HRP20200666T1 - Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze - Google Patents
Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze Download PDFInfo
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- HRP20200666T1 HRP20200666T1 HRP20200666TT HRP20200666T HRP20200666T1 HR P20200666 T1 HRP20200666 T1 HR P20200666T1 HR P20200666T T HRP20200666T T HR P20200666TT HR P20200666 T HRP20200666 T HR P20200666T HR P20200666 T1 HRP20200666 T1 HR P20200666T1
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- ASHZGMCLOXNDFT-UHFFFAOYSA-N 1H-pyridin-2-one 1H-quinolin-2-one Chemical class O=C1C=CC=CN1.C1=CC=C2NC(=O)C=CC2=C1 ASHZGMCLOXNDFT-UHFFFAOYSA-N 0.000 title 1
- 101710088194 Dehydrogenase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 2
- 238000004458 analytical method Methods 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000004296 chiral HPLC Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000007903 gelatin capsule Substances 0.000 claims 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 claims 1
Classifications
-
- 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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
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- 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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (11)
1. Farmaceutski sastav koji sadrži spoj formule I-13 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač:
[image]
gdje sastav sadrži od oko 0,1% do oko 99% spoja formule I-13 u odnosu na masu ili volumen.
2. Farmaceutski sastav prema zahtjevu 1, gdje sastav sadrži od oko 5% do oko 90% spoja formule I-13 u odnosu na masu ili volumen.
3. Farmaceutski sastav prema zahtjevu 1 ili zahtjevu 2, gdje je postotak spoja formule I-13 prisutan u sastavu mjeren u odnosu na masu.
4. Farmaceutski sastav prema zahtjevu 1, gdje je spoj formule I-13 prisutan u enantiomernoj čistoći (ee%) većoj od 98% što je određeno kiralnom HPLC analizom.
5. Farmaceutski sastav prema zahtjevu 1, gdje je sastav tableta ili želatinska kapsula.
6. Smjesa koja sadrži spoj formule I-13 kako je definirano u zahtjevu 1 i spoj formule II-1 i spoj formule III:
[image]
Hal=Cl ili F
7. Smjesa prema zahtjevu 6, gdje je spoj formule III spoj formule III-1:
[image]
III-1
8. Postupak za dobivanje spoja formule I-13 ili njegove farmaceutski prihvatljive soli:
[image]
gdje spomenuti postupak obuhvaća korak reagiranja spoja formule II-1 sa spojem formule III:
[image]
Hal = Cl ili F.
9. Postupak prema zahtjevu 8, gdje spoj formule II-1 ima enantiomerni višak (ee%) veći od 98%.
10. Postupak prema zahtjevu 8 ili zahtjevu 9, gdje je spoj formule III spoj formule III-1:
[image]
III-1
11. Postupak prema bilo kojem od zahtjeva 8-10, gdje je reakcija spoja formule II-1 sa spojem formule III izvedena pod uvjetom pogodnim za nukleofilnu supstituciju.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462053006P | 2014-09-19 | 2014-09-19 | |
| US201562128089P | 2015-03-04 | 2015-03-04 | |
| US201562150812P | 2015-04-21 | 2015-04-21 | |
| EP18198969.0A EP3447050B1 (en) | 2014-09-19 | 2015-09-18 | Pyridin-2(1h)-one quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200666T1 true HRP20200666T1 (hr) | 2020-07-24 |
Family
ID=54291606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200666TT HRP20200666T1 (hr) | 2014-09-19 | 2020-04-24 | Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze |
Country Status (36)
| Country | Link |
|---|---|
| US (8) | US9834539B2 (hr) |
| EP (4) | EP3194376B1 (hr) |
| JP (1) | JP6648115B2 (hr) |
| KR (1) | KR102209667B1 (hr) |
| CN (3) | CN117695280A (hr) |
| AU (3) | AU2015317329B2 (hr) |
| BR (1) | BR112017005238B1 (hr) |
| CA (1) | CA2961817C (hr) |
| CL (1) | CL2017000658A1 (hr) |
| CO (1) | CO2017003241A2 (hr) |
| CY (2) | CY1121149T1 (hr) |
| DK (2) | DK3447050T3 (hr) |
| EA (1) | EA034336B1 (hr) |
| EC (1) | ECSP17022933A (hr) |
| ES (3) | ES2953347T3 (hr) |
| FI (1) | FI3733662T3 (hr) |
| HR (1) | HRP20200666T1 (hr) |
| HU (2) | HUE062424T2 (hr) |
| IL (3) | IL292608A (hr) |
