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United States Patent 19 11 Patent Number: 5,439,930 Seredenin Et Al

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United States Patent 19 11 Patent Number: 5,439,930 Seredenin Et Al US005439930A United States Patent 19 11 Patent Number: 5,439,930 Seredenin et al. 45. Date of Patent: Aug. 8, 1995 54 BIOLOGICALLY ACTIVE al., pp. 293-301, "Variations in the Turn-Forming N-ACYLPROLYDIPEPTDES HAVING Characteristics of N-Acyl Proline Units’. ANTIAMNESTIC, ANTIHYPOXIC AND European Biophysical Journal, vol. 14, No. 1, (1986) pp. ANOREXIGENCEFFECTS 43-51, M. McHarfi et al., "Backbone Side-Chain Inter 75) Inventors: Sergei B. Seredenin; Tatiana A. actions in Peptides'. Voronina; Tatiana A. Gudasheva; Rita Inorganic Chemistry, vol. 27, No. 22, (Nov. 2, 1988) pp. U. Ostrovskaya; Grigori G. 4046-4052, Y. N. Belokon, “Copper(II) Ion Promoted Rozantsev; Alexander P. Skoldinov; Direct Hydrolysis of 2-Cyanopyridine to Picolinic Sergei S. Trophimov, all of Moscow, Acid, Intramolecular Catalysis by the Coordinated Russian Federation; James A. N-beta-Hydroxyethyl Group'. Halikas, North Oaks, Minn.; Taisija Peptides 1990, Proceedings of the 21. Peptide Sympo L. Garibova, Moscow, Russian sium, Sep. 2-8, (1990), E. Giralt and D. Andreu, 1991 Federation ESCOM Publishers, Leiden, NL, pp. 462-464, G. Pietr zynski et al., "Conformational Propensities of Moel 73) Assignee: Russian-American Institute for New Peptides with Alpha, Beta-Dehydroamino Acids'. Drug Development, Bloomington, Journal of the Chemical Society, Perkin Transaction 1, Minn. (1981) pp. 1639-1646, J. S. Davies and R. J. Thomas, 21 Appl. No.: 960,905 "Studies on the Diastereoisomeric and Conformational Aspects of Benzoyl Dipeptide Esters, as a Means of 22 Filed: Oct. 14, 1992 Assessing Racemisation using Neuclear Magnetic Reso nance Spectroscopy'. Related U.S. Application Data 63 Continuation-in-part of Ser. No. 868,000, Apr. 14, (List continued on next page.) 1992, abandoned. Primary Examiner-Joseph Paul Brust 51) Int. Cl...................... A61K 31/40; C07D 207/12 Attorney, Agent, or Firm-Merchant, Gould, Smith, 52 U.S.C. .................................... 514/423: 548/533; Edell, Welter & Schmidt 54.8/537 58) Field of Search ................. 548/533, 537; 514/423 57 ABSTRACT A novel class of substances of N-acyl-prolyldipeptides, 56) References Cited which possess psychotropic activity and particularly U.S. PATENT DOCUMENTS facilitate learning and memory are described. The N 4,093,713 6/1978 Sestanjet al........................ 424/177 acyl-prolyldipeptides of the invention have the formula: 4,743,616 5/1988 Tanaka et al. ...................... 514/423 (1) OTHER PUBLICATIONS O R2 O Journal of the Chemical Society, Perkin Transactions 1, No. 11, (Nov. 1990) pp. 3103-3108; B. C. Challis et al. N C-NHCHCCH2)C “Synthesis and Characterisation of Some New N-Ni o=-R R3 trosodipeptides'. wherein R=(C4-Cs) alkyl, cycloalkyl, aralkyl, or aryl; Biopolymers, vol. 28, No. 1, (Jan. 1989) pp. 109-122, A. R2=H (C1-C4) alkyl, carbamidoalkyl, or carbalkoxy Aubry and M. Marraud, "Pseudopeptides and beta alkyl; R3 = NH2, NH(alkyl), N(alkyl)2, OH, or alkoxy; Folding: X-Ray Structures Compared with Structures and n=0-3, preferably 0–2. in Solution'. Biopolymers, vol. 32, No. 3, (Mar. 1992) G. B. Liang et 25 Claims, No