SG10201408063SA - Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof - Google Patents
Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereofInfo
- Publication number
- SG10201408063SA SG10201408063SA SG10201408063SA SG10201408063SA SG10201408063SA SG 10201408063S A SG10201408063S A SG 10201408063SA SG 10201408063S A SG10201408063S A SG 10201408063SA SG 10201408063S A SG10201408063S A SG 10201408063SA SG 10201408063S A SG10201408063S A SG 10201408063SA
- Authority
- SG
- Singapore
- Prior art keywords
- piperazin
- dimethoxy
- ethyl
- crystalline forms
- phenylamino
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 3
- QADPYRIHXKWUSV-UHFFFAOYSA-N BGJ-398 Chemical compound C1CN(CC)CCN1C(C=C1)=CC=C1NC1=CC(N(C)C(=O)NC=2C(=C(OC)C=C(OC)C=2Cl)Cl)=NC=N1 QADPYRIHXKWUSV-UHFFFAOYSA-N 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 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 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000004683 dihydrates Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/495—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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- C07D403/10—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 carbon chain containing aromatic rings
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26715509P | 2009-12-07 | 2009-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG10201408063SA true SG10201408063SA (en) | 2015-01-29 |
Family
ID=43983750
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10201408063SA SG10201408063SA (en) | 2009-12-07 | 2010-12-06 | Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof |
Country Status (32)
Families Citing this family (56)
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| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| EP2830626B1 (en) * | 2012-03-30 | 2019-01-02 | Novartis AG | Fgfr inhibitor for use in the treatment of hypophosphatemic disorders |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| WO2014155268A2 (en) | 2013-03-25 | 2014-10-02 | Novartis Ag | Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| AU2014287209B2 (en) * | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| SG11201602069WA (en) * | 2013-10-18 | 2016-04-28 | Eisai R&D Man Co Ltd | Pyrimidine fgfr4 inhibitors |
| MY194303A (en) * | 2013-12-13 | 2022-11-27 | Novartis Ag | Pharmaceutical dosage forms |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| WO2016027781A1 (ja) | 2014-08-18 | 2016-02-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 単環ピリジン誘導体の塩およびその結晶 |
| WO2016055916A1 (en) | 2014-10-06 | 2016-04-14 | Novartis Ag | Therapeutic combination for the treatment of cancer |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016151501A1 (en) | 2015-03-25 | 2016-09-29 | Novartis Ag | Pharmaceutical combinations |
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| CN107660200B (zh) | 2015-04-14 | 2022-01-11 | 卫材R&D管理有限公司 | 结晶fgfr4抑制剂化合物和其用途 |
| CN104803925B (zh) * | 2015-04-16 | 2018-01-12 | 温州医科大学 | 一类以fgfr为靶点的2，4，5‑三取代嘧啶类化合物及其制备方法和用途 |
| WO2016189472A1 (en) | 2015-05-28 | 2016-12-01 | Novartis Ag | Fgfr inhibitor for use in the treatment of the phosphaturic mesenchymal tumor |
| AU2016374441B2 (en) | 2015-12-17 | 2021-10-21 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
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| BR112019003722A2 (pt) * | 2016-08-23 | 2019-05-28 | Eisai R&D Man Co Ltd | terapias de combinação para o tratamento de carcinoma hepatocelular |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN107176954B (zh) * | 2017-06-02 | 2019-01-11 | 无锡双良生物科技有限公司 | 一种egfr抑制剂的药用盐及其晶型、制备方法和应用 |
| AU2018361264B2 (en) | 2017-11-01 | 2021-04-01 | Guangdong Xianqiang Pharmaceutical Co., Ltd | Salt form and crystal form of compound as FGFR4 inhibitor and preparation method thereof |
