ES2656623T3 - Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma - Google Patents
Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma Download PDFInfo
- Publication number
- ES2656623T3 ES2656623T3 ES13817593.0T ES13817593T ES2656623T3 ES 2656623 T3 ES2656623 T3 ES 2656623T3 ES 13817593 T ES13817593 T ES 13817593T ES 2656623 T3 ES2656623 T3 ES 2656623T3
- Authority
- ES
- Spain
- Prior art keywords
- dimaleate
- crystalline form
- tyrosine kinase
- kinase inhibitor
- preparation methods
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 238000002360 preparation method Methods 0.000 title 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 title 1
- 238000002441 X-ray diffraction Methods 0.000 abstract 2
- 239000013078 crystal Substances 0.000 abstract 2
- -1 4- (3-chloro-4- (pyridin-2-ylmethoxy) -phenylamino) -3-cyano-7-ethoxyquinolin-6-yl Chemical group 0.000 abstract 1
- ATYQRIKLLZQHFG-UHFFFAOYSA-N N-(1-methylpyrrolidin-2-yl)prop-2-enamide Chemical compound C(C=C)(=O)NC1N(CCC1)C ATYQRIKLLZQHFG-UHFFFAOYSA-N 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/08—Malonic acid
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Forma cristalina I de dimaleato de (R,E)-N-(4-(3-cloro-4-(piridin-2-ilmetoxi)-fenilamino)-3-ciano-7-etoxiquinolin-6-il)- 3-(1-metilpirrolidin-2-il)acrilamida, caracterizada por que se usa radiación Kα de Cu para obtener los patrones de difracción de rayos X representados por ángulos 2θ y distancia de cristal interplanar, teniendo el cristal patrones de difracción de rayos X como se muestra en la Figura 1 en la que hay picos característicos en 6,28(14,06), 6,74(13,10), 10,60(8,34), 11,58(7,64), 13,50(6,55), 14,90(5,94), 15,80(5,60), 18,26(4,85), 20,66(4,30), 21,14(4,20), 22,96(3,87), 24,34(3,65), 25,54(3,49) y 26,12(3,41).
Description
Claims (1)
-
imagen1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210240697.0A CN103539783A (zh) | 2012-07-12 | 2012-07-12 | 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法 |
| CN201210240697 | 2012-07-12 | ||
| PCT/CN2013/076717 WO2014008794A1 (zh) | 2012-07-12 | 2013-06-04 | 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2656623T3 true ES2656623T3 (es) | 2018-02-27 |
Family
ID=49915377
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13817593.0T Active ES2656623T3 (es) | 2012-07-12 | 2013-06-04 | Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9309226B2 (es) |
| EP (1) | EP2873664B1 (es) |
| JP (1) | JP6170146B2 (es) |
| KR (1) | KR102078077B1 (es) |
| CN (2) | CN103539783A (es) |
| AU (1) | AU2013289789B2 (es) |
| BR (1) | BR112015000045B1 (es) |
| CA (1) | CA2876884C (es) |
| DK (1) | DK2873664T3 (es) |
| ES (1) | ES2656623T3 (es) |
| HU (1) | HUE037946T2 (es) |
| MX (1) | MX349672B (es) |
| NO (1) | NO2873664T3 (es) |
| PL (1) | PL2873664T3 (es) |
| PT (1) | PT2873664T (es) |
| RU (1) | RU2631321C2 (es) |
| TW (1) | TWI597277B (es) |
| UA (1) | UA113658C2 (es) |
| WO (1) | WO2014008794A1 (es) |
| ZA (1) | ZA201500471B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105985408B (zh) * | 2015-02-12 | 2020-06-26 | 正大天晴药业集团股份有限公司 | 一种卡非佐米的纯化方法 |
| CN108026059A (zh) | 2015-07-22 | 2018-05-11 | 阿纳韦克斯生命科学公司 | 四氢-n,n-二甲基-2,2-二苯基-3-呋喃甲胺盐酸盐的晶型,制备这样晶型的方法,及其药物组合物 |
| CA3008701A1 (en) | 2016-01-27 | 2017-08-03 | Jiangsu Hengrui Medicine Co., Ltd. | Method for preparing pharmaceutical composition comprising quinoline derivative or salt thereof |
| CN108354909B (zh) * | 2016-01-27 | 2021-05-14 | 江苏恒瑞医药股份有限公司 | 一种含有喹啉衍生物或其盐的药物组合物 |
| WO2017129094A1 (zh) * | 2016-01-28 | 2017-08-03 | 江苏恒瑞医药股份有限公司 | 一种egfr/her2受体酪氨酸激酶抑制剂在制备治疗her2突变癌症药物中的用途 |
| CA3016092C (en) * | 2016-03-22 | 2025-03-11 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | POLYCRYSTALLINE FORM OF FREE BASIC OR SALT EGFR INHIBITOR ACID, PROCESS FOR ITS PREPARATION AND APPLICATION |
| CN113769097A (zh) | 2017-01-22 | 2021-12-10 | 江苏恒瑞医药股份有限公司 | Egfr/her2抑制剂联合嘧啶类抗代谢药物的用途 |
| WO2019029477A1 (zh) * | 2017-08-07 | 2019-02-14 | 江苏恒瑞医药股份有限公司 | 一种酪氨酸激酶抑制剂的二马来酸盐的晶型及其制备方法 |
