Asymmetric synthesis of ?-(heteroaryl)alkylamines and ?-amino acids via nucleophilic 1,2-addition of lithiated heterocycles to aldehyde SAMP-hydrazones
Substituted peptide compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Linear constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues and at least one amino acid surrogate of formula I:
where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group covalently bound to a reactive group of at least one of the amino acid residues or surrogates, pharmaceutical compositions including such linear constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Substituted proline compounds, composition and method of use
申请人:E. R. Squibb & Sons, Inc.
公开号:US04621092A1
公开(公告)日:1986-11-04
Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Ring-constrained amino acid surrogates of formula I:
where R
1
, R
2
, R
3
, R
4
, R
5
, R
6a
, R
6b
, R
7
, and y are as defined in the specification, methods for synthesizing ring-constrained amino acid surrogates of formula I, methods of use of ring-constrained amino acid surrogates of formula I, including use in linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I and linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I.