Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-07
1998-01-13
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514259, 514260, 544238, 544284, 544285, 544287, 544289, A61K 31505, C07D23990
Patent
active
057079927
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), Ecesry 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 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.
Ashton et al., "Synthesis of 5-Substituted Quinazolines as Potential Antimalarial Agents," J. Med. Chem., 16, 1973, 1233-1237.
Marvel et al., "Isatin," Organic Synthesis, 327-330.
Krowicki, "4-Mercapto-2(1H)-Pyridinethione," Polish Journal of Chemistry, 53, 1979, 701-707.
Ghose et al., "General Distance Geometry Three-Dimensional Receptor Model for Diverse Dihydrofolate Reductase Inhibitors," J. Med. Chem., 27, 1984, 901-914.
Fukunaga et al., "Inhibition of Dihydrofolate Reductase. Structure-Activity Correlations of Quinazolines," J. Med. Chem., 19, 1976, 605-611.
Crippen, "Distance Geometry Approach to Rationalizing Binding Data," J. Med. Chem., 22, 1979, 988-997.
Ghose et al., "Quantitative Structure-Activity Relationship by Distance Geometry: Quinazolines as Dihydrofolate Reductase Inhibitors,"J. Med. Chem., 25, 1982, 892-899.
Ghose et al., "Combined Distance Geometry Analysis of Dihydrofolate Reductase Inhibition by Quinazolines and Triazines," J. Med. Chem., 26, 1983, 996-1010.
Jones et al., "A Potent Antitumor Quinazoline Inhibitor of Thymidylate Synthetase: Synthesis, Biological Properties and Therapeutic Results in Mice," Europ. J. Cancer, 17, 1981, 11-19.
Calvert et al., "A Phase I Evaluation of the Quinazoline Antifolate Thymidylate Synthase Inhibitor, N.sup.10 -Propargyl 5,8-Dideazafolic Acid," Journal of Clinical Oncology, 4(8), 1986, 1245-1252.
Hynes et al., "Synthesis of Analogs of 6-Arylthio, 6-Arylsulfinyl-, and 6-Arylsulfonyl-2,4-diaminoquinazolines as Potential Antimalarial Agents," J. Med. Chem., 17(7), 1974m 682-684.
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., 31, 1988, 449-454.
Singh et al., "Synthesis of 5-Trifluoromethyl-5,8-Dideazafolic Acid and 5-Trifluoromethyl-5,8-dideazaisofolic Acid," J. Heterocyclic Chem., 27, 1990, 2101-2105.
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, 51, 1991, 5579-5586.
Marsham et al., "Quinazoline Antifolate Thymidylate Synthase Inhibitors: Bridge Modifications and Conformationally Restricted Analogues in the C2-Methyl Series," J. Med. Chem., 34, 1991, 2209-2218.
Attard John
Bleckman Ted M.
Jones Terence R.
Varney Michael D.
Webber Stephen E.
Agouron Pharmaceuticals , Inc.
Grumbling Matthew V.
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