CN1292788A - 作为蛋白酪氨酸激酶抑制剂的二环杂芳族化合物 - Google Patents
作为蛋白酪氨酸激酶抑制剂的二环杂芳族化合物 Download PDFInfo
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- CN1292788A CN1292788A CN998038873A CN99803887A CN1292788A CN 1292788 A CN1292788 A CN 1292788A CN 998038873 A CN998038873 A CN 998038873A CN 99803887 A CN99803887 A CN 99803887A CN 1292788 A CN1292788 A CN 1292788A
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
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- C—CHEMISTRY; METALLURGY
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- 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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- 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
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- C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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- C07—ORGANIC CHEMISTRY
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- C07D417/14—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 three or more hetero rings
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- 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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Abstract
Description
底物磷酸化作用 | ||
实施例 | erbB2-测定(b) | EGF-r-测定(a) |
1 | +++ | +++ |
2 | +++ | +++ |
3 | +++ | +++ |
4 | ++ | +++ |
5 | +++ | +++ |
6 | ++ | |
7 | +++ | +++ |
底物磷酸化作用 | |
实施例 | erbB2-测定(b) |
8 | +++ |
9 | +++ |
10 | +++ |
11 | +++ |
12 | ++ |
13 | ++ |
14 | +++ |
15 | +++ |
16 | +++ |
17 | +++ |
18 | +++ |
19 | +++ |
20 | +++ |
21 | +++ |
22 | +++ |
23 | +++ |
24 | +++ |
25 | +++ |
26 | +++ |
27 | +++ |
28 | +++ |
29 | +++ |
33 | +++ |
34 | +++ |
35 | +++ |
36 | +++ |
37 | +++ |
IC50 | 符号 |
<0.10μM | +++ |
0.10-1.0μM | ++ |
1.0-10.0μM | + |
>10.0μM | - |
未测定 | ND |
底物磷酸化作用 | ||
实施例 | 1ck | ZAP-70 |
30 | ++ | ++ |
31 | ++ | ++ |
32 | + | + |
IC50值 | 符号 |
0.01-0.10μM | ++ |
0.10-1.0μM | + |
未测定 | ND |
实施例 | 细胞增殖 | ||||
HB4a erbB2 | HB4a ras | BT474 | HN5 | N87 | |
1 | +++ | + | +++ | +++ | +++ |
2 | +++ | + | +++ | +++ | +++ |
3 | +++ | + | +++ | +++ | +++ |
4 | +++ | - | +++ | +++ | +++ |
5 | +++ | - | +++ | +++ | +++ |
6 | +++ | + | +++ | +++ | +++ |
7 | +++ | ++ | +++ | +++ | +++ |
8 | +++ | ++ | +++ | +++ | +++ |
9 | +++ | ++ | +++ | +++ | +++ |
10 | +++ | ++ | +++ | +++ | +++ |
11 | +++ | - | +++ | +++ | +++ |
12 | +++ | - | +++ | ++ | +++ |
13 | ++ | - | ++ | + | ++ |
14 | +++ | - | +++ | +++ | +++ |
15 | +++ | - | +++ | +++ | +++ |
16 | +++ | ++ | +++ | +++ | +++ |
17 | ++ | ++ | +++ | ++ | ++ |
18 | +++ | ++ | +++ | +++ | +++ |
19 | +++ | - | +++ | +++ | +++ |
20 | +++ | - | +++ | ++ | +++ |
21 | +++ | ++ | +++ | +++ | +++ |
22 | +++ | + | +++ | +++ | +++ |
23 | +++ | + | +++ | +++ | +++ |
24 | ++ | - | ++ | +++ | ++ |
25 | +++ | - | +++ | +++ | +++ |
26 | +++ | ++ | +++ | +++ | +++ |
27 | +++ | ++ | +++ | +++ | +++ |
28 | +++ | + | +++ | +++ | +++ |
29 | +++ | - | +++ | +++ | +++ |
33 | +++ | +++ | +++ | +++ | +++ |
34 | +++ | - | +++ | +++ | +++ |
35 | +++ | + | +++ | +++ | +++ |
36 | ++ | - | ++ | ++ | ++ |
37 | +++ | + | +++ | +++ | +++ |
IC50值 | 符号 |
<5μM | +++ |
5-25μM | ++ |
25-50μM | + |
>50μM | - |
未测定 | ND |
Claims (26)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9800569.7 | 1998-01-12 | ||
GBGB9800569.7A GB9800569D0 (en) | 1998-01-12 | 1998-01-12 | Heterocyclic compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1292788A true CN1292788A (zh) | 2001-04-25 |
CN1134438C CN1134438C (zh) | 2004-01-14 |
Family
ID=10825153
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB998038873A Expired - Lifetime CN1134438C (zh) | 1998-01-12 | 1999-01-08 | 二环杂芳族化合物、其制备方法以及用途 |
Country Status (48)
