TWI348468B - Process for preparing amino crotonyl compounds - Google Patents

Process for preparing amino crotonyl compounds

Info

Publication number: TWI348468B
Authority: TW; Taiwan
Prior art keywords: preparing amino; crotonyl compounds; compounds; amino crotonyl; preparing
Prior art date: 2003-10-17

Application number

TW093131395A

Other languages

English (en)

Other versions

TW200526644A (en

Inventor

Rainer Soyka

Werner Rall

Juergen Schnaubelt

Peter Sieger

Christian Kulinna

Original Assignee

Boehringer Ingelheim Int

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2003-10-17

Filing date

2004-10-15

Publication date

2011-09-11

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34428508&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI348468(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-10-15 Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int

2005-08-16 Publication of TW200526644A publication Critical patent/TW200526644A/zh

2011-09-11 Application granted granted Critical

2011-09-11 Publication of TWI348468B publication Critical patent/TWI348468B/zh

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Gastroenterology & Hepatology (AREA)
Urology & Nephrology (AREA)
Pulmonology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Pyrrole Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

TW093131395A 2003-10-17 2004-10-15 Process for preparing amino crotonyl compounds TWI348468B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
DE10349113A DE10349113A1 (de)	2003-10-17	2003-10-17	Verfahren zur Herstellung von Aminocrotonylverbindungen

Publications (2)

Publication Number	Publication Date
TW200526644A TW200526644A (en)	2005-08-16
TWI348468B true TWI348468B (en)	2011-09-11

Family

ID=34428508

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
TW093131395A TWI348468B (en)	2003-10-17	2004-10-15	Process for preparing amino crotonyl compounds
TW099147116A TWI373470B (en)	2003-10-17	2004-10-15	Process for preparing amino crotonyl compounds

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
TW099147116A TWI373470B (en)	2003-10-17	2004-10-15	Process for preparing amino crotonyl compounds

Country Status (34)

