CAS: 117591-20-5; Benzyl ((S)-4-Methyl-1-Oxo-1-(((S)-1-Oxohexan-2-yl)Amino)Pentan-2-yl)Carbamate

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CAS号2018-66-8 N-苄氧羰基-L-亮氨酸 | CAS号80696-29-3 (S)-(+)-2-氨基-1-己醇

📜Z-Leu-Nleu-Oh置于草酰氯,二甲基亚砜体系中,用 二氯甲烷 用作溶剂,以78%的收率获得((S)-4-甲基-1-氧代-1-(((S)-1-氧代己烷-2-基)氨基)戊-2-基)氨基甲酸苄酯
参考文献:Ketoheterocycle-Based Inhibitors Of Cathepsin K: A Novel Entry Into The Synthesis Of Peptidic Ketoheterocycles
标题:Ketoheterocycle-Based Inhibitors Of Cathepsin K: A Novel Entry Into The Synthesis Of Peptidic Ketoheterocycles
摘要:Ketoheterocyclic Inhibitors Of Cathepsin K Have Been Disclosed. Sar Of Potency Enhancing P-2-P-3 Groups Coupled With Ketoheterocyclic Warheads To Provide Cathepsin K Inhibitors Have Been Described. In Addition,A Novel Route To Access Alpha-Ketothiazoles Using A Key Thioamide Functionality Has Been Disclosed. The Mild Method Employed Allows For The Presence Of Diverse Functional Groups,Such As Amide And Carbamate Functionalities,Commonly Found In Protease Inhibitors That Have Peptidomimetic Scaffolds. This New Method Should Provide A Quick Entry Into Functionally Diverse Protease Inhibitors. (C) 2005 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2005.05.091

专利信息

专利号:US-6887887-B2
优先权日:2001-03-19
标 题:Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor
发明人：BORNMANN WILLIAM G; SIROTNAK FRANCIS; SCHER HOWARD; VIDAL EPHRAIM; BORELLA CHRISTOPHER; SCHEINBERG DAVID
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: n n nwhere R 1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R 1 further comprising a cyclic or bicyclic structure; R 2 is methyl, CH 2 CH 3 , (CH 2 ) 2 CH 3 , C(CH 3 ) 3 , phenyl, 3,4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH 2 -(N-Boc-4-piperidine), 4-tetrahydropyran, CH 2 -4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R 3 is R 2 or C 3-8 alkyl, R 4 is C 1-3 alkyl; and R 5 is NH 2 , OH, NHOH, NHOCH 3 , N(CH 3 )OH, N(CH 3 )OCH 3 , NHCH 2 CH 3 , NH(CH 2 CH 3 ), NHCH 2 (2,4-(OCH3) 2 Ph, NHCH 2 (4-NO 2 )Ph, NHN(CH 3 ) 2 , proline, or 2-hydroxymethyl pyrrolidine. Additionally, a method for the treatment of a neoplastic disease or for the inhibition of tumor cell growth each comprising the step of administering to an individual in need of such treatment a pharmacologically effective dose of the compounds of the present invention are provided.

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-6207878-B1
优先权日:1999-10-21
标题:Sarcospan-deficient mouse as a model for clinical disorders associated with sarcospan mutations
发明人：CAMPBELL KEVIN P; LEBAKKEN CONNIE; CROSBIE RACHELLE; WILLIAMSON ROGER
权利人:UNIV IOWA RES FOUND
摘要:Disclosed is a transgenic knockout mouse whose genome has a homozygous disruption in its endogenous sarcospan gene, wherein the disruption prevents the synthesis of functional sarcospan in cells of the mouse. The mouse is characterized as exhibiting from 1.4 to 6.8 fold larger epididymal fat pad deposits as compared to the epididymal fat pad deposits of a wild type mouse. Methods for production of the mouse are presented. Also disclosed are cells derived from the transgenic knockout mouse. The mouse can be used in a method for identifying therapeutic agents for the treatment of an individual diagnosed with a metabolic disorder associated with a reduction or loss of expression of wild-type sarcospan. An example of such a disorder is weight gain in the individual associated with a reduction or loss of expression of wild-type sarcospan. These specific methods are also provided.

专利号:US-2005272667-A1
优先权日:2001-03-19
标题:Analogs and derivatives of (S,S,R)-(-)-actinonin and uses therefor
发明人：SCHEINBERG DAVID; BORNMANN WILLIAM G; SIROTNAK FRANCIS; SCHER HOWARD; VIDAL EPHRAIM; BORELLA CHRISTOPHER
权利人:SCHEINBERG DAVID; BORNMANN WILLIAM G; SIROTNAK FRANCIS; SCHER HOWARD; VIDAL EPHRAIM; BORELLA CHRISTOPHER
摘要:The present invention provides analog and derivative compounds of (S,S,R)-(−)-actinonin and methods of asymmetric synthesis thereof having a structure: n n nwhere R 1 is hydrogen, C(O)R 6 or R 1 in combination with N is 2-oxomorpholine, R 2 is hydrogen, methyl, CH 2 CH(CH 3 ) 2 , (CH 2 ) 2 CH 3 , CH(CH 3 ) 2 , (CH 2 ) 3 CH 3 , (CH 2 ) 4 NH 2 , (CH 2 ) 3 CO 2 H, phenyl, 3,4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH 2 -(N-Boc-4-piperidine), 4-tetrahydropyran, CH 2 -4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl, R 3 is R 2 or C 3-8 alkyl, R 4 is C 1-3 alkyl, R 5 is NH 2 , OH, NHOH, NHOCH 3 , N(CH 3 )OH, N(CH 3 )OCH 3 , NHCH 2 CH 3 , NH(CH 2 CH 3 ), NHCH 2 (2,4-(OCH 3 ) 2 Ph, NHCH 2 (4-NO 2 )Ph, NHN(CH 3 ) 2 , proline, or 2-hydroxymethyl pyrrolidine and R 6 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine where R 6 further comprising a cyclic or bicyclic structure. Also provided are methods for treating a neoplastic disease or for inhibiting tumor cell growth using the compounds present invention or using the compound (S,S,R)-(−)-actinonin.

专利号:US-2002198156-A1
优先权日:2001-03-19
标 题 :Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor

专利号:US-2004019083-A1
优先权日:2001-03-19
标 题:Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor