Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-06-06
1998-01-27
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514255, A61K 31505, A61K 31535
Patent
active
057122768
ABSTRACT:
A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.
REFERENCES:
patent: 2602794 (1952-07-01), Hitchings et al.
patent: 3940393 (1976-02-01), Greenspan et al.
patent: 3980781 (1976-09-01), Snell et al.
patent: 4005203 (1977-01-01), Stickney et al.
patent: 4005204 (1977-01-01), Stickney et al.
patent: 4006235 (1977-02-01), Stickney et al.
patent: 4496549 (1985-01-01), Oronsky
patent: 4535080 (1985-08-01), Audiau et al.
patent: 4542136 (1985-09-01), Carminati et al.
patent: 4613603 (1986-09-01), Biziere et al.
patent: 4624952 (1986-11-01), Biziere et al.
patent: 4725600 (1988-02-01), Takaya et al.
patent: 5136080 (1992-08-01), Miller et al.
Biziere, et al., "Chemical Abstracts", vol. 105, 1986, Col. 105:97319h.
Griffin et al., Journal of Medicinal Chemistry, vol. 32, No. 11, Nov., 1989, pp. 2468-2474.
Cody, et al., Structural Analysis of Lipophilic Antifolates: Electronic Structure, Conformation and Enzyme Binding.
Cody, et al., Structure-Activity Relationships Among 5-Substituted Lipophilic Diaminopyrimidine Antieoplastic Antifolates.
Ioan Motoc, Match on the Minimal Steric Difference Method.
Leach et al Epilepsia vol. 27 No. 5 1986 pp. 490-497 "Pharmacological Studies on Lamotrigine".
Cavallito et al, "Lipid-Soluble Inhibitors of Dihydrofolate Reductase 1. Kinetics, Tissue Distribution, and Extent of Metabolism of Pyrimethamine, Metoprine, and Etoprine in the Rat, Dog, and Man", vol. 6, No. 3, pp. 329-337, Drug Metabolism and Disposition (1978).
Miller et al New anticonvulsant drugs Epilepsy--Chemotherapy, Anticonvulsants pp. 165-177 "Lamotrigine" (1986).
Georges et al J. Chem. Soc. Perkin Trans II 1989 pp. 449-455 "Structural and Electronic Properties of Anticonvulsant Drugs: Substituted 3-Tertiariy-aminoo-6-aryl-pyridazines,-1,2,4-triazines, and -pyrimidines".
Short Communications Biochemical Pharmacology vol. 27, pp. 1507-1509 "Elevation of brain histamien levels by diamnopyrimidine inhibitors of histamine N-methyl transferase" (1978).
Duch et al Transmethylation Duch 1978 vol. 5 pp. 287-295 "Histamine: Elelvation of Brain Levels by Inhibition of Histamine N-methyl transferase".
Zawilska et al Pol. J. Pharmacol. Pharm. 1985 37 pp. 821-830 "Changes in the Rat Brain Histamine Content Following Metoprine and Other Hisatamine-Methyltransferase (HMT) Inhibitors".
Hough et al Biochemical Pharmacology vol. 35 No. 2 pp. 307-310, 1986 "Inhibition of Brain Histamine Metabolism by Metoprine".
Tuomisto et al Neuropharmacology vol. 25, No. 8, pp. 955-958, 1986 "Is Histamine an Anticonvulsive Inhibitory Transmitter?".
Tuomisto Agents and Actions, vol. 20, 3/4 (1987) pp. 252-254 "Inhibition of sound-induced convulsions by metoprine in the audiogenic seizure susceptible rat".
Nichol et al Cancer Treatment Reports vol. 61 No. 4, Jul. 1977 pp. 559-564 "Lipid-Soluble Diaminopyrimidine Inhibitors of Dihydrofolate Reductase".
Currie et al Cancer Treatment Reports vol. 64, No. 8-9 1980 pp. 951-956 "Phase I Trial of Metoprine in Patients with Advanced Cancer".
