CN106588943A - 一种egfr抑制剂的盐、晶型及其用途 - Google Patents
一种egfr抑制剂的盐、晶型及其用途 Download PDFInfo
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- CN106588943A CN106588943A CN201610911027.5A CN201610911027A CN106588943A CN 106588943 A CN106588943 A CN 106588943A CN 201610911027 A CN201610911027 A CN 201610911027A CN 106588943 A CN106588943 A CN 106588943A
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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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material 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)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
m0(g) | m1(g) | m2(g) | 吸湿增重 |
30.51893 | 0.99751 | 31.51718 | 0.074% |
Claims (15)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2015106774053 | 2015-10-19 | ||
CN201510677405 | 2015-10-19 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN106588943A true CN106588943A (zh) | 2017-04-26 |
CN106588943B CN106588943B (zh) | 2018-10-16 |
Family
ID=58555626
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201610911027.5A Active CN106588943B (zh) | 2015-10-19 | 2016-10-18 | 一种egfr抑制剂的盐、晶型及其用途 |
Country Status (11)
Country | Link |
---|---|
US (1) | US10308658B2 (zh) |
EP (1) | EP3365344B1 (zh) |
JP (1) | JP6812426B2 (zh) |
KR (1) | KR102627044B1 (zh) |
CN (1) | CN106588943B (zh) |
AU (1) | AU2016343517B2 (zh) |
CA (1) | CA3001655C (zh) |
ES (1) | ES2841600T3 (zh) |
HK (1) | HK1254666A1 (zh) |
TW (1) | TWI693225B (zh) |
WO (1) | WO2017067447A1 (zh) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107328871A (zh) * | 2017-05-12 | 2017-11-07 | 中国医学科学院肿瘤医院 | Uplc‑ms/ms联用检测人血浆和/或脑脊液中奥希替尼的药物浓度 |
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 |
CN112969699A (zh) * | 2018-10-09 | 2021-06-15 | 亚狮康私人有限公司 | 瓦利替尼的丙二酸盐 |
CN113929630A (zh) * | 2020-07-13 | 2022-01-14 | 鲁南制药集团股份有限公司 | 一种吉非替尼药物共晶体 |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2017114735A1 (en) * | 2015-12-30 | 2017-07-06 | Synthon B.V. | Process for making crystalline form a of gefitinib |
KR102444835B1 (ko) | 2016-05-26 | 2022-09-19 | 리커리엄 아이피 홀딩스, 엘엘씨 | Egfr 억제제 화합물 |
WO2019165003A1 (en) * | 2018-02-20 | 2019-08-29 | Dawei Zhang | Substituted quinolines useful as kinase inhibitors |
AU2019340598A1 (en) * | 2018-09-14 | 2021-03-18 | Hanmi Pharmaceutical Co., Ltd. | Crystalline forms of a quinazole compound and its hydrochloride salts |
US20220143023A1 (en) * | 2019-03-29 | 2022-05-12 | Board Of Regents, The University Of Texas System | Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 insertions |
CN115028594A (zh) * | 2020-06-03 | 2022-09-09 | 吴卫东 | 恩替他滨药用前体化合物及其制备方法和医学用途 |
UY39342A (es) * | 2020-07-27 | 2022-02-25 | Spectrum Pharmaceuticals Inc | Tratamiento con poziotinib para el cáncer de pulmón de células no pequeñas |
WO2023129667A1 (en) | 2021-12-30 | 2023-07-06 | Biomea Fusion, Inc. | Pyrazine compounds as inhibitors of flt3 |
Citations (8)
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CN103102342A (zh) * | 2011-11-14 | 2013-05-15 | 广东东阳光药业有限公司 | 氨基喹唑啉类衍生物及其盐和使用方法 |
CN103102344A (zh) * | 2011-11-14 | 2013-05-15 | 广东东阳光药业有限公司 | 氨基喹唑啉类衍生物及其盐和使用方法 |
CN105294718A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的马来酸盐及其晶型 |
