CU24698B1 - Inhibidores tricíclicos de kars dependientes de akr1c3 - Google Patents
Inhibidores tricíclicos de kars dependientes de akr1c3Info
- Publication number
- CU24698B1 CU24698B1 CU2022000005A CU20220005A CU24698B1 CU 24698 B1 CU24698 B1 CU 24698B1 CU 2022000005 A CU2022000005 A CU 2022000005A CU 20220005 A CU20220005 A CU 20220005A CU 24698 B1 CU24698 B1 CU 24698B1
- Authority
- CU
- Cuba
- Prior art keywords
- akr1c3
- kars
- inhibitors
- dependent
- tricyclic
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 102000004602 Aldo-Keto Reductase Family 1 Member C3 Human genes 0.000 abstract 3
- 108010065942 Prostaglandin-F synthase Proteins 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 101000588302 Homo sapiens Nuclear factor erythroid 2-related factor 2 Proteins 0.000 abstract 1
- 102000004034 Kelch-Like ECH-Associated Protein 1 Human genes 0.000 abstract 1
- 108090000484 Kelch-Like ECH-Associated Protein 1 Proteins 0.000 abstract 1
- 102000003960 Ligases Human genes 0.000 abstract 1
- 108090000364 Ligases Proteins 0.000 abstract 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 abstract 1
- 239000004472 Lysine Substances 0.000 abstract 1
- ACFIXJIJDZMPPO-NNYOXOHSSA-N NADPH Chemical compound C1=CCC(C(=O)N)=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OC[C@@H]2[C@H]([C@@H](OP(O)(O)=O)[C@@H](O2)N2C3=NC=NC(N)=C3N=C2)O)O1 ACFIXJIJDZMPPO-NNYOXOHSSA-N 0.000 abstract 1
- 102100031701 Nuclear factor erythroid 2-related factor 2 Human genes 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000004077 genetic alteration Effects 0.000 abstract 1
- 231100000118 genetic alteration Toxicity 0.000 abstract 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- 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
- 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
- C07D471/10—Spiro-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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4747—Quinolines; Isoquinolines spiro-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Molecular Biology (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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
<p>La presente invención se refiere a nuevos compuestos tricíclicos de fórmula I, que son inhibidores de KARS dependientes de AKR1C3 que se convierten en inhibidores de lisina ARN-t sintetasa (KARS) por AKR1 C3 en presencia de NADPH. Los nuevos compuestos son útiles para nuevos tratamientos y terapias para pacientes que padecen canceres con alteraciones genéticas en la vía NRF2/KEAP1 o los canceres con alta expresión de AKR1C3.</p>
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962881619P | 2019-08-01 | 2019-08-01 | |
| US202063009513P | 2020-04-14 | 2020-04-14 | |
| US202063033932P | 2020-06-03 | 2020-06-03 | |
| PCT/IB2020/057285 WO2021005586A1 (en) | 2019-08-01 | 2020-07-31 | Tricyclic akr1c3 dependent kars inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CU20220005A7 CU20220005A7 (es) | 2022-09-08 |
| CU24698B1 true CU24698B1 (es) | 2024-03-05 |
Family
ID=71994691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU2022000005A CU24698B1 (es) | 2019-08-01 | 2020-07-31 | Inhibidores tricíclicos de kars dependientes de akr1c3 |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US11970497B2 (es) |
| EP (2) | EP4013500B1 (es) |
| JP (1) | JP7008161B2 (es) |
| KR (1) | KR102735388B1 (es) |
| CN (1) | CN114206870B (es) |
| AU (1) | AU2020309846B2 (es) |
| BR (1) | BR112022001308A2 (es) |
| CA (1) | CA3139940A1 (es) |
| CL (1) | CL2022000201A1 (es) |
| CO (1) | CO2022000370A2 (es) |
| CR (1) | CR20220031A (es) |
| CU (1) | CU24698B1 (es) |
| DK (1) | DK4013500T3 (es) |
| DO (1) | DOP2022000010A (es) |
| EC (1) | ECSP22005621A (es) |
| ES (1) | ES2969591T3 (es) |
| FI (1) | FI4013500T3 (es) |
| HR (1) | HRP20231734T1 (es) |
| HU (1) | HUE064882T2 (es) |
| IL (1) | IL287792B2 (es) |
| JO (1) | JOP20220020B1 (es) |
| LT (1) | LT4013500T (es) |
