PE20221283A1 - Compuestos triciclicos sustituidos - Google Patents
Compuestos triciclicos sustituidosInfo
- Publication number
- PE20221283A1 PE20221283A1 PE2022001331A PE2022001331A PE20221283A1 PE 20221283 A1 PE20221283 A1 PE 20221283A1 PE 2022001331 A PE2022001331 A PE 2022001331A PE 2022001331 A PE2022001331 A PE 2022001331A PE 20221283 A1 PE20221283 A1 PE 20221283A1
- Authority
- PE
- Peru
- Prior art keywords
- substituted
- unsubstituted
- cycloalkyl
- alkyl
- amino
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- 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
-
- 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
- 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
- C07D498/12—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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Referida a un compuesto de formula general (I), donde: el anillo A se selecciona entre arilo, heteroarilo y heterociclilo; el anillo B es un anillo carbociclico de 5 o 6 miembros 10 sustituido o no sustituido y un anillo heterociclico de 5 o 6 miembros sustituido o no sustituido que contiene de 1 a 3 heteroatomos seleccionados independientemente entre S, O y N; R1 es hidrogeno, alquilo sustituido o no sustituido y cicloalquilo sustituido o no sustituido; R2 y R3 son hidrogeno, halogeno, ciano, alquilo sustituido o no sustituido y cicloalquilo sustituido o no sustituido; R4 es halogeno, ciano, entre otros; "n" es un numero entero seleccionado entre 0, 1, 2 y 3; R5 es hidrogeno, alquilo, perhaloalquilo y cicloalquilo; R6 es hidrogeno, alquilo y cicloalquilo; o R6 junto con el nitrogeno al que estan unidos, forman un anillo de heterociclilo; y R7 es alquilo y cicloalquilo. Son compuestos preferidos: (R)-4-((1-(3-amino-5-(trifluorometil)fenil)etil)amino)-2,6-dimetil-6H- [1,4]oxazino[3,2-g]quinazolin-7(8H)-ona; (R)-4-((1-(3-(1,1-difluoro-2-hidroxietil)-2-fluorofenil)etil)amino)-2,6-dimetil6H-[1,4]oxazino[3,2-g]quinazolin-7(8H)-ona; (R)-4-((1-(3-(1,1-difluoro-2-hidroxi-2-metilpropil)-2-fluorofenil)etil)amino)- 2,6-dimetil-6H-[1,4]oxazino[3,2-g]quinazolin-7(8H)-ona; entre otros. Dichos compuestos son inhibidores de SOS1 y son utiles en el tratamiento de enfermedades o trastornos proliferativos, infecciosos y RASopatias.
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 |
|---|---|
| PE20221283A1 true PE20221283A1 (es) | 2022-09-05 |
Family
ID=74184675
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022001331A PE20221283A1 (es) | 2019-12-27 | 2020-12-27 | Compuestos triciclicos sustituidos |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20230119316A1 (es) |
| EP (1) | EP4081521A1 (es) |
| JP (1) | JP2023514019A (es) |
| KR (1) | KR20220132543A (es) |
| CN (1) | CN115605476B (es) |
| AU (1) | AU2020412429A1 (es) |
| BR (1) | BR112022012641A2 (es) |
| CA (1) | CA3165864A1 (es) |
| CL (1) | CL2022001739A1 (es) |
| CO (1) | CO2022010460A2 (es) |
| CR (1) | CR20220363A (es) |
| EC (1) | ECSP22058816A (es) |
| IL (1) | IL294198A (es) |
| MX (1) | MX2022008066A (es) |
| PE (1) | PE20221283A1 (es) |
| WO (1) | WO2021130731A1 (es) |
| ZA (1) | ZA202207722B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220119094A (ko) | 2019-12-19 | 2022-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| BR112022024156A2 (pt) | 2020-05-29 | 2023-02-14 | Boehringer Ingelheim Animal Health Usa Inc | Compostos heterocílicos antelmínticos |
| KR20230067635A (ko) | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | 암의 치료에서 ras 억제제로서 인돌 유도체 |
| CN116568681A (zh) * | 2020-12-07 | 2023-08-08 | 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 |
| JP2024502886A (ja) * | 2021-01-19 | 2024-01-23 | ルピン・リミテッド | がんを処置及び／又は予防するためのｓｏｓ１阻害薬の医薬組合せ |
| 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 |
| CA3213593A1 (en) | 2021-03-31 | 2022-10-06 | Sevenless Therapeutics Limited | Sos1 inhibitors and ras inhibitors for use in the treatment of pain |
| EP4319757A1 (en) | 2021-04-09 | 2024-02-14 | Boehringer Ingelheim International GmbH | Anticancer therapy |
| 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 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN115536660A (zh) * | 2021-11-04 | 2022-12-30 | 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 |
| CN116265462A (zh) * | 2021-12-17 | 2023-06-20 | 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 |
