CO2017003969A2 - Derivado de isoxazol como inhibidor de isocitrato deshidrogenasa 1 mutante - Google Patents
Derivado de isoxazol como inhibidor de isocitrato deshidrogenasa 1 mutanteInfo
- Publication number
- CO2017003969A2 CO2017003969A2 CONC2017/0003969A CO2017003969A CO2017003969A2 CO 2017003969 A2 CO2017003969 A2 CO 2017003969A2 CO 2017003969 A CO2017003969 A CO 2017003969A CO 2017003969 A2 CO2017003969 A2 CO 2017003969A2
- Authority
- CO
- Colombia
- Prior art keywords
- inhibitor
- isocitrate dehydrogenase
- isoxazole derivative
- mutant isocitrate
- protein
- Prior art date
Links
- 229940123392 Isocitrate dehydrogenase 1 inhibitor Drugs 0.000 title 1
- 150000002545 isoxazoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 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
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Hematology (AREA)
- Oncology (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
Se ha encontrado que un compuesto de la fórmula general (I) que tiene una estructura de isoxazol tiene excelente actividad inhibidora contra la proteína IDH1 mutante e inhibe la producción de 2-HG por esta proteína, mientras que el compuesto también es capaz de inhibir efectivamente el crecimiento de varios tumores que expresan la proteína. En la fórmula, R1, R2, R3, Y y Z son como se definen en la reivindicación 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 |
|---|---|
| CO2017003969A2 true CO2017003969A2 (es) | 2017-07-11 |
Family
ID=55630718
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2017/0003969A CO2017003969A2 (es) | 2014-10-01 | 2017-04-24 | Derivado de isoxazol como inhibidor de isocitrato deshidrogenasa 1 mutante |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US10040791B2 (es) |
| EP (1) | EP3202766B1 (es) |
| JP (1) | JP6087033B2 (es) |
| KR (1) | KR102440429B1 (es) |
| CN (1) | CN106795146B (es) |
| AU (1) | AU2015325279B2 (es) |
| BR (1) | BR112017006425B8 (es) |
| CA (1) | CA2963359C (es) |
| CO (1) | CO2017003969A2 (es) |
| CY (1) | CY1122891T1 (es) |
| DK (1) | DK3202766T3 (es) |
| ES (1) | ES2779305T3 (es) |
| HR (1) | HRP20200395T1 (es) |
| HU (1) | HUE048997T2 (es) |
| IL (1) | IL251305B (es) |
| LT (1) | LT3202766T (es) |
| MX (1) | MX2017003782A (es) |
| PH (1) | PH12017500530A1 (es) |
| PL (1) | PL3202766T3 (es) |
| PT (1) | PT3202766T (es) |
| RS (1) | RS60064B1 (es) |
| RU (1) | RU2692782C2 (es) |
| SG (1) | SG11201702389XA (es) |
| SI (1) | SI3202766T1 (es) |
| SM (1) | SMT202000275T1 (es) |
| WO (1) | WO2016052697A1 (es) |
| ZA (1) | ZA201703013B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017019429A1 (en) * | 2015-07-27 | 2017-02-02 | Eli Lilly And Company | 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds and theit use as mutant idh1 inhibitors |
| ES2814290T3 (es) | 2016-06-06 | 2021-03-26 | Lilly Co Eli | Inhibidores de IDH1 mutante |
| WO2018010142A1 (en) * | 2016-07-14 | 2018-01-18 | Shanghai Meton Pharmaceutical Co., Ltd | Iso-citrate dehydrogenase (idh) inhibitor |
| US20210113598A1 (en) * | 2017-08-01 | 2021-04-22 | Deutsches Krebsforschungszentrum (DKFZ) Stiftung des öffentlichen Rechts | Combination of MIDH1 Inhibitors and DNA Hypomethylating Agents (HMA) |