| BR112020017922A2 (pt) | 2018-03-28 | 2020-12-22 | Eisai R&D Management Co., Ltd. | Agente terapêutico para carcinoma hepatocelular |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| CN119751422A (zh) * | 2019-10-14 | 2025-04-04 | 和记黄埔医药（上海）有限公司 | 化合物的盐及其晶型 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3202267A1 (en) * | 2020-12-18 | 2022-06-23 | Riccardo Panicucci | Methods of treating achondroplasia |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| US11583602B2 (en) | 2021-06-23 | 2023-02-21 | Kimtron, Inc. | System and method for ultra-close proximity irradiation of rotating biomass |
| WO2023174400A1 (zh) * | 2022-03-18 | 2023-09-21 | 上海润石医药科技有限公司 | 一种取代的氨基六元氮杂环类化合物的盐及其晶型、制备方法和应用 |
| CN115785001B (zh) * | 2022-11-23 | 2023-09-15 | 斯坦德药典标准物质研发(湖北)有限公司 | 一种英菲格拉替尼的制备方法 |
| WO2024186882A1 (en) | 2023-03-06 | 2024-09-12 | Qed Therapeutics, Inc. | Methods of treating skeletal dysplasias |
| AU2024345848A1 (en) * | 2023-09-18 | 2026-04-09 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Pharmaceutical composition containing heteroaryl oxynaphthalene compound, preparation method therefor, and use thereof |
| WO2025090870A1 (en) | 2023-10-27 | 2025-05-01 | Qed Therapeutics, Inc. | Infigratinib and metabolites thereof for use in methods of treating skeletal disorders |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| CN101242843A (zh) * | 2005-06-10 | 2008-08-13 | 詹森药业有限公司 | 作为激酶调节剂的氨基嘧啶类化合物 |
| US20070129353A1 (en) * | 2005-11-08 | 2007-06-07 | Michael Kahn | Alpha-helix mimetics and method relating to the treatment of cancer stem cells |
| ME00011A (me) * | 2005-12-21 | 2009-02-10 | Novartis Ag | Derivati pirimidinilaril uree kao fgf inhibitori |
| BRPI0911491A2 (pt) * | 2008-04-29 | 2016-01-05 | Novartis Ag | métodos de monitoramento da modulação de atividade de quinase de receptor de fator de crescimento de fibroblasto e usos dos ditos métodos. |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
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2010
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- 2010-12-05 JO JOP/2010/0433A patent/JO3061B1/ar active
- 2010-12-06 BR BR112012013784-0A patent/BR112012013784B1/pt active IP Right Grant
- 2010-12-06 DK DK10788479.3T patent/DK2509963T3/en active
- 2010-12-06 PE PE2012000772A patent/PE20121499A1/es active IP Right Grant
- 2010-12-06 SG SG10201408063SA patent/SG10201408063SA/en unknown
- 2010-12-06 MY MYPI2012002222A patent/MY158333A/en unknown
- 2010-12-06 TW TW099142438A patent/TWI526440B/zh active
- 2010-12-06 HU HUE10788479A patent/HUE026983T2/en unknown
- 2010-12-06 AU AU2010328391A patent/AU2010328391B2/en active Active
- 2010-12-06 US US13/514,308 patent/US9067896B2/en active Active
- 2010-12-06 CN CN201911273119.5A patent/CN111100078A/zh active Pending
- 2010-12-06 CN CN201911278014.9A patent/CN111269186A/zh active Pending
- 2010-12-06 CN CN2010800550783A patent/CN102639510A/zh active Pending
- 2010-12-06 RU RU2012128351/04A patent/RU2572848C2/ru active
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- 2010-12-06 CN CN201911272657.2A patent/CN111100077A/zh active Pending
- 2010-12-06 HR HRP20160126T patent/HRP20160126T1/hr unknown
- 2010-12-06 CN CN201510484635.8A patent/CN105061332A/zh active Pending
- 2010-12-06 NZ NZ600070A patent/NZ600070A/en unknown
- 2010-12-06 PH PH12014502593A patent/PH12014502593A1/en unknown
- 2010-12-06 WO PCT/US2010/059108 patent/WO2011071821A1/en not_active Ceased
- 2010-12-06 CA CA2781431A patent/CA2781431C/en active Active
- 2010-12-06 NZ NZ624315A patent/NZ624315A/en unknown
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- 2010-12-06 KR KR1020127017618A patent/KR101787784B1/ko active Active
- 2010-12-06 ES ES10788479.3T patent/ES2562462T3/es active Active
- 2010-12-06 MX MX2012006562A patent/MX2012006562A/es active IP Right Grant
- 2010-12-06 SI SI201031119A patent/SI2509963T1/sl unknown
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2012
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2015
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