| WO2023114954A1 (en) | 2021-12-17 | 2023-06-22 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| WO2023135260A1 (en) | 2022-01-14 | 2023-07-20 | 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 |
| TW202404581A (zh) | 2022-05-25 | 2024-02-01 | 美商醫肯納腫瘤學公司 | Ｍｅｋ抑制劑及其用途 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
| US5019369A (en) | 1984-10-22 | 1991-05-28 | Vestar, Inc. | Method of targeting tumors in humans |
| US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| CA2148082A1 (en) * | 1993-09-03 | 1995-03-09 | Daisuke Machii | Imidazoquinazoline derivatives |
| TW372967B (en) | 1994-12-27 | 1999-11-01 | Kanebo Ltd | 1,4 benzoxazine derivative, pharmaceutical composition containing the same and use thereof |
| WO2004003152A2 (en) | 2002-06-26 | 2004-01-08 | Chiron Corporation | Sos1 inhibitors |
| WO2008079759A1 (en) | 2006-12-20 | 2008-07-03 | Bristol-Myers Squibb Company | Bicyclic lactam factor viia inhibitors useful as anticoagulants |
| TWI434690B (zh) | 2007-12-19 | 2014-04-21 | Dainippon Sumitomo Pharma Co | 雜雙環衍生物 |
| WO2009106599A2 (en) | 2008-02-29 | 2009-09-03 | Novartis Ag | Substituted piperidines as therapeutic compounds |
| CN102633812B (zh) * | 2012-04-06 | 2014-11-12 | 中国药科大学 | 噁唑酮并喹唑啉衍生物、制备方法及用途 |
| CA2906740A1 (en) | 2013-03-15 | 2014-09-18 | Dana-Farber Cancer Institute, Inc. | Stabilized sos1 peptides |
| DK3674302T3 (da) | 2014-04-23 | 2023-04-03 | Incyte Holdings Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner |
| WO2016077793A1 (en) | 2014-11-14 | 2016-05-19 | Children's Hospital Medical Center | Sos1 inhibitors for cancer treatment |
| JP6959650B2 (ja) * | 2015-08-21 | 2021-11-02 | アルデイラ セラピューティクス， インコーポレイテッド | アルデヒドコンジュゲートおよびその使用 |
| TW201711999A (zh) | 2015-09-03 | 2017-04-01 | 佛瑪治療公司 | ﹝６，６﹞稠合雙環組蛋白脫乙醯基酶８（ｈｄａｃ８）抑制劑 |
| EP3558979B1 (en) * | 2016-12-22 | 2021-02-17 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| US20220235013A1 (en) | 2017-03-21 | 2022-07-28 | Bayer Pharma Aktiengesellschaft | 2-methyl-quinazolines |
| JOP20190221A1 (ar) | 2017-04-05 | 2019-09-23 | Seal Rock Therapeutics Inc | مركبات مثبطات كيناز منظم لإشارات الاستماتة 1 (ask1) واستخداماتها |
| KR20200111163A (ko) | 2017-12-21 | 2020-09-28 | 베링거 인겔하임 인터내셔날 게엠베하 | Sos1 억제제로서의 신규 벤질아미노 치환 피리도피리미디논 및 유도체 |
| EP3781565A1 (en) | 2018-04-18 | 2021-02-24 | Bayer Pharma Aktiengesellschaft | 2-methyl-aza-quinazolines |
| WO2019243823A1 (en) | 2018-06-21 | 2019-12-26 | Curadev Pharma Limited | Azaheterocyclic small molecule modulators of human sting |
| MX2021010319A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos biciclicos de heteroarilo y usos de estos. |
| CA3130083A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
-
2020
- 2020-12-27 JP JP2022539232A patent/JP2023514019A/ja active Pending
- 2020-12-27 MX MX2022008066A patent/MX2022008066A/es unknown
- 2020-12-27 CR CR20220363A patent/CR20220363A/es unknown
- 2020-12-27 AU AU2020412429A patent/AU2020412429A1/en active Pending
- 2020-12-27 BR BR112022012641A patent/BR112022012641A2/pt unknown
- 2020-12-27 PE PE2022001331A patent/PE20221283A1/es unknown
- 2020-12-27 CA CA3165864A patent/CA3165864A1/en active Pending
- 2020-12-27 US US17/789,293 patent/US20230119316A1/en active Pending
- 2020-12-27 IL IL294198A patent/IL294198A/en unknown
- 2020-12-27 CN CN202080097766.XA patent/CN115605476B/zh active Active
- 2020-12-27 KR KR1020227026096A patent/KR20220132543A/ko unknown
- 2020-12-27 EP EP20842043.0A patent/EP4081521A1/en active Pending
- 2020-12-27 WO PCT/IB2020/062462 patent/WO2021130731A1/en active Application Filing
-
2022
- 2022-06-23 CL CL2022001739A patent/CL2022001739A1/es unknown
- 2022-07-12 ZA ZA2022/07722A patent/ZA202207722B/en unknown
- 2022-07-26 EC ECSENADI202258816A patent/ECSP22058816A/es unknown
- 2022-07-26 CO CONC2022/0010460A patent/CO2022010460A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4081521A1 (en) | 2022-11-02 |
| JP2023514019A (ja) | 2023-04-05 |
| US20230119316A1 (en) | 2023-04-20 |
| ECSP22058816A (es) | 2022-08-31 |
| IL294198A (en) | 2022-08-01 |
| KR20220132543A (ko) | 2022-09-30 |
| WO2021130731A1 (en) | 2021-07-01 |
| BR112022012641A2 (pt) | 2022-09-06 |
| CR20220363A (es) | 2022-09-23 |
| CN115605476A (zh) | 2023-01-13 |
| CO2022010460A2 (es) | 2022-08-09 |
| CA3165864A1 (en) | 2021-07-01 |
| ZA202207722B (en) | 2023-03-29 |
| CL2022001739A1 (es) | 2023-03-31 |
| MX2022008066A (es) | 2022-08-15 |
| CN115605476B (zh) | 2024-05-24 |
| AU2020412429A1 (en) | 2022-08-18 |
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