PE20212303A1 - Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancer - Google Patents
Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancerInfo
- Publication number
- PE20212303A1 PE20212303A1 PE2021001090A PE2021001090A PE20212303A1 PE 20212303 A1 PE20212303 A1 PE 20212303A1 PE 2021001090 A PE2021001090 A PE 2021001090A PE 2021001090 A PE2021001090 A PE 2021001090A PE 20212303 A1 PE20212303 A1 PE 20212303A1
- Authority
- PE
- Peru
- Prior art keywords
- aza
- methods
- alkyl
- group
- cancer
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 201000011510 cancer Diseases 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 101000947881 Homo sapiens S-adenosylmethionine synthase isoform type-2 Proteins 0.000 title 1
- 102100035947 S-adenosylmethionine synthase isoform type-2 Human genes 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 108010034457 5'-methylthioadenosine phosphorylase Proteins 0.000 abstract 2
- 102000007357 Methionine adenosyltransferase Human genes 0.000 abstract 2
- 108010007784 Methionine adenosyltransferase Proteins 0.000 abstract 2
- 102100034187 S-methyl-5'-thioadenosine phosphorylase Human genes 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 206010027406 Mesothelioma Diseases 0.000 abstract 1
- 206010029260 Neuroblastoma Diseases 0.000 abstract 1
- 108010029485 Protein Isoforms Proteins 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 238000012217 deletion Methods 0.000 abstract 1
- 230000037430 deletion Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
-
- 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
-
- 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
- A61K31/395—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms
-
- 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
- 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
- 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
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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Referido a un compuesto de formula I, en donde X1 es N o CR5; X2 es N o CR6, en donde X1 y X2 no son simultaneamente N; L es O, S, NR, o un enlace; R es H o alquilo C1-C6; R1 se selecciona del grupo que consiste en alquilo C1-C6, alquenilo C2-C6, entre otros; R2 y R3 se seleccionan independientemente del grupo que consiste en arilo C6-C10, carbociclilo C3-C6, entre otros; R4 se selecciona del grupo que consiste en H, alquilo C1-C6, alcoxi C1-C6, entre otros; o una sal farmaceuticamente aceptable de este. Estos compuestos son aza-heterobiciclicos inhibidores de la isoforma 2A de la metionina adenosiltransferasa (MAT2A). Tambien se refiere a composiciones farmaceuticas y metodos para tratar el cancer, que incluyen algunos canceres con eliminacion del gen que codifica la metiltioadenosina fosforilasa (MTAP), tal como mesotelioma, neuroblastoma, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862785574P | 2018-12-27 | 2018-12-27 | |
| PCT/US2019/068653 WO2020139992A1 (en) | 2018-12-27 | 2019-12-27 | Aza-heterobicyclic inhibitors of mat2a and methods of use for treating cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20212303A1 true PE20212303A1 (es) | 2021-12-10 |
Family
ID=69400626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001090A PE20212303A1 (es) | 2018-12-27 | 2019-12-27 | Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancer |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20220098203A1 (es) |
| EP (1) | EP3902804A1 (es) |
| JP (1) | JP2022516882A (es) |
| KR (1) | KR20220050832A (es) |
