| PATENT ASSIGNEE'S COUNTRY | USA |
| UPDATE | 05.00 |
| PATENT NUMBER | This data is not available for free |
| PATENT GRANT DATE | 09.05.00 |
| PATENT TITLE |
Azolo triazines and pyrimidines |
| PATENT ABSTRACT | Corticotropin releasing factor (CRF) antagonists of formula I or II: ##STR1## and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress. |
| PATENT INVENTORS | This data is not available for free |
| PATENT ASSIGNEE | This data is not available for free |
| PATENT FILE DATE | 28.01.98 |
| PATENT REFERENCES CITED |
Arch. Pharm. (Weinheim) 320, 487-491 (1987). Psychopharmacology (Britton, Lee, Koob) 94:306-311 (1988). Life Sciences (Britton, Koob, Rivier, Vale) 31:363-367 (1982). Bull. Soc. Chim. Belg. (Maquestiau, Taghret, Eynde) vol. 101/No. 2/1992. J. Med. Chem. (Senga, et al.) 25:243-249 (1982). J. Med. Chem. (Senga, et al.) 25:243-249 (1982). Synapse (Battaglia, Webster, De Souza), 1:572-581 (1987). Science (Nemeroff, et al.) 226:1342 (1984). Brain Research Reviews (Dunn, Berridge) 15:71-100 (1990). Proc. Natl. Acad. Sci. (Rivier, Spiess, Vale) 80:4851-4855 (1983). Recent Progress in Hormone Research (Vale, et al.) 39:245-271 (1983). Journal of Neuroscience (De Souza, et al.) vol. 5, No. 12, p. 3189-3203 (1985). Perspectives on Behavioral Medicine (Koob) 2:39-52 (1985). Biol. Psychiatry (France, et al.) 23:86-88 (1988). Hormones and Behavior (Berridge, Dunn) 21:393-401 (1987). Hospital Practice (De Souza) p. 59-71 (1988). Arch. Gen. Psychiatry (Sapolsky) 46:1047-1051 (1989). Psychopharmacology (Britton, et al.) 86:170-174 (1985). Biol. Psychiatry (Arato, et al.) 25:355-359 (1989). Regulatory Peptides (Berridge, Dunn) 16:83-93 (1986). Neuropsychopharmacology (Grigoriadis, et al.) vol. 2, No. 1, p. 53-60 (1989). Psychopharmacology (Swerdlow, Geyer, Vale, Koob) 88:147-152 (1986). Am. J. Psychiatry (Banki, et al.) 144:873-877 (1987). Arch. Gen. Psychiatry (Nemeroff, et al.) 45:577-579 (1988). New Eng. J. Med. (Gold, et al.) vol. 314, No. 21, p. 1329-1335 (1986). Life Sciences (Morley, et al.) 41:527-544 (1987). Physiological Reviews (Blalock) vol. 69, No. 1, p. 1-33 (1989). Journal f.prakt. Chemie. (Joshi, Dubey) Band 321, Heft 2, p. 341-344 (1979). Journal of Medicinal Chemistry (Springer, et al.) vol. 19, No. 2, p. 291-296 (1976). J. Heterocyclic Chem. (O'Brien, et al.) 22:601-634 (1985). J. Med. Chem. (Senga, Novinson, Wilson) 24:610-613 (1981). Science, (Vale, et al.) 213:1394-1397 (1981). Chemical Abstracts, vol. 67, No. 28, 1967, abstract # 108663r. Chemical Abstracts, vol. 74, No. 28, 1971, abstract # 22867t. Chemical Abstracts, vol. 74, No. 28, 1971, abstract # 22872r. Chemical Abstracts, vol. 68, No. 28, 1968, abstract # 114635v. Corticotropin Releasing Factor: Basic and Clinical Studies of a Neuropeptide (De Souza, Nemeroff) p. 221-224 (1990). Comprehensive Organic Synthesis (Trost, Fleming) 3:481-520 (1991). Comprehensive Organic Synthesis (Trost, Fleming) 7:762-769 (1991). Remington's Pharmaceutical Sciences (Gennaro, ed.) 17.sup.th ed. P. 1418-1419 (1985). |
| PATENT PARENT CASE TEXT | This data is not available for free |
| PATENT CLAIMS |
What is claimed is: 1. A compound of Formulae (1) or (2): ##STR48## and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein: Z is N or CR.sup.2 ; Ar is selected from phenyl, naphthyl, pyridyl, pyrimidinyl, triazinyl, furanyl, thienyl, benzothienyl, benzofuranyl, 2,3-dihydrobenzofuranyl, 2,3-dihydrobenzothienyl, indanyl, 1,2-benzopyranyl, 3,4-dihydro-1,2-benzopyranyl, tetralinyl, each Ar optionally substituted with 1 to 5 R.sup.4 groups and each Ar is attached to an unsaturated carbon atom; R is independently selected at each occurrence from H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.7 cycloalkylalkyl, halo, CN, C.sub.1 -C.sub.4 haloalkyl; R.sup.1 is independently selected at each occurrence from H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, halo, CN, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.12 hydroxyalkyl, C.sub.2 -C.sub.12 alkoxyalkyl, C.sub.2 -C.sub.10 cyanoalkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, NR.sup.9 R.sup.10, C.sub.1 -C.sub.4 alkyl-NR.sup.9 R.sup.10, NR.sup.9 COR.sup.10, OR.sup.11, SH or S(O).sub.n R.sup.12 ; R.sup.2 is selected from