JP7219218B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
JP7219218B2
JP7219218B2 JP2019534303A JP2019534303A JP7219218B2 JP 7219218 B2 JP7219218 B2 JP 7219218B2 JP 2019534303 A JP2019534303 A JP 2019534303A JP 2019534303 A JP2019534303 A JP 2019534303A JP 7219218 B2 JP7219218 B2 JP 7219218B2
Authority
JP
Japan
Prior art keywords
alkyl
group
aryl
cycloalkyl
membered
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.)
Active
Application number
JP2019534303A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020504742A (ja
JP2020504742A5 (enExample
Inventor
ミヒャエル グマッシュ
ミヒャエル サンダーソン
ディルク ケスラー
クリスティアーネ コフィンク
マシュー ラッセル ネザートン
ユルゲン ラムハーター
トビアス ヴンベルク
マルコ ホフマン
ファビオ サバリース
アンケ バウム
ドロテーア ルドルフ
Original Assignee
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
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 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 filed Critical 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
Publication of JP2020504742A publication Critical patent/JP2020504742A/ja
Publication of JP2020504742A5 publication Critical patent/JP2020504742A5/ja
Application granted granted Critical
Publication of JP7219218B2 publication Critical patent/JP7219218B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • A61K31/7068Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pyridine Compounds (AREA)
JP2019534303A 2016-12-22 2017-12-21 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 Active JP7219218B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16206422.4 2016-12-22
EP16206422 2016-12-22
PCT/EP2017/084265 WO2018115380A1 (en) 2016-12-22 2017-12-21 Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors

Publications (3)

Publication Number Publication Date
JP2020504742A JP2020504742A (ja) 2020-02-13
JP2020504742A5 JP2020504742A5 (enExample) 2021-02-04
JP7219218B2 true JP7219218B2 (ja) 2023-02-07

Family

ID=57777432

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019534303A Active JP7219218B2 (ja) 2016-12-22 2017-12-21 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

Country Status (5)

Country Link
US (2) US10898487B2 (enExample)
EP (2) EP3558979B1 (enExample)
JP (1) JP7219218B2 (enExample)
CN (1) CN110167928A (enExample)
WO (1) WO2018115380A1 (enExample)

