DETAILED DESCRIPTION OF THE INVENTION The present invention pertains to novel immunoconjugates, intermediates thereto, pharmaceutical compositions and methods of use.
Throughout the present document, all temperatures are in degrees celsius.
All expressions of percentage, concentration and the like are in weight units, unless otherwise stated.
All references to concentrations and dosages of drug conjugates are in terms of the amount or concentration of the drug contained in the conjugate.
In the above formulae, the general and specific chemical terms used have their normal meanings in organic and, especially, amino acid chemistry.
For example, the term "C.
sub.
1 -C.
sub.
4 alkyl" refers to straight or branched aliphatic chains of 1-4 carbon atoms including methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl.
The carboxy protecting groups of R.
sup.
4 and R.
sup.
7, when R.
sup.
7 is neither H nor an activating group, denote groups which generally are not found in final therapeutic conjugates, but which are intentionally introduced during a portion of the synthetic process to protect a group which otherwise might react in the course of chemical manipulations, and is then removed at a later stage of the synthesis.
Since compounds bearing such protecting groups are of importance primarily as chemical intermediates, their precise structure is not critical.
Numerous reactions are described in a number of standard works including for example, Protective Groups in Organic Chemistry, Plenum Press, (London and New York, 1973); Green, T.
W.
, et al.
(eds), Protective Groups in Organic Synthesis, Wiley (New York, 1981); and Schroeder, et al.
(eds.
), The Peptides, Vol.
I, Academic Press (London and New York, 1965).
Preferred R.
sup.
4 and R.
sup.
7 carboxy protecting groups include C.
sub.
1 -C.
sub.
4 alkyl, phenyl which maybe substituted, and benzyl which may be substituted.
The term "phenyl which may be substituted" denotes an unsubstituted or substituted phenyl residue, optionally having one or two substituents selected from halo (bromo, chloro, fluoro, and iodo), nitro, C
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