Title:
混合ジスルファニルの形態のジスルファニル基を含有するアミノ酸誘導体とアミノペプチダーゼ阻害剤
Document Type and Number:
Japanese Patent JP5177889
Kind Code:
B2
Abstract:
Amino acid derivatives (I) are new. Amino acid derivatives of formula H 2NCH(R 1)CH 2SSCH 2CH(R 2)C(O)NHCH(R 3)C(O)OR 4 (I) and their mineral or organic acid addition salts are new. R 1 = 1-6C optionally unsaturated hydrocarbyl (optionally substituted by OR, SR, S(O)R, phenyl or benzyl), phenyl or benzyl (both optionally substituted by OR, SR or S(O)R or 1-5 halo, preferably F) or T; R = H, 1-4C hydrocarbyl, phenyl or benzyl; T = methylene substituted by aromatic or saturated 5-6 membered heterocycle containing heteroatoms such as N or S, preferably as N-oxide or S-oxide; R 2 = phenyl or benzyl (both optionally substituted by OR, SR, S(O)R, amino (optionally mono- or disubsituted by 1-6C aliphatic group), 5-6 membered aromatic ring or 1-5 halogen (preferably F)), 5-6 membered heteroaromatic ring contaning one O, S or N or T; R 3 = H, OH, OR, 1-6C saturated alkyl (optionally substituted by OR or SR), phenyl or benzyl (both optionally substituted by 1-5 halogen (particularly F), OR or SR); and OR 4 = hydrophilic ester where the hydrophilicity of the ester provides an octanol-water division coefficient (log K ow) 1.7 to (I). ACTIVITY : Antidepressant; Antiinflammatory; Analgesic. MECHANISM OF ACTION : Neprilysine inhibitor; N-Amino peptidase inhibitor.
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Inventors:
Roku, Bernard
Fournier-Zarski, Marie-Claude
Fournier-Zarski, Marie-Claude
Application Number:
JP2008537082A
Publication Date:
April 10, 2013
Filing Date:
October 24, 2006
Export Citation:
Assignee:
PHARMALEADS
International Classes:
C07C323/60; A61K31/221; A61K31/351; A61K31/352; A61K31/381; A61P25/04; A61P25/24; A61P29/00; C07D309/10; C07D333/20
Domestic Patent References:
| JP5502016A |
Other References:
Noble, Florence; Smadja, Claire; Valverde, Olga; Maldonado, Rafael; Coric, Pascale; Turcaud, Serge; Fournie-Zaluski, Marie-Claude; Roques, Bernard P.,Pain-suppressive effects on various nociceptive stimuli (thermal, chemical, electrical and inflammatory) of the first orally active enkephalin-metabolizing enzyme inhibitor RB 120,Pain ,1997年,73(3),383-391
Attorney, Agent or Firm:
Hatsushi Shimizu
Masao Haruna
Hirotaka Yamaguchi
Toshi Gobe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Shinichi Watanabe
Masato Ozeki
Yoshihiro Igarashi
Kazuya Kawamoto
Masao Haruna
Hirotaka Yamaguchi
Toshi Gobe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Shinichi Watanabe
Masato Ozeki
Yoshihiro Igarashi
Kazuya Kawamoto