MX2017011392A - P-toluensulfonato para inhibidor de mek cinasa, y su forma de cristal y su metodo de preparacion. - Google Patents
P-toluensulfonato para inhibidor de mek cinasa, y su forma de cristal y su metodo de preparacion.Info
- Publication number
- MX2017011392A MX2017011392A MX2017011392A MX2017011392A MX2017011392A MX 2017011392 A MX2017011392 A MX 2017011392A MX 2017011392 A MX2017011392 A MX 2017011392A MX 2017011392 A MX2017011392 A MX 2017011392A MX 2017011392 A MX2017011392 A MX 2017011392A
- Authority
- MX
- Mexico
- Prior art keywords
- crystal form
- toluenesulfonate
- preparation
- kinase inhibitor
- mek kinase
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 5
- 238000002360 preparation method Methods 0.000 title abstract 3
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 title abstract 3
- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 102000001291 MAP Kinase Kinase Kinase Human genes 0.000 abstract 1
- 108060006687 MAP kinase kinase kinase Proteins 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- ZHNUHDYFZUAESO-UHFFFAOYSA-N formamide Substances NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se describe un p-toluensulfonato para un inhibidor de MEK cinasa, y una forma de cristal del mismo y un método de preparación del mismo. De manera específica, se describe p-toluensulfonato de 2-((2-fluorine-4-yodofenil)amino)-1-metil-4-((6-metilpiridin-3-gr upo)oxigrupo)-6-carbonil-1,6-dihidropiridin-3-formamida (un compuesto representado por la fórmula (I)), y una forma de cristal I y un método de preparación del mismo. La forma de cristal I obtenida del compuesto representada por la fórmula (I) tiene buena estabilidad de forma de cristal y estabilidad química, y un solvente de cristalización usado tiene baja toxicidad y bajo residuo y puede usarse mejor en el tratamiento clínico. (ver Fórmula).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510141303 | 2015-03-27 | ||
| PCT/CN2016/075853 WO2016155473A1 (zh) | 2015-03-27 | 2016-03-08 | 一种mek激酶抑制剂的对甲苯磺酸盐、其结晶形式及制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017011392A true MX2017011392A (es) | 2018-01-15 |
| MX382056B MX382056B (es) | 2025-03-13 |
Family
ID=57005438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017011392A MX382056B (es) | 2015-03-27 | 2016-03-08 | P-toluensulfonato para inhibidor de mek cinasa, y su forma de cristal y su método de preparación. |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10118911B2 (es) |
| EP (1) | EP3275866B1 (es) |
| JP (1) | JP2018509407A (es) |
| KR (1) | KR20170131506A (es) |
| CN (1) | CN106795116B (es) |
| AU (1) | AU2016239028B2 (es) |
| BR (1) | BR112017018580A2 (es) |
| CA (1) | CA2978796A1 (es) |
| MX (1) | MX382056B (es) |
| RU (1) | RU2704251C2 (es) |
| TW (1) | TWI705060B (es) |
| WO (1) | WO2016155473A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201818936A (zh) | 2016-11-25 | 2018-06-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種吡啶酮類衍生物醫藥組成物及其製備方法 |
| TW201821408A (zh) * | 2016-12-01 | 2018-06-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種吡啶酮類衍生物的製備方法及其中間體 |
| CN113423398A (zh) * | 2019-01-29 | 2021-09-21 | 贝达药业股份有限公司 | Mek抑制剂及其在医药上的应用 |
| WO2021018112A1 (zh) * | 2019-07-29 | 2021-02-04 | 江苏恒瑞医药股份有限公司 | 一种1,6-二氢吡啶-3-甲酰胺衍生物的制备方法 |
