专利号:US-9458188-B2 优先权日:2010-12-22 标 题 :Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT; BTG INT LTD 摘要:A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
专利号:US-11612556-B2 优先权日:2014-12-16 标 题:Peptidic compounds, compositions comprising them and uses of said compounds, in particular cosmetic uses 发明人:PESCHARD OLIVIER; DOUCET ANNE; LEROUX RICHARD; MONDON PHILIPPE 权利人:SEDERMA SA 摘要:The peptidic compound comprises at least an aminoacid which is lysine, ornithine, diaminopropionic acid or diaminobutyric acid or a derivative of these aminoacids, on which a carboxylic acid is grafted via a peptidic bound on the nitrogen of the lateral chain, said carboxylic acid comprising a (poly)cycle or (poly)heterocycle. Preferably, the grafted carboxylic acid is an aminoacid or a derivative, in particular selected from, a proline, a hydroxyproline or pyroglutamic acid.The peptidic compound can stimulate the synthesis of the main molecules constituting the extracellular matrix of the skin, especially collagen 1 and 4 and elastin. It can be used for topical cosmetic treatment such as a global anti-aging treatment, or for specific activities, including anti-wrinkles, moisturizing, to improve the mechanical properties of the skin, firmness/tone/elasticity/flexibility, to increase density and volume of the skin, improve skin radiance, for a restructuring effect and/or to fight stretch marks.
专利号:WO-2013132505-A1 优先权日:2012-03-09 标题 :Improved process for preparation of octreotide by solution phase peptide synthesis 发明人:KOTA SATYANARAYANA; TALLAPANENI VENKATESWARLU; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD; KOTA SATYANARAYANA; TALLAPANENI VENKATESWARLU; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 摘要:The present invention relates to a novel processes for commercial production of pharmaceutical grade octreotide using classical solution phase peptide synthesis in high yield and purity and using inexpensive amino acid derivatives. Thus the protected octapeptide alcohol Boc -D- Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - Cys (Trt) - Thr - OL is prepared by condensation of hexapeptide acid Boc -D - Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - OH with dipeptide alcohol H- Cys (Trt) - Thr - OL. The hexapeptide Boc -D- Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - OMe is prepared by condensing Boc - D - Phe - Cys (Trt) - OH with tetrapeptide H-Phe -D - Trp - Lys (Boc) - Thr - OMe followed by hydrolysis. The linear octapeptide alcohol is treated with cocktail mixture TFA /water/ TIS (9.0:0.5:0.25), in one step removes the Trt and Boc groups, followed by oxidation with hydrogen peroxide to affords octreotide.
专利号:US-7585846-B2 优先权日:2003-11-25 标 题 :Compounds for delivering amino acids or peptides with antioxidant activity into mitochondria and use thereof 发明人:SHEU SHEY-SHING; ANDERS MARION W; XU LIN; SHARMA VIRENDRA K 权利人:UNIV ROCHESTER 摘要:Disclosed are hydrophilic choline/N-heterocycle ester compounds containing single amino acids, peptides, or derivatives thereof which have the potential to express anti-oxidant activity capable of reducing reactive oxygen species in cells. These compounds may be used to inhibit oxidative stress-induced cell injury or death both in vivo and ex vivo. In addition, methods for the synthesis of these compounds are disclosed.
专利号:US-10030002-B2 优先权日:2015-04-16 标 题 :Coumarin derivative for detection of cysteine and process for the synthesis thereof 发明人:DAS AMITAVA; HOSKERE ANILA ASHOKA; GANDRA UPENDAR REDDY; ALI FIROJ 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a coumarin derivative of Formula (L) for detection of cysteine and process for preparation thereof. The present invention further relates to a process of detection of cysteine residues present in protein as well as the cysteine released by the enzymatic action of aminoacylase 1 by using coumarin derivative of Formula (L).
专利号:US-6809202-B2 优先权日:1996-11-07 标 题 :Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof 发明人:NEFZI ADEL; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.