Peptide cpds. contg. tyrosine, glycine, phenylalanine and d-amino acid - local anaesthetics, smooth muscle relaxants, adrenergic neutron blockers, beta-stimulants etc.
Номер патента: FR2359817A1
Опубликовано: 24-02-1978
Автор(ы):
Принадлежит: Reckitt and Colman Products Ltd
Опубликовано: 24-02-1978
Автор(ы):
Принадлежит: Reckitt and Colman Products Ltd
Реферат: Peptides of formula (I) and their acid addn. salts are new: R1R2Tyre-B-GHy-Phe-W (I). In the formula R1 = H, 1-4C alkyl, 1-10, e.g. 3-5C, alkenyl, propargyl, 4-8C cycloalkylmethyl or phenyl (1-3C) alkyl. R2 = H or 1-4C alkyl, W = NR8R9 or AR3. R8 = 1-10 C alkyl, 3-6C cycloalkyl, 1-5C alkyl substd. by -CH(CH2OH)-, 3-6C cycloalkyl or phenyl, or is phenyl, CpH2pXCqH2q+1 (p = 2-6, q = 1-5, X=O or S), CH(CH2OH)(CH2)2SCH3 or H. R9 = H, 1-10C alkyl, phenyl or phenyl (1-6C)alkyl, or NR8R9 is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino opt. substd. by 1-3C alkyl or phenyl. A = Met, Lew, Ile, Nle or Val residue. R3 = OR4, NR4R5, Pro-OR4, Pro-NR4Rk (R4 and R5 = H or 1-3C alkyl). B is (a) when W = nr8r9, d-Ser, D-Thr (or its 1-4C alkyl ester), D-Pro, D-Try, D-Phe, D-Met a gp. NHCR6R7CO (R6 = 1-5C alkyl and R7 = H or CH3) or a gp. n = 2-5. or (b) when W = AR3, B is D-Met, D-Set, D-Thr or residue of D-alpha-aminobutyric acid, Opt. Phe is N-substd. by 1-10C alkyl. All amino acids have L configuration unless stated. (I) have potential value as local anaesthetic, smooth muscle relaxants, adrenergic neuron blockers, stimulants for presynaptic alpha-receptors, beta-stimulants, narcotic agonists, and antidiarrhoea agents. A specifically claimed cpd. is L-Tyr-D-Ala-Gly-L-Phe-3-methylbutylamide.
D-amino acid peptides
Номер патента: CA2529027C. Автор: David M. Goldenberg,William J. Mcbride. Владелец: Immunomedics Inc. Дата публикации: 2013-09-10.