CN102432552B - 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 - Google Patents
作为受体酪氨酸激酶抑制剂的喹唑啉类似物 Download PDFInfo
- Publication number
- CN102432552B CN102432552B CN201110283526.1A CN201110283526A CN102432552B CN 102432552 B CN102432552 B CN 102432552B CN 201110283526 A CN201110283526 A CN 201110283526A CN 102432552 B CN102432552 B CN 102432552B
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- China
- Prior art keywords
- group
- base
- alkyl
- phenyl
- quinazoline
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title abstract 2
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 65
- 229910052799 carbon Inorganic materials 0.000 claims abstract description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 18
- 125000003118 aryl group Chemical group 0.000 claims description 59
- 125000001072 heteroaryl group Chemical group 0.000 claims description 56
- 229910052760 oxygen Inorganic materials 0.000 claims description 53
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 38
- 125000004429 atom Chemical group 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 29
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 29
- 125000000217 alkyl group Chemical group 0.000 claims description 26
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 15
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- 239000011737 fluorine Substances 0.000 claims description 15
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- 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
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- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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Applications Claiming Priority (5)
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US10/642,440 US7501427B2 (en) | 2003-08-14 | 2003-08-14 | Quinazoline analogs as receptor tyrosine kinase inhibitors |
US10/642,440 | 2003-08-14 | ||
US55171804P | 2004-03-10 | 2004-03-10 | |
US60/551,718 | 2004-03-10 | ||
CNA2004800264589A CN1852714A (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
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CNA2004800264589A Division CN1852714A (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
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CN102432552A CN102432552A (zh) | 2012-05-02 |
CN102432552B true CN102432552B (zh) | 2016-01-20 |
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CN201110283526.1A Expired - Lifetime CN102432552B (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
CN201310428856.4A Expired - Lifetime CN103664802B (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
CN201310581100.3A Expired - Lifetime CN103772373B (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
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CN201310428856.4A Expired - Lifetime CN103664802B (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
CN201310581100.3A Expired - Lifetime CN103772373B (zh) | 2003-08-14 | 2004-08-10 | 作为受体酪氨酸激酶抑制剂的喹唑啉类似物 |
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CA2535614C (en) * | 2003-08-14 | 2009-12-22 | Array Biopharma Inc. | Quinazoline analogs as receptor tyrosine kinase inhibitors |
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CA2852060A1 (en) | 2011-10-14 | 2013-04-18 | Array Biopharma Inc. | Polymorphs of arry-380, a selective herb2 inhibitor and pharmaceutical compositions containing them |
SI2765990T1 (sl) | 2011-10-14 | 2017-11-30 | Array Biopharma, Inc. | Trdna disperzija |
RS57140B1 (sr) | 2012-03-23 | 2018-07-31 | Array Biopharma Inc | Amorfna čvrsta disperzija za korišćenje u lečenju raka mozga |
WO2017037292A1 (en) | 2015-09-04 | 2017-03-09 | Aslan Pharmaceuticals Pte Limited | Combination of a dhodh inhibitor and a her inhibitor for use in the treatment of cancer |
US20190134034A1 (en) * | 2016-04-21 | 2019-05-09 | Aslan Pharmaceuticals Pte. Ltd. | Method of Treating Liver Cancer |
GB201611580D0 (en) * | 2016-07-01 | 2016-08-17 | Aslan Pharmaceuticals Pte Ltd | Method |
CN106279135A (zh) * | 2016-08-09 | 2017-01-04 | 浙江医药高等专科学校 | 一种噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂 |
CN106349231A (zh) * | 2016-08-09 | 2017-01-25 | 浙江医药高等专科学校 | 一类含卤代噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂 |
CN106317040A (zh) * | 2016-08-09 | 2017-01-11 | 浙江医药高等专科学校 | 含噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及用途 |
CN106317039A (zh) * | 2016-08-09 | 2017-01-11 | 浙江医药高等专科学校 | 一种含噻吩磺酰胺结构的乙氧苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及用途 |
CN106349230A (zh) * | 2016-08-09 | 2017-01-25 | 浙江医药高等专科学校 | 一种含硝基噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂及用途 |
WO2018038684A1 (en) | 2016-08-26 | 2018-03-01 | Agency For Science, Technology And Research | Macrophage stimulating protein receptor (or ron - recepteur d' origine nantais) antibodies and uses thereof |
WO2018160138A1 (en) | 2017-03-02 | 2018-09-07 | Aslan Pharmaceuticals Pte Ltd | Dhodh inhibitor for treating haematological cancer |
AU2018258663B2 (en) | 2017-04-28 | 2022-08-04 | Seagen Inc. | Treatment of HER2 positive cancers |
WO2018222134A1 (en) | 2017-06-02 | 2018-12-06 | Aslan Pharmaceuticals Pte Ltd | Cancer therapy |
WO2018222135A1 (en) | 2017-06-02 | 2018-12-06 | Aslan Pharmaceuticals Pte Ltd | Cancer therapy |
EP4360713A3 (en) | 2018-09-18 | 2024-05-22 | F. Hoffmann-La Roche AG | Quinazoline derivatives as antitumor agents |
SG11202104073XA (en) * | 2018-10-09 | 2021-05-28 | Aslan Pharmaceuticals Pte Ltd | Malonate salt of varlitinib |
CN111499622B (zh) * | 2019-07-08 | 2023-06-06 | 山东省科学院菏泽分院 | 一种治疗胆管癌的药物的制备方法 |
TW202214641A (zh) | 2020-06-30 | 2022-04-16 | 美商艾瑞生藥股份有限公司 | Her2突變抑制劑 |
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Patent Citations (3)
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CN1211240A (zh) * | 1996-02-14 | 1999-03-17 | 曾尼卡有限公司 | 作为抗肿瘤剂的喹唑啉衍生物 |
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