CAS: 2018-66-8; N-Cbz-L-Leucine

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N-苄氧羰基-L-亮氨酸 二环己基铵盐置于盐酸,水,Magnesium Sulfate体系中,用 乙酸乙酯 用作溶剂,化学反应生成N-苄氧羰基-L-亮氨酸
参考文献:Metastin Derivative And Use Thereof
标题:Metastin Derivative And Use Thereof
摘要:这项发明提供了一种稳定的metastin衍生物,具有优异的生物活性(抑制癌症转移活性,抑制癌细胞增殖活性,促进促性腺激素分泌活性,促进性激素分泌活性等).通过将metastin的组成氨基酸替换为本发明的特定氨基酸,可以更进一步提高metastin衍生物的血液稳定性和溶解性,减少metastin衍生物的凝胶倾向,改善其药代动力学,使其表现出优异的抑制癌症转移和抑制癌细胞增殖活性.该metastin衍生物还可以表现出抑制促性腺激素分泌活性,抑制性激素分泌活性等.

专利信息

专利号:WO-9213549-A1
优先权日:1991-02-07
标题:Inhibition of cell proliferation by hydrophobic peptides
发明人：HATHAWAY DAVID R; MARCH KEITH L
权利人:RES CORP TECHNOLOGIES INC
摘要:The present invention is directed a method of using certain hydrophobic peptides for the inhibition of cell proliferation, wherein the peptides have the general formula: R-Xaa1-(Xaa)m-Xaac. The subject peptides have 2-7 amino acids such as alanine (Ala), arginine (Arg), cysteine (Cys), isoleucine (Ile), leucine (Leu), lysine (Lys), methionine (Met), norleucine (nLeu), phenylalanine (Phe), proline (Pro), threonine (Thr), tyrosine (Tyr), tryptophan (Trp), or valine (Val). In accordance with the present invention, these peptides are potent inhibitors of cell proliferation as well as inhibitors of the synthesis of two cellular proto-oncogenes. One aspect of the present invention provides for the prevention and treatment of cancer by administration of the subject peptides. A further aspect of the present invention provides for inhibiting cell proliferation using the subject peptides in the treatment and prevention of prostatic hypertrophy, arterial occlusion (restenosis), arteriosclerosis, and smooth muscle cell diseases.

专利号:US-5985844-A
优先权日:1992-03-26
标题:Homoerythromycin A derivatives modified at the 4'-and 8A-positions
发明人：HECK JAMES V; LEANZA WILLIAM J; RATCLIFFE RONALD W; SALZMANN THOMAS N; SHANKARAN KOTHANDARAMAN; SZYMONIFKA MICHAEL J; WILKENING ROBERT R
权利人:MERCK & CO INC
摘要:Compounds of the formula: where R is hydrogen, hydroxyl, alkyl or acyl, R' and R'' together are oxo, hydroxyimino or alkoxyimino, and R' and R'' independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.

专利号:EP-0508699-B1
优先权日:1991-04-04
标 题 :9-Deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4'- and 8a-positions
发明人：HECK JAMES V; LEANZA WILLIAM J; RATCLIFFE RONALD W; SALZMANN THOMAS N; WILKENING ROBERT R; SZYMONIFKA MICHAEL J; SHANKARAN KOTHANDARAMAN
权利人:MERCK & CO INC
摘要:Compounds of the formula: where R is hydrogen, hydroxyl, alkyl or acyl, R min and R sec together are oxo, hydroxyimino or alkoxyimino, and R min and R sec independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.