发明名称 PEPTIDE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF INHIBITION OF TACHYKININ EFFECT
摘要 FIELD: chemistry of peptides. SUBSTANCE: products: derivatives of peptides of the formula (I): <EMI ID=0.110 HE=27 WI=78 TI=CHI> where R<SB>1</SB> is hydrogen, (lower)-alkyl; R<SB>2</SB> is (lower)-alkyl, halogen; R<SB>3</SB> is hydrogen, (lower)-alkyl, halogen; R<SB>4</SB> is (lower)- -alkyl; R<SB>5</SB> is aryl, (lower)-alkyl; R<SB>6</SB> is NH<SB>2</SB> or optionally substituted hydroxyl-group, or their pharmaceutically acceptable salts. Compounds of the formula (I) are synthesized by interaction of compound (II): <EMI ID=0.111 HE=18 WI=66 TI=CHI> or its amino-group reactive derivative and compound (III): <EMI ID=0.112 HE=12 WI=33 TI=CHI>, or its amino-group reactive derivative. Invention relates to also pharmaceutical composition containing an effective amount of peptide derivative of the formula (I) as an active component or its pharmaceutically acceptable salt, method of inhibition of tachykinin effect by effect on tachykinin receptors - derivative of peptide of the formula (I) at effective amount. The synthesized compounds can be used for treatment of patients with respiratory diseases (asthma, bronchitis, rhinitis and others), ophthalmic diseases, skin diseases (contact dermatitis, diffuse neurodermitis, nettle rash), inflammatory diseases (rheumatic arthritis, osteoarthritis), pains (migraine, headache, tooth, cancer, back pains and others) in humans and animals. Synthesized compounds show antagonism with respect to tachykinin. EFFECT: improved method of synthesis, enhanced effectiveness of compounds synthesized. 6 cl, 4 dwg, 1 tbl, 28 ex
申请公布号 RU2119922(C1) 申请公布日期 1998.10.10
申请号 RU19940045881 申请日期 1993.04.09
申请人 FUDZISAVA FARMAS'JUTIKAL KO., LTD. 发明人 MASAAKI MATSUO;DAJDZHIRO KHAGIVARA;KHIROSI MIJAKE
分类号 A61K38/00;A61K38/06;A61P11/00;A61P25/04;A61P27/02;A61P29/00;A61P43/00;C07K1/02;C07K5/02;C07K5/078;C07K5/097;(IPC1-7):C07K5/097 主分类号 A61K38/00
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