Drawings 5,439,930 Page 2 OTHER PUBLICATIONS T. A. Gudasheva et al., Chem. Pharmac. J., 1988, N 3, pp. 271-275. Chemical Abstracts, vol. 111, No. 19, (Nov. 6, 1989), G. B. Liang et al., Chem. Abs., 116, Abstract No. Columbus, Ohio, U.S.; abstract No. 16676, T. A. Guda 116:214897k (1992). sheva et al., "Topological Proline-based Analogs of V. Y. Podlipskii et al., Chem. Abs., 112, 780, Abstract Piracetam and their Nootropic Activity'. No. 112:158881d (1990). L. Amaducci et al., Pharmacopsychiatry, 23, 171-175 V. Y. Podlipskii et al., Chem. Abs., 112, 786, Abstract (1990). No. 112:158955f (1990). A. Aubry et al., Chem. Abs., 87, 614, Abstract No. R. C. Thompson et al., Chem. Abs., 78, 184, Abstract 87:168404e (1977). No.78:107639c (1973). G. Boussard et al., Chem. Abs., 81, 458, Abstract No. T. A. Voronina et al., Ann. Ist. Super. Sanita, 24, N 3, 81:136515b (1974). pp. 461–466 (1988). G. Boussard et al., Chem. Abs., 91, Abstract No. T. A. Voronina et al., Ann. Ist. Super. Sanita, 26, N 1, 91:141207p (1979). pp. 55-60 (1990). T. A. Gudasheva et al., Chem. Pharmac. J., 1985, N 11, T. A. Voronina et al., Drug Development Research, 14, pp. 1322-1329. 353-358 (1988). 5,439,930 1. BIOLOGICALLY ACTIVE (l) N-ACYTLPROLYDIPEPTOES HAVING O ANTIAMNESTIC, ANTIHYPOXIC AND ( y i. ANOREXIGENCEFFECTS N c-NHCHCH) o=l-R R3 CROSS REFERENCE TO RELATED APPLICATIONS wherein: R=(C4-Cs) alkyl, cycloalkyl, aralkyl, or aryl; The present application is a Continuation-In-Part 10 R2=H1 (C1-C4) alkyl, carbamidoalkyl, or carbalk application of U.S. application Ser. No. 07/868,000, oxyalkyl; filed Apr. 14, 1992, now abandoned. R3=NH2, NH(alkyl), N(alkyl)2, OH, or alkoxy; and BACKGROUND OF THE INVENTION n=0-3, preferably 0-2. In the compound represented by Formula 1, R is Nootropic agents (cognitive enhancers) constitute a 15 preferably selected from the group consisting of isobu promising group of medicines. Known nootropic agents tyl, pentyl, 1-adamantyl, phenyl, phenylmethyl, and include piracetam (N-carbamido-methyl-pyrrolidone phenylpropyl, and more preferably selected from the 2), which was introduced into wide medical practice in the early 1980s. Other N-substituted-2-pyrrollidones group consisting of phenylmethyl and phenyl. R3 is 20 preferably selected from the group consisting of amino (e.g. etiracetan, oxiracetam, aniracetam, pramiracetan, (NH2), methylamino (NHCH3), dimethylamino rolziracetam, etc.) have been synthesized. (N(CH3)2), hydroxy (OH), and ethoxy (OC2H5), and U.S. Pat. No. 4,743,616 to Tanaka et al. describes more preferably selected from the group consisting of N-acyl pyrrolidine compounds having endopeptidase amino and ethoxy. inhibitory activity and which are reported to exhibit 25 Compounds of Formula 1 differ from known noo antiamnestic effects. Unlike the piracetam derivatives, tropic agents in that the compounds of Formula 1 con the compounds described by Tanaka et al. contain a tain in their structure a residue of the natural amino proline group. acid, L-proline (instead of pyrrolidone), together with a Biologically active N-terminal pyroglutamic acid residue of a second natural amino acid. These N-acyl-L- compounds having the formula: 30 proline derived dipeptide compounds have an ex tremely low toxicity and are highly active. Following are compounds illustrative of the scope of this invention: OA N \,C-NHCHCONH2 . 