CN102358736A - 4-甲基-n-[3-（4-甲基-咪唑-1-基）-5-三氟甲基-苯基]-3-（4-吡啶-3-基-嘧啶-2-基氨基）-苯甲酰胺的晶形 - Google Patents
4-甲基-n-[3-（4-甲基-咪唑-1-基）-5-三氟甲基-苯基]-3-（4-吡啶-3-基-嘧啶-2-基氨基）-苯甲酰胺的晶形 Download PDFInfo
- Publication number
- CN102358736A CN102358736A CN2011102583896A CN201110258389A CN102358736A CN 102358736 A CN102358736 A CN 102358736A CN 2011102583896 A CN2011102583896 A CN 2011102583896A CN 201110258389 A CN201110258389 A CN 201110258389A CN 102358736 A CN102358736 A CN 102358736A
- Authority
- CN
- China
- Prior art keywords
- methyl
- trifluoromethyl
- pyridin
- phenyl
- imidazoles
- 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.)
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- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 title abstract description 3
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- SNIABFMMCKVXSY-UHFFFAOYSA-N benzoylazanium;chloride Chemical compound Cl.NC(=O)C1=CC=CC=C1 SNIABFMMCKVXSY-UHFFFAOYSA-N 0.000 description 2
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Images
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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring 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
- A61K31/495—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
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70140505P | 2005-07-20 | 2005-07-20 | |
| US60/701,405 | 2005-07-20 | ||
| US71621405P | 2005-09-12 | 2005-09-12 | |
| US60/716,214 | 2005-09-12 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200680026434.2A Division CN101228150B (zh) | 2005-07-20 | 2006-07-18 | 4-甲基-n-[3-(4-甲基-咪唑-1-基)-5-三氟甲基-苯基]-3-(4-吡啶-3-基-嘧啶-2-基氨基)-苯甲酰胺的晶形 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102358736A true CN102358736A (zh) | 2012-02-22 |
Family
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Family Applications (2)
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|---|---|---|---|
| CN2011102583896A Pending CN102358736A (zh) | 2005-07-20 | 2006-07-18 | 4-甲基-n-[3-（4-甲基-咪唑-1-基）-5-三氟甲基-苯基]-3-（4-吡啶-3-基-嘧啶-2-基氨基）-苯甲酰胺的晶形 |
| CN201310349258.8A Pending CN103804356A (zh) | 2005-07-20 | 2006-07-18 | 4-甲基-n-[3-（4-甲基-咪唑-1-基）-5-三氟甲基-苯基]-3-（4-吡啶-3-基-嘧啶-2-基氨基）-苯甲酰胺的晶形 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310349258.8A Pending CN103804356A (zh) | 2005-07-20 | 2006-07-18 | 4-甲基-n-[3-（4-甲基-咪唑-1-基）-5-三氟甲基-苯基]-3-（4-吡啶-3-基-嘧啶-2-基氨基）-苯甲酰胺的晶形 |
Country Status (42)
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106496193A (zh) * | 2016-09-13 | 2017-03-15 | 福格森（武汉）生物科技股份有限公司 | 一种高纯度尼罗替尼的制备方法 |
| CN113292537A (zh) * | 2018-06-15 | 2021-08-24 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| CN113788817A (zh) * | 2021-09-27 | 2021-12-14 | 南京海润医药有限公司 | 一种尼罗替尼半盐酸盐一水合物晶型及其制备方法 |
| US12186316B2 (en) | 2020-09-29 | 2025-01-07 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GT200600315A (es) | 2005-07-20 | 2007-03-19 | Formas cristalinas de 4-metilo-n-[3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo]-3-(4-pyridina-3-ilo-pirimidina-2-iloamino)-benzamida | |
| GT200600316A (es) * | 2005-07-20 | 2007-04-02 | Sales de 4-metilo-n-(3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo)-3-(4-piridina-3-ilo-pirimidina-2-iloamino)- benzamida. | |
| MX2008012903A (es) * | 2006-04-07 | 2008-10-13 | Novartis Ag | Uso de inhibidores de c-src en combinacion con un compuesto de pirimidilaminobenzamida para el tratamiento de la leucemia. |
| EP1923053A1 (en) | 2006-09-27 | 2008-05-21 | Novartis AG | Pharmaceutical compositions comprising nilotinib or its salt |
