UA73588C2 - Polymorph forms/hydrates of dihydrochloride of n-[4-(3-chloro-4-flurophenylamino)-7-(3-morpholine-4-ylpropoxy)quinazoline-6-yl]-acrylamide and a method for the preparation thereof - Google Patents
Polymorph forms/hydrates of dihydrochloride of n-[4-(3-chloro-4-flurophenylamino)-7-(3-morpholine-4-ylpropoxy)quinazoline-6-yl]-acrylamide and a method for the preparation thereof Download PDFInfo
- Publication number
- UA73588C2 UA73588C2 UA2003010793A UA2003010793A UA73588C2 UA 73588 C2 UA73588 C2 UA 73588C2 UA 2003010793 A UA2003010793 A UA 2003010793A UA 2003010793 A UA2003010793 A UA 2003010793A UA 73588 C2 UA73588 C2 UA 73588C2
- Authority
- UA
- Ukraine
- Prior art keywords
- dihydrochloride
- water
- ylpropoxy
- dihydrochloride according
- chloro
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract description 18
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 150000004677 hydrates Chemical class 0.000 title claims abstract description 11
- 230000002427 irreversible effect Effects 0.000 claims abstract description 4
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims abstract description 3
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims abstract description 3
- 230000002401 inhibitory effect Effects 0.000 claims abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 29
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 20
- 238000001228 spectrum Methods 0.000 claims description 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 11
- 239000000843 powder Substances 0.000 claims description 9
- 239000012458 free base Substances 0.000 claims description 8
- 238000001035 drying Methods 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 238000002425 crystallisation Methods 0.000 claims description 6
- 230000008025 crystallization Effects 0.000 claims description 6
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 6
- 239000013078 crystal Substances 0.000 claims description 5
- 229940126601 medicinal product Drugs 0.000 claims description 4
- 238000004090 dissolution Methods 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000012050 conventional carrier Substances 0.000 claims 1
- 238000007796 conventional method Methods 0.000 claims 1
- 238000001704 evaporation Methods 0.000 claims 1
- 230000008020 evaporation Effects 0.000 claims 1
- 238000012876 topography Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 4
- 239000000047 product Substances 0.000 description 11
- 230000010354 integration Effects 0.000 description 10
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- 238000003756 stirring Methods 0.000 description 8
- 239000011149 active material Substances 0.000 description 5
- 238000000921 elemental analysis Methods 0.000 description 5
- 238000001159 Fisher's combined probability test Methods 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000000706 filtrate Substances 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- USFZMSVCRYTOJT-UHFFFAOYSA-N Ammonium acetate Chemical compound N.CC(O)=O USFZMSVCRYTOJT-UHFFFAOYSA-N 0.000 description 1
- 239000005695 Ammonium acetate Substances 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
- 201000009273 Endometriosis Diseases 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 238000002083 X-ray spectrum Methods 0.000 description 1