| CN (1) | CN113474347A (es) |
| AR (1) | AR115296A1 (es) |
| AU (1) | AU2019414446A1 (es) |
| BR (1) | BR112021012599A2 (es) |
| CA (1) | CA3124678A1 (es) |
| CL (1) | CL2021001722A1 (es) |
| CO (1) | CO2021009882A2 (es) |
| CR (1) | CR20210409A (es) |
| EA (1) | EA202191800A1 (es) |
| IL (1) | IL284324A (es) |
| JO (1) | JOP20210171A1 (es) |
| MA (1) | MA54609A (es) |
| MX (1) | MX2021007833A (es) |
| PE (1) | PE20212303A1 (es) |
| PH (1) | PH12021551493A1 (es) |
| SG (1) | SG11202106627WA (es) |
| TW (1) | TW202039489A (es) |
| WO (1) | WO2020139992A1 (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2019395338B2 (en) | 2018-12-10 | 2025-11-13 | Ideaya Biosciences, Inc. | 2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors |
| US12077534B2 (en) * | 2018-12-27 | 2024-09-03 | Les Laboratoires Servier | Aza-heterobicyclic inhibitors of MAT2A and methods of use for treating cancer |
| WO2021219731A2 (en) * | 2020-04-28 | 2021-11-04 | Iomx Therapeutics Ag | Bicyclic kinase inhibitors and uses thereof |
| BR112022026105A2 (pt) * | 2020-06-22 | 2023-01-17 | Hoffmann La Roche | Compostos, composições farmacêuticas, método para o tratamento ou prevenção de adenocarcinoma pulmonar, uso de compostos e invenção |
| WO2021259815A1 (en) * | 2020-06-22 | 2021-12-30 | F. Hoffmann-La Roche Ag | Amidopyrimidone derivatives |
| WO2022052924A1 (zh) * | 2020-09-11 | 2022-03-17 | 上海凌达生物医药有限公司 | 一类含氮稠环类化合物的制备方法和用途 |
| US20240124454A1 (en) * | 2020-12-31 | 2024-04-18 | Nanjing Zaiming Pharmaceutical Co., Ltd. | Tricyclic compound and use thereof |
| CN115141202A (zh) * | 2021-03-29 | 2022-10-04 | 武汉人福创新药物研发中心有限公司 | 嘧啶并吡嗪酮化合物及其用途 |
| KR20240089791A (ko) | 2021-10-20 | 2024-06-20 | 인실리코 메디신 아이피 리미티드 | 메티오닌 아데노실트랜스퍼라제 2a (mat2a) 억제제 및 그의 용도 |
| CN118414338A (zh) * | 2021-12-21 | 2024-07-30 | 南京正大天晴制药有限公司 | 蛋氨酸腺苷转移酶2a的杂环抑制剂 |
| TW202333696A (zh) * | 2022-01-26 | 2023-09-01 | 大陸商勤浩醫藥(蘇州)有限公司 | 用於治療ｍｔａｐ缺失型癌症的甲硫氨酸腺苷轉移酶２ａ抑制劑 |
| CN118742550B (zh) * | 2022-03-11 | 2025-09-05 | 赛诺哈勃药业（成都）有限公司 | 甲硫氨酸腺苷转移酶抑制剂、其制备方法及应用 |
| GB202204913D0 (en) | 2022-04-04 | 2022-05-18 | Cambridge Entpr Ltd | antiviral therapy |
| KR20250016234A (ko) | 2022-06-27 | 2025-02-03 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | 삼환 화합물 및 이의 용도 |
| WO2024080788A1 (ko) | 2022-10-13 | 2024-04-18 | 한미약품 주식회사 | 신규한 트리사이클 유도체 화합물 및 이의 용도 |
| WO2024183778A1 (zh) * | 2023-03-06 | 2024-09-12 | 甘李药业股份有限公司 | 一种甲硫氨酸腺苷转移酶2a抑制剂及其医药用途 |
| WO2024255805A1 (zh) * | 2023-06-14 | 2024-12-19 | 南京正大天晴制药有限公司 | 蛋氨酸腺苷转移酶2a杂环抑制剂的晶型、其制备方法及用途 |
| WO2025000265A1 (en) * | 2023-06-28 | 2025-01-02 | Silexon Ai Technology Co., Ltd. | Heterocyclic compounds usefull as sos1 inhibitor |
| WO2025166229A1 (en) | 2024-02-02 | 2025-08-07 | Ideaya Biosciences, Inc. | Tricyclic amidino compounds as prmt5 inhibitors |
| WO2025166274A1 (en) | 2024-02-02 | 2025-08-07 | Ideaya Biosciences, Inc. | Tricyclic guanidino compounds as prmt5 inhibitors |
| WO2025166257A1 (en) | 2024-02-02 | 2025-08-07 | Ideaya Biosciences, Inc. | Amide substituted triheterocyclic guanidino compounds as prmt5 inhibitors |
| WO2025166260A1 (en) | 2024-02-02 | 2025-08-07 | Ideaya Biosciences, Inc. | Amide substituted tricyclic guanidino compounds as prmt5 inhibitors |
| WO2025166215A1 (en) | 2024-02-02 | 2025-08-07 | Ideaya Biosciences, Inc. | Triheterocyclic guanidino compounds as prmt5 inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6576420B1 (en) | 1998-06-23 | 2003-06-10 | Regents Of The University Of California | Method for early diagnosis of, and determination of prognosis in, cancer |
