Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Patent
1992-03-31
1995-07-04
Shah, Mukund J.
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
544284, 544285, 544287, 544288, 544289, A61K 31505, C07D23990
Patent
active
054301483
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), Heintrich et al.
patent: 3542779 (1970-11-01), Ecsery et al.
patent: 3546224 (1970-12-01), Davoll
patent: 4048312 (1977-09-01), Lacefield
patent: 4223143 (1980-09-01), Cuny et al.
patent: 4251531 (1981-02-01), Doria 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
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.
Ashton, Wallace T. and John B. Hynes, "Synthesis of 5-Substituted Quinazolines as Potential Antimalarial Agents", Journal of Medicinal Chemistry 16, 1233-1237 (1973).
Marvel, C. S. and G. S. Hieas, "Isatin", Organic Synthesis, 327-330.
Krowicki, Krysztof, "4-Mercapto-2(1H)-pyridinethione", Polish Journal of Chemistry, 53, 701-707 (1979).
Hynes, et al., "Inhibition of Murine Thymidylate Synthase and Human Dihydrofolate Reductase by 5,8-Dideaza Analogues of Folic Acid and Aminopterin," J. Med. Chem, vol. 31, pp. 449-454 (1988).
Singh, et al., "Synthesis of 5-Trifluoromethyl-5,8-dideazafolic Acid and 5-Trifluoromethyl-5,8-dideazaisofolic Acid," J. Heterocyclic Chem., vol. 27, pp. 2101-2105 (1990).
Jackson, 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," J. Med. Chem., vol. 34, pp. 2209-2218 (1991).
Jones, et al., "A Potent Antitumour Quinazoline Inhibitor of Thymidylate Synthetase: Synthesis, Biological Properties and Therapeutic Results in Mice," Europ. J. Cancer, vol. 17, Pergamon Press Ltd., 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).
Ghose et al., J. Med. Chem. (1984) 27 901-914.
Ashton et al., J. Med. Chem. (1973) 16 1233-1237.
Fukunaga et al., J. Med. Chem. (1976) 19 605-611.
Crippen, J. Med. Chem. (1979) 22 988-997.
Ghose et al., J. Med. Chem. (1982) 25 892-899.
Ghose et al., J. Med. Chem. (1983) 26 996-1010.
Attard John
Bleckman Ted M.
Jones Terence R.
Varney Michael D.
Webber Stephen E.
Agouron Pharmaceuticals , Inc.
Grumling Matthew V.
Shah Mukund J.
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