Families Citing this family (190)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109843856B (zh) 2016-05-18 2023-05-02 米拉蒂治疗股份有限公司 Kras g12c抑制剂
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
US11104955B2 (en) * 2016-12-30 2021-08-31 Children's Medical Center Corporation MAP2K1 (MEK1) as a therapeutic target for arteriovenous malformations and associated disorders
US20220235013A1 (en) * 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
KR102861303B1 (ko) 2017-11-15 2025-09-17 미라티 테라퓨틱스, 인크. Kras g12c 억제제
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
ES2944306T3 (es) 2017-12-21 2023-06-20 Boehringer Ingelheim Int Piridopirimidinonas sustituidas por bencilamino y derivados como inhibidores de SOS1
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CA3097231A1 (en) * 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2020023502A1 (en) 2018-07-23 2020-01-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
JP2022500385A (ja) 2018-09-10 2022-01-04 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
KR102871791B1 (ko) 2018-09-10 2025-10-15 미라티 테라퓨틱스, 인크. 병용 요법
ES3004338T3 (en) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス, インコーポレイテッド Kras g12c阻害剤
JP2022522777A (ja) * 2019-03-01 2022-04-20 レボリューション メディシンズ インコーポレイテッド 二環式ヘテロアリール化合物及びその使用
EP3930845A1 (en) * 2019-03-01 2022-01-05 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
BR112021021738A2 (pt) * 2019-05-31 2021-12-28 Chiesi Farm Spa Derivados de amino quinazolina como inibidores de p2x3
PH12021553105A1 (en) * 2019-06-19 2022-07-25 Boehringer Ingelheim Int Anticancer combination therapy
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
CA3148745A1 (en) 2019-08-29 2021-03-04 Xiaolun Wang Kras g12d inhibitors
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
CR20220175A (es) * 2019-10-22 2022-06-21 Lupin Ltd Combinación farmacéutica de inhibidores de PRMT5
PE20230249A1 (es) 2019-11-08 2023-02-07 Revolution Medicines Inc Compuestos de heteroarilo biciclicos y usos de estos
CN114667144A (zh) 2019-11-18 2022-06-24 应世生物科技(南京)有限公司 Fak抑制剂在制备用于治疗nras突变的肿瘤的药物中的用途
MX2022006475A (es) * 2019-11-29 2022-09-07 Lupin Ltd Compuestos triciclicos sustituidos.
KR20220130126A (ko) * 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
MX2022008066A (es) 2019-12-27 2022-08-15 Lupin Ltd Compuestos triciclicos sustituidos.
WO2023205701A1 (en) * 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN115244058A (zh) * 2020-04-08 2022-10-25 江苏恒瑞医药股份有限公司 嘧啶并二环类衍生物、其制备方法及其在医药上的应用
EP3903581A1 (en) 2020-04-28 2021-11-03 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors i
EP3903582A1 (en) 2020-04-28 2021-11-03 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors ii
KR20230005261A (ko) 2020-04-28 2023-01-09 바스프 에스이 Qo 억제제 II 에 대한 내성을 부여하는 미토콘드리아 시토크롬 b 단백질 내에 아미노산 치환 F129L 을 함유하는 식물병원성 진균의 퇴치를 위한 스트로빌루린 유형 화합물의 용도
EP3903583A1 (en) 2020-04-28 2021-11-03 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors iii
PL4142495T3 (pl) 2020-04-28 2025-11-24 Basf Se Zastosowanie związków typu strobiluryny do zwalczania grzybów fitopatogennych zawierających podstawienie aminokwasowe f129l w mitochondrialnym białku cytochromu b nadające odporność na inhibitory qo (iii)
CA3170923A1 (en) 2020-04-28 2021-11-04 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors i
EP3903584A1 (en) 2020-04-28 2021-11-03 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors iv
AU2021266044A1 (en) 2020-04-28 2022-11-24 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution F129L in the mitochondrial cytochrome b protein conferring resistance to Qo inhibitors IV
WO2021228028A1 (zh) * 2020-05-09 2021-11-18 正大天晴药业集团股份有限公司 含磷的sos1抑制剂
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
AU2021289163B2 (en) 2020-06-09 2024-05-02 Array Biopharma Inc. 4-oxo-3,4-dihydroquinazolinon compounds for the treatment of BRAF-associated diseases and disorders
WO2021249475A1 (zh) * 2020-06-10 2021-12-16 江苏恒瑞医药股份有限公司 稠合喹唑啉类衍生物、其制备方法及其在医药上的应用
CN115605479B (zh) * 2020-06-11 2024-05-14 江苏恒瑞医药股份有限公司 吡啶酮并嘧啶类衍生物、其制备方法及其在医药上的应用
CN113801114B (zh) * 2020-06-11 2022-11-18 江苏恒瑞医药股份有限公司 稠合二环杂芳基类衍生物、其制备方法及其在医药上的应用
EP4171570A1 (en) * 2020-06-24 2023-05-03 Boehringer Ingelheim International GmbH Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
CN113912608B (zh) * 2020-07-10 2023-07-14 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