Country	Link
US (2)	US20050085495A1 (zh)
EP (2)	EP1678165B1 (zh)
JP (2)	JP4594317B2 (zh)
KR (2)	KR101282812B1 (zh)
CN (2)	CN101402631A (zh)
AR (1)	AR046118A1 (zh)
AU (2)	AU2004281938B2 (zh)
BR (2)	BRPI0415424B8 (zh)
CA (2)	CA2759063C (zh)
CY (2)	CY1114866T1 (zh)
DE (1)	DE10349113A1 (zh)
DK (2)	DK2508521T4 (zh)
EA (1)	EA016624B1 (zh)
EC (1)	ECSP066509A (zh)
ES (2)	ES2563211T5 (zh)
HR (2)	HRP20160246T4 (zh)
HU (1)	HUE028254T2 (zh)
IL (2)	IL174951A (zh)
ME (1)	ME00341B (zh)
MX (2)	MX338920B (zh)
MY (2)	MY149921A (zh)
NO (2)	NO333971B1 (zh)
NZ (2)	NZ547154A (zh)
PE (2)	PE20100267A1 (zh)
PL (2)	PL2508521T5 (zh)
PT (2)	PT1678165E (zh)
RS (3)	RS20060260A (zh)
SG (1)	SG139743A1 (zh)
SI (2)	SI2508521T2 (zh)
TW (2)	TWI348468B (zh)
UA (2)	UA91006C2 (zh)
UY (2)	UY28559A1 (zh)
WO (1)	WO2005037824A2 (zh)
ZA (1)	ZA200602234B (zh)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
MEP45508A (en)	1999-06-21	2011-02-10	Boehringer Ingelheim Pharma	Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
US7019012B2 (en)	2000-12-20	2006-03-28	Boehringer Ingelheim International Pharma Gmbh & Co. Kg	Quinazoline derivatives and pharmaceutical compositions containing them
DE10221018A1 (de) *	2002-05-11	2003-11-27	Boehringer Ingelheim Pharma	Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
US20050043233A1 (en) *	2003-04-29	2005-02-24	Boehringer Ingelheim International Gmbh	Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
DE10349113A1 (de) *	2003-10-17	2005-05-12	Boehringer Ingelheim Pharma	Verfahren zur Herstellung von Aminocrotonylverbindungen
KR100832594B1 (ko) *	2005-11-08	2008-05-27	한미약품 주식회사	다중저해제로서의 퀴나졸린 유도체 및 이의 제조방법
DK1948180T3 (da) *	2005-11-11	2013-05-27	Boehringer Ingelheim Int	Kombinationsbehandling af cancer omfattende EGFR/HER2 inhibitorer
WO2007054550A1 (en) *	2005-11-11	2007-05-18	Boehringer Ingelheim International Gmbh	Quinazoline derivatives for the treatment of cancer diseases
EP1981863B1 (en) *	2006-01-26	2012-10-10	Boehringer Ingelheim International GmbH	Process for preparing aminocrotonylamino-substituted quinazoline derivatives
NZ576065A (en) *	2006-09-18	2011-12-22	Boehringer Ingelheim Int	Method for treating cancer harboring egfr mutations
UY31867A (es) *	2008-06-06	2010-01-29	Boehringer Ingelheim Int	Nuevas formulaciones farmacéuticas sólidas que comprenden bibw 2992
US20120157472A1 (en)	2009-01-14	2012-06-21	Boehringer Ingelheim International Gmbh	Method for treating colorectal cancer
US9073916B2 (en)	2009-03-11	2015-07-07	Auckland Uniservices Limited	Prodrug forms of kinase inhibitors and their use in therapy
EP2429520A1 (en)	2009-05-14	2012-03-21	Boehringer Ingelheim International GmbH	New combination therapy in treatment of oncological and fibrotic diseases
RU2012103492A (ru) *	2009-07-02	2013-08-10	Ньюджен Терапьютикс, Инк.	Содержащие фосфор соединения хиназолина и способы применения
