RU2599785C3 - Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина - Google Patents
Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диаминаInfo
- Publication number
- RU2599785C3 RU2599785C3 RU2013132947A RU2013132947A RU2599785C3 RU 2599785 C3 RU2599785 C3 RU 2599785C3 RU 2013132947 A RU2013132947 A RU 2013132947A RU 2013132947 A RU2013132947 A RU 2013132947A RU 2599785 C3 RU2599785 C3 RU 2599785C3
- Authority
- RU
- Russia
- Prior art keywords
- crystalline form
- phenyl
- weight
- less
- total impurities
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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
-
- 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
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Claims (9)
1. Кристаллическая форма А 5-хлор-N2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-N4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина, проявляющая пики порошковой рентгеновской дифракции, имеющие максимумы при углах дифракции, выбранные из 7,2°, 8,1°, 10,8°, 12,0°, 12,4°, 13,4°, 14,4°, 14,8°, 15,7°, 16,9°, 17,7°, 18,5°, 19,0°, 19,5°, 20,0°, 20,3°, 21,1°, 21,6°, 22,4°, 22,6°, 23,0°, 24,1°, 24,5°, 25,5°, 26,0°, 26,2°, 27,0°, 27,3°, 28,3°, 29,0°, 29,1°, 30,6°, 31,3°, 32,8°, 33,5°, 34,2° и 36,4° (2θ градусов).
2. Кристаллическая форма по п. 1, имеющая температуру плавления 174°С как определено дифференциальной сканирующей калориметрией.
3. Кристаллическая форма по п. 1, имеющая температуру разложения выше 250°С и потерю веса при сушке, равную 0,1% при 200°С, как определено термогравиметрическим анализом.
4. Кристаллическая форма по п. 1, имеющая характеристические полосы поглощения инфракрасного излучения при 3440,4, 3318,9, 2973,7, 2931,3, 2921,7, 1596,8, 1562,1, 1498,4, 1442,5, 1409,7, 1382,7, 1311,4, 1284,4, 1270,9, 1251,6, 1224,6, 1139,7, 1126,2, 1139,7, 1126,2, 1105,0, 1081,9, 1049,1, 1020,2, 1012,5, 952,7, 937,3, 894,8, 877,5, 860,1, 848,5, 817,7, 798,4, 781,0, 763,7, 756,0, 732,8, 686,6, 665,3, 644,1, 586,3 и 543,8 (в единицах волновых чисел, см-1).
5. Кристаллическая форма по п. 1, имеющая менее 1,0% по массе общих примесей.
6. Кристаллическая форма по п. 1, имеющая менее 0,5% по массе общих примесей.
7. Кристаллическая форма по п. 1, имеющая менее 0,1% по массе общих примесей.
8. Фармацевтическая композиция для применения для лечения расстройств, опосредованных киназой анапластической лимфомы, содержащая терапевтически эффективное количество кристаллической формы по п. 1 и фармацевтически приемлемый носитель.
9. Применение кристаллической формы 5-хлор-N2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-N4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина по любому из пп. 1-7 для получения лекарственного средства для лечения расстройств, опосредованных киназой анапластической лимфомы.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201061424194P | 2010-12-17 | 2010-12-17 | |
US61/424,194 | 2010-12-17 | ||
PCT/US2011/065030 WO2012082972A1 (en) | 2010-12-17 | 2011-12-15 | Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2016136823A Division RU2746159C2 (ru) | 2010-12-17 | 2011-12-15 | Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина |
Publications (3)
Publication Number | Publication Date |
---|---|
RU2013132947A RU2013132947A (ru) | 2015-01-27 |
RU2599785C2 RU2599785C2 (ru) | 2016-10-20 |
RU2599785C3 true RU2599785C3 (ru) | 2019-04-24 |
Family
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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RU2013132947A RU2599785C3 (ru) | 2010-12-17 | 2011-12-15 | Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина |
RU2016136823A RU2746159C2 (ru) | 2010-12-17 | 2011-12-15 | Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
