KR20050095898A - {6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일}-(3e)의동질다상체 - Google Patents
{6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일}-(3e)의동질다상체 Download PDFInfo
- Publication number
- KR20050095898A KR20050095898A KR1020057015068A KR20057015068A KR20050095898A KR 20050095898 A KR20050095898 A KR 20050095898A KR 1020057015068 A KR1020057015068 A KR 1020057015068A KR 20057015068 A KR20057015068 A KR 20057015068A KR 20050095898 A KR20050095898 A KR 20050095898A
- Authority
- KR
- South Korea
- Prior art keywords
- crystalline polymorph
- crystalline
- bis
- polymorph
- quinazolin
- Prior art date
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Classifications
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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
-
- 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
-
- 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
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
융점(T개시)/[℃] | |
동질다상체 E | 211 내지 214 |
동질다상체 A | 205 내지 208 |
동질다상체 B | 227 내지 231 |
융점(T개시)[℃] | 용액의 열에탄올/물 (45:55 g/g, 45℃)[kJ/mol] | |
동질다상체 E | 211 내지 214 | 56.9 내지 58.4 |
동질다상체 A | 205 내지 208 | 50.0 내지 55.6 |
동질다상체 B | 227 내지 231 | 61.2 내지 62.4 |
물 | 수성 완충액(pH 1) | |
동질다상체 E | 0.191% | 0.011% |
동질다상체 A | 0.194% | 0.017% |
동질다상체 B | 0.098% | 0.003% |
Claims (17)
- 대략 다음과 같은 2-세타(°)에서 나타나는 특징적 피크를 갖는 X-선 분말 회절 패턴에 의해 특징지어지는 [6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)아민 히드로클로라이드의 결정질 동질다상체:.
- 제 1 항에 있어서, 도 1 에 나타낸 X-선 분말 회절 패턴을 특징으로 하는 결정질 동질다상체.
- 대략 3277 cm-1, 3057 cm-1, 1627 cm-1, 1070 cm-1, 1022 cm-1, 892 cm-1, 873 cm-1, 850 cm-1, 780 cm-1, 745 cm-1, 725 cm-1, 652 cm- 1 의 cm- 1 에서 나타나는 특징적 피크를 갖는 IR 흡수 스펙트럼에 의해 특징지어지는 [6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)아민 히드로클로라이드의 결정질 동질다상체.
- 제 3 항에 있어서, 도 2 에 나타낸 IR 흡수 스펙트럼을 특징으로 하는 결정질 동질다상체.
- 융점이 211℃ 내지 214℃ 임을 특징으로 하는 [6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)아민 히드로클로라이드의 결정질 동질다상체.
- 70% 이상이 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체인 [6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)아민 히드로클로라이드 화합물.
- (α,α,α)-트리플루오로톨루엔에서 하기 화학식 Ⅱ의 화합물과 하기 화학식 Ⅲ의 화합물을 반응시키는 것을 포함하는, 제 1 항 내지 제 5 항 중 어느 한 항에 정의된 결정질 동질다상체의 제조 방법:[화학식 Ⅱ],[화학식 Ⅲ].
- 제 1 항 내지 제 5 항 중 어느 한 항에 있어서, 제 7 항에 따른 방법으로 제조된 결정질 동질다상체.
- 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체 및 약학적으로 허용되는 담체 및/또는 보강제를 포함하는 약학적 조성물.
- 제 1 항 내지 제 5 항 중 어느 한 항에 있어서, 치료적 활성 물질로서 사용되는 결정질 동질다상체.
- 제 1 항 내지 제 5 항 중 어느 한 항에 있어서, 표피 성장 인자 수용체와 관계된 질병의 치료 및/또는 예방을 위한 치료적 활성 물질로서 사용되는 결정질 동질다상체.
- 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체를 인간 또는 동물에 투여하는 것을 포함하는, 표피 성장 인자 수용체와 관계된 질병의 치료적 및/또는 예방적 처치, 특히 암의 치료적 및/또는 예방적 처치 방법.
- 표피 성장 인자 수용체와 관계된 질병의 치료적 및/또는 예방적 처치를 위한 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체의 용도.
- 암의 치료적 및/또는 예방적 처치를 위한 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체의 용도.
- 표피 성장 인자 수용체와 관계된 질병의 치료적 및/또는 예방적 처치용 약제의 제조를 위한 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체의 용도.
- 암의 치료적 및/또는 예방적 처치용 약제의 제조를 위한 제 1 항 내지 제 5 항 중 어느 한 항에 따른 결정질 동질다상체의 용도.