WO2022017339A1 (zh) * 2020-07-20 2022-01-27 江苏恒瑞医药股份有限公司 稠合哒嗪类衍生物、其制备方法及其在医药上的应用
EP4186903A4 (en) 2020-07-24 2024-08-07 Medshine Discovery Inc. Quinazoline compound
WO2022028506A1 (zh) * 2020-08-06 2022-02-10 北京泰德制药股份有限公司 Sos1抑制剂、包含其的药物组合物及其用途
EP3970494A1 (en) 2020-09-21 2022-03-23 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors viii
US20230357152A1 (en) 2020-08-11 2023-11-09 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors viii
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER 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
AU2021345111B2 (en) 2020-09-15 2025-11-27 Revolution Medicines, Inc. Indole derivatives as Ras inhibitors in the treatment of cancer
WO2022061348A1 (en) * 2020-09-16 2022-03-24 Biotheryx, Inc. Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
EP4214204A1 (en) * 2020-09-18 2023-07-26 Bayer Aktiengesellschaft Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors
WO2022083657A1 (zh) * 2020-10-20 2022-04-28 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
CN114907324A (zh) * 2021-02-09 2022-08-16 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
CN112174891B (zh) * 2020-11-02 2022-02-01 浙江省农业科学院 一种氟唑菌苯胺代谢物的制备方法
WO2022109171A1 (en) * 2020-11-18 2022-05-27 Modernatx, Inc. Ribonucleic acid purification
WO2022105921A1 (zh) * 2020-11-21 2022-05-27 上海凌达生物医药有限公司 一类嘧啶并杂环类化合物、制备方法和用途
CN114539245A (zh) * 2020-11-26 2022-05-27 上海翰森生物医药科技有限公司 含嘧啶并环类衍生物调节剂、其制备方法和应用
CN116568681B (zh) * 2020-12-07 2026-01-02 北京泰德制药股份有限公司 Sos1抑制剂、包含其的药物组合物及其用途
CN114621231B (zh) * 2020-12-14 2025-09-12 杭州中美华东制药有限公司 一种靶向降解/抑制活性的嵌合化合物及其制备方法和用途
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
EP4267250A1 (en) 2020-12-22 2023-11-01 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
CA3202057A1 (en) * 2020-12-22 2022-06-30 Jae Yul Choi Novel quinazoline derivative compound as sos1 inhibitor, and use thereof
CN114685531B (zh) * 2020-12-25 2024-10-22 武汉誉祥医药科技有限公司 四并环化合物及其药物组合物和应用
US20240254117A1 (en) * 2020-12-27 2024-08-01 Shanghai Ringene Biopharma Co., Ltd. Pyrimido-heterocyclic compounds, and preparation method therefor and use thereof
WO2022143533A1 (zh) * 2020-12-30 2022-07-07 成都百裕制药股份有限公司 喹唑啉衍生物及其在医药上的应用
CN114685488A (zh) * 2020-12-31 2022-07-01 南京圣和药业股份有限公司 作为sos1抑制剂的化合物及其应用
WO2022148442A1 (zh) * 2021-01-07 2022-07-14 武汉人福创新药物研发中心有限公司 6-取代磷酰基喹唑啉类衍生物及其制备方法和用途
CA3203205A1 (en) * 2021-01-19 2022-07-28 Mandar Ramesh Bhonde Pharmaceutical combinations of sos1 inhibitors for treating and/or preventing cancer
WO2022156792A1 (en) * 2021-01-25 2022-07-28 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as sos1 inhibitors
WO2022160931A1 (zh) * 2021-01-28 2022-08-04 浙江海正药业股份有限公司 吡啶并嘧啶类衍生物及其制备方法和用途
CN117279914A (zh) * 2021-01-29 2023-12-22 南京再明医药有限公司 Sos1抑制剂及其制备方法和应用
CN114436976B (zh) * 2021-01-29 2023-07-11 石药集团中奇制药技术(石家庄)有限公司 一种新型喹唑啉类衍生物及其制备和应用
CN114835719A (zh) * 2021-02-01 2022-08-02 苏州泽璟生物制药股份有限公司 取代双环并芳杂环胺类抑制剂及其制备方法和应用
CN114835703A (zh) * 2021-02-02 2022-08-02 苏州泽璟生物制药股份有限公司 取代嘧啶并吡啶酮类抑制剂及其制备方法和应用
CN114853812A (zh) * 2021-02-04 2022-08-05 四川科伦博泰生物医药股份有限公司 含氧化膦基团的化合物、其制备方法及其在医药上的应用
CN114907341A (zh) * 2021-02-08 2022-08-16 武汉人福创新药物研发中心有限公司 吡啶并嘧啶酮类衍生物及其制备方法和用途
CN116669738B (zh) * 2021-02-09 2026-04-03 苏州阿尔脉生物科技有限公司 一种作为sos1抑制剂的嘧啶并吡啶酮类衍生物、其制备方法及用途
CN116568689B (zh) * 2021-02-09 2025-07-11 苏州阿尔脉生物科技有限公司 一种作为sos1抑制剂的多环嘧啶类衍生物、其制备方法及用途
WO2022171018A1 (zh) * 2021-02-09 2022-08-18 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
CN113200981A (zh) * 2021-02-10 2021-08-03 杭州英创医药科技有限公司 作为sos1抑制剂的杂环化合物
CN114907284B (zh) * 2021-02-10 2023-11-03 石药集团中奇制药技术(石家庄)有限公司 一种具有抗肿瘤活性的化合物及其用途
US20240109887A1 (en) * 2021-03-02 2024-04-04 Viva Star Biosciences (Suzhou) Co., Ltd. Novel substituted bicyclic aza-heterocycles as sos1 inhibitors
WO2022187411A1 (en) 2021-03-02 2022-09-09 Kumquat Biosciences Inc. Heterocycles and uses thereof
CN117062818A (zh) * 2021-03-05 2023-11-14 南京再明医药有限公司 新型sos1抑制剂及其制备方法和应用
CN115028644A (zh) * 2021-03-08 2022-09-09 首药控股(北京)股份有限公司 Sos1抑制剂杂环化合物
CN115043817A (zh) * 2021-03-09 2022-09-13 苏州泽璟生物制药股份有限公司 Sos1蛋白水解调节剂及其制备方法和应用
US20240197888A1 (en) * 2021-03-17 2024-06-20 Biotheryx, Inc. Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
WO2022199635A1 (zh) * 2021-03-25 2022-09-29 南京明德新药研发有限公司 苄氨基喹唑啉类衍生物