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RU2016136823A RU2746159C2 (ru) | 2010-12-17 | 2011-12-15 | Кристаллические формы 5-хлор-n2-(2-изопропокси-5-метил-4-пиперидин-4-ил-фенил)-n4-[2-(пропан-2-сульфонил)-фенил]-пиримидин-2,4-диамина |
Country Status (35)
Country | Link |
---|---|
US (2) | US9309229B2 (ru) |
EP (3) | EP3121171B1 (ru) |
JP (1) | JP5916752B2 (ru) |
KR (4) | KR20190022903A (ru) |
CN (7) | CN114989139A (ru) |
AR (2) | AR084309A1 (ru) |
AU (1) | AU2011343775B2 (ru) |
BR (1) | BR112013015000A2 (ru) |
CA (1) | CA2821102C (ru) |
CL (1) | CL2013001723A1 (ru) |
CO (1) | CO6801792A2 (ru) |
CY (2) | CY1119474T1 (ru) |
DK (2) | DK3121171T3 (ru) |
EC (1) | ECSP13012770A (ru) |
ES (3) | ES2696526T3 (ru) |
GT (1) | GT201300153A (ru) |
HR (2) | HRP20171477T1 (ru) |
HU (1) | HUE041845T2 (ru) |
IL (1) | IL226474A (ru) |
LT (2) | LT2651918T (ru) |
MA (1) | MA34771B1 (ru) |
MX (1) | MX338210B (ru) |
MY (2) | MY164810A (ru) |
NZ (1) | NZ610713A (ru) |
PE (1) | PE20140698A1 (ru) |
PL (2) | PL2651918T3 (ru) |
PT (2) | PT3121171T (ru) |
RS (1) | RS57771B1 (ru) |
RU (2) | RU2599785C3 (ru) |
SG (2) | SG190856A1 (ru) |
SI (2) | SI3121171T1 (ru) |
TN (1) | TN2013000216A1 (ru) |
TW (2) | TWI576343B (ru) |
WO (1) | WO2012082972A1 (ru) |
ZA (1) | ZA201303599B (ru) |
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SG190856A1 (en) * | 2010-12-17 | 2013-07-31 | Novartis Ag | Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine |
BR112015010221B1 (pt) | 2012-11-06 | 2022-09-13 | Shanghai Fochon Pharmaceutical Co., Ltd. | Inibidores de quinase alk, seus usos, composição farmacêutica, e método para fabricação de medicamento |
KR101656382B1 (ko) * | 2014-02-28 | 2016-09-09 | 한국화학연구원 | 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 |
CN105272921A (zh) * | 2014-06-09 | 2016-01-27 | 江苏奥赛康药业股份有限公司 | 一种制备Ceritinib的方法及其中间体化合物 |
CN105294649B (zh) * | 2014-07-30 | 2019-05-14 | 江苏奥赛康药业股份有限公司 | 一种Ceritinib化合物及其药物组合物 |
CN105294650A (zh) * | 2014-08-01 | 2016-02-03 | 江苏奥赛康药业股份有限公司 | 一种Ceritinib化合物及其药物组合物 |
KR102331856B1 (ko) | 2014-10-21 | 2021-11-29 | 다케다 야쿠힌 고교 가부시키가이샤 | 결정 형태의 5-클로로-n4-[2-(디메틸포스포릴)페닐]-n2-{2-메톡시-4-[4-(4-메틸피페라진-1-일)피페리딘-1-일]피리미딘-2,4-디아민 |
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CN105601614A (zh) * | 2014-11-21 | 2016-05-25 | 奥浦顿(上海)医药科技有限公司 | 一种色瑞替尼晶型及其制备方法 |
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CN105061397B (zh) * | 2015-08-07 | 2018-01-02 | 武汉英普瑞医药科技有限公司 | 一种色瑞替尼的c型晶型及其制备方法与应用 |
CN106699743B (zh) | 2015-11-05 | 2020-06-12 | 湖北生物医药产业技术研究院有限公司 | 嘧啶类衍生物及其用途 |
WO2017152858A1 (zh) * | 2016-03-11 | 2017-09-14 | 苏州晶云药物科技有限公司 | 色瑞替尼的晶型及其制备方法 |
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SG190856A1 (en) * | 2010-12-17 | 2013-07-31 | Novartis Ag | Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine |
EP2651219A2 (en) | 2010-12-17 | 2013-10-23 | E.I. Du Pont De Nemours And Company | Fungicidal azocyclic amides |
CN105294650A (zh) | 2014-08-01 | 2016-02-03 | 江苏奥赛康药业股份有限公司 | 一种Ceritinib化合物及其药物组合物 |
WO2016081538A1 (en) | 2014-11-18 | 2016-05-26 | Teva Pharmaceuticals International Gmbh | Solid state forms of ceritinib and salts thereof |
DE112015005255B4 (de) | 2014-11-21 | 2023-10-26 | Joyson Safety Systems Acquisition Llc | Airbagmodul |
CN105622577A (zh) | 2014-11-29 | 2016-06-01 | 江苏先声药业有限公司 | 一种色瑞替尼的新晶型及其制备方法 |
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WO2017016529A1 (en) | 2015-07-28 | 2017-02-02 | Zentiva, K.S. | Solid forms of ceritinib free base |
CN105061397B (zh) | 2015-08-07 | 2018-01-02 | 武汉英普瑞医药科技有限公司 | 一种色瑞替尼的c型晶型及其制备方法与应用 |
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2011
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