- 본원에서 정의된 바와 같은 발명.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03003587 | 2003-02-17 | ||
EP03003587.7 | 2003-02-17 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20050095898A true KR20050095898A (ko) | 2005-10-04 |
KR100797430B1 KR100797430B1 (ko) | 2008-01-23 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1020057015068A KR100797430B1 (ko) | 2003-02-17 | 2004-02-11 | {6,7-비스(2-메톡시-에톡시)-퀴나졸린-4-일}-(3e)의동질다상체 |
Country Status (24)
Country | Link |
---|---|
US (1) | US7148231B2 (ko) |
EP (1) | EP1597239B2 (ko) |
JP (1) | JP4456079B2 (ko) |
KR (1) | KR100797430B1 (ko) |
CN (1) | CN100506803C (ko) |
AT (1) | ATE408605T1 (ko) |
AU (1) | AU2004212067C1 (ko) |
BR (1) | BRPI0407520A (ko) |
CA (1) | CA2514977C (ko) |
CO (1) | CO5601019A2 (ko) |
DE (1) | DE602004016628D1 (ko) |
DK (1) | DK1597239T4 (ko) |
ES (1) | ES2314373T5 (ko) |
HR (1) | HRP20050707B1 (ko) |
IL (1) | IL169975A (ko) |
MX (1) | MXPA05008598A (ko) |
NO (1) | NO330781B1 (ko) |
NZ (1) | NZ541500A (ko) |
PL (1) | PL225428B1 (ko) |
PT (1) | PT1597239E (ko) |
RU (1) | RU2376294C2 (ko) |
SI (1) | SI1597239T2 (ko) |
WO (1) | WO2004072049A1 (ko) |
ZA (1) | ZA200506339B (ko) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101441930B1 (ko) * | 2007-04-04 | 2014-09-19 | 시플라 리미티드 | 에르로티닙 및 그의 약학적으로 허용가능한 염의 제조방법 |
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US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
US7625911B2 (en) * | 2005-01-12 | 2009-12-01 | Mai De Ltd. | Amorphous form of erlotinib hydrochloride and its solid amorphous dispersion |
CA2655061A1 (en) | 2006-06-27 | 2008-01-03 | Sandoz Ag | New method for salt preparation |
EP2054393A1 (en) | 2006-07-28 | 2009-05-06 | Synthon B.V. | Crystalline erlotinib |
US8372856B2 (en) | 2006-10-27 | 2013-02-12 | Synthon Bv | Hydrates of erlotinib hydrochloride |
PT2170844T (pt) * | 2007-02-21 | 2016-08-05 | Natco Pharma Ltd | Novos polimorfos de cloridrato de erlotinib e método de preparação |
EP2213665A1 (en) | 2007-08-17 | 2010-08-04 | Hetero Drugs Limited | Erlotinib hydrochloride |
TW200925152A (en) * | 2007-08-23 | 2009-06-16 | Plus Chemicals S A | Processes for the preparation of crystalline forms A, B and pure crystalline form a of erlotinib HCL |
US20090124642A1 (en) * | 2007-08-23 | 2009-05-14 | Augusto Canavesi | Crystalline forms of Erlotinib HCI and formulations thereof |
CA2730226A1 (en) * | 2008-07-07 | 2010-01-14 | Plus Chemicals Sa | Crystalline forms of erlotinib base and erlotinib hcl |
WO2010040212A1 (en) * | 2008-10-08 | 2010-04-15 | Apotex Pharmachem Inc. | Processes for the preparation of erlotinib hydrochloride |
EP2213281A1 (en) | 2009-02-02 | 2010-08-04 | Ratiopharm GmbH | Pharmaceutical composition comprising N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride |
US8440823B2 (en) | 2009-03-26 | 2013-05-14 | Ranbaxy Laboratories Limited | Process for the preparation of erlotinib or its pharmaceutically acceptable salts thereof |
EP2499118A2 (en) | 2009-11-12 | 2012-09-19 | Ranbaxy Laboratories Limited | Processes for the preparation of erlotinib hydrochloride form a and erlotinib hydrochloride form b |
CN101987834B (zh) * | 2010-06-13 | 2012-07-18 | 信泰制药(苏州)有限公司 | 一种结晶形态的盐酸埃罗替尼及其制备方法 |
CA2806273A1 (en) | 2010-07-23 | 2012-03-08 | Generics (Uk) Limited | Pure erlotinib |
WO2012150606A2 (en) | 2011-05-03 | 2012-11-08 | Cadila Healthcare Limited | A process for preparing stable polymophic form of erlotinib hydrochloride |
NZ630289A (en) | 2012-09-04 | 2016-08-26 | Shilpa Medicare Ltd | Crystalline erlotinib hydrochloride process |
