专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-9085550-B2 优先权日:2005-01-21 标题 :Ligands for estrogen related receptors and methods for synthesis of said ligands 发明人:FORMAN BARRY; YU DONNA 权利人:FORMAN BARRY; YU DONNA; HOPE CITY 摘要:Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.
专利号:US-9949970-B2 优先权日:2010-09-14 标题 :Synthesis of new benzothiazole derivatives as potential anti-tubercular agents 发明人:KAMAL AHMED; SHETTI RAJESH VCRNC; SWAPNA PONNAMPALLI; AZEEZA SHAIK; REDDY A MALLA; KHAN INSHAD ALI; ABDULLAH SHEIKH TASDUQ; SHARMA SANDEEP; KALIA NITIN PAL 权利人:COUNCIL SCIENT IND RES 摘要:Disclosed are compounds of general formula A useful as potential anti-tubercular agents. The general formula A is
专利号:US-8034895-B2 优先权日:2004-02-04 标题 :Conjugated thiophenes having conducting properties and synthesis of same 发明人:SKENE WILLIAM G 权利人:UNIV MONTREAL 摘要:The present invention relates to conjugated oligomers and polymers comprising aromatic thiophene cores. The conjugated materials are obtained by simple and efficient condensation of an aryl diamine and an aryl dialdehyde or a bifunctional aryl moiety comprising both an aldehyde and an amine. Condensation of the complementary moieties at temperatures ranging from ambient to refluxing temperatures in various solvents resulted in conjugated oligomers and polymers that can subsequently be cast into thin films. Oligomerization and polymerization can be done under mild conditions with removal of the resulting water bi-product responsible for shifting the equilibrium in favor of the conjugated products. The resulting conjugated compounds can be made conducting with dopants affording electrically conducting materials of either p-type or n-type conductors depending on the dopant selected.
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:WO-2004099199-A1 优先权日:2003-05-06 标 题:Oxazolidinone derivatives as antimicrobials 发明人:MEHTA ANITA; RAO AJJARAPU VENKATA SUBRAHMAN; RATTAN ASHOK 权利人:RANBAXY LAB LTD; MEHTA ANITA; RAO AJJARAPU VENKATA SUBRAHMAN; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula (I) or (II) and to the 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 such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
[参考文献]: Michael P Doyle, Et Al. Asymmetric Hetero-Diels-Alder Reaction Catalyzed By Dirhodium(Ii) Carboxamidates. Proc Natl Acad Sci U S A. 2004 Apr 13;101(15):5391-5. [参考文献]: R J Alaimo, Et Al. Antibacterial 2,3-Dihydro-2-(5-Nitro-2-Thienyl)-Quinazolin-4(1H)-Ones. J Med Chem. 1972 Mar;15(3):335-6.
合成参考文献
摘要:Williams, A. C.; Camp, N., Science of Synthesis, (2003) 14, 426.