| MA (1) | MA71308A (es) |
| MX (1) | MX2022000961A (es) |
| MY (1) | MY206964A (es) |
| PE (1) | PE20220343A1 (es) |
| PH (1) | PH12022550200A1 (es) |
| PL (1) | PL4013500T3 (es) |
| PT (1) | PT4013500T (es) |
| PY (1) | PY2039449A (es) |
| RS (1) | RS65068B1 (es) |
| SA (1) | SA522431533B1 (es) |
| SI (1) | SI4013500T1 (es) |
| TW (1) | TWI864063B (es) |
| UY (1) | UY38806A (es) |
| WO (1) | WO2021005586A1 (es) |
| ZA (1) | ZA202108632B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH12021552839A1 (en) | 2019-06-14 | 2022-10-03 | Janssen Pharmaceutica Nv | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
| JP2022536773A (ja) | 2019-06-14 | 2022-08-18 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピラゾロピラジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用 |
| UY38806A (es) * | 2019-08-01 | 2021-02-26 | Novartis Ag | Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos |
| TWI915409B (zh) | 2020-09-02 | 2026-02-21 | 大陸商深圳艾欣達偉醫藥科技有限公司 | 一種akr1c3檢測方法、檢測akr1c3的診斷試劑盒及其用途 |
| CN113135878A (zh) * | 2021-04-09 | 2021-07-20 | 新沂市凯美斯特医药科技有限公司 | 一种以呋喃为原料合成3-氨基甲基四氢呋喃的方法 |
| LT4334289T (lt) * | 2021-05-07 | 2025-09-25 | Organon R&D Finland Oy | Nauji heterocikliniai junginiai, kompozicijos, jų gamybos būdai ir naudojimo būdai |
| CN115403579A (zh) * | 2021-05-27 | 2022-11-29 | 上海拓界生物医药科技有限公司 | 一种新的螺环衍生物及其用途 |
| WO2023174319A1 (zh) | 2022-03-15 | 2023-09-21 | 深圳艾欣达伟医药科技有限公司 | 治疗brca突变癌症患者的方法 |
| WO2023237080A1 (zh) | 2022-06-10 | 2023-12-14 | 深圳艾欣达伟医药科技有限公司 | Akr1c3酶激活前药治疗癌症患者的方法 |
| EP4561702A1 (en) | 2022-07-26 | 2025-06-04 | Novartis AG | Methods of tricyclic akr1c3 dependent kars inhibitor dosing field of the invention |
| KR20250040690A (ko) | 2022-07-26 | 2025-03-24 | 노파르티스 아게 | 삼환식 akr1c3 의존성 kars 억제제의 제약 조성물 및 이의 제조 방법 |
| WO2024023666A1 (en) | 2022-07-26 | 2024-02-01 | Novartis Ag | Crystalline forms of an akr1c3 dependent kars inhibitor |
| KR20260020475A (ko) | 2023-06-06 | 2026-02-11 | 아센타위츠 파마슈티컬즈 리미티드 | Akr1c3 효소 발현 수준과 kras 돌연변이의 상관관계 및 의학적 용도 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6476019B1 (en) * | 1999-08-13 | 2002-11-05 | Sepracor Inc. | Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof |
| WO2006023821A2 (en) * | 2004-08-20 | 2006-03-02 | The Trustees Of Columbia University In The City Of New York | Ligands for aldoketoreductases |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| UY33779A (es) * | 2010-12-10 | 2012-07-31 | Boehringer Ingelheim Int | ?2-(fenilamino)-1H-bencimidazol-5-carboxamidas novedosas? |
| US9346803B2 (en) | 2011-10-17 | 2016-05-24 | Vanderbilt University | Indomethacin analogs for the treatment of castrate-resistant prostate cancer |
| JP6704421B2 (ja) | 2015-03-10 | 2020-06-03 | アセンタウィッツ ファーマシューティカルズ リミテッド | Ｄｎａアルキル化剤 |
| US10167293B2 (en) * | 2016-05-26 | 2019-01-01 | Bayer Pharma Aktiengesellschaft | [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones |
| JP2022514253A (ja) * | 2018-12-18 | 2022-02-10 | ノバルティス アーゲー | Ｎ－（ピリジン－２－イルスルホニル）シクロプロパンカルボキサミド誘導体及びｃｆｔｒ媒介疾患の処置におけるその使用 |
| UY38806A (es) | 2019-08-01 | 2021-02-26 | Novartis Ag | Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos |
-
2020
- 2020-07-27 UY UY0001038806A patent/UY38806A/es not_active Application Discontinuation
- 2020-07-27 PY PY202002039449A patent/PY2039449A/es unknown
- 2020-07-30 TW TW109125732A patent/TWI864063B/zh active
- 2020-07-31 CR CR20220031A patent/CR20220031A/es unknown
- 2020-07-31 MX MX2022000961A patent/MX2022000961A/es unknown
- 2020-07-31 HR HRP20231734TT patent/HRP20231734T1/hr unknown
- 2020-07-31 MA MA71308A patent/MA71308A/fr unknown
- 2020-07-31 BR BR112022001308A patent/BR112022001308A2/pt unknown
- 2020-07-31 WO PCT/IB2020/057285 patent/WO2021005586A1/en not_active Ceased
- 2020-07-31 DK DK20753456.1T patent/DK4013500T3/da active
- 2020-07-31 HU HUE20753456A patent/HUE064882T2/hu unknown
- 2020-07-31 CU CU2022000005A patent/CU24698B1/es unknown