H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.1 -C.sub.4 hydroxyalkyl, halo, CN, --NR.sup.6 R.sup.7, NR.sup.9 COR.sup.10, --NR.sup.6 S(O).sub.n R.sup.7, S(O).sub.n NR.sup.6 R.sup.7, C.sub.1 -C.sub.4 haloalkyl, --OR.sup.7, SH or --S(O).sub.n R.sup.12 ; R.sup.3 is selected from: --H, OR.sup.7, SH, S(O).sub.n R.sup.13, COR.sup.7, CO.sub.2 R.sup.7, OC(O)R.sup.13, NR.sup.8 COR.sup.7, N(COR.sup.7).sub.2, NR.sup.8 CONR.sup.6 R.sup.7, NR.sup.8 CO.sub.2 R.sup.13, NR.sup.6 R.sup.7, NR.sup.6a R.sup.7a, N(OR.sup.7)R.sup.6, CONR.sup.6 R.sup.7, aryl, heteroaryl and heterocyclyl, or --C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl, C.sub.4 -C.sub.12 cycloalkylalkyl or C.sub.6 -C.sub.10 cycloalkenylalkyl, each optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.13, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.13, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.13, NR.sup.16 R.sup.15, CONR.sup.16 R.sup.15, aryl, heteroaryl and heterocyclyl; R.sup.4 is independently selected at each occurrence from: C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.12 cycloalkylalkyl, NO.sub.2, halo, CN, C.sub.1 -C.sub.4 haloalkyl, NR.sup.6 R.sup.7, NR.sup.8 COR.sup.7, NR.sup.8 CO.sub.2 R.sup.7, COR.sup.7, OR.sup.7, CONR.sup.6 R.sup.7, CO(NOR.sup.9)R.sup.7, CO.sub.2 R.sup.7, or S(O).sub.n R.sup.7, where each such C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.6 cycloalkyl and C.sub.4 -C.sub.12 cycloalkylalkyl are optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.4 alkyl, NO.sub.2, halo, CN, NR.sup.6 R.sup.7, NR.sup.8 COR.sup.7, NR.sup.8 CO.sub.2 R.sup.7, COR.sup.7 OR.sup.7, CONR.sup.6 R.sup.7, CO.sub.2 R.sup.7, CO(NOR.sup.9)R.sup.7, or S(O).sub.n R.sup.7 ; R.sup.6, R7, R.sup.6a and R.sup.7a are independently selected at each occurrence from: --H, --C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 alkenyl, C.sub.3 -C.sub.10 alkynyl, C.sub.1 -C.sub.10 haloalkyl with 1-10 halogens, C.sub.2 -C.sub.8 alkoxyalkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.12 cycloalkylalkyl, C.sub.5 -C.sub.10 cycloalkenyl, or C.sub.6 -C.sub.14 cycloalkenylalkyl, each optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.13, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.13, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.13, NR.sup.16 R.sup.15, CONR.sup.16 R.sup.15, aryl, heteroaryl or heterocyclyl, -aryl, aryl(C.sub.1 -C.sub.4 alkyl), heteroaryl, heteroaryl(C.sub.1 -C.sub.4 alkyl), heterocyclyl or heterocyclyl(C.sub.1 -C.sub.4 alkyl), alternatively, NR.sup.6 R.sup.7 and NR.sup.6a R.sup.7a are independently piperidine, pyrrolidine, piperazine, N-methylpiperazine, morpholine or thiomorpholine, each optionally substituted with 1-3 C.sub.1 -C.sub.4 alkyl groups; R.sup.8 is independently selected at each occurrence from H or C.sub.1 -C.sub.4 alkyl; R.sup.9 and R.sup.10 are independently selected at each occurrence from H, C.sub.1 -C.sub.4 alkyl, or C.sub.3 -C.sub.6 cycloalkyl; R.sup.11 is selected from H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, or C.sub.3 -C.sub.6 cycloalkyl; R.sup.12 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl; R.sup.13 is selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.8 alkoxyalkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.12 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.4 alkyl)-, heteroaryl or heteroaryl(C.sub.1 -C.sub.4 alkyl)-; R.sup.14 is selected from C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 alkenyl, C.sub.3 -C.sub.10 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.4 -C.sub.12 cycloalkylalkyl, each optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.15, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.15, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.15, NR.sup.16 R.sup.15, CONR.sup.16 R.sup.15, and C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl and C.sub.1 -C.sub.6 alkylsulfonyl; R.sup.15 and R.sup.16 are independently selected at each occurrence from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.4 -C.sub.16 cycloalkylalkyl, except that for S(O).sub.n R.sup.15, R.sup.15 cannot be H; aryl is phenyl or naphthyl, each optionally substituted with 1 to 5 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.15, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R15, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.15, NR.sup.16 