| TW201932120A (zh) * | 2018-01-29 | 2019-08-16 | 日商富士軟片股份有限公司 | 用於具有異檸檬酸脫氫酶突變的腫瘤的藥物組成物與抗腫瘤劑及其應用 |
| MD4010331T2 (ro) | 2019-08-08 | 2024-03-31 | Servier Lab | Procedeu de obținere a ivosidenibului și a unui intermediar al acestuia |
| EP4114378A1 (en) | 2020-03-05 | 2023-01-11 | Université de Lausanne | Modulators of aralar for treating neurological disorders |
| MX2023000902A (es) * | 2020-07-21 | 2023-02-22 | Daiichi Sankyo Co Ltd | Combinacion farmaceutica de temozolomida e inhibidor de la enzima mutante idh1. |
| WO2022092247A1 (ja) | 2020-10-30 | 2022-05-05 | 第一三共株式会社 | ３－メチル－４－ハロ－インドール誘導体の製造方法 |
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 |
| AU678186B2 (en) | 1992-10-23 | 1997-05-22 | Merck Sharp & Dohme Limited | 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 |
| KR20070058599A (ko) * | 2004-09-10 | 2007-06-08 | 신젠타 리미티드 | 살진균제로서의 치환된 이속사졸 |
| EP2593425B1 (en) | 2010-07-16 | 2018-10-17 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their method of use |
| EP2691391A4 (en) | 2011-03-29 | 2014-09-10 | Broad Inst Inc | COMPOUNDS AND METHODS OF TREATING DISORDERS MEDIATED BY ISOCITRATE DEHYDROGENASE |
| 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 |
| 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 |
| JP6026544B2 (ja) * | 2011-09-27 | 2016-11-16 | ノバルティス アーゲー | 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類 |
| ES2698625T3 (es) | 2012-01-19 | 2019-02-05 | Agios Pharmaceuticals Inc | Compuestos terapéuticamente activos y sus métodos de uso |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
-
2015
- 2015-10-01 CA CA2963359A patent/CA2963359C/en active Active
- 2015-10-01 CN CN201580050809.8A patent/CN106795146B/zh active Active
- 2015-10-01 HR HRP20200395TT patent/HRP20200395T1/hr unknown
- 2015-10-01 AU AU2015325279A patent/AU2015325279B2/en active Active
- 2015-10-01 SI SI201531109T patent/SI3202766T1/sl unknown
- 2015-10-01 US US15/516,362 patent/US10040791B2/en active Active
- 2015-10-01 MX MX2017003782A patent/MX2017003782A/es unknown
- 2015-10-01 SM SM20200275T patent/SMT202000275T1/it unknown
- 2015-10-01 PT PT158455493T patent/PT3202766T/pt unknown
- 2015-10-01 JP JP2016552161A patent/JP6087033B2/ja active Active
- 2015-10-01 ES ES15845549T patent/ES2779305T3/es active Active
- 2015-10-01 SG SG11201702389XA patent/SG11201702389XA/en unknown
- 2015-10-01 HU HUE15845549A patent/HUE048997T2/hu unknown
- 2015-10-01 PL PL15845549T patent/PL3202766T3/pl unknown
- 2015-10-01 BR BR112017006425A patent/BR112017006425B8/pt active IP Right Grant
- 2015-10-01 KR KR1020177011877A patent/KR102440429B1/ko active Active
- 2015-10-01 WO PCT/JP2015/077916 patent/WO2016052697A1/ja not_active Ceased
- 2015-10-01 EP EP15845549.3A patent/EP3202766B1/en active Active
- 2015-10-01 RU RU2017114005A patent/RU2692782C2/ru active
- 2015-10-01 RS RS20200290A patent/RS60064B1/sr unknown
- 2015-10-01 LT LTEP15845549.3T patent/LT3202766T/lt unknown
- 2015-10-01 DK DK15845549.3T patent/DK3202766T3/da active
-
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
- 2020-03-13 CY CY20201100221T patent/CY1122891T1/el unknown
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