SA522433155B1 - مركبات ثلاثية الحلقة مستبدلة - Google Patents
مركبات ثلاثية الحلقة مستبدلةInfo
- Publication number
- SA522433155B1 SA522433155B1 SA522433155A SA522433155A SA522433155B1 SA 522433155 B1 SA522433155 B1 SA 522433155B1 SA 522433155 A SA522433155 A SA 522433155A SA 522433155 A SA522433155 A SA 522433155A SA 522433155 B1 SA522433155 B1 SA 522433155B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- compound
- formula
- rasopathy
- proliferative
- infectious
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- C07D498/20—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
مركبات ثلاثية الحلقة مستبدلة SUBSTITUTED TRICYCLIC COMPOUNDS الملخـــص يتعلق الاختراع الحالي بمركبات الصيغة العامة (I)، في صورتها الصنوانية، أيزومير فراغي، ملح مقبول صيدلانيا منها، متعدد الأشكال، أو تذاوب منها، حيث تكون الحلقة A، الحلقة B، R1 إلى R4، و n كما تم تعريفهم في الوصف التفصيلي، لاستخدامها كمثبطات SOS1 (Son of sevenless homolog 1) في علاج الأمراض أو الاضطرابات التكاثرية، المُعدية وRASopathy (المتلازمات التنموية التي تسببها طفرات السلالة الجرثومية). يتعلق الاختراع أيضًا بطرق لتصنيع مركب الصيغة I، التركيبات الصيدلانية التي تحتوي على مركب الصيغة I، طريقة لعلاج الأمراض أو الاضطرابات التكاثرية، المُعدية وRASopathy، على سبيل المثال، السرطان، من خلال إعطاء المركب المذكور وتركيبات مركب الصيغة I مع المكونات النشطة الأخرى.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201921054254 | 2019-12-27 | ||
| IN201921049099 | 2019-12-29 | ||
| IN202021022668 | 2020-05-29 | ||
| IN202021032769 | 2020-07-30 | ||
| IN202021035200 | 2020-08-14 | ||
| PCT/IB2020/062462 WO2021130731A1 (en) | 2019-12-27 | 2020-12-27 | Substituted tricyclic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SA522433155B1 true SA522433155B1 (ar) | 2025-04-20 |
Family
ID=74184675
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA522433155A SA522433155B1 (ar) | 2019-12-27 | 2022-06-27 | مركبات ثلاثية الحلقة مستبدلة |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US20230119316A1 (ar) |
| EP (1) | EP4081521B1 (ar) |
| JP (1) | JP7642647B2 (ar) |
| KR (1) | KR20220132543A (ar) |
| CN (1) | CN115605476B (ar) |
| AU (1) | AU2020412429B2 (ar) |
| BR (1) | BR112022012641A2 (ar) |
| CA (1) | CA3165864A1 (ar) |
| CL (1) | CL2022001739A1 (ar) |
| CO (1) | CO2022010460A2 (ar) |
| CR (1) | CR20220363A (ar) |
| DK (1) | DK4081521T3 (ar) |
| EC (1) | ECSP22058816A (ar) |
| FI (1) | FI4081521T3 (ar) |
| GE (2) | GEAP202416015A (ar) |
| HR (1) | HRP20260329T1 (ar) |
| IL (1) | IL294198B1 (ar) |
| LT (1) | LT4081521T (ar) |
| MA (1) | MA58181B1 (ar) |
| MX (1) | MX2022008066A (ar) |
| PE (1) | PE20221283A1 (ar) |
| PH (1) | PH12022551585A1 (ar) |
| PT (1) | PT4081521T (ar) |
| RS (1) | RS67848B1 (ar) |
| SA (1) | SA522433155B1 (ar) |
| WO (1) | WO2021130731A1 (ar) |
| ZA (1) | ZA202207722B (ar) |
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| BR112019015484A2 (pt) | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| AU2019301510B2 (en) | 2018-07-09 | 2024-06-13 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Anthelminthic heterocyclic compounds |
| CA3133100A1 (en) | 2019-03-19 | 2020-09-24 | Boehringer Ingelheim Animal Health USA Inc. | Anthelmintic aza-benzothiophene and aza-benzofuran compounds |
| CA3165168A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| KR20230028268A (ko) | 2020-05-29 | 2023-02-28 | 뵈링거 잉겔하임 애니멀 헬스 유에스에이 인코포레이티드 | 구충성 헤테로시클릭 화합물 |
| MX2023003060A (es) | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
| EP4234548A4 (en) * | 2020-10-20 | 2024-10-23 | Suzhou Zelgen Biopharmaceutical Co., Ltd. | SUBSTITUTED BENZO OR PYRIDOPYRIMIDINE AMINE INHIBITOR, ITS PREPARATION METHOD AND ITS APPLICATION |
| WO2022121813A1 (zh) * | 2020-12-07 | 2022-06-16 | 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 |
| MX2023008460A (es) * | 2021-01-19 | 2023-09-12 | Lupin Ltd | Combinaciones farmacéuticas de inhibidores de sos1 para el tratamiento y/o prevención del cáncer. |
| 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 |
| 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 |
| EP4313151A1 (en) | 2021-03-31 | 2024-02-07 | Sevenless Therapeutics Limited | Sos1 inhibitors and ras inhibitors for use in the treatment of pain |
| WO2022214594A1 (en) | 2021-04-09 | 2022-10-13 | Boehringer Ingelheim International Gmbh | Anticancer therapy |
| TWI807787B (zh) * | 2021-04-19 | 2023-07-01 | 大陸商昆藥集團股份有限公司 | 苯並嘧啶三環衍生物及製備方法和應用 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| UY39995A (es) | 2021-11-01 | 2023-05-15 | Boehringer Ingelheim Vetmedica GmbH | Compuestos de pirrolopiridazina como antihelmínticos |
