-
1
-
-
0000549359
-
Antipsychotic agents
-
Wolf, M. E., Ed. 5th. edition. Therapeutic Agents. Wiley Interscience
-
1. Martin, A. R. Antipsychotic Agents. In Burger's Medicinal Chemistry and Drug Discovery; Wolf, M. E., Ed. 5th. edition. Therapeutic Agents. Wiley Interscience, 1997; vol 5, p. 195.
-
(1997)
Burger's Medicinal Chemistry and Drug Discovery
, vol.5
, pp. 195
-
-
Martin, A.R.1
-
2
-
-
0344937935
-
-
2. (a) Seemann, P. Synapse 1987, 192, 481-483;
-
(1987)
Synapse
, vol.192
, pp. 481-483
-
-
Seemann, P.1
-
4
-
-
0025599851
-
-
3. For a review of pharmacological properties and therapeutic uses of clozapine see Fitton, A.; Heel, R. C. Drugs 1990, 40, 722
-
(1990)
Drugs
, vol.40
, pp. 722
-
-
Fitton, A.1
Heel, R.C.2
-
5
-
-
0024447747
-
-
4. Ereshevsky, L.; Watanabe, N. D.; Trau-Johnson, T. K. Clin. Pharm. 1989, 8, 691.
-
(1989)
Clin. Pharm.
, vol.8
, pp. 691
-
-
Ereshevsky, L.1
Watanabe, N.D.2
Trau-Johnson, T.K.3
-
6
-
-
0021943587
-
-
5. Ceulemans, D. L. S.; Gelders, Y. G.; Hoppenbrouwers, M. L.; Reyntjens, A. J. M.; Janssen, P. A. J. Psychopharmacology 1985, 85, 329.
-
(1985)
Psychopharmacology
, vol.85
, pp. 329
-
-
Ceulemans, D.L.S.1
Gelders, Y.G.2
Hoppenbrouwers, M.L.3
Reyntjens, A.J.M.4
Janssen, P.A.J.5
-
7
-
-
0023850460
-
-
6. (a) Janssen, P. A. J.; Niemegeers, C. J. E.; Awouters, F.; Schellekens, K. H.; Megens, A. A. H. P.; Meert, T. F. J. J. Pharmacol. Exp. Ther. 1988, 244, 685-693;
-
(1988)
J. Pharmacol. Exp. Ther.
, vol.244
, pp. 685-693
-
-
Janssen, P.A.J.1
Niemegeers, C.J.E.2
Awouters, F.3
Schellekens, K.H.4
Megens, A.A.H.P.5
Meert, T.F.J.6
-
8
-
-
0023756442
-
-
(b) Leysen, J. E.; Gommeren, W.; Eens, A.; De Chaffoy de Courcelles, D.; Stoof, J. C.; Jansen, P. A. J. J. Pharmacol. Exp. Ther. 1988, 247, 661-670.
-
(1988)
J. Pharmacol. Exp. Ther.
, vol.247
, pp. 661-670
-
-
Leysen, J.E.1
Gommeren, W.2
Eens, A.3
De Chaffoy De Courcelles, D.4
Stoof, J.C.5
Jansen, P.A.J.6
-
9
-
-
0024466603
-
-
7. (a) Meltzer, H. Y. ; Matsubara, S.; Lee, J. C. J. Pharmacol. Exp. Ther. 1989, 251, 238 ;
-
(1989)
J. Pharmacol. Exp. Ther.
, vol.251
, pp. 238
-
-
Meltzer, H.Y.1
Matsubara, S.2
Lee, J.C.3
-
10
-
-
0024854809
-
-
(b) Meltzer, H. C. ; Matsubara, S.; Lee, J. C. Psychopharmacol. Bull. 1989, 255, 390;
-
(1989)
Psychopharmacol. Bull.
, vol.255
, pp. 390
-
-
Meltzer, H.C.1
Matsubara, S.2
Lee, J.C.3
-
12
-
-
0025783781
-
-
8. Cortizo, L.; Santana, L.; Raviña, E.; Orallo, F.; Fontenla, J. A.; Castro, E.; de Ceballos, M. J. Med. Chem. 1991, 34, 2242-2247.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2242-2247
-
-
Cortizo, L.1
Santana, L.2
Raviña, E.3
Orallo, F.4
Fontenla, J.A.5
Castro, E.6
De Ceballos, M.7
-
13
-
-
0026353198
-
-
9. Loza, I.; Verde, I.; Orallo, F.; Fontenla, J. A.; Calleja, J. M.; Raviña, E.; Cortizo, L.; de Ceballos, M. Bioorg. Med. Chem. Lett. 1991, 1, 717-720.
-
(1991)
Bioorg. Med. Chem. Lett.
, vol.1
, pp. 717-720
-
-
Loza, I.1
Verde, I.2
Orallo, F.3
Fontenla, J.A.4
Calleja, J.M.5
Raviña, E.6
Cortizo, L.7
De Ceballos, M.8
-
14
-
-
0027174892
-
-
10. Loza, I.; Ferreiro, T. G.; Sanz, F.; Lozoya, E.; Rodriguez, J.; Manaut, F.; Verde, I.; Castro, E.; Fontenla, J. A.; Cadavid, I.; Honrubia, M.; Fueyo, J.; Raviña, E. J. Pharm. Sci. 1993, 82, 513.
