Quinazoline derivatives

Details Quinazoline derivatives Quinazoline derivatives

1997-04-10

1998-06-23

Grumbling, Matthew V.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544293, A61K 31495, A61K 3150, C07D40302, C07D40314

Patent

active

057706034

ABSTRACT:
The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1,2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;

REFERENCES:
patent: 3266990 (1966-08-01), Lutz et al.
patent: 4343940 (1982-08-01), Kreighbaum et al.
patent: 5457105 (1995-10-01), Barker
patent: 5475001 (1995-12-01), Barker
patent: 5580870 (1996-12-01), Barker et al.
patent: 5616582 (1997-04-01), Barker
Rewcastle et al., "Tyrosine Kinase Inhibitors. 5. Synthesis and 4-(Phenylamino)quinazolines as Potent Adenosine 5'-Triphosphate Binding Site Inhibitors of the Tyrosine Kinase Domain of the Epidermal Growth Factor Receptor", J.Med.Chem. 1995, vol. 38, pp. 3482-3487.
Burke, Jr., "Protein-tyrosine kinase inhibitors," Drugs of the Future 1992, vol. 17(2), pp. 119-131.
Spence, "Inhibitors of Tyrosine Kinase Activity as Anticancer Therapeutics: Recent Developments," Expert Opinion in Therapeutic Patents, Jan. 1993, Patent Update, Anticancers, etc., pp. 3-9, Current Drugs Ltd. ISSN 0962-2594.
Spada, et al., Small molecule inhibitors of tyrosine Kinase activity, Exp.Opin.Ther.Patents (1995), 5(8):805-817, Patent Update, Oncologic, Endocrine & Metabolic, Ashley Publications Ltd ISSN 1354-3776.
Bridges, "The current status of tyrosine kinase inhibitors: do the diarylamine inhibitors of the EGF receptor represent a new beginning?," Exp.Opin.Ther.Patents (1995), 5)(12): 1245-1257, Editorial, Oncologic, Endocrine & Metabolic, 1995 Ashley Publications Ltd. ISSN 1354-3776.
Traxler, et al., "Recent advances in protein typrosine kinase inhibitors," Drugs of the Future 1995, vol. 20(12, pp. 1261-1274.
Iyer, et al., "Studies In Potential Amoebicides: Part III--Synthesis of .sub.4 -Substituted Amino-8-Hydroxy) Quinazolines & .sub.3 -Substituted 8-Hydroxy(&8-Methody)-.sub.4 -Quinazolones," J.Sci.Industr.Res., vol. 15C, Jan. 1956, pp. 1-7.
Derwent Abstract 82-87077, vol. 6, No. 244, Dec. 1982, JP 57-144266, Kobayashi, Sep. 1982, "4-Anilinoquinazoline Derivative, its Preparation and Analgesic and Antiphlogistic Agent Containing Said Derivative as Active Component".
Derwent Abstract 81-28290, JP 56-20577, Feb. 1981, Sankyo and Ube, "4-(N-alkyl:anilino) quinazoline derivs . . . having analgesic and antiinflammatory actions".
Derwent Abstract 84-53835, JP 59-13765, Jan. 1984, Kyorin, "2-(4-Quinazolinyl)amino benzoic acid derivs . . . having analgesic and antiinflammatory activities".
Chem.Abs., vol. 92:76445u, 1980, pp. 674-675, Li, et al.
Chem.Abs., vol. 96:122728w, 1982, p. 695, Lin et al.
Fry et al., "A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase," Science, vol. 265, Aug. 19, 1994, pp. 1093-1095.
Buchdunger, et al., "4,5-Dianilinophthalimide: A protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity," Proc.Natl.Acad.Sci., USA, vol. 91, pp. 2334-2338, Mar. 1994, Applied Biological Sciences.
Trinks, et al., "Dianilinophthalimides: Potent and Selective, ATP-Competitive Inhibitors of the EGF-Receptor Protein Tyrosine Kinase," J.Med. Chem. 1994, vol. 37, pp. 1015-1027.
Maguire, et al., "A New Series of PDGF Receptor Tyrosine Kinase Inhibitors: 3-Substituted Quinoline Derivatives,", J.Med.Chem. 1994, vol. 37, pp. 2129-2137.
Dolle, et al., "5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a Potent and Selective Inhibitor of Human Vascular .beta.-Type Platelet-Derived Growth Factor Receptor Tyrosine Kinase," J.Med.Chem. 1994, vol. 37, pp. 2627-2629.
Bridges, et al., "Enantioselective Inhibition of the Epidermal Growth Factor Receptor Tyrosine Kinase by 4-(.alpha.-Phenethylamino)quinazolines," Bioorganic & Medicinal Chemistry, vol. 3, No. 12, pp. 1651-1656, 1995.
Ward, et al., "Epidermal Growth Factor Receptor Tyrosine Kinase--Investigation of Catalytic Mechanism, Structure-Based Searching and Discovery of a Potent Inhibitor," Biochem.Pharmacology, vol. 48, No. 4, pp. 659-666 (1994).

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