Claims
- 1. A compound having the formula ##STR319## wherein A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR320## represents a radical of the formula ##STR321## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R.sup.6 and R.sup.7 are hydrogen or C.sub.1 -C.sub.4 alkyl; ##STR322## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl or phenyl(C.sub.1 -C.sub.4)alkyl; ##STR323## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl or carboxy(C.sub.1 -C.sub.4 alkyl and R.sup.6 is C.sub.1 -C.sub.4 alkyl or carboxy(C.sub.1 -C.sub.4)alkyl) ##STR324## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; ##STR325## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; ##STR326## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; or ##STR327## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof.
- 2. A compound having the formula ##STR328## wherein A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR329## represents a radical of the formula ##STR330## or a pharmaceutically acceptable salt thereof.
- 3. A compound having the formula ##STR331## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion and wherein ##STR332## wherein the .sup.1 HNMR (D.sub.2 O) spectrum shows characteristic peaks at .delta.: 1.23 (3H, d, J=6.4 Hz), 3.12 (2H, q, J=1.4, 8.9 Hz); 3.39 (1H, q, J=2.7, 6.0 Hz), 4.07-4.68 (10H, m), 8.19 (1H, s); ##STR333## wherein the .sup.1 HNMR (D.sub.2 O) spectrum shows characteristic peaks at .delta.: 1.23 (3H, d, J=6.4 Hz), 3.15 (2H, q, J=3.7, 9.0 Hz), 3.37 (1H, q, J=2.6, 6.0 Hz), 3.95-4.65 (10H, m), 8.62 (1H, s); ##STR334## or a pharmaceutically acceptable salt thereof.
- 4. A compound of the formula ##STR335## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 5. The compound according to claim 4 wherein R.sup.2 is p-nitrobenzyl.
- 6. The compound according to claim 4 wherein R.sup.2 is an anionic charge.
- 7. A compound of the formula ##STR336## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or pharmaceutically acceptable salt thereof.
- 8. The compound according to claim 7 wherein R.sup.2 is p-nitrobenzyl.
- 9. The compound according to claim 7 wherein R.sup.2 is an anionic charge.
- 10. A compound of the formula ##STR337## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 11. The compound according to claim 10 wherein R.sup.2 is p-nitrobenzyl.
- 12. The compound according to claim 10 wherein R.sup.2 is an anionic charge.
- 13. A compound of the formula ##STR338## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 14. The compound according to claim 13 wherein R.sup.2 is p-nitrobenzyl.
- 15. The compound according to claim 13 wherein R.sup.2 is an anionic charge.
- 16. A compound of the formula ##STR339## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 17. The compound according to claim 16 wherein R.sup.2 is p-nitrobenzyl.
- 18. The compound according to claim 16 wherein R.sup.2 is an anionic charge.
- 19. A compound of the formula ##STR340## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 20. The compound according to claim 19 wherein R.sup.2 is p-nitrobenzyl.
- 21. The compound of claim 19 wherein R.sup.2 is an anionic charge.
- 22. A compound of the formula ##STR341## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 23. The compound according to claim 22 wherein R.sup.2 is p-nitrobenzyl.
- 24. The compound according to claim 22 wherein R.sup.2 is an anionic charge.
- 25. A compound of the formula ##STR342## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 26. The compound according to claim 25 wherein R.sup.2 is p-nitrobenzyl.
- 27. The compound according to claim 25 wherein R.sup.2 is an anionic charge.
- 28. A compound of the formula ##STR343## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 29. The compound according to claim 28 wherein R.sup.2 is p-nitrobenzyl.
- 30. The compound according to claim 28 wherein R.sup.2 is an anionic charge.
- 31. A compound of the formula ##STR344## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 32. The compound according to claim 31 wherein R.sup.2 is p-nitrobenzyl.
- 33. The compound according to claim 31 wherein R.sup.2 is an anionic charge.
- 34. A compound of the formula ##STR345## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 35. The compound according to claim 34 wherein R.sup.2 is p-nitrobenzyl.
- 36. The compound according to claim 34 wherein R.sup.2 is an anionic charge.
- 37. A compound of the formula ##STR346## wherein the .sup.1 HNMR (D.sub.2 O) spectrum shows characteristic peaks at .delta.: 1.23 (3H, d, J=6.4 Hz), 3.12 (2H, q, J=1.4, 8.9 Hz), 3.39 (1H, q, J=2.7, 6.0 Hz), 4.07-4.68 (10H, m), 8.19 (1H, s), or a pharmaceutically acceptable salt or ester thereof.
- 38. The compound according to claim 37 wherein the carboxyl group is protected as a p-nitrobenzyl ester.