- IXUZXIMQZIMPSQ-ZBRNBAAYSA-N [(4s)-4-amino-4-carboxybutyl]azanium;(2s)-2-amino-4-hydroxy-4-oxobutanoate Chemical compound OC(=O)[C@@H](N)CCC[NH3+].[O-]C(=O)[C@@H](N)CC(O)=O IXUZXIMQZIMPSQ-ZBRNBAAYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 229940043376 ammonium acetate Drugs 0.000 description 1
- 235000019257 ammonium acetate Nutrition 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 235000013405 beer Nutrition 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 239000001110 calcium chloride Substances 0.000 description 1
- 229910001628 calcium chloride Inorganic materials 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000001061 forehead Anatomy 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000053 physical method Methods 0.000 description 1
- 238000002601 radiography Methods 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10031971A DE10031971A1 (de) | 2000-06-30 | 2000-06-30 | Polymorphe Formen/Hydrate von N-[4-(3-Chlor-4-fluor-phenylamino)-7-(3-morpholin-4-yl-propoxy)-chinazolin-6-yl]-acrylamid Dihydrochlorid, Verfahren zu ihrer Herstellung sowie die Verwendung derselben zur Herstellung von Medikamenten mit irreversibler Tyrosinkinasehemmwirkung |
| PCT/EP2001/006733 WO2002000630A1 (en) | 2000-06-30 | 2001-06-15 | Polymorphic forms/hydrates of n-[4-(3-chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)-quinazolin-6-yl]-acrylamide dihydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA73588C2 true UA73588C2 (en) | 2005-08-15 |
Family
ID=7647397
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2003010793A UA73588C2 (en) | 2000-06-30 | 2001-06-15 | Polymorph forms/hydrates of dihydrochloride of n-[4-(3-chloro-4-flurophenylamino)-7-(3-morpholine-4-ylpropoxy)quinazoline-6-yl]-acrylamide and a method for the preparation thereof |
Country Status (39)
| Country | Link |
|---|---|
| US (1) | US20040034022A1 (es) |
| EP (1) | EP1299363A1 (es) |
| JP (1) | JP2004501902A (es) |
| KR (1) | KR20030014403A (es) |
| CN (1) | CN1438994A (es) |
| AP (1) | AP2002002694A0 (es) |
| AR (1) | AR031854A1 (es) |
| AU (1) | AU2001283861A1 (es) |
| BG (1) | BG107352A (es) |
| BR (1) | BR0112082A (es) |
| CA (1) | CA2412535A1 (es) |
| CZ (1) | CZ20024037A3 (es) |
| DE (1) | DE10031971A1 (es) |
| DZ (1) | DZ3342A1 (es) |
| EA (1) | EA005294B1 (es) |
| EC (1) | ECSP024413A (es) |
| EE (1) | EE200200714A (es) |
| GT (1) | GT200100124A (es) |
| HN (1) | HN2001000134A (es) |
| HR (1) | HRP20021019A2 (es) |
| HU (1) | HUP0300900A3 (es) |
| IL (1) | IL152419A0 (es) |
| IS (1) | IS6596A (es) |
| MA (1) | MA26924A1 (es) |
| MX (1) | MXPA03000101A (es) |
| NO (1) | NO20026193L (es) |
| NZ (1) | NZ522001A (es) |
| OA (1) | OA12301A (es) |
| PA (1) | PA8520801A1 (es) |
| PE (1) | PE20020116A1 (es) |
| PL (1) | PL365127A1 (es) |
| SK (1) | SK17642002A3 (es) |
| SV (1) | SV2002000517A (es) |
| TN (1) | TNSN01090A1 (es) |
| UA (1) | UA73588C2 (es) |
| UY (1) | UY26803A1 (es) |
| WO (1) | WO2002000630A1 (es) |
| YU (1) | YU99802A (es) |
| ZA (1) | ZA200209717B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005239878B9 (en) * | 2004-05-06 | 2010-01-07 | Warner-Lambert Company Llc | 4-phenylamino-quinazolin-6-yl-amides |
| DE102006000122A1 (de) * | 2006-03-17 | 2007-09-20 | Aug. Winkhaus Gmbh & Co. Kg | Schlüssel für einen Schließzylinder und Schließzylinder für einen solchen Schlüssel |