-
(1993)
J. Pharm. Sci.
, vol.82
, pp. 513
-
-
Loza, I.1
Ferreiro, T.G.2
Sanz, F.3
Lozoya, E.4
Rodriguez, J.5
Manaut, F.6
Verde, I.7
Castro, E.8
Fontenla, J.A.9
Cadavid, I.10
Honrubia, M.11
Fueyo, J.12
Raviña, E.13
-
15
-
-
0028040921
-
-
11. Fontenla, J. A.; Osuna, J. A.; Rosa, E.; Castro, E.; Loza, I.; G-Ferreiro, T.; Calleja, J. M.; Sanz, F.; Rodriguez, J.; Fueyo, J.; Raviña, E.; Masaguer, C. F.; Vidal, A.; de Ceballos, M. J. Med. Chem. 1994, 37, 2564-2573.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 2564-2573
-
-
Fontenla, J.A.1
Osuna, J.A.2
Rosa, E.3
Castro, E.4
Loza, I.5
G-Ferreiro, T.6
Calleja, J.M.7
Sanz, F.8
Rodriguez, J.9
Fueyo, J.10
Raviña, E.11
Masaguer, C.F.12
Vidal, A.13
De Ceballos, M.14
-
16
-
-
0029989582
-
-
12. Raviña, E., Fueyo, J.; Masaguer, C. F.; Negreira, J.; Cid, J.; Loza, I.; Honrubia, H.; Tristan, H.; Ferreiro, T. G.; Fontenla, J. A.; Rosa, E.; Calleja, J. M.; de Ceballos, M. L. Chem. Pharm. Bull. 1996, 44, 534-541.
-
(1996)
Chem. Pharm. Bull.
, vol.44
, pp. 534-541
-
-
Raviña, E.1
Fueyo, J.2
Masaguer, C.F.3
Negreira, J.4
Cid, J.5
Loza, I.6
Honrubia, H.7
Tristan, H.8
Ferreiro, T.G.9
Fontenla, J.A.10
Rosa, E.11
Calleja, J.M.12
De Ceballos, M.L.13
-
17
-
-
0028947553
-
-
13. Raviña, E.; Masaguer, C. F.; Cid, J.; Casariego, I.; Fontenla, J. A.; Ferreiro, T. G.; Cadavid, I.; Loza, I.; de Ceballos, M. L. Bioorg. Med. Chem. Lett. 1995, 5, 579-584.
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 579-584
-
-
Raviña, E.1
Masaguer, C.F.2
Cid, J.3
Casariego, I.4
Fontenla, J.A.5
Ferreiro, T.G.6
Cadavid, I.7
Loza, I.8
De Ceballos, M.L.9
-
19
-
-
0030907274
-
-
15. Masaguer, C. F.; Raviña, E.; Fontenla, J. A.; Loza, I. Bioorg. Med. Chem. Lett. 1997, 7, 913-918.
-
(1997)
Bioorg. Med. Chem. Lett.
, vol.7
, pp. 913-918
-
-
Masaguer, C.F.1
Raviña, E.2
Fontenla, J.A.3
Loza, I.4
-
21
-
-
24544438607
-
2C) Affinities. Sinthesis of Aminoalquil thienocycloalkanones as Putative Atypical Antipsychotics
-
submitted
-
2C) Affinities. Sinthesis of Aminoalquil thienocycloalkanones as Putative Atypical Antipsychotics. J. Med. Chem. (submitted).
-
J. Med. Chem.
-
-
Raviña, E.1
Negreira, J.2
Cid, J.3
Masaguer, C.F.4
Rosa, E.5
Rivas, M.E.6
Fontenla, J.A.7
Loza, I.8
Cadavid, I.9
Sanz, F.10
Carotti, A.11
Carrieri, A.12
-
23
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0344937931
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note
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19. Compound QF 0510B does not produce catalepsy at dose as high as 20 mg/Kg.
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24
-
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0017916143
-
-
20. (a) Boswell, R. F.; Welstead, W. J.; Duncan, R. C.; Funderburk, W. H. J. Med. Chem. 1978, 21, 136;
-
(1978)
J. Med. Chem.
, vol.21
, pp. 136
-
-
Boswell, R.F.1
Welstead, W.J.2
Duncan, R.C.3
Funderburk, W.H.4
-
25
-
-
0027082075
-
-
(b) Herndon, J. L.; Ismaiel, A.; Ingher, S. P.; Teitler, M.; Glennon, R. A. J. Med. Chem. 1992, 35, 4903.
