 2019-12-27 2022-08-12 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
US11312724B2 (en) 2020-01-08 2022-04-26 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
WO2021152149A1 (en) 2020-01-31 2021-08-05 Jazz Pharmaceuticals Ireland Limited Ras inhibitors and methods of using the same
US12612387B2 (en) 2020-01-31 2026-04-28 Jazz Pharmaceuticals Ireland Limited RAS inhibitors and methods of using the same
WO2021169990A1 (zh) * 2020-02-24 2021-09-02 泰励生物科技（上海）有限公司 用于癌症治疗的kras抑制剂
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
CN115427414A (zh) * 2020-04-28 2022-12-02 贝达药业股份有限公司 稠环化合物及其在医药上的应用
WO2021219072A1 (zh) * 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
CN116194456A (zh) * 2020-04-30 2023-05-30 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
CN116194456B (zh) * 2020-04-30 2025-08-29 上海科州药物股份有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
WO2021245051A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
US11945812B2 (en) 2020-06-02 2024-04-02 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
US12545670B2 (en) 2020-06-02 2026-02-10 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN115836072B (zh) * 2020-06-04 2025-10-14 上海德琪医药科技有限公司 Kras g12c蛋白的抑制剂和其用途
CN115836072A (zh) * 2020-06-04 2023-03-21 上海德琪医药科技有限公司 Kras g12c蛋白的抑制剂和其用途
WO2021257736A1 (en) 2020-06-18 2021-12-23 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2021259972A1 (en) 2020-06-24 2021-12-30 Boehringer Ingelheim International Gmbh Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
CN113912608A (zh) * 2020-07-10 2022-01-11 江苏恒瑞医药股份有限公司 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用
US12365676B2 (en) 2020-08-28 2025-07-22 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US12286427B2 (en) 2020-08-28 2025-04-29 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
US12286431B2 (en) 2020-09-11 2025-04-29 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
CN116601151A (zh) * 2020-09-11 2023-08-15 米拉蒂治疗股份有限公司 Kras g12c抑制剂的晶型
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
WO2022056307A1 (en) * 2020-09-11 2022-03-17 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
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
US12281113B2 (en) 2020-09-11 2025-04-22 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
WO2022060836A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
US12162893B2 (en) 2020-09-23 2024-12-10 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022087270A1 (en) 2020-10-23 2022-04-28 Mirati Therapeutics, Inc. Methods for treatment of lung cancers
WO2022089604A1 (en) * 2020-10-30 2022-05-05 Novartis Ag New crystalline forms of a kras g12c inhibitor compound
EP4237412A4 (en) * 2020-10-30 2024-04-10 Novartis AG NEW CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR COMPOUND
CN116472039A (zh) * 2020-10-30 2023-07-21 诺华股份有限公司 Kras g12c抑制剂化合物的新结晶形式
EP4247807A4 (en) * 2020-11-23 2024-10-16 Merck Sharp & Dohme LLC 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
US12421253B2 (en) 2020-12-16 2025-09-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
US11845761B2 (en) 2020-12-18 2023-12-19 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022129925A1 (en) 2020-12-18 2022-06-23 Amphista Therapeutics Limited Novel bifunctional molecules for targeted protein degradation
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022135346A1 (en) * 2020-12-22 2022-06-30 Novartis Ag Pharmaceutical combinations comprising a kras g12c inhibitor and uses of a kras g12c inhibitor for the treatment of cancers
EP4284370A4 (en) * 2021-01-29 2024-12-11 Mirati Therapeutics, Inc. POLYTHERAPIES
WO2022161443A1 (zh) * 2021-02-01 2022-08-04 南京明德新药研发有限公司 嘧啶并吡喃类化合物
TWI793999B (zh) * 2021-02-01 2023-02-21 大陸商南京明德新藥研發有限公司 嘧啶並吡喃化合物
WO2022187527A1 (en) * 2021-03-05 2022-09-09 Nikang Therapeutics, Inc Quinazoline nitrile derivatives as kras inhibitors
WO2022216648A1 (en) 2021-04-08 2022-10-13 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
WO2022214594A1 (en) 2021-04-09 2022-10-13 Boehringer Ingelheim International Gmbh Anticancer therapy
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
WO2022235864A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors
US20220395507A1 (en) * 2021-05-27 2022-12-15 Mirati Therapeutics, Inc. Combination therapies
US12280055B2 (en) * 2021-05-27 2025-04-22 Mirati Therapeutics, Inc. Combination therapies
EP4346826A1 (en) 2021-05-27 2024-04-10 Mirati Therapeutics, Inc. Combination therapies
WO2022261154A1 (en) 2021-06-09 2022-12-15 Eli Lilly And Company Substituted fused azines as kras g12d 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
