CN1440403A - 喹唑啉二甲苯磺酸盐化合物 - Google Patents
喹唑啉二甲苯磺酸盐化合物 Download PDFInfo
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- CN1440403A CN1440403A CN01812051A CN01812051A CN1440403A CN 1440403 A CN1440403 A CN 1440403A CN 01812051 A CN01812051 A CN 01812051A CN 01812051 A CN01812051 A CN 01812051A CN 1440403 A CN1440403 A CN 1440403A
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- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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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
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
两θ角(度) | 空间距(埃) |
4.8 | 18 |
8.7 | 10 |
18.0 | 4.9 |
18.9 | 4.7 |
21.0 | 4.2 |
22.3 | 4.0 |
两θ角(度) | 空间距(埃) |
6.6 | 13 |
8.3 | 10 |
11.5 | 7.7 |
18.1 | 4.9 |
21.1 | 4.2 |
水体积(%) | 水摩尔分数 | RH%) | 平衡形式 |
0 | 0.00 | 0 | 无水合物 |
2 | 0.04 | 7 | 无水合物 |
5 | 0.11 | 15 | 一水合物 |
10 | 0.20 | 26 | 一水合物 |
20 | 0.36 | 43 | 一水合物 |
40 | 0.60 | 66 | 一水合物 |
60 | 0.77 | 80 | 一水合物 |
80 | 0.90 | 91 | 一水合物 |
90 | 0.95 | 95 | 一水合物 |
100 | 1.00 | 100 | 一水合物 |
IC50值 | 符号 |
<0.10uM | +++ |
0.10-1.0uM | ++ |
1.0-10.0uM | + |
>10.0uM | - |
未测定 | ND |
实施例 | N87IC50uM细胞 | BT474IC50uM细胞 | HN5IC50uM细胞 |
8 | +++ | +++ | +++ |
12 | +++ | +++ | +++ |
13 | +++ | +++ | +++ |
IC50值 | 符号 |
<5μM | +++ |
5-25μM | ++ |
25-50μM | + |
>50μM | - |
未确定 | ND |
Claims (27)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US21550800P | 2000-06-30 | 2000-06-30 | |
US60/215,508 | 2000-06-30 | ||
US27184501P | 2001-02-27 | 2001-02-27 | |
US60/271,845 | 2001-02-27 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2004100898675A Division CN1305872C (zh) | 2000-06-30 | 2001-06-28 | 喹唑啉类化合物的制备方法 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1440403A true CN1440403A (zh) | 2003-09-03 |
CN1211382C CN1211382C (zh) | 2005-07-20 |
Family
ID=26910112
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2004100898675A Expired - Fee Related CN1305872C (zh) | 2000-06-30 | 2001-06-28 | 喹唑啉类化合物的制备方法 |
CNB018120512A Expired - Lifetime CN1211382C (zh) | 2000-06-30 | 2001-06-28 | 喹唑啉二甲苯磺酸盐化合物 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2004100898675A Expired - Fee Related CN1305872C (zh) | 2000-06-30 | 2001-06-28 | 喹唑啉类化合物的制备方法 |
Country Status (26)
Country | Link |
---|---|
US (2) | US7157466B2 (zh) |
EP (1) | EP1294715B1 (zh) |
JP (2) | JP4102185B2 (zh) |
KR (2) | KR100815681B1 (zh) |
CN (2) | CN1305872C (zh) |
AR (1) | AR031248A1 (zh) |
AT (1) | ATE353891T1 (zh) |
AU (3) | AU2001273071B2 (zh) |
BR (1) | BR0111947A (zh) |
CA (1) | CA2413134C (zh) |
CY (1) | CY1107054T1 (zh) |
CZ (2) | CZ300945B6 (zh) |
DE (1) | DE60126611T2 (zh) |
DK (1) | DK1294715T3 (zh) |
ES (1) | ES2280382T3 (zh) |
HK (1) | HK1051041A1 (zh) |
HU (1) | HU229624B1 (zh) |
IL (3) | IL153111A0 (zh) |
MX (1) | MXPA02012681A (zh) |
MY (1) | MY133667A (zh) |
NO (2) | NO324637B1 (zh) |
NZ (1) | NZ522989A (zh) |
PL (1) | PL204958B1 (zh) |
PT (1) | PT1294715E (zh) |
TW (2) | TWI307339B (zh) |
WO (1) | WO2002002552A1 (zh) |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010054528A1 (zh) * | 2008-11-17 | 2010-05-20 | Cen Junda | 喹唑啉类化合物 |
CN1984656B (zh) * | 2004-06-04 | 2010-05-26 | 史密丝克莱恩比彻姆(科克)有限公司 | 癌症治疗药物 |
WO2011160594A1 (zh) * | 2010-06-24 | 2011-12-29 | 齐鲁制药有限公司 | 拉帕替尼的新制备方法 |
CN101203211B (zh) * | 2005-04-19 | 2012-08-08 | 史密丝克莱恩比彻姆(科克)有限公司 | 药物组合物 |
US8507010B2 (en) | 2008-05-21 | 2013-08-13 | Shanghai Allist Pharmaceuticals, Inc. | Compositions comprising quinazoline derivatives |
WO2013131465A1 (zh) * | 2012-03-06 | 2013-09-12 | 齐鲁制药有限公司 | N-(4-(3-氟苄氧基)-3-氯苯基)-6-(5-((2-(甲基亚砜基)乙基氨基)甲基)-2-呋喃基)-喹唑啉-4-胺二甲苯磺酸盐的多晶型物及其制备方法和用途 |
CN102079759B (zh) * | 2009-12-01 | 2014-09-17 | 天津药物研究院 | 6位取代的喹唑啉类衍生物、其制备方法和用途 |
CN104788434A (zh) * | 2014-01-16 | 2015-07-22 | 江苏恒瑞医药股份有限公司 | 一种蛋白酪氨酸激酶抑制剂的二苯磺酸盐 |
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BR0114020A (pt) * | 2000-09-20 | 2003-07-22 | Merck Patent Gmbh | 4-amino-quinazolinas |
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AU2003251010A1 (en) * | 2002-07-15 | 2004-02-02 | Janssen Pharmaceutica N.V. | 3-furanyl analogs of toxoflavine as kinase inhibitors |
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ES2344294T3 (es) * | 2003-05-02 | 2010-08-24 | Globopharm Pharmazeutische Produktions- Und Handelsgesellschaft M.B.H. | Preparacion farmaceutica solida que contiene sales de levotiroxina y/o liotironina. |
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WO2010054528A1 (zh) * | 2008-11-17 | 2010-05-20 | Cen Junda | 喹唑啉类化合物 |
CN102079759B (zh) * | 2009-12-01 | 2014-09-17 | 天津药物研究院 | 6位取代的喹唑啉类衍生物、其制备方法和用途 |
WO2011160594A1 (zh) * | 2010-06-24 | 2011-12-29 | 齐鲁制药有限公司 | 拉帕替尼的新制备方法 |
WO2013131465A1 (zh) * | 2012-03-06 | 2013-09-12 | 齐鲁制药有限公司 | N-(4-(3-氟苄氧基)-3-氯苯基)-6-(5-((2-(甲基亚砜基)乙基氨基)甲基)-2-呋喃基)-喹唑啉-4-胺二甲苯磺酸盐的多晶型物及其制备方法和用途 |
CN104788434A (zh) * | 2014-01-16 | 2015-07-22 | 江苏恒瑞医药股份有限公司 | 一种蛋白酪氨酸激酶抑制剂的二苯磺酸盐 |
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