Serano et al Cancer Treatment Reports vol. 66, No. 1, 1982 pp. 99-106 "Evaluation of the Lipid-Soluble Diaminopyrimidines, Metoprine and Etoprine, in the Avian Sarcoma Virus Rat Glioma Model".
Hamrell Oncology 41: 343-348 (1984) "Inhibition of Dihydrofolate Reductase and Cell Growth by Antifolates in a Methotrexate-Resistant Cell Line".
Sternberg et al Cancer Treatment Reports vol. 68, No. 7-8 1984 pp. 1053-1054 "Phase II Evaluation of Metoprine in Advanced Pancreatic Adenocarcinoma".
ASCO Abstracts, 1982 Clinical Pharmacology Proceedins of ASCO p. 22 C-88.
Clinical Investigations AACR Abstracts, 1983 pp. 149 588 and 589.
Budesinsky, et al., Ceskoslov. Farm., 15, pp. 345-355 (1962).
Ried, et al., Chem. Ber., 112, pp. 640-647 (1979).
Leach, et al., Epilepsia, vol. 27, No. 5, pp. 490-497 (1986).
McCullough, et al., Biochemical Pharmacology, vol. 20, pp. 561-567 (1971).
Russell, Chem. Soc., pp. 2951-2955 (1954).
Cody, et al., Med. Chem., vol. 25, No. 4, pp. 427-430 (1982).
Rothman, et al., Anals. of Neurology, vol. 19, No. 2, pp. 105-111 (1986).
Maragos, et al., TINS, 10, pp. 65-68 (1987).
Meldrum, Clinical Science, 68, pp. 113-122 (1985).
Turnball, Canadian Journal of Neurological Science, vol. 14, No. 2, pp. 122-126 (1987).
McDonald, et al., European Journal of Pharmacology, 140, pp. 359-361 (1987).
Welsh, et al., Cancer Biochem Biophys., vol. 7, pp. 27-38 (1983).
Kavai, et al., J. Med. Chem., vol. 18, No. 3, pp. 272-275 (1975).
Welsh, et al., Chem. Biol. Pferidines, pp. 463-468 (1982).
Falco, et al., Brit. J. Pharmacol., 6, pp. 185-200 (1951).
Perina, et al., Chem. Abstr., vol. 38, p. 1774 (1964).
Budesinsky, et al., Chem. Abstr., vol. 60, p. 6095 (1975).
Lux, Antibiotics & Chemotherapy, vol. IV, No. 9, pp. 971-975 (1975).
Braden, et al., Angew Chem. Int. Ed., vol. 9, No. 1, pp. 65-66 (1970).
Bliss, et al., J. Chem. Soc. Perkin Trans., 1, pp. 2217-2228 (1987).
Delacotte, et al., J. Heterocycl. Chem., 24, (3), pp. 571-575 (1987).
McCormack, et al., J. Med. Chem., vol. 12, pp. 662-668 (1969).
Roth, et al., J. Org. Chem., vol. 34, No. 4, pp. 821-836 (1969).
Budesinsky, et al., Cesk. Farm., vol. 15, pp. 432-437 (1966).
Simon, et al., J. Theor. Biol., 66, pp. 485-495 (1966).
Goodwin, Nature, No. 4183, p. 1133 (Dec. 31, 1949).
Rupe, et al., Helv. Chem. Acta., vol. X, p. 299 (1927).
Chase, et al., J. Chem. Soc., pp. 3518-3525 (1953).
Hitchings, et al., Advances in Enzymology, 27, pp. 417-468 (1965).
Chase, et al., J. Chem. Soc., pp. 3439-3444 (1951).
Falco, et al., J. Am. Chem. Soc., vol. 73, pp. 3753-3762 (1951).
Hyde Richard Martin
Leach Michael John
Miller Alistair Ainslie
Nobbs Malcolm Stuart
Dentz Bernard
Glaxo Wellcome Inc.
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