Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-03-05
2000-06-20
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544280, A61K 31505, C07D47104
Patent
active
06077844&
ABSTRACT:
This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
REFERENCES:
patent: 3904624 (1975-09-01), Perronnet et al.
patent: 4435570 (1984-03-01), Nishimura et al.
patent: 4923872 (1990-05-01), Kostlan et al.
patent: 4996206 (1991-02-01), Taylor et al.
patent: 5028608 (1991-07-01), Taylor et al.
patent: 5248775 (1993-09-01), Taylor et al.
patent: 5254687 (1993-10-01), Taylor et al.
patent: 5344932 (1994-09-01), Taylor
patent: 5346900 (1994-09-01), Gangjee
patent: 5508281 (1996-04-01), Gangjee
patent: 5939420 (1999-08-01), Gangjee
Chem. Abst: Frass et al., 1980:586714, 1980.
Rosowsky et al., J. Het. Chem., vol. 6 p 614, 1969.
Rosowsky et al., J. Heterocyclic Chem., 6(5) 1969. Abst.
Hurlbert et al., "Studies on Condensed Pyrimidine Systems. XXIII. Synthesis of 2,4-Diaminopyrido[2,3-d]pyrimidines from 6-Keto Esters", J. Med. Chem., vol. 11, pp. 703-707 (1968).
Hurlbert et al., "Studies on Condensed Pyrimidine Systems. XXIV. The Condensation of 2,4,6-Triaminopyrimidine with Malondialdehyde Derivatives", J. Med. Chem., vol. 11, pp. 708-710 (1968).
Hurlbert et al., "Studies on Condensed Pyrimidine Systems. XXV. 2,4-Diaminopyrido[2,3-d]pyrimidines. Biological Data", J. Med. Chem., vol. 11, pp. 711-717 (1968).
Grivsky et al., "Synthesis and Antitumor Activity of 2,4-Diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidine", J. Med. Chem., vol. 23, pp. 327-329 (1980).
Elslager et al., "Folate Antagonists. 20. Synthesis and Antitumor and Antimalarial Properties of Trimetrexate and Related 6-[(phenylamino)methyl]2,4-quinazolinediamines", J. Med. Chem., vol. 26, pp. 1753-1760 (1983).
Piper et al., "Synthesis and Antifolate Activity of 5-Methyl-5-deaza Analogues of Aminopterin, Methotrexate, Folic Acid, and N.sup.10 -Methylfolic Acid", J. Med. Chem., vol. 29, pp. 1080-1087 (1986).
Werbel et al., "Synthesis and Antimalarial Activity of a Series of 2,4-Diamino-6-[(N-alkylanilino)methyl]quinazolines", J. Hetercyclic Chem., vol. 24, pp. 345-349 (1987).
Miwa et al., "Novel Pyrrolo[2,3-d]pyrimidine Antifolates: Synthesis and Antitumor Activities", Journal of Medicinal Chemistry, 1991, pp. 555-560, vol. 34, No. 2.
Gangjee et al., "Classical and Nonclassical Furo[2,3-d]pyrimidines as Novel Antifolates: Synthesis and Biological Activities", Journal of Medicinal Chemistry, 1994, pp. 1169-1176, vol. 37, No. 8.
Gangjee et al., "Novel 2,4-Diamino-5-Substituted-pyrrolo[2,3-d]pyrimidines as Classical and Nonclassical Antifolate Inhibitors of Dihydrofolate Reductases", Journal of Medicinal Chemistry, 1995, pp. 2158-2165, vol. 38, No. 12.
Gangjee et al., "Effect of Bridge Region Variation on Antifolate and Antitumor Activity of Classical 5-Substituted 2,4-Diaminofuro[2,3-d]pyrimidines", Journal of Medicinal Chemistry, 1995, pp. 3798-3805, vol. 38, No. 19.
Gangjee et al., "5-Arylthio-Substituted 2-Amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine Antifolates as Thymidylate Synthase Inhibitors and Anitumor Agents", Journal of Medicinal Chemistry, 1995, pp. 4495-4502, vol. 38, No. 22.
Gangjee et al., "2-Amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as Nonclassical Antifolate Inhibitors of Thymidylate Synthase", J. Med. Chem., 1996, pp. 4563-4568, vol. 39, No. 23.
Gangjee et al., "Classical and Nonclassical Antifolates as Potential Antitumor, Antipneumocystis and Antitoxoplasma Agents", Current Pharmaceutical Design, 1996, pp. 263-280, vol. 2.
Gangjee et al., "Effect of N.sup.9 Methylation and Bridge Atom Variation on the Activity of 5-Substituted 2,4-Diaminopyrrolo[2,3-d]pyrimidines against Dihydrofolate Deductases from Pneumocystis carinii and Toxoplasma gondii", J. Med. Chem., 1997, pp. 1173-1177, vol. 40.
Cody et al., "Comparison of Ternary Complexes of Pneumocystis carinii and Wild-Type Human Dihydrofolate Reductase with Coenzyme NADPH and a Novel Classical Antitumor Furo[2m3-d]pyrimidine Antifolate", Acta. Cryst., 1997, pp. 638-649, vol. D53.
Shih et al., "LY231514, a Pyrrolo[2,3-d]pyrimidine-based Antifolate that Inhibits Multiple Folate-requiring Enzymes", Cancer Research, Mar. 15, 1997, pp. 1116-1123, vol. 57.
Gangjee et al., "Synthesis and Biological Activities of Tricyclic Conformationally Restricted Tetrahydropyrido Annulated Furo[2,3-d]pyrimidines as Inhibitors of Dihydrofolate Reductases", J. Med. Chem., 1998, pp. 1409-1416. vol. 41.
Gangjee et al., "Selective Pneumocystis carinii Dihydrofolate Reductase Inhibitors: Design, Synthesis, and Biological Evaluation of New 2,4-Diamino-5-substituted-furo[2,3-d]pyrimidines", Journal of Medicinal Chemistry, 1988, pp. 1263-1271, vol. 44, No. 8.
Duquesne University of the Holy Ghost
Meyers Diane R.
Shah Mukund J.
Sripada Pavanaram K
LandOfFree
Pyrimidine derivatives and methods of making and using these der does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pyrimidine derivatives and methods of making and using these der, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrimidine derivatives and methods of making and using these der will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1853888