CN116917286B (zh) * 2021-03-26 2026-04-28 无锡瓴方生物医药科技有限公司 6-氨基甲酸酯取代的杂芳环衍生物
AU2022250712A1 (en) 2021-03-31 2023-10-05 Sevenless Therapeutics Limited Sos1 inhibitors and ras inhibitors for use in the treatment of pain
GB202104609D0 (en) 2021-03-31 2021-05-12 Sevenless Therapeutics Ltd New Treatments for Pain
WO2022212546A1 (en) * 2021-03-31 2022-10-06 Acerand Therapeutics (Usa) Limited Pyridopyrimidinone compounds
EP4319745A1 (en) * 2021-04-09 2024-02-14 Revolution Medicines, Inc. Use of sos1 inhibitors with ras inhibitors to treat cancers
US20240238294A1 (en) 2021-04-09 2024-07-18 Boehringer Ingelheim International Gmbh Anticancer therapy
CA3213079A1 (en) 2021-04-13 2022-10-20 Kristin Lynne ANDREWS Amino-substituted heterocycles for treating cancers with egfr mutations
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
CN115215847B (zh) * 2021-04-16 2025-05-13 中国科学院上海药物研究所 一类kras-sos1抑制剂、其制备方法及其应用
WO2022222875A1 (zh) * 2021-04-19 2022-10-27 昆药集团股份有限公司 一种苯并嘧啶三环衍生物及其制备方法和应用
CN115215884A (zh) * 2021-04-19 2022-10-21 昆药集团股份有限公司 苯并嘧啶三环类衍生物及其制备方法和应用
WO2022223034A1 (zh) * 2021-04-23 2022-10-27 上海领泰生物医药科技有限公司 Sos1降解剂及其制备方法和应用
WO2022251193A1 (en) * 2021-05-27 2022-12-01 Mirati Therapeutics, Inc. Combination therapies
WO2022258057A1 (en) * 2021-06-11 2022-12-15 Jingrui Biopharma Co., Ltd. Compounds as anticancer agents
JP2024522768A (ja) * 2021-06-16 2024-06-21 バイオセリックス, インコーポレイテッド Sos1タンパク質分解剤、その医薬組成物及びそれらの治療的応用
WO2022262691A1 (en) * 2021-06-17 2022-12-22 Beijing Innocare Pharma Tech Co., Ltd. Heterocyclic compounds as sos1 inhibitors
EP4358963A4 (en) 2021-06-21 2025-04-02 Mirati Therapeutics, Inc. SOS1 INHIBITORS
CN117580836A (zh) * 2021-06-24 2024-02-20 四川汇宇制药股份有限公司 一种嘧啶并环结构衍生物及其用途
CN117769556A (zh) * 2021-07-23 2024-03-26 浙江海正药业股份有限公司 嘧啶并环类衍生物及其制备方法和用途
CN115677699B (zh) * 2021-07-23 2024-11-22 武汉誉祥医药科技有限公司 三并环化合物及其药物组合物和应用
CN115677824B (zh) * 2021-07-26 2026-02-03 中国科学院上海药物研究所 可诱导sos1蛋白质降解的化合物、制备方法和用途
CN115677601B (zh) * 2021-07-29 2025-06-03 石药集团中奇制药技术(石家庄)有限公司 一种具有抗肿瘤活性的化合物及其用途
EP4375284A1 (en) * 2021-08-03 2024-05-29 Evopoint Biosciences Co., Ltd. Fused ring compound, pharmaceutical composition, and application thereof
US20240382475A1 (en) * 2021-08-30 2024-11-21 Zhejiang Hisun Pharmaceutical Co., Ltd. Quinazoline Derivative, Or Preparation Method Therefor And Use Thereof
CN115417868B (zh) * 2021-09-13 2024-04-02 石药集团中奇制药技术(石家庄)有限公司 一种具有抗肿瘤活性的杂环化合物及其用途
CN117986265A (zh) * 2021-09-14 2024-05-07 北京福元医药股份有限公司 苄氨基取代的嘧啶并吡喃酮衍生物及其组合物、制剂和用途
EP4417607A4 (en) 2021-09-17 2025-08-06 Nanjing Zaiming Pharmaceutical Co Ltd HETEROCYCLIC COMPOUND USED AS AN SOS1 INHIBITOR AND USES THEREOF
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
US20240425501A1 (en) * 2021-10-21 2024-12-26 Sanjita Sasmal Novel bicyclic heteroaryl derivatives as sos1:kras proteinprotein interaction inhibitors
WO2023072671A1 (en) 2021-10-28 2023-05-04 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors ix
WO2023072670A1 (en) 2021-10-28 2023-05-04 Basf Se Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors x
CN120923498A (zh) * 2021-11-04 2025-11-11 北京福元医药股份有限公司 苄氨基取代的杂多环化合物及其组合物、制剂和用途
CN116143708A (zh) * 2021-11-21 2023-05-23 四川汇宇制药股份有限公司 一种多取代苯并氮杂芳基衍生物及其用途
EP4441051A1 (en) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
CN119013272A (zh) 2021-12-01 2024-11-22 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物
WO2023099623A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CR20240233A (es) 2021-12-01 2024-07-17 Univ Vanderbilt Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer
EP4441056A1 (en) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023098825A1 (zh) * 2021-12-02 2023-06-08 勤浩医药(苏州)有限公司 Sos1抑制剂、包含其的药物组合物及其用途
JP2024545073A (ja) 2021-12-08 2024-12-05 アレイ バイオファーマ インコーポレイテッド N-(2-クロロ-3-((5-クロロ-3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イル)アミノ)-4-フルオロフェニル)-3-フルオロアゼチジン-1-スルホンアミドの結晶形態
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
KR20240122545A (ko) 2021-12-17 2024-08-12 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 항종양 활성을 갖는 헤테로고리 화합물 및 그 용도
US20250154147A1 (en) 2022-01-14 2025-05-15 Jazz Pharmaceuticals Ireland Limited Novel amine-substituted phthalazines and derivatives as sos1 inhibitors
EP4467542A4 (en) * 2022-01-21 2025-07-02 Medshine Discovery Inc CRYSTALLINE FORM OF AN ALLYL METHYLPYRIDOPYRIMIDINE COMPOUND