| CN109516976B (zh) * | 2017-09-19 | 2022-05-27 | 南京圣和药业股份有限公司 | 取代嘧啶类pi3k抑制剂甲磺酸盐的晶型及其制备方法 |
| CA3079916A1 (en) | 2017-10-24 | 2019-05-02 | Jiangsu Hengrui Medicine Co., Ltd. | Pharmaceutical composition containing quinoline derivative |
| CN110960529A (zh) * | 2018-09-30 | 2020-04-07 | 江苏恒瑞医药股份有限公司 | 一种降低了毒性杂质含量的酪氨酸激酶抑制剂的原料药 |
| MX2021004600A (es) | 2018-10-22 | 2021-06-15 | Jiangsu Hengrui Medicine Co | Forma cristalina del inhibidor de maleato de tirosina quinasa y metodo de preparacion para el mismo. |
| CN111138414A (zh) * | 2018-11-05 | 2020-05-12 | 江苏恒瑞医药股份有限公司 | 一种酪氨酸激酶抑制剂的晶型及其制备方法 |
| WO2021037185A1 (zh) * | 2019-08-30 | 2021-03-04 | 江苏恒瑞医药股份有限公司 | 一种低杂质含量的酪氨酸激酶抑制剂 |
| CN114674937B (zh) * | 2020-12-24 | 2024-07-05 | 沈阳药科大学 | 一种马来酸长链脂肪酰胺中长链脂肪胺的测定方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA73073C2 (uk) * | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| WO2001051919A2 (en) * | 2000-01-07 | 2001-07-19 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
| US8022216B2 (en) * | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| CN101824029A (zh) * | 2009-03-05 | 2010-09-08 | 厦门艾德生物医药科技有限公司 | 酪氨酸激酶不可逆抑制剂、其药物组合物及其用途 |
| CN102020639A (zh) * | 2009-09-14 | 2011-04-20 | 上海恒瑞医药有限公司 | 6-氨基喹唑啉或3-氰基喹啉类衍生物、其制备方法及其在医药上的应用 |
| CN102675287A (zh) * | 2011-03-11 | 2012-09-19 | 江苏恒瑞医药股份有限公司 | (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用 |
-
2012
- 2012-07-12 CN CN201210240697.0A patent/CN103539783A/zh active Pending
-
2013
- 2013-06-04 DK DK13817593.0T patent/DK2873664T3/en active
- 2013-06-04 CA CA2876884A patent/CA2876884C/en active Active
- 2013-06-04 CN CN201380004046.4A patent/CN103974949B/zh active Active
- 2013-06-04 HU HUE13817593A patent/HUE037946T2/hu unknown
- 2013-06-04 WO PCT/CN2013/076717 patent/WO2014008794A1/zh not_active Ceased
- 2013-06-04 BR BR112015000045-2A patent/BR112015000045B1/pt active IP Right Grant
- 2013-06-04 US US14/412,762 patent/US9309226B2/en not_active Expired - Fee Related
- 2013-06-04 EP EP13817593.0A patent/EP2873664B1/en active Active
- 2013-06-04 AU AU2013289789A patent/AU2013289789B2/en not_active Ceased
- 2013-06-04 KR KR1020157002815A patent/KR102078077B1/ko active Active
- 2013-06-04 PT PT138175930T patent/PT2873664T/pt unknown
- 2013-06-04 JP JP2015520803A patent/JP6170146B2/ja not_active Expired - Fee Related
- 2013-06-04 PL PL13817593T patent/PL2873664T3/pl unknown
- 2013-06-04 MX MX2014015623A patent/MX349672B/es active IP Right Grant
- 2013-06-04 NO NO13817593A patent/NO2873664T3/no unknown
- 2013-06-04 UA UAA201500919A patent/UA113658C2/uk unknown
- 2013-06-04 ES ES13817593.0T patent/ES2656623T3/es active Active
- 2013-06-04 RU RU2015103065A patent/RU2631321C2/ru active
- 2013-06-20 TW TW102121870A patent/TWI597277B/zh not_active IP Right Cessation
-
2015
- 2015-01-22 ZA ZA2015/00471A patent/ZA201500471B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UA113658C2 (xx) | 2017-02-27 |
| EP2873664A1 (en) | 2015-05-20 |
| CA2876884C (en) | 2019-12-10 |
| JP2015522042A (ja) | 2015-08-03 |
| HK1199027A1 (zh) | 2015-06-19 |
| AU2013289789A1 (en) | 2015-01-22 |
| EP2873664B1 (en) | 2017-11-01 |
| CN103974949B (zh) | 2015-11-25 |
| CN103539783A (zh) | 2014-01-29 |
| US9309226B2 (en) | 2016-04-12 |
| KR20150036336A (ko) | 2015-04-07 |
| KR102078077B1 (ko) | 2020-02-17 |
| MX349672B (es) | 2017-08-08 |
| RU2631321C2 (ru) | 2017-09-21 |
| MX2014015623A (es) | 2015-06-23 |
| US20150166511A1 (en) | 2015-06-18 |
| TWI597277B (zh) | 2017-09-01 |
| JP6170146B2 (ja) | 2017-07-26 |
| ZA201500471B (en) | 2016-10-26 |
| BR112015000045B1 (pt) | 2021-10-26 |
| NO2873664T3 (es) | 2018-03-31 |
| PT2873664T (pt) | 2018-01-24 |
| CA2876884A1 (en) | 2014-01-16 |
| CN103974949A (zh) | 2014-08-06 |
| BR112015000045A2 (pt) | 2017-06-27 |
| EP2873664A4 (en) | 2015-12-30 |
| TW201402563A (zh) | 2014-01-16 |
| RU2015103065A (ru) | 2016-08-27 |
| AU2013289789B2 (en) | 2017-06-29 |
| DK2873664T3 (en) | 2018-01-08 |
| PL2873664T3 (pl) | 2018-06-29 |
| HUE037946T2 (hu) | 2018-09-28 |
| WO2014008794A1 (zh) | 2014-01-16 |
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