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-2024174698-A1 优先权日:2022-09-23 标题 :Modular synthesis of 1,2-azaborines via ring-opening bn-isostere benzannulation 发明人:DONG GUANGBIN; LYU HAIRONG; CHEN ZHIJIE; WU YIFEI; CHOI SHINYOUNG 权利人:UNIV CHICAGO 摘要:The present disclosure relates generally to 1,2-azaborines and methods of making the same.
专利号:US-7365197-B2 优先权日:2000-12-29 标题 :Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines 发明人:BERGER DAN MAARTEN; BIRNBERG GARY HAROLD; WANG YANONG 权利人:WYETH CORP 摘要:This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.
专利号:US-2005124683-A1 优先权日:2003-09-17 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:ALEGRIA LARRY A; CANAN-KOCH STACIE S; DRESS KLAUS R; HUANG BUWEN; KUMPF ROBERT A; LEWIS KATHLEEN K; MATTHEWS JEAN J; SAKATA SYLVIE K; VIRGIL SCOTT C 权利人:AGOURON PHARMA 摘要:The present invention relates to a series of chemical compounds useful as Human Immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing such antiviral agents, and their uses and materials for their synthesis
专利号:US-7179918-B2 优先权日:2001-06-11 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-2009215080-A1 优先权日:2005-10-13 标题:Methods for identification of inhibitors of enzyme activity 发明人:SINHA SUKANTO; CHILCOTE TAMIE JO 权利人:ACTIVESITE PHARMACEUTICALS 摘要:The invention discloses compositions and methods of synthesis to create novel ligands and drugs and identifying such compounds as inhibitors of enzyme targets for use in the treatment of clinical disorders, including cancer, infectious diseases, parasitic infestations, neurological disorders, reproductive disorders, inflammatory disorders, circulatory disorders, and metabolic disorders.
摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 295. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 320. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 321. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 294. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 294.