CN118574830A (zh) * 2022-01-28 2024-08-30 中山优理生物医药有限公司 一种哒嗪并吡啶酮类化合物、其药物组合物及应用
KR20230121208A (ko) 2022-02-10 2023-08-18 (주)파로스아이바이오 Sos1 억제제 및 이의 유도체
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CN116768858B (zh) * 2022-03-15 2025-09-12 杭州中美华东制药有限公司 具有kras-sos1抑制或降解活性的嵌合化合物及其用途
US12419962B2 (en) 2022-03-16 2025-09-23 Biotheryx, Inc. Quinazolines, pharmaceutical compositions, and therapeutic applications
GB202203976D0 (en) 2022-03-22 2022-05-04 Jazz Pharmaceuticals Ireland Ltd Tricyclic phthalazines and derivatives as sos1 inhibitors
WO2023190748A1 (ja) 2022-03-31 2023-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
IL315648A (en) * 2022-04-08 2024-11-01 Mirati Therapeutics Inc Combination therapy of SOS1 inhibitor and MEK inhibitor
IL315645A (en) * 2022-04-08 2024-11-01 Mirati Therapeutics Inc Combination therapies comprising a sos1 inhibitor and an egfr inhibitor
CA3246750A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. MACROCYCLES AND HETEROCYCLES AND THEIR USES
CN117024404A (zh) * 2022-05-10 2023-11-10 四川汇宇制药股份有限公司 苯并吡啶衍生物及其用途
AU2023285116A1 (en) 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN117263950A (zh) * 2022-06-13 2023-12-22 上海优理惠生医药有限公司 一种哒嗪类化合物、其药物组合物及应用
TW202404605A (zh) * 2022-07-07 2024-02-01 大陸商武漢人福創新藥物研發中心有限公司 包含sos1抑制劑的藥物組成物
JP2025528836A (ja) 2022-08-17 2025-09-02 ツリーライン バイオサイエンシズ インコーポレイテッド ピリドピリミジンKRas阻害剤
CN119894893A (zh) 2022-09-16 2025-04-25 拜耳公司 用于治疗癌症的砜取代的吡啶并[3,4-d]嘧啶衍生物
CN119894894B (zh) * 2022-09-23 2025-12-05 无锡瓴方生物医药科技有限公司 喹唑啉类化合物的晶型及其制备方法
WO2024074827A1 (en) 2022-10-05 2024-04-11 Sevenless Therapeutics Limited New treatments for pain
KR20240049772A (ko) * 2022-10-07 2024-04-17 제일약품주식회사 신규한 바이사이클릭 헤테로사이클릴 화합물 및 이의 용도
CN120112538A (zh) 2022-10-13 2025-06-06 拜耳公司 Sos1抑制剂
WO2024083255A1 (zh) * 2022-10-21 2024-04-25 上海领泰生物医药科技有限公司 苄基或噻吩亚甲基取代的氨基喹唑啉衍生物及其作为sos1降解剂的用途
WO2024119028A1 (en) * 2022-12-02 2024-06-06 Accutar Biotechnology, Inc. Substituted quinoline derivatives having sos1 inhibition activities and uses thereof
DE102024102431A1 (de) 2023-02-01 2024-08-01 Deutsche Institute für Textil- und Faserforschung Denkendorf Stiftung des öffentlichen Rechts Amin-funktionalisiertes Cellulosematerial, Verfahren zu dessen Herstellung und Verwendung als CO2-Adsorber
CN120813358A (zh) 2023-04-06 2025-10-17 卫材R&D管理有限公司 用于治疗肿瘤的药物组合物
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
EP4688790A1 (en) 2023-04-07 2026-02-11 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
EP4720059A1 (en) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
US20250019385A1 (en) 2023-05-30 2025-01-16 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
AU2024280280C1 (en) 2023-05-31 2026-01-15 Sichuan Huiyu Pharmaceutical Co., Ltd. Nitrogen-containing functional group-substituted pyridazinopyridone derivative and use thereof
CN116444447B (zh) * 2023-06-19 2023-09-22 中国药科大学 一种sos1和hdac双靶点喹唑啉羟肟酸化合物及其制法和应用
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
TW202504599A (zh) 2023-06-30 2025-02-01 美商必治妥美雅史谷比公司 Kras抑制劑
TW202515575A (zh) 2023-09-11 2025-04-16 美商金橘生物科技公司 細胞增殖調節劑及其用途
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
AU2024344161A1 (en) 2023-09-21 2026-03-26 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyridine kras inhibitors
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
AU2024369088A1 (en) 2023-10-25 2026-05-07 Kumquat Biosciences Inc. Combinations of sos-1 inhibitors with osimertinib and/or met inhibitors to treat cancer
WO2025090810A1 (en) 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Use of sos1 inhibitors and amivantamab to treat cancer
WO2025090812A1 (en) * 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Methods of modulating cell proliferation
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025202022A1 (en) 2024-03-27 2025-10-02 Bayer Aktiengesellschaft Anticancer macrocyclic quinazoline-based inhibitors of the ineraction between ras and sos1
WO2025210042A1 (en) 2024-04-03 2025-10-09 Boehringer Ingelheim International Gmbh Combination of zongertinib with a sos1 inhibitor for use in the treatment of cancer
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010529115A (ja) 2007-06-05 2010-08-26 ハンミ ファーム. シーオー., エルティーディー. 癌細胞成長抑制用新規アミド誘導体
WO2016077793A1 (en) 2014-11-14 2016-05-19 Children's Hospital Medical Center Sos1 inhibitors for cancer treatment