WO2014118737A1 (en) | 2013-01-31 | 2014-08-07 | Ranbaxy Laboratories Limited | Erlotinib salts |
CN103333124B (zh) * | 2013-05-28 | 2015-03-25 | 埃斯特维华义制药有限公司 | 一种制备盐酸厄洛替尼晶型f的方法 |
WO2016082879A1 (en) * | 2014-11-27 | 2016-06-02 | Synthon B.V. | Pharmaceutical composition comprising erlotinib hydrochloride |
RU2610337C1 (ru) * | 2015-12-10 | 2017-02-09 | Индивидуальный предприниматель Михайлов Олег Ростиславович | Кристаллическая β-модификация N-(3-этинилфенил)-6,7-бис(2 метоксиэтокси)хиназолин-4-амин гидрохлорида, способ её получения и фармацевтическая композиция на её основе |
JP2019059685A (ja) * | 2017-09-26 | 2019-04-18 | 日本化薬株式会社 | エルロチニブを有効成分とする医薬錠剤 |
JP2020090456A (ja) * | 2018-12-05 | 2020-06-11 | 日本化薬株式会社 | エルロチニブを有効成分とする医薬錠剤 |
Family Cites Families (6)
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JPS6434574A (en) * | 1987-07-30 | 1989-02-06 | Mazda Motor | Full mold casting device |
DK0817775T3 (da) | 1995-03-30 | 2001-11-19 | Pfizer | Quinazolinderivater |
US5747498A (en) † | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
ATE295839T1 (de) | 1998-04-29 | 2005-06-15 | Osi Pharm Inc | N-(3-ethinylphenylamino)-6,7-bis(2-methoxyethox )-4-chinazolinamin-mesylat-anhydrat und -monohydrat |
RS49836B (sr) | 1999-03-31 | 2008-08-07 | Pfizer Products Inc., | Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja |
UA74803C2 (uk) | 1999-11-11 | 2006-02-15 | Осі Фармасьютікалз, Інк. | Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування |
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2004
- 2004-02-03 US US10/771,217 patent/US7148231B2/en not_active Expired - Lifetime
- 2004-02-11 NZ NZ541500A patent/NZ541500A/en not_active IP Right Cessation
- 2004-02-11 BR BRPI0407520-0A patent/BRPI0407520A/pt not_active Application Discontinuation
- 2004-02-11 AT AT04710031T patent/ATE408605T1/de active
- 2004-02-11 MX MXPA05008598A patent/MXPA05008598A/es active IP Right Grant
- 2004-02-11 PL PL378561A patent/PL225428B1/pl unknown
- 2004-02-11 ES ES04710031T patent/ES2314373T5/es not_active Expired - Lifetime
- 2004-02-11 RU RU2005128774/04A patent/RU2376294C2/ru active
- 2004-02-11 AU AU2004212067A patent/AU2004212067C1/en not_active Expired
- 2004-02-11 PT PT04710031T patent/PT1597239E/pt unknown
- 2004-02-11 EP EP04710031.8A patent/EP1597239B2/en not_active Expired - Lifetime
- 2004-02-11 JP JP2005518421A patent/JP4456079B2/ja not_active Expired - Lifetime
- 2004-02-11 WO PCT/EP2004/001244 patent/WO2004072049A1/en active IP Right Grant
- 2004-02-11 DE DE602004016628T patent/DE602004016628D1/de not_active Expired - Lifetime
- 2004-02-11 SI SI200430902T patent/SI1597239T2/sl unknown
- 2004-02-11 KR KR1020057015068A patent/KR100797430B1/ko active IP Right Grant
- 2004-02-11 CA CA2514977A patent/CA2514977C/en not_active Expired - Lifetime
- 2004-02-11 DK DK04710031.8T patent/DK1597239T4/da active
- 2004-02-11 CN CNB2004800043815A patent/CN100506803C/zh not_active Expired - Lifetime
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2005
- 2005-07-28 IL IL169975A patent/IL169975A/en active IP Right Grant
- 2005-08-08 ZA ZA200506339A patent/ZA200506339B/en unknown
- 2005-08-10 HR HRP20050707AA patent/HRP20050707B1/hr not_active IP Right Cessation
- 2005-08-18 CO CO05082094A patent/CO5601019A2/es not_active Application Discontinuation
- 2005-08-25 NO NO20053953A patent/NO330781B1/no unknown
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101441930B1 (ko) * | 2007-04-04 | 2014-09-19 | 시플라 리미티드 | 에르로티닙 및 그의 약학적으로 허용가능한 염의 제조방법 |
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