专利号:WO-0100609-A1 优先权日:1999-06-29 标题:Method for synthesis of n-homocysteine thiolactonyl retinamide 发明人:KAZIMIR MICHAEL; WILSON RAY E II 权利人:UNIV BAYLOR; KAZIMIR MICHAEL; WILSON RAY E II 摘要:The present invention describes methods of synthesis for N-homocysteine thiolactonyl retinamide (thioretinamide), a compound that has anticancer and antiatherogenic properties. The present invention further describes methods for the synthesis of N-homocysteine thiolactonyl retinamido cobalamin (thioretinaco), a compound that has potential anticancer, antineoplastic, antiviral, and antiatherogenic properties.
专利号:US-5124478-A 优先权日:1987-12-22 标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
专利号:US-4922015-A 优先权日:1987-04-08 标 题:Synthesis of peptide amides by means of a solid phase method using acid-labile anchoring groups 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl or optionally substituted (C 6 -C 14 )-aryl, R 2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or -O-(CH 2 ) n -COOH (with n=1 to 6), one of these radicals being -O-(CH 2 ) n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.
专利号:US-5565606-A 优先权日:1986-10-21 标 题:Synthesis of peptide aminoalkylamides and peptide hydrazides by the solid-phase method 发明人:BREIPHOL GERHARD; KNOLLE JOCHEN 权利人:HOECHST AG 摘要:The invention relates to compounds of the formula I in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y1, Y2, Y3 and Y4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes -[CH2]n- or -O-[CH2]n-, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.
专利号:US-6217857-B1 优先权日:1989-06-28 标题 :Cytokine synthesis inhibitory factor (IL-10) and pharmaceutical compositions thereof 发明人:MOSMANN TIMOTHY R; MOORE KEVIN W; BOND MARTHA W; VIEIRA PAULO J M 权利人:SCHERING CORP 摘要:Mammalian genes and proteins, designated cytokine synthesis inhibitory factors (CSIF's, now known as Interleukin-10 (IL-10)), are provided which are capable of inhibiting the synthesis of cytokines associated with delayed type hypersensitivity responses, and which, together with antagonists, are useful in treating diseases associated with cytokine imbalances, such as leishmaniasis and other parasitic infections, and certain immune disorders including MHC associated autoimmune diseases caused by excessive production of interferon-gamma.
专利号:US-5948693-A 优先权日:1994-09-01 标题:Solid phase synthesis of immunosuppressive agents 发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
参考标题:Benzotriazole-Mediated Synthesis Of Aza-Peptides: En Route To An Aza-Leuenkephalin Analogue 作者:Nader E. Abo-Dya,Suvendu Biswas,Akash Basak,Ilker Avan,Khalid A. Alamry,Alan R. Katritzky |发布日期:2013.4.19 摘要:With An Ester Bond 26B, And A Hybrid Azatripeptide With An Ester Bond 28. A New Protocol For The Synthesis Of N-Pg-Azatripeptides 33A,B And 35A,B, Each Containing A Natural Amino Acid At The N-Terminus, Avoids The Low Coupling Rates Of The Aza-Amino Acid Residue And Enables The Solution-Phase Synthesis Of An Azaphenylalanine Analogue Of Leu-Enkephalin 40.