CN102838550A - 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 - Google Patents
喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 Download PDFInfo
- Publication number
- CN102838550A CN102838550A CN2012100785900A CN201210078590A CN102838550A CN 102838550 A CN102838550 A CN 102838550A CN 2012100785900 A CN2012100785900 A CN 2012100785900A CN 201210078590 A CN201210078590 A CN 201210078590A CN 102838550 A CN102838550 A CN 102838550A
- Authority
- CN
- China
- Prior art keywords
- cancer
- quinazoline
- prodrug
- metabolism
- bolites
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 0 CC(Nc1c(cc(c(O*)c2)NC(C=CCN*)=O)c2ncn1)=CC(Cl)=C Chemical compound CC(Nc1c(cc(c(O*)c2)NC(C=CCN*)=O)c2ncn1)=CC(Cl)=C 0.000 description 1
- IZCDASYZDZJINB-SNAWJCMRSA-N Cc1cc(Nc2c(cc(c(OC(F)F)c3)NC(/C=C/CN(C)C)=O)c3ncn2)ccc1F Chemical compound Cc1cc(Nc2c(cc(c(OC(F)F)c3)NC(/C=C/CN(C)C)=O)c3ncn2)ccc1F IZCDASYZDZJINB-SNAWJCMRSA-N 0.000 description 1
Images
Classifications
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D405/14—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 three or more hetero rings
Abstract
Description
肿瘤细胞系 | IC50(μM) |
A431 | 0.652 |
BT474 | 0.034 |
H292 | 2.65 |
H1975 | 0.80 |
Hcc827 | 0.002 |
MDA-MB-231 | 大于10000 |
SK-Br-3 | 0.23 |
A549 | 3.722 |
H1650 | 3.238 |
H1734 | 0.539 |
Claims (10)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201210078590.0A CN102838550B (zh) | 2011-06-21 | 2012-03-23 | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 |
PCT/CN2013/072528 WO2013135176A1 (zh) | 2012-03-16 | 2013-03-13 | 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201110166370.9 | 2011-06-21 | ||
CN201110166370 | 2011-06-21 | ||
CN201210078590.0A CN102838550B (zh) | 2011-06-21 | 2012-03-23 | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN102838550A true CN102838550A (zh) | 2012-12-26 |
CN102838550B CN102838550B (zh) | 2014-10-01 |
Family
ID=47366310
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201210069348.7A Active CN102838590B (zh) | 2011-06-21 | 2012-03-16 | 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
CN201210078590.0A Active CN102838550B (zh) | 2011-06-21 | 2012-03-23 | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201210069348.7A Active CN102838590B (zh) | 2011-06-21 | 2012-03-16 | 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
Country Status (2)
Country | Link |
---|---|
US (1) | US20150065709A1 (zh) |
CN (2) | CN102838590B (zh) |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103288808A (zh) * | 2013-05-16 | 2013-09-11 | 苏州明锐医药科技有限公司 | 一种阿法替尼的制备方法 |
WO2013135176A1 (zh) * | 2012-03-16 | 2013-09-19 | 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 |
CN104151359A (zh) * | 2014-07-15 | 2014-11-19 | 杭州华东医药集团新药研究院有限公司 | 喹唑啉类化合物及其制备方法和在制备酪氨酸激酶抑制剂中的应用 |
CN105777655A (zh) * | 2014-12-25 | 2016-07-20 | 深圳海王药业有限公司 | 萘普替尼对甲苯磺酸盐的α晶型及制备方法和含有其的药物组合物 |
CN105777656A (zh) * | 2014-12-25 | 2016-07-20 | 深圳海王药业有限公司 | 萘普替尼对甲苯磺酸盐的β晶型及制备方法和含有其的药物组合物 |
CN105859641A (zh) * | 2015-05-05 | 2016-08-17 | 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 |
CN106432105A (zh) * | 2016-08-26 | 2017-02-22 | 苏州汉酶生物技术有限公司 | 一种迈华替尼的化学合成方法 |
CN108779079A (zh) * | 2016-01-06 | 2018-11-09 | 特里乌姆治疗公司 | 作为egfr抑制剂的新的氟化喹唑啉衍生物 |
