SG11201901962QA - Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof - Google Patents
Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereofInfo
- Publication number
- SG11201901962QA SG11201901962QA SG11201901962QA SG11201901962QA SG11201901962QA SG 11201901962Q A SG11201901962Q A SG 11201901962QA SG 11201901962Q A SG11201901962Q A SG 11201901962QA SG 11201901962Q A SG11201901962Q A SG 11201901962QA SG 11201901962Q A SG11201901962Q A SG 11201901962QA
- Authority
- SG
- Singapore
- Prior art keywords
- preparation
- crystalline form
- formula
- compound
- method therefor
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 238000002360 preparation method Methods 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- 101000715361 Streptomyces griseus Zinc carboxypeptidase Proteins 0.000 abstract 1
- 238000011031 large-scale manufacturing process Methods 0.000 abstract 1
- 239000002075 main ingredient Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
CPSG 0133P00457P01 58 POLYMORPHIC FORMS OF KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING SAME, PREPARATION METHOD THEREFOR AND USE THEREOF 5 The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or 10 crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production. 15 formula I (Fig. 1) NH F O NH O NH N N O
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610866253 | 2016-09-29 | ||
| PCT/CN2017/104506 WO2018059556A1 (en) | 2016-09-29 | 2017-09-29 | Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201901962QA true SG11201901962QA (en) | 2019-04-29 |
Family
ID=61763329
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201901962QA SG11201901962QA (en) | 2016-09-29 | 2017-09-29 | Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US11053224B2 (en) |
| EP (1) | EP3502105B8 (en) |
| JP (2) | JP7253491B2 (en) |
| KR (1) | KR102289684B1 (en) |
| CN (1) | CN108884080B (en) |
| AU (1) | AU2017336889B2 (en) |
| BR (1) | BR112019006023A2 (en) |
| CA (1) | CA3035124A1 (en) |
| EA (1) | EA201990688A1 (en) |
| ES (1) | ES2914294T3 (en) |
| HK (1) | HK1257194A1 (en) |
| IL (2) | IL265266B1 (en) |
| MY (1) | MY194364A (en) |
| PH (1) | PH12019500681A1 (en) |
| PL (1) | PL3502105T3 (en) |
| SG (1) | SG11201901962QA (en) |
| TW (1) | TWI647224B (en) |
| WO (1) | WO2018059556A1 (en) |
| ZA (1) | ZA201901717B (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI647224B (en) * | 2016-09-29 | 2019-01-11 | 大陸商貝達藥業股份有限公司 | Polymorph of kinase inhibitor compound, pharmaceutical composition containing same, preparation method and application thereof |
| PL3884929T3 (en) | 2020-03-25 | 2023-10-09 | Ocular Therapeutix, Inc. | Ocular implant containing a tyrosine kinase inhibitor |
| JP2024511348A (en) * | 2021-03-16 | 2024-03-13 | エイチケー イノ．エヌ コーポレーション | Crystal forms of heterocyclic compounds as protein kinase inhibitors |
| JP7138982B1 (en) * | 2021-09-24 | 2022-09-20 | 東海物産株式会社 | Anserine crystals and method for producing the same |
| WO2023173088A1 (en) | 2022-03-11 | 2023-09-14 | EyePoint Pharmaceuticals, Inc. | Method of preventing age-related macular degeneration by administering an ocular drug delivery insert |
| WO2023173093A1 (en) | 2022-03-11 | 2023-09-14 | EyePoint Pharmaceuticals, Inc. | Continuous dosing regimen for treatment of a condition of the eye |
| TW202345804A (en) | 2022-03-11 | 2023-12-01 | 美商視點製藥有限公司 | Method of treating wet age-related macular degeneration |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6642232B2 (en) * | 2001-10-10 | 2003-11-04 | Sugen, Inc. | 3-[4-Substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2- indolinone derivatives as kinase inhibitors |
| CA2662902C (en) * | 2006-09-15 | 2015-11-24 | Xcovery, Inc. | Kinase inhibitor compounds |
