专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-2004028702-A1 优先权日:2002-07-26 标 题:Muramic acid derivative compounds 发明人:MALETIC MILANA M; LEEMAN AARON H; SANTORELLI GINA M; WADDELL SHERMAN T 摘要:The present invention pertains to the combinatorial synthesis of antibacterial agents that inhibit the Mur-pathway enzymes involved in bacterial cell wall assembly. The method uses p-alkoxybenzylidene as the linker for the attachment of a derivatized muramic acid to the polymeric resin support. This intermediate becomes the starting point for the combinatorial synthesis, which in conjunction with split-pooling techniques allows rapid synthesis of diverse analogues for high-throughput screening (HTS). The invention is further directed to the libraries of these finished compounds that vary at the peptide, N-acyl and anomeric UDP positions.
专利号:US-2008214565-A1 优先权日:2003-04-07 标 题:Oxazolidinone Derivatives as Antimicrobials 发明人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK 权利人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula I and H and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:JP-2001112495-A 优先权日:1997-09-24 标 题 :Synthesis of optically active phenylalanine analogs by microbial conversion
摘要:U.S. Department of Health, Education & Welfare, Public Health Service. Center for Disease Control, National Institute for Occupational Safety & Health. Registry of Toxic Effects of Chemical Substances. 1977 edition. Washington, D. C.: U.S. Government Printing Office, 1977., p. 301 摘要:Weast, R.C. and M.J. Astle. CRC Handbook of Data on Organic Compounds. Volumes I and II. Boca Raton, FL: CRC Press Inc. 1985., p. V1 437