PT2451445T (pt)	2009-07-06	2019-07-10	Boehringer Ingelheim Int	Processo para secagem de bibw2992, dos seus sais e de formulações farmacêuticas sólidas compreendendo este ingrediente ativo
EP2509592A1 (en)	2009-12-07	2012-10-17	Boehringer Ingelheim International GmbH	Bibw 2992 for use in the treatment of triple negative breast cancer
US20120107304A1 (en)	2010-04-27	2012-05-03	Boehringer Ingelheim International Gmbh	Combination therapy in treatment of oncological and fibrotic diseases
NO2608792T3 (zh)	2010-08-26	2018-03-10
CN103476770B (zh) *	2010-11-25	2017-02-15	拉蒂欧制药有限责任公司	阿法替尼盐和多晶型物
SG10201913982WA (en)	2011-03-04	2020-03-30	Newgen Therapeutics Inc	Alkyne Substituted Quinazoline Compound And Methods Of Use
CN102731485B (zh) *	2011-04-02	2016-06-15	齐鲁制药有限公司	4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途
CN102918029B (zh) *	2011-05-17	2015-06-17	江苏康缘药业股份有限公司	4-苯胺-6-丁烯酰胺-7-烷醚喹唑啉衍生物及其制备方法和用途
US8828391B2 (en)	2011-05-17	2014-09-09	Boehringer Ingelheim International Gmbh	Method for EGFR directed combination treatment of non-small cell lung cancer
CN102838590B (zh) *	2011-06-21	2014-07-09	苏州迈泰生物技术有限公司	氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途
US20170079444A1 (en) *	2011-09-22	2017-03-23	Future Foam, Inc.	Enhanced washable mattress topper
US20150232457A1 (en)	2011-10-06	2015-08-20	Ratiopharm Gmbh	Crystalline forms of afatinib di-maleate
CN103073539B (zh) *	2011-10-26	2016-05-11	齐鲁制药有限公司	4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途
EP2875020B1 (en)	2012-07-19	2017-09-06	Boehringer Ingelheim International GmbH	Process for the preparation of a fumaric acid salt of 9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy- chinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one
US20150368230A1 (en)	2013-02-01	2015-12-24	Boehringer Ingelheim International Gmbh	Radiolabeled quinazoline derivatives
CN103254156B (zh) *	2013-05-10	2015-08-26	苏州明锐医药科技有限公司	阿法替尼中间体的制备方法
WO2014180271A1 (zh) *	2013-05-10	2014-11-13	苏州明锐医药科技有限公司	阿法替尼及其中间体的制备方法
CN103288808B (zh) *	2013-05-16	2015-11-11	苏州明锐医药科技有限公司	一种阿法替尼的制备方法
CN103242303B (zh) *	2013-05-16	2015-03-25	苏州明锐医药科技有限公司	阿法替尼的制备方法
WO2015007206A1 (zh) *	2013-07-16	2015-01-22	杭州普晒医药科技有限公司	阿法替尼酸加成盐及其晶型、其制备方法及药物组合物
CN104513229A (zh)	2013-09-28	2015-04-15	正大天晴药业集团股份有限公司	喹唑啉衍生物及其制备方法
CN104710413B (zh) *	2013-12-16	2019-05-03	江苏豪森药业集团有限公司	二马来酸阿法替尼的制备方法
CN104744445A (zh) *	2013-12-30	2015-07-01	广东东阳光药业有限公司	一种酪氨酸激酶抑制剂的晶型
US9242965B2 (en)	2013-12-31	2016-01-26	Boehringer Ingelheim International Gmbh	Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
WO2015103456A1 (en) *	2014-01-02	2015-07-09	Teva Pharmaceuticals International Gmbh	Crystalline forms of afatinib di-maleate
CN104803992A (zh) *	2014-01-25	2015-07-29	广东东阳光药业有限公司	阿法替尼盐的晶型
WO2016001844A1 (en) *	2014-06-30	2016-01-07	Sun Pharmaceutical Industries Limited	Amorphous form of afatinib dimaleate
CN105315263B (zh) *	2014-07-30	2018-11-27	正大天晴药业集团股份有限公司	阿法替尼中间体的合成方法