- 39. A compound of the formula ##STR347## wherein the .sup.1 HNMR (D.sub.2 O) spectrum shows characteristic peaks at .delta.: 1.23 (3H, d, J=6.4 Hz), 3.15 (2H, q, J=3.7, 9.0 Hz), 3.37 (1H, q, J=2.6, 6.0 Hz), 3.95-4.65 (10H, m), 8.62 (1H, s), or a pharmaceutically acceptable salt or ester thereof.
- 40. The compound according to claim 39 wherein the carboxyl group is protected as a p-nitrobenzyl ester.
- 41. A compound having the formula ##STR348## wherein A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR349## represents a radical of the formula ##STR350## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R.sup.6 and R.sup.7 are hydrogen or C.sub.1 -C.sub.4 alkyl; ##STR351## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl or phenyl(C.sub.1 -C.sub.4)alkyl; ##STR352## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl or carboxy(C.sub.1 -C.sub.4)alkyl and R.sup.6 is C.sub.1 -C.sub.4 alkyl or carboxy(C.sub.1 -C.sub.4)alkyl ##STR353## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; ##STR354## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; ##STR355## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; or ##STR356## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl and R is C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof.
- 42. A compound having the formula ##STR357## wherein A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR358## represents a radical of the formula ##STR359##
- 43. A compound of the formula ##STR360## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 44. A compound of the formula ##STR361## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 45. A compound of the formula ##STR362## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 46. A compound of the formula ##STR363## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 47. A compound of the formula ##STR364## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 48. A compound of the formula ##STR365## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 49. A compound of the formula ##STR366## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 50. A compound of the formula ##STR367## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 51. A compound of the formula ##STR368## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; or a pharmaceutically acceptable salt thereof.
- 52. A compound of the formula ##STR369## wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl;
- A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR370## represents a radical selected from the group consisting of ##STR371## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optionally substituted on a carbon atom by one or more C.sub.1 -C.sub.4 alkyl substituents; ##STR372## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optionally substituted on a carbon atom by C.sub.1 -C.sub.4 alkyl; and ##STR373## wherein R is C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof.
- 53. A compound according to claim 52 wherein A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --.
- 54. A compound of the formula ##STR374## wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl;
- A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR375## represents a radical of the formula ##STR376## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optionally substituted on a carbon atom by one or more C.sub.1 -C.sub.4 alkyl substituents; or a pharmaceutically acceptable salt thereof.
- 55. A compound of claim 54 wherein A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --.
- 56. A compound of the formula ##STR377## wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl;
- A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR378## represents a radical of the formula ##STR379## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optionally substituted on a carbon atom by a C.sub.1 -C.sub.4 alkyl substituent;
- or a pharmaceutically acceptable salt thereof.
- 57. A compound according to claim 56 wherein A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --.
- 58. A compound of the formula ##STR380## wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl;
- A is C.sub.1 -C.sub.6 straight or branched chain alkylene;
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR381## represents a radical of the formula ##STR382## wherein R is C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof.
- 59. A compound according to claim 58 wherein A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --.
- 60. A compound of the formula ##STR383## wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl;
- R.sup.16 is C.sub.1 -C.sub.6 alkyl;
- A is C.sub.1 -C.sub.6 straight or branched chain alkylene,
- R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion; and ##STR384## represents a radical selected from the group consisting of ##STR385## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optionally substituted on a carbon atom by one or more C.sub.1 -C.sub.4 alkyl substituents; ##STR386## wherein X is O, S or NR in which R is C.sub.1 -C.sub.4 alkyl; said radical being optional substituted on a carbon atom by C.sub.1 -C.sub.4 alkyl; and ##STR387## wherein R is C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof.
- 61. A compound according to claim 60 wherein A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --.
- 62. A compound of the formula ##STR388## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion;
- or a pharmaceutically acceptable salt thereof.
- 63. A compound of the formula ##STR389## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion;
- or a pharmaceutically acceptable salt thereof.
- 64. A compound of the formula ##STR390## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion;
- or a phamaceutically acceptable salt thereof.
- 65. A compound of the formula ##STR391## wherein R.sup.2 is hydrogen, an anionic charge or a conventional readily removable carboxyl protecting group, providing that when R.sup.2 is hydrogen or a protecting group, there is also present a counter ion;
- or a pharmaceutically acceptable salt thereof.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a division of may co-pending application Ser. No. 705,780, filed Feb. 22, 1985, now U.S. Pat. No. 4,644,041, which in turn was a continuation-in-part of application Ser. No. 530,011, filed Sept. 9, 1983, now abandoned, which in turn was a continuation-in-part of application Ser. No. 425,755, filed Sept. 28, 1982, now abandoned.
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Divisions (1)
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Number |
Date |
Country |
Parent |
705780 |
Feb 1985 |
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Continuation in Parts (2)
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Number |
Date |
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Parent |
530011 |
Sep 1983 |
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Parent |
425755 |
Sep 1982 |
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