CN101878218B - 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 - Google Patents
埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 Download PDFInfo
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- CN101878218B CN101878218B CN2009801006661A CN200980100666A CN101878218B CN 101878218 B CN101878218 B CN 101878218B CN 2009801006661 A CN2009801006661 A CN 2009801006661A CN 200980100666 A CN200980100666 A CN 200980100666A CN 101878218 B CN101878218 B CN 101878218B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61P13/00—Drugs for disorders of the urinary system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
- A61P17/16—Emollients or protectives, e.g. against radiation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
- 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
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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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- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- 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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- Urology & Nephrology (AREA)
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- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
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- Pain & Pain Management (AREA)
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- Obesity (AREA)
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- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims (23)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201410833295.0A CN104592242B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN2009801006661A CN101878218B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 |
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN200810132631.3 | 2008-07-08 | ||
CN200810132631 | 2008-07-08 | ||
CN200810132458.7 | 2008-07-17 | ||
CN200810132458 | 2008-07-17 | ||
CN200810188272.3 | 2008-12-23 | ||
CN200810188272 | 2008-12-23 | ||
CN2009801006661A CN101878218B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 |
PCT/CN2009/000773 WO2010003313A1 (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 |
Related Child Applications (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201210438377.6A Division CN102911179B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201410828693.3A Division CN104530061B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201210437345.4A Division CN103254204B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201410833295.0A Division CN104592242B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101878218A CN101878218A (zh) | 2010-11-03 |
CN101878218B true CN101878218B (zh) | 2013-01-02 |
Family
ID=41506667
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201410833295.0A Active CN104592242B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201210437345.4A Active CN103254204B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201210438377.6A Active CN102911179B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201410828693.3A Active CN104530061B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN2009801006661A Active CN101878218B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 |
Family Applications Before (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201410833295.0A Active CN104592242B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201210437345.4A Active CN103254204B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201210438377.6A Active CN102911179B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
CN201410828693.3A Active CN104530061B (zh) | 2008-07-08 | 2009-07-07 | 埃克替尼盐酸盐晶型、药物组合物和用途 |
Country Status (11)
Country | Link |
---|---|
US (2) | US8822482B2 (zh) |
EP (1) | EP2392576B1 (zh) |
JP (2) | JP5719770B2 (zh) |
KR (1) | KR20110031370A (zh) |
CN (5) | CN104592242B (zh) |
AU (1) | AU2009267683B2 (zh) |
CA (1) | CA2730311A1 (zh) |
HK (1) | HK1145319A1 (zh) |
IL (1) | IL210447A0 (zh) |
NZ (1) | NZ590334A (zh) |
WO (1) | WO2010003313A1 (zh) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8822482B2 (en) * | 2008-07-08 | 2014-09-02 | Beta Pharma, Inc. | Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof |
CN107721958A (zh) * | 2010-03-19 | 2018-02-23 | 北京强新生物科技有限公司 | 靶向癌症干细胞的新的化合物和组合物 |
SG187064A1 (en) * | 2010-07-14 | 2013-02-28 | Zhejiang Beta Pharma Inc | NOVEL FUSED HETEROCYCLIC DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS |
WO2012075210A2 (en) * | 2010-12-01 | 2012-06-07 | Niiki Pharma Inc. | Method for treating refractory cancer |
TWI505828B (zh) * | 2010-12-20 | 2015-11-01 | 葛蘭素史克智慧財產(第二)有限公司 | 新穎醫藥組成物 |
ES2641953T3 (es) * | 2011-10-31 | 2017-11-14 | Beta Pharmaceuticals Co., Ltd. | Métodos de preparación de Icotinib e hidrocloruro de Icotinib, e intermediarios de los mismos |
