Claims
- 1. A compound of the formula: ##STR14## wherein: R.sub.1a and R.sub.1b are the same or different and are C.sub.1 to C.sub.6 alkyl or phenyl;
- R.sub.2 is hydrogen, halo, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, perfluoro C.sub.2 to C.sub.4 alkyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl, phenyl, substituted phenyl, a heterocyclic ring, nitro or cyano;
- a group of the formula
- --CX.sub.3
- wherein X is fluoro, chloro, bromo or iodo;
- a group of the formula ##STR15## wherein Z is 0, 1 or 2 and R.sub.7 is C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, C.sub.2 to C.sub.7 alkenyl, C.sub.2 to C.sub.7 alkynyl, phenyl, substituted phenyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl or a heterocyclic ring;
- a group of the formula
- COR.sub.8
- wherein R.sub.8 is hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, perfluoro C.sub.2 to C.sub.4 alkyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl, phenyl, substituted phenyl, amino, (monosubstituted)amino, or (disubstituted)amino;
- a group of the formula ##STR16## wherein R.sub.8 is as defined above and R.sub.8 ' is hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.2 to C.sub.7 alkenyl, C.sub.2 to C.sub.7 alkynyl, phenyl, substituted phenyl, C.sub.7 to C.sub.12 phenylalkyl, or C.sub.7 to C.sub.12 substituted phenylalkyl;
- a group of the formula
- --COOR.sub.9
- wherein R.sub.9 is C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl, phenyl, substituted phenyl, a carboxy-protecting group, or a non-toxic, metabolically-labile, ester-forming group;
- a group of the formula
- --PO.sub.3 (R.sub.10).sub.2
- wherein R.sub.10 is C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl, phenyl, or substituted phenyl; or
- a group of the formula
- --CH.sub.2 --S--Heterocyclic ring;
- R.sub.3 and R.sub.4 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 substituted alkyl, C.sub.7 to C.sub.12 phenylalkyl, C.sub.7 to C.sub.12 substituted phenylalkyl, phenyl, substituted phenyl or a group of the formula
- --COOR.sub.12
- wherein R.sub.12 has the same definition as R.sub.9 ;
- R.sub.5 and R.sub.6 are:
- (1) each hydrogen;
- (2) taken together and form a phthalimido group; or
- (3) different and are either hydrogen or an amino-protecting group; and
- R.sub.11 is a carboxy-protecting group or a non-toxic, metabolically-labile, ester-forming group;
- or a pharmaceutically-acceptable salt thereof.
- 2. A compound of claim 1, wherein R.sub.3 and R.sub.4 are hydrogen.
- 3. A compound of claim 2, wherein either R.sub.5 or R.sub.6 is hydrogen and the other is an amino-protecting group; and wherein R.sub.11 is a carboxy-protecting group.
- 4. A compound of claim 3, wherein R.sub.2 is a group of the formula
- --COOR.sub.9.
- 5. A compound of claim 4, wherein R.sub.9 is methyl, ethyl, n-propyl or benzyl.
- 6. A compound of claim 5, wherein R.sub.1a and R.sub.1b are the same and are methyl and ethyl; wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group, and wherein R.sub.11 is an allyl group.
- 7. A compound of claim 3, wherein R.sub.2 is a group of the formula
- --COR.sub.8.
- 8. A compound of claim 7, wherein R.sub.8 is methyl or monofluoromethyl.
- 9. A compound of claim 8, wherein R.sub.1a and R.sub.1b are the same and are methyl; wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group; and wherein R.sub.11 is an allyl group.
- 10. A compound of claim 3, wherein R.sub.2 is cyano.
- 11. A compound of claim 10, wherein R.sub.1a and R.sub.1b are each hydrogen; wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group; and wherein R.sub.11 is an allyl group.
- 12. A compound of claim 3, wherein R.sub.2 is a group of the formula ##STR17##
- 13. A compound of claim 12, wherein R.sub.7 is methyl and Z is 2.
- 14. A compound of claim 13, wherein R.sub.1a and R.sub.1b are each methyl; wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group; and wherein R.sub.11 is an allyl group.
- 15. A compound of claim 1 of the formula ##STR18##
- 16. A compound of claim 15, wherein R.sub.3 and R.sub.4 are each hydrogen; either R.sub.5 or R.sub.6 is hydrogen and the other is an amino-protecting group, and wherein R.sub.11 is a carboxy-protecting group.
- 17. A compound of claim 16, wherein R.sub.2 is cyano.
- 18. A compound of claim 17, wherein R.sub.1a and R.sub.1b are each ethyl; wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group; and wherein R.sub.11 is an allyl group.
- 19. A compound of claim 15 wherein R.sub.2 is a group of the formula ##STR19## wherein z is 2 and R.sub.7 is C.sub.1 -C.sub.6 alkyl.
- 20. A compound of claim 19 wherein R.sub.7 is methyl or ethyl.
- 21. A compound of claim 20, wherein either R.sub.5 or R.sub.6 is hydrogen and the other is a t-butoxycarbonyl group, R.sub.11 is an allyl group, and wherein R.sub.1a or R.sub.1b are methyl or ethyl.
- 22. A compound of claim 21, wherein R.sub.7 is methyl and R.sub.1a and R.sub.1b are methyl.
Priority Claims (1)
Number |
Date |
Country |
Kind |
86303174.6 |
Apr 1986 |
EPX |
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CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a continuation-in-part of application Ser. No. 07/042,196, filed Apr. 23, 1987, now abandoned which was a continuation of application Ser. No. 06/862,916, filed May 14, 1986, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4465679 |
Huang et al. |
Aug 1984 |
|
4716232 |
Ternansky |
Dec 1987 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
23636 |
Feb 1981 |
EPX |
Non-Patent Literature Citations (2)
Entry |
Dorn et al, Z. Chem., vol. 8 (1968) pp. 218-219. |
Dorn et al, Z. Chem., vol. 8 (1968) pp. 270-271. |
Continuations (1)
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Number |
Date |
Country |
Parent |
862916 |
May 1986 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
42196 |
Apr 1987 |
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