专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-6198000-B1 优先权日:1997-07-07 标 题:Intermediates useful in the synthesis of quinoline antibiotics 发明人:HAWKINS JOEL M 权利人:PFIZER 摘要:A process for preparing a compound of the formula n wherein R 1 , m, o and p are described below, which comprises adding a base of the formula n wherein R 2 , R 3 and R 4 are as described below, to a solution comprising a compound of the formula n wherein R 1 , m, o and p are as described below, and a halonitromethane of the formula O 2 NCH 2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R 2 is butyl, R 3 is hydrogen and each R 4 is t-butyl.
专利号:US-5510516-A 优先权日:1990-07-06 标 题 :Process for selective epoxidation of unsaturated (meth)acrylates, new functional (meth)acrylates obtained and their application to the synthesis of new polymers 发明人:CAUBERE PAUL; FORT YVES; ORTAR AGNES 权利人:ATOCHEM 摘要:An unsaturated (meth) acrylic compound of formula: (I) (X=O, S, NH, NR3 (R3=C1-12-alkyl) or O-(CH2)n (where n=1-16 approximately); R2=C2-20 straight-chain or branched alkyl, monocyclic or polycyclic cycloalkyl or heterocycloalkyl, or alkylaryl hydrocarbon chain, comprising an olefinic double bond in the chain, or at the end of the chain in the case of alkyl or alkylaryl, or an exocyclic or endocyclic olefinic double bond in the case of monocyclic or polycyclic cycloalkyl or heterocycloalkyl; and R1=H or C1-5-alkyl), is reacted at 10 DEG -60 DEG C. with at least one oxidising compound (hydrogen peroxide) in the presence of at least one catalyst (alkali metal molybdates and tungstates) and in the presence of at least one phase transfer agent and when R2=polycyclic cycloalkyl or hetercycloalkyl, an organic peracid or hydrogen peroxide in the presence of at least one heteropolyacid. To open the epoxide function, the epoxide obtained is reacted with a compound chosen from strong inorganic acids, boron trifluoride etherate complexes, acid salts in the presence of the corresponding acid, halides of trialkylsilanes or trialkoxysilanes, and ketones in the presence of cationic resins.
专利号:US-7351781-B2 优先权日:2001-04-24 标题 :Synthesis of vinyl polymers by controlled radical polymerization 发明人:WHITE DANIELA; O'DWYER JAMES B 权利人:PPG IND OHIO INC 摘要:A controlled free radical polymerization process, which includes the steps of: adding a monofunctional iniferter compound to an oxygen-free solvent; heating the solution to a temperature sufficient to allow the iniferter compound to form two carbon centered radical residues; adding a first monomer composition comprising one or more monomers to the solution containing the radical containing residues; polymerizing the first monomer composition to form a quasi-living polymer; and optionally polymerizing a second monomer composition comprising one or more monomers, which are different than the first monomer composition. The resulting non-random copolymer having the general formula:n nφ-[-A p -B s -] t -φn nwhere A and B are different compositions of ethylenically unsaturated monomers; p is an integer from 1 to 1,000; s is an integer from 0 to 1,000; t is an integer from 1 to 100; and φ is a residue from the iniferter.
专利号:EP-0627420-B1 优先权日:1992-01-30 标 题 :Process for the synthesis of maleimide compound improved in storage stability 发明人:KITA YUICHI; NAKAGAWA KOICHI; KISHINO KAZUO 权利人:NIPPON CATALYTIC CHEM IND 摘要:A stabilized maleimide compound which is hardly discolored during storage, wherein the content of primary amines is 500 ppm or less, that of maleic anhydride is 5-2,000 ppm, and that of 2-amino-N-substituted succinimide is 300 ppm or less. It is preferable that the content of chlorine compounds be 10 ppm or less in terms of chlorine and that of volatile components having each a boiling point of 200 °C or below under an ordinary pressure be 2,000 ppm or less.
参考标题:Synthesis Of Azabicyclo[3.1.0]Amine Analogues Of Anacardic Acid As Potent Antibacterial Agents 作者:Ravi Kumar Vempati,N.S. Reddy,Srinivasa Rao Alapati,P.K. Dubey 摘要:Azabicyclo[3.1.0]Amine Analogues Of Anacardic Acid (16A, 16B, 18A, 18B, 19 And 19B) Were Synthesized From Anacardic Acid And Tested For Their Antibacterial Activity Against Gram Positive And Gram Negative Bacteria. Most Of The Compounds Are Having Potency At Par With Ampicillin And Inferior With Other Standard Drugs.