| LT (2) | LT3194376T (hr) |
| MA (2) | MA40481A (hr) |
| ME (1) | ME03776B (hr) |
| MX (2) | MX2017003404A (hr) |
| MY (2) | MY176250A (hr) |
| NZ (2) | NZ758641A (hr) |
| PE (1) | PE20171056A1 (hr) |
| PH (1) | PH12017500517A1 (hr) |
| PL (3) | PL3194376T3 (hr) |
| PT (3) | PT3447050T (hr) |
| RS (2) | RS60140B1 (hr) |
| SA (1) | SA517381129B1 (hr) |
| SG (1) | SG11201702194SA (hr) |
| SI (2) | SI3194376T1 (hr) |
| TW (1) | TWI686390B (hr) |
| WO (1) | WO2016044789A1 (hr) |
| ZA (2) | ZA201702127B (hr) |
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| CA2793835C (en) | 2009-10-21 | 2021-07-20 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| RS57843B1 (sr) | 2014-02-06 | 2018-12-31 | Heptares Therapeutics Ltd | Biciklična aza jedinjenja kao agonisti muskarinskog receptora m1 |
| BR112017005444A2 (pt) | 2014-09-19 | 2018-04-24 | Bayer Pharma AG | indazoles substituídos por benzil como inibidores bub1. |
| JP6648116B2 (ja) * | 2014-09-19 | 2020-02-14 | フォーマ セラピューティクス，インコーポレイテッド | 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのキノリノンピリミジン組成物 |
| US9771349B2 (en) | 2014-09-19 | 2017-09-26 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| CA2961807A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| JP6648115B2 (ja) | 2014-09-19 | 2020-02-14 | フォーマ セラピューティクス，インコーポレイテッド | 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのピリジン−２（１ｈ）−オンキノリノン誘導体 |
| CA2971872C (en) | 2014-12-22 | 2023-10-10 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Mutant idh1 inhibitors useful for treating cancer |
| US9624175B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016171756A1 (en) | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| ES2919280T3 (es) | 2017-05-04 | 2022-07-22 | Bayer Cropscience Ag | Derivados de 2-{[2-(feniloximetil)piridin-5-il]oxi}-etanamina y compuestos relacionados como pesticidas, por ejemplo para la protección de plantas |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| EP3720442B1 (en) | 2018-05-16 | 2022-12-28 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| FI3720442T3 (fi) | 2018-05-16 | 2023-03-17 | Forma Therapeutics Inc | Mutantti idh-1:n inhibitio |
| US11013733B2 (en) * | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| WO2020232381A1 (en) | 2019-05-16 | 2020-11-19 | Forma Therapeutics, Inc. | INHIBITING MUTANT ISOCITRATE DEHYDROGENASE 1 (mIDH-1) |
| WO2019222551A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Solid forms of ((s)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile |
| TW202104207A (zh) * | 2019-04-17 | 2021-02-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| US11566013B1 (en) * | 2019-11-20 | 2023-01-31 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH1) |
| CN112321571B (zh) * | 2020-10-27 | 2022-06-03 | 浙江工业大学 | 2-呋喃-喹啉-4-甲酰胺类化合物及其应用 |
| CN112341389B (zh) * | 2020-10-27 | 2022-07-29 | 浙江工业大学 | 一种含氮芳杂环取代的喹啉甲酰胺类衍生物及其应用 |
| CN115850240B (zh) * | 2022-12-28 | 2023-09-19 | 北京康立生医药技术开发有限公司 | 一种治疗急性髓系白血病药物奥卢他西尼的合成方法 |
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2015
- 2015-09-18 JP JP2017515059A patent/JP6648115B2/ja active Active
- 2015-09-18 US US14/858,167 patent/US9834539B2/en active Active
- 2015-09-18 FI FIEP20157755.8T patent/FI3733662T3/fi active
- 2015-09-18 DK DK18198969.0T patent/DK3447050T3/da active
- 2015-09-18 EP EP15778433.1A patent/EP3194376B1/en active Active
- 2015-09-18 ES ES20157755T patent/ES2953347T3/es active Active
- 2015-09-18 SG SG11201702194SA patent/SG11201702194SA/en unknown
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- 2015-09-18 MX MX2017003404A patent/MX2017003404A/es active IP Right Grant
- 2015-09-18 EP EP20157755.8A patent/EP3733662B1/en active Active
- 2015-09-18 RS RS20200418A patent/RS60140B1/sr unknown
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- 2015-09-18 MA MA040481A patent/MA40481A/fr unknown
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- 2015-09-18 MA MA053352A patent/MA53352A/fr unknown
- 2015-09-18 ME MEP-2020-78A patent/ME03776B/me unknown
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