| EP2145505A1 (en) * | 2007-05-07 | 2010-01-20 | Baumer Electric AG | Acoustic transducer |
| US20100256392A1 (en) * | 2007-11-21 | 2010-10-07 | Teva Pharmaceutical Industries Ltd. | Polymorphs of sunitinib base and processes for preparation thereof |
| EP2280960A1 (en) * | 2008-04-16 | 2011-02-09 | Natco Pharma Limited | Novel polymorphic forms of sunitinib base |
| RU2468022C2 (en) * | 2008-05-23 | 2012-11-27 | Шанхай Инститьют Оф Фармасьютикал Индастри | Dihydroindolone derivatives |
| EP2186809A1 (en) | 2008-11-13 | 2010-05-19 | LEK Pharmaceuticals D.D. | New crystal form of sunitinib malate |
| EP2264027A1 (en) * | 2009-05-27 | 2010-12-22 | Ratiopharm GmbH | Process for the preparation of N-[2-(Diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide |
| CN106928114B (en) * | 2015-12-31 | 2020-07-28 | 韶远科技（上海)有限公司 | Cyclic chiral amino compound containing carbamido group and its amplifying process and use |
| TWI647224B (en) * | 2016-09-29 | 2019-01-11 | 大陸商貝達藥業股份有限公司 | Polymorph of kinase inhibitor compound, pharmaceutical composition containing same, preparation method and application thereof |
-
2017
- 2017-09-29 TW TW106133830A patent/TWI647224B/en active
- 2017-09-29 EA EA201990688A patent/EA201990688A1/en unknown
- 2017-09-29 SG SG11201901962QA patent/SG11201901962QA/en unknown
- 2017-09-29 IL IL265266A patent/IL265266B1/en unknown
- 2017-09-29 PL PL17855006T patent/PL3502105T3/en unknown
- 2017-09-29 CN CN201780008042.1A patent/CN108884080B/en active Active
- 2017-09-29 EP EP17855006.7A patent/EP3502105B8/en active Active
- 2017-09-29 JP JP2019538551A patent/JP7253491B2/en active Active
- 2017-09-29 KR KR1020197008752A patent/KR102289684B1/en active IP Right Grant
- 2017-09-29 AU AU2017336889A patent/AU2017336889B2/en active Active
- 2017-09-29 BR BR112019006023A patent/BR112019006023A2/en unknown
- 2017-09-29 US US16/338,357 patent/US11053224B2/en active Active
- 2017-09-29 IL IL311631A patent/IL311631A/en unknown
- 2017-09-29 ES ES17855006T patent/ES2914294T3/en active Active
- 2017-09-29 MY MYPI2019000596A patent/MY194364A/en unknown
- 2017-09-29 WO PCT/CN2017/104506 patent/WO2018059556A1/en unknown
- 2017-09-29 CA CA3035124A patent/CA3035124A1/en active Pending
-
2018
- 2018-12-18 HK HK18116171.7A patent/HK1257194A1/en unknown
-
2019
- 2019-03-19 ZA ZA201901717A patent/ZA201901717B/en unknown
- 2019-03-28 PH PH12019500681A patent/PH12019500681A1/en unknown
-
2021
- 2021-06-15 US US17/348,482 patent/US20220356173A1/en active Pending
-
2023
- 2023-03-28 JP JP2023052465A patent/JP2023082086A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN108884080B (en) | 2020-10-27 |
| EP3502105B1 (en) | 2022-03-30 |
| EP3502105B8 (en) | 2022-06-01 |
| CN108884080A (en) | 2018-11-23 |
| JP7253491B2 (en) | 2023-04-06 |
| IL265266B1 (en) | 2024-04-01 |
| BR112019006023A2 (en) | 2019-06-18 |
| AU2017336889B2 (en) | 2021-11-25 |
| EP3502105A1 (en) | 2019-06-26 |
| JP2023082086A (en) | 2023-06-13 |
| CA3035124A1 (en) | 2018-04-05 |
| KR102289684B1 (en) | 2021-08-12 |
| ZA201901717B (en) | 2019-11-27 |
| TW201815785A (en) | 2018-05-01 |
| US20190233403A1 (en) | 2019-08-01 |
| ES2914294T3 (en) | 2022-06-08 |
| KR20190039823A (en) | 2019-04-15 |
| PH12019500681A1 (en) | 2019-11-25 |
| US11053224B2 (en) | 2021-07-06 |
| AU2017336889A1 (en) | 2019-04-11 |
| WO2018059556A1 (en) | 2018-04-05 |
| JP2019529568A (en) | 2019-10-17 |
| TWI647224B (en) | 2019-01-11 |
| EA201990688A1 (en) | 2019-08-30 |
| PL3502105T3 (en) | 2022-07-11 |
| US20220356173A1 (en) | 2022-11-10 |
| MY194364A (en) | 2022-11-29 |
| EP3502105A4 (en) | 2020-04-15 |
| IL311631A (en) | 2024-05-01 |
| HK1257194A1 (en) | 2019-10-18 |
| IL265266A (en) | 2019-05-30 |
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