RU2746159C2 - 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-диамина Download PDFInfo
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- RU2746159C2 RU2746159C2 RU2016136823A RU2016136823A RU2746159C2 RU 2746159 C2 RU2746159 C2 RU 2746159C2 RU 2016136823 A RU2016136823 A RU 2016136823A RU 2016136823 A RU2016136823 A RU 2016136823A RU 2746159 C2 RU2746159 C2 RU 2746159C2
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- Russia
- Prior art keywords
- phenyl
- isopropoxy
- methyl
- chloro
- piperidin
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- -1 2-isopropoxy-5-methyl-4-piperidine-4-yl-phenyl Chemical group 0.000 title description 22
- 239000013078 crystal Substances 0.000 title description 10
- YZVRDSIPTUIXBL-UHFFFAOYSA-N 4-(2-propan-2-ylsulfonylphenyl)-1h-pyrimidine-2,4-diamine Chemical compound CC(C)S(=O)(=O)C1=CC=CC=C1C1(N)C=CN=C(N)N1 YZVRDSIPTUIXBL-UHFFFAOYSA-N 0.000 title 1
- VERWOWGGCGHDQE-UHFFFAOYSA-N ceritinib Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCNCC1 VERWOWGGCGHDQE-UHFFFAOYSA-N 0.000 claims abstract description 47
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- WWVLDJAVSQZSKO-UHFFFAOYSA-N 2,5-dichloro-n-(2-propan-2-ylsulfonylphenyl)pyrimidin-4-amine Chemical compound CC(C)S(=O)(=O)C1=CC=CC=C1NC1=NC(Cl)=NC=C1Cl WWVLDJAVSQZSKO-UHFFFAOYSA-N 0.000 claims abstract description 4
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- GRRXEYVKIONDRW-UHFFFAOYSA-N 5-methyl-4-piperidin-4-yl-2-propan-2-yloxyaniline;dihydrochloride Chemical compound Cl.Cl.C1=C(N)C(OC(C)C)=CC(C2CCNCC2)=C1C GRRXEYVKIONDRW-UHFFFAOYSA-N 0.000 claims abstract 3
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- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 description 1
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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
- C07D401/02—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
-
- 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
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201061424194P | 2010-12-17 | 2010-12-17 | |
| US61/424,194 | 2010-12-17 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013132947A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016136823A RU2016136823A (ru) | 2018-12-11 |
| RU2016136823A3 RU2016136823A3 (enExample) | 2020-02-06 |
| RU2746159C2 true RU2746159C2 (ru) | 2021-04-08 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
| 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (36)
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2651918T (pt) | 2010-12-17 | 2017-10-17 | Novartis Ag | Formas cristalinas de 5-cloro-n2-(2-isopropoxi-5-metil-4-piperidin-4-il-fenil)-n4-[2-(propano-2-sulfonil)-fenil]-pirimidin-2,4-diamina |
| KR102156398B1 (ko) | 2012-11-06 | 2020-09-15 | 상하이 포천 파마슈티컬 씨오 엘티디 | Ａｌｋ 키나아제 억제제 |
| 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 |
| LT3209647T (lt) | 2014-10-21 | 2020-09-25 | Ariad Pharmaceuticals, Inc. | Kristalinės 5-chlor-n4-[-2-(dimetilfosforil)fenil]-n2-{2-metoksi-4-[4-(4-metilpiperazin-1-il) piperidin-1-il]pirimidin-2,4-diamino formos |
| WO2016081538A1 (en) | 2014-11-18 | 2016-05-26 | Teva Pharmaceuticals International Gmbh | Solid state forms of ceritinib and salts thereof |
| 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 |
| WO2016082795A1 (zh) * | 2014-11-28 | 2016-06-02 | 苏州晶云药物科技有限公司 | 色瑞替尼的晶型i及其制备方法 |
| 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 |
| WO2016108123A2 (en) * | 2014-12-17 | 2016-07-07 | Dr. Reddy’S Laboratories Limited | Pure amorphous and amorphous solid dispersion of ceritinib |
| WO2016098070A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Crystalline form of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2, 4-diamine |
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