| WO2000024744A1 (en) * | 1998-10-23 | 2000-05-04 | F. Hoffmann-La Roche Ag | Bicyclic nitrogen heterocycles |
| CA2388142C (en) * | 1999-10-21 | 2008-12-09 | F. Hoffmann-La Roche Ag | Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase |
| PA8577501A1 (es) * | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
| US7084270B2 (en) * | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| US7129351B2 (en) * | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| WO2004089955A1 (en) * | 2003-04-10 | 2004-10-21 | F.Hoffmann-La Roche Ag | Pyrimido compounds |
| US7897762B2 (en) * | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US8367706B2 (en) | 2007-06-20 | 2013-02-05 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| CN104418860B (zh) * | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| MX390277B (es) * | 2016-08-31 | 2025-03-20 | Servier Lab | Inhibidores de procesos metabolicos celulares. |
| WO2019029541A1 (zh) * | 2017-08-08 | 2019-02-14 | 南京药捷安康生物科技有限公司 | 成纤维细胞生长因子受体抑制剂及其用途 |
| JP7350005B2 (ja) * | 2018-03-30 | 2023-09-25 | レ ラボラトワール セルヴィエ | Ｍａｔ２ａの複素二環式阻害剤、およびがんの治療のための使用方法 |
-
2019
- 2019-12-27 PH PH1/2021/551493A patent/PH12021551493A1/en unknown
- 2019-12-27 CR CR20210409A patent/CR20210409A/es unknown
- 2019-12-27 EA EA202191800A patent/EA202191800A1/ru unknown
- 2019-12-27 BR BR112021012599-0A patent/BR112021012599A2/pt not_active Application Discontinuation
- 2019-12-27 EP EP19845797.0A patent/EP3902804A1/en not_active Withdrawn
- 2019-12-27 TW TW108148080A patent/TW202039489A/zh unknown
- 2019-12-27 MA MA054609A patent/MA54609A/fr unknown
- 2019-12-27 US US17/418,406 patent/US20220098203A1/en not_active Abandoned
- 2019-12-27 PE PE2021001090A patent/PE20212303A1/es unknown
- 2019-12-27 KR KR1020217023830A patent/KR20220050832A/ko not_active Withdrawn
- 2019-12-27 WO PCT/US2019/068653 patent/WO2020139992A1/en not_active Ceased
- 2019-12-27 AR ARP190103901A patent/AR115296A1/es not_active Application Discontinuation
- 2019-12-27 JO JOP/2021/0171A patent/JOP20210171A1/ar unknown
- 2019-12-27 MX MX2021007833A patent/MX2021007833A/es unknown
- 2019-12-27 JP JP2021538125A patent/JP2022516882A/ja active Pending
- 2019-12-27 CA CA3124678A patent/CA3124678A1/en active Pending
- 2019-12-27 CN CN201980092839.3A patent/CN113474347A/zh active Pending
- 2019-12-27 AU AU2019414446A patent/AU2019414446A1/en not_active Abandoned
- 2019-12-27 SG SG11202106627WA patent/SG11202106627WA/en unknown
-
2021
- 2021-06-23 IL IL284324A patent/IL284324A/en unknown
- 2021-06-25 CL CL2021001722A patent/CL2021001722A1/es unknown
- 2021-07-27 CO CONC2021/0009882A patent/CO2021009882A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112021012599A2 (pt) | 2021-09-08 |
| AR115296A1 (es) | 2020-12-16 |
| SG11202106627WA (en) | 2021-07-29 |
| US20220098203A1 (en) | 2022-03-31 |
| CR20210409A (es) | 2022-01-24 |
| PH12021551493A1 (en) | 2022-04-11 |
| MA54609A (fr) | 2022-04-06 |
| JOP20210171A1 (ar) | 2023-01-30 |
| EP3902804A1 (en) | 2021-11-03 |
| TW202039489A (zh) | 2020-11-01 |
| IL284324A (en) | 2021-08-31 |
| EA202191800A1 (ru) | 2021-09-13 |
| CO2021009882A2 (es) | 2021-10-29 |
| CN113474347A (zh) | 2021-10-01 |
| CA3124678A1 (en) | 2020-07-02 |
| AU2019414446A1 (en) | 2021-07-15 |
| JP2022516882A (ja) | 2022-03-03 |
| KR20220050832A (ko) | 2022-04-25 |
| WO2020139992A1 (en) | 2020-07-02 |
| MX2021007833A (es) | 2021-10-26 |
| CL2021001722A1 (es) | 2022-02-18 |
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