WO2022269525A1 (en) 2021-06-23 2022-12-29 Novartis Ag Pharmaceutical combinations comprising a kras g12c inhibitor and uses thereof for the treatment of cancers
WO2023280280A1 (zh) * 2021-07-07 2023-01-12 微境生物医药科技(上海)有限公司 作为KRas G12D抑制剂的稠环化合物
WO2023284730A1 (en) 2021-07-14 2023-01-19 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
WO2023283933A1 (en) * 2021-07-16 2023-01-19 Silexon Biotech Co., Ltd. Compounds useful as kras g12d inhibitors
WO2023008462A1 (ja) 2021-07-27 2023-02-02 東レ株式会社 癌の治療及び／又は予防のための医薬品
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
WO2023039020A1 (en) 2021-09-09 2023-03-16 Mirati Therapeutics, Inc. Processes and intermediates for synthesis of adagrasib
WO2023060253A1 (en) 2021-10-08 2023-04-13 Revolution Medicines, Inc. Ras inhibitors
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
US12291539B2 (en) 2021-11-05 2025-05-06 Frontier Medicines Corporation KRAS G12C inhibitors
US12060367B2 (en) 2021-12-01 2024-08-13 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023117681A1 (en) 2021-12-22 2023-06-29 Boehringer Ingelheim International Gmbh Heteroaromatic compounds for the treatment of cancer
WO2023126822A1 (en) 2021-12-28 2023-07-06 Astrazeneca Uk Limited Combination of antibody-drug conjugate and rasg12c inhibitor
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
US12209102B2 (en) 2022-03-11 2025-01-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2023183585A1 (en) 2022-03-25 2023-09-28 Eli Lilly And Company Kras inhibitors
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
EP4511372A4 (en) * 2022-04-18 2026-04-01 Mirati Therapeutics Inc PROCESSES AND INTERMEDIARIES FOR ADAGRASIB SYNTHESIS
US12410212B2 (en) 2022-05-06 2025-09-09 Chugai Seiyaku Kabushiki Kaisha Cyclic compound having selective KRAS inhibitory effect on HRAS and NRAS
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2023240189A1 (en) * 2022-06-10 2023-12-14 Bristol-Myers Squibb Company Tetrahydropyrido 3,4-d pyrimidine derivatives as kras inhibitors
US12059425B2 (en) 2022-08-05 2024-08-13 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US12383503B2 (en) 2022-08-19 2025-08-12 Mirati Therapeutics, Inc. Adagrasib solid pharmaceutical compositions
WO2024047135A1 (en) 2022-08-31 2024-03-07 Jazz Pharmaceuticals Ireland Limited Substituted heterocycles as ras inhibitors
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024206747A1 (en) 2023-03-30 2024-10-03 Eli Lilly And Company Kras inhibitors
WO2024206766A1 (en) 2023-03-31 2024-10-03 Eli Lilly And Company Kras inhibitors
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
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024246114A1 (en) 2023-05-31 2024-12-05 Boehringer Ingelheim International Gmbh Survivin as a biomarker for predicting the responsiveness of cancer treatment
WO2024248123A1 (ja) 2023-06-02 2024-12-05 第一三共株式会社 抗ｈｅｒ３抗体－薬物コンジュゲートとｒａｓｇ１２ｃ阻害剤の組み合わせ
US12606572B2 (en) 2023-06-06 2026-04-21 Kumquat Biosciences Inc. Substituted heterocycles and uses thereof
WO2025019688A3 (en) * 2023-07-20 2025-04-10 Mirati Therapeutics, Inc. Crystalline forms of salts of adagrasib
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025072457A1 (en) 2023-09-27 2025-04-03 Eli Lilly And Company Kras inhibitors
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
US12466840B2 (en) 2023-10-20 2025-11-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS proteins
WO2025132549A1 (en) 2023-12-20 2025-06-26 Boehringer Ingelheim International Gmbh Cancer combination therapy using zongertinib and a kras g12c inhibitor
WO2025145207A1 (en) 2023-12-29 2025-07-03 Bristol-Myers Squibb Company Combination therapy of kras inhibitor and treg-depleting agent
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025242126A1 (zh) * 2024-05-22 2025-11-27 上海正大天晴医药科技开发有限公司 一种药物组合及其应用
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026003808A1 (en) 2024-06-28 2026-01-02 Assia Chemical Industries Ltd. Solid state form of adagrasib and process for preparation
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026059955A1 (en) 2024-09-11 2026-03-19 Eli Lilly And Company (3-((6-(2-amino-benzo[d]thiazol-4-yl)-3-(pyrrolidin-1-yl)-7,9-dihydrofuro[3,4-f]quinazolin-1-yl)amino)- piperidin-2-one derivatives as kras inhibitors for the treatment of cancer
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026075942A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
WO2026075945A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors

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