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6174899B1 (en) 1998-05-14 2001-01-16 Morton Shulman Orally administered analgesic composition comprising myfadol
WO2004003152A2 (en) * 2002-06-26 2004-01-08 Chiron Corporation Sos1 inhibitors
JP2010521513A (ja) 2007-03-23 2010-06-24 エフ.ホフマン−ラ ロシュ アーゲー アザ−ピリドピリミジノン誘導体
US8383635B2 (en) 2008-08-12 2013-02-26 Glaxosmithkline Llc Chemical compounds
MX2011005664A (es) 2008-11-28 2011-06-16 Novartis Ag Inhibidores de hsp90 para tratamiento terapeutico.
EP2376116B1 (en) 2008-12-12 2015-12-09 Boehringer Ingelheim International GmbH Anti-igf antibodies
MX2012004846A (es) 2009-10-29 2012-10-05 Genosco Inhibidores de cinasa.
JP2013544524A (ja) 2010-12-06 2013-12-19 ターポン バイオシステムズ,インコーポレイテッド 生物学的生成物の連続プロセス法
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
IN2014MN01754A (enExample) 2012-03-14 2015-07-03 Lupin Ltd
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Kras g12c之共價抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
EP4378957A3 (en) 2015-07-29 2024-08-07 Novartis AG Combination therapies comprising antibody molecules to pd-1
US10898487B2 (en) * 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
US20220235013A1 (en) 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
PH12021553105A1 (en) 2019-06-19 2022-07-25 Boehringer Ingelheim Int Anticancer combination therapy

