TWI869913B - 吡啶并[4,3-d]嘧啶化合物 - Google Patents
吡啶并[4,3-d]嘧啶化合物 Download PDFInfo
- Publication number
- TWI869913B TWI869913B TW112124839A TW112124839A TWI869913B TW I869913 B TWI869913 B TW I869913B TW 112124839 A TW112124839 A TW 112124839A TW 112124839 A TW112124839 A TW 112124839A TW I869913 B TWI869913 B TW I869913B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- tautomer
- hydrate
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/16—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263358324P | 2022-07-05 | 2022-07-05 | |
| US63/358,324 | 2022-07-05 | ||
| US202263394338P | 2022-08-02 | 2022-08-02 | |
| US63/394,338 | 2022-08-02 | ||
| US202263414939P | 2022-10-11 | 2022-10-11 | |
| US63/414,939 | 2022-10-11 | ||
| US202363502931P | 2023-05-18 | 2023-05-18 | |
| US63/502,931 | 2023-05-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202409047A TW202409047A (zh) | 2024-03-01 |
| TWI869913B true TWI869913B (zh) | 2025-01-11 |
Family
ID=87426656
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW112124839A TWI869913B (zh) | 2022-07-05 | 2023-07-04 | 吡啶并[4,3-d]嘧啶化合物 |
| TW113147938A TW202513571A (zh) | 2022-07-05 | 2023-07-04 | 吡啶并[4,3-d]嘧啶化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113147938A TW202513571A (zh) | 2022-07-05 | 2023-07-04 | 吡啶并[4,3-d]嘧啶化合物 |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP4551296A1 (enExample) |
| JP (1) | JP2025525406A (enExample) |
| KR (1) | KR20250029954A (enExample) |
| CN (1) | CN119585286A (enExample) |
| AU (1) | AU2023302139A1 (enExample) |
| CA (1) | CA3261000A1 (enExample) |
| CL (1) | CL2024003699A1 (enExample) |
| CO (1) | CO2024016875A2 (enExample) |
| CR (1) | CR20240556A (enExample) |
| DO (1) | DOP2024000275A (enExample) |
| IL (1) | IL317957A (enExample) |
| MA (1) | MA71388A (enExample) |
| MX (1) | MX2024015001A (enExample) |
| PE (1) | PE20250259A1 (enExample) |
| PY (1) | PY2352053A (enExample) |
| TW (2) | TWI869913B (enExample) |
| WO (1) | WO2024009191A1 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| MD4051678T2 (en) | 2019-10-28 | 2026-07-31 | Merck Sharp & Dohme Llc | Small molecule inhibitors of the KRAS G12C mutant |
| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| US12702658B2 (en) | 2020-04-24 | 2026-08-11 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| WO2022109487A1 (en) | 2020-11-23 | 2022-05-27 | Merck Sharp & Dohme Corp. | Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant |
| US20260200925A1 (en) * | 2021-11-24 | 2026-07-16 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras mutated proteins |
| WO2023172737A1 (en) | 2022-03-11 | 2023-09-14 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| AU2023320565A1 (en) | 2022-08-05 | 2025-01-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2024032703A1 (en) * | 2022-08-11 | 2024-02-15 | Beigene, Ltd. | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
| AU2023321005A1 (en) * | 2022-08-12 | 2025-03-20 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Tricyclic compounds and medical use thereof |
| TW202434606A (zh) * | 2022-11-17 | 2024-09-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合三環類化合物、其製備方法及其在醫藥上的應用 |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
| WO2024178304A1 (en) * | 2023-02-24 | 2024-08-29 | Alterome Therapeutics, Inc. | Kras modulators |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| CR20250413A (es) * | 2023-04-05 | 2025-11-06 | Pfizer | Compuestos de pirido[4,3–d]pirimidina |
| WO2024218686A1 (en) * | 2023-04-20 | 2024-10-24 | Pfizer Inc. | Pyrido[4,3-d]pyrimidine compounds |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121194980A (zh) * | 2023-05-16 | 2025-12-23 | 和记黄埔医药（上海）有限公司 | 三环类化合物及其用途 |
| EP4724445A1 (en) | 2023-06-06 | 2026-04-15 | Kumquat Biosciences Inc. | Substituted heterocycles and uses thereof |
| EP4735451A1 (en) | 2023-06-30 | 2026-05-06 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| WO2025006967A1 (en) | 2023-06-30 | 2025-01-02 | Bristol-Myers Squibb Company | Kras inhibitors |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20260096846A (ko) | 2023-10-20 | 2026-06-24 | 머크 샤프 앤드 돔 엘엘씨 | Kras 단백질의 소분자 억제제 |
| AU2024404270A1 (en) * | 2023-12-19 | 2026-07-23 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Fused tricyclic compound and medical use thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202608896A (zh) * | 2024-04-30 | 2026-03-01 | 大陸商和記黃埔醫藥（上海）有限公司 | 抗體藥物偶聯物及其用途 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| TW202615038A (zh) | 2024-08-07 | 2026-04-16 | 美商太斯萊特醫藥美國有限責任公司 | 包含拓樸異構酶有效載荷之靶向ｋｒａｓ之共價誘導之藥物結合物 |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