| 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 |
| CA3240780A1 (en) * | 2021-12-17 | 2023-06-22 | Zhenyu Wang | Heterocyclic compound having anti-tumor activity and use thereof |
| TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
| EP4463454A1 (en) | 2022-01-14 | 2024-11-20 | Jazz Pharmaceuticals Ireland Limited | Novel amine-substituted phthalazines and derivatives as sos1 inhibitors |
| 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 |
| WO2023165438A1 (zh) * | 2022-03-03 | 2023-09-07 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
| GB202203976D0 (en) | 2022-03-22 | 2022-05-04 | Jazz Pharmaceuticals Ireland Ltd | Tricyclic phthalazines and derivatives as sos1 inhibitors |
| IL316768A (en) | 2022-05-25 | 2025-01-01 | Ikena Oncology Inc | MEK inhibitors and their uses |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20260005904A (ko) | 2023-04-07 | 2026-01-12 | 레볼루션 메디슨즈, 인크. | 매크로사이클릭 ras 억제제 |
| CN121263418A (zh) | 2023-04-07 | 2026-01-02 | 锐新医药公司 | 大环ras抑制剂 |
| KR20250172857A (ko) | 2023-04-14 | 2025-12-09 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형 |
| 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 |
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2020
- 2020-12-27 KR KR1020227026096A patent/KR20220132543A/ko active Pending
- 2020-12-27 AU AU2020412429A patent/AU2020412429B2/en active Active
- 2020-12-27 JP JP2022539232A patent/JP7642647B2/ja active Active
- 2020-12-27 GE GEAP202416015A patent/GEAP202416015A/en unknown
- 2020-12-27 WO PCT/IB2020/062462 patent/WO2021130731A1/en not_active Ceased
- 2020-12-27 MX MX2022008066A patent/MX2022008066A/es unknown
- 2020-12-27 DK DK20842043.0T patent/DK4081521T3/da active
- 2020-12-27 FI FIEP20842043.0T patent/FI4081521T3/fi active
- 2020-12-27 LT LTEPPCT/IB2020/062462T patent/LT4081521T/lt unknown
- 2020-12-27 US US17/789,293 patent/US20230119316A1/en active Pending
- 2020-12-27 EP EP20842043.0A patent/EP4081521B1/en active Active
- 2020-12-27 MA MA58181A patent/MA58181B1/fr unknown
- 2020-12-27 CN CN202080097766.XA patent/CN115605476B/zh active Active
- 2020-12-27 RS RS20260291A patent/RS67848B1/sr unknown
- 2020-12-27 CA CA3165864A patent/CA3165864A1/en active Pending
- 2020-12-27 BR BR112022012641A patent/BR112022012641A2/pt unknown
- 2020-12-27 HR HRP20260329TT patent/HRP20260329T1/hr unknown
- 2020-12-27 PE PE2022001331A patent/PE20221283A1/es unknown
- 2020-12-27 PH PH1/2022/551585A patent/PH12022551585A1/en unknown
- 2020-12-27 PT PT208420430T patent/PT4081521T/pt unknown
- 2020-12-27 GE GEAP202016015A patent/GEP20247653B/en unknown
- 2020-12-27 CR CR20220363A patent/CR20220363A/es unknown
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2022
- 2022-06-22 IL IL294198A patent/IL294198B1/en unknown
- 2022-06-23 CL CL2022001739A patent/CL2022001739A1/es unknown
- 2022-06-27 SA SA522433155A patent/SA522433155B1/ar unknown
- 2022-07-12 ZA ZA2022/07722A patent/ZA202207722B/en unknown
- 2022-07-26 CO CONC2022/0010460A patent/CO2022010460A2/es unknown
- 2022-07-26 EC ECSENADI202258816A patent/ECSP22058816A/es unknown
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|---|---|
| FI4081521T3 (fi) | 2026-03-11 |
| DK4081521T3 (da) | 2026-03-09 |
| JP7642647B2 (ja) | 2025-03-10 |
| KR20220132543A (ko) | 2022-09-30 |
| AU2020412429A1 (en) | 2022-08-18 |
| PE20221283A1 (es) | 2022-09-05 |
| JP2023514019A (ja) | 2023-04-05 |
| CN115605476B (zh) | 2024-05-24 |
| US20230119316A1 (en) | 2023-04-20 |
| GEAP202416015A (en) | 2024-04-10 |
| BR112022012641A2 (pt) | 2022-09-06 |
| EP4081521A1 (en) | 2022-11-02 |
| CR20220363A (es) | 2022-09-23 |
| ZA202207722B (en) | 2023-03-29 |
| ECSP22058816A (es) | 2022-08-31 |
| MX2022008066A (es) | 2022-08-15 |
| IL294198A (en) | 2022-08-01 |
| CL2022001739A1 (es) | 2023-03-31 |
| IL294198B1 (en) | 2026-03-01 |
| PH12022551585A1 (en) | 2023-11-29 |
| RS67848B1 (sr) | 2026-03-31 |
| PT4081521T (pt) | 2026-03-31 |
| WO2021130731A1 (en) | 2021-07-01 |
| AU2020412429B2 (en) | 2025-12-04 |
| HRP20260329T1 (hr) | 2026-04-10 |
| CO2022010460A2 (es) | 2022-08-09 |
| GEP20247653B (en) | 2024-08-12 |
| MA58181B1 (fr) | 2026-03-31 |
| CA3165864A1 (en) | 2021-07-01 |
| CN115605476A (zh) | 2023-01-13 |
| EP4081521B1 (en) | 2025-12-10 |
| LT4081521T (lt) | 2026-03-25 |
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