-
(1992)
J. Med. Chem.
, vol.35
, pp. 4903
-
-
Herndon, J.L.1
Ismaiel, A.2
Ingher, S.P.3
Teitler, M.4
Glennon, R.A.5
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26
-
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0020052842
-
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21. (a) Shustke, G. M.; Setescak, L. L.; Allen, R. C.; Davis, L.; Effland, R. E.; Ranbom, K.; Kitzen, J. M.; Wilker, J. C.; Novick, W. J. J. Med. Chem. 1982, 25, 36;
-
(1982)
J. Med. Chem.
, vol.25
, pp. 36
-
-
Shustke, G.M.1
Setescak, L.L.2
Allen, R.C.3
Davis, L.4
Effland, R.E.5
Ranbom, K.6
Kitzen, J.M.7
Wilker, J.C.8
Novick, W.J.9
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27
-
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0021808398
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(b) Strupezewski, J. T.; Allen, R. C.; Gardenr, B. A.; Schmid, B. L.; Stache, U ; Glankowski, E. J.; Jones, M. C.; Ellis, D. B.; Huger, F. P.; Dunn, R. W. J. Med. Chem. 1985, 28, 761.
-
(1985)
J. Med. Chem.
, vol.28
, pp. 761
-
-
Strupezewski, J.T.1
Allen, R.C.2
Gardenr, B.A.3
Schmid, B.L.4
Stache, U.5
Glankowski, E.J.6
Jones, M.C.7
Ellis, D.B.8
Huger, F.P.9
Dunn, R.W.10
-
30
-
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0000414271
-
-
23. For the Fischer indolization mechanism, see: Hughes, D. L.; Zhao, D. J. Org. Chem. 1993, 58, 228.
-
(1993)
J. Org. Chem.
, vol.58
, pp. 228
-
-
Hughes, D.L.1
Zhao, D.2
-
31
-
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0017916143
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24. The 4-(p-fluorobenzoyl)piperidine fragment may be considered as a butyrophenone moiety constrained in a six-membered ring. The importance of this fragment on CNS agents acting compounds is well known. See, among others, (a) Boswell, R. F., Jr.; Welstead, W. J., Jr.; Duncan, R. L., Jr.; Johnson, D. N.; Funderburk, W. H. J. Med. Chem. 1978, 21, 136-138;
-
(1978)
J. Med. Chem.
, vol.21
, pp. 136-138
-
-
Boswell, R.F.J.1
Welstead W.J., Jr.2
Duncan R.L., Jr.3
Johnson, D.N.4
Funderburk, W.H.5
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32
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0027082075
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(b) Herndon, J. L.; Ismaiel, A.; Ingher, S. P.; Teitler, M.; Glennon, R. A. J. Med. Chem. 1992, 35, 4903-4910;
-
(1992)
J. Med. Chem.
, vol.35
, pp. 4903-4910
-
-
Herndon, J.L.1
Ismaiel, A.2
Ingher, S.P.3
Teitler, M.4
Glennon, R.A.5
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33
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0028943137
-
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(c) Ismaiel, A. M.; Arruda, K.; Teitler, M.; Glennon, R. A. J. Med. Chem. 1995, 38, 1196-1202.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 1196-1202
-
-
Ismaiel, A.M.1
Arruda, K.2
Teitler, M.3
Glennon, R.A.4
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34
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0028943137
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2A receptor interactions. A key structural feature that may play a prominent role in these interactions would be the benzylic carbonyl group. Ismaiel, A. M.; Arruda, K.; Teitler, M.; Glennon, R. A. J. Med. Chem. 1995, 38, 1196-1202.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 1196-1202
-
-
Ismaiel, A.M.1
Arruda, K.2
Teitler, M.3
Glennon, R.A.4
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35
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0020052842
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26. The bioisosteric relationships between benzoyl and 1,2-benzisoxazole moieties are notheworthy. See: (a) Shustke, G. M.; Setescak, L. L.; Allen, R. C.; Davis, L.; Effland, R. E.; Ranbom, K.; Kitzen, J. M.; Wilker, J. C.; Novick, W. J. J. Med. Chem. 1982, 25, 36-44;
-
(1982)
J. Med. Chem.
, vol.25
, pp. 36-44
-
-
Shustke, G.M.1
Setescak, L.L.2
Allen, R.C.3
Davis, L.4
Effland, R.E.5
Ranbom, K.6
Kitzen, J.M.7
Wilker, J.C.8
Novick, W.J.9
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36
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0021808398
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(b) Strupezewski, J. T.; Allen, R.C.; Gardenr, B. A.; Schimid, B. L.; Stache, U.; Glankowzki, E. J.; Jones, M. C.; Ellis, D. B.; Huger, F. P.; Dunn, R. W. J. Med. Chem. 1985, 28, 761-769.
-
(1985)
J. Med. Chem.
, vol.28
, pp. 761-769
-
-
Strupezewski, J.T.1
Allen, R.C.2
Gardenr, B.A.3
Schimid, B.L.4
Stache, U.5
Glankowzki, E.J.6
Jones, M.C.7
Ellis, D.B.8
Huger, F.P.9
Dunn, R.W.10
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37
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0344075890
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note
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2O: C, 76.02%; H, 8.51%; N, 9.85%. Found: C, 76.30%; H, 8.63%; N, 9.57%.
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38
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0344075889
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note
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13C-NMR, FTIR, MS). Yields given correspond to isolated pure compounds.
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