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010529115A (ja) 2007-06-05 2010-08-26 ハンミ ファーム. シーオー., エルティーディー. 癌細胞成長抑制用新規アミド誘導体
WO2016077793A1 (en) 2014-11-14 2016-05-19 Children's Hospital Medical Center Sos1 inhibitors for cancer treatment

Also Published As

Publication number Publication date
US12053473B2 (en) 2024-08-06
JP2020504742A (ja) 2020-02-13
EP3558979A1 (en) 2019-10-30
CN110167928A (zh) 2019-08-23
US10898487B2 (en) 2021-01-26
WO2018115380A1 (en) 2018-06-28
US20190358230A1 (en) 2019-11-28
EP3558979B1 (en) 2021-02-17
EP3878850A1 (en) 2021-09-15
US20210177851A1 (en) 2021-06-17

Similar Documents

Publication Publication Date Title
JP7808058B2 (ja) がんを治療するための縮合環化2-アミノ-3-シアノチオフェン及び誘導体
JP7189956B2 (ja) Sos1阻害剤としての新規なベンジルアミノ置換ピリドピリミジノンおよび誘導体
JP2020504742A (ja) 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
WO2023099608A1 (en) Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099612A1 (en) Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4441054A1 (en) Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099624A1 (en) Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4441050A1 (en) Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
JP2022537044A (ja) 抗がん併用療法
JP2023512174A (ja) HER2阻害薬としての[1,3]ジアジノ[5,4-d]ピリミジン
HK40097417A (en) Benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors
HK40039222A (en) Benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors
HK40039222B (en) Benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors
BR112020010123B1 (pt) Piridopirimidinonas substituídas por benzilamino, derivados como inibidores de sos1, composições e preparações farmacêuticas, bem como seus usos

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201221

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201221

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211117

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20211125

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220210

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220413

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220517

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220801

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221031

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20221227

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230126

R150 Certificate of patent or registration of utility model

Ref document number: 7219218

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250