WO2001034574A1 - Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof - Google Patents
Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof Download PDFInfo
- Publication number
- WO2001034574A1 WO2001034574A1 PCT/US2000/031009 US0031009W WO0134574A1 WO 2001034574 A1 WO2001034574 A1 WO 2001034574A1 US 0031009 W US0031009 W US 0031009W WO 0134574 A1 WO0134574 A1 WO 0134574A1
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- WIPO (PCT)
- Prior art keywords
- polymorph
- methoxyethoxy
- bis
- ethynylphenyl
- compound
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- 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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- 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
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- 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
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- 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
- C07D239/88—Oxygen atoms
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- 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
Abstract
Description
Claims
Priority Applications (24)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
UA2002064754A UA74803C2 (en) | 1999-11-11 | 2000-09-11 | A stable polymorph of n-(3-ethynylphenyl)-6,7-bis(2-methoxyetoxy)-4-quinazolinamine hydrochloride, a method for producing thereof (variants) and pharmaceutical use |
AU17621/01A AU784243B2 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of N-(3-ethynylphenyl)-6,7-bis (2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
DE60041415T DE60041415D1 (en) | 1999-11-11 | 2000-11-09 | STABLE POLYMORPH OF N- (3-EHYNYLPHENYLAMINO) -6,7-BIS (2-METHOXYETHOXY) -4-CHINAZOLINE HYDROCHLORIDE, UTICAL APPLICATION |
BR0015544-6A BR0015544A (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n- (3-ethynylphenylamino) -6,7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride, production methods, and pharmaceutical uses thereof |
NZ518406A NZ518406A (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride useful in treating cancer |
JP2001536522A JP4689916B2 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of N- (3-ethynylphenylamino) -6,7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride |
EA200200546A EA005318B1 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
HU0302665A HU226857B1 (en) | 1999-11-11 | 2000-11-09 | Pharmaceutical compositions containing stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride |
MEP-2008-363A ME00328B (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
SI200031024T SI1233948T1 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
CA002389333A CA2389333C (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
EP00980346A EP1233948B1 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
IL14922200A IL149222A0 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynlamino)-6,7-bis (2-metoxyethoxy)- 4-quinaolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
DK00980346T DK1233948T3 (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of N- (3-ethynylphenylamino) -6,7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride, methods of preparation and pharmaceutical applications thereof |
APAP/P/2002/002542A AP1434A (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of N-(3-Ethynylphenylamino) -6, 7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof. |
MEP-363/08A MEP36308A (en) | 1999-11-11 | 2000-11-09 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis (2-methoxyethoxy)- 4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
SK581-2002A SK286995B6 (en) | 1999-11-11 | 2000-11-09 | Pharmaceutical composition adapted for solid oral administration comprising crystalline polymorph of N-(3-ethynylphenylamino)-6,7- bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride and its use |
NO20021910A NO327082B1 (en) | 1999-11-11 | 2002-04-23 | Pharmaceutical composition comprising stable polymorph of N- (3-ethynylphenylamino) -6,7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride |
IS6359A IS2612B (en) | 1999-11-11 | 2002-04-24 | Stable polymorph of N- (3-ethynylphenyl) -6,7-bis (2-methoxyethoxy) -4-quinazolinamine hydrochloride, methods of its preparation and use for pharmaceutical purposes. |
HRP20020388AA HRP20020388B1 (en) | 1999-11-11 | 2002-05-03 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-qui-nazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
BG106761A BG65880B1 (en) | 1999-11-11 | 2002-05-31 | Stable polymorph of n-3-ethynylphenylamino-6,7-bis 2-methoxyethoxy-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
HK03101231.4A HK1049663B (en) | 1999-11-11 | 2003-02-18 | Stable polymorph of n-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
AU2006201815A AU2006201815B2 (en) | 1999-11-11 | 2006-05-01 | Stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof |
IL177827A IL177827A (en) | 1999-11-11 | 2006-08-31 | Use of a crystalline polymorph of the hydrochloride salt of n-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine in combination with gemcitabine in the preparation of medicaments for treating pancreatic cancer |
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