R.sup.15, and CONR.sup.16 R.sup.15 ; heteroaryl is pyridyl, pyrimidinyl, triazinyl, furanyl, pyranyl, quinolinyl, isoquinolinyl, thienyl, imidazolyl, thiazolyl, indolyl, pyrrolyl, oxazolyl, benzofuranyl, benzothienyl, benzothiazolyl, isoxazolyl, pyrazolyl, 2,3-dihydrobenzothienyl or 2,3-dihydrobenzofuranyl, each being optionally substituted with 1 to 5 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.15, --COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.15, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.15, NR.sup.16 R.sup.15, and CONR.sup.16 R.sup.15 ; heterocyclyl is saturated or partially saturated heteroaryl, optionally substituted with 1 to 5 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.15, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.15, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, NR.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.15, NR.sup.15 R.sup.16, and CONR.sup.16 R.sup.15 ; n is independently at each occurrence 0, 1 or 2; with the provisos that: (1) when Z is CR.sup.2, then R.sup.2 is not --NR.sup.6 SO.sub.2 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7 ; (2) when Z is CR.sup.2 and R.sup.2 is H, phenyl or alkyl and R.sup.3 is NR.sup.8 COR.sup.7 and Ar is phenyl or phenyl substituted with phenylthio, then R.sup.7 is not aryl, aryl(C.sub.1 -C.sub.4 alkyl), heteroaryl, heteroaryl(C.sub.1 -C.sub.4 alkyl), heterocyclyl or heterocycly(C.sub.1 -C.sub.4 alkyl); (3) when Z is CR.sup.2 and R.sup.2 is H or alkyl and Ar is phenyl and R.sup.3 is SR.sup.13 or NR.sup.6a R.sup.7a, then R.sup.13 is not aryl or heteroaryl and R.sup.6a and R.sup.7a are not H or aryl; or (4) when Z is CR.sup.2 and R.sup.1 is OR.sup.11 and R.sup.2 is H and R.sup.3 is OR.sup.7 and R.sup.7 and R.sup.11 are both H, then Ar is not phenyl, p-Br-phenyl, p-Cl-phenyl, p-NHCOCH.sub.3 -phenyl, p-CH.sub.3 -phenyl, pyridyl or naphthyl; (5) when Z is CR.sup.2 and R.sup.2 is H and Ar is unsubstituted phenyl and R.sup.3 is CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or C.sub.6 H.sub.4 F, then R.sub.1 is not CF.sub.3 or C.sub.2 F.sub.5 ; (6) when R is H and Z is CR.sup.2 and R.sup.2 is OH and R.sup.1 and R.sup.3 are H, then Ar is not phenyl; (7) when R is H and Z is CR.sup.2 and R.sup.2 is OH or NH.sub.2 and R.sup.1 and R.sup.3 are CH.sub.3, then Ar is not 4-phenyl-3-cyano-2-aminopyrid-2-yl; and (7) when R is H and Z is CR.sup.2 and R.sup.1 and R.sup.2 are CH.sub.3 and Ar is 2-methyl-4-methoxyphenyl, then R.sup.3 is not 3-pentylamino. 2. A compound of claim 1 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl, each optionally substituted with 1 to 4 R.sup.4 substituents. 3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1. 4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 2. 5. A compound of Formula (2) of claim 1 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof. 6. A compound of claim 5 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl and each Ar is optionally substituted with 1 to 4 R.sup.4 substituents. 7. A compound of claim 5 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein R.sup.3 is NR.sup.6a R.sup.7a or OR.sup.7. 8. A compound of claim 5 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl, and each Ar is optionally substituted with 1 to 4 R.sup.4 substituents, and R.sup.3 is NR.sup.6a R.sup.7a or OR.sup.7. 9. A compound of Formula (1) of claim 1 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Z is CR.sup.2. 10. A compound of claim 9 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl and each Ar is optionally substituted with 1 to 4 R.sup.4 substituents. 11. A compound of claim 9 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein R.sup.3 is NR.sup.6a R.sup.7a or OR.sup.7. 12. A compound of claim 9 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl, and each Ar is optionally substituted with 1 to 4 R.sup.4 substituents, and R.sup.3 is NR.sup.6a R.sup.7a or OR.sup.7. 13. A compound of claim 12 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein R.sup.6a and R.sup.7a are independently H or C.sub.1 -C.sub.10 alkyl, and each such C.sub.1 -C.sub.10 alkyl is optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.13, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.13, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, R.