| CN119874616B (zh) * | 2025-03-28 | 2025-05-30 | 四川美域高生物医药科技有限公司 | 一种有机中间体及其制备方法和应用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022132200A1 (en) * | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| TW202315626A (zh) * | 2021-08-31 | 2023-04-16 | 大陸商勁方醫藥科技(上海)有限公司 | 嘧啶并環類化合物及其製法和用途 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR045563A1 (es) | 2003-09-10 | 2005-11-02 | Warner Lambert Co | Anticuerpos dirigidos a m-csf |
| SI2242771T1 (sl) | 2007-12-14 | 2013-09-30 | Bristol-Myers Squibb Company | Vezane molekule k humanemu ox40 receptorju |
| SA112330278B1 (ar) | 2011-02-18 | 2015-10-09 | ستيم سينتركس، انك. | مواد ضابطة جديدة وطرق للاستخدام |
| EP2760857A1 (en) | 2011-09-27 | 2014-08-06 | F.Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| EP2780039B9 (en) | 2011-11-17 | 2018-04-18 | Pfizer Inc | Cytotoxic peptides and antibody drug conjugates thereof |
| MX2016017393A (es) | 2014-07-01 | 2017-09-05 | Pfizer | Diacuerpos heterodimericos biespecificos y sus usos. |
| HUE057285T2 (hu) | 2015-04-13 | 2022-04-28 | Pfizer | Terápiás ellenanyagok és alkalmazásaik |
| WO2017175156A1 (en) | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
| SG10201900628RA (en) | 2016-04-07 | 2019-02-27 | Glaxosmithkline Ip Dev Ltd | Heterocyclic amides useful as protein modulators |
| US11589667B2 (en) | 2016-11-16 | 2023-02-28 | Wink Robotics | Deformable end effectors for cosmetic robotics |
| WO2018206539A1 (en) * | 2017-05-11 | 2018-11-15 | Astrazeneca Ab | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| CN111148762A (zh) | 2017-05-31 | 2020-05-12 | 斯特库伯株式会社 | 免疫特异性结合至btn1a1的抗体和分子及其治疗性用途 |
| JP7234142B2 (ja) | 2017-06-02 | 2023-03-07 | ファイザー・インク | Ｆｌｔ３に特異的な抗体およびその使用 |
| MA49772A (fr) | 2017-08-04 | 2021-04-21 | Merck Sharp & Dohme | Agonistes benzo[b]thiophène de sting pour le traitement du cancer |
| EP3964516A4 (en) * | 2019-04-28 | 2023-01-11 | Genfleet Therapeutics (Shanghai) Inc. | OXAAZACHUINAZOLINE-7( 8H)-KETONE COMPOUND, PROCESS FOR ITS PRODUCTION AND ITS PHARMACEUTICAL APPLICATION |
| CN114615981B (zh) | 2019-08-29 | 2024-04-12 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂 |
| CN113980032B (zh) * | 2020-07-27 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 稠合四环类衍生物、其制备方法及其在医药上的应用 |
| CN117083281A (zh) * | 2021-03-24 | 2023-11-17 | 南京明德新药研发有限公司 | 嘧啶并杂环类化合物及其应用 |
| CN118019746A (zh) * | 2021-09-27 | 2024-05-10 | 北京加科思新药研发有限公司 | 多环稠环衍生物及其用途 |
-
2023
- 2023-06-30 MA MA71388A patent/MA71388A/fr unknown
- 2023-06-30 CN CN202380051793.7A patent/CN119585286A/zh active Pending
- 2023-06-30 PE PE2024002870A patent/PE20250259A1/es unknown
- 2023-06-30 JP JP2024576355A patent/JP2025525406A/ja active Pending
- 2023-06-30 WO PCT/IB2023/056844 patent/WO2024009191A1/en not_active Ceased
- 2023-06-30 CR CR20240556A patent/CR20240556A/es unknown
- 2023-06-30 KR KR1020257003513A patent/KR20250029954A/ko not_active Withdrawn
- 2023-06-30 EP EP23744558.0A patent/EP4551296A1/en active Pending
- 2023-06-30 CA CA3261000A patent/CA3261000A1/en active Pending
- 2023-06-30 AU AU2023302139A patent/AU2023302139A1/en active Pending
- 2023-06-30 IL IL317957A patent/IL317957A/en unknown
- 2023-07-04 TW TW112124839A patent/TWI869913B/zh active
- 2023-07-04 TW TW113147938A patent/TW202513571A/zh unknown
- 2023-07-04 PY PY202302352053A patent/PY2352053A/es unknown
-
2024
- 2024-12-02 CL CL2024003699A patent/CL2024003699A1/es unknown
- 2024-12-03 MX MX2024015001A patent/MX2024015001A/es unknown
- 2024-12-09 CO CONC2024/0016875A patent/CO2024016875A2/es unknown
- 2024-12-30 DO DO2024000275A patent/DOP2024000275A/es unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022132200A1 (en) * | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| TW202315626A (zh) * | 2021-08-31 | 2023-04-16 | 大陸商勁方醫藥科技(上海)有限公司 | 嘧啶并環類化合物及其製法和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| TW202409047A (zh) | 2024-03-01 |
| CA3261000A1 (en) | 2024-01-11 |
| AU2023302139A1 (en) | 2024-12-19 |
| MX2024015001A (es) | 2025-01-09 |
| CO2024016875A2 (es) | 2024-12-19 |
| PY2352053A (es) | 2025-03-06 |
| TW202513571A (zh) | 2025-04-01 |
| KR20250029954A (ko) | 2025-03-05 |
| EP4551296A1 (en) | 2025-05-14 |
| CL2024003699A1 (es) | 2025-04-11 |
| JP2025525406A (ja) | 2025-08-05 |
| IL317957A (en) | 2025-02-01 |
| MA71388A (fr) | 2025-04-30 |
| CR20240556A (es) | 2025-01-29 |
| CN119585286A (zh) | 2025-03-07 |
| DOP2024000275A (es) | 2025-01-31 |
| PE20250259A1 (es) | 2025-01-29 |
| WO2024009191A1 (en) | 2024-01-11 |
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