| JP2024521788A (ja) | 2021-05-27 | 2024-06-04 | ミラティ セラピューティクス, インコーポレイテッド | 併用療法 |
| AU2023276599A1 (en) * | 2022-05-25 | 2024-12-05 | Imagenebio, Inc. | Mek inhibitors and uses thereof |
| CN120441478A (zh) * | 2024-02-07 | 2025-08-08 | 成都赜灵生物医药科技有限公司 | 一种六元内酰胺类化合物及其应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1272290B (it) * | 1994-06-20 | 1997-06-16 | Avantgarde Spa | Sale della l-carnitina e composizioni farmaceutiche che lo contengono per il trattamento di affezioni cutanee |
| US7732616B2 (en) * | 2003-11-19 | 2010-06-08 | Array Biopharma Inc. | Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof |
| US20110039819A1 (en) | 2008-04-22 | 2011-02-17 | Marion Hitchcock | Substituted phenoxybenzamides |
| KR20110103968A (ko) * | 2008-12-23 | 2011-09-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 유기 화합물의 염 형태 |
| CN102459188A (zh) * | 2009-06-15 | 2012-05-16 | 凯美隆(北京)药业技术有限公司 | 新型6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂 |
| US20120238599A1 (en) * | 2011-03-17 | 2012-09-20 | Chemizon, A Division Of Optomagic Co., Ltd. | Heterocyclic compounds as mek inhibitors |
| WO2014204263A1 (en) * | 2013-06-20 | 2014-12-24 | The Asan Foundation | Substituted pyridinone compounds as mek inhibitors |
| US9914703B2 (en) * | 2013-10-25 | 2018-03-13 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Pyridic ketone derivatives, method of preparing same, and pharmaceutical application thereof |
-
2016
- 2016-03-08 BR BR112017018580-6A patent/BR112017018580A2/pt active Search and Examination
- 2016-03-08 RU RU2017134709A patent/RU2704251C2/ru active
- 2016-03-08 KR KR1020177029896A patent/KR20170131506A/ko not_active Ceased
- 2016-03-08 CN CN201680001860.4A patent/CN106795116B/zh active Active
- 2016-03-08 WO PCT/CN2016/075853 patent/WO2016155473A1/zh not_active Ceased
- 2016-03-08 JP JP2017545735A patent/JP2018509407A/ja active Pending
- 2016-03-08 AU AU2016239028A patent/AU2016239028B2/en not_active Ceased
- 2016-03-08 CA CA2978796A patent/CA2978796A1/en not_active Abandoned
- 2016-03-08 EP EP16771228.0A patent/EP3275866B1/en active Active
- 2016-03-08 MX MX2017011392A patent/MX382056B/es unknown
- 2016-03-08 US US15/559,516 patent/US10118911B2/en not_active Expired - Fee Related
- 2016-03-22 TW TW105108789A patent/TWI705060B/zh not_active IP Right Cessation
-
2018
- 2018-09-10 US US16/125,896 patent/US20180370948A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| BR112017018580A2 (pt) | 2018-04-24 |
| US20180370948A1 (en) | 2018-12-27 |
| TW201634459A (zh) | 2016-10-01 |
| CN106795116A (zh) | 2017-05-31 |
| CN106795116B (zh) | 2019-11-01 |
| RU2017134709A3 (es) | 2019-07-17 |
| JP2018509407A (ja) | 2018-04-05 |
| US10118911B2 (en) | 2018-11-06 |
| EP3275866B1 (en) | 2019-12-04 |
| WO2016155473A1 (zh) | 2016-10-06 |
| EP3275866A4 (en) | 2018-08-15 |
| RU2017134709A (ru) | 2019-04-29 |
| US20180118715A1 (en) | 2018-05-03 |
| AU2016239028A1 (en) | 2017-09-14 |
| AU2016239028B2 (en) | 2019-09-19 |
| KR20170131506A (ko) | 2017-11-29 |
| EP3275866A1 (en) | 2018-01-31 |
| RU2704251C2 (ru) | 2019-10-25 |
| MX382056B (es) | 2025-03-13 |
| TWI705060B (zh) | 2020-09-21 |
| CA2978796A1 (en) | 2016-10-06 |
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