WO2016027243A1 (en) *	2014-08-21	2016-02-25	Dr. Reddy’S Laboratories Limited	Novel solid state forms of afatinib dimaleate
US10011591B2 (en) *	2014-10-01	2018-07-03	Sun Pharmaceutical Industries Limited	Crystalline form of afatinib dimaleate
CN105534920B (zh) *	2014-10-29	2020-07-10	江苏豪森药业集团有限公司	一种药物组合物及其制备方法
CN104402872B (zh) *	2014-11-14	2016-08-24	广东东阳光药业有限公司	一种结晶除杂方法
CN104447713B (zh) *	2014-11-18	2019-03-29	江苏奥赛康药业股份有限公司	阿法替尼化合物的制备方法
EP3023421A1 (en) *	2014-11-21	2016-05-25	Sandoz Ag	Crystalline forms of afatinib dimaleate
CN104529800B (zh) *	2014-12-08	2017-01-25	重庆威鹏药业有限公司	反式‑4‑二甲基氨基巴豆酸及盐的制备方法
CN105801567A (zh) *	2014-12-31	2016-07-27	徐州万邦金桥制药有限公司	一种双马来酸阿法替尼的纯化方法
CN105801568B (zh) *	2015-01-15	2019-07-30	杭州普晒医药科技有限公司	阿法替尼一马来酸盐晶型及其制备方法和药物组合物
HK1244278B (zh)	2015-03-20	2020-04-17	正大天晴药业集团股份有限公司	喹唑啉衍生物的盐及其制备方法
JP2018511646A (ja) *	2015-04-17	2018-04-26	ヘテロラボズリミテッドＨｅｔｅｒｏＬａｂｓＬｔｄ	多形体及びキナゾリニル誘導体の調製プロセス
CN105859641B (zh) *	2015-05-05	2018-11-16	杭州华东医药集团新药研究院有限公司	喹唑啉巴豆基化合物二马来酸盐的晶体及其制备方法和用途
CN104892584B (zh) *	2015-05-27	2018-03-23	重庆泰濠制药有限公司	一种阿法替尼双马来酸盐无定型态及其制备方法、制剂
AU2016276426B2 (en) *	2015-06-12	2019-12-05	Fresenius Kabi Oncology Ltd.	Polymorphic forms of Afatinib free base and Afatinib dimaleate
CN104926800A (zh) *	2015-06-26	2015-09-23	河北神威药业有限公司	一种阿法替尼二马来酸盐的结晶形式及其制备方法
CN105175331B (zh) *	2015-08-14	2019-04-26	江苏苏中药业集团股份有限公司	一种egfr类分子靶向抗肿瘤药物的制备方法
US10525059B2 (en)	2015-08-21	2020-01-07	Fresenius Kabi Oncology, Ltd.	Pharmaceutical compositions comprising Afatinib
WO2017093789A1 (en) *	2015-12-03	2017-06-08	Mylan Laboratories Ltd.	Polymorphic forms of afatinib dimaleate
CN106831733B (zh) *	2015-12-07	2021-05-11	海南先声药业有限公司	阿法替尼顺式异构体的制备方法与应用
CN106866641A (zh) *	2015-12-11	2017-06-20	河北神威药业有限公司	一种阿法替尼的精制方法
CN106916147A (zh) *	2015-12-25	2017-07-04	中美华世通生物医药科技（武汉）有限公司	化合物及其制备方法和用途
CN108430990B (zh) *	2015-12-25	2020-08-25	山东轩竹医药科技有限公司	喹唑啉衍生物的晶体及其制备方法
CN105669658B (zh) *	2016-04-05	2018-06-29	北京民康百草医药科技有限公司	一种阿法替尼的精制方法
CN107488194B (zh) *	2016-06-10	2021-07-30	山东新时代药业有限公司	一种阿法替尼中间体及其制备方法
CN107488153B (zh) *	2016-06-10	2020-06-23	山东新时代药业有限公司	一种阿法替尼中间体化合物
CN107488171B (zh) *	2016-06-10	2020-08-28	山东新时代药业有限公司	一种阿法替尼制备方法
CN107488172B (zh) *	2016-06-10	2020-06-12	山东新时代药业有限公司	一种阿法替尼的制备方法
CN106243092B (zh) *	2016-07-28	2019-02-15	南京臣功制药股份有限公司	一种高选择性制备马来酸阿法替尼的方法
US11446302B2 (en)	2016-11-17	2022-09-20	Board Of Regents, The University Of Texas System	Compounds with anti-tumor activity against cancer cells bearing EGFR or HER2 exon 20 mutations
TWI808958B (zh)	2017-01-25	2023-07-21	美商特普醫葯公司	涉及二芳基巨環化合物之組合療法
WO2018187643A1 (en)	2017-04-06	2018-10-11	Johnson Matthey Public Limited Company	Novel forms of afatinib dimaleate
CN108358900A (zh) *	2018-03-30	2018-08-03	东北制药集团股份有限公司	一种阿法替尼及其马来酸盐的制备方法
KR20190141607A (ko)	2018-06-14	2019-12-24	주식회사 에이티파머	알로페론을 포함하는 췌장암 치료용 조성물 및 치료 보조제
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CN114315808A (zh) *	2020-10-10	2022-04-12	西安新通药物研究有限公司	一种高收率马来酸阿法替尼的制备方法