Cited By (15)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2008098485A1 (fr) | 2007-02-14 | 2008-08-21 | Shanghai Allist Pharmaceuticals, Inc. | Sels de dérivé de 4-aniline quinazoline |
WO2009094831A1 (fr) * | 2008-01-22 | 2009-08-06 | Sun, Piaoyang | Composés hétéroaromatiques, leur procédé de préparation et leur utilisation |
CN102558159A (zh) * | 2010-12-20 | 2012-07-11 | 天津药物研究院 | 4-取代间甲磺酰胺苯胺基-喹唑啉衍生物及其制备方法和用途 |
CN102558160A (zh) * | 2010-12-20 | 2012-07-11 | 天津药物研究院 | 4-取代对甲磺酰胺苯胺基-喹唑啉衍生物及其制备方法和用途 |
US8507010B2 (en) | 2008-05-21 | 2013-08-13 | Shanghai Allist Pharmaceuticals, Inc. | Compositions comprising quinazoline derivatives |
CN103554091A (zh) * | 2013-11-05 | 2014-02-05 | 沈阳工业大学 | 喹唑啉衍生物及其制备方法和用途 |
WO2014071824A1 (zh) * | 2012-11-06 | 2014-05-15 | 深圳海王药业有限公司 | 4-氨基喹唑啉杂环化合物及其用途 |
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 |
US9090588B2 (en) | 2011-03-04 | 2015-07-28 | Newgen Therapeutics, Inc. | Alkyne substituted quinazoline compound and methods of use |
US9187459B2 (en) | 2011-05-17 | 2015-11-17 | Newgen Therapeutics, Inc. | Quinazoline-7-ether compounds and methods of use |
CN105705494A (zh) * | 2013-07-18 | 2016-06-22 | 锦州奥鸿药业有限责任公司 | 喹唑啉衍生物及其药物组合物,以及作为药物的用途 |
CN106279307A (zh) * | 2015-05-19 | 2017-01-04 | 正大天晴药业集团股份有限公司 | 芳氨代葡萄糖衍生物、其制备方法及抗肿瘤用途 |
CN107531665A (zh) * | 2014-12-15 | 2018-01-02 | 密执安大学评议会 | Egfr和pi3k的小分子抑制剂 |
CN111182903A (zh) * | 2017-07-28 | 2020-05-19 | 特普医药公司 | 巨环化合物及其用途 |
CN112351985A (zh) * | 2018-06-27 | 2021-02-09 | 奥斯考泰克公司 | 吡啶并嘧啶酮衍生物用作axl抑制剂 |
Families Citing this family (399)
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ES2289791T3 (es) | 1997-08-22 | 2008-02-01 | Astrazeneca Ab | Derivados de oxindolilquinazolina como inhibidores de la angiogenesis. |
RS49779B (sr) * | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
DK1119567T3 (da) | 1998-10-08 | 2005-07-25 | Astrazeneca Ab | Quinazolinderivater |
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US6933299B1 (en) | 1999-07-09 | 2005-08-23 | Smithkline Beecham Corporation | Anilinoquinazolines as protein tyrosine kinase inhibitors |
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BR0113056A (pt) | 2000-08-09 | 2003-07-08 | Astrazeneca Ab | Composto, processo papa a preparação do mesmo, composição farmacêutica, e, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, e, uso de um composto |
MXPA03002410A (es) | 2000-09-20 | 2003-06-19 | Merck Patent Gmbh | 4-amino-quinazolinas. |
EP1415987B1 (en) | 2000-10-20 | 2007-02-28 | Eisai R&D Management Co., Ltd. | Nitrogenous aromatic ring compounds as anti cancer agents |
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US7253184B2 (en) | 2000-11-02 | 2007-08-07 | Astrazeneca Ab | 4-Substituted quinolines as antitumor agents |
AU2002210714A1 (en) | 2000-11-02 | 2002-06-11 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
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2014
- 2014-11-10 US US14/536,896 patent/US9199973B2/en not_active Expired - Fee Related
-
2015
- 2015-10-20 US US14/887,434 patent/US20160051551A1/en not_active Abandoned
-
2016
- 2016-08-03 US US15/226,949 patent/US20160339027A1/en not_active Abandoned
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WO2008098485A1 (fr) | 2007-02-14 | 2008-08-21 | Shanghai Allist Pharmaceuticals, Inc. | Sels de dérivé de 4-aniline quinazoline |
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US8507010B2 (en) | 2008-05-21 | 2013-08-13 | Shanghai Allist Pharmaceuticals, Inc. | Compositions comprising quinazoline derivatives |
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US9090588B2 (en) | 2011-03-04 | 2015-07-28 | Newgen Therapeutics, Inc. | Alkyne substituted quinazoline compound and methods of use |
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