WO2020011020A1 (zh) * | 2018-07-10 | 2020-01-16 | 杭州华东医药集团生物医药有限公司 | 迈华替尼组合物、相关化合物及其制备方法和用途 |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106146412B (zh) * | 2015-03-31 | 2019-05-24 | 广州市恒诺康医药科技有限公司 | 喹唑啉衍生物及其制备方法和应用 |
CN104774184A (zh) * | 2015-04-17 | 2015-07-15 | 中国药科大学 | α-氰基-α,β-不饱和酰胺类化合物及其医药用途 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1867564A (zh) * | 2003-10-17 | 2006-11-22 | 贝林格尔·英格海姆国际有限公司 | 氨基巴豆基化合物的制备方法 |
CN1972688A (zh) * | 2004-05-06 | 2007-05-30 | 沃尼尔·朗伯有限责任公司 | 4-苯胺基-喹唑啉-6-基-酰胺类化合物 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6626899B2 (en) * | 1999-06-25 | 2003-09-30 | Nidus Medical, Llc | Apparatus and methods for treating tissue |
US6653305B2 (en) * | 2000-08-26 | 2003-11-25 | Boehringer Ingelheim Pharma Kg | Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them |
DE10063435A1 (de) * | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
DE102005005505A1 (de) * | 2005-02-04 | 2006-08-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung der chronischen Rhinosinusitis |
DK2068880T3 (da) * | 2006-09-18 | 2012-07-23 | Boehringer Ingelheim Int | Fremgangsmåde til behandling af cancer, der huser EGFR-mutationer |
CN101824029A (zh) * | 2009-03-05 | 2010-09-08 | 厦门艾德生物医药科技有限公司 | 酪氨酸激酶不可逆抑制剂、其药物组合物及其用途 |
CN105541836A (zh) * | 2009-03-11 | 2016-05-04 | 奥克兰联合服务有限公司 | 激酶抑制剂的前药形式及其在治疗中的用途 |
-
2012
- 2012-03-16 CN CN201210069348.7A patent/CN102838590B/zh active Active
- 2012-03-23 CN CN201210078590.0A patent/CN102838550B/zh active Active
-
2013
- 2013-03-13 US US14/385,734 patent/US20150065709A1/en not_active Abandoned
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1867564A (zh) * | 2003-10-17 | 2006-11-22 | 贝林格尔·英格海姆国际有限公司 | 氨基巴豆基化合物的制备方法 |
CN1972688A (zh) * | 2004-05-06 | 2007-05-30 | 沃尼尔·朗伯有限责任公司 | 4-苯胺基-喹唑啉-6-基-酰胺类化合物 |
Cited By (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013135176A1 (zh) * | 2012-03-16 | 2013-09-19 | 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 |
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 |
CN103288808A (zh) * | 2013-05-16 | 2013-09-11 | 苏州明锐医药科技有限公司 | 一种阿法替尼的制备方法 |
CN107141261A (zh) * | 2014-07-15 | 2017-09-08 | 杭州华东医药集团新药研究院有限公司 | 喹唑啉类化合物及其制备方法和在制备酪氨酸激酶抑制剂中的应用 |
CN104151359A (zh) * | 2014-07-15 | 2014-11-19 | 杭州华东医药集团新药研究院有限公司 | 喹唑啉类化合物及其制备方法和在制备酪氨酸激酶抑制剂中的应用 |
CN107141261B (zh) * | 2014-07-15 | 2020-05-05 | 杭州华东医药集团新药研究院有限公司 | 喹唑啉类化合物及其制备方法和在制备酪氨酸激酶抑制剂中的应用 |
CN105777656B (zh) * | 2014-12-25 | 2018-02-02 | 深圳海王医药科技研究院有限公司 | 萘普替尼对甲苯磺酸盐的β晶型及制备方法和含有其的药物组合物 |
CN105777656A (zh) * | 2014-12-25 | 2016-07-20 | 深圳海王药业有限公司 | 萘普替尼对甲苯磺酸盐的β晶型及制备方法和含有其的药物组合物 |
CN105777655A (zh) * | 2014-12-25 | 2016-07-20 | 深圳海王药业有限公司 | 萘普替尼对甲苯磺酸盐的α晶型及制备方法和含有其的药物组合物 |
CN105777655B (zh) * | 2014-12-25 | 2018-02-02 | 深圳海王医药科技研究院有限公司 | 萘普替尼对甲苯磺酸盐的α晶型及制备方法和含有其的药物组合物 |
US10065931B2 (en) | 2015-05-05 | 2018-09-04 | Hangzhou Huadong Medicine Group Biopharmaceutical Co. Ltd. | Quinazolin crotyl compound dimaleate crystals and preparation methods and uses thereof |
CN105859641A (zh) * | 2015-05-05 | 2016-08-17 | 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 |
JP2018515508A (ja) * | 2015-05-05 | 2018-06-14 | 杭州華東医薬集団新薬研究院有限公司 | キナゾリンクロチル化合物二マレイン酸塩結晶、ならびに、その調製方法および使用 |
