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 PDFInfo
- 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
Links
Images
Classifications
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
- A61K31/495—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
- A61K31/5375—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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/08—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/10—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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)
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)
| 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)
| 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)
| 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 |
-
2017
- 2017-12-21 US US16/472,433 patent/US10898487B2/en active Active
- 2017-12-21 JP JP2019534303A patent/JP7219218B2/ja active Active
- 2017-12-21 CN CN201780083358.7A patent/CN110167928A/zh active Pending
- 2017-12-21 WO PCT/EP2017/084265 patent/WO2018115380A1/en not_active Ceased
- 2017-12-21 EP EP17828914.6A patent/EP3558979B1/en active Active
- 2017-12-21 EP EP20216236.8A patent/EP3878850A1/en not_active Withdrawn
-
2020
- 2020-10-22 US US17/077,232 patent/US12053473B2/en active Active
Patent Citations (2)
| 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 |