RU2017132330A - Соли производного хиназолина и способ их получения - Google Patents
Соли производного хиназолина и способ их получения Download PDFInfo
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- RU2017132330A RU2017132330A RU2017132330A RU2017132330A RU2017132330A RU 2017132330 A RU2017132330 A RU 2017132330A RU 2017132330 A RU2017132330 A RU 2017132330A RU 2017132330 A RU2017132330 A RU 2017132330A RU 2017132330 A RU2017132330 A RU 2017132330A
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- Prior art keywords
- formula
- compound
- maleate
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- pharmaceutical composition
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
-
- 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
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Plural Heterocyclic Compounds (AREA)
Claims (12)
1. Малеат соединения формулы I,
2. Малеат соединения формулы I по п. 1, в котором молярное отношение соединения формулы I к малеиновой кислоте составляет 1:0,5-4.
3. Малеат соединения формулы I по п. 2, в котором молярное отношение соединения формулы I к малеиновой кислоте составляет 1:1 или 1:2.
4. Способ получения малеата соединения формулы I по любому из пп. 1-3, включающий (1) получение раствора соединения формулы I; (2) смешивание раствора соединения формулы I, полученного из стадии (1), с малеиновой кислотой; и (3) высушивание распылением реакционной смеси, полученной из стадии (2), с получением малеата соединения формулы I.
5. Способ по п. 4, при котором молярное отношение количества соединения формулы I к количеству малеиновой кислоты составляет 1:1-20, предпочтительно 1:1-15 и более предпочтительно 1:1-10.
6. Способ по п. 4, при котором на стадии (1) соединение формулы I растворяют в органическом растворителе для получения раствора соединения формулы I, и органический растворитель представляет собой предпочтительно DMF.
7. Способ по п. 6, при котором растворитель, смешивающийся с органическим растворителем, добавляют перед высушиванием распылением, и растворитель, смешивающийся с органическим растворителем, представляет собой предпочтительно воду.
8. Фармацевтическая композиция, содержащая малеат соединения формулы I по любому из пп. 1-3 и фармацевтически приемлемый носитель, вспомогательное вещество, разбавитель и/или основу.
9. Применение малеата соединения формулы I по любому из пп. 1-3 или фармацевтической композиции по п. 8 в получении лекарственного средства для лечения опухоли.
10. Способ лечения опухоли, включающий введение малеата соединения формулы I по любому из пп. 1-3 или фармацевтической композиции по п. 8 нуждающемуся в этом субъекту.
11. Применение малеата соединения формулы I по любому из пп. 1-3 или фармацевтической композиции по п. 8 для лечения опухоли.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510125962 | 2015-03-20 | ||
| CN201510125962.4 | 2015-03-20 | ||
| PCT/CN2016/076693 WO2016150340A1 (zh) | 2015-03-20 | 2016-03-18 | 喹唑啉衍生物的盐及其制备方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2017132330A true RU2017132330A (ru) | 2019-04-22 |
| RU2017132330A3 RU2017132330A3 (ru) | 2019-07-24 |
| RU2720810C2 RU2720810C2 (ru) | 2020-05-13 |
Family
ID=56977000
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017132330A RU2720810C2 (ru) | 2015-03-20 | 2016-03-18 | Соли производного хиназолина и способ их получения |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10231973B2 (ru) |
| EP (1) | EP3272746B1 (ru) |
| JP (1) | JP6704422B2 (ru) |
| CN (1) | CN107406430B (ru) |
| ES (1) | ES2775614T3 (ru) |
| HK (1) | HK1244278B (ru) |
| RU (1) | RU2720810C2 (ru) |