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB8618846D0 (en)	1986-08-01	1986-09-10	Smithkline Beckman Corp	Chemical process
JPS6442472A (en)	1987-08-10	1989-02-14	Kanebo Ltd	Quinazoline derivative, production thereof and brain function disorder improving agent containing said derivative as active ingredient
GB9005014D0 (en) *	1990-03-06	1990-05-02	Janssen Pharmaceutica Nv	N.(4.piperidinyl)(dihydrobenzofuran or dihydro.2h.benzopyran)carboxamide derivatives
RU2043352C1 (ru) *	1991-07-01	1995-09-10	Пермский фармацевтический институт	2-пропил-3- (5-нитрофурфулиден)амино- 4(3н)-хиназолинон, проявляющий противостафилококковую и анальгетическую активность
AU661533B2 (en)	1992-01-20	1995-07-27	Astrazeneca Ab	Quinazoline derivatives
GB9401182D0 (en)	1994-01-21	1994-03-16	Inst Of Cancer The Research	Antibodies to EGF receptor and their antitumour effect
EP2163546B1 (en)	1995-03-30	2016-06-01	Pfizer Products Inc.	Quinazoline derivatives
GB9508538D0 (en)	1995-04-27	1995-06-14	Zeneca Ltd	Quinazoline derivatives
TR199800012T1 (xx)	1995-07-06	1998-04-21	Novartis Ag	Piroloprimidinler ve preparasyon i�in tatbikler.
DE69710712T3 (de)	1996-04-12	2010-12-23	Warner-Lambert Co. Llc	Umkehrbare inhibitoren von tyrosin kinasen
UA73073C2 (uk)	1997-04-03	2005-06-15	Уайт Холдінгз Корпорейшн	Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
ZA986732B (en)	1997-07-29	1999-02-02	Warner Lambert Co	Irreversible inhibitiors of tyrosine kinases
ZA986729B (en)	1997-07-29	1999-02-02	Warner Lambert Co	Irreversible inhibitors of tyrosine kinases
TW436485B (en)	1997-08-01	2001-05-28	American Cyanamid Co	Substituted quinazoline derivatives
RS49779B (sr)	1998-01-12	2008-06-05	Glaxo Group Limited,	Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
US6297258B1 (en)	1998-09-29	2001-10-02	American Cyanamid Company	Substituted 3-cyanoquinolines
US6262088B1 (en)	1998-11-19	2001-07-17	Berlex Laboratories, Inc.	Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
KR20020068261A (ko) *	1999-02-27	2002-08-27	베링거 잉겔하임 파르마 카게	티로신 키나제에 의해 매개되는 신호 변환에 대한 억제효과를 갖는 4-아미노-퀴나졸린 및 퀴놀린 유도체
DE19911366A1 (de)	1999-03-15	2000-09-21	Boehringer Ingelheim Pharma	Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19911509A1 (de)	1999-03-15	2000-09-21	Boehringer Ingelheim Pharma	Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
MEP45508A (en)	1999-06-21	2011-02-10	Boehringer Ingelheim Pharma	Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
US6627634B2 (en)	2000-04-08	2003-09-30	Boehringer Ingelheim Pharma Kg	Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
US20030158196A1 (en)	2002-02-16	2003-08-21	Boehringer Ingelheim Pharma Gmbh Co. Kg	Pharmaceutical compositions based on anticholinergics and EGFR kinase inhibitors
US7019012B2 (en)	2000-12-20	2006-03-28	Boehringer Ingelheim International Pharma Gmbh & Co. Kg	Quinazoline derivatives and pharmaceutical compositions containing them
DE10063435A1 (de)	2000-12-20	2002-07-04	Boehringer Ingelheim Pharma	Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE10204462A1 (de)	2002-02-05	2003-08-07	Boehringer Ingelheim Pharma	Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
US20030225079A1 (en)	2002-05-11	2003-12-04	Boehringer Ingelheim Pharma Gmbh & Co. Kg	Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy
DE10221018A1 (de)	2002-05-11	2003-11-27	Boehringer Ingelheim Pharma	Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
PE20040945A1 (es)	2003-02-05	2004-12-14	Warner Lambert Co	Preparacion de quinazolinas substituidas
US20050043233A1 (en)	2003-04-29	2005-02-24	Boehringer Ingelheim International Gmbh	Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
DE10349113A1 (de)	2003-10-17	2005-05-12	Boehringer Ingelheim Pharma	Verfahren zur Herstellung von Aminocrotonylverbindungen
US20060058311A1 (en)	2004-08-14	2006-03-16	Boehringer Ingelheim International Gmbh	Combinations for the treatment of diseases involving cell proliferation
WO2007054550A1 (en)	2005-11-11	2007-05-18	Boehringer Ingelheim International Gmbh	Quinazoline derivatives for the treatment of cancer diseases
DK1948180T3 (da)	2005-11-11	2013-05-27	Boehringer Ingelheim Int	Kombinationsbehandling af cancer omfattende EGFR/HER2 inhibitorer
EP1981863B1 (en)	2006-01-26	2012-10-10	Boehringer Ingelheim International GmbH	Process for preparing aminocrotonylamino-substituted quinazoline derivatives
NZ576065A (en)	2006-09-18	2011-12-22	Boehringer Ingelheim Int	Method for treating cancer harboring egfr mutations
US8022216B2 (en)	2007-10-17	2011-09-20	Wyeth Llc	Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
UY31867A (es)	2008-06-06	2010-01-29	Boehringer Ingelheim Int	Nuevas formulaciones farmacéuticas sólidas que comprenden bibw 2992
US20120157472A1 (en)	2009-01-14	2012-06-21	Boehringer Ingelheim International Gmbh	Method for treating colorectal cancer
PT2451445T (pt)	2009-07-06	2019-07-10	Boehringer Ingelheim Int	Processo para secagem de bibw2992, dos seus sais e de formulações farmacêuticas sólidas compreendendo este ingrediente ativo
EP2509592A1 (en)	2009-12-07	2012-10-17	Boehringer Ingelheim International GmbH	Bibw 2992 for use in the treatment of triple negative breast cancer
CN103476770B (zh)	2010-11-25	2017-02-15	拉蒂欧制药有限责任公司	阿法替尼盐和多晶型物
US20150232457A1 (en)	2011-10-06	2015-08-20	Ratiopharm Gmbh	Crystalline forms of afatinib di-maleate
WO2015007206A1 (zh)	2013-07-16	2015-01-22	杭州普晒医药科技有限公司	阿法替尼酸加成盐及其晶型、其制备方法及药物组合物
WO2016027243A1 (en)	2014-08-21	2016-02-25	Dr. Reddy’S Laboratories Limited	Novel solid state forms of afatinib dimaleate
CN104892584B (zh)	2015-05-27	2018-03-23	重庆泰濠制药有限公司	一种阿法替尼双马来酸盐无定型态及其制备方法、制剂
CN104926800A (zh)	2015-06-26	2015-09-23	河北神威药业有限公司	一种阿法替尼二马来酸盐的结晶形式及其制备方法

