Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-09-04
1999-03-23
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514259, 514260, 514898, 514895, 514896, 544238, 544284, 544285, 544287, 544289, A61K 31505, A61K 3154, C07D23990, C07D40302
Patent
active
058859969
ABSTRACT:
Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
REFERENCES:
patent: 1817982 (1931-08-01), Hentrich et al.
patent: 3542779 (1970-11-01), Ecersy et al.
patent: 3546224 (1970-12-01), Davoll
patent: 4048312 (1977-09-01), Lacefield
patent: 4223143 (1980-09-01), Cuny
patent: 4251531 (1981-02-01), Dorie et al.
patent: 4391809 (1983-07-01), Elslager
patent: 4564616 (1986-01-01), Jones et al.
patent: 4668682 (1987-05-01), Sekiya et al.
patent: 4749698 (1988-06-01), Neiss et al.
patent: 4853221 (1989-08-01), Elslager et al.
patent: 4857530 (1989-08-01), Berman et al.
patent: 4981856 (1991-01-01), Hughes
patent: 4985441 (1991-01-01), Hughes et al.
patent: 5089499 (1992-02-01), Barker et al.
patent: 5430148 (1995-07-01), Webber et al.
patent: 5707992 (1998-01-01), Webber et al.
Ashton, et al., "Synthesis of 5-Substituted Quinazolines as Potential Antimalarial Agents," Journal of Medicinal Chemistry, vol. 16, 1233-1237 (1973).
Marvel, C.S., et al., "Isatin," Organic Synthesis, 327-330.
Krowicki, "4-Mercapto-2(1H)-pyridinethione," Polish Journal of Chemistry, vol. 53, 701-707 (1979).
Ghose et al., "General Distance Geometry Three-Dimensional Receptor Model for Diverse Dihydrofolate Reductase Inhibitors," Journal of Medicinal Chemistry, vol. 27 (1984), pp. 901-914.
Fukunaga et al., "Inhibition of Dihydrofolate Reductase. Structure-Activity Correlations of Quinazolines," Journal of Medicinal Chemistry, vol. 19 (1976), pp. 605-611.
Jones et al., "A Potent Antitumour Quinazoline Inhibitor of Thymidylate Synthetase: Synthesis, Biological Properties and Therapeutic Results in Mice," European Journal of Cancer, vol. 17, pp. 11-19 (1981).
Calvert et al., "A Phase I Evaluation of the Quinazoline Antifolate Thymidylate Synthase Inhibitor, N.sup.10 -Propargyl-5,8-Dideazafolic Acid, CB3717," Journal of Clinical Oncology, vol. 4, No. 8, pp. 1245-1252 (1986).
Hynes et al., "Synthesis of Analogs of 6-Arylthio-, 6-Arylsulfinyl-, and 6-Arylsulfonyl-2,4-diaminoquinazolines as Potential Antimalarial Agents," Journal of Medicinal Chemistry, vol. 17, No. 7, pp. 682-684 (1974).
Hynes et al., "Inhibition of Murine Thymidylate Synthase and Human Dihydrofolate Reductase by 5,8-Dideaza Analogues of Folic Acid and Aminopterin," Journal of Medicinal Chemistry, vol. 31, pp. 449-454 (1988).
Singh et al., "Synthesis of 5-Trifluoromethyl-5,8-dideazafolic Acid and 5-Trifluoromethyl-5,8-dideazaisofolic Acid," Journal of Heterocyclic Chemistry, vol. 27, pp. 2101-2105 (1990).
Jackman et al., "ICI D1694, a Quinazoline Antifolate Thymidylate Synthase Inhibitor That Is a Potent Inhibitor of L1210 Tumor Cell Growth In Vitro and In Vivo: A New Agent for Clinical Study," Cancer Research, vol. 51, pp. 5579-5586 (1991).
Marsham et al., "Quinazoline Antifolate Thymidylate Synthase Inhibitors: Bridge Modifications and Conformationally Restricted Analogues in the C2-Methyl Series," Journal of Medicinal Chemistry, vol. 34, pp. 2209-2218 (1991).
Taylor, et al., "Pyridine-1-Oxides. II. A New Synthesis of Ricinine," Journal of Chemistry, vol. 78 (1956), pp. 214-217.
Von Hoff, et al., "Prospective Clinical Trial of a Human Tumor Cloning System," Cancer Research, vol. 43 (1983), pp. 1926-1931.
Baker, et al., An Antimalarial Alkaloid from Hydrangea. XVI. Synthesis of 5-, 6-, 7-, and 8-Derivatives with Two Different Substituents, Journal of Chemistry, 1952, pp. 157-163.
Hertog, et al., "Reactivity of 4-Nitropyridine-N-Oxide," Recueil, vol. 70 (1951), pp. 581-589.
Kubo, et al., "Synthesis of Antiulcer Agents," Chem. Pharm. Bulletin, vol. 38, No. 10 (1990), pp. 2853-2858.
Ashimori, et al., "Novel 1,4-Dihydropyridine Calcium Antagonists. I. Synthesis and Hypotensive Activity of 4-(Substituted Pyridyl)-1,4-Dihydropyridine Derivatives," Chem. Pharm. Bulletin, vol. 38, No. 9 (1990), pp. 2446-2458.
V. Balasubramaniyam, Chemical Reviews, vol. 66, No. 6 (1966), pp. 567-641.
Webber et al., J. Med. Chem. (1993), 36(6), 733-46, Feb. 1993.
Crippen et al., J. Med. Chem., 22(8), 998-97, May 1979.
Ghose et al., J. Med. Chem., 25(8), 892-9, Feb. 1982.
Ghose et al., J. Med. Chem. 26(7) 996-1010, Feb. 1983.
Attard John
Bleckman Ted M.
Jones Terrence R.
Varney Michael D.
Webber Stephen E.
Agouron Pharmaceuticals , Inc.
Grumbling Matthew V.
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