EA201001173A1 - 6,7-диалкокси хиназолиновые производные, эффективные для лечения нарушений, связанных с раком - Google Patents
6,7-диалкокси хиназолиновые производные, эффективные для лечения нарушений, связанных с ракомInfo
- Publication number
- EA201001173A1 EA201001173A1 EA201001173A EA201001173A EA201001173A1 EA 201001173 A1 EA201001173 A1 EA 201001173A1 EA 201001173 A EA201001173 A EA 201001173A EA 201001173 A EA201001173 A EA 201001173A EA 201001173 A1 EA201001173 A1 EA 201001173A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- surprising
- compounds
- hinazolin
- dialkoxi
- derivatives
- Prior art date
Links
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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Ввиду большого предложения соединений хиназолинового класса проведен синтез и скрининг большого количества новых химических структурных элементов с новыми структурными свойствами. Было удивительно и неожиданно обнаружить, что хиназолины, содержащие 3-этинил анилиновую группу в положении 4, и особенно замещенные алкоксигруппы в положениях 6 и 7 обеспечивают гораздо более сильные и особые антипролиферативные свойства по сравнению с другими известными членами хиназолинового класса лекарственных препаратов. Также удивительно, что соединения данного изобретения гораздо менее токсичны и профиль безопасности крайне благоприятен для терапевтических применений. Новые химические структурные единицы, описанные в данном изобретении, обозначены общей структурой (I) и не были синтезированы ранее или исследованы на их терапевтические эффекты и профиль безопасности. Соединение (I) представляет собой NRC-2694 в случае структуры (А).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IN2008/000036 WO2009090661A1 (en) | 2008-01-18 | 2008-01-18 | 6.7-dialkoxy ouinazoline derivatives useful for treatment of cancer related disorders |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201001173A1 true EA201001173A1 (ru) | 2011-04-29 |
EA018514B1 EA018514B1 (ru) | 2013-08-30 |
Family
ID=39769348
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201001173A EA018514B1 (ru) | 2008-01-18 | 2008-01-18 | 6,7-диалкокси хиназолиновые производные, эффективные для лечения нарушений, связанных с раком |
Country Status (27)
Country | Link |
---|---|
US (5) | US8143250B2 (ru) |
EP (2) | EP2229369B1 (ru) |
JP (1) | JP2011509995A (ru) |
KR (2) | KR101762306B1 (ru) |
CN (1) | CN101918374A (ru) |
AP (1) | AP2886A (ru) |
AU (1) | AU2008347940A1 (ru) |
BR (1) | BRPI0822012A2 (ru) |
CA (1) | CA2711737C (ru) |
CY (1) | CY1118193T1 (ru) |
DK (2) | DK3012251T3 (ru) |
EA (1) | EA018514B1 (ru) |
ES (2) | ES2642159T3 (ru) |
HR (1) | HRP20161522T1 (ru) |
HU (1) | HUE030640T2 (ru) |
IL (1) | IL207046A (ru) |
LT (1) | LT2229369T (ru) |
MA (1) | MA32081B1 (ru) |
MX (1) | MX2010007852A (ru) |
NZ (1) | NZ586946A (ru) |
PL (1) | PL2229369T3 (ru) |
PT (1) | PT2229369T (ru) |
SG (1) | SG187490A1 (ru) |
SI (1) | SI2229369T1 (ru) |
UA (1) | UA101010C2 (ru) |
WO (1) | WO2009090661A1 (ru) |
ZA (1) | ZA201005116B (ru) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
LT2229369T (lt) * | 2008-01-18 | 2016-09-26 | Natco Pharma Limited | 6,7-dialkoksi-chinazolino dariniai, tinkami panaudoti su vėžiu susijusių susirgimų gydymui |
US9050341B2 (en) * | 2009-07-14 | 2015-06-09 | Natco Pharma Limited | Methods of treating drug resistant and other tumors by administering 6,7-dialkoxy quinazoline derivatives |
CN101857618B (zh) * | 2010-06-13 | 2015-11-25 | 中国海洋大学 | 作为蛋白酪氨酸激酶抑制剂的一系列喹唑啉糖衍生物,其制备方法和应用 |
CN103874696B (zh) * | 2011-10-12 | 2015-06-03 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的喹唑啉衍生物及其使用方法 |
AR092289A1 (es) * | 2011-11-14 | 2015-04-15 | Sunshine Lake Pharma Co Ltd | Derivados de aminoquinazolina y sus sales y metodos de uso |
EP2796451B1 (en) * | 2011-12-20 | 2018-08-01 | Wei Qian | Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof |
US20150087687A1 (en) | 2012-03-23 | 2015-03-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
CN105916506B (zh) | 2013-11-20 | 2020-01-07 | 圣诺康生命科学公司 | 作为tam家族激酶抑制剂的喹唑啉衍生物 |
JP6740354B2 (ja) | 2015-10-05 | 2020-08-12 | ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
ES2899145T3 (es) | 2017-04-15 | 2022-03-10 | Natco Pharma Ltd | Un proceso mejorado para la preparación de diclorhidrato de N-(3-etinilfenil)-7-metoxi-6-(3-morfolinopropoxi)quinazolin-4-amina |
CN111499577A (zh) * | 2019-01-30 | 2020-08-07 | 华东师范大学 | 邻二苯基取代五元含氮芳杂环类类化合物及其应用 |
AU2022291015A1 (en) | 2021-06-10 | 2023-12-21 | Natco Pharma Limited | Egfr inhibitor for the treatment of head and neck cancer |
GB202108302D0 (en) * | 2021-06-10 | 2021-07-28 | Natco Pharma Ltd | New treatment |
CN115518071B (zh) * | 2021-06-24 | 2024-03-19 | 中国人民解放军联勤保障部队第九〇一医院 | 一种化合物在制备抗食管癌的药物中的应用 |