- 2020-07-31 JP JP2021507653A patent/JP7008161B2/ja active Active
- 2020-07-31 SI SI202030346T patent/SI4013500T1/sl unknown
- 2020-07-31 EP EP20753456.1A patent/EP4013500B1/en active Active
- 2020-07-31 US US16/973,836 patent/US11970497B2/en active Active
- 2020-07-31 PL PL20753456.1T patent/PL4013500T3/pl unknown
- 2020-07-31 KR KR1020227002658A patent/KR102735388B1/ko active Active
- 2020-07-31 CA CA3139940A patent/CA3139940A1/en active Pending
- 2020-07-31 AU AU2020309846A patent/AU2020309846B2/en active Active
- 2020-07-31 PE PE2022000125A patent/PE20220343A1/es unknown
- 2020-07-31 CN CN202080053804.1A patent/CN114206870B/zh active Active
- 2020-07-31 PT PT207534561T patent/PT4013500T/pt unknown
- 2020-07-31 FI FIEP20753456.1T patent/FI4013500T3/fi active
- 2020-07-31 ES ES20753456T patent/ES2969591T3/es active Active
- 2020-07-31 EP EP23195635.0A patent/EP4349839A3/en active Pending
- 2020-07-31 MY MYPI2021006666A patent/MY206964A/en unknown
- 2020-07-31 RS RS20240042A patent/RS65068B1/sr unknown
- 2020-07-31 IL IL287792A patent/IL287792B2/en unknown
- 2020-07-31 LT LTEPPCT/IB2020/057285T patent/LT4013500T/lt unknown
- 2020-07-31 PH PH1/2022/550200A patent/PH12022550200A1/en unknown
-
2021
- 2021-11-04 ZA ZA2021/08632A patent/ZA202108632B/en unknown
-
2022
- 2022-01-18 CO CONC2022/0000370A patent/CO2022000370A2/es unknown
- 2022-01-20 DO DO2022000010A patent/DOP2022000010A/es unknown
- 2022-01-24 EC ECSENADI20225621A patent/ECSP22005621A/es unknown
- 2022-01-25 CL CL2022000201A patent/CL2022000201A1/es unknown
- 2022-01-25 JO JOJO/P/2022/0020A patent/JOP20220020B1/ar active
- 2022-01-29 SA SA522431533A patent/SA522431533B1/ar unknown
-
2024
- 2024-03-04 US US18/594,323 patent/US20240262827A1/en not_active Abandoned
-
2025
- 2025-01-31 US US19/042,086 patent/US20250179072A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX2021002804A (es) | Terapias de combinacion. | |
| MX2024008551A (es) | Terapias de combinacion. | |
| CL2018002703A1 (es) | Agentes de iarn, composiciones y métodos de uso de los mismos para tratar enfermedades asociadas con transtiretina (ttr). (divisional solicitud 201401291) | |
| CL2020002082A1 (es) | Inhibidores pd-1/pd-l1. | |
| PE20210452A1 (es) | Inhibidores de la arginasa | |
| PY2020118A (es) | Conjugados de anticuerpo-fármaco inhibidores de mcl-1 y sus métodos de uso | |
| CO2019011543A2 (es) | Inhibidores de pd-1/pd-l1 | |
| CO2022001210A2 (es) | Conjugados de il-2 y métodos de uso para tratar enfermedades autoinmunes | |
| CO2019005992A2 (es) | Composiciones de arni de serpina1 y sus métodos de uso | |
| MX2022007968A (es) | Dosificacion de gamma-hidroxibutirato (ghb). | |
| PE20200733A1 (es) | Inhibidores de kras g 12c y metodos para su uso | |
| BR112021024978A2 (pt) | Composições engajadoras específicas para macrófagos e métodos de uso das mesmas | |
| AR107529A1 (es) | Compuestos, composiciones y métodos para la estratificación de pacientes de cáncer y su tratamiento | |
| UY37800A (es) | AGENTES DE iARN PARA LA INHIBICIÓN DE LA EXPRESIÓN DE ALFA-ENaC Y MÉTODOS DE USO | |
| BR112017017700A2 (pt) | métodos, composições e kits para tratamento do câncer | |
| CR20170217A (es) | Composiciones anticancerígenas | |
| MX2020003594A (es) | Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd. | |
| CR20170216A (es) | Composiciones anticancerígenas | |
| CR20170218A (es) | Composiciones anticancerígenas | |
| CU20220005A7 (es) | Inhibidores tricíclicos de kars dependientes de akr1c3 | |
| BR112015026021A2 (pt) | terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer | |
| CL2023002223A1 (es) | Inhibidores de cdk2 y métodos de uso de los mismos | |
| BR112022009290A2 (pt) | Terapia para malignidades de células hematopoiéticas com o uso de células t geneticamente modificadas visando cd70 | |
| CR20220280A (es) | Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2 | |
| CL2020003380A1 (es) | Compuestos que aumentan la actividad del proteosoma. |