CY1122891T1 - Παραγωγο ισοξαζολιου ως μεταλλαγμενος αναστολεας ισοκιτρικης αφυδρογονασης 1 - Google Patents
Παραγωγο ισοξαζολιου ως μεταλλαγμενος αναστολεας ισοκιτρικης αφυδρογονασης 1Info
- Publication number
- CY1122891T1 CY1122891T1 CY20201100221T CY201100221T CY1122891T1 CY 1122891 T1 CY1122891 T1 CY 1122891T1 CY 20201100221 T CY20201100221 T CY 20201100221T CY 201100221 T CY201100221 T CY 201100221T CY 1122891 T1 CY1122891 T1 CY 1122891T1
- Authority
- CY
- Cyprus
- Prior art keywords
- isoxazole derivative
- dehydrogenation
- inhibitor
- mutated isocitrate
- isocitrate
- Prior art date
Links
- 238000006356 dehydrogenation reaction Methods 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- ODBLHEXUDAPZAU-UHFFFAOYSA-N isocitric acid Chemical compound OC(=O)C(O)C(C(O)=O)CC(O)=O ODBLHEXUDAPZAU-UHFFFAOYSA-N 0.000 title 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical class C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 abstract 1
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 abstract 1
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Ανακαλύφθηκε ότι μία ένωση του γενικού τύπου (Ι) η οποία έχει σκελετό ισοξαζολίου έχει εξαιρετική ανασταλτική δραστικότητα επί μεταλλαγμένης IDH1 πρωτεΐνης, αναστέλλει παραγωγή 2-ΗG με την προαναφερθείσα πρωτεΐνη και μπορεί αποτελεσματικά να αναστέλλει τον πολλαπλασιασμό διαφόρων όγκων που εκφράζουν την προαναφερθείσα πρωτεΐνη, στο γενικό τύπο (Ι), R1, R2, R3, Υ και Ζ εκάστη είναι όπως ορίζεται στην αξίωση 1.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014203475 | 2014-10-01 | ||
| JP2015116774 | 2015-06-09 | ||
| PCT/JP2015/077916 WO2016052697A1 (ja) | 2014-10-01 | 2015-10-01 | 変異型イソクエン酸デヒドロゲナーゼ１阻害剤としてのイソキサゾール誘導体 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1122891T1 true CY1122891T1 (el) | 2021-05-05 |
Family
ID=55630718
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20201100221T CY1122891T1 (el) | 2014-10-01 | 2020-03-13 | Παραγωγο ισοξαζολιου ως μεταλλαγμενος αναστολεας ισοκιτρικης αφυδρογονασης 1 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US10040791B2 (el) |
| EP (1) | EP3202766B1 (el) |
| JP (1) | JP6087033B2 (el) |
| KR (1) | KR102440429B1 (el) |
| CN (1) | CN106795146B (el) |
| AU (1) | AU2015325279B2 (el) |
| BR (1) | BR112017006425B8 (el) |
| CA (1) | CA2963359C (el) |
| CO (1) | CO2017003969A2 (el) |
| CY (1) | CY1122891T1 (el) |
| DK (1) | DK3202766T3 (el) |
| ES (1) | ES2779305T3 (el) |
| HR (1) | HRP20200395T1 (el) |
| HU (1) | HUE048997T2 (el) |
| IL (1) | IL251305B (el) |
| LT (1) | LT3202766T (el) |
| MX (1) | MX2017003782A (el) |
| PH (1) | PH12017500530A1 (el) |
| PL (1) | PL3202766T3 (el) |
| PT (1) | PT3202766T (el) |
| RS (1) | RS60064B1 (el) |
| RU (1) | RU2692782C2 (el) |
| SG (1) | SG11201702389XA (el) |
| SI (1) | SI3202766T1 (el) |
| WO (1) | WO2016052697A1 (el) |
| ZA (1) | ZA201703013B (el) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2764523T3 (es) * | 2015-07-27 | 2020-06-03 | Lilly Co Eli | Compuestos de 7-feniletilamino-4H-pirimido[4,5-D][1,3]oxazin-2-ona y su uso como inhibidores de IDH1 mutantes |
| WO2017213910A1 (en) | 2016-06-06 | 2017-12-14 | Eli Lilly And Company | Mutant idh1 inhibitors |
| WO2018010142A1 (en) | 2016-07-14 | 2018-01-18 | Shanghai Meton Pharmaceutical Co., Ltd | Iso-citrate dehydrogenase (idh) inhibitor |
| CA3070878A1 (en) * | 2017-08-01 | 2019-02-07 | Deutsches Krebsforschungszentrum | Combination of midh1 inhibitors and dna hypomethylating agents (hma) |