EP2752413B1 (en) * | 2012-03-26 | 2016-03-23 | Fujian Institute Of Research On The Structure Of Matter, Chinese Academy Of Sciences | Quinazoline derivative and application thereof |
WO2014028914A1 (en) * | 2012-08-17 | 2014-02-20 | Beta Pharma, Inc. | Deuterated icotinib derivatives |
US9994574B2 (en) * | 2012-11-12 | 2018-06-12 | Victoria Link Limited | Salt and polymorphic forms of (3R,4S)-L-((4-amino-5H-pyrrolo[3,2,-d]pyrimidin-7-yl)methyl)-4(methylthiomethyl)pyrodin-3-ol(MTDIA) |
KR101672223B1 (ko) * | 2012-12-28 | 2016-11-04 | 베타 파머수티컬 컴퍼니 리미티드 | 아이코티닙, 아이코티닙 하이드로클로라이드 및 이의 중간체의 제조방법 |
ES2638646T3 (es) | 2013-06-09 | 2017-10-23 | Betta Pharmaceuticals Co., Ltd. | Nuevas formas polimorfas de fosfato de Icotinib y utilizaciones de las mismas |
CN104470929B (zh) * | 2013-06-09 | 2018-11-30 | 贝达药业股份有限公司 | 埃克替尼的晶型及其应用 |
WO2014198210A1 (en) * | 2013-06-09 | 2014-12-18 | Betta Pharmaceuticals Co., Ltd | Polymorph forms of icotinib maleate and uses thereof |
KR101804449B1 (ko) * | 2013-06-09 | 2017-12-04 | 베타 파머수티컬 컴퍼니 리미티드 | 아이코티닙의 다형체 형태 및 이의 용도 |
CN104487443B (zh) * | 2013-06-09 | 2016-03-23 | 贝达药业股份有限公司 | 埃克替尼马来酸盐的晶型及其用途 |
CN104470526B (zh) * | 2013-06-09 | 2016-07-13 | 贝达药业股份有限公司 | 埃克替尼磷酸盐的晶型及其用途 |
CA2926874C (en) * | 2013-10-11 | 2018-12-11 | Yinxiang Wang | Icotinib-containing topical skin pharmaceutical compositions and uses thereof |
CN109512779A (zh) * | 2013-10-11 | 2019-03-26 | 贝达药业股份有限公司 | 一种含埃克替尼的皮肤外用药物组合物及其应用 |
CN103784412A (zh) * | 2014-01-15 | 2014-05-14 | 青岛市肿瘤医院 | 一种盐酸埃克替尼分散片及其制备方法 |
CN103860521A (zh) * | 2014-03-05 | 2014-06-18 | 王栾秋 | 盐酸埃克替尼胶囊组合物及其制备方法 |
CN106924739B (zh) * | 2017-03-10 | 2022-07-29 | 上海交通大学医学院 | Egfr抑制剂在制备治疗muc1阳性肿瘤药物中的应用 |
CN111362957B (zh) * | 2020-04-21 | 2022-02-18 | 上海百利佳生医药科技有限公司 | 一种埃克替尼关键中间体的制备方法 |
CN111909163B (zh) * | 2020-04-21 | 2022-02-01 | 南开大学 | 具有ido1抑制功能的喹啉胺类化合物及其制备方法 |
CN111763214B (zh) * | 2020-08-10 | 2022-03-15 | 苏州富士莱医药股份有限公司 | 一种埃克替尼的制备方法 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1534026A (zh) * | 2002-03-28 | 2004-10-06 | �Ϳ���ҽҩ��˾ | 新型作为酪氨酸激酶抑制剂的稠合的喹唑啉衍生物 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002338577A (ja) | 2001-05-15 | 2002-11-27 | Orient Chem Ind Ltd | 分子内架橋クラウンエーテル環を有するフタロシアニン誘導体及びその製造方法 |
US8822482B2 (en) * | 2008-07-08 | 2014-09-02 | Beta Pharma, Inc. | Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof |
-
2009
- 2009-07-07 US US13/003,216 patent/US8822482B2/en not_active Expired - Fee Related
- 2009-07-07 KR KR1020117002841A patent/KR20110031370A/ko not_active Application Discontinuation
- 2009-07-07 CA CA2730311A patent/CA2730311A1/en not_active Abandoned
- 2009-07-07 CN CN201410833295.0A patent/CN104592242B/zh active Active
- 2009-07-07 CN CN201210437345.4A patent/CN103254204B/zh active Active
- 2009-07-07 EP EP09793788.2A patent/EP2392576B1/en not_active Not-in-force
- 2009-07-07 JP JP2011516948A patent/JP5719770B2/ja active Active
- 2009-07-07 AU AU2009267683A patent/AU2009267683B2/en not_active Ceased
- 2009-07-07 WO PCT/CN2009/000773 patent/WO2010003313A1/zh active Application Filing
- 2009-07-07 CN CN201210438377.6A patent/CN102911179B/zh active Active
- 2009-07-07 CN CN201410828693.3A patent/CN104530061B/zh active Active
- 2009-07-07 CN CN2009801006661A patent/CN101878218B/zh active Active
- 2009-07-07 NZ NZ590334A patent/NZ590334A/xx not_active IP Right Cessation
-
2010
- 2010-12-07 HK HK10111360.7A patent/HK1145319A1/xx unknown
-
2011
- 2011-01-03 IL IL210447A patent/IL210447A0/en unknown
-
2014
- 2014-07-31 US US14/448,070 patent/US9359370B2/en active Active
-
2015
- 2015-02-13 JP JP2015026902A patent/JP2015110649A/ja active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1534026A (zh) * | 2002-03-28 | 2004-10-06 | �Ϳ���ҽҩ��˾ | 新型作为酪氨酸激酶抑制剂的稠合的喹唑啉衍生物 |
Also Published As
Publication number | Publication date |
---|---|
AU2009267683B2 (en) | 2014-04-03 |
US20140343082A1 (en) | 2014-11-20 |
JP2011527291A (ja) | 2011-10-27 |
NZ590334A (en) | 2012-12-21 |
CN101878218A (zh) | 2010-11-03 |
JP2015110649A (ja) | 2015-06-18 |
CN104592242A (zh) | 2015-05-06 |
WO2010003313A1 (zh) | 2010-01-14 |
WO2010003313A8 (zh) | 2010-04-22 |
IL210447A0 (en) | 2011-03-31 |
CN104530061B (zh) | 2017-05-10 |
CN103254204B (zh) | 2014-10-22 |
AU2009267683A1 (en) | 2010-01-14 |
JP5719770B2 (ja) | 2015-05-20 |
CN103254204A (zh) | 2013-08-21 |
CA2730311A1 (en) | 2010-01-14 |
CN102911179B (zh) | 2015-04-08 |
EP2392576A1 (en) | 2011-12-07 |
CN104592242B (zh) | 2017-01-25 |
KR20110031370A (ko) | 2011-03-25 |
US8822482B2 (en) | 2014-09-02 |
CN104530061A (zh) | 2015-04-22 |
US20110182882A1 (en) | 2011-07-28 |
US9359370B2 (en) | 2016-06-07 |
CN102911179A (zh) | 2013-02-06 |
EP2392576A4 (en) | 2012-04-11 |
EP2392576B1 (en) | 2016-02-17 |
HK1145319A1 (en) | 2011-04-15 |
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