35 H I. N-phenacetyl-L-prolylglycine ethyl ester II. N-phenacetyl-L-prolylglycine amide have been reported by T. Gudasheva and R. Ostrov III. N-phenacetyl-L-prolyl-6-alanine ethyl ester skaya (Chem. Pharmac. J., 1985, N 11, pp. 1322-1329). IV. N-phenylacetyl-L-prolyl-3-alanine amide Another reported (T. A. Gudasheva et al., Chem. Phar V. N-phenylacetyl-L-prolyl-L-aspartic acid diethyl mac. J., 1988, N 3, pp. 271-275) biologically active ester compound is N-acylproline having the formula: VI. N-phenylacetyl-L-prolyl-L-asparagine amide VII. N-benzoyl-L-prolylglycine ethyl ester VIII. N-isovaleryl-L-prolylglycine ethyl ester 45 IX. N-phenylacetyl-L-prolyl-L-valine ethyl ester X. N-benzoyl-L-prolyl-L-valine ethyl ester XI. N-benzoyl-L-prolyl-g-alanine ethyl ester XII. N-benzoyl-L-prolyl-g-alanine amide XIII. N-benzoyl-L-prolylglycine amide 50 XIV. N-phenylacetyl-L-prolylglycine N-methylamide XV. N-phenylacetyl-L-prolylglycine dimethylamide A substantial need exists for highly active and non XVI. N-phenylacetyl-L-prolyl-L-glutamic acid diethyl toxic nootropic agents which can be used for treatment ester of mental decline, caused by different damaging factors. XVII. N-phenylacetyl-L-prolyl-L-leucine amide The present invention is directed to addressing this 55 XVIII. N-phenylacetyl-L-prolylglycine need. XIX. N-phenylacetyl-L-prolyl-GABA methylester XX. N-phenylacetyl-L-prolyl-L-alanine ethyl ester SUMMARY OF THE INVENTION XXI. N-caproyl-L-prolylglycine ethyl ester The present invention relates to a novel group of XXII. N-(1-adamantoyl)-L-prolylglycine ethyl ester compounds, which possess different types of psycho 60 XXIII. N-phenylbutyl-L-prolyl-glycine ethylester tropic activity, particularly antiamnestic, antihypoxic and anorexigenic effects. The invention also relates to a The present invention is also directed to a pharma method for chemical synthesis of such novel con ceutical compositions and methods of medical treat pounds as well as their use as drugs for treatment, espe 65 ment that include as an active substance a pharmaceuti cially of different forms of memory disturbances. cally effective amount of an N-acylprolyldipeptide of The present invention provides N-acyl-prolyldipep Formula 1, as defined above, preferably a compound of tides of the formula: the formula: 5,439,930 3 4 by converting it into a phosphite-amide or by resorting to the “phosphoraso' method. R--L-pro-Gly-R The most common techniques for the above conden O sation reactions are: the carbodiimide method; the azide 5 method; the method of mixed anhydrides; and the wherein R is preferably selected from the group con method of activated esters. These methods are de sisting of iso-butyl, pentyl, 1-adamantyl, phenyl, phe scribed in “The Peptides', Vol. 1, 1965 (Academic nylmethyl, and phenylpropyl; and R3 is preferably se Press), E. Schröder and K. Libke, or in “The Pep lected from the group consisting of NH2, NHCH3, tides', Vol. 1, 1979 (Academic Press), E. Gross and L. N(CH3)2, OH, and OC2H5. More preferably, the phar 10 Meinhofen. maceutical compositions and methods of treatment of The preferable condensation methods of obtaining the present invention include an effective dose of a Formula 1 peptides are the method of mixed anhydrides compound of the formula: or the carbodiimide method.
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