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Also Published As

Publication number	Publication date
NO333971B1 (no)	2013-11-04
ECSP066509A (es)	2006-10-10
MX338920B (es)	2016-05-06
RS20060260A (sr)	2008-06-05
RS60563B1 (sr)	2020-08-31
TWI373470B (en)	2012-10-01
BR122013033343B8 (pt)	2021-05-25
KR20120037987A (ko)	2012-04-20
CY1114866T1 (el)	2016-12-14
ES2563211T3 (es)	2016-03-11
UY28559A1 (es)	2005-05-31
SI2508521T1 (sl)	2016-03-31
EA016624B1 (ru)	2012-06-29
EP2508521A2 (de)	2012-10-10
CY1117279T1 (el)	2017-04-26
RS20130524A3 (en)	2015-08-31
IL216249A0 (en)	2011-12-29
PT2508521E (pt)	2016-03-31
JP4594317B2 (ja)	2010-12-08
IL174951A0 (en)	2006-08-20
KR20060120121A (ko)	2006-11-24
PE20100267A1 (es)	2010-04-21
JP5264830B2 (ja)	2013-08-14
WO2005037824A3 (de)	2005-07-21
AU2004281938B2 (en)	2011-04-14
MY155425A (en)	2015-10-15
EA200600604A1 (ru)	2006-10-27
MEP50808A (en)	2011-02-10
HRP20160246T4 (hr)	2022-11-11
UA91006C2 (ru)	2010-06-25
JP2007510624A (ja)	2007-04-26
TW200526644A (en)	2005-08-16
DK2508521T4 (da)	2022-10-03
PE20050965A1 (es)	2005-12-19
EP2508521B1 (de)	2015-12-30
EP2508521A3 (de)	2013-01-23
EP2508521B2 (de)	2022-09-07
SG139743A1 (en)	2008-02-29
CA2759063C (en)	2012-04-17
AR046118A1 (es)	2005-11-23
JP2010202668A (ja)	2010-09-16
PL2508521T3 (pl)	2016-06-30
HUE028254T2 (en)	2016-12-28
SI1678165T1 (sl)	2013-12-31
PL1678165T3 (pl)	2014-03-31
SI2508521T2 (sl)	2022-11-30
AU2011201171A1 (en)	2011-04-07
PL2508521T5 (pl)	2023-03-27
UA91401C2 (en)	2010-07-26
RS53398B (sr)	2014-10-31
CA2541928C (en)	2012-12-11
NO20062181L (no)	2006-05-15
CA2541928A1 (en)	2005-04-28
MY149921A (en)	2013-10-31
RS20130524A2 (sr)	2014-06-30
CN1867564B (zh)	2011-06-08
ME00341B (me)	2011-05-10
UY35979A (es)	2016-09-30
DE10349113A1 (de)	2005-05-12
ES2563211T5 (es)	2022-12-27
NO20130663L (no)	2006-05-15
KR101180752B1 (ko)	2012-09-10
HK1095817A1 (zh)	2007-05-18
EP1678165B1 (de)	2013-09-25
NZ583049A (en)	2011-08-26
CN101402631A (zh)	2009-04-08
CN1867564A (zh)	2006-11-22
US20070027170A1 (en)	2007-02-01
AU2004281938A1 (en)	2005-04-28
MXPA06004076A (es)	2006-06-27
KR101282812B1 (ko)	2013-07-05
ZA200602234B (en)	2007-09-26
HRP20131214T1 (hr)	2014-01-31
BRPI0415424B8 (pt)	2021-05-25
IL216249A (en)	2015-05-31
PT1678165E (pt)	2013-11-07
NZ547154A (en)	2010-02-26
IL174951A (en)	2012-03-29
HRP20160246T1 (hr)	2016-04-08
TW201118086A (en)	2011-06-01
US8426586B2 (en)	2013-04-23
DK2508521T3 (en)	2016-03-29
CA2759063A1 (en)	2005-04-28
WO2005037824A2 (de)	2005-04-28
AU2011201171B2 (en)	2012-02-09
ES2440466T3 (es)	2014-01-29
EP1678165A2 (de)	2006-07-12
US20050085495A1 (en)	2005-04-21
NO335103B1 (no)	2014-09-15
BR122013033343B1 (pt)	2020-10-13
BRPI0415424B1 (pt)	2019-01-22
DK1678165T3 (da)	2013-12-09
BRPI0415424A (pt)	2006-12-05

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