| WO2019146129A1 (ja) * | 2018-01-29 | 2019-08-01 | 富士フイルム株式会社 | イソクエン酸デヒドロゲナーゼ変異を有する腫瘍に対する医薬組成物および抗腫瘍剤ならびにその利用 |
| WO2021176098A1 (en) | 2020-03-05 | 2021-09-10 | Université de Lausanne | Modulators of aralar for treating neurological disorders |
| JP2022021331A (ja) | 2020-07-21 | 2022-02-02 | 第一三共株式会社 | テモゾロミドと変異型ｉｄｈ１酵素阻害剤の組み合わせ医薬 |
| TW202233576A (zh) | 2020-10-30 | 2022-09-01 | 日商第一三共股份有限公司 | ３－甲基－鹵－吲哚衍生物之製造方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3194811A (en) | 1963-09-05 | 1965-07-13 | Merck & Co Inc | Aroyl-benzindolyl acids |
| EP0665833B1 (en) | 1992-10-23 | 1999-07-14 | MERCK SHARP & DOHME LTD. | Dopamine receptor subtype ligands |
| WO1994024095A1 (en) | 1993-04-16 | 1994-10-27 | Abbott Laboratories | Immunosuppressive agents |
| GB2284600A (en) | 1994-01-21 | 1995-06-14 | Shell Int Research | Herbicidal 3-(hetero)aryl-4-acylisoxazole compositions and compounds |
| EA009919B1 (ru) | 2003-02-11 | 2008-04-28 | Вернэлис (Кембридж) Лимитед | Соединения изоксазола |
| RU2392273C2 (ru) * | 2004-09-10 | 2010-06-20 | Синджента Лимитед | Замещенные изоксазолы в качестве фунгицидов |
| BR112013001122B1 (pt) * | 2010-07-16 | 2021-06-08 | Agios Pharmaceuticals, Inc | composto de fórmula ii, uso do composto e composição farmacêutica compreendendo dito composto |
| WO2012173682A2 (en) | 2011-03-29 | 2012-12-20 | The Broad Institute, Inc. | Compounds and methods for the treatment of isocitrate dehydrognase related diseases |
| CN102827073A (zh) * | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| CN102827170A (zh) * | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| MX342326B (es) * | 2011-09-27 | 2016-09-26 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. |
| US20150087600A1 (en) | 2012-01-19 | 2015-03-26 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
-
2015
- 2015-10-01 RU RU2017114005A patent/RU2692782C2/ru active
- 2015-10-01 AU AU2015325279A patent/AU2015325279B2/en active Active
- 2015-10-01 PT PT158455493T patent/PT3202766T/pt unknown
- 2015-10-01 KR KR1020177011877A patent/KR102440429B1/ko active IP Right Grant
- 2015-10-01 CN CN201580050809.8A patent/CN106795146B/zh active Active
- 2015-10-01 PL PL15845549T patent/PL3202766T3/pl unknown
- 2015-10-01 WO PCT/JP2015/077916 patent/WO2016052697A1/ja active Application Filing
- 2015-10-01 ES ES15845549T patent/ES2779305T3/es active Active
- 2015-10-01 DK DK15845549.3T patent/DK3202766T3/da active
- 2015-10-01 EP EP15845549.3A patent/EP3202766B1/en active Active
- 2015-10-01 BR BR112017006425A patent/BR112017006425B8/pt active IP Right Grant
- 2015-10-01 CA CA2963359A patent/CA2963359C/en active Active
- 2015-10-01 RS RS20200290A patent/RS60064B1/sr unknown
- 2015-10-01 SG SG11201702389XA patent/SG11201702389XA/en unknown
- 2015-10-01 LT LTEP15845549.3T patent/LT3202766T/lt unknown
- 2015-10-01 MX MX2017003782A patent/MX2017003782A/es unknown
- 2015-10-01 HU HUE15845549A patent/HUE048997T2/hu unknown
- 2015-10-01 US US15/516,362 patent/US10040791B2/en active Active
- 2015-10-01 JP JP2016552161A patent/JP6087033B2/ja active Active
- 2015-10-01 SI SI201531109T patent/SI3202766T1/sl unknown
-
2017
- 2017-03-21 IL IL251305A patent/IL251305B/en active IP Right Grant
- 2017-03-22 PH PH12017500530A patent/PH12017500530A1/en unknown
- 2017-04-24 CO CONC2017/0003969A patent/CO2017003969A2/es unknown
- 2017-04-28 ZA ZA2017/03013A patent/ZA201703013B/en unknown
-
2020
- 2020-03-10 HR HRP20200395TT patent/HRP20200395T1/hr unknown
- 2020-03-13 CY CY20201100221T patent/CY1122891T1/el unknown
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