CN105294715A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的富马酸盐及其晶型 |
CN105294719A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的二对甲苯磺酸盐及其晶型 |
CN105294717A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种egfr抑制剂的盐、晶型及其用途 |
CN105294716A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的二水杨酸盐及其晶型 |
CN105461729A (zh) * | 2015-11-18 | 2016-04-06 | 乳源瑶族自治县大众药品贸易有限公司 | 一种egfr抑制剂的盐、晶型及其用途 |
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-
2016
- 2016-10-18 WO PCT/CN2016/102453 patent/WO2017067447A1/en active Application Filing
- 2016-10-18 CA CA3001655A patent/CA3001655C/en active Active
- 2016-10-18 AU AU2016343517A patent/AU2016343517B2/en active Active
- 2016-10-18 JP JP2018519750A patent/JP6812426B2/ja active Active
- 2016-10-18 KR KR1020187014069A patent/KR102627044B1/ko active IP Right Grant
- 2016-10-18 EP EP16856878.0A patent/EP3365344B1/en active Active
- 2016-10-18 CN CN201610911027.5A patent/CN106588943B/zh active Active
- 2016-10-18 US US15/769,065 patent/US10308658B2/en active Active
- 2016-10-18 ES ES16856878T patent/ES2841600T3/es active Active
- 2016-10-19 TW TW105133729A patent/TWI693225B/zh active
-
2018
- 2018-10-24 HK HK18113646.1A patent/HK1254666A1/zh unknown
Patent Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
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CN103102342A (zh) * | 2011-11-14 | 2013-05-15 | 广东东阳光药业有限公司 | 氨基喹唑啉类衍生物及其盐和使用方法 |
CN103102344A (zh) * | 2011-11-14 | 2013-05-15 | 广东东阳光药业有限公司 | 氨基喹唑啉类衍生物及其盐和使用方法 |
CN105294718A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的马来酸盐及其晶型 |
CN105294715A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的富马酸盐及其晶型 |
CN105294719A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的二对甲苯磺酸盐及其晶型 |
CN105294717A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种egfr抑制剂的盐、晶型及其用途 |
CN105294716A (zh) * | 2015-11-18 | 2016-02-03 | 乳源瑶族自治县大众药品贸易有限公司 | 一种氨基喹唑啉类衍生物的二水杨酸盐及其晶型 |
CN105461729A (zh) * | 2015-11-18 | 2016-04-06 | 乳源瑶族自治县大众药品贸易有限公司 | 一种egfr抑制剂的盐、晶型及其用途 |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107328871A (zh) * | 2017-05-12 | 2017-11-07 | 中国医学科学院肿瘤医院 | Uplc‑ms/ms联用检测人血浆和/或脑脊液中奥希替尼的药物浓度 |
CN112969699A (zh) * | 2018-10-09 | 2021-06-15 | 亚狮康私人有限公司 | 瓦利替尼的丙二酸盐 |
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 |
CN113929630A (zh) * | 2020-07-13 | 2022-01-14 | 鲁南制药集团股份有限公司 | 一种吉非替尼药物共晶体 |
CN113929630B (zh) * | 2020-07-13 | 2024-04-19 | 山东新时代药业有限公司 | 一种吉非替尼药物共晶体 |
Also Published As
Publication number | Publication date |
---|---|
HK1254666A1 (zh) | 2019-07-26 |
CA3001655C (en) | 2023-08-01 |
US10308658B2 (en) | 2019-06-04 |
AU2016343517B2 (en) | 2020-04-30 |
AU2016343517A1 (en) | 2018-05-24 |
EP3365344B1 (en) | 2020-12-09 |
JP6812426B2 (ja) | 2021-01-13 |
CA3001655A1 (en) | 2017-04-27 |
US20180298019A1 (en) | 2018-10-18 |
JP2018534289A (ja) | 2018-11-22 |
TWI693225B (zh) | 2020-05-11 |
EP3365344A1 (en) | 2018-08-29 |
TW201718596A (zh) | 2017-06-01 |
CN106588943B (zh) | 2018-10-16 |
EP3365344A4 (en) | 2019-05-22 |
KR102627044B1 (ko) | 2024-01-18 |
ES2841600T3 (es) | 2021-07-08 |
KR20180064533A (ko) | 2018-06-14 |
WO2017067447A1 (en) | 2017-04-27 |
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