| JP6674027B2 (ja) * | 2015-12-25 | 2020-04-01 | シュアンチュー ファーマ カンパニー，リミティド | キナゾリン誘導体の結晶及びその調製方法 |
| JP6717947B2 (ja) * | 2015-12-25 | 2020-07-08 | シュアンチュー ファーマ カンパニー，リミティド | キナゾリン誘導体の結晶及びその調製方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL190489B1 (pl) * | 1996-04-12 | 2005-12-30 | Warner Lambert Co | Nieodwracalne inhibitory kinaz tyrozyny, kompozycja farmaceutyczna je zawierająca i ich zastosowanie |
| EE200100271A (et) * | 1998-11-19 | 2002-10-15 | Warner-Lambert Company | N-[4-(3-kloro-4-fluorofenüülamino)-7-(3-morfoliin-4-üülpropoksü)kinasoliin-6-üül]ak rüülamiid kui türosiinkinaaside pöördumatu inhibiitor |
-
2000
- 2000-06-30 DE DE10031971A patent/DE10031971A1/de not_active Withdrawn
-
2001
- 2001-06-15 HU HU0300900A patent/HUP0300900A3/hu unknown
- 2001-06-15 YU YU99802A patent/YU99802A/sh unknown
- 2001-06-15 US US10/312,173 patent/US20040034022A1/en not_active Abandoned
- 2001-06-15 UA UA2003010793A patent/UA73588C2/uk unknown
- 2001-06-15 PL PL01365127A patent/PL365127A1/xx not_active Application Discontinuation
- 2001-06-15 WO PCT/EP2001/006733 patent/WO2002000630A1/en active IP Right Grant
- 2001-06-15 JP JP2002505378A patent/JP2004501902A/ja not_active Withdrawn
- 2001-06-15 NZ NZ522001A patent/NZ522001A/en unknown
- 2001-06-15 CZ CZ20024037A patent/CZ20024037A3/cs unknown
- 2001-06-15 IL IL15241901A patent/IL152419A0/xx unknown
- 2001-06-15 EP EP01962739A patent/EP1299363A1/en not_active Withdrawn
- 2001-06-15 MX MXPA03000101A patent/MXPA03000101A/es unknown
- 2001-06-15 TN TNTNSN01090A patent/TNSN01090A1/fr unknown
- 2001-06-15 DZ DZ013342A patent/DZ3342A1/fr active
- 2001-06-15 AP APAP/P/2002/002694A patent/AP2002002694A0/en unknown
- 2001-06-15 OA OA1200200394A patent/OA12301A/fr unknown
- 2001-06-15 CN CN01811998A patent/CN1438994A/zh active Pending
- 2001-06-15 AU AU2001283861A patent/AU2001283861A1/en not_active Abandoned
- 2001-06-15 SK SK1764-2002A patent/SK17642002A3/sk unknown
- 2001-06-15 KR KR1020027017829A patent/KR20030014403A/ko not_active Application Discontinuation
- 2001-06-15 EE EEP200200714A patent/EE200200714A/xx unknown
- 2001-06-15 BR BR0112082-4A patent/BR0112082A/pt not_active IP Right Cessation
- 2001-06-15 CA CA002412535A patent/CA2412535A1/en not_active Abandoned
- 2001-06-15 EA EA200300094A patent/EA005294B1/ru not_active IP Right Cessation
- 2001-06-21 PA PA20018520801A patent/PA8520801A1/es unknown
- 2001-06-25 GT GT200100124A patent/GT200100124A/es unknown
- 2001-06-26 PE PE2001000623A patent/PE20020116A1/es not_active Application Discontinuation
- 2001-06-26 HN HN2001000134A patent/HN2001000134A/es unknown
- 2001-06-27 UY UY26803A patent/UY26803A1/es not_active Application Discontinuation
- 2001-06-29 SV SV2001000517A patent/SV2002000517A/es not_active Application Discontinuation
- 2001-06-29 AR ARP010103135A patent/AR031854A1/es unknown
-
2002
- 2002-10-28 IS IS6596A patent/IS6596A/is unknown
- 2002-11-29 ZA ZA200209717A patent/ZA200209717B/en unknown
- 2002-12-04 BG BG107352A patent/BG107352A/bg unknown
- 2002-12-19 HR HR20021019A patent/HRP20021019A2/xx not_active Application Discontinuation
- 2002-12-23 NO NO20026193A patent/NO20026193L/no not_active Application Discontinuation
- 2002-12-30 MA MA26984A patent/MA26924A1/fr unknown
- 2002-12-30 EC EC2002004413A patent/ECSP024413A/es unknown
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