WO2016177308A1 (zh) * | 2015-05-05 | 2016-11-10 | 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 |
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 |
US10640470B2 (en) | 2015-05-05 | 2020-05-05 | Hangzhou Huadong Medicine Group Biopharmaceutical Co. Ltd. | Quinazolin crotyl compound dimaleate crystals and preparation methods and uses thereof |
CN108779079A (zh) * | 2016-01-06 | 2018-11-09 | 特里乌姆治疗公司 | 作为egfr抑制剂的新的氟化喹唑啉衍生物 |
EP3400216A4 (en) * | 2016-01-06 | 2019-08-14 | Trillium Therapeutics Inc. | NOVEL FLUORINATED QUINAZOLINE DERIVATIVES AS INHIBITORS OF EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) |
CN106432105B (zh) * | 2016-08-26 | 2019-06-11 | 苏州汉酶生物技术有限公司 | 一种迈华替尼的化学合成方法 |
CN106432105A (zh) * | 2016-08-26 | 2017-02-22 | 苏州汉酶生物技术有限公司 | 一种迈华替尼的化学合成方法 |
WO2020011020A1 (zh) * | 2018-07-10 | 2020-01-16 | 杭州华东医药集团生物医药有限公司 | 迈华替尼组合物、相关化合物及其制备方法和用途 |
Also Published As
Publication number | Publication date |
---|---|
CN102838590B (zh) | 2014-07-09 |
CN102838550B (zh) | 2014-10-01 |
CN102838590A (zh) | 2012-12-26 |
US20150065709A1 (en) | 2015-03-05 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN102838550B (zh) | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 | |
US11007197B2 (en) | EGFR modulators and uses thereof | |
CN105254615B (zh) | 苯胺嘧啶衍生物及其在制备抗恶性肿瘤药物中的用途 | |
CN104350049B (zh) | 作为激酶抑制剂的取代氨基喹唑啉 | |
JPWO2015030021A1 (ja) | ピリミジン化合物を有効成分とする医薬組成物 | |
CN110372669A (zh) | 一种基于crbn配体诱导egfr降解的化合物及其制备方法、药物组合物和应用 | |
US10774079B2 (en) | Quinazoline derivative | |
CN105980377B (zh) | 作为egfr-t790m激酶抑制剂的取代的嘧啶类化合物 | |
WO2016023217A1 (zh) | 喹唑啉衍生物、其制备方法、药物组合物和应用 | |
TW200410695A (en) | Quinazolinone derivatives useful as anti-hyperalgesic agents | |
WO2019031472A1 (ja) | 新規アントラニル酸系化合物、並びにそれを用いたPin1阻害剤、炎症性疾患の治療剤及び癌の治療剤 | |
CN102838539A (zh) | 喹啉烯酰胺衍生物及其在制备抗恶性肿瘤药物中的用途 | |
CN101967142B (zh) | 噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途 | |
CN112300082B (zh) | 一种苯基哌嗪喹唑啉类化合物或其药学上可接受的盐、制法与用途 | |
WO2015021894A1 (zh) | 新型羟肟酸衍生物及其医疗应用 | |
WO2014063631A1 (zh) | 酪氨酸激酶不可逆抑制剂及其制备方法和用途 | |
US11465986B2 (en) | Crystal form of c-MET inhibitor and salt form thereof and preparation method therefor | |
CN113444074A (zh) | 一种具有EGFR和Wnt双重抑制作用的化合物及其制备方法和应用 | |
JP2022527279A (ja) | キノリン誘導体及び癌の治療のためのその使用 | |
JP2017511348A (ja) | Bcr−Abl二倍体の阻害剤、その調製方法及びその用途 | |
WO2023030492A1 (zh) | 一种ep4拮抗剂化合物及其盐、多晶型和用途 | |
CN101175732B (zh) | 一种喹唑啉衍生物的制备方法及用作制备治疗肿瘤疾病药物的应用 | |
CN105037399B (zh) | 一类Bcr‑Abl双倍体抑制剂及制备方法与用途 | |
CN110294706A (zh) | 抗肿瘤药物及其制法和用途 | |
WO2013135176A1 (zh) | 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
C41 | Transfer of patent application or patent right or utility model | ||
TR01 | Transfer of patent right |
Effective date of registration: 20151127 Address after: 215600 Zhangjiagang, Suzhou, Cathay Pacific North Road, building F, No., building 2, building 1 Patentee after: Metabomics Inc. Patentee after: HANGZHOU HUADONG MEDICINE GROUP NEW MEDICINE RESEARCH INSTITUTE CO., LTD. Patentee after: Zhongmei Huadong Pharmaceutical Co., Ltd., Hangzhou Address before: 215600 Zhangjiagang, Suzhou, Cathay Pacific North Road, building F, No., building 2, building 1 Patentee before: Metabomics Inc. |