Substituted 5-alkynyl pyrimidines having neurotrophic activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S252140, C514S256000, C514S275000, C544S122000, C544S325000, C544S326000, C544S330000, C544S332000

Reexamination Certificate

active

10333447

ABSTRACT:
The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy.

REFERENCES:
patent: 2691655 (1954-10-01), Hitchings et al.
patent: 3154551 (1964-10-01), Hitchings et al.
patent: 3862190 (1975-01-01), Lipinski et al.
patent: 3947441 (1976-03-01), Schweizer et al.
patent: 4508560 (1985-04-01), Brunner et al.
patent: 4626272 (1986-12-01), Brunner et al.
patent: 4663334 (1987-05-01), Carson
patent: 5075305 (1991-12-01), Hobbs et al.
patent: 5525604 (1996-06-01), Lee et al.
patent: 5719303 (1998-02-01), Yoshida et al.
patent: 6440965 (2002-08-01), Kelley et al.
patent: 6583148 (2003-06-01), Kelley et al.
patent: 2045327 (1992-01-01), None
patent: 25 33 710 (1976-02-01), None
patent: 2 829 820 (1979-02-01), None
patent: 0 372 934 (1990-06-01), None
patent: 0 459 819 (1991-12-01), None
patent: 0 508 469 (1992-10-01), None
patent: 0 640 599 (1995-03-01), None
patent: 0 826 674 (1998-03-01), None
patent: 2 358 148 (1978-02-01), None
patent: 2 262 096 (1993-06-01), None
patent: 08 283246 (1996-10-01), None
patent: WO 92/18498 (1992-10-01), None
patent: WO 93 08169 (1993-04-01), None
patent: WO 94 14780 (1994-07-01), None
patent: WO 96/31488 (1996-10-01), None
patent: WO 99 02497 (1999-01-01), None
patent: WO 99 19305 (1999-04-01), None
patent: WO 00 61562 (2000-10-01), None
Ulrich, Chapter 4: Crystallization, Kirk-Othmer Encyclopedia of Chemical Technology, Aug. 2002.
Vippagunta et al., Cyrstalline Solids, Advanced Drug Delivery Reviews, 48, pp. 3-26, 2001.
West, Solid Solutions, Solid State Chemistry and its applications, pp. 358 & 365, 1988.
Aroyan, et al., “Pyrimidine derivatives. X. Synthesis of amino and hydrazino derivatives of 2-(methylthio)-5-(p-alkoxybenzyl)-6-methyl pyrimidines, and a study of their antineoplastic activity”,Chemical Abstracts, 1969, p. 347, vol. 71, No. 21.
Aroyan, et al., “Pyrimidine derivatives. XLIV. Synthesis and some reactions of 2-phenyl-4-hydroxy-5-(p-alkoxybenzyl)-6-methylpyrimidines”,Chemical Abstracts, 1976, p. 515, vol. 84, No. 9.
Aroyan, et al., “Pyrimidine derivatives. XXXV. Synthesis of 2, 4-bis(arylamino)- and 2, 4-bis(aryloxy)-5- (p-alkoxybenzyl)-6-methylpyrimidines”,Chemical Abstracts, 1975, p. 601, vol. 82, No. 23.
Aroyan, et al., “Synthesis and some reactions of 4-hydroxy-5-(p-alkoxybenzyl)-6-methyl-2-mercapto- (and 2-amino- )pyrimidines”Chemical Abstracts, 1968, p. 1241, vol. 68, No. 3.
Awaya, et al. “Neurotropic Pyrimidine Heterocycle Compounds. I. The Newly Synthesized Pyrimidine Compounds Promote Neurite Outgrowth of GOTO and Neuro 2a Neuroblastoma Cell Lines, and Potentiate Nerve Growth Factor (NGF)-Induced Neurite Sprouting of PC 12 Cells”,Biol. Pharm. Bull., 1993, pp. 248-253, Pharmaceutical Society of Japan, vol. 16(3).
Chemical Abstracts, 1997, p. 620, col. 2, vol. 126, No. 7, abstract No. 89387x.
Curd, et al. “74. Synthetic antimalarials. Part VII. 2-Arylamino-4-dialkylaminoalkylaminopyrimidines. Variation of substituents in the 5- and the 6-position”J. Chem. Soc., 1946, pp. 378-384.
E.A. Coats et al., “Correlation Analysis of Pyrimidine Folic Acid Antagonists as Antibacterial Agents .I.”,Euro. J. Med. Chem.—Chemica Therapeutica, May 1979, pp. 261-270, vol. 14, No. 3, Editions Scientifique Elsevier, Paris.
Falco, et al. “5-Arylthiopyrimidines. I. 2, 4-Diamino Derivatives”,J. Org. Chem.., 1961, pp. 1143-1146, vol. 26.
Goldberg, A., “No. 218. Préparation de quelques 5-benzyl pyrimidines”Bulletin De La Societe Chimique France, 1951, pp. 895-899.
Hull, et al. “70. Synthetic antimalarials. Part III. Some derivatives of mono- and di-alkylpyrimidines”,J. Chem. Soc., 1946, pp. 357-362.
Hull, et al. “9. Synthetic antimalarials. Part XI. The effect of variation of substituents in derivatives of mono- and di-alkylpyrimidines”J. Chem. Soc., 1947, pp. 41-52.
Kramer, et al., “Pyrimidine derivatives. XVI. 4-(p-Alkoxyphenyl)-2, 6-dimethyl-4-pyrimidinylaminophosphonic diaziridides”,Chemical Abstracts, 1970, p. 326, vol. 73, No. 7.
Lehmann, et al.,Neurite Outgrowth of Neurons of Rat Dorsal Root Ganglia Induced By New Neurotrophic Substances With Guanidine Group, Neuroscience Letters, 1993, pp. 57-60, Elsevier Scientific Publishers Ireland, Ltd. vol. 152.
Ordukhanyan, et al., “Study of the relation between structure and biological activity. II. Antineoplastic activity of pyrimidine derivatives”,Chemical Abstracts, 1980, p. 25, vol. 92, No. 3.
Roth, et al. “5-Arylthiopyrimidines. II. 2- and 4-Alkylamino and 4-Amino Derivatives”,J. Org. Chem.., 1961, pp. 2770-2778, vol. 26.
Roth, et al. “5-Benzyl-2,4-diaminopyrimidines as antibacterial agents. I. Synthesis and antibacterial activity in vitro”J. Med. Pharm. Chem.., 1962, pp. 1103-1123, vol. 5.
Samano, et al., “An Improved Synthesis of 2-Amino-5-[(4-chlorophenyl)thio]-4-morpholinopyrimidine (BW 394U)—A Potential Antisenility Agent”,J. Heterocyclic Chem., Jan.-Feb. 2000, pp. 183-185, vol. 37.
Vaillancourt, et al., “Synthesis and Self-Association of 4-Pyrimidinones”,J. Org. Chem., 1998, pp. 9746-9752, vol. 63, No. 26.

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