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.13, NR.sup.16 R.sup.15, CONR.sup.16 R.sup.15, aryl, heteroaryl or heterocyclyl. 14. A compound of claim 9 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein --Ar is phenyl, pyridyl or 2,3-dihydrobenzofuranyl, and each Ar is optionally substituted with 1 to 4 R.sup.4 substituents, --R.sup.3 is NR.sup.6a R.sup.7a or OR.sup.7 and --R.sup.1 and R.sup.2 are independently selected from H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl. 15. A compound of claim 14 and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof wherein R.sup.6a and R.sup.7a are independently H or C.sub.1 -C.sub.10 alkyl, and each such C.sub.1 -C.sub.10 alkyl is optionally substituted with 1 to 3 substituents independently selected at each occurrence from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo, C.sub.1 -C.sub.4 haloalkyl, cyano, OR.sup.15, SH, S(O).sub.n R.sup.13, COR.sup.15, CO.sub.2 R.sup.15, OC(O)R.sup.13, NR.sup.8 COR.sup.15, N(COR.sup.15).sub.2, R.sup.8 CONR.sup.16 R.sup.15, NR.sup.8 CO.sub.2 R.sup.13, NR.sup.16 R.sup.15, CONR.sup.16 R.sup.15, aryl, heteroaryl or heterocyclyl. 16. A compound of Formula (51) ##STR49## and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof selected from the group consisting of: a compound of Formula (51) wherein R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 oMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(n-Bu)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(n-Pr)(CH.sub.2 OMe), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NH(Et), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH (n-Pr)(CH.sub.2 OMe), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH (n-Pr)(CH.sub.2 OMe), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --N(Bu)(Et), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (51) wherein R.sup.3 is --NEt.sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; and a compound of Formula (51) wherein R.sup.3 is --N(Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H. 17. A compound of Formula (70) ##STR50## and isomers thereof, stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, and pharmaceutically acceptable salt forms thereof selected from the group consisting of: a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(n-Bu)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(n-Pr)(CH.sub.2 OMe), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NH(Et), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH (n-Pr)(CH.sub.2 OMe), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH (n-Pr)(CH.sub.2 OMe), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Br, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is OMe and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Bu)(Et), R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et)CH.sub.2 OMe, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Cl, R.sup.3 is --NEt.sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; and a compound of Formula (70) wherein R is Cl, R.sup.3 is --N(Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(c-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Cl, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(n-Bu)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(n-Pr)(CH.sub.2 OMe), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(Et).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(CH.sub.2 CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NH(Et), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Me, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(n-Pr).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NHCH(CH.sub.2 OMe).sub.2, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is (S)--NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --NH(CH.sub.2 CH.sub.2 OMe)CH.sub.2 OMe, R.sup.4a is Me, R.sup.4b is H, R.sup.4c is Cl, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, R.sup.3 is --N(n-Pr)(CH.sub.2 CH.sub.2 CN), R.sup.4a is Me, R.sup.4b is H, R.sup.4c is OMe, R.sup.4d is H and R.sup.4e is H; a compound of Formula (70) wherein R is Me, |
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