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Branched amides of L-aspartyl-D-amino acid dipeptides
   
Document Number
US Patent 4855454
Issued Date
August 8, 1989
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Abstract
Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.9 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms and the sum of the carbon atoms in R.sup.7, R.sup.8 and R.sup.9 is not greater than six, m and q are the same or different and each have the values previously defined for m; ##STR4## where each of R.sup.12 and R.sup.13 are methyl or ethyl, or R.sup.12 is hydrogen and R.sup.13 is alkyl having from one to four carbon atoms, Z is O or NH and t is 1 or 2, ##STR5## where w is 1-4, R.sup.14 and R.sup.16 are each alkyl having from one to four carbon atoms, R.sup.15 is H, OH, methyl or ethyl and the sum of the carbon atoms in R.sup.14, R.sup.15 and R.sup.16 is not greater than six and when both of R.sup.14 and R.sup.15 are alkyl they are methyl or ethyl, and ##STR6## where R.sup.17 and R.sup.19 are alkyl having from one to four carbon atoms, R.sup.18 and R.sup.20 are H or alkyl having one to two carbon atoms, A is OH and B is H, OH or CH.sub.3 and taken together A and B are ##STR7## where the sum of the carbon atoms in R.sup.17, R.sup.18, R.sup.19 and R.sup.20 is not greater than six and when both of R.sup.17 and R.sup.18 or R.sup.19 and R.sup.20 are alkyl they are methyl or ethyl; said amides are potent sweetners having advantages over the prior art, edible compositions containing them, methods for their use in edible compositions and novel amine and amide intermediates useful in their production.
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Branched amides of L-aspartyl-D-amino acid dipeptides - US Patent 4855454 Drawing
Drawing from US Patent 4855454
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Number of Claims:
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Owner
Pfizer Inc. (New York, NY)
Published
August 8, 1989
Application Number
07/218,245
Filed
July 13, 1988
US Classification
549/68   549/88
Int'l Classification
A23L   1/236   (20060101)   C07C   323/25   (20060101)   C07C   323/00   (20060101)   C07D   307/00   (20060101)   C07C   45/00   (20060101)   C07C   45/64   (20060101)   C07C   45/61   (20060101)   C07C   45/29   (20060101)   C07D   307/32   (20060101)   C07C   45/68   (20060101)   C07C   45/63   (20060101)   C07D   307/22   (20060101)   C07C   45/75   (20060101)   C07K   5/00   (20060101)   C07D   335/02   (20060101)   C07D   333/32   (20060101)   C07D   331/00   (20060101)   C07D   331/04   (20060101)   C07D   335/00   (20060101)   C07D   333/00   (20060101)   C07D   333/36   (20060101)   C07K   5/072   (20060101)  
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Parent Case
This is a continuation of application Ser. No. 496,428 filed May 20, 1983, abandoned, which in turn is a division of application Ser. No. 201,745 filed Nov. 5, 1980, now U.S. Pat. No. 4,411,925 issued Oct. 23, 1983, which in turn is a continuation-in-part of application Ser. No. 113,800 filed Jan. 21, 1980, now abandoned.
USPTO Field of Search
564/455   564/457   564/463   549/68   549/88  
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