| EP2240172B1 (en) | 2007-12-21 | 2014-03-19 | Novartis AG | Combination of nilotinib and chlorambucil for the treatment of chronic lymphocytic leukemia |
| EP2305667A3 (en) | 2008-07-17 | 2011-05-11 | Teva Pharmaceutical Industries Ltd. | Nilotinib intermediates and preparation thereof |
| CN102203084B (zh) * | 2008-11-05 | 2014-10-29 | 特瓦制药工业有限公司 | 盐酸尼洛替尼晶型 |
| EP2186514B1 (en) | 2008-11-14 | 2016-06-29 | Kinki University | Treatment of Malignant Peripheral Nerve Sheath Tumors |
| EP2403492A1 (en) | 2009-03-06 | 2012-01-11 | Novartis AG | Use of pyrimidylaminobenzamide derivatives for the treatment of disorders mediated by the leucine zipper- and sterile alpha motif-containing kinase (zak) |
| TW201102068A (en) | 2009-06-02 | 2011-01-16 | Novartis Ag | Treatment of ophthalmologic disorders mediated by alpha-carbonic anhydrase isoforms |
| PH12012500797A1 (en) | 2009-10-23 | 2012-11-26 | Novartis Ag | Method of treating proliferative disorders and other pathological conditions mediated by bcr-abl, c-kit, ddr1, ddr2 or pdgf-r kinase activity |
| JO3634B1 (ar) | 2009-11-17 | 2020-08-27 | Novartis Ag | طريقة لعلاج اضطرابات تكاثرية وحالات مرضية أخرى متوسطة بنشاط كيناز bcr-abl، c-kit، ddr1، ddr2، أو pdgf-r |
| IN2010KO00035A (enExample) * | 2010-01-15 | 2016-09-02 | ||
| JP2013525296A (ja) | 2010-04-16 | 2013-06-20 | ノバルティス アーゲー | 内分泌療法抵抗性乳癌の処置 |
| EP2382976A1 (en) | 2010-04-30 | 2011-11-02 | Hiroshima University | Use of pdgf-r inhibitors for the treatment of lymph node metastasis of gastric cancer |
| US8937082B2 (en) | 2010-06-21 | 2015-01-20 | Teva Pharmaceutical Industries Ltd. | Nilotinib salts and crystalline forms thereof |
| CN102453024B (zh) * | 2010-10-27 | 2014-09-03 | 浙江九洲药业股份有限公司 | 一种尼罗替尼盐酸盐晶型及其制备方法 |
| EP2648519A4 (en) * | 2010-11-26 | 2014-04-30 | Hetero Research Foundation | NEW POLYMORPH OF NILOTINIB HYDROCHLORIDE |
| AR086913A1 (es) * | 2011-06-14 | 2014-01-29 | Novartis Ag | 4-metil-3-[[4-(3-piridinil)-2-pirimidinil]-amino]-n-[5-(4-metil-1h-imidazol-1-il)-3-(trifluoro-metil)-fenil]-benzamida amorfa, forma de dosificacion que la contiene y metodo para prepararlas |
| WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| EP2770999A1 (en) | 2011-10-28 | 2014-09-03 | Novartis AG | Method of treating gastrointestinal stromal tumors |
| CA2855503A1 (en) | 2011-11-14 | 2013-05-23 | Novartis Ag | Immediate release 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-n-[5-(4-methyl-1h-imidazol-1-yl)-3-(trifluoromethyl)phenyl] benzamide formulation |
| EP2626355B1 (en) * | 2012-02-09 | 2016-02-03 | Natco Pharma Limited | Process for the preparation of nilotinib hydrochloride |
| GB2514285B (en) | 2012-02-13 | 2018-07-18 | Grindeks Jsc | Intermediates for a novel process of preparing imatinib and related tyrosine kinase inhibitors |
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| CN106496193A (zh) * | 2016-09-13 | 2017-03-15 | 福格森（武汉）生物科技股份有限公司 | 一种高纯度尼罗替尼的制备方法 |
| CN113292537A (zh) * | 2018-06-15 | 2021-08-24 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| CN113292537B (zh) * | 2018-06-15 | 2024-04-05 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| US12186316B2 (en) | 2020-09-29 | 2025-01-07 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions |
| CN113788817A (zh) * | 2021-09-27 | 2021-12-14 | 南京海润医药有限公司 | 一种尼罗替尼半盐酸盐一水合物晶型及其制备方法 |
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