| WO (1) | WO2016150340A1 (ru) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3505516B1 (en) * | 2016-08-25 | 2021-10-06 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Crystal of salt of quinazoline derivative |
| CN108069946B (zh) * | 2016-11-08 | 2020-06-05 | 威尚（上海）生物医药有限公司 | 具有穿过血脑屏障能力的取代的喹唑啉化合物 |
| WO2020253836A1 (zh) * | 2019-06-19 | 2020-12-24 | 南京明德新药研发有限公司 | 喹唑啉类化合物的晶型、盐型及其制备方法 |
| CN114401957B (zh) * | 2019-09-04 | 2023-11-21 | 正大天晴药业集团股份有限公司 | 一种喹唑啉衍生物的制备方法及其结晶 |
| CN110627731A (zh) * | 2019-10-09 | 2019-12-31 | 贵州大学 | 一类4-氨基喹唑啉接丙烯酰胺类化合物及其制备方法和应用 |
| CN114787151B (zh) * | 2019-11-01 | 2024-04-16 | 正大天晴药业集团股份有限公司 | 喹唑啉衍生物或其盐、或其药物组合物的用途 |
| JP2023500315A (ja) * | 2019-11-01 | 2023-01-05 | 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 | キナゾリン誘導体またはその塩を含む医薬組成物 |
| WO2021104319A1 (zh) * | 2019-11-25 | 2021-06-03 | 正大天晴药业集团股份有限公司 | 喹唑啉衍生物或其盐的联用药物组合物及其用途 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9508538D0 (en) * | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| JP3687900B2 (ja) | 1998-11-19 | 2005-08-24 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | チロシンキナーゼの不可逆的阻害剤であるｎ−［４−（３−クロロ−４−フルオロフェニルアミノ）−７−（３−モルホリン−４−イルプロポキシ）キナゾリン−６−イル］アクリルアミド |
| DE10063435A1 (de) * | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| RU2370494C2 (ru) | 2003-09-19 | 2009-10-20 | Астразенека Аб | Производные хиназолина |
| DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
| WO2007055513A1 (en) | 2005-11-08 | 2007-05-18 | Hanmi Pharm. Co., Ltd. | Quinazoline derivatives as a signal transduction inhibitor and method for the preparation thereof |
| CN101003514A (zh) | 2006-01-20 | 2007-07-25 | 上海艾力斯医药科技有限公司 | 喹唑啉衍生物、其制备方法及用途 |
| WO2008002039A1 (en) | 2006-06-28 | 2008-01-03 | Hanmi Pharm. Co., Ltd. | Quinazoline derivatives for inhibiting the growth of cancer cell |
| TWI377944B (en) | 2007-06-05 | 2012-12-01 | Hanmi Holdings Co Ltd | Novel amide derivative for inhibiting the growth of cancer cells |
| EP2220054A2 (en) * | 2007-10-29 | 2010-08-25 | Natco Pharma Limited | Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agents |
| MD20140023A2 (ru) | 2011-09-22 | 2014-06-30 | Pfizer Inc. | Пироллпиримидиновые и пуриновые производные |
| KR101272613B1 (ko) | 2011-10-05 | 2013-06-10 | 한미사이언스 주식회사 | 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체 |
| 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 |
| CN103948689A (zh) | 2014-04-15 | 2014-07-30 | 西北农林科技大学 | 用于治疗非小细胞肺癌的药物组合物及其应用 |
-
2016
- 2016-03-18 JP JP2017567522A patent/JP6704422B2/ja active Active
- 2016-03-18 RU RU2017132330A patent/RU2720810C2/ru active
- 2016-03-18 ES ES16767717T patent/ES2775614T3/es active Active
- 2016-03-18 CN CN201680015924.6A patent/CN107406430B/zh active Active
- 2016-03-18 WO PCT/CN2016/076693 patent/WO2016150340A1/zh active Application Filing
- 2016-03-18 US US15/560,099 patent/US10231973B2/en active Active
- 2016-03-18 EP EP16767717.8A patent/EP3272746B1/en active Active
-
2018
- 2018-03-19 HK HK18103795.1A patent/HK1244278B/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US10231973B2 (en) | 2019-03-19 |
| RU2017132330A3 (ru) | 2019-07-24 |
| EP3272746A4 (en) | 2018-11-07 |
| WO2016150340A1 (zh) | 2016-09-29 |
| EP3272746B1 (en) | 2019-12-25 |
| CN107406430B (zh) | 2019-04-26 |
| ES2775614T3 (es) | 2020-07-27 |
| JP6704422B2 (ja) | 2020-06-03 |
| EP3272746A1 (en) | 2018-01-24 |
| US20180085369A1 (en) | 2018-03-29 |
| JP2018508583A (ja) | 2018-03-29 |
| RU2720810C2 (ru) | 2020-05-13 |
| CN107406430A (zh) | 2017-11-28 |
| HK1244278B (zh) | 2020-04-17 |
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