WO2024121861A1 (en) * | 2022-12-08 | 2024-06-13 | Natco Pharma Limited | Egfr inhibitor for the treatment of head and neck cancer |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US690221A (en) | 1901-06-20 | 1901-12-31 | Frederik Christian Viggo Arp | Stand for cycles. |
US5332671A (en) | 1989-05-12 | 1994-07-26 | Genetech, Inc. | Production of vascular endothelial cell growth factor and DNA encoding same |
US5183884A (en) | 1989-12-01 | 1993-02-02 | United States Of America | Dna segment encoding a gene for a receptor related to the epidermal growth factor receptor |
NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
US5811098A (en) | 1992-11-24 | 1998-09-22 | Bristol-Myers Squibb Company | Antibodies to HER4, human receptor tyrosine kinase |
GB9323290D0 (en) | 1992-12-10 | 1994-01-05 | Zeneca Ltd | Quinazoline derivatives |
GB9314884D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Tricyclic derivatives |
GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
DE122005000053I2 (de) | 1995-03-30 | 2008-01-17 | Pfizer Prod Inc | Chinazolinderivate |
GB9508538D0 (en) * | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
US5747498A (en) * | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
US6706721B1 (en) * | 1998-04-29 | 2004-03-16 | Osi Pharmaceuticals, Inc. | N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate |
UA74803C2 (ru) | 1999-11-11 | 2006-02-15 | Осі Фармасьютікалз, Інк. | Стойкий полиморф гидрохлорида n-(3-этинилфенил)-6,7-бис(2-метоксиэтокси)-4-хиназолинамина, способ его получения (варианты) и фармацевтическое применение |
WO2005070909A1 (en) | 2004-01-22 | 2005-08-04 | Natco Pharma Limited | An improved process for the preparation of gefitinib |
WO2006090413A1 (en) | 2005-02-23 | 2006-08-31 | Natco Pharma Limited | Novel crystalline form of gefitinib and a process for its preparation |
PE20070207A1 (es) | 2005-07-22 | 2007-03-09 | Genentech Inc | Tratamiento combinado de los tumores que expresan el her |
US7960545B2 (en) | 2005-11-23 | 2011-06-14 | Natco Pharma Limited | Process for the prepartion of erlotinib |
LT2229369T (lt) * | 2008-01-18 | 2016-09-26 | Natco Pharma Limited | 6,7-dialkoksi-chinazolino dariniai, tinkami panaudoti su vėžiu susijusių susirgimų gydymui |
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2008
- 2008-01-18 LT LTEP08720099.4T patent/LT2229369T/lt unknown
- 2008-01-18 US US12/812,726 patent/US8143250B2/en active Active
- 2008-01-18 ES ES15199926.5T patent/ES2642159T3/es active Active
- 2008-01-18 EP EP08720099.4A patent/EP2229369B1/en active Active
- 2008-01-18 HU HUE08720099A patent/HUE030640T2/en unknown
- 2008-01-18 DK DK15199926.5T patent/DK3012251T3/en active
- 2008-01-18 SI SI200831672A patent/SI2229369T1/sl unknown
- 2008-01-18 ES ES08720099.4T patent/ES2593321T3/es active Active
- 2008-01-18 PL PL08720099T patent/PL2229369T3/pl unknown
- 2008-01-18 BR BRPI0822012-3A patent/BRPI0822012A2/pt not_active Application Discontinuation
- 2008-01-18 CA CA2711737A patent/CA2711737C/en active Active
- 2008-01-18 AP AP2010005357A patent/AP2886A/xx active
- 2008-01-18 UA UAA201010197A patent/UA101010C2/ru unknown
- 2008-01-18 AU AU2008347940A patent/AU2008347940A1/en not_active Abandoned
- 2008-01-18 PT PT87200994T patent/PT2229369T/pt unknown
- 2008-01-18 WO PCT/IN2008/000036 patent/WO2009090661A1/en active Application Filing
- 2008-01-18 DK DK08720099.4T patent/DK2229369T3/en active
- 2008-01-18 KR KR1020167018317A patent/KR101762306B1/ko active IP Right Grant
- 2008-01-18 NZ NZ586946A patent/NZ586946A/en unknown
- 2008-01-18 CN CN2008801248191A patent/CN101918374A/zh active Pending
- 2008-01-18 EP EP15199926.5A patent/EP3012251B1/en active Active
- 2008-01-18 JP JP2010542740A patent/JP2011509995A/ja active Pending
- 2008-01-18 KR KR1020107015858A patent/KR101640161B1/ko active IP Right Grant
- 2008-01-18 EA EA201001173A patent/EA018514B1/ru unknown
- 2008-01-18 SG SG2013004064A patent/SG187490A1/en unknown
- 2008-01-18 MX MX2010007852A patent/MX2010007852A/es active IP Right Grant
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2010
- 2010-07-09 US US12/833,789 patent/US8921362B2/en active Active
- 2010-07-15 IL IL207046A patent/IL207046A/en active IP Right Grant
- 2010-07-19 ZA ZA2010/05116A patent/ZA201005116B/en unknown
- 2010-08-13 MA MA33089A patent/MA32081B1/fr unknown
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2014
- 2014-12-26 US US14/583,286 patent/US9481655B2/en active Active
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2016
- 2016-09-16 CY CY20161100921T patent/CY1118193T1/el unknown
- 2016-10-05 US US15/286,464 patent/US20170079983A1/en not_active Abandoned
- 2016-11-17 HR HRP20161522TT patent/HRP20161522T1/hr unknown
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2019
- 2019-03-11 US US16/298,944 patent/US20190201408A1/en not_active Abandoned
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