JOP20220020A1 - مثبطات kars تعتمد على akr1c3 ثلاثية الحلقة - Google Patents
مثبطات kars تعتمد على akr1c3 ثلاثية الحلقةInfo
- Publication number
- JOP20220020A1 JOP20220020A1 JOP/2022/0020A JOP20220020A JOP20220020A1 JO P20220020 A1 JOP20220020 A1 JO P20220020A1 JO P20220020 A JOP20220020 A JO P20220020A JO P20220020 A1 JOP20220020 A1 JO P20220020A1
- Authority
- JO
- Jordan
- Prior art keywords
- kars
- tricyclic
- inhibitors
- akr1c3
- dependent
- Prior art date
Links
- 230000001419 dependent effect Effects 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 102000004602 Aldo-Keto Reductase Family 1 Member C3 Human genes 0.000 abstract 2
- 108091007984 KARS Proteins 0.000 abstract 2
- 102100035529 Lysine-tRNA ligase Human genes 0.000 abstract 2
- 108010065942 Prostaglandin-F synthase Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- C07D471/02—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
-
- 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
-
- 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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Biochemistry (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)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
يتعلق الاختراع الحالي بمركبات ثلاثية الحلقة جديدة تكون عبارة عن مثبط KARS معتمد على AKR1C3، وعمليات لتحضيرها، وتركيبات صيدلانية، وأدوية تحتوي عليها، واستخدامها في الأمراض واضطرابات ناتجة عن مثبط KARS معتمد على AKR1C3.
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 (1)
Publication Number | Publication Date |
---|---|
JOP20220020A1 true JOP20220020A1 (ar) | 2023-01-30 |
Family
ID=71994691
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JOP/2022/0020A JOP20220020A1 (ar) | 2019-08-01 | 2020-07-31 | مثبطات kars تعتمد على akr1c3 ثلاثية الحلقة |
Country Status (31)
Country | Link |
---|---|
US (1) | US11970497B2 (ar) |
EP (2) | EP4349839A2 (ar) |
JP (1) | JP7008161B2 (ar) |
KR (1) | KR20220025845A (ar) |
CN (1) | CN114206870A (ar) |
AU (1) | AU2020309846B2 (ar) |
BR (1) | BR112022001308A2 (ar) |
CA (1) | CA3139940A1 (ar) |
CL (1) | CL2022000201A1 (ar) |
CO (1) | CO2022000370A2 (ar) |
CR (1) | CR20220031A (ar) |
CU (1) | CU24698B1 (ar) |
DK (1) | DK4013500T3 (ar) |
DO (1) | DOP2022000010A (ar) |
EC (1) | ECSP22005621A (ar) |
ES (1) | ES2969591T3 (ar) |
FI (1) | FI4013500T3 (ar) |
HR (1) | HRP20231734T1 (ar) |
HU (1) | HUE064882T2 (ar) |
IL (1) | IL287792A (ar) |
JO (1) | JOP20220020A1 (ar) |
LT (1) | LT4013500T (ar) |
MX (1) | MX2022000961A (ar) |
PE (1) | PE20220343A1 (ar) |
PL (1) | PL4013500T3 (ar) |
PT (1) | PT4013500T (ar) |
RS (1) | RS65068B1 (ar) |
SI (1) | SI4013500T1 (ar) |
TW (1) | TW202120507A (ar) |
UY (1) | UY38806A (ar) |
WO (1) | WO2021005586A1 (ar) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20220024403A (ko) | 2019-06-14 | 2022-03-03 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로-피라진 및 이들의 glun2b 수용체 조절제로서의 용도 |
UY38806A (es) | 2019-08-01 | 2021-02-26 | Novartis Ag | Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos |
JP2023540283A (ja) | 2020-09-02 | 2023-09-22 | 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 | Akr1c3検出方法、並びにakr1c3検出用診断キットおよびその使用 |
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 |
BR112023022664A2 (pt) * | 2021-05-07 | 2024-01-16 | Organon R&D Finland Ltd | Compostos heterocíclicos inovadores, composições, métodos de preparação e usos dos mesmos |
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 |
WO2024023659A1 (en) | 2022-07-26 | 2024-02-01 | Novartis Ag | Pharmaceutical compositions of tricyclic akr1c3 dependent kars inhibitor and methods for making same |
WO2024023666A1 (en) | 2022-07-26 | 2024-02-01 | Novartis Ag | Crystalline forms of an akr1c3 dependent kars inhibitor |
WO2024023641A1 (en) | 2022-07-26 | 2024-02-01 | Novartis Ag | Methods of tricyclic akr1c3 dependent kars inhibitor dosing field of the invention |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20100048604A1 (en) * | 2004-08-20 | 2010-02-25 | Yee Dominic J | 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 |
US9346803B2 (en) | 2011-10-17 | 2016-05-24 | Vanderbilt University | Indomethacin analogs for the treatment of castrate-resistant prostate cancer |
KR102189066B1 (ko) | 2015-03-10 | 2020-12-09 | 아센타위츠 파마슈티컬즈 리미티드 | Dna 알킬화제 |
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 |
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 unknown
- 2020-07-30 TW TW109125732A patent/TW202120507A/zh unknown
- 2020-07-31 EP EP23195635.0A patent/EP4349839A2/en active Pending
- 2020-07-31 DK DK20753456.1T patent/DK4013500T3/da active
- 2020-07-31 WO PCT/IB2020/057285 patent/WO2021005586A1/en active Application Filing
- 2020-07-31 JP JP2021507653A patent/JP7008161B2/ja active Active
- 2020-07-31 US US16/973,836 patent/US11970497B2/en active Active
- 2020-07-31 EP EP20753456.1A patent/EP4013500B1/en active Active
- 2020-07-31 BR BR112022001308A patent/BR112022001308A2/pt unknown
- 2020-07-31 CN CN202080053804.1A patent/CN114206870A/zh active Pending
- 2020-07-31 HU HUE20753456A patent/HUE064882T2/hu unknown
- 2020-07-31 AU AU2020309846A patent/AU2020309846B2/en active Active
- 2020-07-31 RS RS20240042A patent/RS65068B1/sr unknown
- 2020-07-31 MX MX2022000961A patent/MX2022000961A/es unknown
- 2020-07-31 CU CU2022000005A patent/CU24698B1/es unknown
- 2020-07-31 ES ES20753456T patent/ES2969591T3/es active Active
- 2020-07-31 FI FIEP20753456.1T patent/FI4013500T3/fi active
- 2020-07-31 CA CA3139940A patent/CA3139940A1/en active Pending
- 2020-07-31 PT PT207534561T patent/PT4013500T/pt unknown
- 2020-07-31 PE PE2022000125A patent/PE20220343A1/es unknown
- 2020-07-31 PL PL20753456.1T patent/PL4013500T3/pl unknown
- 2020-07-31 JO JOP/2022/0020A patent/JOP20220020A1/ar unknown
- 2020-07-31 CR CR20220031A patent/CR20220031A/es unknown
- 2020-07-31 LT LTEPPCT/IB2020/057285T patent/LT4013500T/lt unknown
- 2020-07-31 SI SI202030346T patent/SI4013500T1/sl unknown
- 2020-07-31 HR HRP20231734TT patent/HRP20231734T1/hr unknown
- 2020-07-31 KR KR1020227002658A patent/KR20220025845A/ko not_active Application Discontinuation
-
2021
- 2021-11-02 IL IL287792A patent/IL287792A/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
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